alleen voor onderzoeksdoeleinden
Romidepsin (FK228) HDAC Remmer
Cat.nr.S3020
Chemische structuur
Molecuulgewicht: 540.7
Spring naar
Kwaliteitscontrole (Quality Control)
Batch:
Zuiverheid:
99.95%
99.95
Celkweek, behandeling & werkzame concentratie
(Cell Culture, Treatment & Working Concentration)
| Cellijnen | Assaytype | Concentratie | Incubatietijd | Formulering | Activiteitsbeschrijving | PMID |
|---|---|---|---|---|---|---|
| SU-DHL4 | Cell Viability Assay | 2.5-15 nM | 72 h | induces cytotoxicity in a concentration-dependent manner | 25790907 | |
| U2932 | Cell Viability Assay | 2.5-15 nM | 72 h | induces cytotoxicity in a concentration-dependent manner | 25790907 | |
| OCI-LY7 | Cell Viability Assay | 2.5-15 nM | 72 h | induces cytotoxicity in a concentration-dependent manner | 25790907 | |
| Farage | Cell Viability Assay | 2.5-15 nM | 72 h | induces cytotoxicity in a concentration-dependent manner | 25790907 | |
| LY7/EBV | Cell Viability Assay | 2.5-15 nM | 72 h | induces cytotoxicity in a concentration-dependent manner | 25790907 | |
| U2932/EBV | Cell Viability Assay | 2.5-15 nM | 72 h | induces cytotoxicity in a concentration-dependent manner | 25790907 | |
| HCT116 | Growth Inhibition Assay | 5-5000 nM | 24 h | DMSO | induces cell death in a concentration-dependent manner | 25492515 |
| ACH-2 | Function Assay | 1-9 nM | 24 h | induces HIV-1 Env expression | 25149467 | |
| MCF-10A | Growth Inhibition Assay | IC50=0.17±0.01 nM | 24954856 | |||
| MCF-7 | Growth Inhibition Assay | IC50=1.10±0.20 nM | 24954856 | |||
| SK-BR-3 | Growth Inhibition Assay | IC50=1.00±0.35 nM | 24954856 | |||
| MDA-MB-231 | Growth Inhibition Assay | IC50=0.68±0.14 nM | 24954856 | |||
| PC3 | Growth Inhibition Assay | IC50=1.65±0.35 nM | 24954856 | |||
| HCT116 | Growth Inhibition Assay | IC50=1.00±0.00 nM | 24954856 | |||
| HCT116-p21-/- | Growth Inhibition Assay | IC50=1.26±0.37 nM | 24954856 | |||
| S1 | Growth Inhibition Assay | IC50=7.67±0.29 nM | 24954856 | |||
| SW620 | Growth Inhibition Assay | IC50=0.93±0.29 nM | 24954856 | |||
| LOX-IMVI | Growth Inhibition Assay | IC50=0.87±0.03 nM | 24954856 | |||
| UACC-62 | Growth Inhibition Assay | IC50=0.56±0.16 nM | 24954856 | |||
| MDA-MB-435 | Growth Inhibition Assay | IC50=0.90±0.06 nM | 24954856 | |||
| SF-295 | Growth Inhibition Assay | IC50=0.88±0.15 nM | 24954856 | |||
| A549 | Growth Inhibition Assay | IC50=1.26±0.24 nM | 24954856 | |||
| H460 | Growth Inhibition Assay | IC50=2.58±0.80 nM | 24954856 | |||
| EKVX | Growth Inhibition Assay | IC50=1.33±0.34 nM | 24954856 | |||
| H146 | Growth Inhibition Assay | IC50=0.22±0.07 nM | 24954856 | |||
| H526 | Growth Inhibition Assay | IC50=0.15±0.03 nM | 24954856 | |||
| HuT-78 | Growth Inhibition Assay | IC50=1.73±0.44 nM | 24954856 | |||
| HA | Growth Inhibition Assay | 0.625-10nM | 48 h | induces a significantly stronger inhibition of cell proliferation co-treated with bortezomib | 24771510 | |
| MS-275 | Growth Inhibition Assay | 0.625-10nM | 48 h | induces a significantly stronger inhibition of cell proliferation co-treated with bortezomib | 24771510 | |
| CD4 T | Growth Inhibition Assay | 48 h | EC50=4.5±1.0 nM | 24722454 | ||
| CD4 T | Growth Inhibition Assay | 48 h | CC50=107±126 nM | 24722454 | ||
| CD4+ T | Growth Inhibition Assay | EC50=3 nM | 24495105 | |||
| A549 | Growth Inhibition Assay | 10–100 nM | 24/36/48 h | inhibits cell growth in both concentration- and time-dependent manner | 24485799 | |
| JJN3 | Growth Inhibition Assay | 24/48 h | EC50<1 nM; 48 h | 24030150 | ||
| OPM-2 | Growth Inhibition Assay | 24/48 h | EC50s=1 nM; 48 h | 24030150 | ||
| RPMI-8226 | Growth Inhibition Assay | 24/48 h | EC50s=1.8 nM; 48 h | 24030150 | ||
| U266 | Growth Inhibition Assay | 24/48 h | EC50s=10 nM; 48 h | 24030150 | ||
| CA46 | Apoptosis Assay | 6 h | induces blunt apoptosis | 23966164 | ||
| DG75 | Apoptosis Assay | 6 h | induces no apoptosis | 23966164 | ||
| Ramos | Apoptosis Assay | 6 h | induces extensive apoptosis | 23966164 | ||
| ST486 | Apoptosis Assay | 6 h | induces extensive apoptosis | 23966164 | ||
| HuT78 | Apoptosis Assay | 1/10/100 nM | 48 h | induces apoptosis at 1 nM | 23532732 | |
| DpVp35 | Apoptosis Assay | 1/10/100 nM | 48 h | induces blunt apoptosis | 23532732 | |
| DpVp50 | Apoptosis Assay | 1/10/100 nM | 48 h | induces blunt apoptosis | 23532732 | |
| DpP75 | Apoptosis Assay | 1/10/100 nM | 48 h | induces blunt apoptosis | 23532732 | |
| SKOV-3 | Growth Inhibition Assay | 1–20nM | 72 h | DMSO | reduces cell viability alone and combined with cisplatin | 23010348 |
