Thapsigargin

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的、选择性的、非竞争性的肌浆/内质网 Ca2+ ATP 酶 (SERCA) 抑制剂，可引起内质网应激并诱导哺乳动物细胞自噬。

A potent, selective, non-competitive inhibitor of the sarco/endoplasmic reticulum Ca2+ ATPase (SERCA), causes ER stress and induces autophagy in mammalian cells; inhibits the Ca2+ ATPase of rat liver ER about 100% at 170 nM, but no inhibition for skeletal muscle SR; increases the concentration of cytosolic free Ca2+ in sensitive cells by an acute and highly specific arrest of the endoplasmic reticulum Ca2+ pump.

Cell Proliferation Assay Cell Line:MH7A human rheumatoid arthritis synovial cells Concentration:0.001, 0.1, and 1?μM Incubation Time:For 2 and 4 days Result:Arrested cell proliferations in a time- and dose-dependent manner.Apoptosis Analysis Cell Line:MH7A human rheumatoid arthritis synovial cells Concentration:0.001, 0.1, and 1?μM Incubation Time:For 2 and 4 days Result:Induces cell apoptosis in a time- and dose-dependent manner.Western Blot Analysis Cell Line:MH7A human rheumatoid arthritis synovial cells Concentration:0.001, 0.1, and 1?μM Incubation Time:For 2 and 4 days Result:Impairs mTOR activity and leads to cyclin D1 expressions

Animal Model:Male Balb/c mice (20-25 g) Dosage:0.25 ug/g, 0.5 ug/g and 1 ug/g Administration:Injection; 24 hours Result:Increased of 2 to 5-fold in chemokine and pro-inflammatory expression.

G-202 | G 202 | G202

Autophagy

Autophagy

Autophagy

Cancer

——

67526-95-8

650.76

C34H50O12

>98% (HPLC)

In Vitro:?DMSO : 50 mg/mL (76.83 mM)

CCCCCCCC(O[C@@H]1[C@@H](OC(/C(C)=C\C)=O)C(C)=C2[C@@]1([H])[C@@](C)(OC(C)=O)C[C@H](OC(CCC)=O)[C@@]([C@@]3(O)C)(O)[C@@]2([H])OC3=O)=O

(3S,3aR,4S,6S,6AR,7S,8S,9bS)-6- (Acetyloxy)-2,3,3a,4,5,6,6a,7,8,9b-decahydro-3,3a-dihydroxy-3,6,9-trimethyl-8-[[(2Z)-2-methyl-1-oxo-2-butenyl]oxy]-2-oxo-4-(1-oxobutoxy)azuleno[4,5-b]furan-7-yl octanoate

(-20℃)

With Ice Pack

≥ 2 years