LLL-12

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

一种非肽、细胞渗透性 STAT3 抑制剂，可直接与 STAT3 单体的 pTyr705 结合位点结合。

A nonpeptide, cell-permeable STAT3 inhibitor that binds directly to the pTyr705 binding site of the STAT3 monomer; inhibit STAT3 phosphorylation (tyrosine 705) and induces apoptosis in various breast, pancreatic, and glioblastoma cancer cell lines with IC50 of 0.16-3.09 uM; also inhibits STAT3 phosphorylation induced by IL-6 and IFN-α in MM cells, but not STAT1, STAT2, STAT4 and STAT6 phosphorylation; inhibits STAT3 DNA binding activity and STAT3-dependent transcriptional activity, but not STAT1; exhibits potent inhibitory activity on breast and glioblastoma tumor growth in a mouse xenograft model.

Western Blot AnalysisCell Line:A2780, SKOV3, CAOV-3 and OVCAR5 ovarian cancer cell linesConcentration:0.25, 0.5, and 1 μM for A2780 and OVCAR5; 1, 2.5, and 5 μM for SKOV3 and CAOV-3Incubation Time:72 hoursResult:Inhibited STAT3 phosphorylation at Tyr705.

Animal Model:Mouse xenografts with SJSA or OS-33 osteosarcoma cellsDosage:5 mg/kg Administration:Intraperitoneal injection; once daily for 13 days Result:Resulted in a significant reduction in tumor volume and tumor mass in the OS-33 and SJSA xenografted mice.

LLL12 | LLL 12

JAK/STAT Signaling

STAT

STAT

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1260247-42-4

303.29

C14H9NO5S

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (329.72 mM)

O=S(C(C=CC=C1C(C2=C3C=CC=C2O)=O)=C1C3=O)(N)=O

5-hydroxy-9,10-dioxo-9,10-dihydroanthracene-1-sulfonamide

(-20℃)

With Ice Pack

≥ 2 years