MAP4K

HPK1-IN-38 is a selective inhibitor of MAP4K1, also known as HPK1. This compound exhibits potent inhibition of HPK1's kinase activity, making it a valuable tool for studying HPK1-related biological processes. Its application is particularly relevant in research focused on immune response modulation and cancer biology, where HPK1 plays a critical role.

HPK1-IN-20 is a specific inhibitor of hematopoietic progenitor kinase 1 (HPK1), which plays a critical role in immune signaling pathways. This compound demonstrates strong inhibition of HPK1 activity, which may enhance T cell activation and proliferation. It is suitable for research applications focused on immunological studies and potential therapeutic development for immune-related disorders.

HPK1-IN-37 is a selective inhibitor of MAP4K1/HPK1, demonstrating an IC50 of 3.7 nM. Its potent inhibitory activity makes it a valuable tool for investigating HPK1-related disorders, including various cancer types. Researchers can utilize HPK1-IN-37 to elucidate the role of HPK1 in signal transduction pathways and therapeutic interventions.

BAY-405 is a potent MAP4K1 inhibitor that demonstrates nanomolar activity in both biochemical and cellular assays. Its effective inhibition of MAP4K1 has significant implications for research into pathways regulated by this kinase, making it a valuable tool for studying cellular processes such as proliferation, differentiation, and stress response. Additionally, BAY-405 is capable of achieving in vivo exposure following oral administration, enhancing its utility in preclinical studies.

HPK1-IN-30 is a potent inhibitor of hematopoietic progenitor kinase 1 (HPK1), a serine/threonine kinase belonging to the MAP4K family. This compound demonstrates significant biological activity by modulating HPK1 signaling pathways, which are implicated in various cancers. HPK1-IN-30 is valuable for research applications focused on cancer biology and therapeutic development targeting the HPK1 pathway.

HPK1-IN-33 is a potent inhibitor of Hematopoietic Progenitor Kinase 1 (HPK1), exhibiting a Ki value of 1.7 nM. This compound effectively inhibits IL-2 production, demonstrating an EC50 of 286 nM in Jurkat wild-type cells and greater than 10,000 nM in Jurkat HPK1 knockout cells. HPK1-IN-33 is applicable in studies focused on immune response modulation and therapeutic interventions targeting T cell activation.

HPK1-IN-55 is a highly selective inhibitor of hematopoietic progenitor kinase 1 (HPK1), exhibiting an IC50 of less than 0.51 nM. This compound demonstrates significant selectivity for HPK1, with over 637-fold selectivity against GCK-like kinases and over 1022-fold against LCK. HPK1-IN-55 has been shown to possess anticancer properties, making it a valuable tool for research into cancer therapies and the regulation of hematopoietic cells.

HPK1-IN-60 is an inhibitor of the HPK1 protein kinase, which plays a critical role in regulating T cell activation. This compound exhibits significant potential in antitumor immunotherapy research by modulating immune responses. It is a valuable tool for studying the mechanisms of immune regulation and exploring therapeutic strategies in cancer treatment.

HPK1-IN-42 is a potent inhibitor of HPK1, exhibiting an IC50 value of 0.24 nM. This compound is valuable for studying the regulation of T cell receptor signaling and its implications in immune responses. Its use in research can advance understanding of HPK1's role in cellular processes and therapeutic strategies for immune-related diseases.

HPK1-IN-54 is a selective inhibitor of Hematopoietic Progenitor Kinase 1 (HPK1), significantly enhancing T cell activation and proliferation. With an IC50 value of 2.67 nM, it demonstrates over 100-fold selectivity against the MAP4K family and over 300-fold selectivity for other kinases. This compound exhibits potent antitumor effects, evidenced by strong efficacy in a CT26 murine colon cancer model and the ability to synergize with anti-PD-1 therapies. HPK1-IN-54 offers a valuable tool for research in immunotherapy applications.

HPK1-IN-24 is a potent inhibitor of hematopoietic progenitor kinase 1 (HPK1) with a Ki value of 100 nM. This compound is designed for applications in cancer research, where targeting HPK1 may enhance the understanding of tumorigenesis and cellular signaling pathways. Its inhibition of HPK1 allows for the exploration of novel therapeutic strategies in oncology.

PF-06260933 hydrochloride is a selective inhibitor of the MAP4K4 kinase, demonstrating an IC50 of 3.7 nM in enzymatic assays and 160 nM in cellular studies. This compound is orally active and is utilized in research focused on understanding the signaling pathways associated with MAP4K4. Its inhibition of MAP4K4 positions it as a valuable tool for investigating therapeutic strategies in diseases linked to aberrant MAP4K4 activity.

HPK1-IN-46 is a selective inhibitor of HPK1, demonstrating an IC50 value of 1.1 nM. This compound effectively inhibits SLP76 phosphorylation mediated by HPK1, resulting in the reversal of T-cell inhibition and an enhancement of anti-tumor immunity. HPK1-IN-46 is valuable in immunotherapy research for tumors, particularly in exploring T-cell regulatory mechanisms and tumor microenvironment interactions.

