TPCA-1
Based on 43 publication(s) in Google Scholar
TPCA-1 is a potent and selective inhibitor of IKK-2 with IC50 of 17.9 nM. TPCA-1 is an effective inhibitor of STAT3 phosphorylation, DNA binding, and transactivation.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.75%
- No. CAS: 507475-17-4
- Fòrmula: C12H10FN3O2S
- Peso molecular:279.29
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) TPCA-1
More- Signal Transduct Target Ther. 2021 Apr 24;6(1):167. [Abstract]
- Cancer Cell. 2026 May 21:S1535-6108(26)00220-5.
- Cancer Cell. 2024 May 13;42(5):850-868.e9. [Abstract]
- Cell Stem Cell. 2025 Aug 7;32(8):1235-1250.e6. [Abstract]
- Cell Mol Immunol. 2023 Oct;20(10):1203-1215. [Abstract]
- ACS Nano. 2015 Dec 22;9(12):11800-11. [Abstract]
- Nat Commun. 2025 Aug 21;16(1):7689. [Abstract]
- Nat Commun. 2024 Dec 3;15(1):10526. [Abstract]
- Nat Commun. 2024 May 7;15(1):3805. [Abstract]
- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- J Clin Invest. 2025 Oct 7:e193945. [Abstract]
- Pharmacol Res. 2020 Jul;157:104800. [Abstract]
- Cell Death Dis. 2021 Oct 23;12(11):994. [Abstract]
- Cell Death Dis. 2018 Apr 27;9(5):500. [Abstract]
- Cell Death Dis. 2016 Dec 1;7(12):e2505. [Abstract]
- Proc Natl Acad Sci U S A. 2019 Feb 19;116(8):2996-3005. [Abstract]
- Cell Death Discov. 2025 Jul 25;11(1):345. [Abstract]
- Cell Rep. 2023 Jan 31;42(1):112027. [Abstract]
- Anal Chem. 2022 Mar 22;94(11):4695-4702. [Abstract]
- Sci Signal. 2024 May 14;17(836):eadd5073. [Abstract]
- Cancer Cell Int. 2021 Jun 5;21(1):291. [Abstract]
- Int J Mol Med. 2022 Jun;49(6):75. [Abstract]
- J Invest Dermatol. 2022 Oct;142(10):2591-2602.e8. [Abstract]
- Pharmaceutics. 2023 Oct 9;15(10):2435. [Abstract]
- Inflamm Res. 2026 Jun 11;75(1):137. [Abstract]
- Inflammation. 2025 Apr;48(2):820-838. [Abstract]
- Biol Direct. 2024 Jun 21;19(1):48. [Abstract]
- Int J Mol Sci. 2023 Feb 14;24(4):3810. [Abstract]
- Int Immunopharmacol. 2024 Sep 7;142(Pt A):113074. [Abstract]
- Inflamm Bowel Dis. 2023 Jun 10;izad105. [Abstract]
- J Biotechnol. 2025 Mar:399:9-18. [Abstract]
- Aging (Albany NY). 2021 Sep 8;13(17):21547-21570. [Abstract]
- Cell Signal. 2025 Jun 25:111962. [Abstract]
- Exp Cell Res. 2021 Feb 15;399(2):112468. [Abstract]
- J Sci Food Agric. 2019 Mar 30;99(5):2329-2339. [Abstract]
- J Immunol. 2016 May 15;196(10):4322-30. [Abstract]
- PLoS One. 2022 Nov 29;17(11):e0278220. [Abstract]
- bioRxiv. 2026 Mar 31.
- Res Sq. 2026 Jan 9.
- University of Toronto. 2025.
- University of Bonn. 2025.
- SSRN. 2023 Jun 29.
- SSRN. 2023 Jul 10.
Customer Validation & Images
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Cell Proliferation/Viability Assay
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Cell Proliferation/Viability Assay
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WB
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WB
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Cell Proliferation/Viability Assay
Actividad biológica
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IKK-2 17.9 nM (IC50) |
STAT3 |
TPCA-1 inhibits lipopolysaccharide-induced human monocyte production of TNF-α, IL-6, and IL-8 with an IC50 of 170 to 320 nM[1][2].
TPCA-1 (0-2 μM) inhibits STAT3 phosphorylation and transactivation induced by cytokines and nonreceptor tyrosine kinase in dose- and time-dependent manner. TPCA-1 completely inhibits STAT3 phosphorylation without changing total STAT3 levels[3].
TPCA-1 increased sensitivity to ZD1839 in both TKI sensitive cells and insensitive cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human peripheral blood monocytes stimulated with LPS.
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Concentration:0-10 μM.
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Incubation Time:~24 hours.
