| Bioactivity | 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. | ||||||||||||
| Invitro | 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]. Cell Viability Assay[2] Cell Line: | ||||||||||||
| Name | TPCA-1 | ||||||||||||
| CAS | 507475-17-4 | ||||||||||||
| Formula | C12H10FN3O2S | ||||||||||||
| Molar Mass | 279.29 | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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