Home Epigenetics Histone Methyltransferase inhibitor - EZH1/2 inhibitor CPI-360 For research use only.

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.

CPI-360 Chemical Structure

CPI-360 Chemical Structure

CAS No. 1802175-06-9

Purity & Quality Control

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

CPI-360 Related Products

Signaling Pathway

Histone Methyltransferase Signaling Pathways

Histone Methyltransferase Signaling Pathway

Cell Data

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 26189078
Click to View More Cell Line Experimental Data

Biological Activity

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
EZH1 [1]
102.3 nM
In vitro
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 vivo In mice bearing KARPAS-422 xenografts, CPI-360 (200 mg/kg, s.c.) reduces tumor growth by 44%. [1]
Animal Research Animal Models Mice bearing KARPAS-422 tumors
Dosages 200 mg/kg, twice daily
Administration s.c.

Chemical Information & Solubility

Molecular Weight 437.53 Formula

C25H31N3O4
CAS No. 1802175-06-9 SDF Download CPI-360 SDF
Smiles CC1=CC(=C(C(=O)N1)CNC(=O)C2=C(N(C3=CC=CC=C32)C(C)C4CCOCC4)C)OC
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 20 mg/mL ( (45.71 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 18 mg/mL

Water : Insoluble


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In vivo
Batch:

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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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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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