STAT3-IN-13

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

STAT3-IN-13 (compound 6f) 是一种有效的 STAT3 抑制剂。STAT3-IN-13 具有抗增殖作用，并以 0.46 μM 的KD 值与 STAT3 SH2 结构域结合。STAT3-IN-13 抑制 STAT3 Y705 的磷酸化和下游靶基因表达。STAT3-IN-13 在体外诱导细胞凋亡 (apoptosis)，在体内抑制肿瘤的生长和转移。STAT3-IN-13 可用于癌症研究。

STAT3-IN-13 (compound 6f) is a potent STAT3 inhibitor. STAT3-IN-13 has anti-proliferative effects and binds to the STAT3 SH2 domain with a KD of 0.46 μM. STAT3-IN-13 inhibits the phosphorylation of STAT3 Y705 and downstream target gene expression. STAT3-IN-13 induces apoptosis in vitro and suppresses the growth and metastasis of tumor in vivo. STAT3-IN-13 can be used for cancer research.

STAT3-IN-13 (compound 6f) (48 hours) has anti-proliferative activity with IC50 values of 0.25, 0.11 and 0.55 μM for 143B, HOS and MG63 cells, respectively.STAT3-IN-13 (compound 6f) (0.001-100 μM) binds to STAT3 and interacts with STAT3586?685 in a concentration dependent manner with a KD of 0.96 μM.STAT3-IN-13 (compound 6f) (0-1.0 μM; 24 hours; 143B and HOS cells) inhibits STAT3 Y705 phosphorylation and suppresses STAT3 in tumor cells.STAT3-IN-13 (compound 6f) (0-1.0 μM; 48 hours; 143B cells) induces apoptosis in a dose-dependent manner.Apoptosis Analysis Cell Line:143B cells Concentration:0, 0.2, 0.5, and 1 μM Incubation Time:48 hours Result:Increased the percentage of apoptosis rates of 3.4%, 8.7%, 10.7%, and 23.3% at 0, 0.2, 0.5 and 1 μM, respectively. Western Blot Analysis Cell Line:143B and HOS cells Concentration:0, 0.2, 0.5 and 1.0 μM Incubation Time:24 hours Result:Inhibited STAT3 Y705 phosphorylation and downstream target gene expression including Bcl-2 and VEGF, retained good antitumor activities against control tumor cells without STAT3 knockdown.

STAT3-IN-13 (compound 6f) (10-20 mg/kg; i.p.; twice daily, for 4 weeks; nude mice) blocks osteosarcoma growth and metastasis in vivo.Animal Model:Nude mice Dosage:10 and 20 mg/kg Administration:Intraperitoneal injection; twice daily, for 4 weeks Result:Suppressed tumor weight at a dose of 10 mg/kg.

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JAK/STAT Signaling

STAT

STAT

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2248552-86-3

436.49

C21H20N6O3S

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 125 mg/mL (286.38 mM; 超声助溶 )

C(#N)C=1C2=C(SC1NC(=O)C=3C=NN(C)C3)CN(C(NC4=CC=C(OC)C=C4)=O)CC2

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(-20℃)

With Ice Pack

≥ 2 years