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Alteminostat

CAS No. : 1246374-97-9

MCE 站：Alteminostat

产品活性：Alteminostat (CKD-581) 是一种有效的 HDAC 抑制剂。Alteminostat 通过组蛋白 H3 和微管蛋白乙酰化抑制 I-II 类 HDAC 家族。Alteminostat 可用于淋巴瘤和多发性骨髓瘤的研究。

研究领域：Cell Cycle/DNA Damage  |  Epigenetics  |  Apoptosis

作用靶点：HDAC  |  Apoptosis

In Vitro: Alteminostat (CKD-581; 1 nM-10 μM; 72 hours) treatment potently reduces cell viability in all four lymphoma cell lines in a concentration-dependent manner. The IC50 values of Alteminostat in SU-DHL-4, OCI-LY1, SU-DHL-2, and U2932 cells are 1.31 nM, 36.91 nM, 1.18 nM, and 31.99 nM, respectively.
Alteminostat (CKD-581; 10-300 nM; 24 hours) treatment decreases the expression of BCL-6 as well as BCL-2 in cells.
Alteminostat (CKD-581; 30-300 nM; 24 h) treatment results in γH2AX accumulation and PARP1 cleavage in SU-DHL-4, OCI-LY1, SU-DHL-2, and U2932 cells. Alteminostat decreases the protein levels of BCL-XL and MCL-1 in a concentration-dependent manner in OCI-LY1 cells.
Alteminostat (CKD-581; 10-300 nM; 6 hours) treatment increases the acetylation of histone H3 in SU-DHL-2 cells. And tubulin acetylation also increased with 10 nM CKD-581. CKD-581 increased the acetylation of target molecules by inhibiting class I-II HDACs in lymphoma cells.

In Vivo: Alteminostat (CKD-581; 20-40 mg/kg; ntraperitoneal injection; twice a week; for 4 weeks) treatment partially but significantly suppresses tumor growth in SU-DHL-4 xenograft mice.

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