An inhibitor of HDAC6 (IC50 = 1.7 nM); selective for HDAC6 over HDAC1-3 (IC50s = 94

ACY-738 – 1 mg

Brand:
Cayman
CAS:
1375465-91-0
Storage:
-20
UN-No:
Non-Hazardous - /

ACY-738 is an inhibitor of histone deacetylase 6 (HDAC6; IC50 = 1.7 nM).{47573} It is selective for HDAC6 over HDAC1-3 (IC50s = 94, 128, and 218 nM, respectively). ACY-738 (5 mg/kg) increases acetylation of α-tubulin in mouse brain. It increases exploratory activity in a novel open-field test and reduces immobility time in a tail suspension test in wild-type, but not neural cell-selective HDAC6 knockout, mice when administered at a dose of 50 mg/kg, indicating anxiolytic and antidepressant-like activity, respectively. ACY-738 (100 mg/kg in the diet) attenuates decreases in caudal nerve sensory nerve action potential (SNAP) amplitude and increases in hind paw mechanical hypersensitivity in a mouse model of peripheral neuropathy induced by vincristine (Item No. 11764).{47574} It decreases hepatorenal cystogenesis in a rat model of polycystic liver disease when administered at a dose of 30 mg/kg.{47144}  

 

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Description

An inhibitor of HDAC6 (IC50 = 1.7 nM); selective for HDAC6 over HDAC1-3 (IC50s = 94, 128, and 218 nM, respectively); increases acetylation of α-tubulin in mouse brain at 5 mg/kg; increases exploratory activity in a novel open-field test and reduces immobility time in a tail suspension test in wild-type, but not neural cell-selective HDAC6 knockout, mice at 50 mg/kg; attenuates decreases in caudal nerve SNAP amplitude and increases in hind paw mechanical hypersensitivity in a mouse model of vincristine-induced peripheral neuropathy at 100 mg/kg in the diet; decreases hepatorenal cystogenesis in a rat model of polycystic liver disease at 30 mg/kg

Formal name: N-hydroxy-2-[(1-phenylcyclopropyl)amino]-5-pyrimidinecarboxamide

Synonyms: 

Molecular weight: 270.3

CAS: 1375465-91-0

Purity: ≥95%

Formulation: A crystalline solid

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