Catalog No.
Product Name
Application
Product Information
Citations
-
DPP-4 inhibitor
Teneligliptin is a novel, potent, and long-lasting dipeptidyl peptidase-4 inhibitor; competitively inhibited human plasma, rat plasma, and human recombinant DPP-4 in vitro, with IC50 values of approximately 1 nM. -
HIV protease inhibitor
Tipranavir, a nonpeptidic HIV protease inhibitor (NPPI), inhibits the enzymatic activity and dimerization of HIV-1 protease, exerts potent activity against multi-PI-resistant HIV-1 isolates. -
Selective calpain inhibitor
Acetyl-Calpastatin (184-210) (human), selective calpain inhibitor. Strongly inhibits calpain I (Ki = 0.2 nM) and II but does not inhibit papain, trypsin and cathepsin L (Ki = 6 uM). Increases secretion of amyoid β-protein (Aβ) 42, Aβ40 and Aβ42 ratio. -
Fluorogenic caspase substrate
Ac-LEHD-AFC, fluorogenic caspase substrate. Analog of the caspase-9 substrate, LEHD-AFC. -
Caspase-3 inhibitor
AZ 10417808, selective non-peptide inhibitor of caspase-3 (Ki = 247 nM); displays > 40-fold selectivity over caspases 1, 2, 6, 7 and 8 (Ki > 10 uM). -
Gamma-secretase modulator
Compound W is a γ-secretase inhibitor that has been shown to lower the levels of secreted Aβ42 and Nβ25. -
DPP-4 inhibitor
DPPI 1c hydrochloride is a dicyanopyrrolidine compound that acts as a slow-binding and active site-targeting inhibitor of CD26 (DPP 4), with an IC50 = 106 nM and little activity against DPP II, DPP III, DPP VIII, DPP IX, FAP, or APP even at concentrations as high as 30 μM. -
Aminopeptidase inhibitor
Fumagillin is a complex natural product antibiotic which covalently binds a key histidine residue of methionine aminopeptidase type II (MetAP-2), inhibiting endothelial cell proliferation and angiogenesis. -
γ-secretase inhibitor
MRK 560 is an orally bioavailable gamma-secretase inhibitor with the ability to markedly reduce Abeta peptide in the brain and CSF of the rat and confirm the utility of the rat for assessing the effects of gamma-secretase inhibitors on central nervous system Abeta(40) levels in vivo. -
DPP-4 inhibitor
PK 44 phosphate is a potent inhibitor of dipeptidyl peptidase IV (DPP-IV) with an IC50 value of 15.8 nM. -
MMP inhibitor
Ro 32-3555 is a potent, collagenase-selective MMP inhibitor . -
Human cathepsin L inhibitor
SID 26681509 is a reversible and potent human cathepsin L inhibitor. SID 26681509 displays no inhibitory activity of cathepsin G. -
MMP-13 inhibitor
WAY 170523 has been reported to be a selective and potent inhibitor of MMP-13. -
Fluorogenic caspase substrate
Ac-LEHD-AFC is a fluorogenic substrate for caspase-4, caspase-5, and caspase-9. -
DPP-4 inhibitor
NVP DPP 728 dihydrochloride is a potent and orally active inhibitor of dipeptidyl peptidase (DPP)-IV with Ki and IC50 values of 11 nM and 14 nM, respectively. -
Urokinase (uPA) inhibitor
4-Chlorophenylguanidine hydrochloride is a potent and specific inhibitor of uPA (urokinase). -
Urokinase (uPA) inhibitor
BC 11 hydrobromide, belective urokinase (uPA) inhibitor (IC50 = 8.2 μM). Inhibits clot lysis with no effect on clot formation and exhibits no activity at 8 other uPA related enzymes. -
MMP Inhibitor
Batimastat is an anticancer drug that belongs to the family of drugs called angiogenesis inhibitors. Batimastat (BB-94) is a potent, broad spectrum matrix metalloprotease (MMP) inhibitor. -
serine/threonine phosphatase inhibitor
Fumonisin B1 is a fungal metabolite produced by Fusarium moniliforme, that has been shown to inhibit protein serine/threonine phosphatases (PP1, PP2A, PP2B, PP2C, and PP5/T/K/H), and is most effective with PP5. -
MMP Inhibitor
20(R)-Ginsenoside Rh2 is a matrix metalloproteinase (MMP) inhibitor that acts as a cell antiproliferator. -
20S proteasome inhibitor
Clasto-lactacystin b-lactone was later identified as the active metabolite of lactacystin, resulting from the elimination of cysteine and the formation of a reactive b-lactone. -
DPP-4 inhibitor
Teneligliptin is a novel, potent, and long-lasting dipeptidyl peptidase-4 inhibitor; competitively inhibited human plasma, rat plasma, and human recombinant DPP-4 in vitro, with IC50 values of approximately 1 nM. -
DPP4 Inhibitor
Evogliptin is an orally active inhibitor of DPP4 (dipeptidyl peptidase-4), demonstrating notable and sustained hypoglycemic effects in murine models. In addition to its antidiabetic properties, Evogliptin exerts effects by inhibiting the production of inflammatory and fibrotic signals in hepatocytes through the induction of autophagy. This compound is particularly relevant for research applications related to type 2 diabetes, osteoporosis, renal impairment, and chronic liver inflammation. -
20S proteasome Inhibitor
BSc2118 is a potent inhibitor of the 20S proteasome, exhibiting an IC50 of approximately 50 nM. This compound induces G2/M phase cell cycle arrest and apoptosis in myeloma cells while inhibiting cytoprotective autophagy and tumor angiogenesis. Additionally, BSc2118 reduces matrix metalloproteinase 9 (MMP9) activity, promotes angioneurogenesis, and mitigates cerebral toxicity associated with recombinant tissue-type plasminogen activator. Its applications are relevant in the studies of cerebral ischemia and multiple myeloma. -
