product name CPI-360
Description: CPI-360 is a potent, selective,and SAM-competitive EZH1 inhibitor with IC50 of 102.3 NM. CPI-360 functions on the basis of S-adenosyl-Lmethionine (SAM)-competition, inhibits EZH1 about 100-fold less and shows exquisite selectivity across a large panel of histone lysine and arginine, and DNA methyltransferases. CPI-360 potently reduced global H3K27me3 and H3K27me2 levels in a dosedependent manner. CPI-360 effectively suppressed heavy H3K27me3 incorporation in KARPAS-422 cells without affecting total histone turnover.
References: Chem Biol. 2014 Nov 20;21(11):1463-75.
437.53
Formula
C25H31N3O4
CAS No.
1802175-06-9
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 20 mg/mL (45.7 mM)
Water: <1 mg/mL
Ethanol: 18 mg/mL (41.1 mM)
Solubility (In vivo)
10% DMSO+60% PEG 400+ddH2O: 20 mg/mL
Synonyms
other peoduct :
| In Vitro |
In vitro activity: In KARPAS-422 cells, CPI-360 potently reduces global H3K27me3 and H3K27me2 levels with EC50 of 56 nM and 65 nM, respectively. CPI-360 also causes time-dependent transcriptional changes, and affects the viability of Y641N mutant EZH2-containing KARPAS-422 cells. In addition, CPI-360 gradually arrests KARPAS-422 cells in the G1 cell cycle stage followed by the induction of apoptosis. Kinase Assay: CPI-360 is a potent, selectiveEZH2inhibitor with IC50 of 0.5 nM and 2.5 nM nM for wt EZH2 and Y641N EZH2, respectively. Cell Assay: CPI-360 functions on the basis of S-adenosyl-Lmethionine (SAM)-competition, inhibits EZH1 about 100-fold less and shows exquisite selectivity across a large panel of histone lysine and arginine, and DNA methyltransferases. CPI-360 potently reduced global H3K27me3 and H3K27me2 levels in a dosedependent manner. CPI-360 effectively suppressed heavy H3K27me3 incorporation in KARPAS-422 cells without affecting total histone turnover. CPI-360 treatment causes time-dependent transcriptional changes in germinal center B cell-like diffuse large B cell lymphoma. |
|---|---|
| In Vivo | In mice bearing KARPAS-422 xenografts, CPI-360 (200 mg/kg, s.c.) reduces tumor growth by 44%. |
| Animal model | Mice bearing KARPAS-422 tumors |
| Formulation & Dosage | Dissolved in 10% DMSO + 60% polytheylene glycol 400 + 30% ddH2O; 200 mg/kg; s.c.injection |
| References | Chem Biol. 2014 Nov 20;21(11):1463-75. |
