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 |
---|---|---|---|---|
V74418 | HPK1-IN-32 | 2766481-17-6 | HPK1-IN-32 is a potent and specific HPK1 inhibitor (antagonist) with IC50 of 65 nM. | |
V74423 | HPK1-IN-33 | 2920000-86-6 | HPK1-IN-33 (compound 21) is a potent inhibitor of hematopoietic progenitor kinase 1 (HPK1) with a Ki of 1.7 µM. | |
V74422 | HPK1-IN-34 | 2380300-99-0 | HPK1-IN-34 (Compound 143) is a hematopoietic progenitor kinase 1 (HPK1) inhibitor (antagonist) with IC50 <100 nM. | |
V74421 | HPK1-IN-35 | 2935903-77-6 | HPK1-IN-35 is a potent and specific HPK1 inhibitor (antagonist) with IC50 of 3.5 nM. | |
V79825 | HPK1-IN-36 | HPK1-IN-36 (compound 2) is a potent HPK1 inhibitor (antagonist) with IC50 of 0.5 nM. | ||
V74415 | HPK1-IN-37 | 2766481-68-7 | HPK1-IN-37 (compound A85) | |
V74414 | HPK1-IN-38 | 2578802-72-7 | HPK1-IN-38 (compound 15) is a MAP4K1/HPK1 inhibitor that may be utilized in the research/study of HPK1-related diseases. | |
V78722 | HPK1-IN-39 | HPK1-IN-39 (Compound 10n) is a selective HPK1 inhibitor (IC50= 29 nM). | ||
V74400 | HPK1-IN-4 | 2739844-28-9 | HPK1-IN-4 (comp 22) is an inhibitor (blocker/antagonist) of HPK1 (MAPK41) (IC50 = 0.061 nM) and may be used in immunological research. | |
V79108 | HPK1-IN-40-d2 | HPK1-IN-40 is a highly efficient and selective HPK1 inhibitor (antagonist) with IC50 of 0.9 nM. | ||
V60136 | HPK1-IN-7 | 2320462-65-3 | HPK1-IN-7 is a highly effective, orally active inhibitor of HPK1 (hematopoietic progenitor kinase 1, or MAP4K1) with excellent family and kinome selectivity (IC50=2.6 nM). | |
V74402 | HPK1-IN-8 | 1214561-09-7 | HPK1-IN-8 is an allosteric, inactive conformation-selective full-length HPK1 inhibitor. | |
V4602 | NG-25 | 1315355-93-1 | NG25 is a novel, potent and synthesized dual TAK1 (TGFβ-activated kinase 1) and MAP4K2 (mitogen-activated protein kinase kinase kinase kinase 2) inhibitor, with IC50s of 149 nM and 21.7 nM, respectively. | |
V3214 | PF-06260933 | 1811510-56-1 | PF-06260933 is a highly selective small-molecule inhibitor of MAP4K4 (Mitogen-activated protein kinase kinase kinase kinase 4) with IC50 values of 3.7 and 160 nM for cell-freel assay (kinase) and cell assay, respectively. | |
V76481 | SS47 TFA | SS47 TFA is a PROTAC-based HPK1 degrader that exerts proteasome-mediated degradation of HPK1. | ||
V74405 | TNIK&MAP4K4-IN-1 | 2478592-86-6 | TNIK&MAP4K4-IN-1 (compound A-39) is a dual (bifunctional) inhibitor of TNIK and MAP4K4/HGK with IC50 of 1.29 nM and <10 nM, respectively, in human hepatic stellate cells LX-2. |