DPP4 Inhibitor
(Rac)-Sitagliptin is a potent and selective inhibitor of dipeptidyl peptidase-4 (DPP4), exhibiting an IC50 of 19 nM in Caco-2 cell extracts. This compound plays a significant role in the modulation of glucose metabolism, making it relevant for diabetes research. Its ability to enhance insulin secretion and decrease glucagon levels underscores its potential applications in studying metabolic disorders and developing therapeutic strategies for type 2 diabetes. -
Calpain/Cathepsin Inhibitor
ALLM, also known as Calpain inhibitor II, acts as a potent inhibitor of calpain and cathepsin proteases. This compound is known to mitigate neuronal cell death, thereby enhancing chronic neurological function following spinal cord injury (SCI). Its utility in research extends to studies investigating protease activity and the mechanisms underlying neuroprotection in trauma-related conditions. -
Calpain Inhibitor
(Rac)-Neurodegenerative Disorder-Targeting Compound 1 is a calpain inhibitor that selectively modulates calpain activity, implicated in neurodegenerative processes. This compound is designed for research applications focused on neurodegeneration, providing a valuable tool for investigating the role of calpain in cellular function and injury. The inhibition of calpain activity may contribute to understanding the molecular mechanisms underlying neurodegenerative disorders. -
Tyrosinase Inhibitor
Swertiajaponin is a potent tyrosinase inhibitor that interacts with the enzyme's binding pocket through hydrogen bonding and hydrophobic interactions, exhibiting an IC50 of 43.47 μM. It effectively inhibits oxidative stress-mediated MAPK/MITF signaling pathways, resulting in a reduction of tyrosinase protein levels. Additionally, Swertiajaponin demonstrates strong anti-oxidative activity and suppresses melanin accumulation, making it a valuable tool for research aimed at understanding pigmentation disorders and oxidative stress. -
Tyrosinase Antagonist
Tyrosinase-IN-22 is a potent inhibitor of the enzyme tyrosinase, effectively targeting its substrates L-tyrosine and L-DOPA with IC50 values of 60 nM and 30 nM, respectively. This compound exhibits significant antioxidant and anti-melanogenic properties, making it valuable for research in skin pigmentation disorders and oxidative stress studies. Its ability to modulate tyrosinase activity positions it as a useful tool in the investigation of melanin synthesis and related biological pathways. -
Aldose reductase Inhibitor
Danshenol A is a potent aldose reductase inhibitor, exhibiting an IC50 of 0.1 μM. This abietane-type diterpenoid demonstrates protective effects on endothelial cells against oxidative stress through direct scavenging of reactive oxygen species (ROS). Additionally, Danshenol A possesses notable anti-inflammatory and antitumor properties, making it a valuable compound for research focused on atherosclerosis and related pathologies. -
DPP-4 Inhibitor
PB01 is a selective DPP-4 inhibitor with an IC50 of 15.66 nM. It effectively reduces high glucose-induced reactive oxygen species (ROS) production and mitochondrial superoxide generation while significantly decreasing cellular DPP-4 expression. In vivo studies demonstrate that PB01 can lower blood glucose levels in diabetic mice, indicating its potential therapeutic application. Furthermore, PB01 exhibits minimal cytotoxicity at a concentration of 100 μM, making it a promising candidate for diabetes-related research. -
Tyrosinase Inhibitor
Tyrosinase-IN-12 is a potent non-competitive inhibitor of tyrosinase, demonstrating an IC50 value of 49.33 ± 2.64 µM and a Ki value of 31.25 ± 0.25 µM. This compound exhibits strong radical scavenging activity, effectively reducing the production of reactive oxygen species (ROS) with an IC50 of 25.39 ± 0.77 µM. Tyrosinase-IN-12 is applicable in research focusing on the mitigation of browning in food products and agricultural applications. -
DPP-IV Inhibitor
DPP-4-IN-3 is a potent inhibitor of dipeptidyl peptidase IV (DPP-IV), exhibiting an IC50 value of 0.75 nM. This compound demonstrates significant antioxidant properties alongside insulinotropic activity, making it a valuable tool for diabetes research and the study of metabolic disorders. Its ability to modulate the DPP-IV pathway underscores its potential in therapeutic applications aimed at enhancing glucose homeostasis. -
DHODH Inhibitor
JNJ-74856665 is a potent inhibitor of dihydroorotate dehydrogenase (DHODH), exhibiting an IC50 of 0.396 nM for human DHODH. This compound disrupts pyrimidine synthesis, making it a valuable tool for studying the role of DHODH in various biological processes, including cell proliferation and immune response modulation. JNJ-74856665 has potential applications in research related to autoimmune diseases and cancer therapeutic strategies.
