hpk1

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.