MAP4K
MAPK Kinase Kinase Kinase
MAP kinase kinase kinase kinases (MAP4Ks) belong to the mammalian Ste20-like family of serine/threonine kinases. MAP4Ks including MAP4K1/HPK1, MAP4K2/GCK, MAP4K3/GLK, MAP4K4/HGK, MAP4K5/KHS, and MAP4K6/MINK have been reported to induce JNK activation through activating the MAP3K-MAP2K cascade. MAP4Ks play important roles in the regulation of cell apoptosis, cell survival, cell autophagy, and cell migration. Several studies reported that MAP4Ks are involved in the regulation of immune-cell responses through JNK-independent pathways.
MAP4K1/HPK1 and MAP4K4/HGK play negative roles in T-cell activation and inflammatory responses. In contrast, MAP4K3/GLK plays a positive role in T-cell activation and autoimmune responses. Moreover, MAP4K1 downregulation and MAP4K3 overexpression in T cells are involved in human autoimmune diseases such as psoriatic arthritis, rheumatoid arthritis (RA), adult-onset Still’s disease, and SLE.
MAP4K Isoform Specific Products
All Product Categories
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MAP4K Related Products (133)
Related Products (133)
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MAP4K Isoform Comparison
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HPK1-IN-64
0 ImagesCat. No.: HY-179111CAS No.: 3034320-17-4HPK1-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.
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3,4-Dephostatin
0 ImagesCat. No.: HY-124152CAS No.: 173043-84-0Synonyms: Methyl-3,4-dephostatin3,4-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.
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HPK1 ligand 6
0 ImagesCat. No.: HY-179196CAS No.: 3056139-31-9
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HPK1-IN-27
0 ImagesCat. No.: HY-143868CAS No.: 2268794-52-9HPK1-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).
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RET-IN-19
0 ImagesCat. No.: HY-151377CAS No.: 2484919-71-1RET-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.
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F1386-0303
0 ImagesCat. No.: HY-W207224CAS No.: 287177-12-2F1386-0303 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.
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FLT3/ITD-IN-4
0 ImagesCat. No.: HY-146680CAS No.: 2278278-04-7FLT3/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.
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HPK1-IN-40-d2
0 ImagesCat. No.: HY-149773SCAS No.: 3032624-35-1HPK1-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.
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PROTAC HPK1 Degrader-8
0 ImagesCat. No.: HY-184230CAS No.: 3120899-50-2PROTAC HPK1 Degrader-8 is a HPK1 PROTAC degrader with a DC50 of 1-10 nM. PROTAC HPK1 Degrader-8 promotes HPK1 ubiquitination and degradation. PROTAC HPK1 Degrader-8 induces IL-2 production, with an EC50 of 3 nM. PROTAC HPK1 Degrader-8 can be used in research related to hematologic malignancies and solid tumors.
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HPK1-IN-44
0 ImagesCat. No.: HY-163495CAS No.: 3034319-27-9HPK1-IN-44 (Compound 1) is an inhibitor of HPK1 (IC50=0.1 nM (40 μM ATP)).
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HPK1-IN-28
0 ImagesCat. No.: HY-143869CAS No.: 2699603-89-7HPK1-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).
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HPK1-IN-35
0 ImagesCat. No.: HY-149232CAS No.: 2935903-77-6HPK1-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.
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HPK1-IN-49
0 ImagesCat. No.: HY-161917CAS No.: 2845144-97-8HPK1-IN-49 (Compound I-4) is an inhibitor for hematopoietic progenitor kinase 1 (HPK1) with an IC50 >100 nM.
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PROTAC HPK1 Degrader-4
0 ImagesCat. No.: HY-174135PROTAC HPK1 Degrader-4 (compound E3) is a selective and orally active PROTAC HPK1 degrader with a DC50 of 3.16 nM. PROTAC HPK1 Degrader-4 demonstrates >1000-fold selectivity over GLK. PROTAC HPK1 Degrader-4 promotes immune activation. PROTAC HPK1 Degrader-4 can be used for the study of colon cancer and lymphoma (Pink: ligand for target protein (HY-174355); Blue: ligand for E3 ligase CRBN (HY-45808); Black: Linker (HY-174356); Target protein ligand-linker Conjugate (HY-174357)).
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HPK1-IN-2 TFA
0 ImagesCat. No.: HY-132150CPurity: 99.56%
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HPK1-IN-29
0 ImagesCat. No.: HY-143870CAS No.: 2699604-50-5HPK1-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).
