TPCA-1

• 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.

• CAS Number :

  [507475-17-4]

• UNSPSC :

  12352005

• Hazard Statement :

  H302, H319

• Target :

  Apoptosis; IKK; STAT

• Type :

  Reference compound

• Related Pathways :

  Apoptosis; JAK/STAT Signaling; NF-κB; Stem Cell/Wnt

• Applications :

  COVID-19-immunoregulation

• Field of Research :

  Inflammation/Immunology; Cancer

• Assay Protocol :

  https://www.medchemexpress.com/TPCA-1.html

• Purity :

  99.66

• Solubility :

  DMSO : ≥ 100 mg/mL

• Smiles :

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

• Molecular Formula :

  C12H10FN3O2S

• Molecular Weight :

  279.29

• Precautions :

  H302, H319

• References & Citations :

  [1]Sachse F, et al. IKK-2 inhibitor TPCA-1 represses nasal epithelial inflammation in vitro.Rhinology. 2011 Jun;49 (2) :168-73.|[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|[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.

• Shipping Conditions :

  Room Temperature

• Storage Conditions :

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category :

  Reference compound1

• Clinical Information :

  No Development Reported

• Isoform :

  IKK-β; STAT3