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MAP4K Inhibitors

Cat.No. Product Name Information Product Use Citations Product Validations
S8392 NCB-0846 NCB-0846 is a novel, orally small-molecule Wnt inhibitor that inhibits TNIK (TRAF2 and NCK-Interacting Kinase, MAP4K7) with an IC50 value of 21 nM.
Nat Commun, 2024, 15(1):2551
Genes Dis, 2024, 11(3):100997
Sci Rep, 2022, 12(1):7
S6499 PF-6260933 PF-6260933 (PF-06260933) is a potent inhibitor of MAP4K4 with an IC50 of 3.7 nM, possessing excellent kinome selectivity.
bioRxiv, 2023, 2023.04.24.538014
Biomed Pharmacother, 2022, 149:112810
J Cell Sci, 2020, 14;133(9) pii: jcs240077
S0268 DMX-5084 DMX-5804 is a potent, orally active and selective inhibitor of Mitogen-activated protein kinase kinase kinase kinase-4 (MAP4K4) with IC50 of 3 nM for human MAP4K4. DMX-5804 is more potent on human MAP4K4 with pIC50 of 8.55 than MINK1/MAP4K6 and TNIK/MAP4K7 with pIC50 of 8.18 and 7.96, respectively.
Commun Biol, 2022, 5-1:1071
E1297 BGB 15025 BGB-15025 is a potent and selective HPK1 inhibitor. It is used in the treatment of various cancers.
EMBO Mol Med, 2025, 10.1038/s44321-025-00220-8
E2376 KY-05009 KY-05009 is an ATP-competitive Traf2- and Nck-interacting kinase (TNIK) inhibitor with a Ki of 100 nM, which inhibits the protein expression of TNIK and transcriptional activity of Wnt target genes and induces apoptosis in cancer cells.
Front Public Health, 2025, 13:1582860
E4726New NDI-101150 NDI-101150 is a potent HPK1 (MAP4K1) inhibitor that selectively activates immune cells such as T cells, B cells, and dendritic cells. It significantly inhibits tumor growth and induces complete tumor regression in the EMT-6 mouse model.
E4710 KHK-6 KHK-6 is a potent ATP-competitive inhibitor of HPK1 kinase activity with an IC50 value of 20 nM. It significantly enhances CD3/CD28-induced production of cytokines by downregulating the HPK1-SLP-76 signaling cascade in the TCR signaling pathway.
E5947New AZ3246 AZ3246 is a selective inhibitor of HPK1 with an IC50 value of <3 nM. AZ3246 induces IL-2 secretion in T cells with an EC50 of 90 nM and demonstrates antitumor activity in in vivo models.
E1944 Rentosertib (INS018-055, ISM001-055) INS018-055 (ISM001-055, TNIK&MAP4K4-IN-2, compound 112) is an inhibitor of TNIK and MAP4K4. It exhibits an IC50 values of 12-120 nM on TNIK.
E5816New PF-07265028 PF-07265028 is a potent and selective inhibitor of hematopoietic progenitor kinase 1 (HPK1/MAP4K1) with a Ki of <0.05 nM, and exhibits potent cellular activity, with a pSLP76 IC50 of 17 nM.
E1161 CompK CompK (compound K), a potent and selective hematopoietic progenitor kinase 1 (HPK1 or MAP4K1) small molecule inhibitor, significantly improves human T-cell functions, with enhanced T-cell receptor avidity to recognize tumor-associated antigens and tumor cytolytic activity by CD8+ T cells.
E4722 GNE-495 GNE-495 is a potent and selective inhibitor of MAP4K4 with an IC50 value of 3.7 nM. It demonstrates excellent potency and good Pharmacokinetics in in vivo efficacy in a retinal angiogenesis model.
E0946 MAP4K4-IN-3 MAP4K4-IN-3 is a potent and selective Mitogen-activated protein kinase 4 (MAP4K4) inhibitor with an IC50 of 14.9 nM in kinase assay, an IC50 of 470 nM in cell assay.
S8868 NG25 NG25 is a novel inhibitor of TAK1 with enzymatic IC50s of 149 and 21.7 nM for TAK1 and MAP4K2 respectively.
Int J Biol Sci, 2024, 20(2):606-620
Biochem J, 2022, 479(20):2195-2216
Lab Invest, 2021, 10.1038/s41374-021-00671-w