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PARP-1 inhibitor
TAK1/MAP4K2 inhibitor 1 is a potent dual inhibitor targeting transforming growth factor β-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2), exhibiting IC₅₀ values of 41.1 nM and 18.2 nM, respectively.
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MAP4K4 inhibitor
PF-06260933 is a potent, selective, orally available MAP4K4 inhibitor with IC50 of 3.7 nM. -
HPK1 inhibitor
NDI-101150 is an orally active, potent, and selective inhibitor of hematopoietic progenitor kinase 1 (HPK1). It enhances T cell activation and exhibits antitumor activity by promoting immune-mediated tumor suppression, making it a promising candidate for cancer immunotherapy research. -
HPK1/MAP4K1 inhibitor
PF-07265028 is a selective inhibitor of hematopoietic progenitor kinase 1 (HPK1/MAP4K1) with potent cellular activity, demonstrated by a pSLP76 IC50 of 17 nM. It is a promising compound for cancer research, particularly in studies involving immune regulation and tumor immunotherapy. -
PROTAC HPK1 degrader
SS47 TFA is a PROTAC-based degrader targeting hematopoietic progenitor kinase 1 (HPK1), an immunosuppressive regulatory kinase. It induces proteasome-mediated degradation of HPK1 and significantly enhances the antitumor efficacy of BCMA CAR-T cell therapy in vivo. In addition to its biological function, SS47 TFA is also a click chemistry reagent containing an alkyne group, allowing it to participate in copper-catalyzed azide–alkyne cycloaddition (CuAAC) with azide-functionalized molecules. This dual functionality makes SS47 TFA a valuable tool in both cancer immunotherapy research and chemical biology applications. -
Kinases PROTAC
DB1113 is a bifunctional compound designed for targeted protein degradation of various kinases. It effectively induces degradation of ABL1, ABL2, BLK, CDK4, CDK11B, EPHA3, MAPK7, RIPK1, and others, facilitating the investigation of kinase-related signaling pathways. DB1113 is suitable for research focusing on diseases or disorders associated with dysregulated kinase activity, providing a valuable tool for exploring therapeutic interventions in cancer and other conditions. -
MAP4K4 Inhibitor
PF-06745013 is a selective inhibitor of MAP4K4, exhibiting an IC50 of 0.4 nM. This compound is distinguished by its lack of time-dependent inhibition risk for CYP3A4 and demonstrates non-ATP competitive activity. PF-06745013 has potential applications in the study of inflammatory diseases, including diabetes and cancer, making it a valuable tool in related research. -
GCK/MAP4K2 Inhibitor
TL4-12 is a selective inhibitor of MAP4K2 and GCK, demonstrating a dose-dependent ability to downregulate IKZF1 and BCL-6. This compound effectively inhibits cell proliferation in multiple myeloma with an IC50 of 37 nM, and it also induces apoptosis in cancerous cells. TL4-12 holds potential for overcoming resistance to immunomodulatory agents in the treatment of multiple myeloma. -
HPK1 Inhibitor
HPK1-IN-61 is a potent inhibitor of hematopoietic progenitor kinase 1 (HPK1), exhibiting a Ki value of 0.4 nM. Additionally, it demonstrates strong inhibitory activity against Abl with an IC50 of less than 0.51 nM, and LCK with an IC50 of 24 nM. This compound is valuable for research applications focused on immune signaling and kinase regulation. -
HPK1 Inhibitor
HPK1-IN-2 dihydrochloride is a potent inhibitor of hematopoietic progenitor kinase-1 (HPK1), exhibiting an IC50 of less than 0.05 μM. This compound also demonstrates inhibitory effects on Lck kinase with an IC50 range between 0.05 μM and 0.5 μM, as well as on Flt3, with an IC50 of less than 0.05 μM. Its biological activity and targeted inhibition make HPK1-IN-2 dihydrochloride a valuable tool for research focused on antitumor mechanisms and kinase pathway analyses. -
TNIK/MAP4K4 Inhibitor
