2. Signaling Pathways
  3. MAPK/ERK Pathway
  4. MAP4K

MAP4K

MAPK Kinase Kinase Kinase

MAP4K

Related Products

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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:

MAP4K Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-177272
    HPK1-IN-61
    		Inhibitor
    HPK1-IN-61 (Compound 1) is an inhibitor of hematopoietic progenitor kinase 1 (HPK1) (Ki = 0.4 nM) and an inhibitor of Abl (IC50 < 0.51 nM). HPK1-IN-61 also shows inhibitory activity againstLCK with an IC50 of 24 nM.
    HPK1-IN-61
  • HY-153448
    HPK1-IN-36
    		Inhibitor
    HPK1-IN-36 (compound 2) is a potent HPK1 inhibitor with an IC50 value of 0.5 nM.
    HPK1-IN-36
  • HY-160217
    HPK1-IN-41
    HPK1-IN-41 (compound Z389) is an inhibitor of HPK1 with an IC50 value of 0.21 nM.
    HPK1-IN-41
  • HY-175547
    PROTAC HPK1 Degrader-5
    		Degrader
    PROTAC HPK1 Degrader-5 is a potent and orally active HPK1 PROTAC degrader (DC50 = 5.0 nM; Dmax ≥ 99%). PROTAC HPK1 Degrader-5 significantly inhibits SLP76 phosphorylation and enhanced ERK pathway activation through degrading HPK1, thereby stimulating IL-2 and IFN-γ release. PROTAC HPK1 Degrader-5 exhibits the ability to overcome the immunosuppressive effects imposed by PGE2, NECA or TGF-β. PROTAC HPK1 Degrader-5 alone efficaciously inhibits tumor growth in an MC38 syngeneic mouse model. PROTAC HPK1 Degrader-5 can be used for the study of tumor (such as colorectal cancer) immunotherapy (Pink: Target protein ligand (HY-175549); Blue: E3 ligand (HY-W023573); Black: Linker; E3 ligand + Linker (HY-175551)).
    PROTAC HPK1 Degrader-5
  • HY-175549
    HPK1 ligand 4
    		Ligand
    HPK1 ligand 4 is a PROTAC target protein ligand that can be used for synthesis of PROTACs, such as PROTAC HPK1 Degrader-5 (HY-175547). PROTAC HPK1 Degrader-5 is a potent and orally active HPK1 PROTAC degrader with anti-tumor activity.
    HPK1 ligand 4
  • HY-124152
    3,4-Dephostatin
    		Inhibitor
    3,4-Dephostatin (Methyl-3,4-dephostatin) is an inhibitor of protein-tyrosine phosphatase (PTPase). 3,4-Dephostatin accelerates nerve growth factor (NGF)-induced neurite formation in PC12h cells. 3,4-Dephostatin sustains the NGF-induced tyrosine phosphorylation of proteins, most prominently that of mitogen-activated protein (MAP) kinase. 3,4-Dephostatin also prolongs epidermal growth factor (EGF)-induced tyrosine phosphorylation and activation of MAP kinase.
    3,4-Dephostatin
  • HY-143868
    HPK1-IN-27
    		Inhibitor
    HPK1-IN-27 is a potent inhibitor of HPK1. MAP4K1 is also known as hematopoietic progenitor kinase 1 (HPK1). MAP4K1 is a serine/threonine kinase and member of the germinal center kinase family. HPK1-IN-27 has the potential for the research of cancer diseases (extracted from patent WO2019016071A1, compound 38).
    HPK1-IN-27
  • HY-151377
    RET-IN-19
    		Inhibitor
    RET-IN-19 (compound 59) is a potent RET inhibitor, with IC50 values of 6.8 and 13.51 nM against RET-wt and RET V804M, respectively. RET-IN-19 shows anticancer activity. RET-IN-19 can be used for non-small cell lung cancer (NSCLC) research.
    RET-IN-19
  • HY-172674
    HPK1-IN-59
    		Inhibitor
    HPK1-IN-59 (compound 39) is an orally active HPK1 inhibitor with an IC50 of 0.70 nM. HPK1-IN-59 has favorable oral bioavailability in mice.
