BH3I-1 - CAS:300817-68-9 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	BH3I-1
英文名称:	BH3I-1
别名:	5-(p-Bromobenzylidine)-α-isopropyl-4-oxo-2-thioxo-3-thiozolidineacetic acid
CAS No:	300817-68-9	分子式:	C₁₅H₁₄BrNS₂O₃	分子量:	400.31
CAS No:	300817-68-9
分子式:	C₁₅H₁₄BrNS₂O₃
分子量:	400.31
MDL:	MFCD03453544

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B70011 BH3I-1 ≥97% (HPLC) (psaitong)

相关产品

包装规格：

5mg 10mg 50mg in glass bottle

溶解性：

溶于DMSO和水

产品描述：

基本信息

产品编号：B70011
产品名称：BH3I-1
CAS:	300817-68-9	储存条件	粉末	2-8℃	四年

分子式：	C15H14BrNS2O3		溶于液体	-80℃	六个月
分子量	573.70			-20℃	一个月
化学名：
Solubility (25°C)	体外	DMSO	64mg/mL warmed with 50ºC water bath (159.87mM)
		Ethanol	13mg/mL warmed with 50ºC water bath (32.47mM)
		Water	Insoluble
	体内（现配现用）
＜1mg/ml表示微溶或不溶。
普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。
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。

制备储备液

浓度溶液体积质量	1mg	5mg	10mg
1mM	2.4981mL	12.4903mL	24.9806mL
5mM	0.4996mL	2.4981mL	4.9961mL
10mM	0.2498mL	1.2490mL	2.4981mL
50mM	0.0500mL	0.2498mL	0.4996mL

生物活性

产品描述	一种有效的 Bcl-2 抑制剂，作用于 Mcl-1，Bcl-2 和 Bcl-xL，Ki 值分别为 260，290 和 1110nM。
靶点/IC50	BH3-Bcl-xL interaction	p53/MDM2
	2.4μM(Ki)	5.3μM(Kd)
体外研究	BH3I-1, while inhibiting its reported target Bcl-2/Bim and Bcl-xL/Bim, shows significant inhibition of both the p53/hDM2 and p300/Hif-1αinteractions. This surprising promiscuity, displays by a well studied compound leads to further interrogate the p53/hDM2 interaction utilizing a standard fluorescence polarization (FP) assay with purified protein. The results from the FP assay validates the split-luciferase screen and demonstrates that BH3I-1 has a Kd=5.3μM against the p53/mDM2 pair, which is comparable to its low micromolar potency reported for the BH3 family of receptors. BH3I-1 inhibits interaction between the BH3 domain and Bcl-xL. NMR analyses reveal that BH3I-1 targets the BH3-binding pocket of Bcl-xL with a Ki of 7.8±0.9μM.

推荐实验方法(仅供参考)

细胞实验:

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; 30μM and 90μM)for 48 h. For zVAD-FMK protection experiments, cells are preincubated with 100μM zVAD-FMK for 1h 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 2μg/mL PI. Cell death is determined by FACS analysis in a FACSCalibur machine.

保存条件：

2-8℃

UN码：

HazardClass：

危害声明：

安全说明：

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