| Brca1 WT | Growth Inhibition Assay | 1–20nM | 72 h | DMSO | reduces cell viability alone and combined with cisplatin | 23010348 |
| Brca1 Null | Growth Inhibition Assay | 1–20nM | 72 h | DMSO | reduces cell viability alone and combined with cisplatin | 23010348 |
| OVCAR-8 | Growth Inhibition Assay | 1–20nM | 72 h | DMSO | reduces cell viability alone and combined with cisplatin | 23010348 |
| NCI/ADR-RES | Growth Inhibition Assay | 1–20nM | 72 h | DMSO | reduces cell viability alone and combined with cisplatin | 23010348 |
| HCT116 | Growth Inhibition Assay | 5 nM-50 μM | 24 h | DMSO | inhibits cell growth in a concentration-dependent manner | 22924958 |
| RKO | Growth Inhibition Assay | 5 nM-50 μM | 24 h | DMSO | inhibits cell growth in a concentration-dependent manner | 22924958 |
| CO115 | Growth Inhibition Assay | 5 nM-50 μM | 24 h | DMSO | inhibits cell growth in a concentration-dependent manner | 22924958 |
| HFS | Growth Inhibition Assay | 5 nM | 24/48/72 h | inhibits cell growth time-dependently | 22106282 | |
| LNCaP | Growth Inhibition Assay | 5 nM | 24/48/72 h | inhibits cell growth time-dependently | 22106282 | |
| A549 | Growth Inhibition Assay | 5 nM | 24/48/72 h | inhibits cell growth time-dependently | 22106282 | |
| 697 | Growth Inhibition Assay | IC50 = 2.5 nM | 21538216 | |||
| 697-R | Growth Inhibition Assay | IC50 = 8.6 nM | 21538216 | |||
| HUT78 | Growth Inhibition Assay | IC50=1 nM | 21198545 | |||
| THJ-16T | Growth Inhibition Assay | 1 nM | 24 h | inhibits cell growth | 20810568 | |
| HCT116 | Function Assay | 20 nM | 8 h | modulates transcript levels for hundreds of genes in either direction | 20739454 | |
| B104 | Function Assay | 2 nM | 24/48/72 h | increases the surface expression of CD20 | 20686505 | |
| HL-60 | Cytotoxicity Assay | 1-500 nM | 24 h | induces cytotoxicity in a concentration-dependent manner | 20624163 | |
| HP100 | Cytotoxicity Assay | 1-500 nM | 24 h | induces cytotoxicity in a concentration-dependent manner | 20624163 | |
| HL-60 | Function Assay | 10 nM | 4/6/16 h | induces the generation of hydrogen peroxide from 4h | 20624163 | |
| HP100 | Function Assay | 10 nM | 4/6/16 h | induces the generation of hydrogen peroxide from 4h | 20624163 | |
| HL-60 | Function Assay | 10-500 nM | 4 h | decreases the histone deacetylase (HDAC) activity | 20624163 | |
| HP100 | Function Assay | 10-500 nM | 4 h | decreases the histone deacetylase (HDAC) activity | 20624163 | |
| 11z | Kinase Assay | 3-100 nM | reduces HDAC enzymatic activity (IC50 = 6.5 ± 0.6 nmol/L) | 20605144 | ||
| SKOV-3 | Growth Inhibition Assay | 4/8/16 nM | 48 h | inhibits cell growth in a concentration-dependent manner | 20404564 | |
| OVCAR-3 | Growth Inhibition Assay | 4/8/16 nM | 48 h | inhibits cell growth in a concentration-dependent manner | 20404564 | |
| HBL-2 | Growth Inhibition Assay | 2-10 nM | 24 h | IC50=4.3 nM | 20068080 | |
| Jeko-1 | Growth Inhibition Assay | 2-50 nM | 24 h | IC50=11 nM | 20068080 | |
| Granta-519 | Growth Inhibition Assay | 5-40 nM | 24 h | IC50=58.5 nM | 20068080 | |
| L1236 | Cytotoxicity Assay | 1 nM-100 μM | 48 h | EC50=0.07 μM | 19233470 | |
| L428 | Cytotoxicity Assay | 1 nM-100 μM | 48 h | EC50=0.43 μM | 19233470 | |
| KM-H2 | Cytotoxicity Assay | 1 nM-100 μM | 48 h | EC50=0.58 μM | 19233470 | |
| L540Cy | Cytotoxicity Assay | 1 nM-100 μM | 48 h | EC50=0.16 μM | 19233470 | |
| G401 | Function Assay | 10 nM | 24/48/72 h | DMSO | increases CDKN1C expression | 19221586 |
| STM91-01 | Function Assay | 10 nM | 24/48/72 h | DMSO | increases CDKN1C expression | 19221586 |
| SJSC | Function Assay | 10 nM | 24/48/72 h | DMSO | increases CDKN1C expression | 19221586 |
| BT16 | Function Assay | 10 nM | 24/48/72 h | DMSO | increases CDKN1C expression | 19221586 |
| NCI-H1299 | Growth Inhibition Assay | IC50=4.6±0.2 ng/ml | 19179890 | |||
| NCI-2882 | Growth Inhibition Assay | IC50=1.6±0.04 ng/ml | 19179890 | |||
| HCC95 | Growth Inhibition Assay | IC50=2.5±0.05 ng/ml | 19179890 | |||
| NCI-H23 | Growth Inhibition Assay | IC50=2.9±0.2 ng/ml | 19179890 | |||
| NCI-H157 | Growth Inhibition Assay | IC50=1.6±0.02 ng/ml | 19179890 | |||
| NCI-H460 | Growth Inhibition Assay | IC50=2.1±0.07 ng/ml | 19179890 | |||
| NCI-H1975 | Growth Inhibition Assay | IC50=1.3±0.04 ng/ml | 19179890 | |||
| NCI-H820 | Growth Inhibition Assay | IC50=2.4±0.1 ng/ml | 19179890 | |||
| NCI-H1650 | Growth Inhibition Assay | IC50=4.9±0.3 ng/ml | 19179890 | |||
| DTC1 | Growth Inhibition Assay | IC50=0.51 nM | 18566246 | |||
