MAP kinase kinase kinase kinases (MAP4Ks) belong to the mammalian Ste20-like family of serine/threonine kinases.According to studies, MAP4Ks such as MAP4K1/HPK1, MAP4K2/GCK, MAP4K3/GLK, MAP4K4/HGK, MAP4K5/KHS, and MAP4K6/MINK cause JNK activation by triggering the MAP3K-MAP2K cascade. The regulation of cell migration, autophagy, apoptosis, and survival is greatly influenced by MAP4Ks. According to a number of studies, MAP4Ks control immune-cell responses through JNK-independent pathways.
When T-cells are activated and inflammatory responses are triggered, MAP4K1/HPK1 and MAP4K4/HGK play harmful roles. In contrast, MAP4K3/GLK contributes to the activation of T cells and autoimmune responses. Additionally, human autoimmune diseases like psoriatic arthritis, rheumatoid arthritis (RA), adult-onset Still's disease, and SLE involve MAP4K1 downregulation and MAP4K3 overexpression in T cells.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V87077 | (3S,4R)-GNE-6893 | 2415374-97-7 | (3S,4R)-GNE-6893 is an orally available HPK1 inhibitor. |
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V94597 | BAY-405 | 2442532-66-1 | BAY-405 (compound 38) is a MAP4K1 inhibitor that exhibits nanomolar potency in biochemical and cellular assays and achieves in vivo exposure after oral administration. |
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V4271 | DMX-5804 | 2306178-56-1 | DMX-5804 is a novel, potent, orally bioactive and selectiveMAP4K4(Mitogen-activated protein kinase kinase kinase kinase-4) inhibitor with anIC50of 3 nM, apIC50of 8.55 for human MAP4K4, less potent on MINK1/MAP4K6 (pIC50, 8.18), and TNIK/MAP4K7 (pIC50, 7.96). |
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V77906 | DS21150768 | DS21150768 is a potent orally bioactive HPK1 inhibitor. | |
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V74401 | GNE-1858 | 2680616-96-8 | GNE-1858 is a potent ATP-competitive hematopoietic progenitor cell kinase-1 (HPK1) inhibitor, with IC50s of 1.9 nM, 1.9 nM, and 4.5 against wild-type and active mimic mutant strains HPK1-TSEE and HPK1-SA, respectively. |
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V4550 | GNE-495 | 1449277-10-4 | GNE-495 is a novel, potent and selectiveMAP4K4(mitogen-activated protein kinase kinase kinase kinase 4) inhibitor with anIC50of 3.7 nM.Diverse biological roles for mitogen-activated protein kinase kinase kinase kinase 4 (MAP4K4) have necessitated the identification of potent inhibitors in order to study its function in various disease contexts. |
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V74424 | GNE-6893 | 2415374-98-8 | GNE-6893 is an orally bioavailable HPK1 inhibitor. |
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V87083 | HMC-B17 | 2935913-83-8 | HMC-B17 is a selective, orally bioavailable HPK1 inhibitor (IC50 = 1.39 nM) that enhances anti-PD-L1 efficacy. |
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V74416 | HPK1 antagonist-1 | 2628489-56-3 | HPK1 antagonist-1 (I-792) is an Hpk1 antagonist that may be utilized in cancer and immune disease study. |
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V119094 | HPK1 ligand 4 | HPK1 ligand 4 is a PROTAC target protein ligand that can be used to synthesize PROTACs, such as PROTAC HPK1 degrader-5. | |
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V116635 | HPK1 ligand 6 | 3056139-31-9 | HPK1 ligand 6 is an HPK1 ligand. |
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V119247 | HPK1 ligand-Linker Conjugate 1 | 3061690-80-7 | HPK1 ligand-linker conjugate 1 is a synthetic target protein ligand-linker complex that can be used to synthesize PROTACs, such as PROTAC HPK1 degrader-5. |
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V74410 | HPK1-IN-10 | 2734168-69-3 | HPK1-IN-10 is an effective HPK1 inhibitor. |
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V74403 | HPK1-IN-11 | 2734167-68-9 | HPK1-IN-11 is an effective HPK1 inhibitor. |
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V74412 | HPK1-IN-12 | 2734168-51-3 | HPK1-IN-12 is an effective HPK1 inhibitor. |
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V74407 | HPK1-IN-13 | 2734168-30-8 | HPK1-IN-13 is an effective HPK1 inhibitor. |
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V74411 | HPK1-IN-14 | 2734168-45-5 | HPK1-IN-14 is an effective HPK1 inhibitor. |
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V74406 | HPK1-IN-15 | 2201098-03-3 | HPK1-IN-15 is a potent and specific HPK1 inhibitor. |
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V74409 | HPK1-IN-16 | 2294965-95-8 | HPK1-IN-16 is a potent and specific HPK1 inhibitor. |
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V74413 | HPK1-IN-17 | 2403600-07-5 | HPK1-IN-17 is a potent and specific HPK1 inhibitor. |
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