Quisinostat (JNJ-26481585) 2HCl

  Cat. No.:  DC7176   Featured
Chemical Structure
875320-29-9
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Field of application
Quisinostat (JNJ-26481585) 2HCl is a novel second-generation HDAC inhibitor with highest potency for HDAC1 with IC50 of 0.11 nM in a cell-free assay, modest potent to HDACs 2, 4, 10, and 11.
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
Synonyms: JNJ26481585,JNJ 26481585
SMILES: C(N1CCC(CN(C2C3=C(N(C)C=2)C=CC=C3)C)CC1)1=NC=C(C(NO)=O)C=N1.[H]Cl.[H]Cl
Formula: C21H28Cl2N6O2
M.Wt: 467.39
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: Quisinostat (JNJ-26481585) is an orally available, potent HDAC inhibitor with an IC50 of 0.11 nM for HDAC1.
In Vivo: JNJ-26481585 induces continuous H3 acetylation in tumor tissue in vivo. JNJ-26481585, a “second-generation” HDAC inhibitor with prolonged pharmacodynamic response in vivo. In agreement with the hypothesis, JNJ-26481585 showed superior efficacy compared with both standard of care agents and first-generation HDAC inhibitors in preclinical tumor models. These studies suggest that an HDAC inhibitor with continuous pharmacodynamic activity may show activity in solid tumor malignancies[1].
In Vitro: Quisinostat exerts broad-spectrum antiproliferative activity against a wide panel of cancer cell lines including lung, colon, breast, prostate, and ovarian cell lines at nanomolar concentrations. JNJ-26481585 shows activity toward all HDAC enzymes tested with highest potency in vitro observed toward recombinant HDAC1 (IC50, 0.11±0.03 nM), which is comparable with the potency observed toward HDAC1-immunoprecipitated complexes from tumor cells (IC50, 0.16±0.02 nM). Lowest in vitro potency is observed toward HDAC6, 7 and 9 (IC50, 32.1-119 nM) [1].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
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DC3110 CUDC-907 (PI3K/HDAC InhibitorI) CUDC-907 (PI3K/HDAC Inhibitor I) is a dual PI3K and HDAC inhibitor for PI3Kɑ, HDAC1, HDAC2, HDAC3 and HDAC10 with IC50 of 19 nM, 1.7 nM, 5 nM, 1.8 nM and 2.8 nM, respectively.
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DC6304 Tubastatin A Tubastatin A is a potent and selective HDAC6 inhibitor with IC50 of 15 nM. It is selective against all the other isozymes (1000-fold) except HDAC8 (57-fold).
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DC7716 TMP269 TMP269 is a novel and selective class IIa histone deacetylase inhibitor with IC50s of 126/80/36/9 nM for HDAC 4/5/7/9, respectively; 20-400 fold selectivity over class1 HDACs.
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