ACY-738

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

ACY-738 (ACY738) 是一种有效且特异性的 HDAC6 抑制剂 (IC50=1.7 nM)，具有改善的大脑生物利用度；与 I 类 HDAC 相比，选择性高出 60-1500 倍。

ACY-738 (ACY738) is a potent and specific HDAC6 inhibitor (IC50=1.7 nM) with improved brain bioavailability; displays 60-1500 fold selectivity over class I HDACs; induces dramatic increase in α-tubulin acetylation in brain and stimulates mouse exploratory behaviors; increases the innervation of the neuromuscular junctions in the gastrocnemius muscle and improves the motor and sensory nerve conduction in the mutant HSPB1-induced CMT2 mouse model.Depression Preclinical.

ACY-738 (2.5?μM) increases the acetylated (lysine 40) fraction of α-tubulin in RN46A-B14 cells. ACY-738 (10 μM) induces cell death comparable to LBH589 and FK228.

ACY-738 (5?mg/kg) leads to significant increase in α-tubulin acetylation in whole-brain lysates. ACY-738 (50?mg/kg) fails to produce an enhancement of locomotor activity in WT mice tested in a home cage environment. ACY-738 (5 mg/kg) reaches a maximum plasma concentration of 1310 ng/mL at 0.0830 h following treatment. ACY-738 (5 mg/kg BW) alters BM B cell differentiation, but shows no significant effect on IgG and C3 deposition in NZB/W mice. ACY-738 (20 mg/kg) significantly attenuates the severity of proteinuria in NZB/W F1 mice. ACY-738 (5 mg/kg) shows a significant decrease in anti-dsDNA production in NZB/W mice as they aged. ACY-738 (5, 20 mg/kg) attenuates sera IL-1β production as the NZB/W mice aged. ACY-738 (5 mg/kg) significantly reduces glomerular IL-6 and IL-10 mRNA levels by more than 50% while treatment with 20 mg/kg ACY-738 reduced IL-6 and IL-10 mRNA to non-detectable levels.

ACY738 | ACY 738

Cell Cycle/DNA Damage

HDAC

HDAC6

Neurological Disease

Depression

1375465-91-0

270.2866

C14H14N4O2

>98% (HPLC)

DMSO: ≥ 32 mg/mL

O=C(C1=CN=C(NC2(C3=CC=CC=C3)CC2)N=C1)NO

5-Pyrimidinecarboxamide, N-hydroxy-2-[(1-phenylcyclopropyl)amino]-

(-20℃)

With Ice Pack

≥ 2 years