C188-9

SKU: orb1302682

Description

C188-9 (TTI-101) is a potent small molecule inhibitor of Signal Transducer and Activator of Transcription 3 (Stat3), exhibiting an IC50 in the range of 4-7 μM. It is widely used in research to investigate Stat3-dependent signaling in cancer and inflammatory diseases, with applications in both in vitro cellular assays and in vivo animal models.

Research Area

Cell Biology, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 432001-19-9
• MW: 471.52
• Purity: 99.19%
• Formula: C₂₇H₂₁NO₅S
• SMILES: COc1ccc(cc1)S(=O)(=O)Nc1cc(c(O)c2ccccc12)-c1c(O)ccc2ccccc12
• Target: STAT,Apoptosis
• Solubility: DMSO:262.5 mg/mL (556.71 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:6 mg/mL (12.72 mM)

Bioactivity

• Target IC50:
  STAT3:4-7 μM
• In Vivo:
  In an analysis of approximately 13,528 discernible genes, C188 influences the expression of 37 gene transcripts (17 downregulated and 20 upregulated, false discovery rate (fdr)<0.01, fold change≥1.5), including 7 known targets of STAT3. Conversely, C188-9 exhibits a broader impact, modifying the expression of 384 genes related to oncogenesis (95 down- and 289 up-regulated), 76 of which are regulated by STAT3 (38 down-regulated and 38 up-regulated). Notably, C188-9 treatment downregulates 24 out of 38 genes (63%) previously identified as upregulated by STAT3. Furthermore, C188-9 downregulates an additional 10 genes (fdr <0.01, fold change≥1.5) known to be upregulated by STAT1, suggesting that 83.3% (40 out of 48) of the genes downregulated by C188-9 are positively regulated by STAT1. This includes sixteen genes co-regulated by both STAT3 and STAT1. The findings suggest that C188-9's modulation of gene transcript levels in head and neck squamous cell carcinoma (HNSCC) tumors may be attributed to its dual influence on STAT3 and STAT1 pathways.
• In Vitro:
  For apoptosis studies, AML cell lines and primary samples are treated for 24 hours with C188-9, then apoptotic cells are quantified by FACS analysis for annexin V-labeled cells. The EC50s for apoptosis induction are quite variable, ranging from 6 μM to over 50 μM

Storage & Handling

• Storage: store under nitrogen | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Apoptosis, C188 9, C1889, C-188-9, C188-9, Inhibitor, inhibit, STAT3, STAT, TTI 101, TTI101, TTI-101

Compound Identifiers

PubChem CID

1324494