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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 | ¥ 219 | 现货 | |
| 5 mg | ¥ 485 | 现货 | |
| 10 mg | ¥ 779 | 现货 | |
| 25 mg | ¥ 1,450 | 现货 | |
| 50 mg | ¥ 2,570 | 现货 | |
| 100 mg | ¥ 3,530 | 现货 | |
| 1 mL x 10 mM (in DMSO) | ¥ 810 | 现货 |
BIX-01294 相关产品
| 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) |
| 颜色 | Yellow |
| 物理性状 | Solid |
| 存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| 溶解度信息 | DMSO: 84.17 mg/mL (171.55 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| 体内实验配方 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.3 mg/mL (6.73 mM), Sonication is recommended. 请按顺序添加溶剂,在添加下一种溶剂之前,尽可能使溶液澄清。如有必要,可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考,体内配方并不是绝对的,请根据不同情况进行调整。 | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
DMSO
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