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CPI-455

Catalog No.: 17109005
Cas No.: 1628208-23-0
Purity : 98% 
17109005 - CPI-455 | CAS 1628208-23-0

Catalog number : 17109005

CAS number : 1628208-23-0

Molecular Formula : C16H15ClN4O 

Molecular Weight : 314.77 

Iupac Chemical Name : CPI-455 

Smile : C(C)(C)C1=C(NC=2N(C1=O)N=CC2C#N)C2=CC=CC=C2

InChiKey : DHXKRMSKXLDZGY-UHFFFAOYSA-N

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SynonymsN/A 
Molecular FormulaC16H15ClN4O 
Molecular Weight314.77 
Appearancecrystalline solid 
Purity98% 
SolubilitySoluble in DMSO 
Storage3 years -20ºCpowder 
Shipping ConditionShipped under ambient temperature as non-hazardous chemical. 
SmileC(C)(C)C1=C(NC=2N(C1=O)N=CC2C#N)C2=CC=CC=C2
InChiKeyDHXKRMSKXLDZGY-UHFFFAOYSA-N
InChiInChI=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
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CPI-455 is a specific KDM5 inhibitor, elevating 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.


CPI-455 has improved potency against KDM5A while demonstrating ~200-fold selectivity for KDM5A over KDM4C. CPI-455 inhibits KDM5A, KDM5B and KDM5C to similar extents but showed substantially weaker potency toward KDM4C and KDM7B (~200- and 770-fold, respectively) and no measurable inhibition of KDM2B, KDM3B or KDM6A. CPI-455-mediated KDM5 inhibition results in a dose-dependent increase in global H3K4me3 in HeLa cells. CPI-455 specifically alters H3K4 methylation in cells and binds at the demethylase active site.  


 

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