    HPK1-IN-59
  • HY-146680
    FLT3/ITD-IN-4
    		Inhibitor
    FLT3/ITD-IN-4 (Compound 16) is a selective FMS-like tyrosine kinase 3 internal tandem duplications (FLT3-ITD) inhibitor with an IC50 of 2.3 nM. FLT3/ITD-IN-4 can be used for acute myeloid leukemia research.
    FLT3/ITD-IN-4
  • HY-163496
    HPK1-IN-45
    		Inhibitor
    HPK1-IN-45 (Compound 3) is a HPK1 inhibitor, with an IC50 of 0.3 nM. HPK1-IN-45 inhibits SLP-76 phosphorylation (IC50 = 57.52 nM) and IL-2 release (IC50 = 38 nM). HPK1-IN-45 can be used for the research of cancer.
    HPK1-IN-45
  • HY-149773S
    HPK1-IN-40-d2
    		Inhibitor
    HPK1-IN-40 (compound 49) is a potent and selective HPK1 inhibitor with an IC50 of 0.9 nM. HPK1-IN-40 reinvigorates T-cell receptor (TCR) signaling, promoting T-cell function and cytokine production in T cells while having anti-cancer activity.
    HPK1-IN-40-d<sub>2</sub>
  • HY-163495
    HPK1-IN-44
    		Inhibitor
    HPK1-IN-44 (Compound 1) is an inhibitor of HPK1 (IC50=0.1 nM (40 μM ATP)).
    HPK1-IN-44
  • HY-143869
    HPK1-IN-28
    		Inhibitor
    HPK1-IN-28 is a potent inhibitor of HPK1. Hematopoietic progenitor kinase 1 (HPK1) is a negative regulator of the activation response of dendritic cells (DCs), T cells and B cells. HPK1-IN-28 enhances the body's anti-tumor immunity. HPK1-IN-28 has the potential for the research of immune-related diseases, especially tumor (extracted from patent WO2021175270A1, compound 1).
    HPK1-IN-28
  • HY-149232
    HPK1-IN-35
    		Inhibitor
    HPK1-IN-35 is a potent and selective HPK1 inhibitor with an IC50 value of 3.5 nM. HPK1-IN-35 decreases the expression of p-SLP76 and promotes IL-2 secretion.
    HPK1-IN-35
  • HY-161917
    HPK1-IN-49
    		Inhibitor
    HPK1-IN-49 (Compound I-4) is an inhibitor for hematopoietic progenitor kinase 1 (HPK1) with an IC50 >100 nM.
    HPK1-IN-49
  • HY-174135
    PROTAC HPK1 Degrader-4
    		Degrader
    PROTAC HPK1 Degrader-4 (compound E3) is a selective and orally active PROTAC HPK1 degrader with a DC50 of 3.16 nM. PROTAC HPK1 Degrader-4 demonstrates >1000-fold selectivity over GLK. PROTAC HPK1 Degrader-4 promotes immune activation. PROTAC HPK1 Degrader-4 can be used for the study of colon cancer and lymphoma (Pink: ligand for target protein (HY-174355); Blue: ligand for E3 ligase CRBN (HY-45808); Black: Linker (HY-174356); Target protein ligand-linker Conjugate (HY-174357)).
    PROTAC HPK1 Degrader-4
  • HY-143870
    HPK1-IN-29
    		Inhibitor
    HPK1-IN-29 is a potent inhibitor of HPK1. Hematopoietic progenitor kinase 1 (HPK1) is a negative regulator of the activation response of dendritic cells (DCs), T cells and B cells. HPK1-IN-29 enhances the body's anti-tumor immunity. HPK1-IN-29 has the potential for the research of immune-related diseases, especially tumor (extracted from patent WO2021175270A1, compound 38).
    HPK1-IN-29
  • HY-162545
    HPK1-IN-47
    		Inhibitor
    HPK1-IN-47 is a HPK1 ligand. HPK1-IN-47 can be used for synthesis of PROTACs, such as PROTAC HPK1 Degrader-2 (HY-162544). HPK1-IN-47 can be used for research of HPK1-mediated diseases including cancer.
    HPK1-IN-47
  • 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.
    HPK1-IN-52
MAP4K Isoform Comparison

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