Description
CPI-455 is a potent and selective inhibitor of KDM5 demethylases which reduces survival of drug-tolerant cancer cells. CPI-455 mediated KDM5 inhibition, elevated global levels of H3K4 trimethylation (H3K4me3) and decreased the number of DTPs in multiple cancer cell line models treated with standard chemotherapy or targeted agents. Pretreatment of cancer cells with a KDM5-specific inhibitor results in the ablation of a subpopulation of cancer cells that can serve as the founders for therapeutic relapse.
Product information
CAS Number: 1628208-23-0
Molecular Weight: 278.31
Formula: C16H14N4O
Chemical Name: 6-isopropyl-7-oxo-5-phenyl-4,7-dihydropyrazolo[1,5-a]pyrimidine-3-carbonitrile
Smiles: CC(C)C1C(=O)N2N=CC(C#N)=C2NC=1C1C=CC=CC=1
InChiKey: DHXKRMSKXLDZGY-UHFFFAOYSA-N
InChi: InChI=1S/C16H14N4O/c1-10(2)13-14(11-6-4-3-5-7-11)19-15-12(8-17)9-18-20(15)16(13)21/h3-7,9-10,19H,1-2H3
Technical Data
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO up to 50 mM
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:
KDM5-C70 was used at 1-10 µM in vitro and cellular assays.
References:
- Vinogradova M, et al. An inhibitor of KDM5 demethylases reduces survival of drug-tolerant cancer cells. (2016) Nat Chem Biol. 12(7):531-8.
Products are for research use only. Not for human use.
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