MAP4K

NG25 is a potent and cell-permeable inhibitor of transforming growth factor-β-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2), with IC 50 values of 149nM and 21.7nM, respectively.

GNE-495 is an orally bioavailable, potent, and selective MAP4K4 inhibitor (IC50 = 3.7 nM).

NCB-0846 is an orally available TNIK inhibitor with an IC50 of 21 nM.

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.

PF-06260933 is an orally active and highly selective inhibitor of MAP4K4 with IC50s of 3.7 and 160 nM for kinase and cell, respectively.

GNE-220 is a potent and selective inhibitor of MAP4K4 with an IC50 of 7 nM.

GNE 220 (hydrochloride) is a potent and selective inhibitor of MAP4K4, with an IC50 of 7 nM.

MAP4K4 (HGK) inhibitor; also inhibits MINK and TNIK

Potent MAP4K2 (GCK) inhibitor

HPK1-IN-3 is a potent and selective ATP-competitive hematopoietic progenitor kinase 1 (HPK1; MAP4K1) inhibitor with an IC50 of 0.25 nM.

HPK1-IN-7 is a potent, orally active HPK1 (hematopoietic progenitor kinase 1, MAP4K1) inhibitor (IC50=2.6 nM) with excellent family and kinome selectivity. HPK1-IN-7 shows selectivity against IRAK4 (59 nM) and GLK (140 nM). HPK1-IN-7 shows robust efficacy against MC38 syngeneic tumor model in combination with anti-PD1.

MAP4K4-IN-3 (Compound 17) is a potent and selective MAP4K4 inhibitor with an IC50 of 14.9 nM in kinase assay, an IC50 of 470 nM in cell assay.

HPK1-IN-8 is an allosteric, inactive conformation-selective inhibitor of full-length HPK1.

HPK1-IN-4 (comp 22) is a HPK1 (MAPK41) inhibitor (IC50 of 0.061 nM) as preclinical immunotherapy tool compound.

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).

KIF18A-IN-1 is an inhibitor of hematopoietic progenitor kinase 1 (HPK1), and more information can be found in compound I-47 in patent document WO2018102366A1.

ZYF0033 (HPK1-IN-22, compound ZYF0033) is a hematopoietic progenitor kinase 1 (HPK1) inhibitor with an IC50 of less than 10 nM based on its inhibitory effect on MBP protein phosphorylation. ZYF0033 reduces the phosphorylation of SLP76 (serine 376). ZYF0033 promotes anti-cancer immune response. ZYF0033 inhibits tumor growth in the 4T-1 syngeneic mouse model and leads to increased infiltration of DC, NK cells, and CD107a+CD8+ T cells into tumors but decreased infiltration of T cells, PD-1+CD8+ T cells, TIM-3+CD8+ T cells, and LAG3+CD8+ T cells.

HPK1-IN-32 is a highly selective, orally active small-molecule inhibitor of hematopoietic progenitor kinase 1 (HPK1/MAP4K1) with an IC 50 of 1.04nM.

HPK1-IN-26 is a HPK1 and GLK inhibitor extracted from patent WO2021254118A1 compound 1.

HPK1-IN-2 didrochloride is a potent and orally active hematopoietic progenitor kinase-1 (HPK1) inhibitor (IC50<0.05 µΜ) with antitumor activity.

GNE-6893 is a potent and orally active HPK1 inhibitor.

(3S,4R)-GNE-6893 is a potent and orally active HPK1 inhibitor.

HPK1-IN-34 (Compound 143) is a Hematopoietic progenitor kinase 1 (HPK1) inhibitor with an IC50 of <100 nM.