Rentosertib is an orally active inhibitor of TNIK and MAP4K4, exhibiting IC50 values of 12-120 nM for both targets. This compound plays a crucial role in the modulation of signaling pathways involved in cell proliferation and survival. Relying on its potent inhibition, rentosertib is utilized in research applications exploring cancer biology and potential therapeutic interventions for related disorders. -
HPK1 Inhibitor
GNE-6893 is a selective inhibitor of HPK1, demonstrating a Ki of less than 0.02 nM. This compound enhances T cell receptor signaling and promotes IL-2 production in stimulated primary human T cells, making it valuable for the investigation of T cell activation mechanisms. GNE-6893 is particularly relevant for research applications focused on chronic refractory cancers. -
HPK1 Inhibitor
AZ3246 is a selective inhibitor of HPK1, exhibiting an IC50 of less than 3 nM. This compound promotes IL-2 secretion in T cells, with an EC50 of 90 nM, highlighting its immunomodulatory properties. AZ3246 serves as a valuable tool for research in cancer biology, particularly in the study of breast cancer therapeutics. -
HPK1 Inhibitor
HPK1-IN-68 is a potent inhibitor of hematopoietic progenitor kinase 1 (HPK1), with an IC50 value of 2.8 nM. This compound effectively blocks HPK1 signaling pathways, inhibits the phosphorylation of SLP76, and stimulates the production of the IL-2 cytokine. Additionally, HPK1-IN-68 counteracts the immunosuppressive effects of prostaglandin E2 (PGE2) and promotes the infiltration of CD3+/CD8+ T cells into tumor microenvironments, demonstrating T cell-dependent antitumor activity in a mouse colon cancer model. It is particularly relevant for research into colon cancer therapeutics. -
HPK1 Inhibitor
HPK1-IN-56 is a potent HPK1 inhibitor with an IC50 of 2.70 nM. It effectively inhibits downstream phosphorylation of SLP76, demonstrating an IC50 of 8.1 nM in Jurkat T cells. This compound induces IL-2 production in human peripheral blood mononuclear cells (PBMCs) and enhances T-cell cytotoxicity, contributing to its anticancer properties. HPK1-IN-56 also improves the antitumor efficacy of anti-PD-1 antibody therapies, making it a valuable tool for cancer immunotherapy research. -
HPK1 Inhibitor
HPK1-IN-64 is a highly selective, orally bioavailable inhibitor of HPK1, featuring an IC50 of 1.9 nM. It demonstrates significant selectivity for HPK1 over GLK, MAP4K5, TBK1, and TNIK, with respective selectivity ratios exceeding 100-fold. This compound effectively inhibits SLP76 protein phosphorylation and reduces IL-2 secretion, making it a valuable tool for investigating signaling pathways in cancer research, particularly colorectal cancer. -
HPK1 Inhibitor
HPK1-IN-69 is a potent inhibitor of HPK1 with an IC50 of 1.7 nM. This compound disrupts the HPK1-mediated T cell receptor signaling pathway, decreasing SLP76 phosphorylation and enhancing IL-2 release. In vivo studies demonstrate its anti-tumor efficacy in mouse models, making it a valuable reagent for investigating colorectal cancer and MC38 syngeneic tumors. -
TAK1/MAP4K2 Inhibitor
NG25 trihydrochloride is a potent dual inhibitor of TAK1 and MAP4K2, exhibiting IC50 values of 149 nM and 21.7 nM, respectively. This compound enhances the sensitivity of breast cancer cells to Doxorubicin, promoting apoptotic processes. NG25 trihydrochloride serves as a valuable tool for investigating therapeutic strategies in various cancer research applications. -
MAP4K4 Inhibitor
MAP4K4-IN-7 is a selective inhibitor of MAP4K4 that demonstrates moderate inhibitory activity against TNIK, MAP4K4, and MINK1, with pIC50 values of 6.8, 6.8, and 6.7, respectively. This compound can be utilized in research focused on cancer and neurological disorders, including conditions such as schizophrenia. Its ability to modulate MAP4K4 activity makes it a valuable tool for exploring therapeutic strategies in related pathologies. -
HPK1 Inhibitor
