1. NF-κB
    Stem Cell/Wnt
    JAK/STAT Signaling
    Apoptosis
  2. IKK
    STAT
    Apoptosis
  3. TPCA-1

TPCA-1 

Cat. No.: HY-10074 Purity: 99.54%
Handling Instructions

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.

For research use only. We do not sell to patients.

TPCA-1 Chemical Structure

TPCA-1 Chemical Structure

CAS No. : 507475-17-4

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 101 In-stock
Estimated Time of Arrival: December 31
5 mg USD 92 In-stock
Estimated Time of Arrival: December 31
10 mg USD 172 In-stock
Estimated Time of Arrival: December 31
100 mg USD 594 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 11 publication(s) in Google Scholar

Top Publications Citing Use of Products

    TPCA-1 purchased from MCE. Usage Cited in: ACS Nano. 2015 Dec 22;9(12):11800-11.

    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).

    TPCA-1 purchased from MCE. Usage Cited in: J Immunol. 2016 May 15;196(10):4322-30.

    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.

    TPCA-1 purchased from MCE. Usage Cited in: Cell Death Dis. 2018 Apr 27;9(5):500.

    Western blotting analysis of lysates from 3×HA-IκBα-expressing HT-29 cells treated as indicated for 8 h.

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    Description

    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.

    IC50 & Target[3]

    IKK-2

    17.9 nM (IC50)

    STAT3

     

    In Vitro

    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].

    Cell Viability Assay[2]

    Cell Line: human peripheral blood monocytes stimulated with LPS.
    Concentration: 0-10 μM.
    Incubation Time: ~24 hours.
    Result: TPCA-1 Inhibits LPS-Induced TNF-α, IL-6, and IL-8 production by human monocytes.

    Cell Viability Assay[3]

    Cell Line: HCC827 and H1975 cells.
    Concentration: 0-10 μM.
    Incubation Time: 0.5-2 hours.
    Result: Suppressed proliferation of HCC827 and H1975 cells.
    Led to a G2-M cell-cycle arrest in HCC827 but not A549.

    Western Blot Analysis[3]

    Cell Line: HEK-293T cell lines.
    Concentration: 0-2 μM (before IL-2 or IFN-α treatment).
    Incubation Time: 0.5-2 hours.
    Result: Inhibited STAT3 phosphorylation and transactivation induced by cytokines and nonreceptor tyrosine kinase in dose- and time-dependent manner.
    In Vivo

    TPCA-1 (3, 10, or 20 mg/kg, i.p.) results in a dose-dependent reduction in the severity of murine collagen-induced arthritis (CIA)[2].
    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].

    Animal Model: 10-12 weeks old male DBA/1 OlaHsd mice[2].
    Dosage: 3, 10, or 20 mg/kg.
    Administration: I.P., b.i.d, from days 1 to 47.
    Result: Reduced the severity and delays the onset of CIA.
    Attenuated ex vivo antigen-induced T cell proliferation in CIA.
    Animal Model: Six-week-old BALB/c female nude mice injected subcutaneously with HCC827 cells (5×106)[3].
    Dosage: 10 mg/kg.
    Administration: Intraperitoneally daily.
    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.
    Molecular Weight

    279.29

    Formula

    C₁₂H₁₀FN₃O₂S

    CAS No.

    507475-17-4

    SMILES

    O=C(C1=C(NC(N)=O)SC(C2=CC=C(F)C=C2)=C1)N

    Shipping

    Room temperature in continental US; may vary elsewhere

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 100 mg/mL (358.05 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.5805 mL 17.9025 mL 35.8051 mL
    5 mM 0.7161 mL 3.5805 mL 7.1610 mL
    10 mM 0.3581 mL 1.7903 mL 3.5805 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

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

      Solubility: ≥ 2.5 mg/mL (8.95 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (8.95 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (8.95 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
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    Product Name:
    TPCA-1
    Cat. No.:
    HY-10074
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