CPI-455 Chemical Properties

Boiling point:

488.7±55.0 °C(Predicted)

Density 

1.28±0.1 g/cm3(Predicted)

storage temp. 

-20°C

solubility 

Soluble in DMSO (up to at least 25 mg/ml)

form 

solid

pka

-5.10±0.60(Predicted)

color 

Off-white

Stability:

Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.

CPI-455 Usage And Synthesis

Description

CPI-455 (1628208-23-0) is a potent (IC50?= 10 nM) and selective inhibitor of the lysine demethylase KDM5 (equal inhibition of KDM5A, 5B, 5C).1?CPI-455 reduced the number of drug-tolerant persister cancer cells (DTPs) in a dose-dependent, KDM5-dependent manner in multiple cell lines treated with standard chemotherapy or targeted agents. CPI-455 synergized with 5-aza-2’-deoxycytidine (DAC) to reduce the viability of luminal breast cancer cells?in vitro.2?KDM5 demethylases have recently been shown to repress the immune response to tumors?via?suppression of STING.3

Uses

CPI-455 is a potent KDM5 demethylase inhibitor.

References

1) Vinogradova?et al.?(2016),?An inhibitor of KDM5 demethylases reduces survival of drug-tolerant cancer cells;?Nat. Chem. Biol.?12?531 2) Leadem?et al.?(2018),?A KDM5 Inhibitor Increases Global H3K4 Trimethylation Occupancy and Enhances the Biological Efficacy of 5-Aza-2’-Deoxycytidine;?Cancer Res.?78?1127 3) Wu?et al.?(2018),?KDM5 histone demethylases repress immune response via suppression of STING;?PLoS Biol.?16?e2006134dfd

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