ZYF0033 is a potent inhibitor of hematopoietic progenitor kinase 1 (HPK1), achieving an IC50 of less than 10 nM by inhibiting the phosphorylation of MBP protein. This compound enhances anti-cancer immune responses, leading to a reduction in serine 376 phosphorylation of SLP76. In preclinical studies with the 4T-1 syngeneic mouse model, ZYF0033 demonstrated significant tumor growth inhibition and increased intratumoral infiltration of dendritic cells, natural killer cells, and CD107a+CD8+ T cells, while decreasing infiltration of various PD-1+ and TIM-3+ CD8+ T cell subsets. -
HPK1 Inhibitor
HPK1-IN-3 is a potent and selective ATP-competitive inhibitor of hematopoietic progenitor kinase 1 (HPK1; MAP4K1), exhibiting an IC50 of 0.25 nM. The compound demonstrates significant IL-2 potency, with an EC50 of 108 nM in human peripheral blood mononuclear cells (PBMCs). This makes HPK1-IN-3 a valuable tool for investigating the role of HPK1 in immune modulation and cellular signaling pathways. Its targeted inhibition offers potential applications in the study of hematopoietic cell functions and autoimmune disorders. -
HPK1 Inhibitor
DS21150768 is a selective inhibitor of HPK1, a key regulator of T-cell activation. This compound enhances T-cell function and may exhibit potential anticancer effects by modulating immune responses. DS21150768 is suitable for research applications focused on cancer immunotherapy and T-cell biology. -
MAP4K4 Inhibitor
MAP4K4-IN-3 is a potent and selective inhibitor of MAP4K4, exhibiting an IC50 of 14.9 nM in kinase assays and 470 nM in cellular assays. This compound demonstrates significant antidiabetic activity, making it a valuable tool for research in diabetes and metabolic disorders. Its specific action on the MAP4K4 pathway allows for detailed investigation of its biological effects and potential therapeutic applications. -
MAP4K Inhibitor
Famlasertib is a potent inhibitor of MAP4K, specifically targeting HGK (MAP4K4), MLK3, and MLK1 with IC50 values of 0.3 nM, 23.7 nM, and 44.7 nM, respectively. This compound demonstrates neuroprotective and anti-inflammatory effects, making it a valuable tool in research focused on amyotrophic lateral sclerosis (ALS). Famlasertib's ability to penetrate the blood-brain barrier enhances its potential for exploring therapeutic interventions in neurodegenerative diseases. -
HPK1 Inhibitor
HPK1-IN-32 is a potent and selective inhibitor of HPK1, exhibiting an IC50 of 65 nM. This compound is valuable for investigating HPK1-related disorders and diseases, making it an essential tool for research applications targeting cellular signaling pathways associated with immune responses and inflammation. -
HPK1 Inhibitor
HPK1-IN-7 is a potent inhibitor of hematopoietic progenitor kinase 1 (HPK1, MAP4K1) with an IC50 of 2.6 nM, demonstrating excellent selectivity among kinases. It exhibits some selectivity against IRAK4 and GLK, with IC50 values of 59 nM and 140 nM, respectively. This compound has shown significant efficacy in the MC38 syngeneic tumor model, particularly when used in combination with anti-PD1 therapy, highlighting its potential in immuno-oncology research. -
HPK1/GLKb Inhibitor
HPK1/GLK-IN-1 is an inhibitor targeting HPK1 and GLK, demonstrating potent inhibition of GLK with an IC50 value of 33 nM. This compound is primarily utilized in research focused on the modulation of HPK1/GLK signaling pathways, making it a valuable tool for studying animal pathogen infections and related biological mechanisms. Its specificity and potency provide researchers with an effective means to explore therapeutic interventions targeting these kinases. -
HPK1 Inhibitor
GNE-1858 is a highly potent inhibitor of hematopoietic progenitor kinase-1 (HPK1), acting through ATP-competitive mechanisms with IC50 values of 1.9 nM for wild-type HPK1 and 4.5 nM for the active mimetic mutant HPK1-SA. Its remarkable selectivity and efficacy make it an invaluable tool for studying HPK1-related pathways in cellular signaling. GNE-1858 has potential applications in cancer research and immunology, particularly in the modulation of T cell responses and hematopoiesis. -
MAP4K Inhibitor
