MAP4K
MAPK Kinase Kinase Kinase
MAP kinase kinase kinase kinases (MAP4Ks) belong to the mammalian Ste20-like family of serine/threonine kinases. MAP4Ks including MAP4K1/HPK1, MAP4K2/GCK, MAP4K3/GLK, MAP4K4/HGK, MAP4K5/KHS, and MAP4K6/MINK have been reported to induce JNK activation through activating the MAP3K-MAP2K cascade. MAP4Ks play important roles in the regulation of cell apoptosis, cell survival, cell autophagy, and cell migration. Several studies reported that MAP4Ks are involved in the regulation of immune-cell responses through JNK-independent pathways.
MAP4K1/HPK1 and MAP4K4/HGK play negative roles in T-cell activation and inflammatory responses. In contrast, MAP4K3/GLK plays a positive role in T-cell activation and autoimmune responses. Moreover, MAP4K1 downregulation and MAP4K3 overexpression in T cells are involved in human autoimmune diseases such as psoriatic arthritis, rheumatoid arthritis (RA), adult-onset Still’s disease, and SLE.
MAP4K Isoform Specific Products
All Product Categories
-
MAP4K Related Products (133)
Related Products (133)
-
MAP4K Isoform Comparison
-
HPK1-IN-42
0 ImagesCat. No.: HY-160218CAS No.: 2848684-50-2HPK1-IN-42 (compound 185) ia a HPK1 inhibitor with the IC50 50 of 0.24 nM.
-
Octahydrocurcumin (Standard)
0 ImagesSynonyms: Hexahydrobisdemethoxycurcumin (Standard)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
0 ImagesCat. No.: HY-178775PI4K-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)
0 ImagesCat. No.: HY-15434RCAS No.: 1315355-93-1NG25 (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.
-
NCB-0846 (Standard)
0 ImagesNCB-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)
0 ImagesCat. No.: HY-100343RCAS No.: 1449277-10-4
-
HPK1-IN-54
0 ImagesCat. No.: HY-159905CAS No.: 3048537-48-7HPK1-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-24
0 ImagesCat. No.: HY-144091CAS No.: 2294966-07-5HPK1-IN-24 (example 51) is a hematopoietic progenitor kinase 1 (HPK1) inhibitor with a Ki of 100 nM. HPK1-IN-24 has the potential for cancer research.
-
HPK1-IN-46
0 ImagesCat. No.: HY-160940CAS No.: 2810880-82-9HPK1-IN-46 (Compound 36) is an efficient and highly selective HPK1 reverse indazole inhibitor with an IC50 value of 1.1 nM. HPK1-IN-46 exhibits high selectivity for CDK2, JAK1, and JAK2. HPK1-IN-46 inhibits SLP76 phosphorylation mediated by HPK1, reverses T-cell inhibition, and enhances anti-tumor immunity. HPK1-IN-46 can be used in immunotherapy research for tumors.
-
HPK1-IN-25
0 ImagesCat. No.: HY-144092CAS No.: 2403600-50-8HPK1-IN-25 (example 94) is a hematopoietic progenitor kinase 1 (HPK1) inhibitor with a enzymatic activity IC50 of 129 nM. HPK1-IN-25 has the potential for cancer research.
