Search Result
Results for "
HPK1
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
1
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-148847
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MAP4K
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Cancer
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HPK1-IN-32 is a potent and selective HPK1 inhibitor with an IC50 of 65 nM. HPK1-IN-32 can be used for the research of HPK1 related disorders or diseases [1].
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- HY-138568
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MAP4K
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Inflammation/Immunology
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HPK1-IN-3 is a potent and selective ATP-competitive hematopoietic progenitor kinase 1 (HPK1; MAP4K1) inhibitor with an IC50 of 0.25 nM. HPK1-IN-3 has IL-2 cellular potency with an EC50 of 108 nM in human peripheral blood mononuclear cells (PBMCs) [1].
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- HY-138742
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MAP4K
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Cancer
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HPK1-IN-7 is a potent, orally active HPK1 (hematopoietic progenitor kinase 1, MAP4K1) inhibitor (IC50=2.6 nM) with excellent family and kinome selectivity. HPK1-IN-7 shows selectivity against IRAK4 (59 nM) and GLK (140 nM). HPK1-IN-7 shows robust efficacy against MC38 syngeneic tumor model in combination with anti-PD1 [1].
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- HY-163372
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PROTACs
MAP4K
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Cancer
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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 [1].
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- HY-144093
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MAP4K
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Infection
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HPK1/GLK-IN-1 is a HPK1 and GLK inhibitor. HPK1/GLK-IN-1 (compound 38) potently inhibits GLK with an IC50 of 33 nM . HPK1-IN-26 can be used for the research of animal pathogen infection [1].
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- HY-W058423
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Drug Intermediate
MAP4K
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Cardiovascular Disease
Inflammation/Immunology
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6-Bromo-3-fluoropyridine-2-carbaldehyde (synthetic intermediate of Compound I-90) is a synthetic intermediate. 6-Bromo-3-fluoropyridine-2-carbaldehyde can be used in the synthesis of HPK1 inhibitors. 6-Bromo-3-fluoropyridine-2-carbaldehyde is applicable to research on immune diseases and hematological diseases [1].
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- HY-135892
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MAP4K
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Inflammation/Immunology
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GNE-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 [1].
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- HY-144088
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ZYF0033
2 Publications Verification
HPK1-IN-22
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MAP4K
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Inflammation/Immunology
Cancer
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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 [1] .
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- HY-157149
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MAP4K
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Cancer
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DS21150768 is a potent, orally active HPK1 inhibitor. DS21150768 shows potent activity to enhance T-cell function. DS21150768 has anticancer effects [1].
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- HY-173006
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MAP4K
Interleukin Related
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Cancer
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AZ3246 is an orally active and selective inhibitor of HPK1 with an IC50 of < 3 nM. AZ3246 induces IL-2 secretion in T cells with an EC50 of 90 nM. AZ3246 is a low-clearance antitumor compound that can be used for the study of breast cancer [1].
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- HY-175551
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Target Protein Ligand-Linker Conjugates
MAP4K
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Cancer
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HPK1 ligand-Linker Conjugate 1 is a synthesized target protein ligand-linker conjugate 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 [1].
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- HY-159643
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MAP4K
IFNAR
Interleukin Related
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Inflammation/Immunology
Cancer
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NDI-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 [1] .
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- HY-149056
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MAP4K
Interleukin Related
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Cancer
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GNE-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 [1].
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- HY-146231
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PROTACs
MAP4K
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Inflammation/Immunology
Cancer
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SS47, a PROTAC-based HPK1 degrader, exerts proteasome-mediated HPK1 degradation. The degradation of HPK1 via SS47 also significantly enhances the antitumor efficacy [1].
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- HY-174357
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Target Protein Ligand-Linker Conjugates
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Cancer
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HPK1 ligand 3-dimethylph tetrahydropyridine is a Target Protein Ligand-Linker Conjugate. HPK1 ligand 3-dimethylph tetrahydropyridine can be used to synthesize PROTAC HPK1 Degrader-4 (HY-174135) [1].
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- HY-146231A
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MAP4K
PROTACs
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Inflammation/Immunology
Cancer
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SS47 TFA, a PROTAC-based HPK1 degrader, exerts proteasome-mediated HPK1 degradation. The degradation of HPK1 via SS47 also significantly enhances the in vivo antitumor efficacy of BCMA CAR-T cell research. HPK1, an immunosuppressive regulatory kinase, is a promising target for cancer immunotherapies [1]. SS47 (TFA) 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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- HY-160940
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MAP4K
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Cancer
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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 [1].