| KAO | Growth Inhibition Assay | IC50=0.91 nM | 18566246 | |||
| SU-CCS-1 | Growth Inhibition Assay | IC50=0.89 nM | 18566246 | |||
| SYO-1 | Growth Inhibition Assay | IC50=0.67 nM | 18566246 | |||
| FUJI | Growth Inhibition Assay | IC50=1.31 nM | 18566246 | |||
| SKNMC | Growth Inhibition Assay | IC50=1.17 nM | 18566246 | |||
| 402-91 | Growth Inhibition Assay | IC50=1.26 nM | 18566246 | |||
| 1765-92 | Growth Inhibition Assay | IC50=1.77 nM | 18566246 | |||
| JN-DSRCT-1 | Growth Inhibition Assay | IC50=1.25 nM | 18566246 | |||
| NMS-2PC | Growth Inhibition Assay | IC50=0.81 nM | 18566246 | |||
| HL60 | Growth Inhibition Assay | IC50=1.86 nM | 18566246 | |||
| A549 | Growth Inhibition Assay | IC50=3.24 nM | 18566246 | |||
| SW480 | Growth Inhibition Assay | IC50=2.69 nM | 18566246 | |||
| MCF7 | Growth Inhibition Assay | IC50=3.55 nM | 18566246 | |||
| PC-3 | Growth Inhibition Assay | IC50=2.51 nM | 18566246 | |||
| MMRU | Growth Inhibition Assay | IC50=2.57 nM | 18566246 | |||
| Hs68 | Growth Inhibition Assay | IC50=>10 nM | 18566246 | |||
| hMSC-001F | Growth Inhibition Assay | IC50=>10 nM | 18566246 | |||
| mammalian cells | Function assay | Inhibition of Histone deacetylase 4 in mammalian cells, IC50 = 0.51 μM. | 14584932 | |||
| mammalian cells | Function assay | Inhibition of Histone deacetylase 1 induced acetylated histone in mammalian cells., EC50 = 36 μM. | 14584932 | |||
| MCF7 | Growth inhibition assay | Growth inhibition of MCF7 cells, IC50 = 0.00075 μM. | 17958342 | |||
| A498 | Cytotoxicity assay | 6 days | Cytotoxicity against human A498 cells after 6 days by MTT assay, TGI = 0.028 μM. | 21967146 | ||
| COLO205 | Cytotoxicity assay | 6 days | Cytotoxicity against human COLO205 cells after 6 days by MTT assay, TGI = 0.031 μM. | 21967146 | ||
| U251 | Cytotoxicity assay | 6 days | Cytotoxicity against human U251 cells after 6 days by MTT assay, TGI = 0.031 μM. | 21967146 | ||
| RXF393 | Cytotoxicity assay | 6 days | Cytotoxicity against human RXF393 cells after 6 days by MTT assay, TGI = 0.062 μM. | 21967146 | ||
| MDA-MB-468 | Cytotoxicity assay | 6 days | Cytotoxicity against human MDA-MB-468 cells after 6 days by MTT assay, TGI = 0.09 μM. | 21967146 | ||
| COLO205 | Cytotoxicity assay | 6 days | Cytotoxicity against human COLO205 cells after 6 days by MTT assay, LC50 = 0.092 μM. | 21967146 | ||
| UACC257 | Cytotoxicity assay | 6 days | Cytotoxicity against human UACC257 cells after 6 days by MTT assay, TGI = 0.095 μM. | 21967146 | ||
| U251 | Cytotoxicity assay | 6 days | Cytotoxicity against human U251 cells after 6 days by MTT assay, LC50 = 0.13 μM. | 21967146 | ||
| A498 | Cytotoxicity assay | 6 days | Cytotoxicity against human A498 cells after 6 days by MTT assay, LC50 = 0.2 μM. | 21967146 | ||
| NCI-H322M | Cytotoxicity assay | 6 days | Cytotoxicity against human NCI-H322M cells after 6 days by MTT assay, TGI = 0.23 μM. | 21967146 | ||
| SF295 | Cytotoxicity assay | 6 days | Cytotoxicity against human SF295 cells after 6 days by MTT assay, TGI = 0.25 μM. | 21967146 | ||
| RXF393 | Cytotoxicity assay | 6 days | Cytotoxicity against human RXF393 cells after 6 days by MTT assay, LC50 = 0.3 μM. | 21967146 | ||
| NCI60 | Cytotoxicity assay | 6 days | Cytotoxicity against human NCI60 cells after 6 days by MTT assay, TGI = 0.33 μM. | 21967146 | ||
| SN12C | Cytotoxicity assay | 6 days | Cytotoxicity against human SN12C cells after 6 days by MTT assay, TGI = 0.34 μM. | 21967146 | ||
| MDA-MB-231 | Cytotoxicity assay | 6 days | Cytotoxicity against human MDA-MB-231 cells after 6 days by MTT assay, TGI = 0.35 μM. | 21967146 | ||
| ACHN | Cytotoxicity assay | 6 days | Cytotoxicity against human ACHN cells after 6 days by MTT assay, TGI = 0.73 μM. | 21967146 | ||
| SN12C | Cytotoxicity assay | 6 days | Cytotoxicity against human SN12C cells after 6 days by MTT assay, LC50 = 1.5 μM. | 21967146 | ||
| UO31 | Cytotoxicity assay | 6 days | Cytotoxicity against human UO31 cells after 6 days by MTT assay, TGI = 1.55 μM. | 21967146 | ||
| Caki1 | Cytotoxicity assay | 6 days | Cytotoxicity against human Caki1 cells after 6 days by MTT assay, TGI = 1.89 μM. | 21967146 | ||
| NCI60 | Cytotoxicity assay | 6 days | Cytotoxicity against human NCI60 cells after 6 days by MTT assay, LC50 = 3.5 μM. | 21967146 | ||
| MDA-MB-231 | Cytotoxicity assay | 6 days | Cytotoxicity against human MDA-MB-231 cells after 6 days by MTT assay, LC50 = 4.08 μM. | 21967146 | ||
| MDA-MB-468 | Cytotoxicity assay | 6 days | Cytotoxicity against human MDA-MB-468 cells after 6 days by MTT assay, LC50 = 4.14 μM. | 21967146 | ||
