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SLP-76 phosphorylation

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-163372
    PROTAC HPK1 Degrader-1

    		PROTACs MAP4K Cancer
    PROTAC HPK1 Degrader-1 (Compound B1) is a potent HPK1 degrader with DC50 value of 1.8 nM. PROTAC HPK1 Degrader-1 inhibits phosphorylation of the SLP76 protein with IC50 value of 496.1 nM. PROTAC HPK1 Degrader-1 is a bona fide HPK1-PROTAC degrader, which provided a potential tool for further HPK1 investigation in TCR signaling .
    PROTAC HPK1 Degrader-1
  • HY-144088
    ZYF0033
    2 Publications Verification

    HPK1-IN-22

    		 MAP4K Inflammation/Immunology Cancer
    ZYF0033 is an orally active inhibitor of the hematopoietic progenitor cell kinase HPK1 with an IC50 of less than 10 nM based on the phosphorylation inhibition of MBP protein. ZYF0033 promotes anti-cancer immune responses and reduces phosphorylation of SLP76 (serine 376). ZYF0033 inhibits tumor growth in the 4T-1 syngeneic mouse model and leads to increased intratumoral infiltration of DCs, NK cells, and CD107a +CD8 + T cells, but not T cells, PD-1 +CD8 + T cells, TIM-3 +CD8 + Infiltration of T cells and LAG3 +CD8 + T cells was reduced .
    ZYF0033
  • HY-160940
    HPK1-IN-46

    		MAP4K Cancer
    HPK1-IN-46 (Compound 36) is an efficient and highly selective HPK1 reverse indazole inhibitor with an IC50 value of 1.1 nM. HPK1-IN-46 exhibits high selectivity for CDK2, JAK1, and JAK2. HPK1-IN-46 inhibits SLP76 phosphorylation mediated by HPK1, reverses T-cell inhibition, and enhances anti-tumor immunity. HPK1-IN-46 can be used in immunotherapy research for tumors .
    HPK1-IN-46
  • HY-163496
    HPK1-IN-45

    		MAP4K Cancer
    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-161335
    HPK1-IN-43

    		MAP4K Interleukin Related IFNAR Cancer
    HPK1-IN-43 (compound 9f) is a HPK1 kinase inhibitor with the IC50 value of 0.32 nM. HPK1-IN-43 inhibits the phosphorylation of the downstream protein SLP-76 and enhances the secretion of interleukin-2 (IL-2) and interferon-γ (IFN-γ). HPK1-IN-43 can be used in cancer research .
    HPK1-IN-43
  • HY-163717
    HPK1-IN-48

    		MAP4K Cancer
    HPK1-IN-48 (compound 14g) is a potent Hematopoietic Progenitor Kinase 1 (HPK1) inhibitor with a IC50 of 0.15 nM. HPK1-IN-48 significantly suppresses the phosphorylation of SLP76 with a IC50 of 27.92 nM .
    HPK1-IN-48
  • HY-149520
    HPK1-IN-39

    		MAP4K Cancer
    HPK1-IN-39 (Compound 10n) is a selective HPK1 Inhibitor (IC50: 29 nM). HPK1-IN-39 inhibits the phosphorylation of SLP76. HPK1-IN-39 can be used for research of cancer immunotherapy .
    HPK1-IN-39
  • HY-168282
    DD205-291

    		PROTACs MAP4K Cancer
    DD205-291 is an orally active PROTAC HPK1 degrader, with a DC50 value of 5.3 nM. DD205-291 inhibits SLP-76 phosphorylation and induces IL-2 and IFN-γ expression (Pink: HPK1 protein ligand HY-168283; E3+linker: HY-168284; Blue: E3: HY-W115490; Black: linker: HY-W210252) .
    DD205-291
  • HY-172594
    HPK1-IN-57