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- HY-145107
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- HY-153362
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MAP4K
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Cancer
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HPK1-IN-34 (Compound 143) is a Hematopoietic progenitor kinase 1 (HPK1) inhibitor with an IC50 of <100 nM [1]. 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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- HY-178459
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PROTACs
MAP4K
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Cancer
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PROTAC HPK1 Degrader-6 (314) is a highly efficient and effective PROTAC degrader targeting HPK1 (IC50 < 50 nM). PROTAC HPK1 Degrader-6 can be used for the study of leukemia. Red: HPK1 ligand (HY-179196); Blue: E3 ligase CRBN ligand (HY-179197) [1].
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- HY-174135
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PROTACs
MAP4K
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Cancer
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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)) [1].
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- HY-174355
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- HY-153553
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- HY-162544
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PROTACs
MAP4K
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Cancer
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PROTAC HPK1 Degrader-2 (compound 3) is a PROTAC degrader of HPK1, with the DC50 of 23 nM in human PBMC. PROTAC HPK1 Degrader-2 plays an important role in cancer research [1].
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- HY-145035
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MAP4K
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Inflammation/Immunology
Cancer
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HPK1-IN-9 is potent inhibitor of HPK1. HPK1 is a serine/threonine protein kinase cloned from hematopoietic progenitor cells and belongs to the MAP4K family of mammalian Ste-20-related protein kinases. HPK1-IN-9 has the potential for the research of HPK1 related diseases (extracted from patent WO2021213317A1, compound 112) [1].
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- HY-175547
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PROTACs
MAP4K
ERK
Interleukin Related
IFNAR
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Inflammation/Immunology
Cancer
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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)) [1].
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- HY-162816
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PROTACs
MAP4K
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Cancer
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PROTAC HPK1 Degrader-3 (compound C3) is an orally effective PROTAC targeting HPK1 (DC50=21.26 nM). HPK1 is a negative regulator of T cell receptors, which can lead to T cell dysfunction after abnormal activation. PROTAC HPK1 Degrader-3 can inhibit SLP76 and NF-κB signaling pathways and inhibit MAPK signal transduction, and has anticancer activity and immune activation. PROTAC HPK1 Degrader-3 has a certain oral bioavailability and can be combined with PD-L1 antibody therapy to achieve a tumor growth inhibition rate of 65.58%. PROTAC HPK1 Degrader-3 is composed of E3 ligase ligand Thalidomide (HY-14658; blue part), PROTAC linker tert-Butyl 3-oxoazetidine-1-carboxylate (HY-40146; black part), and target protein ligand HPK1-IN-51 (HY-162842; red part); the activity control of the target protein ligand can be HPK1 ligand 1 (HY-162841) [1] .
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- HY-132150A
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- HY-168283
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- HY-162841
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Ligands for Target Protein for PROTAC
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Cancer
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HPK1 ligand 1 is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs). HPK1 ligand 1 can be used for synthesis PROTAC PD-L1 degrader-2 (HY-162816) [1].
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- HY-153448
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MAP4K
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Cancer
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HPK1-IN-36 (compound 2) is a potent HPK1 inhibitor with an IC50 value of 0.5 nM [1].
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- HY-177272
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MAP4K
Bcr-Abl
Src
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Others
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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 against LCK with an IC50 of 24 nM [1].
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- HY-179196
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- HY-179727
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PROTACs
MAP4K
Interleukin Related
IFNAR
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Inflammation/Immunology
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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 [1].
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- HY-160217
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MAP4K
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Cancer
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HPK1-IN-41 (compound Z389) is a HPK1 inhibitor with an IC50 value of 0.21 μM. HPK1-IN-41 can be used for the research of preventing and/or treating diseases or conditions associated with HPK1 activity [1].
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- HY-175347
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- HY-156508
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MAP4K
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Cancer
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HPK1-IN-37 (compound A85) is an inhibitor of HPK1 (IC50=3.7 nM). HPK1-IN-37 can be used for research in HPK1 related disorders or diseases including cancers [1].
