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- 详细信息
- 技术资料
- 保存条件:
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 库存:
货期:1-2天
- 供应商:
MedChemExpress LLC
- CAS号:
935693-62-2
- 规格:
10 mM * 1 mL/1 mg/5 mg/10 mg/25 mg/50 mg/100 mg
| 规格: | 10 mM * 1 mL | 产品价格: | ¥1268.0 |
|---|---|---|---|
| 规格: | 1 mg | 产品价格: | ¥327.0 |
| 规格: | 5 mg | 产品价格: | ¥720.0 |
| 规格: | 10 mg | 产品价格: | ¥1153.0 |
| 规格: | 25 mg | 产品价格: | ¥2400.0 |
| 规格: | 50 mg | 产品价格: | ¥3100.0 |
| 规格: | 100 mg | 产品价格: | ¥4650.0 |
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BIX-01294
CAS No. : 935693-62-2
MCE 国际站:BIX-01294
产品活性:BIX-01294 是一种可逆且高度选择性的 G9a 和 GLP 组蛋白甲基转移酶抑制剂,IC50 分别为 1.9 μM 和 0.7 μM。BIX-01294 通过与底物赖氨酸残基 N 端的氨基酸竞争结合来抑制 G9a/GLP。BIX-01294 是一种 (1H-1,4-diazepin-1-yl)-quinazolin-4-yl 胺衍生物,可诱导坏死性凋亡 (necroptosis) 和自噬。BIX-01294 在复发性肿瘤细胞中具有抗肿瘤活性。
研究领域:Epigenetics | Autophagy
作用靶点:Histone Methyltransferase | Autophagy
In Vitro: BIX-01294 (2 μM; 48 h) selectively inhibits recurrent tumor cell growth.
BIX-01294 (1 μM) leads to a marked increase in phosphorylation of S345 of MLKL.
BIX-01294 (1 μM) significantly upregulates the canonical p53 targets Cdkn1a (p21) and Gadd45a in recurrent tumor cell lines.
BIX-01294 (1 μM; 6 days) causes the reduction in H3K9me2 levels in primary and recurrent tumor cells.
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).
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.
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).
BIX-01294 inhibits G9a in an uncompetitive manner with S-adenosyl-methionine (SAM).
BIX-01294 (1 µg/mL) causes reduction in the BrdU incorporation of fetal PASMCs. BIX-01294 treatment decreases the PASMCs migration induced by PDGF.
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.
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