C188-9 - 98%, high purity , CAS No.432001-19-9, Inhibitor of signal transducer and activator of transcription 3

Item Number

C414081

• Synonyms: GTPL12268 | N-(4-hydroxy-3-(2-hydroxynaphthalen-1-yl)naphthalen-1-yl)-4-methoxybenzenesulfonamide | EX-A1961 | CS-0044737 | C 188-9 | C75162 | BCP28881 | N-(1',2-dihydroxy-[1,2'-binaphthalen]-4'-yl)-4-methoxybenzenesulfonamide | UNII-KZ3DLD11RQ | NCGC0026
• Specifications & Purity: Moligand™, ≥98%
• Biochemical and Physiological Mechanisms: C188-9 (TTI 101) is a potent inhibitor of STAT3 that binds to STAT3 with high affinity (KD=4.7±0.4 nM). C188-9 is well tolerated in mice, shows good oral bioavailability, and is concentrated in tumors.
• Storage Temp: Protected from light,Store at -20°C
• Shipped In: Ice chest + Ice pads
• Grade: Moligand™
• Action Type: INHIBITOR
• Mechanism of action: Inhibitor of signal transducer and activator of transcription 3

Product Description

Information

C188-9 (TTI 101) is a potent inhibitor ofSTAT3that binds to STAT3 with high affinity (KD=4.7±0.4 nM). C188-9 is well tolerated in mice, shows good oral bioavailability, and is concentrated in tumors.

Targets

STAT3 (Cell-free) 4.7 nM(Kd)

In vitro

C188-9 is a small-molecule inhibitor of Stat3 that targets the phosphotyrosyl peptide binding site within the Stat3 Src homology 2 (SH2) domain with Ki 136 nM. It does not inhibit upstream Jak or Src kinases.

In vivo

Treatment of nude mice bearing xenografts of UM-SCC-17B, a radioresistant HNSCC line, with C188-9, but not C188, prevented tumor xenograft growth. C188-9 was well tolerated in mice, showed good oral bioavailability, and was concentrated in tumors.

Cell Research(from reference)

Cell lines：HNSCC cell line, UM-SCC-17B 

Concentrations：0, 0.1, 0.3, 1, 3, 10, 30 μM 

Incubation Time：24 h