2. JAK/STAT Signaling Stem Cell/Wnt Apoptosis Epigenetics
  3. STAT Apoptosis DNA Methyltransferase
  4. C188-9

C188-9 (TTI-101) is a STAT3 inhibitor with a Kd value of 4.7 nM. C188-9 targets the SH2 domain of STAT3, blocks the processes of STAT3 ligand binding, receptor recruitment, homodimerization and phosphorylation, and regulates STAT3-mediated genes associated with tumorigenesis and radioresistance. C188-9 regulates STAT1-mediated genes related to radioresistance and reduces the activation level of STAT1. C188-9 downregulates the expression of DNMT1, enhances DAC-induced demethylation and re-expression of RASSF1A, and simultaneously potentiates the anti-tumor effect of DAC on pancreatic cancer cells. C188-9 inhibits both anchorage-dependent and anchorage-independent growth of cancer cells, induces Apoptosis, blocks the growth of tumor xenografts, and suppresses muscle atrophy. C188-9 maintains muscle mass, increases body weight and improves grip strength in tumor-bearing mice. C188-9 can be used in research related to head and neck squamous cell carcinoma, pancreatic cancer, sepsis-related skeletal muscle wasting, non-small cell lung cancer, acute myeloid leukemia and cancer cachexia.

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CAS No. : 432001-19-9

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고객리뷰

Based on 32 publication(s) in Google Scholar

C188-9 Related Antibodies

Top Publications Citing Use of Products

32 Publications Citing Use of MCE C188-9

WB
Cell Proliferation/Viability Assay
RT-PCR
In Vivo Efficacy Study
Histological Imaging/Staining
Cell Imaging/Staining

    C188-9 purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2025 Jan;15(1):409-423.

    Karpas299 cells were treated with C188-9 (5, 20 μM) for 4 h. STAT3 and p-STAT3 were analyzed by Western blotting.

    C188-9 purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2020 Nov 23;39(1):252.  [Abstract]

    CCK-8 and Transwell assays detecting the cell viability and invasion in circ-LRIG3-overexpressing HepG2 cells treated with C188–9.

    C188-9 purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2020 Nov 23;39(1):252.  [Abstract]

    qRT-PCR analysis of circ-LRIG3 in HepG2 and SMMC-7721 cells treated with colivelin and C188–9.

    C188-9 purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2020 Nov 23;39(1):252.  [Abstract]

    The image, volume weight of mice bearing tumors of circ-LRIG3-overexpressing cells treated with C188–9 (50 mg/kg, i.p.).

    C188-9 purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2020 Nov 23;39(1):252.  [Abstract]

    H&E and IHC staining in tumor tissues of nude mice treated with C188–9 treated with C188–9 (50 mg/kg, i.p.).

    C188-9 purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2020 Nov 23;39(1):252.  [Abstract]

    TUNEL staining in tumor tissues of nude mice treated with C188–9 treated with C188–9 (50 mg/kg, i.p.).

    View All STAT Isoform Specific Products:

    View All Isoforms
    STAT3 STAT5 STAT6 STAT1

    View All DNA Methyltransferase Isoform Specific Products:

    View All Isoforms
    DNA Methyltransferase DNMT1 DNMT3 MGMT

    • Biological Activity

    • 순도&문서

    • References

    • 고객리뷰

    제품 설명

    C188-9 (TTI-101) is a STAT3 inhibitor with a Kd value of 4.7 nM. C188-9 targets the SH2 domain of STAT3, blocks the processes of STAT3 ligand binding, receptor recruitment, homodimerization and phosphorylation, and regulates STAT3-mediated genes associated with tumorigenesis and radioresistance. C188-9 regulates STAT1-mediated genes related to radioresistance and reduces the activation level of STAT1. C188-9 downregulates the expression of DNMT1, enhances DAC-induced demethylation and re-expression of RASSF1A, and simultaneously potentiates the anti-tumor effect of DAC on pancreatic cancer cells. C188-9 inhibits both anchorage-dependent and anchorage-independent growth of cancer cells, induces Apoptosis, blocks the growth of tumor xenografts, and suppresses muscle atrophy. C188-9 maintains muscle mass, increases body weight and improves grip strength in tumor-bearing mice. C188-9 can be used in research related to head and neck squamous cell carcinoma, pancreatic cancer, sepsis-related skeletal muscle wasting, non-small cell lung cancer, acute myeloid leukemia and cancer cachexia[1][2][3][4][5][6].

