MAP4K

MAP4K inhibitors act on Ste20-related serine/threonine kinases at the top of stress-activated kinase cascades. Mitogen-activated protein kinase kinase kinase kinases (MAP4Ks) include hematopoietic progenitor kinase 1 (HPK1, MAP4K1), germinal center kinase (GCK, MAP4K2) and HPK/GCK-like kinase (HGK, MAP4K4). In 1995 human GCK was shown to activate the stress-activated protein kinase (SAPK) pathway. HPK1 was reported in 1996 to activate the c-Jun N-terminal kinase (JNK) cascade in hematopoietic cells. GNE-495 and PF-6260933 inhibit MAP4K4, while HPK1 is targeted by the inhibitor PF-07265028 and by SS47 TFA, a proteolysis-targeting chimera (PROTAC) degrader. NG25 inhibits MAP4K2 and transforming growth factor β-activated kinase 1 (TAK1), and NCB-0846 targets Traf2- and Nck-interacting kinase (TNIK).

2 Items

  • SS47 TFA
    Cat. No.
    A23977

    SS47 TFA

    SS47 TFA is a PROTAC-based degrader targeting hematopoietic progenitor kinase 1 (HPK1), an immunosuppressive regulatory kinase. It induces proteasome-mediated degradation of HPK1 and significantly enhances the antitumor efficacy of BCMA CAR-T cell therapy in vivo. In addition to its biological function, SS47 TFA is also a click chemistry reagent containing an alkyne group, allowing it to participate in copper-catalyzed azide–alkyne cycloaddition (CuAAC) with azide-functionalized molecules. This dual functionality makes SS47 TFA a valuable tool in both cancer immunotherapy research and chemical biology applications.

    1 mg
    $405.00
    5 mg
    $1,215.00
    All 4 sizes
  • DB1113
    Cat. No.
    A24837

    DB1113

    DB1113 is a bifunctional compound designed for targeted protein degradation of various kinases. It effectively induces degradation of ABL1, ABL2, BLK, CDK4, CDK11B, EPHA3, MAPK7, RIPK1, and others, facilitating the investigation of kinase-related signaling pathways. DB1113 is suitable for research focusing on diseases or disorders associated with dysregulated kinase activity, providing a valuable tool for exploring therapeutic interventions in cancer and other conditions.

    5 mg
    $695.00
    10 mg
    $1,220.00
    All 2 sizes

2 Items

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