Description
EML741 is a histone lysine methyltransferase G9a/GLP inhibitor, with an IC50 of 23 nM, Kd of 1.13 μM for G9a. EML741 also inhibits DNMT1 (IC50, 3.1 μM), with no effect on DNMT3a or DNMT3b. EML741 exhibits low cell toxicity, and is membrane permeable and blood-brain barrier penetrated.
Product information
CAS Number: 2328074-38-8
Molecular Weight: 523.75
Formula: C31H49N5O2
Chemical Name: 2-cyclohexyl-7-methoxy-N-[1-(propan-2-yl)piperidin-4-yl]-8-[3-(pyrrolidin-1-yl)propoxy]-3H-1,4-benzodiazepin-5-amine
Smiles: CC(C)N1CCC(CC1)NC1=NCC(=NC2=CC(OCCCN3CCCC3)=C(C=C12)OC)C1CCCCC1
InChiKey: CEYUGMZUIYBLTQ-UHFFFAOYSA-N
InChi: InChI=1S/C31H49N5O2/c1-23(2)36-17-12-25(13-18-36)33-31-26-20-29(37-3)30(38-19-9-16-35-14-7-8-15-35)21-27(26)34-28(22-32-31)24-10-5-4-6-11-24/h20-21,23-25H,4-19,22H2,1-3H3,(H,32,33)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
EML741 (Compound 12a) shows a similar high inhibition potency against G9a (97%, 98% inhibition at 10 μM and 25 μM, respectively) and GLP (95%, 98% inhibition at 10 μM and 25 μM, respectively).
Products are for research use only. Not for human use.
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