MAP4K Inhibitor

HPK1-IN-69 is an orally active HPK1 inhibitor with an IC₅₀ of 1.7 nM. HPK1-IN-69 inhibits the HPK1-mediated TCR signaling pathway, reduces the phosphorylation level of SLP76, and promotes the release of IL-2. HPK1-IN-69 exhibits in vivo anti-tumor activity in mouse models. HPK1-IN-69 can be used for the research of colorectal cancer and MC38 syngeneic tumors.

HPK1-IN-38 (compound 15) is a MAP4K1/HPK1 inhibitor，can be used for HPK1 related disorders research.

HPK1-IN-72 is an orally active and selective HPK1/MAP4K1 inhibitor with an IC₅₀ of 52.4 nM against human targets. HPK1-IN-72 inhibits HPK1 activation, blocks the negative regulation of T cell receptor signaling, restores T cell receptor signal transduction and enhances T cell function. HPK1-IN-72 suppresses tumor growth, exhibits potent single-agent anti-tumor efficacy, and also produces synergistic effects with anti-PD-1 antibodies or anti-PD-L1/IL-15 immunocytokine prodrugs. HPK1-IN-72 can be used in research related to breast cancer, colorectal cancer and prostate cancer.

HPK1-IN-65 is a selective and orally active HPK1 inhibitor with an IC₅₀ value of < 5 nM. HPK1-IN-65 inhibits HPK1 kinase activity and displays 1257-fold selectivity over the MAP4K kinase family member GLK. HPK1-IN-65 exhibits an IC₅₀ of 92.3 nM for inhibiting pSLP76 phosphorylation. HPK1-IN-65 demonstrates an EC₅₀ of 398 nM for stimulating IL-2 production. HPK1-IN-65 inhibits TCR-induced phosphorylation of SLP76 at Ser376 in a dose-dependent manner. HPK1-IN-65 can be further utilized for colorectal cancer research.

HPK1-IN-20 (Compound 106) is a hematopoietic progenitor kinase 1 (HPK1) inhibitor.

HPK1-IN-37 (compound A85) is an inhibitor of HPK1 (IC₅₀=3.7 nM). HPK1-IN-37 can be used for research in HPK1 related disorders or diseases including cancers.

BAY-405 (compund 38) is a MAP4K1 inhibitor that exhibits nanomolar potency in biochemical and cellular assays and achieves in vivo exposure after oral administration.

HPK1-IN-30 is a potent inhibitor of HPK1. MAP4K1 is also known as hematopoietic progenitor kinase 1 (HPK1). MAP4K1 is a serine/threonine kinase and member of the germinal center kinase family. HPK1-IN-30 has the potential for the research of cancer diseases (extracted from patent WO2021175271A1, compound 3).

TNIK-IN-11 is a TNIK inhibitor with a human TNIK pIC₅₀ of 7.80. TNIK-IN-11 inhibits TNIK kinase activity and promotes neurite outgrowth. TNIK-IN-11 activates AKT signaling via increased phosphorylated AKT levels, and induces gene expression changes including upregulation of neuronal differentiation and morphological remodeling genes. TNIK-IN-11 can be used for the research of dup15q syndrome.

Multi kinase ligand 4 is a target protein ligand used in the synthesis of PROTAC DB-0646 (HY-137343).

HPK1-IN-33 (compound 21) is a potent Hematopoietic Progenitor Kinase 1 (HPK1) inhibitor with a K_i value of 1.7 nM. HPK1-IN-33 inhibits the produce of IL-2 with EC₅₀s of 286, >10000 nM in Jurkat WT and Jurkat HPK1 KO cells, respectively.

HPK1-IN-71 is a potent and selective HPK1 inhibitor with an IC₅₀ of 26.3 nM. HPK1-IN-71 can inhibit the phosphorylation of SLP76, promote the secretion of IL-2 and show high selectivity for other kinases and immune-targeting kinases. HPK1-IN-71 can be used in colon cancer research.

HPK1-IN-55 (compound 19) is a selective and orally active hematopoietic progenitor kinase 1 (HPK1) inhibitor with an IC₅₀ of <0.51 nM. HPK1-IN-55 shows excellent kinase selectivity (>637-fold vs GCK-like kinase and >1022-fold vs LCK). HPK1-IN-55 has anticancer effects.

HPK1-IN-60 (Compound 1) is a HPK1 inhibitor. HPK1-IN-60 can be used for antitumor immunotherapy research.

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.

PI4K-IN-3 (Compound 27) is an orally active PI4K inhibitor with an IC₅₀ of 1.9  nM for Plasmodium vivax PI4K. PI4K-IN-3 has no hERG channel inhibition and mammalian cytotoxicity. PI4K-IN-3 has significant selectivity against the human MINK1 and MAP4K4 kinases but with low selectivity against human PI3Kα and PI4Kβ. PI4K-IN-3 has potent antimalarial activity and significantly reduces parasitaemia in NSG mice mouse models of Plasmodium falciparum malaria.

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.