Quisinostat

SKU: orb1223772

Description

Quisinostat (JNJ-26481585) is a novel second-generation HDAC inhibitor with highest potency for HDAC1 with IC50 of 0.11 nM, modest potent to HDACs 2, 4, 10, and 11; greater than 30-fold selectivity against HDACs 3, 5, 8, and 9 and lowest potency to HDACs 6 and 7. Phase 2.(In Vitro):Quisinostat inhibits HDAC isozymes in vitro.Quisinostat (30-1000 nM; 24 hours) is a potent pan-HDAC inhibitor in tumor cells.Quisinostat has a broad spectrum antiproliferative activity against solid and hematologic cancer cell lines and induces apoptosis.(In Vivo):Quisinostat (40 mg/kg; p.o.; once daily; for 3 days) acts as a potent HDAC1 inhibitor p21waf1,cip1 ZsGreen tumors in vivo.Quisinostat induces continuous H3 acetylation in tumor tissue in vivo.Quisinostat (10 mg/kg; once daily; i.p.; for 14 days) strongly inhibits the growth of large pre-established HCT116 colon xenografts.

Key Properties

• CAS Number: 875320-29-9
• MW: 394.476
• Purity: >98% (HPLC)
• Formula: C₂₁H₂₆N₆O₂
• SMILES: O=C(C1=CN=C(N2CCC(CNCC3=CN(C)C4=C3C=CC=C4)CC2)N=C1)NO
• Target: HDAC
• Solubility: DMSO:79 mg/mL (200.26 mM); Ethanol:<1 mg/mL (<1 mM); Water:<1 mg/mL (<1 mM)

Bioactivity

• In Vivo:
  Quisinostat (40 mg/kg; p.o. ; once daily; for 3 days) acts as a potent HDAC1 inhibitor that inhibits p21waf1, cip1 ZsGreen tumors In vivo. Quisinostat induces continuous H3 acetylation in tumor tissue In vivo. Quisinostat (10 mg/kg; once daily; i.p.; for 14 days) strongly inhibits the growth of large pre-established HCT116 colon xenografts. Animal model: NMRI nude mice, with HCT116 colon carcinoma cells xenografts. Dosage: 10 mg/kg. Administration: Intraperitoneal injection, once daily, for 14 days. Result: Strongly inhibited the growth of large pre-established HCT116 colon xenografts.
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• In Vitro:
  Quisinostat inhibits HDAC isozymes in vitro. Quisinostat (30-1000 nM; 24 hours) is a potent pan-HDAC inhibitor in tumor cells. Quisinostat has a broad spectrum antiproliferative activity against solid and hematologic cancer cell lines and induces apoptosis. Western blot analysis. Cell line: Human A2780 ovarian carcinoma cells. Concentration: 30 nM, 100 nM, 300 nM, 1000 nM. Incubation time: 24 hours. Result: Induced H3 and H4 acetylation at concentrations as low as 30 to 100 nM.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

(JNJ-26481585)

Quick Database Links

Gene Symbol

HDAC