| ACHN | Cytotoxicity assay | 6 days | Cytotoxicity against human ACHN cells after 6 days by MTT assay, LC50 = 5.37 μM. | 21967146 | ||
| UACC257 | Cytotoxicity assay | 6 days | Cytotoxicity against human UACC257 cells after 6 days by MTT assay, LC50 = 5.46 μM. | 21967146 | ||
| NCI-H322M | Cytotoxicity assay | 6 days | Cytotoxicity against human NCI-H322M cells after 6 days by MTT assay, LC50 = 9.02 μM. | 21967146 | ||
| SF295 | Cytotoxicity assay | 6 days | Cytotoxicity against human SF295 cells after 6 days by MTT assay, LC50 = 10.2 μM. | 21967146 | ||
| Caki1 | Cytotoxicity assay | 6 days | Cytotoxicity against human Caki1 cells after 6 days by MTT assay, LC50 = 20.9 μM. | 21967146 | ||
| NCI-H23 | Antitumor assay | 1.6 to 2.4 mg/kg | up to 5 days | Antitumor activity against human NCI-H23 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay | 21967146 | |
| NCI-H522 | Antitumor assay | 1.6 to 2.4 mg/kg | up to 5 days | Antitumor activity against human NCI-H522 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay | 21967146 | |
| OVCAR5 | Antitumor assay | 1.6 to 2.4 mg/kg | up to 5 days | Antitumor activity against human OVCAR5 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay | 21967146 | |
| SW620 | Antitumor assay | 1.6 to 2.4 mg/kg | up to 5 days | Antitumor activity against human SW620 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay | 21967146 | |
| MDA-MB-435 | Antitumor assay | 1.6 to 2.4 mg/kg | up to 5 days | Antitumor activity against human MDA-MB-435 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay | 21967146 | |
| COLO205 | Antitumor assay | 1.6 to 2.4 mg/kg | up to 5 days | Antitumor activity against human COLO205 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay | 21967146 | |
| LOXIMVI | Antitumor assay | 1.6 to 2.4 mg/kg | up to 5 days | Antitumor activity against human LOXIMVI cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay | 21967146 | |
| UACC62 | Antitumor assay | 1.6 to 2.4 mg/kg | up to 5 days | Antitumor activity against human UACC62 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay | 21967146 | |
| MDA-MB-231 | Antitumor assay | 1.6 to 2.4 mg/kg | up to 5 days | Antitumor activity against human MDA-MB-231 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay | 21967146 | |
| SF295 | Antitumor assay | 1.6 to 2.4 mg/kg | up to 5 days | Antitumor activity against human SF295 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay | 21967146 | |
| U251 | Antitumor assay | 1.6 to 2.4 mg/kg | up to 5 days | Antitumor activity against human U251 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay | 21967146 | |
| OVRAC3 | Antitumor assay | 1.6 to 2.4 mg/kg | up to 5 days | Antitumor activity against human OVRAC3 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay | 21967146 | |
| LLC | Function assay | Inhibition of HDAC-mediated HIF-1alpha activity in mouse LLC cells, IC50 = 2 μM. | 22305612 | |||
| NCI-H522 | Growth inhibition assay | Growth inhibition of human NCI-H522 cells by sulforhodamine B colorimetric method, GI50 = 0.0018 μM. | 23313638 | |||
| LOXIMVI | Growth inhibition assay | Growth inhibition of human LOXIMVI cells by sulforhodamine B colorimetric method, GI50 = 0.0025 μM. | 23313638 | |||
| A549 | Growth inhibition assay | Growth inhibition of human A549 cells by sulforhodamine B colorimetric method, GI50 = 0.0026 μM. | 23313638 | |||
| OVCAR5 | Growth inhibition assay | Growth inhibition of human OVCAR5 cells by sulforhodamine B colorimetric method, GI50 = 0.0028 μM. | 23313638 | |||
| MKN74 | Growth inhibition assay | Growth inhibition of human MKN74 cells by sulforhodamine B colorimetric method, GI50 = 0.003 μM. | 23313638 | |||
| NCI-H460 | Growth inhibition assay | Growth inhibition of human NCI-H460 cells by sulforhodamine B colorimetric method, GI50 = 0.003 μM. | 23313638 | |||
| HCT116 | Growth inhibition assay | Growth inhibition of human HCT116 cells by sulforhodamine B colorimetric method, GI50 = 0.0031 μM. | 23313638 | |||
| HCC2998 | Growth inhibition assay | Growth inhibition of human HCC2998 cells by sulforhodamine B colorimetric method, GI50 = 0.0031 μM. | 23313638 | |||
| MKN1 | Growth inhibition assay | Growth inhibition of human MKN1 cells by sulforhodamine B colorimetric method, GI50 = 0.0032 μM. | 23313638 | |||
| SKOV3 | Growth inhibition assay | Growth inhibition of human SKOV3 cells by sulforhodamine B colorimetric method, GI50 = 0.0033 μM. | 23313638 | |||
| HT-29 | Growth inhibition assay | Growth inhibition of human HT-29 cells by sulforhodamine B colorimetric method, GI50 = 0.0033 μM. | 23313638 | |||
