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
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Alteminostat
CAS number：1246374-97-9 molecular formula：C27H36N6O3
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| Chinese alias | 阿替诺特 | ||
| English alias | - | ||
| CAS number | 1246374-97-9 | molecular formula | C27H36N6O3 |
| molecular weight | 492.61 g/mol | Exact mass | ≥98% |
| PSA | 93.900 Ų | logp | 2.800 |
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