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UNC0646
- Soluble in DMSO
- MF: C36H59N7O2
- MW: 621.9
Description
UNC0646 is a very potent and selective G9a/GLP histone lysine methyltransferase inhibitor with reported IC50 values of 6 nM for G9a and 15 nM for GLP.
G9a (EHMT2) and GLP (EHMT1) catalyze repressive H3K9 methylation and regulate chromatin state, gene expression and cell identity. UNC0646 is a cell-active epigenetic probe with strong separation between functional potency and cytotoxicity.
Key Features
- Potent G9a/GLP methyltransferase inhibitor
- IC50: 6 nM for G9a and 15 nM for GLP
- Cell-active epigenetic probe with favorable toxicity separation
- Modulates H3K9 methylation and transcriptional regulation
Applications
- G9a/EHMT2 and GLP/EHMT1 pharmacology
- Histone H3K9 methylation studies
- Epigenetic gene-regulation assays
- Cancer, differentiation and chromatin-state research
More Information
| Parent CAS No. | 1320288-17-2 |
|---|---|
| Chemical Name | N-(1-cyclohexylpiperidin-4-yl)-2-(4-isopropyl-1,4-diazepan-1-yl)-6-methoxy-7-(3-(piperidin-1-yl)propoxy)quinazolin-4-amine |
| SMILES | N1=C2C(C=C(OC)C(OCCCN3CCCCC3)=C2)=C(NC2CCN(C3CCCCC3)CC2)N=C1N1CCCN(C(C)C)CC1 |
| MFCD | N.A. |
| InChi | InChI=1S/C36H59N7O2/c1-28(2)41-19-10-20-43(24-23-41)36-38-32-27-34(45-25-11-18-40-16-8-5-9-17-40)33(44-3)26-31(32)35(39-36)37-29-14-21-42(22-15-29)30-12-6-4-7-13-30/h26-30H,4-25H2,1-3H3,(H,37,38,39) |
| InChiKey | OUKWLRHRXOPODD-UHFFFAOYSA-N |
| CID | 53315882 |
| Short Description | G9a HMTase inhibitor |
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