A STAT3 inhibitor
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SH-4-54

Item No. 25982

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[[(4-cyclohexylphenyl)methyl][2-[methyl[(2,3,4,5,6-pentafluorophenyl)sulfonyl]amino]acetyl]amino]-benzoic acid
CAS Number
1456632-40-8
Molecular Formula
C29H27F5N2O5S
Formula Weight
610.6
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlEthanol: 20 mg/ml
SMILES
O=C(O)C1=CC=C(N(C(CN(C)S(C2=C(F)C(F)=C(F)C(F)=C2F)(=O)=O)=O)CC3=CC=C(C4CCCCC4)C=C3)C=C1
InChi Code
InChI=1S/C29H27F5N2O5S/c1-35(42(40,41)28-26(33)24(31)23(30)25(32)27(28)34)16-22(37)36(21-13-11-20(12-14-21)29(38)39)15-17-7-9-19(10-8-17)18-5-3-2-4-6-18/h7-14,18H,2-6,15-16H2,1H3,(H,38,39)
InChi Key
VFPYGNNOSJWBHF-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

    $120

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    10 mg

    $219

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    25 mg

    $420

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    Product Description

    SH-4-54 is an inhibitor of signal transducer and activator of transcription 3 (STAT3; IC50 = 4.7 μM for STAT3 homodimer DNA binding activity).1 It selectively inhibits STAT3 homodimer over STAT1 and STAT5 homodimer and STAT3:STAT1 heterodimer DNA binding in EGF-stimulated NIH3T3/hEGFR nuclear extracts containing activated STAT1, STAT3, and STAT5 and decreases STAT3 iNOS, Survivin, and Bcl-2 promoter occupancy in MDA-MB-231 cells. SH-4-54 inhibits growth of glioma, breast, and prostate cancer cell lines that express constitutively active STAT3 (IC50s = 1-7.4, 3.8-4.5, and 5.3-5.8 μM, respectively). In vivo, SH-4-54 (3 mg/kg per day) inhibits tumor growth in the U251MG glioma and MDA-MB-231 breast cancer mouse xenograft models.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Yue, P., Lopez-Tapia, F., Paladino, D., et al. Hydroxamic acid and benzoic acid-based STAT3 inhibitors suppress human glioma and breast cancer phenotypes in vitro and in vivo. Cancer Res. 76(3), 652-663 (2016).