IIC1001-Thapsigargin

Thapsigargin，>98%

【英文同义名】：CHEMBL96926; CHEBI:9516; TG

【中文同义名】：毒胡萝卜素

订购信息：（原装进口，常备现货）

品牌	产品名称	产品货号	规格	目录价（元）
Gene Operation	Thapsigargin (SER Ca²⁺ ATPase inhibitor）	IIC1001-0001MG	1 MG	1129.00
Gene Operation	Thapsigargin (SER Ca²⁺ ATPase inhibitor）	IIC1001-0005MG	5 MG	3989.00

产品描述

Thapsigargi (同义名：CHEMBL96926; CHEBI:9516; TG)是sarco/endoplasmic reticulum Ca2⁺ATP酶的非竞争性，细胞通透的强效抑制剂。 Thapsigargi分离自植物 Thapsia garganica，是一种非TPA型皮肤癌致癌物，可诱导小鼠耳朵炎症反应及小鼠皮肤中HDC活性^[1]。它 Thapsigargin使内质网钙池排空，通过抑制肌质网/内质网Ca2⁺ATP酶来抑制Ca2⁺流向内质网，从而提高胞质内Ca2⁺浓度^[2]。 Thapsigargin诱导ATF3启动子/荧光素酶报告基因转录，并可以上调不同细胞中ATF3的表达，如人HaCaT角化细胞，神经胶质瘤细胞，肝瘤细胞，视网膜色素表皮细胞和呼吸道上皮细胞^[3,4]。另外，thapsigargin还可以诱导成神经细胞瘤细胞（SH-SY5Y）及胎鼠大脑皮层细胞凋亡^[5]。Thapsigargin能显著提高DN 14-3-3η转基因小鼠中GRP78和TRAF2的表达^[6]。已有报道称thapsigargin会引起围产期啮齿类动物大脑组织损伤^[7]。

靶点

靶点	ATPase
IC50（半数有效浓度）

化学特性

Cas No.: 67526-95-8	分子量: 650.76
分子式: C₃₄H₅₀O₁₂	纯度: >98%
同义名: CHEMBL96926; CHEBI:9516; TG
化学名: (3S,3aR,4S,6S,6aR,7S,8S,9bS)-6-(acetyloxy)-4-(butyryloxy)-3,3a-dihydrox y-3,6,9-trimethyl-8-{[(2Z)-2-methylbut-2-enoyl]oxy}-2-oxo-2,3,3a,4,5,6,6a,7,8,9b-decahydroazuleno[4,5-b]furan-7-yl octanoate
外观: 无色或白色的固体
溶解: 溶于DMSO(up to 100 mg/ml)
保存：3年 -20℃ 固体

储存液配制

储存液 (1 ml DMSO体系)	1 mM	5 mM	10 mM	25 mM	50 mM	100 mM
质量(mg)	0.6508	3.2538	6.5076	16.2590	32.5380	65.0760

结构式

使用浓度(仅作参考)

Thapsigargin的具体使用浓度请参考相关文献，并根据自身实验条件（如实验目的，细胞种类，培养特性等）进行摸索和优化。

参考文献

[1] Hakii H., et al. Thapsigargin, a histamine secretagogue, is a non-12-O-tetradecanolphorbol-

13- acetate (TPA) type tumor promoter in two-stage mouse skin carcinogenesis. J Cancer Res Clin Oncol. 111 (3): 177–81 (1986).

[2] Davidson GA, et al. Kinetics of thapsigargin-Ca(2+)-ATPase (sarcoplasmic reticulum) inter- action reveals a two-step binding mechanism and picomolar inhibition. J Biol Chem. 270(20): 11731-4 (1995).

[3] Thastrup O, et al. Thapsigargin, a novel molecular probe for studying intracellular calcium release and storage. Agents Actions. 27(1-2):17-23 (1989).

[4] Inesi G, et al. Thapsigargin, a high affinity and global inhibitor of intracellular Ca2+ transport ATPases. Arch Biochem Biophys. 98(2):313-7 (1992).

[5] Treiman M, et al. A tool coming of age: thapsigargin as an inhibitor of sarco-endoplasmic reticulum Ca(2+)-ATPases. Trends Pharmacol Sci. 19(4):131-5 (1998).

[6] Jackisch C, et al. Delayed micromolar elevation in intracellular calcium precedes induction of apoptosis in thapsigargin-treated breast cancer cells. Clin Cancer Res. 6(7):2844-50 (2000).

[7] Ding WX, et al. Differential effects of endoplasmic reticulum stress-induced autophagy on cell survival. J Biol Chem. 282(7):4702-10 (2007).

外观: 无色或白色的固体

储存液配制

结构式

使用浓度(仅作参考)

参考文献