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HA14-1

目录号 M3753 所有产品仅供科研使用,严禁用于人或动物的治疗等任何其他用途,不为任何个人提供产品和服务  


HA14-1是非肽类Bcl-2表面口袋配体,IC50为9 μM。

HA14-1结构式
规格 价格 库存状态
10mg ¥ 400 中国库存现货
50mg ¥ 1200 中国库存现货
其他规格数量报价?

质量标准及产品资料
生物活性

HA14-1是非肽类Bcl-2表面口袋配体,IC50为9 μM。HA14-1 is a small molecule which has the potential of inducing apoptosis in cancerous cells. HA14-1 manifests an antagonistic effect on antiapoptotic protein Bcl-2 and consequently induces cell death in various cancerous cell lines. HA-14-1 also has the ability to inhibit ceramide glucosyltransferase. The IC50 value of HA14-1 against ceramide glucosyltransferase is 4.5μM, which is lower than that reported for Bcl-2 in vitro. Kinetic analyses revealed that HA14-1 is a competitive and mixed-type inhibitor with respect to C6-NBD-ceramide and UDP-glucose, respectively.P53 pathway to be the probable mechanism of action for the induction of apoptosis in HeLa cell by downregulating the effect of anti-apoptotic proteins suggesting that HA14-1 may provide therapeutic potential for the treatment of human cervical cancer.

实验参考
体外实验*
细胞系 HF1A3, HF4.9 and HF28RA cells
方法 Determining the cytotoxic effects of HA14-1 against different FL cell lines by the MTT assay. Briefly, incubating the cells (5000/well) in triplicate in 96-well plate in the presence or absence of HA14-1 for 20 h at 37 °C. Thereafter, adding the MTT solution to each well. After 4 h incubation at 37 °C, measuring the optical density (OD) by means of 96-well plate reader, with the extraction buffer as a blank. The following formula is used: percentage cell viability = (OD of the experiment samples/OD of the control) ?100. Sigmoidal dose-response curves are fitted to the mean cell viability plotted against log HA14-1 dose and lethal concentration 50% (LC50) values are calculated from the resulting curves using Prism 4.0 softw
浓度 ~25 μM
处理时间 20 h

*上述方法来自公开文献,仅供相同目的实验参考。如实验目的、材料、方法不同,请参考其他文献。

体内实验*
动物模型 Female Swiss nude mice bearing BeGBM xenografts
配制 Free RPMI 1640-50% DMSO.
剂量 400 nM
给药处理 Inject at the site of cell injection.

*上述方法来自公开文献,仅供相同目的实验参考。如实验目的、材料、方法不同,请参考其他文献。

化学性质
分子量 409.23
分子式 C17H17BrN2O5
CAS号 65673-63-4
溶解性(25°C) DMSO
储存条件 粉末型式       -20°C   3年;4°C   2年
溶于溶剂       -80°C   6个月;-20°C   1个月
运输方式 冰袋运输,根据产品的不同,可能会有相应调整。
储备液配制

*下述溶液配置方法仅为基于分子量计算出的理论值。不同产品在配置溶液前,需考虑其在不同溶剂中的溶解度限制。

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.4436 mL 12.2181 mL 24.4361 mL
5 mM 0.4887 mL 2.4436 mL 4.8872 mL
10 mM 0.2444 mL 1.2218 mL 2.4436 mL
不同实验动物依据体表面积的等效剂量转换表(参考来源于公开文献
小鼠 大鼠 豚鼠 仓鼠
重量 (kg) 0.02 0.15 1.8 0.4 0.08 10
体表面积 (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km 系数 3 6 12 8 5 20
动物 A (mg/kg) = 动物 B (mg/kg) ×  动物 B的Km系数
动物 A的Km系数

例如,依据体表面积折算法,将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量,需要将20 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到化合物用于大鼠的等效剂量为10 mg/kg。

参考文献

[1] Rehman K, et al. Chem Biol Drug Des. Effect of HA14-1 on apoptosis-regulating proteins in HeLa cells.

[2] Ranjan K, et al. Biofactors. Regulation of HA14-1 mediated oxidative stress, toxic response, and autophagy by curcumin to enhance apoptotic activity in human embryonic kidney cells.

[3] Niino S, et al. Biochem Biophys Res Commun. A small molecule inhibitor of Bcl-2, HA14-1, also inhibits ceramide glucosyltransferase.

[4] Nyhan MJ, et al. Br J Cancer. The BH3 mimetic HA14-1 enhances 5-fluorouracil-induced autophagy and type II cell death in oesophageal cancer cells.

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关键词:HA14-1, HA14-1供应商, Bcl-2抑制剂, 购买HA14-1, HA14-1溶解度, HA14-1结构式








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