Alteminostat(Synonyms: CKD-581)

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Alteminostat (Synonyms: CKD-581)

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。

Alteminostat(Synonyms: CKD-581)

Alteminostat Chemical Structure

CAS No. : 1246374-97-9

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生物活性

Alteminostat (CKD-581) is a potent HDAC inhibitor. Alteminostat inhibits the class I-II HDAC family via histone H3 and tubulin acetylation. Alteminostat can be used for lymphoma and multiple myeloma research[1].

体外研究
(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[1].
Alteminostat (CKD-581; 10-300 nM; 24 hours) treatment decreases the expression of BCL-6 as well as BCL-2 in cells[1].
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[1].
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[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: SU-DHL-4, OCI-LY1, SU-DHL-2, and U2932 cells
Concentration: 1 nM-10 μM
Incubation Time: 72 hours
Result: Potently reduced cell viability in all four lymphoma cell lines in a concentration-dependent manner.

Western Blot Analysis[1]

Cell Line: SU-DHL-4 and OCI-LY1 cells
Concentration: 10 nM, 30 nM, 100 nM, 300 nM
Incubation Time: 24 hours
Result: Decreased the expression of BCL-6 as well as BCL-2 in cells.

体内研究
(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[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male NOD.CB17 SCID injected with SU-DHL-4 cells[1]
Dosage: 20 mg/kg or 40 mg/kg
Administration: Intraperitoneal injection; twice a week; for 4 weeks
Result: Partially but significantly suppressed tumor growth.

Clinical Trial

分子量

492.61

Formula

C27H36N6O3
CAS 号

1246374-97-9
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Soo Jin Kim, et al. Anti-Cancer Effects of CKD-581, a Potent Histone Deacetylase Inhibitor against Diffuse Large B-Cell Lymphoma. Int J Mol Sci. 2020 Jun 19;21(12):4377.

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