MAP4K Inhibitor

HPK1-IN-42 (compound 185) ia a HPK1 inhibitor with the IC₅₀ 50 of 0.24 nM.

Octahydrocurcumin (Hexahydrobisdemethoxycurcumin) is a hydrogenated derivative of curcumin and a metabolite of curcumin. Octahydrocurcumin is an orally active anticancer and anti-inflammatory agent, and is the final hydrogenated metabolite of Curcumin (HY-N0005) in vivo. Octahydrocurcumin exerts its anti-tumor and anti-inflammatory effects by inducing the mitochondrial apoptosis pathway and inhibiting the TAK1-NF-κB-COX-2 pathway, respectively.

NG25 (Standard) is the analytical standard of NG25. This product is intended for research and analytical applications. NG25 is a potent dual TAK1 and MAP4K2 inhibitor, with IC50s of 149 nM and 21.7 nM, respectively.

DMX-5804 (Standard) is the analytical standard of DMX-5804 (HY-111754). This product is intended for research and analytical applications. DMX-5804 is a potent, orally active and selective MAP4K4 inhibitor, with an IC₅₀ of 3 nM, a pIC₅₀ of 8.55 for human MAP4K4, less potent on MINK1/MAP4K6 (pIC₅₀, 8.18), and TNIK/MAP4K7 (pIC₅₀, 7.96). DMX-5804 enhances cardiomyocyte survival, and reduces ischemia-reperfusion injury in mice.

NCB-0846 (Standard) is the analytical standard of NCB-0846 (HY-100830). This product is intended for research and analytical applications. NCB-0846 is an orally active, selective inhibitor for Wnt, that inhibits Traf2- and Nck-interacting kinase (TNIK) with an IC50 of 21 nM. NCB-0846 blocks TGF-β signaling pathway by inhibiting SMAD2/3 phosphorylation and nuclear translocation.

GNE-495 (Standard) is the analytical standard of GNE-495 (HY-100343). This product is intended for research and analytical applications. GNE-495 is a potent and selective MAP4K4 inhibitor with an IC50 of 3.7 nM.

HPK1-IN-54 is a potent HPK1 (Hematopoietic Progenitor Kinase 1) inhibitor that enhances T cell activation and proliferation by inhibiting HPK1 activity, thereby exhibiting antitumor effects. Its IC₅₀ value against HPK1 is 2.67 nM, with excellent selectivity over the MAP4K family (>100-fold) and other selected kinases (>300-fold). HPK1-IN-54 displayed moderate in vivo clearance and reasonable oral exposure in mice and rats. Additionally, HPK1-IN-54 demonstrated strong antitumor efficacy in a CT26 murine colon cancer model and synergistic effects when combined with anti-PD-1 (HY-P9902A). HPK1-IN-54 shows promise for research in the field of immunotherapy.

HPK1-IN-48 (compound 14g) is a potent Hematopoietic Progenitor Kinase 1 (HPK1) inhibitor with a IC₅₀ of 0.15 nM. HPK1-IN-48 significantly suppresses the phosphorylation of SLP76 with a IC₅₀ of 27.92 nM.

HPK1-IN-53 (compund 3a) is the potent HPK1 inhibitor (IC₅₀=48 nM).