TPCA-1

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.

Product Specifications

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.