MAP4K Inhibitor

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.

HPK1-IN-64 is a potent, selective, and orally active HPK1 inhibitor with an IC₅₀ value of 1.9 nM. HPK1-IN-64 exhibits selectivity exceeding 100-fold, 80-fold, 300-fold, and 350-fold against off-target kinases such as GLK, MAP4K5, TBK1, and TNIK, respectively. HPK1-IN-64 inhibits SLP76 protein phosphorylation and IL-2 secretion. HPK1-IN-64 may be used in cancer research, such as for colorectal cancer.

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-67, a HPK1 inhibitor, is a ligand for target protein for PROTAC. HPK1-IN-67 can be used for synthesis of PROTACs, such as PROTAC HPK1 Degrader-7 (HY-179727).

RET-IN-19 (compound 59) is a potent RET inhibitor, with IC₅₀ values of 6.8 and 13.51 nM against RET-wt and RET V804M, respectively. RET-IN-19 shows anticancer activity. RET-IN-19 can be used for non-small cell lung cancer (NSCLC) research.

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.

F1386-0303 is a highly selective MAP4K4 inhibitor with an IC₅₀ of 34 nM against human targets. F1386-0303 exerts cardiomyocyte protective and function-preserving effects through mechanisms such as alleviating oxidative stress, inhibiting caspases, and maintaining mitochondrial membrane potential, while it does not interfere with the activity of Doxorubicin (HY-15142A) in cancer cells. F1386-0303 is rapidly cleared and has no bioavailability in mice, but it is well-suited as a tool compound for target validation. F1386-0303 can be applied to studies related to cardiac ischemia-reperfusion injury, Doxorubicin-induced cardiotoxicity, myocardial infarction and other related conditions.

FLT3/ITD-IN-4 (Compound 16) is a selective FMS-like tyrosine kinase 3 internal tandem duplications (FLT3-ITD) inhibitor with an IC₅₀ of 2.3 nM. FLT3/ITD-IN-4 can be used for acute myeloid leukemia research.

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-44 (Compound 1) is an inhibitor of HPK1 (IC₅₀=0.1 nM (40 μM ATP)).

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-35 is a potent and selective HPK1 inhibitor with an IC₅₀ value of 3.5 nM. HPK1-IN-35 decreases the expression of p-SLP76 and promotes IL-2 secretion.

HPK1-IN-49 (Compound I-4) is an inhibitor for hematopoietic progenitor kinase 1 (HPK1) with an IC₅₀ >100 nM.

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

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).

HPK1-IN-47 is a HPK1 ligand. HPK1-IN-47 can be used for synthesis of PROTACs, such as PROTAC HPK1 Degrader-2 (HY-162544). HPK1-IN-47 can be used for research of HPK1-mediated diseases including cancer.

HPK1-IN-52 is a potent and orally active hematopoietic progenitor kinase 1 (HPK1) inhibitor with an IC₅₀ value of 10.4 nM. HPK1-IN-52 exhibits anti-tumor activities.

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).