Home Epigenetics Histone Methyltransferase inhibitor CPI-360

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CPI-360 Histone Methyltransferase inhibitor

Cat.No.S7656

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

Chemical Structure

Molecular Weight: 437.53

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Quality Control

Batch: S765601 DMSO]20 mg/mL]false]Ethanol]18 mg/mL]false]Water]Insoluble]false Purity: 99.72%
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99.72

Cell Culture, Treatment & Working Concentration

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human HeLa cells Function assay 72 h Inhibition of EZH2 in human HeLa cells assessed as reduction in H3K27me3 levels incubated for 72 hrs by ELISA method, IC50=0.075 μM
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 20 mg/mL (45.71 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 18 mg/mL

Water : Insoluble

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Mass Concentration Volume Molecular Weight
Dilution Calculator Molecular Weight Calculator

In vivo
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In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

Molecular Weight 437.53 Formula

C25H31N3O4

 Storage (From the date of receipt)
CAS No. 1802175-06-9 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CC1=CC(=C(C(=O)N1)CNC(=O)C2=C(N(C3=CC=CC=C32)C(C)C4CCOCC4)C)OC

Mechanism of Action

Targets/IC50/Ki
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. This compound also causes time-dependent transcriptional changes, and affects the viability of Y641N mutant EZH2-containing KARPAS-422 cells. In addition, it gradually arrests KARPAS-422 cells in the G1 cell cycle stage followed by the induction of apoptosis.
In vivo
In mice bearing KARPAS-422 xenografts, CPI-360 (200 mg/kg, s.c.) reduces tumor growth by 44%.
References

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