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BIX-01294 是高度选择性的G9a 和GLP 组蛋白甲基转移酶可逆抑制剂。它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,可诱导坏死性凋亡和自噬,具有抗肿瘤活性。
BIX-01294 是高度选择性的G9a 和GLP 组蛋白甲基转移酶可逆抑制剂。它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,可诱导坏死性凋亡和自噬,具有抗肿瘤活性。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 269 | 现货 | |
2 mg | ¥ 378 | 现货 | |
5 mg | ¥ 595 | 现货 | |
10 mg | ¥ 957 | 现货 | |
25 mg | ¥ 1,790 | 现货 | |
50 mg | ¥ 3,180 | 现货 | |
100 mg | ¥ 4,360 | 现货 | |
200 mg | ¥ 6,430 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 995 | 现货 |
产品描述 | BIX-01294 is an G9a Histone Methyltransferase inhibitor(IC50 : 1.9 μM). |
靶点活性 | G9a:1.9 μM |
体外活性 | BIX-01294在人类膀胱癌细胞中诱导了依赖caspase的凋亡。通过上调DDIT3促进内质网应激(ER stress)并增加了PMAIP1的表达。此外,BIX-01294通过下调去泛素化酶USP9X,进而减少MCL1的表达,最终导致凋亡[1]。 |
细胞实验 | On the first day, cells were seeded in 96 well plates.?Twenty-four hours later, BIX-01294 was added at the indicated concentrations in each well.?After treatment by BIX-01294 for another 24 h, we used 10% TCA to immobilize the cells and then evaluated the living cell numbers using the sulforhodamine B assay as previously described[1] |
分子量 | 490.64 |
分子式 | C28H38N6O2 |
CAS No. | 935693-62-2 |
Smiles | N(C=1C2=C(N=C(N1)N3CCN(C)CCC3)C=C(OC)C(OC)=C2)C4CCN(CC5=CC=CC=C5)CC4 |
密度 | 1.195 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 98 mg/mL (163.33 mM) | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
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