TPCA-1

507475-17-4

C12H10FN3O2S

DMSO : >= 100 mg/mL (358.05 mM)

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

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: IC50: 17.9 nM (IKK)^[1][2].
STAT3^[3]. In Vitro: TPCA-1 inhibits lipopolysaccharide-induced human monocyte production of TNF-alpha, IL-6, and IL-8 with an IC₅₀ of 170 to 320 nM^[1][2].
TPCA-1 (0-2 uM) 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]. 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].