MAP4K Inhibitor

NG25 trihydrochloride is a dual TAK1 and MAP4K2 inhibitor (IC₅₀: 149 nM and 21.7 nM respectively). NG25 sensitizes the breast cancer cells to Doxorubicin (HY-15142A), and enhances apoptosis. NG25 trihydrochloride can be used for research of various cancers.

HPK1-IN-57 (Compound 10c) is a hematopoietic progenitor kinase 1 (HPK1) inhibitor with an IC₅₀ value of 0.09 nM. HPK1-IN-57 inhibits the activity of HPK1 kinase, hindering the phosphorylation of the downstream adaptor protein SLP76 (IC₅₀ is 33.74 nM) and effectively stimulating the secretion of the T cell activation marker IL-2 (EC₅₀ is 84.24 nM). HPK1-IN-57 is promising for research of tumor immunotherapy.

HPK1-IN-39 (Compound 10n) is a selective HPK1 Inhibitor (IC₅₀: 29 nM). HPK1-IN-39 inhibits the phosphorylation of SLP76. HPK1-IN-39 can be used for research of cancer immunotherapy.

HMC-B17 is a selective, orally bioavailable HPK1 inhibitor (IC₅₀ = 1.39 nM) that potentiates anti-PD-L1 efficacy. HMC-B17 potently enhances the IL-2 secretion in Jurkat cells (EC₅₀ = 11.56 nM). HMC-B17 can be used for the research of cancer.

HPK1-IN-58 (Compound 26) is an inhibitor of HPK1 (IC₅₀: 2.6 nM) and SLP76 (IC₅₀: 20 nM). HPK1-IN-58 enhances IL-2 secretion and reverses PGE2-induced immunosuppression. HPK1-IN-58 can be used in anti-tumor immunity research.

HPK1-IN-61 (Compound 1) is an inhibitor of hematopoietic progenitor kinase 1 (HPK1) (K_i = 0.4 nM) and an inhibitor of Abl (IC₅₀ < 0.51 nM). HPK1-IN-61 also shows inhibitory activity against LCK with an IC₅₀ of 24 nM.

HPK1-IN-41 (compound Z389) is a HPK1 inhibitor with an IC₅₀ value of 0.21 μM. HPK1-IN-41 can be used for the research of preventing and/or treating diseases or conditions associated with HPK1 activity.

3,4-Dephostatin (Methyl-3,4-dephostatin) is an inhibitor of protein-tyrosine phosphatase (PTPase). 3,4-Dephostatin accelerates nerve growth factor (NGF)-induced neurite formation in PC12h cells. 3,4-Dephostatin sustains the NGF-induced tyrosine phosphorylation of proteins, most prominently that of mitogen-activated protein (MAP) kinase. 3,4-Dephostatin also prolongs epidermal growth factor (EGF)-induced tyrosine phosphorylation and activation of MAP kinase.

HPK1-IN-27 is a potent inhibitor of HPK1. MAP4K1 is also known as hematopoietic progenitor kinase 1 (HPK1). MAP4K1 is a serine/threonine kinase and member of the germinal center kinase family. HPK1-IN-27 has the potential for the research of cancer diseases (extracted from patent WO2019016071A1, compound 38).

HPK1-IN-59 (compound 39) is an orally active HPK1 inhibitor with an IC₅₀ of 0.70 nM. HPK1-IN-59 has favorable oral bioavailability in mice.

HPK1-IN-45 (Compound 3) is a HPK1 inhibitor, with an IC₅₀ of 0.3 nM. HPK1-IN-45 inhibits SLP-76 phosphorylation (IC₅₀ = 57.52 nM) and IL-2 release (IC₅₀ = 38 nM). HPK1-IN-45 can be used for the research of cancer.

HPK1-IN-40 (compound 49) is a potent and selective HPK1 inhibitor with an IC₅₀ of 0.9 nM. HPK1-IN-40 reinvigorates T-cell receptor (TCR) signaling, promoting T-cell function and cytokine production in T cells while having anti-cancer activity.

HPK1-IN-28 is a potent inhibitor of HPK1. Hematopoietic progenitor kinase 1 (HPK1) is a negative regulator of the activation response of dendritic cells (DCs), T cells and B cells. HPK1-IN-28 enhances the body's anti-tumor immunity. HPK1-IN-28 has the potential for the research of immune-related diseases, especially tumor (extracted from patent WO2021175270A1, compound 1).

HPK1-IN-29 is a potent inhibitor of HPK1. Hematopoietic progenitor kinase 1 (HPK1) is a negative regulator of the activation response of dendritic cells (DCs), T cells and B cells. HPK1-IN-29 enhances the body's anti-tumor immunity. HPK1-IN-29 has the potential for the research of immune-related diseases, especially tumor (extracted from patent WO2021175270A1, compound 38).

MAP4K4-IN-6 (Compound 15f) is a MAP4K4 inhibitor (IC₅₀: 80 nM). MAP4K4-IN-6 reduces the c-Jun phosphorylation. MAP4K4-IN-6 has neuroprotective effects. MAP4K4-IN-6 increases the viability of motor neurons. MAP4K4-IN-6 can be used for research of Amyotrophic lateral sclerosis (ALS).

HPK1-IN-38 (compound 15) is a MAP4K1/HPK1 inhibitor，can be used for HPK1 related disorders research.

HPK1-IN-20 (Compound 106) is a hematopoietic progenitor kinase 1 (HPK1) inhibitor.

HPK1-IN-37 (compound A85) is an inhibitor of HPK1 (IC₅₀=3.7 nM). HPK1-IN-37 can be used for research in HPK1 related disorders or diseases including cancers.

BAY-405 (compund 38) is a MAP4K1 inhibitor that exhibits nanomolar potency in biochemical and cellular assays and achieves in vivo exposure after oral administration.

HPK1-IN-30 is a potent inhibitor of HPK1. MAP4K1 is also known as hematopoietic progenitor kinase 1 (HPK1). MAP4K1 is a serine/threonine kinase and member of the germinal center kinase family. HPK1-IN-30 has the potential for the research of cancer diseases (extracted from patent WO2021175271A1, compound 3).