A STAT3 inhibitor; binds to the STAT3 SH2 domain (Ki = 136 nM) and inhibits G-CSF-induced activation of STAT3 in patient-derived AML cells (IC50s = 8-18 µM); induces apoptosis in patient-derived AML cells (EC50s = 6-50 µM); reduces viability of HepG2

C188-9 – 50 mg

Brand:
Cayman
CAS:
432001-19-9
Storage:
-20
UN-No:
Non-Hazardous - /

C188-9 is a STAT3 inhibitor.{59189,59190} It binds to the phosphotyrosyl peptide binding site in the STAT3 Src homology 2 (SH2) domain (Ki = 136 nM) and inhibits G-CSF-induced activation of STAT3 in patient-derived acute myeloid leukemia (AML) cells (IC50s = 8-18 µM). C188-9 induces apoptosis in patient-derived AML cells (EC50s = 6-50 µM) and reduces viability of HepG2, Huh7, and PLC/PRF/5 hepatoma cells (IC50s = 10.19, 11.27, and 11.83 µM, respectively).{59190,59191} In vivo, C188-9 (100 mg/kg) reduces hepatic Pten deletion-induced hepatic macro- and microsteatosis, which reduces the development of hepatocellular carcinomas in mice. C188-9 (12.5 mg/kg) increases muscle fiber size in a murine Lewis lung carcinoma model of cancer cachexia.{59189}  

 

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Description

A STAT3 inhibitor; binds to the STAT3 SH2 domain (Ki = 136 nM) and inhibits G-CSF-induced activation of STAT3 in patient-derived AML cells (IC50s = 8-18 µM); induces apoptosis in patient-derived AML cells (EC50s = 6-50 µM); reduces viability of HepG2, Huh7, and PLC/PRF/5 hepatoma cells (IC50s = 10.19, 11.27, and 11.83 µM, respectively); reduces hepatic Pten deletion-induced hepatic macro- and microsteatosis which reduces the development of hepatocellular carcinomas in mice at 100 mg/kg; increases muscle fiber size in a murine Lewis lung carcinoma model of cancer cachexia at 12.5 mg/kg

Formal name: N-(1′,2-dihydroxy[1,2′-binaphthalen]-4′-yl)-4-methoxy-benzenesulfonamide

Synonyms: 

Molecular weight: 471.5

CAS: 432001-19-9

Purity: ≥98%

Formulation: A crystalline solid

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