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MedChemExpress - Model Quisinostat dihydrochloride -875320-31-3

Quisinostat dihydrochloride (JNJ-26481585 dihydrochloride) is an orally available, potent pan-HDAC inhibitor with IC50s of 0.11 nM, 0.33 nM, 0.64 nM, 0.46 nM, and 0.37 nM for HDAC1, HDAC2, HDAC4, HDAC10 and HDAC11, respectively. Quisinostat dihydrochloride has a broad spectrum antitumoral activity[1].

Quisinostat dihydrochloride

MCE China：Quisinostat dihydrochloride

Brand：MedChemExpress (MCE)

Cat. No.HY-15433A

CAS：875320-31-3

Synonyms：JNJ-26481585 dihydrochloride

Purity：99.05%

Storage：4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Quisinostat dihydrochloride (JNJ-26481585 dihydrochloride) is an orally available, potent pan-HDAC inhibitor with IC50s of 0.11 nM, 0.33 nM, 0.64 nM, 0.46 nM, and 0.37 nM for HDAC1, HDAC2, HDAC4, HDAC10 and HDAC11, respectively. Quisinostat dihydrochloride has a broad spectrum antitumoral activity.

In Vitro：JNJ-26481585 inhibits HDAC isozymes in vitro[1]. JNJ-26481585 (30-1000 nM; 24 hours) is a potent pan-HDAC inhibitor in tumor cells[1]. JNJ-26481585 has broad spectrum antiproliferative activity against solid and hematologic cancer cell lines and induces apoptosis[1].

In Vivo：JNJ-26481585 (40 mg/kg; p.o.; once daily, for 3 days) as a potent HDAC1 inhibitor p21waf1,cip1 ZsGreen tumors in vivo[1]. JNJ-26481585 induces continuous H3 acetylation in tumor tissue in vivo[1]. JNJ-26481585 (10 mg/kg; once daily; i.p.; for 14 days) strongly inhibits the growth of large pre-established HCT116 colon xenografts[1].

IC50 & Target：HDAC1 0.11 nM (IC50) HDAC2 0.33 nM (IC50) HDAC3 4.86 nM (IC50) HDAC4 0.64 nM (IC50) HDAC5 3.69 nM (IC50) HDAC6 76.8 nM (IC50) HDAC7 119 nM (IC50) HDAC8 4.26 nM (IC50) HDAC9 32.1 nM (IC50) HDAC10 0.46 nM (IC50) HDAC11 0.37 nM (IC50)

References：

[1]. Arts J, 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. [Content Brief]

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MedChemExpress - Model Quisinostat dihydrochloride -875320-31-3

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Quisinostat dihydrochloride