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CPI-360

Catalog No. T6810   CAS 1802175-06-9
Synonyms: CPI360, CPI 360

CPI-360 is a potent, selective, and SAM-competitive EZH1 inhibitor with IC50 of 102.3 nM, >100-fold selectivity over other methyltransferases.

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CPI-360, CAS 1802175-06-9
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Purity: 98%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description CPI-360 is a potent, selective, and SAM-competitive EZH1 inhibitor with IC50 of 102.3 nM, >100-fold selectivity over other methyltransferases.
Targets&IC50 EZH1:102.3 nM
In vitro 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. [1]
In vivo In mice bearing KARPAS-422 xenografts, CPI-360 (200 mg/kg, s.c.) reduces tumor growth by 44%. [1]
Synonyms CPI360, CPI 360
Molecular Weight 437.54
Formula C25H31N3O4
CAS No. 1802175-06-9

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 16 mg/mL (36.6 mM)

H2O: <1 mg/mL

Ethanol: 15 mg/mL (34.3 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Bradley WD, et al. Chem Biol. 2014, 21(11), 1463-1475.

Related Products

Related compounds with same targets
(S)-(−)-Perillyl alcohol CPI-360 Diclofenac Potassium PF-543 GSK1904529A Ezatiostat LYN-1604 Curzerene

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

CPI-360 1802175-06-9 表观遗传 凋亡 Apoptosis Histone Methyltransferase CPI360 CPI 360 Inhibitor inhibitor inhibit