UNC0638, G9a HMTase Inhibitor

Catalog No. size PriceQuantity
M66056-2D 10 mM in DMSO (0.393 mL) $89
M66056-2S 2mg solid $89
M66056-10S 10mg solid $352


Product Information
Molecular Weight: 509.73
Formula: C30H47N5O2
Purity: ≥98%
CAS#: 1255580-76-7
Solubility: DMSO up to 100mM
Chemical Name: 2-Cyclohexyl-N-(1-isopropylpiperidin-4-yl)-6-methoxy-7-(3-(pyrrolidin-1-yl)propoxy) quinazolin-4-amine
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.


Biological Activity:

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.


How to Use:


  •  In vitro:  UNC0638 was used at 0.5µM in vitro and cellular assays.
  •  In vivo: n/a




  • 1. Vedadi M, et al. A chemical probe selectively inhibits G9a and GLP methyltransferase activity in cells. (2011) Nat Chem Biol. 7(8):566-74.
  • 2. Kubicek S. et al. Reversal of H3K9me2 by a small-molecule inhibitor for the G9a histone methyltransferase. (2007) Mol. Cell 25, 473–481.
  • 3. Shi Y, et al. Induction of pluripotent stem cells from mouse embryonic fibroblasts by Oct4 and Klf4 with small-molecule compounds. (2008) Cell Stem Cell. 3(5):568-74

Products are for research use only. Not for human use.

Payment & Security

American Express Apple Pay Diners Club Discover Elo Google Pay JCB Mastercard PayPal Shop Pay Venmo Visa

Your payment information is processed securely. We do not store credit card details nor have access to your credit card information.

Estimate shipping

You may also like

Recently viewed