HPK1-IN-25 is a selective inhibitor of hematopoietic progenitor kinase 1 (HPK1) with an enzymatic activity IC50 of 129 nM. This compound is valuable for cancer research, as HPK1 plays a significant role in regulating cell proliferation and apoptosis. Researchers may utilize HPK1-IN-25 to investigate its effects on tumor growth and lymphocyte signaling pathways.

GNE-495 is a potent and selective MAP4K4 inhibitor with an IC50 of 3.7 nM.

TAK1/MAP4K2 inhibitor 1 is a potent dual inhibitor targeting transforming growth factor β-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2), exhibiting IC₅₀ values of 41.1 nM and 18.2 nM, respectively.

PF-06260933 is a potent, selective, orally available MAP4K4 inhibitor with IC50 of 3.7 nM.

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

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).

NG25, a TAK1 inhibitor, inhibited the activation of IKK by TLR7 and TLR9 agonists and prevented the secretion of type 1 IFNs induced by these ligands in Gen2.2 cells.

TL4-12 is a selective inhibitor of MAP4K2 and GCK, demonstrating a dose-dependent ability to downregulate IKZF1 and BCL-6. This compound effectively inhibits cell proliferation in multiple myeloma with an IC50 of 37 nM, and it also induces apoptosis in cancerous cells. TL4-12 holds potential for overcoming resistance to immunomodulatory agents in the treatment of multiple myeloma.

HPK1-IN-56 is a potent HPK1 inhibitor with an IC50 of 2.70 nM. It effectively inhibits downstream phosphorylation of SLP76, demonstrating an IC50 of 8.1 nM in Jurkat T cells. This compound induces IL-2 production in human peripheral blood mononuclear cells (PBMCs) and enhances T-cell cytotoxicity, contributing to its anticancer properties. HPK1-IN-56 also improves the antitumor efficacy of anti-PD-1 antibody therapies, making it a valuable tool for cancer immunotherapy research.

HPK1-IN-64 is a highly selective, orally bioavailable inhibitor of HPK1, featuring an IC50 of 1.9 nM. It demonstrates significant selectivity for HPK1 over GLK, MAP4K5, TBK1, and TNIK, with respective selectivity ratios exceeding 100-fold. This compound effectively inhibits SLP76 protein phosphorylation and reduces IL-2 secretion, making it a valuable tool for investigating signaling pathways in cancer research, particularly colorectal cancer.

HPK1-IN-61 is a potent inhibitor of hematopoietic progenitor kinase 1 (HPK1), exhibiting a Ki value of 0.4 nM. Additionally, it demonstrates strong inhibitory activity against Abl with an IC50 of less than 0.51 nM, and LCK with an IC50 of 24 nM. This compound is valuable for research applications focused on immune signaling and kinase regulation.

HPK1-IN-2 dihydrochloride is a potent inhibitor of hematopoietic progenitor kinase-1 (HPK1), exhibiting an IC50 of less than 0.05 μM. This compound also demonstrates inhibitory effects on Lck kinase with an IC50 range between 0.05 μM and 0.5 μM, as well as on Flt3, with an IC50 of less than 0.05 μM. Its biological activity and targeted inhibition make HPK1-IN-2 dihydrochloride a valuable tool for research focused on antitumor mechanisms and kinase pathway analyses.

Rentosertib is an orally active inhibitor of TNIK and MAP4K4, exhibiting IC50 values of 12-120 nM for both targets. This compound plays a crucial role in the modulation of signaling pathways involved in cell proliferation and survival. Relying on its potent inhibition, rentosertib is utilized in research applications exploring cancer biology and potential therapeutic interventions for related disorders.

GNE-6893 is a selective inhibitor of HPK1, demonstrating a Ki of less than 0.02 nM. This compound enhances T cell receptor signaling and promotes IL-2 production in stimulated primary human T cells, making it valuable for the investigation of T cell activation mechanisms. GNE-6893 is particularly relevant for research applications focused on chronic refractory cancers.

AZ3246 is a selective inhibitor of HPK1, exhibiting an IC50 of less than 3 nM. This compound promotes IL-2 secretion in T cells, with an EC50 of 90 nM, highlighting its immunomodulatory properties. AZ3246 serves as a valuable tool for research in cancer biology, particularly in the study of breast cancer therapeutics.

HPK1-IN-68 is a potent inhibitor of hematopoietic progenitor kinase 1 (HPK1), with an IC50 value of 2.8 nM. This compound effectively blocks HPK1 signaling pathways, inhibits the phosphorylation of SLP76, and stimulates the production of the IL-2 cytokine. Additionally, HPK1-IN-68 counteracts the immunosuppressive effects of prostaglandin E2 (PGE2) and promotes the infiltration of CD3+/CD8+ T cells into tumor microenvironments, demonstrating T cell-dependent antitumor activity in a mouse colon cancer model. It is particularly relevant for research into colon cancer therapeutics.