hpk1

HPK1-IN-36 (compound 2) is a potent inhibitor of hematopoietic progenitor kinase 1 (HPK1), demonstrating an inhibitory concentration 50 (IC50) of 0.5 nM [1].

HPK1-IN-4 is an HPK1 (MAPK41) inhibitor with an IC 50 of 0.061 nM. HPK1-IN-4 is often used as a preclinical immunotherapy tool compound.

GNE-1858 is an ATP-competitive hematopoietic progenitor kinase-1 (HPK1) inhibitor (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).

HPK1-IN-8 is an allosteric, inactive, conformation-selective triazolopyrimidine ketone HPK1 inhibitor.

PROTACHPK1 Degrader-1 (Compound B1) is a potent HPK1 degrader with a DC50 value of 1.8 nM. It effectively inhibits the phosphorylation of the SLP76 protein, with an IC50 of 496.1 nM. As a genuine HPK1-PROTAC degrader, PROTACHPK1 Degrader-1 offers a valuable tool for further investigation into HPK1 in TCR signaling pathways.

HPK1 ligand 3-dimethylph tetrahydropyridine is a Target Protein Ligand-Linker Conjugate. It is utilized in the synthesis of PROTACHPK1 Degrader-4.

HPK1 ligand 3 is a PROTAC target protein ligand (ligand for target protein for PROTAC) used in the synthesis of PROTAC HPK1 Degrader-4.

PROTACHPK1 Degrader-5 is a potent, orally active HPK1 PROTAC degrader with a DC50 of 5.0 nM and a Dmax of at least 99%. It significantly inhibits HPK1 by degrading it, reducing SLP76 phosphorylation, and enhancing ERK pathway activation, which in turn stimulates the release of IL-2 and IFN-γ. This compound effectively counteracts immune suppression induced by PGE2, NECA, or TGF-β. Alone, PROTACHPK1 Degrader-5 is capable of suppressing tumor growth in MC38 syngeneic mouse models. It is used in research for immunotherapy applications in cancers such as colorectal cancer.

HPK1 ligand 4 is a PROTAC (proteolysis-targeting chimeras) target protein ligand used in the synthesis of PROTACs, such as PROTACHPK1 Degrader-5. PROTACHPK1 Degrader-5 is a potent and orally active HPK1 PROTAC degrader demonstrating antitumor activity.

HPK1 ligand-Linker Conjugate 1 is a synthetic target protein ligand-linker compound used in the synthesis of PROTACs, such as PROTACHPK1 Degrader-5. PROTACHPK1 Degrader-5 is a potent and orally active HPK1 PROTAC degrader with anti-tumor activity.

HPK1 ligand 6 is an HPK1 ligand that can be used for the synthesis of PROTAC[HPK1 Degrader-6].

PROTACHPK1 Degrader-7 (compound D02) is a potent and selective PROTACHPK1 degrader with a DC50 of 3.07 nM, showing selectivity for GLK. It induces HPK1 degradation in a CRBN and proteasome-dependent manner. Additionally, PROTACHPK1 Degrader-7 inhibits the phosphorylation of SLP-76 and stimulates the secretion of IL-2 and IFN-γ by human primary T cells, making it useful for immunological research.

HPK1 antagonist-1 (I-792) is an HPK1 inhibitor with potential applications in cancer and immune disease research [1].

PROTACHPK1 Degrader-4 (compound E3) is an orally active, selective PROTACHPK1 degrader with a DC50 of 3.16 nM. It exhibits over 1000 times greater selectivity for PROTACHPK1 compared to GLK. PROTACHPK1 Degrader-4 enhances immune activation and is useful in research for colon cancer and lymphoma.

PROTACHPK1 Degrader-2 (compound 3) is a PROTAC degrader of HPK1, exhibiting a DC50 of 23 nM in human PBMCs. This compound plays a crucial role in cancer research.

HPK1-IN-34 (Compound 143) is an inhibitor of HPK1 (Haematopoietic progenitor kinase 1) with an IC₅₀ < 0.1 μM, suitable for cancer and immunology research.

HPK1-IN-52 is an effective orally active hematopoietic progenitor kinase 1 (HPK1) inhibitor, displaying anti-tumor activity with an IC50 value of 10.4 nM.

HPK1 Ligand 2 is a PROTAC target protein ligand (Ligand for Target Protein for PROTAC). It is utilized in the synthesis of DD205-291.

HPK1-IN-54 (Compound 16) is a potent inhibitor of HPK1 (hematopoietic progenitor kinase 1), enhancing T cell activation and proliferation by blocking HPK1 activity to exert antitumor effects. It has an IC50 of 2.67 nM for HPK1, showing excellent selectivity over the MAP4K family (>100-fold) and other selected kinases (>300-fold). HPK1-IN-54 exhibits moderate in vivo clearance and reasonable oral exposure in both mice and rats. Additionally, in the CT26 mouse colon cancer model, HPK1-IN-54 demonstrates significant antitumor activity and shows a synergistic effect when combined with anti-PD-1 therapy. HPK1-IN-54 holds promise for research in the field of immunology.

HPK1-IN-55 (compound 19) is a selective and orally active inhibitor of hematopoietic progenitor kinase 1 (HPK1) with an IC50 of less than 0.51 nM. It exhibits exceptional kinase selectivity, being over 637 times more selective for HPK1 compared to GCK kinase and over 1022 times compared to LCK. HPK1-IN-55 possesses anti-cancer properties.

HPK1-IN-56 (Compound A29) is an HPK1 inhibitor with an IC50 of 2.70 nM. It inhibits downstream p-SLP76 in Jurkat T cells with an IC50 of 8.1 nM. Additionally, HPK1-IN-56 induces IL-2 production in human PBMCs. This compound exhibits anticancer properties, enhancing T cell cytotoxicity and the antitumor efficacy of anti-PD-1 antibodies.

HPK1-IN-57 (Compound 10c) is an inhibitor of hematopoietic progenitor kinase 1 (HPK1) with an IC50 of 0.09 nM. It suppresses the activity of HPK1 kinase, inhibits the phosphorylation of downstream adaptor protein SLP76 (IC50 of 33.74 nM), and effectively induces the secretion of the T cell activation marker IL-2 (EC50 of 84.24 nM). HPK1-IN-57 holds promise for research in tumor immunotherapy.

HPK1-IN-58 is an inhibitor of HPK1 (IC50: 2.6 nM) and SLP76 (IC50: 20 nM). It enhances IL-2 secretion, thereby reversing PGE2-induced immunosuppression. HPK1-IN-58 is applicable for research in antitumor immunity.

HPK1-IN-43 (compound 9f) is an HPK1 kinase inhibitor with an IC50 value of 0.32 nM. It inhibits the phosphorylation of the downstream protein SLP-76 in PBMC cells and enhances the secretion of interleukin 2 (IL-2) and interferon-γ (IFN-γ). HPK1-IN-43 is applicable to cancer research.