Item no. |
HY-10587-5mg |
Manufacturer |
MedChem Express
|
CASRN |
935693-62-2 |
Amount |
5 mg |
Quantity options |
10 mM/1 mL
10 mg
25 mg
50 mg
5 mg
|
Category |
|
Type |
Inhibitors |
Specific against |
other |
Purity |
98.75 |
Formula |
C28H38N6O2 |
Citations |
[1]Kubicek S, et al. Reversal of H3K9me2 by a small-molecule inhibitor for the G9a histone methyltransferase. Mol Cell. 2007 Feb 9;25(3):473-81. [2]Yang Q, et al. 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. [3]Nathaniel W Mabe, et al. G9a Promotes Breast Cancer Recurrence through Repression of a Pro-inflammatory Program. Cell Rep. 2020 Nov 3;33(5):108341. [4]Iwona Anna Ciechomska, et al. BIX01294, an inhibitor of histone methyltransferase, induces autophagy-dependent differentiation of glioma stem-like cells. Sci Rep [5]Yanqi Chang, et al.Structural basis for G9a-like protein lysine methyltransferase inhibition by BIX-01294. Nat Struct Mol Biol. 2009 Mar;16(3):312-7. |
Smiles |
COC1=C(OC)C=C(C(NC2CCN(CC3=CC=CC=C3)CC2)=NC(N4CCN(C)CCC4)=N5)C5=C1 |
ECLASS 10.1 |
32160490 |
ECLASS 11.0 |
32160490 |
UNSPSC |
12000000 |
Shipping condition |
Room temperature |
Available |
|
Manufacturer - Type |
Reference compound |
Manufacturer - Applications |
Cancer-programmed cell death |
Manufacturer - Targets |
Autophagy; Histone Methyltransferase |
Shipping Temperature |
Room Temperature |
Storage Conditions |
-20°C, 3 years; 4°C, 2 years (Powder) |
Molecular Weight |
490.64 |
Product Description |
BIX-01294 is a reversible and highly selective G9a and GLP Histone Methyltransferase inhibitor, with IC50s of of 1.7 μM and 0.9 μM, respectively. BIX-01294 inhibits G9a/GLP by competing for binding with the amino acids N-terminal of the substrate lysine residue. BIX-01294, a (1H-1, 4-diazepin-1-yl)-quinazolin-4-yl amine derivative, induces necroptosis and autophagy. BIX-01294 has antitumor activity in recurrent tumor cells[1][2][3][4][5]. |
Manufacturer - Research Area |
Cancer |
Solubility |
DMSO : ≥ 110 mg/mL|H2O : < 0.1 mg/mL (ultrasonic) |
Manufacturer - Pathway |
Autophagy; Epigenetics |
Isoform |
EHMT1/GLP/KMT1D; EHMT2/G9a/KMT1C |
Clinical information |
No Development Reported |
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All products are intended for research use only (RUO). Not for human, veterinary or therapeutic use.