MAP4K
MAPK Kinase Kinase Kinase
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
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MAP4K Related Products (135)
Related Products (135)
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MAP4K Isoform Comparison
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TL4-12
0 ImagesTL4-12 is a selective MAP4K2/GCK inhibitor, dose-dependently downregulates IKZF1 and BCL-6 and leads to MM cell proliferation inhibition (IC50=37 nM) accompanied by induction of apoptosis. TL4-12 can be used to overcome immunomodulatory agent resistance in multiple myeloma (MM).
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SB1-G-187
0 ImagesSB1-G-187 is a multi-target kinase PROTAC degrader with activity against various kinases including GCK, YES1, IRAK1 and LYN. SB1-G-187 induces degradation of target kinases via a p97-dependent pathway, and forms ternary complexes with CRBN and specific functional kinases. SB1-G-187 can be used in tumor-related research.
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PROTAC HPK1 Degrader-1
0 ImagesPROTAC HPK1 Degrader-1 (compound B1) is a PROTAC degrader that recruits cereblon to induce HPK1 degradation, with a DC50 of 1.8 nM. PROTAC HPK1 Degrader-1 inhibits HPK1 kinase activity, with an IC50 of 140.5 nM. PROTAC HPK1 Degrader-1 suppresses the phosphorylation of SLP76 protein, with an IC50 of 496.1 nM. PROTAC HPK1 Degrader-1 can be used to investigate non-kinase-dependent signaling of HPK1 in the TCR pathway and cancer-related research.
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Pyrrolo[2,1-f][1,2,4]triazin-4-amine
![Pyrrolo[2,1-f][1,2,4]triazin-4-amine](https://file.medchemexpress.com/product_pic/hy-w003471.gif "Click to View Pyrrolo[2,1-f][1,2,4]triazin-4-amine Product Detail")
0 ImagesCat. No.: HY-W003471CAS No.: 159326-68-8Pyrrolo[2,1-f][1,2,4]triazin-4-amine is a MAP4K4 inhibitor with a surface plasmon resonance (SPR) Kd of 88 μM and a ligand efficiency of 0.56.
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GNE-1858
0 ImagesGNE-1858 is a potent and ATP-competitive hematopoietic progenitor kinase-1 (HPK1) inhibitor, with IC50s of 1.9 nM, 1.9 nM, and 4.5 nM for wild-type and the active mimetic mutants HPK1-TSEE and HPK1-SA, respectively.
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TINK-IN-1
0 ImagesTINK-IN-1 (Compound 9) is a potent and selective Traf2- and Nck-interacting kinase (TNIK) inhibitor with an IC50 of 8 nM. TINK-IN-1 inhibits colorectal cancer cells viability.
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HPK1-IN-4
0 ImagesHPK1-IN-4 (comp 22) is a HPK1 (MAPK41) inhibitor (IC50 of 0.061 nM) as preclinical immunoresearch tool compound.
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HPK1-IN-34
0 ImagesCat. No.: HY-153362CAS No.: 2380300-99-0HPK1-IN-34 (Compound 143) is a Hematopoietic progenitor kinase 1 (HPK1) inhibitor with an IC50 of <100 nM. HPK1-IN-34 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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GNE-6893
0 ImagesGNE-6893 is an orally active, selective HPK1 inhibitor with a Ki < 0.02 nM. GNE-6893 enhances T cell receptor signaling in primary human T cells. GNE-6893 increases IL2 production in stimulated primary human T cells. GNE-6893 can be used for the research of chronic refractory cancers.
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GNE 220 hydrochloride
0 ImagesGNE 220 (hydrochloride) is a potent and selective inhibitor of MAP4K4, with an IC50 of 7 nM.
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SS47 TFA
0 ImagesCat. No.: HY-146231APurity: 99.55%SS47 TFA is a hematopoietic progenitor kinase HPK1 PROTAC-class degrader and immune activator. SS47 TFA promotes the proliferation of CD4+ and CD8+ T cells as well as IFN-γ secretion, and enhances the anti-tumor cytotoxicity and in vivo efficacy of BCMA CAR-T cells. SS47 TFA also inhibits tumor growth in mouse models, and when combined with anti-PD-1 therapy, it improves the immune response of 4T1 tumor-bearing mice. SS47 TFA can be used in breast cancer-related research.
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HPK1-IN-19
0 ImagesHPK1-IN-19 (Compound I-47) is a hematopoietic progenitor kinase 1 (HPK1) inhibitor.
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TNIK&MAP4K4-IN-1
0 ImagesTNIK&MAP4K4-IN-1 (compound A-39) is a dual inhibitor of TNIK and MAP4K4/HGK with IC50s of 1.29 nM and <10 nM，respectively，in human hepaticstellate cell LX-2. TNIK&MAP4K4-IN-1 can be used for cancer and fibrosis inhibition.
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PROTAC HPK1 Degrader-5
0 ImagesCat. No.: HY-175547CAS No.: 3108744-13-1PROTAC HPK1 Degrader-5 is an orally effective and selective HPK1 PROTAC degrader with a DC50 of 5.0 nM. PROTAC HPK1 Degrader-5 recruits the CRBN E3 ligase to specifically induce the degradation of HPK1 via the ubiquitin-proteasome system, which in turn significantly inhibits SLP76 phosphorylation and enhances the activation of the ERK pathway, thereby stimulating the release of IL-2 and IFN-γ. PROTAC HPK1 Degrader-5 can be used in studies related to tumor immunity (e.g., colorectal cancer).
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NDI-101150
0 ImagesCat. No.: HY-159643CAS No.: 2628486-22-4NDI-101150 is an orally active, potent and selective hematopoietic progenitor cell kinase 1 (HPK1) inhibitor with an IC50 of 0.7 nM. NDI-101150 blocks HPK1-mediated negative regulation of immune receptor signaling, inhibits immunosuppression of T cell activation, enhances antigen-specific antibody production and augments B-cell activation. NDI-101150 inhibits tumor growth in syngeneic tumor models, establishes durable antitumor immune memory, and synergizes with anti-PD1 to enhance exhausted T cell activity and drive tumor regressions. NDI-101150 can be used for the research of cancer, such as breast cancer and colon cancer.
