|1-(3,6-二溴-9H-咔唑-9-基)-3-(哌嗪-1-基)丙-2-醇|CsnPharm

CAS No.: 335165-68-9

1-(3,6-Dibromo-9H-carbazol-9-yl)-3-(piperazin-1-yl)propan-2-ol Catalog No. CSN23881

Synonyms: Bax channel blocker;Brain-specific angiogenesis inhibitor 1

BAI1 is an inhibitor of Bax-mediated mitochondrial cytochrome c release (IC50 = 0.52 μM).

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技术信息

生物活性

描述The Bcl-2 family is a group of anti- and pro-apoptotic proteins that plays essential roles in regulating programmed cell death. The activation of BAX, a pro-apoptotic member of the Bcl-2 family, is critical for the induction of mitochondrial outer membrane permeabilization. BAX activation inhibitor 1 (BAI1) dose-dependently inhibited tBID-induced BAX-mediated membrane permeabilization with an IC₅₀ value of 3.3 μM. The dissociation constant for BAI1 with BAX was 15.0 ± 4 μΜ. BAI1 dose-dependently inhibited tBID- and BIM SAHB-induced BAX membrane association and translocation with IC₅₀ values of 5 ± 1 and 2 ± 1 μΜ, respectively. In mouse embryonic fibroblasts, BAI1 inhibited TNF-α/cyclohexamide-induced apoptosis in a dose-dependent manner with an IC₅₀ value of 1.8 μM^[1].
作用机制BAI1 demonstrated an inhibitory effect on BAX activation by binding directly to an allosteric site of BAX.
参考文献

[1] Garner TP, Amgalan D, Reyna DE, Li S, Kitsis RN, Gavathiotis E. Small-molecule allosteric inhibitors of BAX. Nat Chem Biol. 2019 Apr;15(4):322-330. doi: 10.1038/s41589-018-0223-0. Epub 2019 Feb 4. PMID: 30718816; PMCID: PMC6430685.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.1404 mL
- 10.7021 mL
- 21.4041 mL
- 5 mM
- 0.4281 mL
- 2.1404 mL
- 4.2808 mL
- 10 mM
- 0.2140 mL
- 1.0702 mL
- 2.1404 mL

技术信息

CAS号

335165-68-9

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C19H21Br2N3O

运输

蓝冰

分子量

467.20

别名

Bax channel blocker;Brain-specific angiogenesis inhibitor 1

溶解度

DMSO	10.33 mg/mL (22.1 mM)
Water	insoluble

动物实验配方

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1-(3,6-Dibromo-9H-carbazol-9-yl)-3-(piperazin-1-yl)propan-2-ol Catalog No. CSN23881

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