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Catalog No.
Product Name
Application
Product Information
Citations
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pan-WNK-kinase inhibitor
WNK463 is an orally bioavailable pan-WNK-kinase inhibitor.- Lu DC, .et al. , Pflugers Arch, 2019, Dec;471(11-12):1539-1549 PMID: 31729557
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PfGSK3/PfPK6 Inhibitor
PfGSK3/PfPK6-IN-1 is a selective inhibitor targeting PfGSK3 and PfPK6, with IC50 values of 97 nM and 8 nM, respectively. This compound effectively inhibits the proliferation of blood-stage Plasmodium falciparum 3D7 parasites, making it a valuable tool for malaria research. Additionally, PfGSK3/PfPK6-IN-1 exhibits low cytotoxicity in hepatocyte cultures at concentrations up to 200 nM, with a significant reduction in cell viability observed at 2 μM. Its dual action enhances its potential in studying malaria-related mechanisms and potential therapeutic strategies. -
Serine/Threonine Kinase Inhibitor
ST045945 is a selective inhibitor of serine/threonine kinases, specifically targeting CHK1 and CHK2 pathways that regulate cell cycle checkpoints. This compound effectively induces G2/M phase arrest in tumor cells, leading to DNA damage and inhibition of cell proliferation. ST045945 is utilized in cancer research to explore therapeutic strategies by disrupting critical signaling pathways associated with tumor progression and resistance to chemotherapy. -
Serine Protease Inhibitor
VD5123 is a potent serine protease inhibitor that effectively targets TMPRSS2, HGFA, matriptase, and hepsin, exhibiting IC50 values of 15 nM, 3980 nM, 140 nM, and 37 nM, respectively. This compound is particularly useful for antiviral research, including studies focused on SARS-CoV-2 and a broad spectrum of coronaviruses, as well as influenza viruses. Its ability to inhibit key proteases makes VD5123 an important tool in the investigation of viral pathogenesis and therapeutic development. -
Ser/Thr Protease Inhibitor
Nacresertib is a selective Ser/Thr protease inhibitor that targets specific proteolytic pathways within cells. This compound is pivotal in studying cellular signaling mechanisms and apoptosis, making it valuable for research focused on cancer and neurodegenerative diseases. Its ability to modulate protease activity allows for the exploration of therapeutic strategies in various pathological states. -
Ser/Thr Protease Inhibitor
ZK824859 hydrochloride is a selective inhibitor of urokinase plasminogen activator (uPA) with a potent IC50 of 79 nM. It also demonstrates varied inhibitory effects on tissue plasminogen activator (tPA) and plasmin, with respective IC50s of 1580 nM and 1330 nM. This compound is particularly relevant for research applications focusing on serine/threonine proteases and their roles in pathological processes, including fibrinolysis and tumor progression. Its oral bioavailability makes it a valuable tool for in vivo studies targeting uPA-mediated pathways. -
Ser/Thr Protease Inhibitor
PCSK9-IN-1 is a potent cyclic peptide inhibitor of Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9) with a Ki value of 1.46 nM. This compound effectively inhibits the catalytic activity of PCSK9, leading to increased low-density lipoprotein receptor (LDLR) levels. PCSK9-IN-1 can be utilized in research focused on cholesterol metabolism, cardiovascular disease, and the development of therapeutics targeting dyslipidemia. -
Ser/Thr Kinase Inhibitor
Milciclib maleate is a cyclin-dependent kinase inhibitor that primarily targets Ser/Thr kinases, disrupting cell cycle progression in melanoma. It exerts substantial antiproliferative effects by down-regulating genes such as PTTG1, thereby modulating gene expression linked to cell growth regulation. This compound enhances therapeutic sensitivity in p53-mutated melanoma cells, particularly when used in conjunction with PTTG1 silencing, making it valuable for cancer research and potential therapeutic applications. -
Ser/Thr Protease Inhibitor
IPR-803 is a potent Ser/Thr protease inhibitor that specifically targets the uPAR·uPA protein-protein interaction. By binding directly to uPAR with sub-micromolar affinity, IPR-803 effectively disrupts this critical interaction. This compound exhibits significant anti-tumor activity, making it a valuable reagent for cancer research and studies focused on protease-related pathways. -
Ser/Thr Protease Inhibitor
RWJ-58643 is a selective Ser/Thr protease inhibitor that primarily targets β-trypsin, modulating allergic inflammation pathways. This compound has demonstrated significant efficacy in reducing nasal allergy symptoms, eosinophil infiltration, and IL-5 levels at low doses, while high doses have been associated with late eosinophilia and increased IL-5 levels. RWJ-58643 functions by inhibiting the release of β-trypsin from mast cells, making it a valuable tool for research into allergic responses and related inflammatory conditions. -
ATP-competitive STK19 inhibitor
ZT-12-037-01 is a potent, selective, ATP-competitive STK19 inhibitor. ZT-12-037-01 effectively blocks oncogenic NRAS-driven melanocyte malignant transformation and melanoma growth in vitro and in vivo. -
TPPII inhibitor
Butabindide oxalate is a selective and potent inhibitor of TPPII (tripeptidyl peptidase II). -
BUB1 kinase inhibitor
BAY-1816032 is a potent and oral available BUB1 (budding uninhibited by benzimidazoles 1) kinase inhibitor with an IC50 of 7 nM. -
STK16 kinase inhibitor
STK16-IN-1 is a STK16 kinase inhibitor with an IC50 of 295 nM. -
Ser/Thr Protease Inhibitor
Antipain dihydrochloride is a potent Ser/Thr protease inhibitor derived from Actinomycetes. It is known to inhibit N-methyl-N'-nitro-N-nitrosoguanidine (MNNG)-induced transformation, leading to an increase in chromosomal aberrations. Additionally, Antipain dihydrochloride has been shown to restrict uterine DNA synthesis and functionality in murine models, making it a valuable tool for studying proteolytic processes and their implications in cellular biology and genetics. -
Ser/Thr Protease Inhibitor
ONO-3403 is an orally active serine/threonine protease inhibitor that targets key proteolytic processes. This compound has been shown to inhibit lipopolysaccharide (LPS)-induced production of tumor necrosis factor-alpha (TNF-α) and nitric oxide, demonstrating anti-inflammatory properties. Additionally, ONO-3403 exhibits cytotoxic effects by inhibiting cell growth and inducing apoptosis, making it a valuable tool in antitumor research. -
Ser/Thr Protease Inhibitor
Antipain is a serine/threonine protease inhibitor derived from Actinomycetes. It exhibits significant biological activity by inhibiting N-methyl-N'-nitro-N-nitrosoguanidine (MNNG)-induced cellular transformation and promoting chromosomal aberrations. Additionally, Antipain has been shown to impair uterine DNA synthesis and function in murine models, making it a valuable reagent for studies related to cellular transformation, DNA damage response, and reproductive biology.
