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 doe
Storage Temp
Store at -20°C
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
Inhibitor of euchromatic histone lysine methyltransferase 1;Inhibitor of euchromatic histone lysine methyltransferase 2
Note
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
Product Description
BIX01294 is an inhibitor of G9a histone methyltransferase with IC50 of 2.7 μM A selective large conductance calcium activated potassium channel activator
Associated Targets
DNMT1Tclin DNA (cytosine-5)-methyltransferase 1 0 Activities
1.Chang Y, Zhang X, Horton JR, Upadhyay AK, Spannhoff A, Liu J, Snyder JP, Bedford MT, Cheng X. (2009) Structural basis for G9a-like protein lysine methyltransferase inhibition by BIX-01294.. Nat Struct Mol Biol, 16 (3):(312-7). [PMID:19219047]
2.Kubicek S, O'Sullivan RJ, August EM, Hickey ER, Zhang Q, Teodoro ML, Rea S, Mechtler K, Kowalski JA, Homon CA et al.. (2007) Reversal of H3K9me2 by a small-molecule inhibitor for the G9a histone methyltransferase.. Mol Cell, 25 (3):(473-81). [PMID:17289593]
3.Chase KA, Feiner B, Ramaker MJ, Hu E, Rosen C, Sharma RP. (2019) Examining the effects of the histone methyltransferase inhibitor BIX-01294 on histone modifications and gene expression in both a clinical population and mouse models.. PLoS ONE, 14 (6):(e0216463). [PMID:31185023]
4.Ryu TY et al.. (2022) Human gut-microbiome-derived propionate coordinates proteasomal degradation via HECTD2 upregulation to target EHMT2 in colorectal cancer.. ISME J, 16 (5):(1205-1221). [PMID:34972816]
5.Kim SK et al.. (2019) The novel prognostic marker, EHMT2, is involved in cell proliferation via HSPD1 regulation in breast cancer.. Int J Oncol, 54 (65-76). [PMID:30365075]
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H1601083