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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Name | CPI-455 |
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Iupac Chemical Name | CPI-455 |
Synonyms | N/A |
Molecular Formula | C16H15ClN4O |
Molecular Weight | 314.77 |
Smile | C(C)(C)C1=C(NC=2N(C1=O)N=CC2C#N)C2=CC=CC=C2 |
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 |
CAS Number | 1628208-23-0 |
Related CAS |
Packaging | Price | Availability | Purity | Shipping Time |
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Formulation | crystalline solid |
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Purity | 98% |
Storage | 3 years -20ºCpowder |
Solubility | Soluble in DMSO |
Handling | |
Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. |
HS Code |
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Mechanism | |
Cell study | |
Animal study | |
Clinical study |