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- HY-145109
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- HY-152257
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MAP4K
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Inflammation/Immunology
Cancer
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HPK1-IN-31 (compound 5i) is an orally active hematopoietic progenitor kinase 1 (HPK1) inhibitor with an IC50 value of 0.8 nM. HPK1-IN-31 has anti-tumour activity and has great potential for immunoresearch [1].
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- HY-172594
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MAP4K
Interleukin Related
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Inflammation/Immunology
Cancer
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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 [1].
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- HY-144091
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MAP4K
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Cancer
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HPK1-IN-24 (example 51) is a hematopoietic progenitor kinase 1 (HPK1) inhibitor with a Ki of 100 nM. HPK1-IN-24 has the potential for cancer research [1].
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- HY-144092
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MAP4K
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Cancer
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HPK1-IN-25 (example 94) is a hematopoietic progenitor kinase 1 (HPK1) inhibitor with a enzymatic activity IC50 of 129 nM. HPK1-IN-25 has the potential for cancer research [1].
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- HY-168110
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MAP4K
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Cancer
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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 [1].
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- HY-163717
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MAP4K
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Cancer
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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 [1].
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- HY-145039
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MAP4K
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Inflammation/Immunology
Cancer
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HPK1-IN-13 is potent inhibitor of HPK1. HPK1 is a serine/threonine protein kinase cloned from hematopoietic progenitor cells and belongs to the MAP4K family of mammalian Ste-20-related protein kinases. HPK1-IN-13 has the potential for the research of HPK1 related diseases (extracted from patent WO2021213317A1, compound 64) [1].
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- HY-145038
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MAP4K
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Inflammation/Immunology
Cancer
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HPK1-IN-12 is potent inhibitor of HPK1. HPK1 is a serine/threonine protein kinase cloned from hematopoietic progenitor cells and belongs to the MAP4K family of mammalian Ste-20-related protein kinases. HPK1-IN-12 has the potential for the research of HPK1 related diseases (extracted from patent WO2021213317A1, compound 85) [1].
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- HY-145040
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MAP4K
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Inflammation/Immunology
Cancer
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HPK1-IN-14 is potent inhibitor of HPK1. HPK1 is a serine/threonine protein kinase cloned from hematopoietic progenitor cells and belongs to the MAP4K family of mammalian Ste-20-related protein kinases. HPK1-IN-14 has the potential for the research of HPK1 related diseases (extracted from patent WO2021213317A1, compound 79) [1].
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- HY-145037
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MAP4K
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Inflammation/Immunology
Cancer
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HPK1-IN-11 is potent inhibitor of HPK1. HPK1 is a serine/threonine protein kinase cloned from hematopoietic progenitor cells and belongs to the MAP4K family of mammalian Ste-20-related protein kinases. HPK1-IN-11 has the potential for the research of HPK1 related diseases (extracted from patent WO2021213317A1, compound 2) [1].
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- HY-145036
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MAP4K
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Inflammation/Immunology
Cancer
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HPK1-IN-10 is potent inhibitor of HPK1. HPK1 is a serine/threonine protein kinase cloned from hematopoietic progenitor cells and belongs to the MAP4K family of mammalian Ste-20-related protein kinases. HPK1-IN-10 has the potential for the research of HPK1 related diseases (extracted from patent WO2021213317A1, compound 103) [1].
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- HY-149206
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MAP4K
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Cancer
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HPK1-IN-33 (compound 21) is a potent Hematopoietic Progenitor Kinase 1 (HPK1) inhibitor with a Ki value of 1.7 nM. HPK1-IN-33 inhibits the produce of IL-2 with EC50s of 286, >10000 nM in Jurkat WT and Jurkat HPK1 KO cells, respectively [1].
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- HY-170365
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MAP4K
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Inflammation/Immunology
Cancer
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HPK1-IN-55 (compound 19) is a selective and orally active hematopoietic progenitor kinase 1 (HPK1) inhibitor with an IC50 of <0.51 nM. HPK1-IN-55 shows excellent kinase selectivity (>637-fold vs GCK-like kinase and >1022-fold vs LCK). HPK1-IN-55 has anticancer effects [1].
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- HY-143869
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MAP4K
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Cancer
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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) [1].
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- HY-143870
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MAP4K
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Cancer
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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) [1].
