SH5-07

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

SH5-07 (SH-5-07, SH 5-07) 是一种有效的、选择性的小分子 STAT3 抑制剂，IC50 为 3.9 uM。

SH5-07 (SH-5-07, SH 5-07) is a potent, selective small-molecule STAT3 inhibitor with IC50 of 3.9 uM; preferentially inhibits Stat3:Stat3 DNA-binding activity, shows no inhibition of Stat1:Stat1 or Stat5:Stat5 activity; exerts pY705 Stat3 inhibition in human glioma, breast, and prostate cancer cells, blocks STAT3-dependent gene transcription along with Bcl-2, Bcl-xL, Mcl-1, cyclin D1, c-Myc, and survivin expression; decreases the proliferation and viability of glioma, breast, and prostate cancer cells and v-Src-transformed murine fibroblasts harboring constitutively active STAT3; effectively inhibits tumor growth in mouse xenograft models of glioma and breast cancer.

SH5-07 is a hydroxamic acid analog of BP-1-102. SH5-07 dose-dependently inhibits Stat3 activity with an IC50 of 3.9±0.6 μM in in vitro assay. It preferentially inhibits Stat3:Stat3 DNA-binding activity, ahead of inhibiting Stat1:Stat3 activity, with minimal effects on Stat1:Stat1 activity. SH5-07 binds Stat3, disrupts Stat3 association with growth factor receptor, and thereby inhibits Stat3 phosphorylation. It induces antitumor cell effects against malignant cells harboring constitutively-active Stat3. SH5-07 inhibits the expression of known Stat3-regulated genes. Bcl-2, Bcl-xL, c-Myc, Survivin, Cyclin D1 and Mcl-1 expression is reduced in response to 24 h, 5 μM SH5-07 treatment.

Tail vein injection or oral gavage delivery of SH5-07 or SH4-54 inhibits growth of 90-150 mm3 established subcutaneous mouse xenografts of human glioma (U251MG) and breast (MDA-MB-231) tumors that harbor aberrantly-active Stat3, associated with decreased c-Myc, Mcl-1 and Cyclin D1 expression. No significant changes in body weights, blood cell counts, or the gross anatomy of organs, or obvious signs of toxicity are observed.

SH-5-07 | SH 5-07

JAK/STAT Signaling

STAT

STAT

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1456632-41-9

625.6068

C29H28F5N3O5S

>98% (HPLC)

DMSO: 10 mM

O=C(NO)C1=CC=C(N(CC2=CC=C(C3CCCCC3)C=C2)C(CN(C)S(=O)(C4=C(F)C(F)=C(F)C(F)=C4F)=O)=O)C=C1

Benzamide, 4-[[(4-cyclohexylphenyl)methyl][2-[methyl[(2,3,4,5,6-pentafluorophenyl)sulfonyl]amino]acetyl]amino]-N-hydroxy-

(-20℃)

With Ice Pack

≥ 2 years