    		MAP4K Interleukin Related Inflammation/Immunology Cancer
    HPK1-IN-57 (Compound 10c) is a hematopoietic progenitor kinase 1 (HPK1) inhibitor with an IC50 value of 0.09 nM. HPK1-IN-57 inhibits the activity of HPK1 kinase, hindering the phosphorylation of the downstream adaptor protein SLP76 (IC50 is 33.74 nM) and effectively stimulating the secretion of the T cell activation marker IL-2 (EC50 is 84.24 nM). HPK1-IN-57 is promising for research of tumor immunotherapy .
    HPK1-IN-57
  • HY-179111
    HPK1-IN-64

    		MAP4K Interleukin Related Cancer
    HPK1-IN-64 is a potent, selective, and orally active HPK1 inhibitor with an IC50 value of 1.9 nM. HPK1-IN-64 exhibits selectivity exceeding 100-fold, 80-fold, 300-fold, and 350-fold against off-target kinases such as GLK, MAP4K5, TBK1, and TNIK, respectively. HPK1-IN-64 inhibits SLP76 protein phosphorylation and IL-2 secretion. HPK1-IN-64 may be used in cancer research, such as for colorectal cancer .
    HPK1-IN-64
  • HY-179727
    PROTAC HPK1 Degrader-7

    		PROTACs MAP4K Interleukin Related IFNAR Inflammation/Immunology
    PROTAC HPK1 Degrader-7 (compound D02) is a potent and selective PROTAC HPK1 degrader with an DC50 of 3.07 nM. PROTAC HPK1 Degrader-7 exhibits selectivity over GLK. PROTAC HPK1 Degrader-7 induces HPK1 degradation in a CRBN- and proteasome-dependent manner. PROTAC HPK1 Degrader-7 inhibits SLP-76 phosphorylation, induces IL-2 and IFN-γ secretion in human primary T cells. PROTAC HPK1 Degrader-7 can be used for immunology research .
    PROTAC HPK1 Degrader-7
  • HY-175547
    PROTAC HPK1 Degrader-5

    		PROTACs MAP4K ERK Interleukin Related IFNAR Inflammation/Immunology Cancer
    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-182238
    HPK1-IN-69

    		MAP4K Interleukin Related Cancer
    HPK1-IN-69 is an orally active HPK1 inhibitor with an IC50 of 1.7 nM. HPK1-IN-69 inhibits the HPK1-mediated TCR signaling pathway, reduces the phosphorylation level of SLP76, and promotes the release of IL-2. HPK1-IN-69 exhibits in vivo anti-tumor activity in mouse models. HPK1-IN-69 can be used for the research of colorectal cancer and MC38 syngeneic tumors .
    HPK1-IN-69
  • HY-179338
    HPK1-IN-65

    		MAP4K HOXA Interleukin Related Cancer
    HPK1-IN-65 is a selective and orally active HPK1 inhibitor with an IC50 value of < 5 nM. HPK1-IN-65 inhibits HPK1 kinase activity and displays 1257-fold selectivity over the MAP4K kinase family member GLK. HPK1-IN-65 exhibits an IC50 of 92.3 nM for inhibiting pSLP76 phosphorylation. HPK1-IN-65 demonstrates an EC50 of 398 nM for stimulating IL-2 production. HPK1-IN-65 inhibits TCR-induced phosphorylation of SLP76 at Ser376 in a dose-dependent manner. HPK1-IN-65 can be further utilized for colorectal cancer research .
    HPK1-IN-65
  • HY-181924
    HPK1-IN-68

    		MAP4K Interleukin Related Inflammation/Immunology Cancer
    HPK1-IN-68 (Compound 39) is a HPK1 inhibitor with an IC50 of 2.8 nM. HPK1-IN-68 blocks HPK1 signaling, inhibits HPK1-mediated phosphorylation of SLP76, and promotes the production of the IL-2 cytokine. HPK1-IN-68 antagonizes the immunosuppressive effect mediated by PGE2. HPK1-IN-68 enhances the infiltration of CD3 +/CD8 + T cells into tumor tissues. HPK1-IN-68 exerts T cell-dependent antitumor efficacy in a mouse colon cancer model. HPK1-IN-68 exhibits significant synergistic antitumor effects when used in combination with anti-PD-1. HPK1-IN-68 is applicable to research related to colon cancer .
    HPK1-IN-68

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