BH3I-1
(Synonyms: BHI1; BH 3I1) 目录号 : GC18136
An inhibitor of anti-apoptotic Bcl-2 proteins
Cas No.:300817-68-9
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cell experiment: | Jurkat cells overexpressing Bcl-xL, FL 5.12 and FL 5.12/Bcl-xL cells (5×104 cells per well) are seeded into white 96-well plates and treated with various concentrations of the compounds (e.g., BH3I-1; 30 μM and 90 μM)for 48 h. For zVAD-FMK protection experiments, cells are preincubated with 100 μM zVAD-FMK for 1 h before the addition of chemicals. Cell viability is determined with an MTS assay with a Victor plate reader. For PI staining experiments, cells are grown in 24-well plates and then incubated with 2 μg/mL PI. Cell death is determined by FACS analysis in a FACSCalibur machine[3]. |
References: [1]. Wang L, et al. Development of dimeric modulators for anti-apoptotic Bcl-2 proteins. Bioorg Med Chem Lett. 2008 Jan 1;18(1):236-40. | |
IC50: 293.95 μM
BH3I-1 is an inhibitor of Bcl-2 or Bcl-XL.
It has been reported that a disregulation of the Bcl-2/ Bcl-XL family proteins may result in the development of cancer, since the failure of the inactivation of pro-apoptotic pathways, or the activation of anti-apoptotic pathways, may occur in the regulation processes.
In vitro: The Bcl-2 inhibitors BH3I-1 and it analog BH3I-2 had been applied as lead compounds to find possible Bcl-2 or Bcl-X(L) inhibitors by using computer-assisted screening of in-house database. The identified compounds were further studied regarding their possible application as a drug. It was found that the induction of apoptosis, which was shown as number of hypodiploid cells, was increased by adding BH3I-1 and it analog BH3I-2 to Bjab Bcl-XL and Bjab neo/mock cells. In addition, the effects of the pro-apoptotic proteins Bax and Bak on the induction of apoptosis via BH3I-1 and it analog BH3I-2 were investigated with a variety of knockout cell lines, and resulted showed that the presence or absence of Bak or Bax has no significant influence on the amount of apoptotic events induced by BH3I-1 and it analog BH3I-2 [1].
In vivo: Currently, there is no animial in vivo data reported.
Clinical trial: Up to now, BH3I-1 is still in the preclinical development stage.
Reference:
[1] Füllbeck M,Gebhardt N,Hossbach J,Daniel PT,Preissner R. Computer-assisted identification of small-molecule Bcl-2 modulators. Comput Biol Chem.2009 Dec;33(6):451-6.
| Cas No. | 300817-68-9 | SDF | |
| 别名 | BHI1; BH 3I1 | ||
| 化学名 | (E)-2-(5-(4-bromobenzylidene)-4-oxo-2-thioxothiazolidin-3-yl)-3-methylbutanoic acid | ||
| Canonical SMILES | CC(C(N(C1=S)C(/C(S1)=C([H])\C2=CC=C(Br)C=C2)=O)C(O)=O)C | ||
| 分子式 | C15H14BrNO3S2 | 分子量 | 400.31 |
| 溶解度 | ≥ 40mg/mL in DMSO | 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。 |
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| 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4981 mL | 12.4903 mL | 24.9806 mL |
| 5 mM | 0.4996 mL | 2.4981 mL | 4.9961 mL |
| 10 mM | 0.2498 mL | 1.249 mL | 2.4981 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。
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