| KM12 | Growth inhibition assay | Growth inhibition of human KM12 cells by sulforhodamine B colorimetric method, GI50 = 0.0034 μM. | 23313638 | |||
| DMS114 | Growth inhibition assay | Growth inhibition of human DMS114 cells by sulforhodamine B colorimetric method, GI50 = 0.0036 μM. | 23313638 | |||
| SF539 | Growth inhibition assay | Growth inhibition of human SF539 cells by sulforhodamine B colorimetric method, GI50 = 0.0036 μM. | 23313638 | |||
| U251 | Growth inhibition assay | Growth inhibition of human U251 cells by sulforhodamine B colorimetric method, GI50 = 0.0039 μM. | 23313638 | |||
| SF295 | Growth inhibition assay | Growth inhibition of human SF295 cells by sulforhodamine B colorimetric method, GI50 = 0.004 μM. | 23313638 | |||
| MCF7 | Growth inhibition assay | Growth inhibition of human MCF7 cells by sulforhodamine B colorimetric method, GI50 = 0.0042 μM. | 23313638 | |||
| NCI-H23 | Growth inhibition assay | Growth inhibition of human NCI-H23 cells by sulforhodamine B colorimetric method, GI50 = 0.0046 μM. | 23313638 | |||
| OVCAR3 | Growth inhibition assay | Growth inhibition of human OVCAR3 cells by sulforhodamine B colorimetric method, GI50 = 0.0046 μM. | 23313638 | |||
| MKN7 | Growth inhibition assay | Growth inhibition of human MKN7 cells by sulforhodamine B colorimetric method, GI50 = 0.0049 μM. | 23313638 | |||
| SF268 | Growth inhibition assay | Growth inhibition of human SF268 cells by sulforhodamine B colorimetric method, GI50 = 0.0049 μM. | 23313638 | |||
| MDA-MB-231 | Growth inhibition assay | Growth inhibition of human MDA-MB-231 cells by sulforhodamine B colorimetric method, GI50 = 0.0055 μM. | 23313638 | |||
| OVCAR8 | Growth inhibition assay | Growth inhibition of human OVCAR8 cells by sulforhodamine B colorimetric method, GI50 = 0.0055 μM. | 23313638 | |||
| DMS273 | Growth inhibition assay | Growth inhibition of human DMS273 cells by sulforhodamine B colorimetric method, GI50 = 0.0058 μM. | 23313638 | |||
| DU145 | Growth inhibition assay | Growth inhibition of human DU145 cells by sulforhodamine B colorimetric method, GI50 = 0.006 μM. | 23313638 | |||
| RXF631L | Growth inhibition assay | Growth inhibition of human RXF631L cells by sulforhodamine B colorimetric method, GI50 = 0.0066 μM. | 23313638 | |||
| HBC4 | Growth inhibition assay | Growth inhibition of human HBC4 cells by sulforhodamine B colorimetric method, GI50 = 0.0069 μM. | 23313638 | |||
| SNB75 | Growth inhibition assay | Growth inhibition of human SNB75 cells by sulforhodamine B colorimetric method, GI50 = 0.0072 μM. | 23313638 | |||
| BSY1 | Growth inhibition assay | Growth inhibition of human BSY1 cells by sulforhodamine B colorimetric method, GI50 = 0.0085 μM. | 23313638 | |||
| NCI-H226 | Growth inhibition assay | Growth inhibition of human NCI-H226 cells by sulforhodamine B colorimetric method, GI50 = 0.0089 μM. | 23313638 | |||
| SNB78 | Growth inhibition assay | Growth inhibition of human SNB78 cells by sulforhodamine B colorimetric method, GI50 = 0.0096 μM. | 23313638 | |||
| HBC5 | Growth inhibition assay | Growth inhibition of human HBC5 cells by sulforhodamine B colorimetric method, GI50 = 0.013 μM. | 23313638 | |||
| MKN45 | Growth inhibition assay | Growth inhibition of human MKN45 cells by sulforhodamine B colorimetric method, GI50 = 0.014 μM. | 23313638 | |||
| MKN28 | Growth inhibition assay | Growth inhibition of human MKN28 cells by sulforhodamine B colorimetric method, GI50 = 0.017 μM. | 23313638 | |||
| PC3 | Growth inhibition assay | Growth inhibition of human PC3 cells by sulforhodamine B colorimetric method, GI50 = 0.018 μM. | 23313638 | |||
| ACHN | Growth inhibition assay | Growth inhibition of human ACHN cells by sulforhodamine B colorimetric method, GI50 = 0.02 μM. | 23313638 | |||
| OVCAR4 | Growth inhibition assay | Growth inhibition of human OVCAR4 cells by sulforhodamine B colorimetric method, GI50 = 0.02 μM. | 23313638 | |||
| St-4 | Growth inhibition assay | Growth inhibition of human St-4 cells by sulforhodamine B colorimetric method, GI50 = 0.022 μM. | 23313638 | |||
| HCT15 | Growth inhibition assay | Growth inhibition of human HCT15 cells by sulforhodamine B colorimetric method, GI50 = 0.45 μM. | 23313638 | |||
| CD4+ T | Function assay | 7 days | Reactivation of latent HIV1 NL4-3-Luc expression in human naive CD4+ T cells treated 7 days post-infection measured after 48 hrs by luminescence plate reader analysis, EC50 = 0.003 μM. | 24495105 | ||
