Description
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.
Product information
CAS Number: 1246374-97-9
Molecular Weight: 492.61
Formula: C27H36N6O3
Chemical Name: N-hydroxy-7-{[4-(1-methyl-1H-indazol-6-yl)phenyl](4-methylpiperazine-1-carbonyl)amino}heptanamide
Smiles: CN1CCN(CC1)C(=O)N(CCCCCCC(=O)NO)C1C=CC(=CC=1)C1=CC2=C(C=NN2C)C=C1
InChiKey: YEQGPOVCXMZUBT-UHFFFAOYSA-N
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)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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.
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.
Products are for research use only. Not for human use.
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