GNE 220 hydrochloride is a potent and selective inhibitor of MAP4K4, exhibiting an IC50 of 7 nM. This compound demonstrates significant inhibitory activity against MAP4K4, making it a valuable tool for research focused on signaling pathways involved in cellular processes such as differentiation, proliferation, and apoptosis. GNE 220 is particularly relevant for studies investigating the role of MAP4K4 in various diseases, including cancer and inflammatory disorders. -
HPK1 Inhibitor
HPK1-IN-4 is a highly potent inhibitor of HPK1 (MAPK41), exhibiting an IC50 value of 0.061 nM. This compound serves as a valuable tool in preclinical immunological research, facilitating the study of HPK1's role in immune signaling pathways. Its specificity and efficacy make it an essential reagent for investigating therapeutic targets in immune-related disorders. -
HPK1 Inhibitor
HPK1-IN-34 is an inhibitor of Hematopoietic progenitor kinase 1 (HPK1), exhibiting an IC50 of less than 100 nM. This compound serves as a valuable tool in the study of HPK1's role in cellular signaling and immune response. Additionally, HPK1-IN-34 features a terminal alkyne group, enabling its application in click chemistry through copper-catalyzed azide-alkyne cycloaddition (CuAAc), facilitating the conjugation with azide-functionalized molecules for various biochemical studies. -
MAP4K4 Inhibitor
Pyrrolo[2,1-f][1,2,4]triazin-4-amine is an inhibitor of MAP4K4, demonstrating a Kd of 88 μM as assessed by surface plasmon resonance (SPR), with a ligand efficiency of 0.56. This compound is valuable for studies investigating the roles of MAP4K4 in cellular signaling and disease pathways. Its inhibitory properties make it suitable for biochemical assays and potential therapeutic research involving MAP4K4 modulation. -
HPK1 Inhibitor
HPK1-IN-19 is a selective inhibitor of hematopoietic progenitor kinase 1 (HPK1), a critical regulator in various cellular processes, including immune responses and cell proliferation. This compound exhibits significant potential in modulating HPK1 activity, making it valuable for research in immunology and cancer biology. Its ability to impact signaling pathways may provide insights into therapeutic strategies for diseases involving dysregulated HPK1 function. -
MAP4K Inhibitor
HPK1-IN-8 is an allosteric inhibitor targeting the MAP4K family, specifically designed to stabilize the inactive conformation of full-length HPK1. This compound demonstrates selective inhibition of HPK1, which is implicated in various cellular signaling pathways. It is a valuable tool for research investigating the modulation of immune responses, cancer biology, and other conditions associated with dysregulated MAP4K signaling. -
TNIK/MAP4K4 Inhibitor
TNIK&MAP4K4-IN-1 is a potent dual inhibitor targeting TNIK and MAP4K4/HGK, demonstrating IC50 values of 1.29 nM and less than 10 nM, respectively, in human hepatic stellate cell line LX-2. This compound exhibits significant biological activity in inhibiting pathways associated with cancer and fibrotic processes. It serves as a valuable tool for researchers studying the roles of TNIK and MAP4K4 in cellular signaling and disease progression. -
HPK1 Inhibitor
(3S,4R)-GNE-6893 is a selective inhibitor of HPK1, an important regulator in immune signaling pathways. This compound exhibits potent and orally bioavailable inhibition, making it a valuable tool for exploring the roles of HPK1 in cancer biology. Its biological activity provides insights for research applications focused on cancer therapeutics and immune modulation. -
MAP4K Inhibitor
GNE-220 is a potent and selective inhibitor of MAP4K4, exhibiting an IC50 of 7 nM. This compound plays a crucial role in modulating MAPK signaling pathways, making it valuable for studying cell proliferation and apoptosis. GNE-220 is applicable in research focused on cancer biology and inflammatory diseases, where MAP4K4 is implicated in disease progression. -
HPK1 Inhibitor
