JG-98

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

JG-98 是一种变构 Hsp70 抑制剂，对乳腺癌细胞系 MDA-MB-231 和 MCF-7 的活性和稳定性比 MKT-077 高 3 倍以上（EC50 分别为 0.4 uM 和 0.7 uM）。

JG-98 is an allosteric Hsp70 inhibitor, displays >3-fold more active, greater stability than MKT-077 against the breast cancer cell lines MDA-MB-231 and MCF-7 (EC50 of 0.4 uM and 0.7 uM, respectively); strongly affects autophagic flux, increases p62 oligomerization and reduces p62 monomer; destabilizes FoxM1 and relieved suppression of downstream effectors, including p21 and p27.

JG-98 (30 nM-30 μM; 72 hours) has antiproliferative activity across a range of cell lines with the EC50s between ~0.3 and 4 μM.JG-98 (10 μM; 48 hours) activates apoptotic mediators (cleavage of caspase-3 and PARP) in MDA-MB-231 cells.JG-98 destabilizes FoxM1 and relieves suppression of downstream effectors, including p21 and p27. Cell Proliferation Assay Cell Line:MCF-7, MDA-MB-231, A375, MeWo, HeLa, HT-29, SKOV3, Jurkat, mouse embryonic fibroblasts (MEF), MM1.R, INA6, RPMI-8226, JJN-3, U266, NCI-H929, L363, MM1.S, KMS11, LP-1, AMO-1, OPM1, OPM2 cells Concentration:30 nM-30 μM Incubation Time:72 hours Result:Active against all of the lines tested, and the EC50s were variable (between ~0.3 μM and 4 μM). Normal MEFs and OPM1 and OPM2 were relatively less sensitive.Western Blot Analysis Cell Line:MDA-MB-231 cells Concentration:10 μM Incubation Time:48 hours Result:Incudes apoptotic mediators cleavage of caspase 3 and PARP.

JG-98 (3 mg/kg; i.p.; on days 0, 2, and 4) suppresses tumor growth in xenograft models bearing MCF7 and HeLa cells. Animal Model:6-week-old NCR mice (xenografts of MCF7 and HeLa cells) Dosage:3 mg/kg Administration:Intraperitoneal injection; on days 0, 2, and 4 Result:Limited tumor growth, but somewhat less effectively.

JG98

Cytoskeleton/Cell Adhesion Molecules

HSP

HSP70

——

——

1456551-16-8

534.532

C24H21Cl2N3OS3

>98% (HPLC)

DMSO: Soluble （ < 1 mg/ml refers to the product slightly soluble or insoluble )

CCN1C(=CC2=[N+](C=CS2)CC3=CC=CC=C3)SC(=C4N(C5=C(S4)C=C(C=C5)Cl)C)C1=O.[Cl-]

Thiazolium,2-[(Z)-[(5E)-5-(6-chloro-3-methyl-2(3H)-benzothiazolylidene)-3-ethyl-4-oxo-2-thiazolidinylidene]methyl]-3-(phenylmethyl)-,chloride (1:1)

(-20℃)

With Ice Pack

≥ 2 years