    IC50 & Target[1]

    STAT3

    4.7 nM (Kd)

    STAT1

     

    DNMT1

     

    Cellular Effect
    Cell Line Type Value Description References
    AGS IC50
    9.99 μM
    Compound: TTI-101; C188-9, 1
    Antiproliferative activity against human AGS cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
    Antiproliferative activity against human AGS cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
    		[PMID: 35944386]
    GDM-1 EC50
    6 μM
    Compound: 54; C188-9
    Induction of apoptosis in human GDM-1 cells incubated for 48 hrs by Annexin V staining assay
    Induction of apoptosis in human GDM-1 cells incubated for 48 hrs by Annexin V staining assay
    		[PMID: 31810784]
    Kasumi 1 EC50
    8 μM
    Compound: 54; C188-9
    Induction of apoptosis in human Kasumi 1 cells incubated for 48 hrs by Annexin V staining assay
    Induction of apoptosis in human Kasumi 1 cells incubated for 48 hrs by Annexin V staining assay
    		[PMID: 31810784]
    MCF7 EC50
    13.75 μM
    Compound: C188-9
    Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by CyQuant assay
    Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by CyQuant assay
    		[PMID: 33352047]
    MDA-MB-231 EC50
    25.7 μM
    Compound: C188-9
    Antiproliferative activity against human MDA-MB-231 cells harbouring STAT3 assessed as reduction in cell viability at upto 10 uM incubated for 72 hrs by CyQuant assay
    Antiproliferative activity against human MDA-MB-231 cells harbouring STAT3 assessed as reduction in cell viability at upto 10 uM incubated for 72 hrs by CyQuant assay
    		[PMID: 33352047]
    MGC-803 IC50
    3.26 μM
    Compound: TTI-101; C188-9, 1
    Antiproliferative activity against human MGC-803 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
    Antiproliferative activity against human MGC-803 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
    		[PMID: 35944386]
    MKN-1 IC50
    10.21 μM
    Compound: TTI-101; C188-9, 1
    Antiproliferative activity against human MKN-1 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
    Antiproliferative activity against human MKN-1 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
    		[PMID: 35944386]
    MKN-28 IC50
    40.01 μM
    Compound: TTI-101; C188-9, 1
    Antiproliferative activity against human MKN-28 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
    Antiproliferative activity against human MKN-28 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
    		[PMID: 35944386]
    In Vitro

    C188-9 (0.1-1000 μM) potently inhibits the binding of recombinant STAT3 to its pY peptide ligand, with a calculated Ki of 12.4 nM[1].
    C188-9 binds directly to STAT3 with high affinity, with a Kd value of 4.7 nM[1].
    C188-9 (1-300 μM; 1 h) inhibits ligand-activated pSTAT3 (IC50 8.9 μM) and pSTAT1 (IC50 9.5 μM) in Kasumi-1 cells[1].
    C188-9 (48 h) potently inhibits the anchorage-dependent growth of UM-SCC-17B head and neck squamous cell carcinoma cells, with an IC50 of 3.2 μM after 48 hours of treatment[1].
    C188-9 (72 h) inhibits the anchorage-independent growth of head and neck squamous cell carcinoma cells including SCC-35, SCC-61, UM-SCC-17B and HN30. After 72 hours of treatment, its IC50 values range from 0.7 to 14.8 μM depending on the cell line[1].
    C188-9 (10 µM) acts synergistically with 1 µM DAC to potently inhibit the proliferation of pancreatic cancer cells BxPC-3 and PANC-1, and this effect is superior to that of high-dose DAC monotherapy[2].
    Pretreatment of differentiated C2C12 mouse skeletal muscle myotubes with C188-9 (10 µM; 1 h) alleviates LPS-induced myotube atrophy by inhibiting the activation of STAT3 and the ubiquitin-proteasome pathway[3].
    C188-9 (24-72 h) inhibits both anchorage-dependent and anchorage-independent proliferation of all tested non-small cell lung cancer (NSCLC) cell lines, with IC50 values ranging from 3.06 to 52.44 μM[4].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    C188-9 Related Antibodies