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- HY-178097
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MAP4K
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Cancer
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HPK1-IN-62 is a selective and orally active HPK-1 inhibitor with an IC50 of 1.22 nM. HPK1-IN-62 significantly improves GLK selectivity (> 665-fold) and LCK selectivity (> 1095-fold). HPK1-IN-62 enhances T-cell activation and demonstrated synergistic effects when combined with anti-mPD-1 therapy in the MC38 tumor model, inhibiting a tumor growth. HPK1-IN-62 can be used in the researchs of colon cancer and cancer immunotherapy [1].
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- HY-175549
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Ligands for Target Protein for PROTAC
MAP4K
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Cancer
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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 [1].
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- HY-145041
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MAP4K
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Inflammation/Immunology
Cancer
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HPK1-IN-15 is a potent and selective inhibitor of HPK1. Hematopoietic progenitor kinase 1 (HPKl) originally cloned from hematopoietic progenitor cells is a member of MAP kinase kinase kinase kinases (MAP4Ks) family. HPK1-IN-15 is useful in researching, preventing or ameliorating diseases or disorders associated with HPK1 activity such as cancer (extracted from patent WO2018049200A1, compound 50) [1].
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- HY-145042
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MAP4K
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Inflammation/Immunology
Cancer
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HPK1-IN-16 is a potent and selective inhibitor of HPK1. Hematopoietic progenitor kinase 1 (HPKl) originally cloned from hematopoietic progenitor cells is a member of MAP kinase kinase kinase kinases (MAP4Ks) family. HPK1-IN-16 is useful in researching, preventing or ameliorating diseases or disorders associated with HPK1 activity such as cancer (extracted from patent WO2019051199A1, compound 39) [1].
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- HY-145044
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MAP4K
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Inflammation/Immunology
Cancer
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HPK1-IN-17 is a potent and selective inhibitor of HPK1. Hematopoietic progenitor kinase 1 (HPKl) originally cloned from hematopoietic progenitor cells is a member of MAP kinase kinase kinase kinases (MAP4Ks) family. HPK1-IN-17 is useful in researching, preventing or ameliorating diseases or disorders associated with HPK1 activity such as cancer (extracted from patent WO2019238067A1, compound 73) [1].
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- HY-145045
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MAP4K
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Inflammation/Immunology
Cancer
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HPK1-IN-18 is a potent and selective inhibitor of HPK1. Hematopoietic progenitor kinase 1 (HPKl) originally cloned from hematopoietic progenitor cells is a member of MAP kinase kinase kinase kinases (MAP4Ks) family. HPK1-IN-18 is useful in researching, preventing or ameliorating diseases or disorders associated with HPK1 activity such as cancer (extracted from patent WO2019238067A1, compound 1) [1].
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- HY-170443
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MAP4K
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Cancer
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PF-07265028 is a selective hematopoietic progenitor kinase 1 (HPK1/MAP4K1). PF-07265028 can be used in the research of cancer. PF-07265028 shows very potent cellular activity as measured by pSLP76 IC50 (17 nM) [1].
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- HY-143868
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MAP4K
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Cancer
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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) [1].
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- HY-143871
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MAP4K
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Cancer
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HPK1-IN-30 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-30 has the potential for the research of cancer diseases (extracted from patent WO2021175271A1, compound 3) [1].
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- HY-179111
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MAP4K
Interleukin Related
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Cancer
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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 [1].
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- HY-160218
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MAP4K
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Cancer
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HPK1-IN-42 (compound 185) ia a HPK1 inhibitor with the IC50 50 of 0.24 nM [1].
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- HY-149773S
-
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MAP4K
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Inflammation/Immunology
Cancer
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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 [1].
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- HY-162545
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MAP4K
Ligands for Target Protein for PROTAC
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Cancer
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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 [1].
|
-
- HY-149520
-
|
|
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 [1].
|
-
- HY-144073
-
|
|
MAP4K
|
Cancer
|
|
HPK1-IN-21 is a potent inhibitor of HPK1 kinase inhibitor (Ki=0.8 nM). HPK1-IN-21 also has orally active [1].
|
-
- HY-172674
-
|
|
MAP4K
|
Cancer
|
|
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 [1].
|
-
- HY-156509
-
|
|
MAP4K
|
Others
|
|
HPK1-IN-38 (compound 15) is a MAP4K1/HPK1 inhibitor,can be used for HPK1 related disorders research [1].
|
-
- HY-163496
-
|
|
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 [1].
|
-
- HY-132926
-
|
|
MAP4K
|
Cancer
|
|
HPK1-IN-8 is an allosteric, inactive conformation-selective inhibitor of full-length HPK1.
