2. Signaling Pathways
  3. MAPK/ERK Pathway
  4. MAP4K
  5. MAP4K5/KHS1 Isoform

MAP4K5/KHS1

MAP4K5/KHS1, also called GCKR, encodes a human SPS1/STE20-like serine/threonine kinase that activates Jun N-terminal kinase (JNK) in mammalian cells[1]. Mechanistically, TNF-α recruits and activates GCKR through TRAF2, and TNF-induced GCKR/SAPK activation further depends on the Ubc13-Uev1A/TRAF2 complex[2][3]. In B lymphocytes, Wnt3a activates GCKR and JNK through APC-Asef-Rac, while GCKR also supports β-catenin accumulation, linking MAP4K5 to canonical and noncanonical Wnt signaling. Disease evidence remains focused on models and associations: MAP4K5 -822G/A associates with reduced type 2 diabetes risk in Shanghai Han subjects, and low MAP4K5 expression correlates with shorter survival and reduced E-cadherin in pancreatic ductal adenocarcinoma[4][5]. Compared with related MAP4K isoforms, KHS/MAP4K5 is distinguished from MAP4K1/HPK1, MAP4K2/GCK, MAP4K3/GLK, MAP4K4/HGK, MAP4K6/MINK1, and MAP4K7/TNIK within the STE20-like MAP4K family[6]. For research design, CRK-family adaptor binding and STRN4-containing MAP4K interactome data support MAP4K5 studies in kinase signaling, protein-interaction mapping, JNK activation, Wnt biology, and cancer-associated epithelial regulation[7][6][5].

MAP4K5/KHS1 Related Products (6):

Cat. No. Product Name Effect Purity
  • HY-111754
    DMX-5804
    		Inhibitor 99.83%
    DMX-5804 is a potent, orally active and selective MAP4K4 inhibitor, with an IC50 of 3 nM, a pIC50 of 8.55 for human MAP4K4, less potent on MINK1/MAP4K6 (pIC50, 8.18), and TNIK/MAP4K7 (pIC50, 7.96). DMX-5804 enhances cardiomyocyte survival, and reduces ischemia-reperfusion injury in mice.
  • HY-148061
    DB1113
    		99.86%
    DB1113 (Example 24) is a bifunctional compound targeted protein degradation of kinases. DB1113 degrades ABL1, ABL2, BLK, CDK11B, CDK4, CSK, EPHA3, FER, GAK, LIMK1, MAP3K20, MAP4K1, MAP4K2, MAP4K3, MAP4K5, MAPK14, MAPK7, MAPK8, MAPK9, MAPKAPK2, MAPKAPK3, NLK, PDIK1L, PTK2B, RIPK1, RPS6KA1, RPS6KA3, SIK2, SIK3, STK35, TNK2, and ULK1. DB1113 can be used for research of disease or disorder mediated by aberrant kinase activity.
  • HY-U00428A
    GNE 220 hydrochloride
    		Inhibitor 98.22%
    GNE 220 (hydrochloride) is a potent and selective inhibitor of MAP4K4, with an IC50 of 7 nM.
  • HY-U00428
    GNE 220
    		Inhibitor
    GNE-220 is a potent and selective inhibitor of MAP4K4 with an IC50 of 7 nM.
  • HY-172107
    HPK1-IN-56
    		Inhibitor
    HPK1-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.
  • HY-168110
    HPK1-IN-52
    		Inhibitor
    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.