Successful, we will reply to you quickly.OK
Please select the quantity.OK
Your message is being sent, please wait.Close
Send mail failed, please send again!Close
Products are for research use only. Not for human use. We do not sell to patients.
(BIX 01294; BIX01294)
BIX-01294 Chemical Structure
|Product name: BIX-01294|
|Cat. No.: HY-10587|
BIX01294 is an inhibitor of G9a histone methyltransferase with IC50 of 2.7 μM.
IC50 Value: 2.7 μM
BIX-01294, a diazepin-quinazolinamine derivative, is a selective inhibitor of G9a histone methyl transferase (G9a HMTase) that impairs G9a HMTase and generation of H3K9me2 in vitro. In its inhibition of the histone lysine methyltransferases, BIX-01294 does not compete with cofactor S-adenosyl-methionine. G9a HMTase regulates gene expression including one of the pluripotency genes Oct4. It is reported that BIX-01294 enhances reprogramming efficiency of neural progenitor cells to the same levels as when four transcription factors (Oct4, Klf4, Sox2 and c-Myc) were introduced to somatic cells for generation of induced pluripotent stem cells. BIX-01294 and valproic acid, a histone deacetylase (HDAC) inhibitor, may replace the requirement for ectopic OCT4 (POU5F1) and cMyc respectively in pluripotent stem cell induction (iPS) recipes.
|M.Wt||490.64||Storage||Please store the product under the recommended conditions in the Certificate of Analysis.|
|Solvent & Solubility||
DMSO 98 mg/mL; Water 98 mg/mL
|1 mg||5 mg||10 mg|
|1 mM||2.0382 mL||10.1908 mL||20.3815 mL|
|5 mM||0.4076 mL||2.0382 mL||4.0763 mL|
|10 mM||0.2038 mL||1.0191 mL||2.0382 mL|
. Park KE, Johnson CM, Cabot RA. IVMBIX-01294, an inhibitor of the histone methyltransferase EHMT2, disrupts histone H3 lysine 9 (H3K9) dimethylation in the cleavage-stage porcine embryo. Reprod Fertil Dev. 2012;24(6):813-21.
. Yang Q, Lu Z, Singh D, Raj JU. BIX-01294 treatment blocks cell proliferation, migration and contractility in ovine foetal pulmonary arterial smooth muscle cells. Cell Prolif. 2012 Aug;45(4):335-44.
A-366 is a peptide-competitive inhibitor of G9a/GLP with an enzymatic IC50 of ~3 nM and >100-fold selectivity over other methyltransferases and other non-epigenetic targets.
AMI-1 is a potent, cell-permeable compound which inhibits protein arginine N-methyltransferases (PRMTs), including human PRMT1 (IC50 = 8.8(mu)M) and yeast-Hmt1p (IC50 = 3.0(mu)M), by blocking peptide-substrate binding.
Amodiaquine dihydrochloride dihydrate is a histamine N-methyltransferase inhibitor, used as an antimalarial and anti-inflammatory agent.
BRD4770 is a novel G9a(EHMT2) inhibitor with EC50 of 5 uM (trimethylated H3K9 in PANC-1 cell).
BRD9539 inhibits G9a activity with an IC50 of 6.3 (mu)M, inhibits PRC2 activity with a similar IC50.
C-7280948 is a PRMT1 inhibitor.
EI1 is a potent and selective small molecule inhibitor of EZH2 with IC50 values of 15 nM and 13 nM for wild type EZH2 and EZH2 Y641F mutant, respectively.
EPZ-5676 is a potent and selective aminonucleoside inhibitor of DOT1L histone methyltransferase with Ki of 80 pM; demonstrating >37,000-fold selectivity against all other PMTs tested, inhibits H3K79 methylation in tumor.
EPZ-6438 is a potent, selective, and orally bioavailable small-molecule inhibitor of EZH2 enzymatic activity with Ki value of 2.5(plusmn)0.5 nM.
EPZ-005687 is a potent and selective inhibitor of EZH2 with Ki of 24 nM, 50-fold selectivity against EZH1 and 500-fold selectivity against 15 other protein methyltransferases.