|
-
- HY-172875
-
|
|
MAP4K
Interleukin Related
|
Inflammation/Immunology
Cancer
|
|
HPK1-IN-58 (Compound 26) is an inhibitor of HPK1 (IC50: 2.6 nM) and SLP76 (IC50: 20 nM). HPK1-IN-58 enhances IL-2 secretion and reverses PGE2-induced immunosuppression. HPK1-IN-58 can be used in anti-tumor immunity research [1].
|
-
- HY-149232
-
|
|
MAP4K
|
Cancer
|
|
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 [1].
|
-
- HY-172107
-
|
|
MAP4K
Interleukin Related
|
Inflammation/Immunology
Cancer
|
|
HPK1-IN-56 (Compound A29) is a HPK1 inhibitor (IC50: 2.70 nM). HPK1-IN-56 inhibits downstream p-SLP76 (IC50: 8.1 nM in Jurkat T cells). HPK1-IN-56 induces the production of IL-2 in human PBMCs. HPK1-IN-56 has anticancer effect, enhances T-cell killing ability and the antitumor efficacy of anti-PD-1 antibody [1].
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-
- HY-168119
-
|
|
MAP4K
|
Cancer
|
|
HPK1-IN-53 (compund 3a) is the potent HPK1 inhibitor (IC50=48 nM) [1].
|
-
- HY-161335
-
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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 [1].
|
-
- HY-159905
-
|
|
MAP4K
|
Inflammation/Immunology
|
|
HPK1-IN-54 is a potent HPK1 (Hematopoietic Progenitor Kinase 1) inhibitor that enhances T cell activation and proliferation by inhibiting HPK1 activity, thereby exhibiting antitumor effects. Its IC50 value against HPK1 is 2.67 nM, with excellent selectivity over the MAP4K family (>100-fold) and other selected kinases (>300-fold). HPK1-IN-54 displayed moderate in vivo clearance and reasonable oral exposure in mice and rats. Additionally, HPK1-IN-54 demonstrated strong antitumor efficacy in a CT26 murine colon cancer model and synergistic effects when combined with anti-PD-1 (HY-P9902A). HPK1-IN-54 shows promise for research in the field of immunotherapy [1].
|
-
- HY-163495
-
-
- HY-161917
-
|
|
MAP4K
|
Inflammation/Immunology
|
|
HPK1-IN-49 (Compound I-4) is an inhibitor for hematopoietic progenitor kinase 1 (HPK1) with an IC50 >100 nM [1].
|
-
- HY-138569
-
|
|
MAP4K
|
Cancer
|
|
HPK1-IN-4 (comp 22) is a HPK1 (MAPK41) inhibitor (IC50 of 0.061 nM) as preclinical immunoresearch tool compound [1].
|
-
- HY-W761300
-
|
|
Ligands for E3 Ligase
|
Others
|
|
1-(4-Pip-Ph)-DHP-dione is an E3 ligase ligand. 1-(4-Pip-Ph)-DHP-dione can be used for synthesis of PROTAC HPK1 Degrader-2 (HY-162544) [1].
|
-
- HY-157838
-
|
|
MAP4K
|
Cancer
|
|
HMC-B17 is a selective, orally bioavailable HPK1 inhibitor (IC50 = 1.39 nM) that potentiates anti-PD-L1 efficacy. HMC-B17 potently enhances the IL-2 secretion in Jurkat cells (EC50 = 11.56 nM). HMC-B17 can be used for the research of cancer [1].
|
-
- HY-179338
-
|
|
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 [1].
|
-
- HY-181924
-
|
|
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 [1].
|
-
- HY-182238
-
|
|
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 [1].
|
-
- HY-179731
-
-
- HY-168282
-
|
|
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) [1].
|
-
- HY-W022880
-
|
|
Drug Intermediate
|
Others
|
|
4-Bromo-6-fluoro-1H-indazole is a drug synthesis intermediate that can be used to synthesize an inhibitor of hematopoietic progenitor kinase 1 (hpk1) [1].
|
-
- HY-162546
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
3-hydroxypropanoic acid-pip-hydroquinone-dihydrouracil is a conjugate of E3 ligase ligand and linker that serve as a key intermediate for the synthesis of complete PROTAC HPK1 Degrader-2 (HY-162544) [1].
