Network Version
BIX-01294 Data Sheet
| Product Name: | BIX-01294 |
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|---|---|---|
| CAS No.: | 935693-62-2 | |
| Cat. No.: | HY-10587 | |
| MWt: | 490.64 | |
| Formula: | C28H38N6O2 | |
| Purity : | >98% | |
| Solubility: | H2O : 1 mg/mL (2.04 mM; Need ultrasonic); DMSO : ≥ 110 mg/mL (224.20 mM) | |
| Mechanisms: | Target: Cancer | |
| Biological Activity: | ||
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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].
IC50 & Target: IC50: 2.7 μM (G9a in DELFIA assay)[2] IC50: 1.9 μM for G9a and 0.7 μM for GLP[5] In Vitro: BIX-01294 (2 μM; 48 h) selectively inhibits recurrent tumor cell growth[1]. BIX-01294 (1 μM) leads to a marked increase in phosphorylation of S345 of MLKL[1]. BIX-01294 (1 μM) significantly upregulates the canonical p53 targets Cdkn1a (p21) and Gadd45a in recurrent tumor cell lines[1]. BIX-01294 (1 μM; 6 days) causes the reduction in H3K9me2 levels in primary and recurrent tumor cells[1]. BIX-01294 leads to necroptotic cell death in recurrent tumor cells. Necrostatin-1 (30 μM) partially reverses cell death induced by BIX-01294 (750 nM; 24 h)[1]. BIX-01294 (4.1 μM; for 2 days) causes around a 20% reduction, concomitant with a comparable increase in the unmodified H3K9 fragment in H3K9me2 in mouse ES cells. BIX-01294 causes pronounced reduction in H3K9me2 and a small decrease for H3K9me3 and H3K9me1 in wild-type ES cells[2]. BIX-01294 has no inhibition of the other histone methyltransferases even at concentrations of 45 μM. BIX-01294 does not affect SUV39H1 (H320R) and PRMT1 within the tested concentration range (up to 10 μM)[2]. BIX-01294 inhibits G9a in an uncompetitive manner with S-adenosyl-methionine (SAM)[2]. BIX-01294 (1 µg/mL) causes reduction in the BrdU incorporation of fetal PASMCs. BIX-01294 treatment decreases the PASMCs migration induced by PDGF[3]. In Vivo: BIX-01294 (10 mg/kg; IP; three times a week for 2 weeks) significantly reduces tumor growth and tumor burden in recurrent tumor cells. Primary tumor growth is not inhibited[1]. |
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