bs-66056C

DATASHEET

Formulation Powder

Storage: Store in dry, dark place at -20C for 1 year.

Product Information:

Molecular Weight: 509.73

Formula: C30 H47 N5 O2

CAS Number: 1255580-76-7

InChi Key: QOECJCJVIMVJGX-UHFFFAOYSA-N

InChi: InChI=1S/C30H47N5O2/c1-22(2)35-17-12-24(13-18-35)31-30-25-20-27(36-3)28(37-19-9-16-34-14-7-8-15-34)21-26(25)32-29(33-30)23-10-5-4-6-11-23/h20-24H,4-19H2,1-3H3,(H,31,32,33)

Smiles: CC(C)N1CCC(CC1)NC1=NC(=NC2=CC(OCCCN3CCCC3)=C(C=C21)OC)C1CCCCC1

Purity: 98.0

Solubility: DMSO up to 100mM

Appearance: Solid Power.

Shelf Life: 1.0 years

Description:

UNC0638 is a potent, selective and cell permeable G9a and GLP inhibitor, with a toxicity/function ratio of >100, compared to <6 for BIX01294. UNC0638 inhibits G9a HMTase with an IC50 ~15 nM and GLP, a closely-related H3K9 HMTase, with an IC50~19 nM, but is more than 10, 000-fold selective over other epigenetic targets. G9a (EHMT2) and GLP (EHMT1) catalyze the mono and dimethylation of lysine 9 of histone 3 (H3K9) and other non-histone substrates such as p53 and WIZ. UNC0638 treatment in a variety of cell lines resulted in lower global H3K9me2 levels, equivalent to levels observed in small hairpin RNA knockdown of G9a and GLP. UNC0638 inhibits H3K9 dimethylation in MDA-MB231 cells with an IC50 of 81 nM. In mouse embryonic stem cells, UNC0638 reactivated G9a-silenced genes and a retroviral reporter gene in a concentration-dependent manner without promoting differentiation.