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在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
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.
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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell 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 AnalysisCell 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.
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 . MCE 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 Dosage: 20 mg/kg or 40 mg/kg Administration: Intraperitoneal injection; twice a week; for 4 weeks Result: Partially but significantly suppressed tumor growth.
Form:Solid