TPCA-1 | CAS:507475-17-4

Chemscene社は、高品質な低分子化合物を提供しているメーカーです。
Chemscene社のTPCA-1(CAS:507475-17-4)をご紹介します。

※本製品は研究用です。研究用以外には使用できません。

Name:TPCA-1; 
Cat. No. :CS-0045
CAS No. :507475-17-4
Formula:C12H10FN3O2S
M. Wt. : 279.29
Solubility:10 mM in DMSO

TPCA-1 is a potent inhibitor of IKK-2 with IC50 of 17.9 nM.IC50 & Target: IC50: 17.9 nM (IKK)In Vitro: TPCA-1 significantly represses pro-inflammatory cytokines IL-8 and GRO-α in NPECs[1]. TPCA-1 inhibit NFκB activity as well as glioma cell proliferation and IL8 expression, and at concentrations of 2.5 and 5 μM, it blocks the TNF-induced p65 translocation into the nucleus of U87 cells[2]. TPCA-1 inhibits lipopolysaccharide-induced human monocyte production of TNF-α, IL-6, and IL-8 with an IC50=170 to 320 nM[3].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). TPCA-1 (10 mg/kg, i.p., b.i.d.) in vivo results in significantly decreased collagen-induced T cell proliferation ex vivo[3].

Du Z, et al. Inhibition of Type I Interferon-Mediated Antiviral Action in Human Glioma Cells by the IKK Inhibitors BMS-345541 and TPCA-1.J Interferon Cytokine Res. 2012 Aug;32(8):368-77. Epub 2012 Apr 17. Sachse F, et al. IKK-2 inhibitor TPCA-1 represses nasal epithelial inflammation in vitro.Rhinology. 2011 Jun;49(2):168-73. Chu D, et al. Neutrophil-Mediated Delivery of Therapeutic Nanoparticles across Blood Vessel Barrier for Treatment of Inflammation and Infection. ACS Nano. 2015 Dec 22;9(12):11800-11. 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