SC-99

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

一种新型选择性 STAT3 抑制剂，可抑制 JAK2-STAT3 激活。

A novel selective STAT3 inhibitor that inhibits JAK2-STAT3 activation but has no effects on other transcription factors such as NF-κB, and kinases such as AKT, ERK, and c-Src; inhibits STAT3 phosphorylation, dimerization and nuclear translocation, downregulates STAT3-modulated gene expression and induces MM cell apoptosis; delays tumor growth in MM xenograft models (30mg/kg); orally active.

SC99 (10 or 30 μM; for 72 hours) induces MM cell death. SC99 (10 μM; 24 hours) decreases the p-STAT3 level but has no effects on total STAT3 expression. SC99 (2.5, 5, 10, 20 μM; for 60 mins) inhibits JAK2 phosphorylation in a concentration-dependent manner but does not inhibit the phosphorylation levels of AKT, ERK, mTOR or c-Src at a concentration up to 20 μM. SC99 (1.25, 2.5, 5 μM; pre-treated for 10 min) inhibits collagen (2 μg/mL) and thrombin (0.02 U/mL) induced phosphorylation of STAT3 in a concentration-dependent manner. SC99 (pre-treated for 2 hours) inhibits IL-6 (50 ng/ml; for 20 min) induced STAT3 nucleartranslocation in OPM2 cells.Apoptosis Analysis Cell Line:Six multiple myeloma (MM) cell lines (LP1, JJN3, RPMI-8226, U266, OPM2 and OCI-MY5)Concentration:10 or 30 μM Incubation Time:For 72 hours Result:Induced MM cell death.Apoptosis Analysis Cell Line:MM cell lines Concentration:10 μM Incubation Time:24 hours Result:Decreased the p-STAT3 level but had no effects on total STAT3 expression in all cell lines examined.

SC99 (30 mg/kg; orally; daily; for continuous 14 or 28 days) delays myeloma tumor growth in xenograft mice models. SC99 (5, 10,?15 mM, 15?μL; ICV) produces an effective inhibitory effect on the phosphorylation of JAK2 and STAT3 in middle cerebral artery occlusion and reperfusion (MCAO/R) model (adult male SD rats; 250-300?g). SC99 ameliorates neuronal apoptosis and degeneration, neurobehavioral deficits, inflammatory response and brain edema. Animal Model:Nude mice with Human MM cells OPM2 or JJN3 Dosage:30 mg/kg Administration:Orally; daily; for continuous 14 or 28 daysResult:Delayed myeloma tumor growth in xenograft mice models and suppressed tumor growth more than 40% in 14 days in the OPM2 model.

STAT3 inhibitor SC99

JAK/STAT Signaling

STAT

STAT

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882290-02-0

336.147

C15H8Cl2FN3O

>98% (HPLC)

In Vitro:?DMSO : 83.33 mg/mL (247.90 mM)

N#C/C(C(C1=CC=C(Cl)C=C1)=O)=N\NC2=CC=C(F)C(Cl)=C2

(E)-N-(3-chloro-4-fluorophenyl)-2-(4-chlorophenyl)-2-oxoacetohydrazonoyl cyanide

(-20℃)

With Ice Pack

≥ 2 years