Alteminostat

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]. 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]. 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].