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JNJ 26481585 dihydrochloride
- Quisinostat dihydrochloride
- Parent CAS: 875320-29-9
- Soluble in DMSO
- MF: C21H26N6O2.2HCl
- MW: 467.39
Description
JNJ 26481585 dihydrochloride (Quisinostat) is a highly potent pan-HDAC inhibitor with sub-nanomolar activity across multiple HDAC isoforms. It produces antiproliferative and pro-apoptotic effects in hematologic malignancy and solid tumor models.
HDAC inhibition alters chromatin acetylation, transcriptional regulation, cell-cycle progression and DNA-damage responses. JNJ 26481585 dihydrochloride is useful for studying broad HDAC blockade and epigenetic anticancer pharmacology.
Key Features
- Potent pan-HDAC inhibitor
- Reported highest IC50: 0.11 nM for HDAC1 with sub-nanomolar activity at several HDACs
- Orally available second-generation HDAC pharmacology
- Active in leukemia and solid tumor models in reported studies
Applications
- HDAC inhibitor pharmacology
- Epigenetic cancer research
- Leukemia and solid tumor model studies
- Histone acetylation and transcription assays
More Information
| Parent CAS No. | 875320-29-9 |
|---|---|
| Chemical Name | N-hydroxy-2-(4-(((1-methyl-1H-indol-3-yl)methylamino)methyl)piperidin-1-yl)pyrimidine-5-carboxamide dihydrochloride |
| SMILES | C1(N2CCC(CNCC3C4=C(N(C)C=3)C=CC=C4)CC2)=NC=C(C(NO)=O)C=N1.Cl.Cl |
| MFCD | N.A. |
| InChi | InChI=1S/C21H26N6O2.2ClH/c1-26-14-17(18-4-2-3-5-19(18)26)11-22-10-15-6-8-27(9-7-15)21-23-12-16(13-24-21)20(28)25-29;;/h2-5,12-15,22,29H,6-11H2,1H3,(H,25,28);2*1H |
| InChiKey | NRUIZESXVMJDKR-UHFFFAOYSA-N |
| CID | 11538455 |
| Short Description | HDAC inhibitor |
References
- S. Deleu et al. The effects of JNJ-26481585, a novel hydroxamate-based histone deacetylase inhibitor, on the development of multiple myeloma in the 5T2MM and 5T33MM murine models. Leukemia. 2009 Oct;23(10):1894-903.
- J. Arts et al. JNJ-26481585, a novel "second-generation" oral histone deacetylase inhibitor, shows broad-spectrum preclinical antitumoral activity. Clin Cancer Res. 2009 Nov 15;15(22):6841-51.
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