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Result:TPCA-1 Inhibits LPS-Induced TNF-α, IL-6, and IL-8 production by human monocytes.
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Cell Line:HCC827 and H1975 cells.
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Concentration:0-10 μM.
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Incubation Time:0.5-2 hours.
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Result:Suppressed proliferation of HCC827 and H1975 cells.
Led to a G2-M cell-cycle arrest in HCC827 but not A549.
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Cell Line:HEK-293T cell lines.
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Concentration:0-2 μM (before IL-2 or IFN-α treatment).
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Incubation Time:0.5-2 hours.
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Result:Inhibited STAT3 phosphorylation and transactivation induced by cytokines and nonreceptor tyrosine kinase in dose- and time-dependent manner.
TPCA-1(10 mg/kg, i.p. daily) inhibits growth of NSCLC with EGFR mutation and potentiates antitumor effect of ZD1839 in xenograft models[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:10-12 weeks old male DBA/1 OlaHsd mice[2].
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Dosage:3, 10, or 20 mg/kg.
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Administration:I.P., b.i.d, from days 1 to 47.
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Result:Reduced the severity and delays the onset of CIA.
Attenuated ex vivo antigen-induced T cell proliferation in CIA.
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Animal Model:Six-week-old BALB/c female nude mice injected subcutaneously with HCC827 cells (5×106)[3].
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Dosage:10 mg/kg.
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Administration:Intraperitoneally daily.
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Result:The tumor weight inhibition rate of TPCA-1, ZD1839, and their combination are 0.419(ETPCA-1), 0.680(EZD1839), and 0.837(Eobserved), respectively.
Chemical Information
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No. CAS 507475-17-4
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Appearance Solid
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Peso molecular 279.29
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Fòrmula C12H10FN3O2S
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Color White to gray
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SMILES
O=C(C1=C(NC(N)=O)SC(C2=CC=C(F)C=C2)=C1)N
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (43)
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Journal Impact Factor
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Most Recent
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Signal Transduct Target Ther
RNA-induced liquid phase separation of SARS-CoV-2 nucleocapsid protein facilitates NF-κB hyper-activation and inflammation. [Abstract]2021 Apr 24;6(1):167. PMID: 33895773 -
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Cancer Cell
2024 May 13;42(5):850-868.e9. PMID: 38670091
TPCA-1 purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2024 May 13;42(5):850-868.e9. [Abstract]
Cell viability assays of Eμ-Myc lymphoma cell lines treated with ADU-S100 (HY-12885A; AH15A/560: 0.5 μg/mL; 47A: 5 μg/mL) and/or TPCA-1 (HY-10074) for 24 h. Error bars represent SD for three independent experiments. Diagram illustrates how TPCA-1 acts to inhibit NF-κB signaling.
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Cell Stem Cell
Bacterial ADP-heptose triggers stem cell regeneration in the intestinal epithelium following injury. [Abstract]2025 Aug 7;32(8):1235-1250.e6. PMID: 40651470 -
Cell Mol Immunol
2023 Oct;20(10):1203-1215. PMID: 37591930 -
ACS Nano
Neutrophil-Mediated Delivery of Therapeutic Nanoparticles across Blood Vessel Barrier for Treatment of Inflammation and Infection. [Abstract]2015 Dec 22;9(12):11800-11. PMID: 26516654
TPCA-1 purchased from MedChemExpress. Usage Cited in: ACS Nano. 2015 Dec 22;9(12):11800-11. [Abstract]
Neutrophil-mediated delivery of TPCA-1 mitigates acute lung inflammation/injury. Numbers of leukocytes and neutrophils, concentrations of IL-6 in BALF 20 h after iv injection of vehicle of TPCA-1 solution, 5% glucose, TPCA-1 solution or TPAC-1 BSA NPs in mice 4 h after LPS challenge (8 mg/kg).
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Nat Commun
Small round cell sarcoma tumoroid biobank reveals CIC::DUX4 sarcoma vulnerability to MCL-1 inhibition. [Abstract]2025 Aug 21;16(1):7689. PMID: 40841360 -
Nat Commun
Dual rectification of metabolism abnormality in pancreatic cancer by a programmed nanomedicine. [Abstract]2024 Dec 3;15(1):10526. PMID: 39627234 -
Nat Commun
FGFR inhibition blocks NF-ĸB-dependent glucose metabolism and confers metabolic vulnerabilities in cholangiocarcinoma. [Abstract]2024 May 7;15(1):3805. PMID: 38714664 -
Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
J Clin Invest
IL-17-producing γδ T cells in the tumor microenvironment promote radioresistance in mice. [Abstract]2025 Oct 7:e193945. PMID: 41055972 -
Pharmacol Res
CCL22 signaling contributes to sorafenib resistance in hepatitis B virus-associated hepatocellular carcinoma. [Abstract]2020 Jul;157:104800. PMID: 32278046 -
Cell Death Dis
Quantitative analysis of phosphoproteome in necroptosis reveals a role of TRIM28 phosphorylation in promoting necroptosis-induced cytokine production. [Abstract]2021 Oct 23;12(11):994. PMID: 34689152 -
Cell Death Dis
Necroptosis promotes cell-autonomous activation of proinflammatory cytokine gene expression. [Abstract]2018 Apr 27;9(5):500. PMID: 29703889
TPCA-1 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2018 Apr 27;9(5):500. [Abstract]
Western blotting analysis of lysates from 3×HA-IκBα-expressing HT-29 cells treated as indicated for 8 h.
