Alteminostat

• CAT Number: I021856
• CAS Number: 1246374-97-9
• Molecular Formula: C27H36N6O3
• Molecular Weight: 492.61
• Purity: ≥95%
• Synonyms: N-[7-(hydroxyamino)-7-oxoheptyl]-4-methyl-N-[4-(1-methylindazol-6-yl)phenyl]piperazine-1-carboxamide
• InChI: InChI=1S/C27H36N6O3/c1-30-15-17-32(18-16-30)27(35)33(14-6-4-3-5-7-26(34)29-36)24-12-10-21(11-13-24)22-8-9-23-20-28-31(2)25(23)19-22/h8-13,19-20,36H,3-7,14-18H2,1-2H3,(H,29,34)
• InChIKey: YEQGPOVCXMZUBT-UHFFFAOYSA-N
• SMILES: CN1CCN(CC1)C(=O)N(CCCCCCC(=O)NO)C2=CC=C(C=C2)C3=CC4=C(C=C3)C=NN4C

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].
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].

Reference

[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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