| CAS NO: | 335165-68-9 |
| 包装 | 价格(元) |
| 10mg | 电议 |
| 50mg | 电议 |
| Cas No. | 335165-68-9 |
| 化学名 | 1-(3,6-dibromocarbazol-9-yl)-3-piperazin-1-ylpropan-2-ol;dihydrochloride |
| Canonical SMILES | C1CN(CCN1)CC(CN2C3=C(C=C(C=C3)Br)C4=C2C=CC(=C4)Br)O.Cl.Cl |
| 分子式 | C19H21Br2N3O.2HCl |
| 分子量 | 540.12 |
| 溶解度 | <46.72mg/ml in DMSO |
| 储存条件 | Desiccate at RT |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 产品描述 | IC50: 0.52 μM in Bax assay Bax channel blocker is an inhibitor of Bax-mediated mitochondrial cytochrome c release. In the cytosol, cytochrome c is found to form a complex with dATP, Apaf-1, and procaspase-9, which results in caspase 9 activation followed by downstream activation of other caspases, such as caspase 8, ultimately leading to the cell death. After caspase 8 cleavage, the 15.5 kDa C-terminal fragment of Bid interacts with Bak and Bax. In vitro: Bax channel blocker, a 3,6-dibromocarbazole derivative, was observed to inhibit cytochrome c releasing from mitochondria by Bax channel modulation. The monohydroxy analogue Bax channel blocker remained the unprecedented inhibition of Bax-induced cytochrome c release at 10 μM. The IC50 value of Bax channel blocker was determined to be 0.52 μM, indicating that Bax channel blocker was a Bax channel inhibitor as hypothesized. Moreover, in the liposome assay, Bax channel blocker showing significant inhibition (>65%) of cytochrome c release at 10 μM also demonstrated sub-micromolar IC50 value [1]. In vivo: So far, there is no animal in vivo study conducted for Bax channel blocker. Clinical trial: N/A Reference: |
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