| NCI-H522 | Cytotoxicity assay | Cytotoxicity against human NCI-H522 cells by SRB assay, GI50 = 0.0018 μM. | 24589486 | |||
| LOXIMVI | Cytotoxicity assay | Cytotoxicity against human LOXIMVI cells by SRB assay, GI50 = 0.0025 μM. | 24589486 | |||
| A549 | Cytotoxicity assay | Cytotoxicity against human A549 cells by SRB assay, GI50 = 0.0026 μM. | 24589486 | |||
| OVCAR5 | Cytotoxicity assay | Cytotoxicity against human OVCAR5 cells by SRB assay, GI50 = 0.0028 μM. | 24589486 | |||
| NCI-H460 | Cytotoxicity assay | Cytotoxicity against human NCI-H460 cells by SRB assay, GI50 = 0.003 μM. | 24589486 | |||
| MKN74 | Cytotoxicity assay | Cytotoxicity against human MKN74 cells by SRB assay, GI50 = 0.003 μM. | 24589486 | |||
| HCC2998 | Cytotoxicity assay | Cytotoxicity against human HCC2998 cells by SRB assay, GI50 = 0.0031 μM. | 24589486 | |||
| HCT116 | Cytotoxicity assay | Cytotoxicity against human HCT116 cells by SRB assay, GI50 = 0.0031 μM. | 24589486 | |||
| MKN1 | Cytotoxicity assay | Cytotoxicity against human MKN1 cells by SRB assay, GI50 = 0.0032 μM. | 24589486 | |||
| HT-29 | Cytotoxicity assay | Cytotoxicity against human HT-29 cells by SRB assay, GI50 = 0.0033 μM. | 24589486 | |||
| SKOV3 | Cytotoxicity assay | Cytotoxicity against human SKOV3 cells by SRB assay, GI50 = 0.0033 μM. | 24589486 | |||
| KM12 | Cytotoxicity assay | Cytotoxicity against human KM12 cells by SRB assay, GI50 = 0.0034 μM. | 24589486 | |||
| SF539 | Cytotoxicity assay | Cytotoxicity against human SF539 cells by SRB assay, GI50 = 0.0036 μM. | 24589486 | |||
| 293T | Function assay | 30 mins | Inhibition of human HDAC1 expressed in human 293T cells using Ac-KGLGK(Ac)-MCA as substrate after 30 mins by fluorescence assay, IC50 = 0.0036 μM. | 24589486 | ||
| DMS114 | Cytotoxicity assay | Cytotoxicity against human DMS114 cells by SRB assay, GI50 = 0.0036 μM. | 24589486 | |||
| U251 | Cytotoxicity assay | Cytotoxicity against human U251 cells by SRB assay, GI50 = 0.0039 μM. | 24589486 | |||
| SF295 | Cytotoxicity assay | Cytotoxicity against human SF295 cells by SRB assay, GI50 = 0.004 μM. | 24589486 | |||
| MCF7 | Cytotoxicity assay | Cytotoxicity against human MCF7 cells by SRB assay, GI50 = 0.0042 μM. | 24589486 | |||
| OVCAR3 | Cytotoxicity assay | Cytotoxicity against human OVCAR3 cells by SRB assay, GI50 = 0.0046 μM. | 24589486 | |||
| NCI-H23 | Cytotoxicity assay | Cytotoxicity against human NCI-H23 cells by SRB assay, GI50 = 0.0046 μM. | 24589486 | |||
| SF268 | Cytotoxicity assay | Cytotoxicity against human SF268 cells by SRB assay, GI50 = 0.0049 μM. | 24589486 | |||
| MKN7 | Cytotoxicity assay | Cytotoxicity against human MKN7 cells by SRB assay, GI50 = 0.0049 μM. | 24589486 | |||
| OVCAR8 | Cytotoxicity assay | Cytotoxicity against human OVCAR8 cells by SRB assay, GI50 = 0.0055 μM. | 24589486 | |||
| MDA-MB-231 | Cytotoxicity assay | Cytotoxicity against human MDA-MB-231 cells by SRB assay, GI50 = 0.0055 μM. | 24589486 | |||
| DMS273 | Cytotoxicity assay | Cytotoxicity against human DMS273 cells by SRB assay, GI50 = 0.0058 μM. | 24589486 | |||
| DU145 | Cytotoxicity assay | Cytotoxicity against human DU145 cells by SRB assay, GI50 = 0.006 μM. | 24589486 | |||
| RXF631L | Cytotoxicity assay | Cytotoxicity against human RXF631L cells by SRB assay, GI50 = 0.0066 μM. | 24589486 | |||
| HBC4 | Cytotoxicity assay | Cytotoxicity against human HBC4 cells by SRB assay, GI50 = 0.0069 μM. | 24589486 | |||
| SNB75 | Cytotoxicity assay | Cytotoxicity against human SNB75 cells by SRB assay, GI50 = 0.0072 μM. | 24589486 | |||
| BSY1 | Cytotoxicity assay | Cytotoxicity against human BSY1 cells by SRB assay, GI50 = 0.0085 μM. | 24589486 | |||
| NCI-H226 | Cytotoxicity assay | Cytotoxicity against human NCI-H226 cells by SRB assay, GI50 = 0.0089 μM. | 24589486 | |||
| SNB78 | Cytotoxicity assay | Cytotoxicity against human SNB78 cells by SRB assay, GI50 = 0.0096 μM. | 24589486 | |||
| HBC5 | Cytotoxicity assay | Cytotoxicity against human HBC5 cells by SRB assay, GI50 = 0.013 μM. | 24589486 | |||
| MKN45 | Cytotoxicity assay | Cytotoxicity against human MKN45 cells by SRB assay, GI50 = 0.014 μM. | 24589486 | |||
| MKN28 | Cytotoxicity assay | Cytotoxicity against human MKN28 cells by SRB assay, GI50 = 0.017 μM. | 24589486 | |||
| PC3 | Cytotoxicity assay | Cytotoxicity against human PC3 cells by SRB assay, GI50 = 0.018 μM. | 24589486 | |||
| ACHN | Cytotoxicity assay | Cytotoxicity against human ACHN cells by SRB assay, GI50 = 0.02 μM. | 24589486 | |||