    Apoptosis Analysis[4]

    Cell Line: A549 (human NSCLC cell line)
    Concentration: No specific explanation
    Incubation Time: 24 h, 48 h
    Result: Increased the percentage of apoptotic A549 cells from 3.25-3.5% in untreated cells to 11.75% after 24 h incubation, and to 82.7% after 48 h incubation.
    Parmacokinetics
    Species Dose Route AUC0-∞ Plasma Concentration
    Mice[1] 10 mg/kg i.p. 12.5 μg·h/mL 1.9 mg/mL
    Mice[1] 10 mg/kg p.o. 12.5 μg·h/mL /
    In Vivo

    C188-9 (100 mg/kg; intraperitoneal injection; 5 times per week) inhibits the growth of UM-SCC-17B xenograft tumors by reducing the levels of pSTAT3 and pSTAT1 in tumors[1].
    C188-9 (100 mg/kg; i.p.; once daily; for 4 consecutive weeks) inhibits orthotopic pancreatic tumor growth in nude mice, reduces the proliferative capacity of tumor cells, decreases the formation of metastatic nodules, regulates epithelial-mesenchymal transition markers, upregulates RASSF1A expression and downregulates DNMT1 expression, without inducing significant body weight loss or hematological toxicity[2].
    C188-9 (50 mg/kg; i.p.) inhibits the activation of STAT3 and the ubiquitin-proteasome pathway, ameliorates sepsis-related skeletal muscle wasting and myasthenia symptoms in mice, and does not affect the autophagy pathway[3].
    C188-9 (i.p., 50 mg/kg, twice daily for 3 weeks) inhibits NSCLC tumor growth in athymic nude mice, reduces tumor weight by 50%, decreases tumor pSTAT3 levels by 65%, and lowers PBMC pSTAT3 levels by 25%[4].
    C188-9 (i.p.; daily; for 14 consecutive days at a dose of 12.5 mg/kg) inhibits cancer cachexia in C26 tumor-bearing CD2F1 mice by suppressing the Stat3 signaling pathway, preserving muscle mass, improving muscle function, normalizing protein turnover, and blocking caspase-3- and ubiquitin-proteasome system-mediated proteolysis[6].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: Athymic nude mice (male, 8-10 weeks old)[1]
    Dosage: 100 mg/kg
    Administration: i.p.; 5 times per week
    Result: Reduced UM-SCC-17B xenograft growth with statistically significant difference compared to control (p=0.027).
    Reduced tumor levels of pSTAT3 by 57% compared to control (p=0.017).
    Reduced tumor levels of pSTAT1 by 80% compared to control (p=0.000003).
    Altered the expression of 384 total genes in tumors, including 76 STAT3-regulated genes and 40 STAT1-regulated genes.
    Animal Model: nude mice (5-week-old, female)[2]
    Dosage: 100 mg/kg
    Administration: i.p.; once daily; 4 weeks
    Result: Reduced tumor volume relative to control group.
    Did not induce significant changes in mouse body weight or white blood cell counts relative to control group.
    Reduced tumor cell proliferation (Ki-67 staining) relative to control group.
    Lowered number of metastatic nodules relative to control group.
    Increased E-cadherin expression in tumor tissue relative to control group.
    Reduced Vimentin, N-cadherin, and Snail1 expression in tumor tissue relative to control group.
    Elevated RASSF1A protein and mRNA expression in tumor tissue relative to control group.
    Reduced DNMT1 protein expression in tumor tissue relative to control group.
    Animal Model: C57BL/6 (male, 8-10 weeks old, 22-26 g)[3]
    Dosage: 50 mg/kg
    Administration: i.p.
    Result: Did not affect acute-phase mortality or appetite loss.
    Significantly reversed sepsis-induced tibialis anterior (TA) muscle atrophy.
    Restored forelimb grip strength.
    Reduced the murine sepsis score at 1 and 3 days post-treatment.
    Rescued sepsis-induced TA muscle fiber shrinkage via immunofluorescence staining.
    Suppressed sepsis-induced activation of phosphorylated STAT3 (Tyr705) and downstream ubiquitin ligase proteins atrogin-1/MAFbx and MuRF1 in TA muscles.
    Did not alter plasma or muscle IL-6/TNF-α levels, or autophagy pathway markers (LC3B-II/LC3B-I ratio, LC3B puncta).
    Animal Model: CD2F1 (female, 8-10 weeks of age, subcutaneous inoculation of isogenic C26 colon carcinoma cells)[6]
    Dosage: 12.5 mg/kg
    Administration: i.p.; daily; 14 days
    Result: Suppressed muscle p-Stat3 activation, and reduced muscle expression of C/EBP-δ and myostatin.
    Increased body weight relative to diluent-treated tumor-bearing mice, and preserved mass of tibialis anterior, extensor digitorum longus, gastrocnemius, and soleus muscles.
    Maintained myofiber size distribution similar to non-tumor-bearing control mice.
    Improved muscle grip strength.
    Increased protein synthesis in soleus and extensor digitorum longus muscles.
    Decreased protein degradation in soleus and extensor digitorum longus muscles.
    Blocked the tumor-induced increase in 14-kDa actin fragment (a marker of caspase-3-mediated proteolysis).
    Reduced tumor-induced elevations in muscle MAFbx/Atrogin-1 and MuRF-1 mRNA and protein levels.
    Suppressed tumor-induced increases in proteasome activity.
    Clinical Trial
    분자량

