TPCA-1

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的、选择性的、口服生物可利用的 IKK-2 抑制剂，IC50 为 63 nM，TNF 细胞 IC50 为 0.4 uM。

A potent, selective and orally bioavailable IKK-2 inhibitor with IC50 of 63 nM, TNF cell IC50 of 0.4 uM; displays >100-fold selectivity over IKK-1.

Cell Viability Assay Cell Line:human peripheral blood monocytes stimulated with LPS.Concentration:0-10 μM.Incubation Time:~24 hours.Result:TPCA-1 Inhibits LPS-Induced TNF-α, IL-6, and IL-8 production by human monocytes.Cell Viability AssayCell Line:HCC827 and H1975 cells.Concentration:0-10 μM.Incubation Time:0.5-2 hours.Result:Suppressed proliferation of HCC827 and H1975 cells. Led to a G2-M cell-cycle arrest in HCC827 but not A549.Western Blot Analysis Cell Line:HEK-293T cell lines.Concentration:0-2 μM (before IL-2 or IFN-α treatment).Incubation Time:0.5-2 hours.Result:Inhibited STAT3 phosphorylation and transactivation induced by cytokines and nonreceptor tyrosine kinase in dose- and time-dependent manner.

Animal Model:10-12 weeks old male DBA/1 OlaHsd mice.Dosage:3, 10, or 20 mg/kg.Administration:I.P., b.i.d, from days 1 to 47.Result:Reduced the severity and delays the onset of CIA.Attenuated ex vivo antigen-induced T cell proliferation in CIA.Animal Model:Six-week-old BALB/c female nude mice injected subcutaneously with HCC827 cells (5×106).Dosage:10 mg/kg.Administration:Intraperitoneally daily.Result:The tumor weight inhibition rate of TPCA-1, ZD1839, and their combination are 0.419(ETPCA-1), 0.680(EZD1839), and 0.837(Eobserved), respectively.

IKK-2 Inhibitor IV

Immunology/Inflammation

IκB kinase (IKK)

IKK2

Inflammation/Immunology

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507475-17-4

279.2901

C12H10FN3O2S

>98% (HPLC)

10 mM in DMSO

O=C(C1=C(NC(N)=O)SC(C2=CC=C(F)C=C2)=C1)N

3-Thiophenecarboxamide, 2-[(aminocarbonyl)amino]-5-(4-fluorophenyl)-

(-20℃)

With Ice Pack

≥ 2 years