|
-
- HY-162842
-
-
- HY-149056A
-
|
|
MAP4K
|
Cancer
|
|
(3S,4R)-GNE-6893 is a potent and orally active HPK1 inhibitor. (3S,4R)-GNE-6893 can be used in research of cancer [1].
|
-
- HY-159123
-
|
|
MAP4K
|
Cancer
|
|
KHK-6 is an inhibitor for serine/threonine kinase hematopoietic progenitor kinase 1 (HPK 1) with an IC50 of 20 nM. KHK-6 enhances CD3/CD28-induced cytokine production, enhances CD69, CD25 and HLA-DR markers on CD4+ and CD8+ T cells, and enhances T cell-mediated killing activity of SKOV3 and A549 cells [1].
|
-
- HY-179197
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Dihydrouracil-Ph-2-Me-piperidine is an E3 ligase ligand. Dihydrouracil-Ph-2-Me-piperidine can be used to synthesize PROTAC HPK1 Degrader-6 (HY-178459) [1]
|
-
- HY-RS08073
-
|
|
Small Interfering RNA (siRNA)
|
Others
|
|
Map4k1 Rat Pre-designed siRNA Set A contains three designed siRNAs for Map4k1 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
Map4k1 Rat Pre-designed siRNA Set A
Map4k1 Rat Pre-designed siRNA Set A
- HY-RS08071
-
|
|
Small Interfering RNA (siRNA)
|
Others
|
|
MAP4K1 Human Pre-designed siRNA Set A contains three designed siRNAs for MAP4K1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
MAP4K1 Human Pre-designed siRNA Set A
MAP4K1 Human Pre-designed siRNA Set A
- HY-RS08072
-
|
|
Small Interfering RNA (siRNA)
|
Others
|
|
Map4k1 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Map4k1 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
Map4k1 Mouse Pre-designed siRNA Set A
Map4k1 Mouse Pre-designed siRNA Set A
- HY-179730
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
CRBN ligand-190 is a is a CRBN-type E3 ubiquitin ligase ligand, can be used for the synthesis of PROTACs, such as PROTAC HPK1 Degrader-7 (HY-179727) [1].
|
-
- HY-181932
-
|
|
MAP4K
|
Cancer
|
|
HDM2004 is a selective, orally active, blood-brain barrier-penetrant HPK1 inhibitor with an IC50 of 1.89 nM. HDM2004 exhibits anticancer activity against colon cancer. HDM2004 shows synergistic activity when combined with anti-PD-L1 in syngeneic mouse models. HDM2004 can be used for the research of colon cancer [1].
|
-
| Cat. No. |
Product Name |
Type |
-
- HY-W022880
-
|
|
Biochemical Assay Reagents
|
|
4-Bromo-6-fluoro-1H-indazole is a drug synthesis intermediate that can be used to synthesize an inhibitor of hematopoietic progenitor kinase 1 (hpk1) [1].
|
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-149773S
-
|
|
|
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 [1].
|
-
| Cat. No. |
Product Name |
|
Classification |
-
- HY-146231
-
|
|
|
PROTAC Synthesis
|
|
SS47, a PROTAC-based HPK1 degrader, exerts proteasome-mediated HPK1 degradation. The degradation of HPK1 via SS47 also significantly enhances the antitumor efficacy [1].
|
-
- HY-146231A
-
|
|
|
PROTAC Synthesis
|
|
SS47 TFA, a PROTAC-based HPK1 degrader, exerts proteasome-mediated HPK1 degradation. The degradation of HPK1 via SS47 also significantly enhances the in vivo antitumor efficacy of BCMA CAR-T cell research. HPK1, an immunosuppressive regulatory kinase, is a promising target for cancer immunotherapies [1]. SS47 (TFA) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
| Cat. No. |
Product Name |
|
Classification |
-
- HY-RS08073
-
|
|
|
siRNAs
Rat Pre-designed siRNA Sets
|
|
Map4k1 Rat Pre-designed siRNA Set A contains three designed siRNAs for Map4k1 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
- HY-RS08071
-
|
|
|
siRNAs
Human Pre-designed siRNA Sets
|
|
MAP4K1 Human Pre-designed siRNA Set A contains three designed siRNAs for MAP4K1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
- HY-RS08072
-
|
|
|
siRNAs
Mouse Pre-designed siRNA Sets
|
|
Map4k1 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Map4k1 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
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