MAP4K Inhibitor

Pyrrolo[2,1-f][1,2,4]triazin-4-amine is a MAP4K4 inhibitor with a surface plasmon resonance (SPR) K_d of 88 μM and a ligand efficiency of 0.56.

GNE-1858 is a potent and ATP-competitive hematopoietic progenitor kinase-1 (HPK1) inhibitor, with IC₅₀s of 1.9 nM, 1.9 nM, and 4.5 nM for wild-type and the active mimetic mutants HPK1-TSEE and HPK1-SA, respectively.

HPK1-IN-2 dihydrochloride is an orally active HPK1 inhibitor (IC₅₀ < 0.05 µM) with antitumor activity. HPK1-IN-2 dihydrochloride inhibits the activity of Lck (IC₅₀ < 0.05 µM) and Flt3 (IC₅₀ < 0.05 µM) kinases.

TINK-IN-1 (Compound 9) is a potent and selective Traf2- and Nck-interacting kinase (TNIK) inhibitor with an IC₅₀ of 8 nM. TINK-IN-1 inhibits colorectal cancer cells viability.

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

HPK1-IN-34 (Compound 143) is a Hematopoietic progenitor kinase 1 (HPK1) inhibitor with an IC₅₀ of <100 nM. HPK1-IN-34 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

GNE-6893 is an orally active, selective HPK1 inhibitor with a K_i < 0.02 nM. GNE-6893 enhances T cell receptor signaling in primary human T cells. GNE-6893 increases IL2 production in stimulated primary human T cells. GNE-6893 can be used for the research of chronic refractory cancers.

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

HPK1-IN-19 (Compound I-47) is a hematopoietic progenitor kinase 1 (HPK1) inhibitor.

PF-07265028 is a selective hematopoietic progenitor kinase 1 (HPK1/MAP4K1). PF-07265028 can be used in the research of cancer. PF-07265028 shows very potent cellular activity as measured by pSLP76 IC₅₀ (17 nM).

NDI-101150 is an orally active, potent and selective hematopoietic progenitor cell kinase 1 (HPK1) inhibitor with an IC₅₀ of 0.7 nM. NDI-101150 blocks HPK1-mediated negative regulation of immune receptor signaling, inhibits immunosuppression of T cell activation, enhances antigen-specific antibody production and augments B-cell activation. NDI-101150 inhibits tumor growth in syngeneic tumor models, establishes durable antitumor immune memory, and synergizes with anti-PD1 to enhance exhausted T cell activity and drive tumor regressions. NDI-101150 can be used for the research of cancer, such as breast cancer and colon cancer.

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

AZ3246 is an orally active and selective inhibitor of HPK1 with an IC₅₀ of < 3 nM. AZ3246 induces IL-2 secretion in T cells with an EC₅₀ of 90 nM. AZ3246 is a low-clearance antitumor compound that can be used for the study of breast cancer.

(3S,4R)-GNE-6893 is a potent and orally active HPK1 inhibitor. (3S,4R)-GNE-6893 can be used in research of cancer.

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

PF-06260933 hydrochloride is the hydrochloride form of PF-06260933 (HY-19562). PF-06260933 hydrochloride is an orally active and highly selective inhibitor of MAP4K4 with IC₅₀s of 3.7 and 160 nM for kinase and cell, respectively.

HPK1-IN-15 is a potent and selective inhibitor of HPK1. Hematopoietic progenitor kinase 1 (HPKl) originally cloned from hematopoietic progenitor cells is a member of MAP kinase kinase kinase kinases (MAP4Ks) family. HPK1-IN-15 is useful in researching, preventing or ameliorating diseases or disorders associated with HPK1 activity such as cancer (extracted from patent WO2018049200A1, compound 50).

HPK1-IN-16 is a potent and selective inhibitor of HPK1. Hematopoietic progenitor kinase 1 (HPKl) originally cloned from hematopoietic progenitor cells is a member of MAP kinase kinase kinase kinases (MAP4Ks) family. HPK1-IN-16 is useful in researching, preventing or ameliorating diseases or disorders associated with HPK1 activity such as cancer (extracted from patent WO2019051199A1, compound 39).

HPK1-IN-13 is potent inhibitor of HPK1. HPK1 is a serine/threonine protein kinase cloned from hematopoietic progenitor cells and belongs to the MAP4K family of mammalian Ste-20-related protein kinases. HPK1-IN-13 has the potential for the research of HPK1 related diseases (extracted from patent WO2021213317A1, compound 64) .

HPK1-IN-12 is potent inhibitor of HPK1. HPK1 is a serine/threonine protein kinase cloned from hematopoietic progenitor cells and belongs to the MAP4K family of mammalian Ste-20-related protein kinases. HPK1-IN-12 has the potential for the research of HPK1 related diseases (extracted from patent WO2021213317A1, compound 85) .