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Cell Death Dis
2016 Dec 1;7(12):e2505. PMID: 27906189 -
Proc Natl Acad Sci U S A
2019 Feb 19;116(8):2996-3005. PMID: 30718432
TPCA-1 purchased from MedChemExpress. Usage Cited in: Proc Natl Acad Sci U S A. 2019 Feb 19;116(8):2996-3005. [Abstract]
HT22 cells were pretreated with the indicated inhibitors (CDDO (Bardoxolone, HY-14909); T0070907 (HY-13202); Troglitazone (HY-50935 ); TPCA-1 (HY-10074); JAKi; STAT3i; AV-412 (HY-10346); and MK2206 (HY-10358)) and then treated with T/Z, T/S/Z, T/C/Z for 9 h or Glutamate, Erastin (T: 20 ng/ml; Z: 50 μM; S: 20 nM; C: 1 μg/ml; Glutamate: 50 mM; Erastin 10 μM) for 12 h. Cell viability was measured by CellTiterGlo assay.
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Cell Death Discov
RIPK1 S213E mutant suppresses RIPK1-dependent cell death by preventing interactions with RIPK3 and CASP8. [Abstract]2025 Jul 25;11(1):345. PMID: 40715038 -
Cell Rep
Oxidized mC modulates synthetic lethality to PARP inhibitors for the treatment of leukemia. [Abstract]2023 Jan 31;42(1):112027. PMID: 36848231 -
Anal Chem
Metal-Enhanced Aggregation-Induced Emission Strategy for the HIV-I RNA-Binding Ligand Assay. [Abstract]2022 Mar 22;94(11):4695-4702. PMID: 35258935 -
Sci Signal
Protein phosphatase 6 activates NF-κB to confer sensitivity to MAPK pathway inhibitors in KRAS- and BRAF-mutant cancer cells. [Abstract]2024 May 14;17(836):eadd5073. PMID: 38743809 -
Cancer Cell Int
Construction of a prognostic model with histone modification-related genes and identification of potential drugs in pancreatic cancer. [Abstract]2021 Jun 5;21(1):291. PMID: 34090418 -
Int J Mol Med
Transcriptome‑based drug repositioning identifies TPCA‑1 as a potential selective inhibitor of esophagus squamous carcinoma cell viability. [Abstract]2022 Jun;49(6):75. PMID: 35417037 -
J Invest Dermatol
Advanced Glycation End Products Promote Melanogenesis by Activating NLRP3 Inflammasome in Human Dermal Fibroblasts. [Abstract]2022 Oct;142(10):2591-2602.e8. PMID: 35421403 -
Pharmaceutics
Enhancing the Treatment of Uncontrolled Inflammation through the Targeted Delivery of TPCA-1-Loaded Nanoparticles. [Abstract]2023 Oct 9;15(10):2435. PMID: 37896195 -
Inflamm Res
Lactate acts as a metabolic brake on inflammation by repressing NLRP3 transcription via NF-κB inhibition. [Abstract]2026 Jun 11;75(1):137. PMID: 42274732 -
Inflammation
Sodium Houttuyfonate Ameliorates DSS-induced Colitis Aggravated by Candida albicans through Dectin-1/NF-κB/miR-32-5p/NFKBIZ Axis Based on Intestinal microRNA Profiling. [Abstract]2025 Apr;48(2):820-838. PMID: 38963571 -
Biol Direct
PNSC928, a plant-derived compound, specifically disrupts CtBP2-p300 interaction and reduces inflammation in mice with acute respiratory distress syndrome. [Abstract]2024 Jun 21;19(1):48. PMID: 38902802 -
Int J Mol Sci
Dual Role of Interleukin-20 in Different Stages of Osteoclast Differentiation and Its Osteoimmune Regulation during Alveolar Bone Remodeling. [Abstract]2023 Feb 14;24(4):3810. PMID: 36835229 -
Int Immunopharmacol
IL-8 promotes lens capsular residual cells migration by down-regulates expression of E-cadherin and ZO-1 via the CXCR1/2-NF-κB-RhoA signal pathway. [Abstract]2024 Sep 7;142(Pt A):113074. PMID: 39244903 -
Inflamm Bowel Dis
Pro-inflammatory Cytokines Promote the Occurrence and Development of Colitis-associated Colorectal Cancer by Inhibiting miR-615-5p. [Abstract]2023 Jun 10;izad105. PMID: 37300504 -
J Biotechnol
2025 Mar:399:9-18. PMID: 39824361 -
Aging (Albany NY)
2021 Sep 8;13(17):21547-21570. PMID: 34495872 -
Cell Signal
