C188-9

Catalog No.S8605 Batch:S860501

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Technical Data

Formula

C27H21NO5S
Molecular Weight 471.52 CAS No. 432001-19-9
Solubility (25°C)* In vitro DMSO 94 mg/mL (199.35 mM)
Ethanol 6 mg/mL (12.72 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description 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.
Targets
STAT3 [1]
(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[1].
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[2].

Protocol (from reference)

Cell Assay:

[2]
  • Cell lines

    HNSCC cell line, UM-SCC-17B

  • Concentrations

    0, 0.1, 0.3, 1, 3, 10, 30 μM

  • Incubation Time

    24 h

  • Method

    UM-SCC-17B cells were incubated with various doses (0/0.1/0.3/1/3/10/30μM) of C188 or C188-9 for 24 hrs.
Animal Study:

[1]
  • Animal Models

    CD2F1 female mice received isogenic C26 tumor cell via s.c injection

  • Dosages

    12.5 mg/kg

  • Administration

    i.p.

Customer Product Validation

Data from [Data independently produced by , , Cells, 2018, 7(8)]

Selleck's C188-9 has been cited by 58 publications

Macrophage biomimetic nanoparticle-targeted functional extracellular vesicle micro-RNAs revealed via multiomics analysis alleviate sepsis-induced acute lung injury [ J Nanobiotechnology, 2024, 22(1):362] PubMed: 38910259
IL-27 disturbs lipid metabolism and restrains mitochondrial activity to inhibit γδ T17 cell-mediated skin inflammation [ Cell Death Dis, 2024, 15(7):491] PubMed: 38982043
The pro-inflammatory cytokines IL-1β and IL-6 promote upregulation of the ST6GAL1 sialyltransferase in pancreatic cancer cells [ J Biol Chem, 2024, S0021-9258(24)02253-1] PubMed: 39260693
EBV + B cell-derived exosomes promote EBV-associated T/NK-cell lymphoproliferative disease immune evasion by STAT3/IL-10/PD-L1 pathway [ Immunol Res, 2024, 10.1007/s12026-024-09531-3] PubMed: 39164446
Targeting FLT3-TAZ signaling to suppress drug resistance in blast phase chronic myeloid leukemia [ Mol Cancer, 2023, 10.1186/s12943-023-01837-4] PubMed: 37932786
FGF19-Induced Inflammatory CAF Promoted Neutrophil Extracellular Trap Formation in the Liver Metastasis of Colorectal Cancer [ Adv Sci (Weinh), 2023, 10(24):e2302613] PubMed: 37345586
Transcriptional and chromatin profiling of human blood innate lymphoid cell subsets sheds light on HIV-1 pathogenesis [ EMBO J, 2023, e114153.] PubMed: 37382276
Inhibiting the glycerophosphodiesterase EDI3 in ER-HER2+ breast cancer cells resistant to HER2-targeted therapy reduces viability and tumour growth [ J Exp Clin Cancer Res, 2023, 42(1):25] PubMed: 36670508
JAK-STAT Signaling in Inflammatory Breast Cancer Enables Chemotherapy-Resistant Cell States [ Cancer Res, 2023, 83(2):264-284] PubMed: 36409824
Hedgehog receptors exert immune-surveillance roles in the epidermis across species [ Cell Rep, 2023, 42(8):112929] PubMed: 37527037

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.