A STAT3 inhibitor (IC50 = 4.7 μM for STAT3 homodimer DNA binding activity); 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

SH-4-54 – 5 mg

Brand:
Cayman
CAS:
1456632-40-8
Storage:
-20
UN-No:
De Minimis - 3077 / 9

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).{47057} 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.  

 

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SKU: 25982 - 5 mg Category:

Description

A STAT3 inhibitor (IC50 = 4.7 μM for STAT3 homodimer DNA binding activity); 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; decreases STAT3 iNOS, Survivin, and Bcl-2 promoter occupancy in MDA-MB-231 cells; 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); inhibits tumor growth in the U251MG glioma and MDA-MB-231 breast cancer mouse xenograft models at 3 mg/kg per day

Formal name: 4-[[(4-cyclohexylphenyl)methyl][2-[methyl[(2,3,4,5,6-pentafluorophenyl)sulfonyl]amino]acetyl]amino]-benzoic acid

Synonyms: 

Molecular weight: 610.6

CAS: 1456632-40-8

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors||Research Area|Cancer|Cell Signaling|JAK/STAT Signaling||Research Area|Cancer|Transcription Factors|STATs

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