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ACY-738

CAS No. : 1375465-91-0

MCE 站：ACY-738

产品活性：ACY-738 是一种有效的，选择性的，可口服的 HDAC6 抑制剂，IC₅₀ 值为 1.7 nM；ACY-738 同时可抑制 HDAC1，HDAC2 和 HDAC3 的活性，IC₅₀ 值分别为 94，128 和 218 nM。

研究领域：Cell Cycle/DNA Damage  |  Epigenetics

作用靶点：HDAC

In Vitro: 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.

In Vivo: 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.

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