| OVCAR4 | Cytotoxicity assay | Cytotoxicity against human OVCAR4 cells by SRB assay, GI50 = 0.02 μM. | 24589486 | |||
| St-4 | Cytotoxicity assay | Cytotoxicity against human St-4 cells by SRB assay, GI50 = 0.022 μM. | 24589486 | |||
| 293T | Function assay | 30 mins | Inhibition of mouse HDAC6 expressed in human 293T cells using Ac-KGLGK(Ac)-MCA as substrate after 30 mins by fluorescence assay, IC50 = 0.39 μM. | 24589486 | ||
| HCT15 | Cytotoxicity assay | Cytotoxicity against human HCT15 cells by SRB assay, GI50 = 0.45 μM. | 24589486 | |||
| mink Mv1Lu | Function assay | 24 hrs | Increase in human wild type p21 protein expression in mink Mv1Lu cells after 24 hrs by p21 promoter assay in presence of 0.1 mM dithiothreitol, EC1000 = 0.0157 μM. | 24997578 | ||
| HCT116 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HCT116 cells after 48 hrs in presence of DTT by MTT assay, IC50 = 0.003 μM. | 25147612 | ||
| MOLT4 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MOLT4 cells after 72 hrs by CCK8 assay, GI50 = 0.00206 μM. | 26331334 | ||
| DU145 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human DU145 cells after 72 hrs by CCK8 assay, GI50 = 0.00255 μM. | 26331334 | ||
| U937 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human U937 cells after 72 hrs by CCK8 assay, GI50 = 0.00341 μM. | 26331334 | ||
| HLF | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HLF cells after 72 hrs by CCK8 assay, GI50 = 0.00489 μM. | 26331334 | ||
| WI38 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human WI38 cells after 72 hrs by CCK8 assay, GI50 = 0.00539 μM. | 26331334 | ||
| U937 | Function assay | 24 hrs | Inhibition of HDAC6 in human U937 cells assessed as reduction of alpha-tubilin acetylation at 5 nM to 5 uM after 24 hrs by Western blot analysis | 26331334 | ||
| HCT116 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HCT116 cells assessed as cell viability incubated for 72 hrs by coulter counter method, IC50 = 0.028 μM. | 26481659 | ||
| IGROV1/Pt1 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human IGROV1/Pt1 cells assessed as cell viability incubated for 72 hrs by coulter counter method, IC50 = 0.08 μM. | 26481659 | ||
| IGROV1 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human IGROV1 cells assessed as cell viability incubated for 72 hrs by coulter counter method, IC50 = 0.22 μM. | 26481659 | ||
| Klik om meer experimentele gegevens over cellijnen te bekijken | ||||||
Chemische informatie, opslag en stabiliteit (Chemical Information, Storage & Stability)
| Molecuulgewicht | 540.7 | Formule | C24H36N4O6S2 |
Opslag (vanaf de datum van ontvangst) | |
|---|---|---|---|---|---|
| CAS-nr. | 128517-07-7 | -- | Opslag van stamoplossingen |
|
|
| Synoniemen | FK228, Depsipeptide, FR 901228, NSC 630176, | Smiles | CC=C1C(=O)NC(C(=O)OC2CC(=O)NC(C(=O)NC(CSSCCC=C2)C(=O)N1)C(C)C)C(C)C | ||
Oplosbaarheid (Solubility)
|
In vitro |
DMSO
: 10 mg/mL
(18.49 mM)
Water : Insoluble Ethanol : Insoluble |
Molariteitscalculator
Verdunningscalculator
Molecuulgewichtcalculator
|
In vivo |
|||||
In vivo formulatiecalculator (heldere oplossing)
Stap 1: Voer onderstaande informatie in (Aanbevolen: een extra dier om rekening te houden met verlies tijdens het experiment)
mg/kg
g
μL
Stap 2: Voer de in vivo formulering in (Dit is alleen de calculator, geen formulering. Neem eerst contact met ons op als er geen in vivo formulering is in de sectie oplosbaarheid.)
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
Berekeningsresultaten:
Werkconcentratie: mg/ml;
Methode voor het bereiden van DMSO-moedervloeistof: mg geneesmiddel vooropgelost in μL DMSO ( Concentratie moedervloeistof mg/mL, Neem eerst contact met ons op als de concentratie de DMSO-oplosbaarheid van de batch van het geneesmiddel overschrijdt. )
Methode voor het bereiden van in vivo formulering: Neem μL DMSO moedervloeistof, voeg daarna toeμL PEG300, mengen en verhelderen, daarna toevoegenμL Tween 80, mengen en verhelderen, daarna toevoegen μL ddH2O, mengen en verhelderen.
Methode voor het bereiden van in vivo formulering: Neem μL DMSO moedervloeistof, voeg daarna toe μL Maïsolie, mengen en verhelderen.
Opmerking: 1. Zorg ervoor dat de vloeistof helder is voordat u het volgende oplosmiddel toevoegt.
2. Zorg ervoor dat u het/de oplosmiddel(en) in de juiste volgorde toevoegt. U moet ervoor zorgen dat de verkregen oplossing, bij de vorige toevoeging, een heldere oplossing is voordat u verdergaat met het toevoegen van het volgende oplosmiddel. Fysieke methoden zoals vortexen, ultrasoon of een warmwaterbad kunnen worden gebruikt om het oplossen te bevorderen.