Ubiquitin-editing enzyme A20 protects the inflammatory injury of human corneal epithelial cells against lipoteichoic acid. [Abstract]2025 Jun 25:111962. PMID: 40578588 -
Exp Cell Res
Continuous NF-κB pathway inhibition promotes expansion of human phenotypical hematopoietic stem/progenitor cells through metabolism regulation. [Abstract]2021 Feb 15;399(2):112468. PMID: 33428903 -
J Sci Food Agric
Ginkgo biloba sarcotesta polysaccharide inhibits inflammatory responses through suppressing both NF-κB and MAPK signaling pathway. [Abstract]2019 Mar 30;99(5):2329-2339. PMID: 30338529 -
J Immunol
Complex Regulation Pattern of IRF3 Activation Revealed by a Novel Dimerization Reporter System. [Abstract]2016 May 15;196(10):4322-30. PMID: 27045107
TPCA-1 purchased from MedChemExpress. Usage Cited in: J Immunol. 2016 May 15;196(10):4322-30. [Abstract]
HEK293T (IRF3-BiLC) cells are pretreated with TPCA-1 for 1 h, stimulated with TNF-α for 12 h, and then transfected with poly(I:C) for 12 h, after which IRF3-BiLC luciferase activity is measured.
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PLoS One
Interleukin-1β triggers matrix metalloprotease-3 expression through p65/RelA activation in melanoma cells. [Abstract]2022 Nov 29;17(11):e0278220. PMID: 36445856 -
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Solvente y solubilidad
DMSO : ≥ 100 mg/mL (358.05 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 7.5 mg/mL (26.85 mM); Clear solution
This protocol yields a clear solution of ≥ 7.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (75.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 7.5 mg/mL (26.85 mM); Clear solution
This protocol yields a clear solution of ≥ 7.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (75.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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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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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureza y Documentación
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Ficha de datos (282 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Sachse F, et al. IKK-2 inhibitor TPCA-1 represses nasal epithelial inflammation in vitro.Rhinology. 2011 Jun;49(2):168-73. [Content Brief]
[2]. Podolin PL, et al. Attenuation of murine collagen-induced arthritis by a novel, potent, selective small molecule inhibitor of IkappaB Kinase 2, TPCA-1 (2-[(aminocarbonyl)amino]-5-(4-fluorophenyl)-3-thiophenecarboxamide), occurs via reduction of proinflamm [Content Brief]
[3]. Nan J, et al. TPCA-1 is a direct dual inhibitor of STAT3 and NF-κB and regresses mutant EGFR-associated human non-small cell lung cancers. Mol Cancer Ther. 2014 Mar;13(3):617-29. [Content Brief]
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.5805 mL | 17.9025 mL | 35.8051 mL | 89.5127 mL |
| 5 mM | 0.7161 mL | 3.5805 mL | 7.1610 mL | 17.9025 mL | |
| 10 mM | 0.3581 mL | 1.7903 mL | 3.5805 mL | 8.9513 mL | |
| 15 mM | 0.2387 mL | 1.1935 mL | 2.3870 mL | 5.9675 mL | |
| 20 mM | 0.1790 mL | 0.8951 mL | 1.7903 mL | 4.4756 mL | |
| 25 mM | 0.1432 mL | 0.7161 mL | 1.4322 mL | 3.5805 mL | |
| 30 mM | 0.1194 mL | 0.5968 mL | 1.1935 mL | 2.9838 mL | |
| 40 mM | 0.0895 mL | 0.4476 mL | 0.8951 mL | 2.2378 mL | |
| 50 mM | 0.0716 mL | 0.3581 mL | 0.7161 mL | 1.7903 mL | |
| 60 mM | 0.0597 mL | 0.2984 mL | 0.5968 mL | 1.4919 mL | |
| 80 mM | 0.0448 mL | 0.2238 mL | 0.4476 mL | 1.1189 mL | |
| 100 mM | 0.0358 mL | 0.1790 mL | 0.3581 mL | 0.8951 mL |
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