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UNC 0379
- Soluble in DMSO
- MF: C23H35N5O2
- MW: 413.56
Description
UNC 0379 is a substrate-competitive inhibitor of SETD8/PR-Set7, the histone H4 lysine 20 methyltransferase. It inhibits H4K20 methylation with selectivity over multiple other lysine methyltransferases.
SETD8 regulates chromatin structure, DNA replication, cell-cycle progression and genome stability through H4K20 methylation. UNC 0379 is useful for probing SETD8-dependent epigenetic regulation and distinguishing substrate-competitive inhibition from SAM-competitive methyltransferase pharmacology.
Key Features
- SETD8/PR-Set7 histone methyltransferase inhibitor
- Reported IC50: 7.3 µM against SETD8
- Substrate-competitive and noncompetitive with SAM
- Selective over a panel of other methyltransferases including G9a and GLP
Applications
- Epigenetic enzyme pharmacology
- H4K20 methylation studies
- Chromatin and cell-cycle research
- Methyltransferase selectivity profiling
More Information
| Parent CAS No. | 1620401-82-2 |
|---|---|
| Chemical Name | 6,7-dimethoxy-2-(pyrrolidin-1-yl)-N-(5-(pyrrolidin-1-yl)pentyl)quinazolin-4-amine |
| SMILES | N1=C2C(C=C(OC)C(OC)=C2)=C(NCCCCCN2CCCC2)N=C1N1CCCC1 |
| MFCD | N.A. |
| InChi | InChI=1S/C23H35N5O2/c1-29-20-16-18-19(17-21(20)30-2)25-23(28-14-8-9-15-28)26-22(18)24-10-4-3-5-11-27-12-6-7-13-27/h16-17H,3-15H2,1-2H3,(H,24,25,26) |
| InChiKey | WEXCGGWTIDNVNT-UHFFFAOYSA-N |
| CID | 78357767 |
| Short Description | SETD8 HMTase inhibitor |
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