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 (135)
Related Products (135)
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MAP4K Isoform Comparison
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CA/PRAK-IN-1
0 ImagesCat. No.: HY-184792CA/PRAK-IN-1 is a dual inhibitor of carbonic anhydrase (Carbonic Anhydrase) and PRAK, with a Ki of 20.1 nM against hCA IX and 16.4 nM against hCA XII. CA/PRAK-IN-1 exhibits inhibitory activity against YES1 kinase, BTK, and MAP4K3. CA/PRAK-IN-1 induces G0/G1 phase arrest of the cancer cell cycle, inhibits DNA synthesis, disrupts hypoxia-driven survival pathways, promotes cell death, and shows broad-spectrum cytotoxicity against tumor cells. CA/PRAK-IN-1 can be used in research on various cancers including leukemia, colon cancer, melanoma, and renal cancer.
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HPK1-IN-62
0 ImagesCat. No.: HY-178097HPK1-IN-62 is a selective and orally active HPK-1 inhibitor with an IC50 of 1.22 nM. HPK1-IN-62 significantly improves GLK selectivity (> 665-fold) and LCK selectivity (> 1095-fold). HPK1-IN-62 enhances T-cell activation and demonstrated synergistic effects when combined with anti-mPD-1 therapy in the MC38 tumor model, inhibiting a tumor growth. HPK1-IN-62 can be used in the researchs of colon cancer and cancer immunotherapy.
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HPK1-IN-57
0 ImagesCat. No.: HY-172594HPK1-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.
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HPK1 antagonist-1
0 ImagesCat. No.: HY-153553CAS No.: 2628489-56-3HPK1 antagonist-1 (I-792) is an Hpk1 antagonist that can be used in the study of cancer and immune disease.
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HPK1-IN-21
0 ImagesCat. No.: HY-144073CAS No.: 2413804-83-6HPK1-IN-21 is a potent inhibitor of HPK1 kinase inhibitor (Ki=0.8 nM). HPK1-IN-21 also has orally active.
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HDM2004
0 ImagesCat. No.: HY-181932CAS No.: 2953016-30-1HDM2004 is a selective, orally active, blood-brain barrier-penetrant HPK1 inhibitor with an IC50 of 1.89 nM. HDM2004 exhibits anticancer activity against colon cancer. HDM2004 shows synergistic activity when combined with anti-PD-L1 in syngeneic mouse models. HDM2004 can be used for the research of colon cancer.
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HPK1 ligand-Linker Conjugate 1
0 ImagesCat. No.: HY-175551CAS No.: 3061690-80-7
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PROTAC HPK1 Degrader-2
0 ImagesCat. No.: HY-162544CAS No.: 2893885-31-7PROTAC HPK1 Degrader-2 (compound 3) is a PROTAC degrader targeting hematopoietic progenitor kinase MAP4K1/HPK1, with a DC50 of 23 nM in human PBMCs. PROTAC HPK1 Degrader-2 is applicable for cancer research.
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HPK1-IN-39
0 ImagesCat. No.: HY-149520HPK1-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.
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PF-06745013
0 ImagesCat. No.: HY-123965CAS No.: 2089334-01-8PF-06745013 (Compound 37) is a MAP4K4 inhibitor without time-dependent inhibition (TDI) risk of CYP3A4 (IC50 of 0.4 nM for MAP4K4). PF-06745013 has no accumulation CNS-impaired and non-ATP competitive activities in mouse models. PF-06745013 can be used for inflammatory diseases like diabetes and cancers research.
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HPK1-IN-56
0 ImagesCat. No.: HY-172107CAS No.: 2901054-39-3HPK1-IN-56 (Compound A29) is a HPK1 inhibitor (IC50: 2.70 nM). HPK1-IN-56 inhibits downstream p-SLP76 (IC50: 8.1 nM in Jurkat T cells). HPK1-IN-56 induces the production of IL-2 in human PBMCs. HPK1-IN-56 has anticancer effect, enhances T-cell killing ability and the antitumor efficacy of anti-PD-1 antibody.
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HMC-B17
0 ImagesCat. No.: HY-157838CAS No.: 2935913-83-8
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HPK1-IN-58
0 ImagesCat. No.: HY-172875CAS No.: 3093724-62-7HPK1-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.
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HPK1-IN-61
0 ImagesCat. No.: HY-177272CAS No.: 875638-86-1
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HPK1-IN-36
0 ImagesCat. No.: HY-153448CAS No.: 2738518-06-2HPK1-IN-36 (compound 2) is a potent HPK1 inhibitor with an IC50 value of 0.5 nM.
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HPK1-IN-41
0 ImagesCat. No.: HY-160217CAS No.: 2828455-23-6HPK1-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.
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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.