HPK1-IN-15 is a selective inhibitor of hematopoietic progenitor kinase 1 (HPK1), a member of the MAP4K family implicated in various signaling pathways. This compound is valuable for investigating the role of HPK1 in diseases such as cancer and for exploring potential therapeutic approaches to modulate HPK1 activity. Its specificity and potency make it an important tool in both basic research and drug development efforts targeting HPK1-related mechanisms. -
HPK1 Inhibitor
HPK1-IN-16 is a selective inhibitor of hematopoietic progenitor kinase 1 (HPK1), a member of the MAP kinase kinase kinase kinase (MAP4K) family. By specifically targeting HPK1, this compound demonstrates potential in the study of various diseases linked to HPK1 activity, including cancer. HPK1-IN-16 is valuable for research applications focused on the modulation of HPK1-related pathways to better understand disease mechanisms and explore therapeutic interventions. -
HPK1 Inhibitor
HPK1-IN-13 is a selective inhibitor of HPK1, a serine/threonine protein kinase implicated in hematopoietic progenitor cell signaling. As a member of the MAP4K family of mammalian Ste-20-related kinases, HPK1 plays a crucial role in various cellular processes. HPK1-IN-13 is designed for research applications targeting HPK1-related diseases, offering potential insights into its role in health and disease states. -
HPK1 Inhibitor
HPK1-IN-12 is a potent inhibitor of HPK1, a serine/threonine protein kinase that is part of the MAP4K family of mammalian Ste-20-related protein kinases. This compound selectively targets HPK1 and demonstrates significant inhibitory effects, making it a valuable tool for studying HPK1-related diseases. Its application in research can contribute to the understanding of the molecular mechanisms underlying various pathologies involving HPK1 signaling pathways. -
HPK1 Inhibitor
HPK1-IN-17 is a selective inhibitor of hematopoietic progenitor kinase 1 (HPK1), a member of the MAP kinase kinase kinase kinase (MAP4K) family. This compound is instrumental in investigating the role of HPK1 in various diseases, particularly in cancer, by modulating its activity. HPK1-IN-17 is valuable for research applications aimed at understanding HPK1's involvement in hematopoiesis and potential therapeutic interventions. -
HPK1 Inhibitor
HPK1-IN-14 is a selective inhibitor of HPK1, a serine/threonine protein kinase that is part of the MAP4K family and is found in hematopoietic progenitor cells. This compound exhibits significant potential for inhibiting HPK1 activity, making it a valuable tool for research into HPK1-related diseases and cellular signaling pathways. Researchers can utilize HPK1-IN-14 to investigate the roles of HPK1 in various biological processes and therapeutic contexts. -
HPK1 Inhibitor
HPK1-IN-11 is a potent inhibitor of HPK1, a serine/threonine protein kinase that is part of the MAP4K family of mammalian Ste-20-related protein kinases. This compound is valuable for investigating HPK1-related diseases and can facilitate research into the molecular mechanisms associated with these conditions. Its inhibitory properties make HPK1-IN-11 a critical tool for studying the role of HPK1 in various biological processes. -
HPK1 Inhibitor
HPK1-IN-10 is a potent inhibitor of the serine/threonine protein kinase HPK1, which is classified within the MAP4K family of mammalian Ste-20-related protein kinases. This compound demonstrates significant biological activity by modulating the signaling pathways associated with HPK1, making it a valuable tool for investigating HPK1-related diseases. Research applications include the study of immune responses and potential therapeutic interventions in related pathologies. -
HPK1 Inhibitor
HPK1-IN-18 is a potent and selective inhibitor of hematopoietic progenitor kinase 1 (HPK1), a member of the MAP kinase kinase kinase kinases (MAP4Ks) family. This compound demonstrates significant biological activity by modulating HPK1 signaling pathways, making it a valuable tool for research into cancer and other disorders associated with HPK1 activity. Its application can aid in elucidating the role of HPK1 in various biological processes and potential therapeutic interventions.