    471.52

    화학식

    C27H21NO5S
    CAS No.
    Appearance

    Solid

    Color

    Light brown to gray

    SMILES

    O=S(C1=CC=C(OC)C=C1)(NC2=C3C=CC=CC3=C(O)C(C4=C5C=CC=CC5=CC=C4O)=C2)=O
    선적

    Room temperature in continental US; may vary elsewhere.
    보관

    4°C, protect from light

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

    용액&용해도
    In Vitro: 

    DMSO : 25 mg/mL (53.02 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.1208 mL 10.6040 mL 21.2080 mL
    5 mM 0.4242 mL 2.1208 mL 4.2416 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • 몰농도 계산기

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    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

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    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.08 mg/mL (4.41 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    In Vivo Dissolution Calculator
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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
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    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    순도&문서

    Purity: 99.84%

    SDS (394 KB)

    COA (256 KB) HNMR (271 KB) LCMS (270 KB) Elemental Analysis Report (114 KB)

    Handling Instructions (2659 KB)
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.1208 mL 10.6040 mL 21.2080 mL 53.0200 mL
    5 mM 0.4242 mL 2.1208 mL 4.2416 mL 10.6040 mL
    10 mM 0.2121 mL 1.0604 mL 2.1208 mL 5.3020 mL
    15 mM 0.1414 mL 0.7069 mL 1.4139 mL 3.5347 mL
    20 mM 0.1060 mL 0.5302 mL 1.0604 mL 2.6510 mL
    25 mM 0.0848 mL 0.4242 mL 0.8483 mL 2.1208 mL
    30 mM 0.0707 mL 0.3535 mL 0.7069 mL 1.7673 mL
    40 mM 0.0530 mL 0.2651 mL 0.5302 mL 1.3255 mL
    50 mM 0.0424 mL 0.2121 mL 0.4242 mL 1.0604 mL
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    C188-9 Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    C188-9432001-19-9TTI-101TTI101TTI 101STATApoptosisDNA MethyltransferaseDNMTsDNA MTasesSH2 domainSTAT3Kasumi-1 cellsacute myeloid leukemiaSTAT1RASSF1Ahead and neck squamous cell carcinomanon-small cell lung cancerpancreatic cancer cellsDNMT1Inhibitorinhibitorinhibit

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    Cat. No.:
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