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].
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].
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. |
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].
| 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. |
[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.