A STAT3 inhibitor
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C188-9

Item No. 30928

Technical Information
Formal Name
N-(1′,2-dihydroxy[1,2′-binaphthalen]-4′-yl)-4-methoxy-benzenesulfonamide
CAS Number
432001-19-9
Molecular Formula
C27H21NO5S
Formula Weight
Purity
≥98%
Formulation
A crystalline solid
DMF: 10 mg/mlDMSO: 10 mg/mlDMSO:PBS (pH 7.2) (1:5): 0.16 mg/ml
λmax
229 nm
SMILES
OC1=C(C2=C(O)C(C=CC=C3)=C3C(NS(C4=CC=C(OC)C=C4)(=O)=O)=C2)C(C=CC=C5)=C5C=C1
InChi Code
InChI=1S/C27H21NO5S/c1-33-18-11-13-19(14-12-18)34(31,32)28-24-16-23(27(30)22-9-5-4-8-21(22)24)26-20-7-3-2-6-17(20)10-15-25(26)29/h2-16,28-30H,1H3
InChi Key
QDCJDYWGYVPBDO-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Certificates of Analysis & Batch Specific Data

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    Cayman Chemical
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    Product Description

    C188-9 is a STAT3 inhibitor.1,2 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).2,3 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.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Silva, K.A.S., Dong, J., Dong, Y., et alInhibition of Stat3 activation suppresses caspase-3 and the ubiquitin-proteasome system, leading to preservation of muscle mass in cancer cachexia. The Journal of Biological Chemisty 290(17), 11177-11187 (2015).

    2. Redell, M.S., Ruiz, M.J., Alonzo, T.A., et alStat3 signaling in acute myeloid leukemia: Ligand-dependent and -independent activation and induction of apoptosis by a novel small-molecule Stat3 inhibitor. Blood 117(21), 5701-5709 (2011).

    3. Jung, K.H., Yoo, W., Stevenson, H.L., et alMultifunctional effects of a small-molecule STAT3 inhibitor on NASH and hepatocellular carcinoma in mice. Clin. Cancer Res. 23(18), 5537-5546 (2017).