| S8392 |
NCB-0846
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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.
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Nat Commun, 2024, 15(1):2551
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Genes Dis, 2024, 11(3):100997
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Sci Rep, 2022, 12(1):7
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| S6499 |
PF-6260933
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PF-6260933 (PF-06260933) is a potent inhibitor of MAP4K4 with an IC50 of 3.7 nM, possessing excellent kinome selectivity.
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bioRxiv, 2023, 2023.04.24.538014
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Biomed Pharmacother, 2022, 149:112810
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J Cell Sci, 2020, 14;133(9) pii: jcs240077
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| S0268 |
DMX-5084
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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.
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Commun Biol, 2022, 5-1:1071
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| E1297 |
BGB 15025
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BGB-15025 is a potent and selective HPK1 inhibitor. It is used in the treatment of various cancers.
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EMBO Mol Med, 2025, 10.1038/s44321-025-00220-8
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| E2376 |
KY-05009
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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.
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Front Public Health, 2025, 13:1582860
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| E4726New |
NDI-101150
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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.
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| E4710 |
KHK-6
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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.
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| E5947New |
AZ3246
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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.
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| E1944 |
Rentosertib (INS018-055, ISM001-055)
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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.
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| E5816New |
PF-07265028
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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.
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