SGC0946 --- DOT1L inhibitor

Overview
Catalog #	bs-60101c-2-mg-solid
Product Name	SGC0946 --- DOT1L inhibitor
Specifications
Storage Buffer	Powder
Storage Condition	Store in dry, dark place at -20C for 1 year.
Target
Product Information	Molecular Weight: 618.57 Formula: C28 H40 Br N7 O4 CAS Number: 1561178-17-3 InChi Key: IQCKJUKAQJINMK-HUBRGWSESA-N InChi: InChI=1S/C28H40BrN7O4/c1-16(2)35(12-6-11-31-27(39)34-18-9-7-17(8-10-18)28(3,4)5)14-20-22(37)23(38)26(40-20)36-13-19(29)21-24(30)32-15-33-25(21)36/h7-10,13,15-16,20,22-23,26,37-38H,6,11-12,14H2,1-5H3,(H2,30,32,33)(H2,31,34,39)/t20-,22-,23-,26-/m1/s1 Smiles: CC(C)N(C[C@H]1O[C@H]([C@H](O)[C@@H]1O)N1C=C(Br)C2=C1N=CN=C2N)CCCNC(=O)NC1C=CC(=CC=1)C(C)(C)C Purity: 98.0 Solubility: DMSO up to 100 mM Appearance: Solid Power. Shelf Life: 1.0 years
Description	SGC0946 is a highly potent and selective inhibitor of DOT1L methyltransferase. It selectively blocks binding of the cofactor, S-adenosylmethionine, to DOT1L, and inhibits the enzyme with an IC50 of 0.3 nM in a radioactive enzyme assay and is over 100-fold selective for other histone methyltransferases/HMTs. SGC0946 potently reduces H3K79 dimethylation with cellular IC50 of 2.6 nM in A431 cells, and 8.8 nM in MCF10A cells, which potently and selectively kills cells containing an MLL translocation. SGC0946 is much more potent than its close analog EPZ004777, and serves as an excellent chemical probe for investigating DOT1L and further development of DOT1L inhibitors for cancer therapy.