Name: TPCA-1
Price: 228.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    TPCA-1 is a novel, potent, and selective inhibitor of human IKK-2.
    Demonstration that IκB kinase 2 (IKK-2) plays a pivotal role in the nuclear factor-κB-regulated production of proinflammatory molecules by stimuli such as tumor necrosis factor (TNF)-α and interleukin (IL)-1 suggests that inhibition of IKK-2 may be beneficial in the treatment of rheumatoid arthritis.
    In vitro: Determination of the activity of TPCA-1 against ten selected kinases, COX-1 and COX-2, showed the compound to be ~550-fold selective for IKK-2 versus ten of these enzymes. 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].
    In vivo: Prophylactic administration of TPCA-1 at 3, 10, or 20 mg/kg resulted in a dose dependent reduction in the severity of murine collagen-induced arthritis. The significantly reduced disease severity and delay of disease onset resulting from administration of TPCA-1 at 10 mg/kg were comparable to the effects of the antirheumatic drug, etanercept [1].
    Clinical trial: No clinical data are available currently.
- Properties
  - Alternative Name
    
    2-(carbamoylamino)-5-(4-fluorophenyl)thiophene-3-carboxamide
    
    CAS Number
    
    507475-17-4
    
    Molecular Formula
    
    C12H10FN3O2S
    
    Molecular Weight
    
    279.29
    
    Appearance
    
    A solid
    
    Purity
    
    99.32%
    
    Solubility
    
    insoluble in H2O; ≥13.95 mg/mL in DMSO; ≥2.53 mg/mL in EtOH with gentle warming and ultrasonic
    
    Storage
    
    Desiccate at -20°C
    
    * For Research Use Only
- Reference
  - 1. Jingchun Du, Yougui Xiang, et al. "RIPK1 dephosphorylation and kinase activation by PPP1R3G/PP1γ promote apoptosis and necroptosis." Nat Commun. 2021 Dec 3;12(1):7067. PMID:34862394
    2. Varga Z, Molnár T, et al. "Differences in the sensitivity of classically and alternatively activated macrophages to TAK1 inhibitor-induced necroptosis." Cancer Immunol Immunother. 2020;10.1007/s00262-020-02623-7. PMID:32472370
    3. Robert J. Posont. "The Role of Inflammatory Pathways in Development, Growth, and Metabolism of Skeletal Muscle in IUGR Offspring; Blood Gene Expression of Inflammatory Factors as Novel Biomarkers for Assessing Stress and Wellbeing in Exotic Species." University of Nebraska-Lincoln. 2019.
    4. Robeson AC, Lindblom KR, et al. "Dimer-specific immunoprecipitation of active caspase-2 identifies TRAF proteins as novel activators." EMBO J. 2018 Jun 6. pii: e97072. PMID:29875129
    5. Kwon Y, Choi SK, et al. "Involvement of inhibitor kappa B kinase 2 (IKK2) in the regulation of vascular tone." Lab Invest. 2018 May 21. PMID:29785049

TPCA-1

TPCA-1

Background

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