TPCA-1
CAS No. : 507475-17-4
| Size | Price | Stock |
|---|---|---|
| 5mg | $77 | In-stock |
| 10mg | $121 | In-stock |
| 50mg | $352 | In-stock |
| 100mg | $539 | In-stock |
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| 500 mg | Get quote | |
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| Cat. No. : | HY-10074 |
| M.Wt: | 279.29 |
| Formula: | C12H10FN3O2S |
| Purity: | >98 % |
| Solubility: | DMSO : ≥ 100 mg/mL (358.05 mM) |
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-α, IL-6, and IL-8 with an IC50 of 170 to 320 nM[1][2].
TPCA-1 (0-2 μM) 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].
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