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Minnelide is a water-soluble prodrug of triptolide that is highly effective in reducing pancreatic tumor growth and spread, and improving survival; efficiently downregulates both CD133(-) and CD133(+) population in the tumors, resulting in a 60% decrease in tumor volume; also is very effective as a therapeutic option against Castration Resistant Prostate Cancer (CRPC)
TAK1-IN-1 is a potent, selective, Type I (ATP-competitive, DFG-in) TAK1 inhibitor with Kd of 59 nM, a thienopyrimidine scaffold that serves as a good starting point for medicinal chemistry.
PF-05381941 (PF 05381941, PF05381941) is a potent, dual TAK1/p38a inhibitor with IC50 of 156/186 nM respectively, with good kinome selectivity against 50 representative kinases; inhibits LPS-stimulated release of TNF-α from human peripheral mononuclear cells with IC50 of 8 nM.
Takinib is a potent, selective TAK1 inhibitor with IC50 of 9.5 nM, selectively induces apoptosis following TNF-a stimulation; weakly inhibits IRAK4, IRAK1, GCK, CLK2, and MINK1 with IC50 of 120-430 nM against the MRC Dundee kinase panel, does not inhibit any of the MAP2Ks or MAP3Ks family members; inhibits phosphorylation of IKK, MAPK 8/9, and c-Jun, induces apoptosis in RA fibroblast-like synoviocytes and reduces IL-6 secretion, induces TNF-α-dependent cell death in rheumatoid arthritis and breast cancer cells.
(5Z)-7-Oxozeaenol is a potent and selective TAK1 inhibitor with IC50 of 8 nM, displays >33-fold and >62-fold selectivity over MEKK1 and MEKK4 respectively; inhibits IL-1-induced activation of NF-κB (IC50 = 83 nM) and JNK/p38; also inhibits production of inflammatory mediators, and sensitizes cells to TRAIL- and TNF-α-induced apoptosis in vitro.
The active diterpene in the traditional Chinese medicine Lei Gong Teng, induces Ca(2+) release by a polycystin-2 (PC2)-dependent mechanism; arrests cellular proliferation and attenuates overall cyst formation by restoring Ca(2+) signaling in a murine model of ADPKD; also covalently binds to human XPB (ERCC3), a subunit of the transcription factor TFIIH, and inhibits its DNA-dependent ATPase activity, which leads to the inhibition of RNA polymerase II-mediated transcription; inhibits TAK1 kinase activity by interfering with the formation of the TAK1-TAB1 complex in macrophages.
5Z-7-Oxozeaenol is a potent, selective TAK1 inhibitor with IC50 of 8 nM, displays >33-fold and >62-fold selectivity over MEKK1 and MEKK4 respectively; inhibits IL-1-induced activation of NF-κB (IC50= 83 nM) and JNK/p38, inhibits production of inflammatory mediators, and sensitizes cells to TRAIL- and TNF-α-induced apoptosis in vitro; significantly enhances chemotherapeutic efficacy in vivo.
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