Werkingsmechanisme (Mechanism of Action)
| Kenmerken |
More effective than other classical HDAC inhibitors such as TSA, TPX, and butyrate.
|
|---|---|
| Targets/IC50/Ki |
HDAC1
(Cell-free assay) 36 nM
HDAC2
(Cell-free assay) 47 nM
|
| In vitro |
In tegenstelling tot TSA remt de actieve vorm redFK van Romidepsin HDAC1 en HDAC2 sterk met IC50 van respectievelijk 1,6 nM en 3,9 nM, maar is relatief zwak in het remmen van HDAC4 en HDAC6 met IC50 van respectievelijk 25 nM en 790 nM. Deze verbinding is 17-23 keer zwakker dan redFK in het remmen van deze HDAC's met IC50 van respectievelijk 36 nM, 47 nM, 510 nM en 14 μM. Behandeling met deze chemische stof in HeLa-cellen induceert histonacetylatie en p21-expressie met EC50 van 3,0 nM, sterker dan redFK met EC50 van 11 nM vanwege de instabiliteit van redFK. Naast G2/M-arrest veroorzaakt deze verbinding cyclin D1-downregulatie en een p53-onafhankelijke p21-inductie, wat leidt tot remming van CDK en defosforylering van Rb, wat resulteert in groeiremming in de vroege G1-fase. Het is 100 keer potenter dan TSA en 1.000.000 keer potenter dan butyraat in het remmen van de proliferatie van de A549-cellen. Dit middel remt de groei van U-937-, K562- en CCRF-CEM-cellen met IC50 van respectievelijk 5,92 nM, 8,36 nM en 6,95 nM. Het bevordert apoptose in chronische lymfatische leukemie (CLL)-cellen bij een concentratie die overeenkomt met die waarbij H3- en H4-acetylatie en HDAC-remming optreden, waarbij selectief activering van caspase 8 en effectorcaspase 3, evenals downregulatie van c-FLIP-eiwit betrokken zijn. In 11 van de 13 (85%) niercelcarcinoom-cellijnen en in 16 van de 37 (43%) andere kankercellijnen reguleert deze verbinding tumor-doodreceptoren op en versterkt het de natuurlijke killer (NK)-gemedieerde tumorvernietiging. Het vertoont concentratieafhankelijke cytotoxiciteit tegen een panel van mantelcellymfoom (MCL)-cellijnen.
|
| Kinase Assay |
HDAC-remmende activiteit
|
|
Voor de enzymassay worden 10 μL [3H]acetyl-gelabelde histonen (25.000 cpm/10 μg) toegevoegd aan 90 μL van de HDAC-enzymfractie geëxtraheerd uit 293T-cellen die HDAC1 of HDAC2 overexpresseren in aanwezigheid van toenemende concentraties Romidepsin, en het mengsel wordt gedurende 15 minuten bij 37 °C geïncubeerd. De enzymreactie is lineair gedurende ten minste 1 uur. De reactie wordt gestopt door de toevoeging van 10 μL geconcentreerd HCl. Het vrijgekomen [3H]azijnzuur wordt geëxtraheerd met 1 mL ethylacetaat, en 0,9 mL van de oplosmiddellaag wordt overgebracht in 5 mL waterige scintillatievloeistof II voor de bepaling van radioactiviteit. De IC50-waarden worden bepaald uit ten minste drie onafhankelijke dosis-responslijnen.
|
|
| In vivo |
Romidepsin-behandeling remt potent de neovascularisatie van kippenembryo's en die van volwassen muizen in de Matrigel-plug-assay. Toediening van deze verbinding in een dosis van 0,1-1 mg/kg tweemaal per week verlengt de overleving van muizen met U-937-lymfoom significant, met mediane overlevingstijden van respectievelijk 30,5 (0,56 mg/kg) en 33 dagen (0,32 mg/kg) (vs. 20 dagen in controlemuizen).
|
Referenties |
|
Toepassingen (Applications)
| Methoden | Biomarkers | Afbeeldingen | PMID |
|---|---|---|---|
| Western blot | p21 / Cyclin D1 AcH3(K9) / Ac-α-Tubulin(K40) / Ac-NFκB2(K310) p65 / 3MeH3(K27) HDAC3 / HDAC4 / HDAC6 / HDAC2 γH2AX / PARP1 / Cleaved caspase3 / BAK / p21(waf1/cip1) / XIAP Cyclin E1 / BRCA1 / E2F1 / Cleaved PARP / H3Ac pAKT(S473) / pAKT(T308) / AKT |
|
19682393 |
| Growth inhibition assay | Cell viability |
|
27444036 |
| Immunofluorescence | SS18/TLE1 Cleaved caspase-3 |
|
27120803 |
Informatie over klinische proeven (Clinical Trial Information)
(gegevens van https://clinicaltrials.gov, bijgewerkt op 2024-05-22)
| NCT-nummer | Werving | Aandoeningen | Sponsor/medewerkers | Startdatum | Fasen |
|---|---|---|---|---|---|
| NCT03770000 | Completed | T Cell Lymphoma |
Rhizen Pharmaceuticals SA |
March 12 2019 | Phase 1|Phase 2 |
| NCT02616965 | Active not recruiting | Cutaneous T-cell Lymphoma (CTCL) |
Fox Chase Cancer Center|Seagen Inc.|Celgene Corporation |
February 22 2017 | Phase 1 |
| NCT02616874 | Completed | HIV |
IrsiCaixa|Germans Trias i Pujol Hospital|Fundación FLS de Lucha Contra el Sida las Enfermedades Infecciosas y la Promoción de la Salud y la Ciencia|Hospital Clinic of Barcelona|Hospital de Sant Pau|HIVACAT|University of Oxford|BCN Checkpoint |
February 2016 | Phase 1 |
Producten zijn uitsluitend voor onderzoeksdoeleinden. Niet voor menselijk gebruik. Wij verkopen niet aan patiënten.
©Copyright 2013 Selleck Chemicals. Alle rechten voorbehouden.