BAM7
(Synonyms: BAM 7;BAM-7) 目录号 : GC12053
A direct activator of Bax
Cas No.:331244-89-4
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
BAM7 is a direct and selective activator of BAX with IC50 value of 3.3uM [1].
In the competitive fluorescence polarization assay (FPA), BAM7 competes with FITC–BIM SAHB for BAX binding site(BH3) in a dose dependent manner. BAM7 shows no antiapoptotic or BAKΔC competitive binding interactions even at 50 μM dosing, revealing a remarkable selectivity of BAM7 for BAX. The interaction between BAM7 and BAX at the very surface induces the characteristic structural changes that yield functional BAX oligomerization. In the in vitro assay, BAM7 induces BAX-dependent cell death but not the cells with BAK. BAM7 could be developed to a new generation of apoptotic modulators that directly activate BCL-2 family executioner proteins in cancer
and other diseases driven by pathologic apoptotic blockades [1].
References:
[1] Evripidis Gavathiotis, Denis E Reyna, Joseph A Bellairs, Elizaveta S Leshchiner, and Loren D Walensky. Direct and selective small-molecule activation of proapoptotic BAX. Nat Chem Biol. 2012 July ; 8(7): 639–645.
| Cell experiment [1]: | |
|
Cell lines |
MEF cells |
|
Preparation method |
Limited solubility. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
|
Reacting condition |
10 μM, 20 μM, 30 μM and 40 μM |
|
Applications |
Co-incubation of BAM7 (10 μM, 20 μM, 30 μM and 40 μM) and monomeric BAX (5 μM) induced dose- and time-responsive BAX oligomerization. BAM7 selectively impaired the viability of Bak-/- MEFs but had no effect on MEFs that lack BAX (Bax-/-) or both BAX and BAK (Bax-/- Bak-/-). BAM7 dose-dependently impaired the viability of BAX-reconstituted, but not BAXK21E-reconstituted, Bax-/- Bak-/- MEFs. Bak-/- MEFs demonstrated the morphologic features of apoptosis in response to BAM7 treatment (15 μM). |
|
Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
|
References: [1]. Gavathiotis E, Reyna D E, Bellairs J A, et al. Direct and selective small-molecule activation of proapoptotic BAX[J]. Nature chemical biology, 2012, 8(7): 639-645. | |
| Cas No. | 331244-89-4 | SDF | |
| 别名 | BAM 7;BAM-7 | ||
| 化学名 | (4E)-4-[(2-ethoxyphenyl)hydrazinylidene]-5-methyl-2-(4-phenyl-1,3-thiazol-2-yl)pyrazol-3-one | ||
| Canonical SMILES | CCOC1=CC=CC=C1NN=C2C(=NN(C2=O)C3=NC(=CS3)C4=CC=CC=C4)C | ||
| 分子式 | C21H19N5O2S | 分子量 | 405.47 |
| 溶解度 | DMF: 5 mg/ml,DMF:PBS (pH 7.2)(1:3): 0.33 mg/ml,DMSO: 2 mg/ml | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
||
| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.4663 mL | 12.3314 mL | 24.6627 mL |
| 5 mM | 0.4933 mL | 2.4663 mL | 4.9325 mL |
| 10 mM | 0.2466 mL | 1.2331 mL | 2.4663 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet