A KDM5 inhibitor; selectively inhibits KDM5A-D (IC50s = 2-10 nM) over KDM2-4

CPI-455 – 5 mg

Brand:
Cayman
CAS:
1628208-23-0
Storage:
-20
UN-No:
Non-Hazardous - /

CPI-455 is an inhibitor of the lysine demethylase 5 family (KDM5A-D).{39079} CPI-455 binds to the demethylase active site and selectively inhibits KDM5A-D (IC50s = 2-10 nM) over KDM2-4, 6, and 7 family members (IC50s = 1 to >25 μM). It increases histone H3K4me2/3 methylation in vitro and decreases the number of drug-tolerant cells in PC9 non-small cell lung, M14 melanoma, and SKBR3 breast cancer cell populations. CPI-455 also reduces growth of glioblastoma cells resistant to temozolomide (TMZ; Item No. 14163) in a dose-dependent manner.{39080}  

 

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Description

A KDM5 inhibitor; selectively inhibits KDM5A-D (IC50s = 2-10 nM) over KDM2-4, 6, and 7 family members (IC50s = 1 to >25 μM); increases histone H3K4me2/3 methylation in vitro; decreases the number of drug-tolerant cancer cells in PC9, M14, and SKBR3 cell populations; reduces growth of TMZ-resistant glioblastoma cells in a dose-dependent manner,

Formal name: 4,7-dihydro-6-(1-methylethyl)-7-oxo-5-phenyl-pyrazolo[1,5-a]pyrimidine-3-carbonitrile

Synonyms: 

Molecular weight: 278.3

CAS: 1628208-23-0

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Demethylases||Research Area

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