UNC669 --- L3MBTL1 Domain Inhibitor

Overview
Catalog #	bs-60083c-5-mg-solid
Product Name	UNC669 --- L3MBTL1 Domain Inhibitor
Specifications
Storage Buffer	Powder
Storage Condition	Store in dry, dark place at -20C for 1 year.
Target
Product Information	Molecular Weight: 338.24 Formula: C15 H20 Br N3 O CAS Number: 1314241-44-5 InChi Key: CQERVFFAOOUFEQ-UHFFFAOYSA-N InChi: InChI=1S/C15H20BrN3O/c16-13-9-12(10-17-11-13)15(20)19-7-3-14(4-8-19)18-5-1-2-6-18/h9-11,14H,1-8H2 Smiles: O=C(C1C=NC=C(Br)C=1)N1CCC(CC1)N1CCCC1 Purity: 98.0 Solubility: DMSO up to 50 mM Appearance: Solid Power. Shelf Life: 1.0 years
Description	UNC669 is a potent and selective small molecule inhibitor for the methyl-lysine (Kme) reading function of L3MBTL1, a member of the malignant brain tumor (MBT) family of chromatin-interacting transcriptional repressors. UNC669 binds L3MBTL1 with a Kd of 5±1 μM (IC50 = 6 ±0.5 μM), exhibiting 5-fold greater affinity than the cognate peptide H4K20Me1, 6-fold selective over its close homologue L3MBTL3 and 10-fold selective over L3MBTL4. The first cocrystal structure of UNC669 bound to L3MBTL1 was determined and provides new insights into binding requirements for further ligand design. UNC669 can serve as a useful chemical tool to interrogate the functions of MBT proteins and probe methyl-lysine reader proteins as a target class.