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Catalog No.
Product Name
Application
Product Information
Citations
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Caspase-1 Inhibitor
CZL55 is a potent inhibitor of caspase-1, exhibiting an IC50 value of 24 nM. It plays a crucial role in modulating inflammatory pathways and apoptosis, making it valuable for studies related to febrile seizures (FS). This compound is useful for researchers investigating the underlying mechanisms of caspase-1 mediated processes in various pathological conditions. -
Caspase3 Inhibitor
(Rac)-M826 is a selective and reversible inhibitor of caspase-3, exhibiting an IC50 value of 0.005 μM. This compound effectively inhibits apoptosis in NT2 cells, making it a valuable tool for research into nervous system diseases. Its specificity for caspase-3 positions it as a significant reagent for studies related to cell survival and neurodegenerative conditions. -
Caspase Inhibitor
Z-Asp-CH2-DCB is an irreversible inhibitor targeting caspases, with broad-spectrum activity against proteases possessing caspase-like functions. This compound effectively blocks the production of pro-inflammatory cytokines such as IL-1β, TNF-α, IL-6, and IFN-γ in staphylococcal enterotoxin B-stimulated peripheral blood mononuclear cells, while also reducing SEB-induced T-cell proliferation in a dose-dependent manner. Additionally, Z-Asp-CH2-DCB mitigates SU5416-induced septal cell apoptosis and the development of emphysema, making it a valuable tool in apoptosis and inflammatory research applications. -
Caspase-10 Inhibitor
Z-AEVD-FMK is a specific inhibitor of caspase-10, playing a critical role in the regulation of apoptosis. By inhibiting caspase-10, Z-AEVD-FMK effectively prevents the activation of Bid and the subsequent release of apoptosis-inducing factor (AIF) from mitochondria. This action leads to a notable reduction in apoptotic cell populations, making it a valuable tool for investigating apoptotic pathways and potential therapeutic interventions in related diseases. -
Caspase Inhibitor
Z-VAD is an irreversible pan-caspase inhibitor that targets multiple caspases, including caspase-3, -6, -7, -8, and -9, while exhibiting a lesser inhibitory effect on caspase-2. This compound is utilized in research for its ability to block apoptosis signaling pathways, promote autophagy and necrosis in tumor cells, and exhibit anti-angiogenic properties. Z-VAD enhances the sensitivity of breast and lung cancer cells to radiotherapy, both in vitro and in vivo, and extends growth delay in tumor xenograft models. It is primarily employed in studies focused on cancer radiosensitization and the regulation of cell death pathways. -
Caspase 8 Inhibitor
Caspase 8 Inhibitor CASP8-IN-1 (Compound 63-R) selectively inhibits caspase 8 with an IC50 value of 0.7 μM. This compound is effective in blocking FasL-induced apoptosis in Jurkat cells, making it a valuable tool for studying apoptotic signaling pathways and cellular responses to death stimuli. Its specificity and potency make CASP8-IN-1 suitable for research applications in cancer biology and therapeutic development targeting caspase-mediated cell death. -
COX-2/MMP-7/TLR4 Inhibitor
Isofraxidin is a coumarin compound derived from *Acanthopanax senticosus* that exhibits anti-invasive and anti-inflammatory properties. It inhibits MMP-7 expression and suppresses cell invasion in human hepatoma cells by reducing ERK1/2 phosphorylation. Isofraxidin also downregulates the expression of iNOS and COX-2 and inhibits the formation of the TLR4/myeloid differentiation protein-2 (MD-2) complex. -
MMP-9 inhibitor
MMP-9-IN-1 is a selective inhibitor of matrix metalloproteinase-9 (MMP-9) that specifically targets the hemopexin (PEX) domain of MMP-9, without affecting other MMP family members. -
MMP Inhibitor/PPARα Agonists
Auraptene is an orally active geranyloxycoumarin compound naturally found in plants of the *Brassicaceae* family. It exhibits a wide range of biological activities, including antibacterial, anti-pathogenic, antioxidant, anti-tumor, and neuroprotective effects. Auraptene has shown therapeutic potential in the management of various chronic conditions such as hypertension and cystic fibrosis, making it a valuable compound for pharmacological and nutraceutical research. -
Caspase-1 inhibitor
Ac-YVAD-cmk (Caspase-1 Inhibitor II) is a selective, irreversible inhibitor of caspase-1 (also known as IL-1β converting enzyme, ICE). It exhibits potent neuroprotective and anti-inflammatory effects by suppressing the expression of proinflammatory cytokines IL-1β and IL-18. Ac-YVAD-cmk also inhibits pyroptosis, a form of inflammatory cell death, making it a valuable tool for studying inflammation-related diseases and neurodegenerative disorders. -
Cathepsin L inhibitor
Z-FY-CHO (Z-Phe-Tyr-CHO) is a potent and specific inhibitor of cathepsin L (CTSL), a lysosomal cysteine protease involved in protein degradation and various pathological processes. It is commonly used as a tool compound in studies of CTSL-related functions and diseases. -
SHP2 inhibitor
Migoprotafib (GDC-1971; compound 199) is a selective SHP2 inhibitor that suppresses the MAPK/ERK signaling pathway. It exhibits antitumor activity and is under investigation for its potential in targeting SHP2-driven cancers. -
PGAM1 inhibitor
HKB99 is an allosteric inhibitor of phosphoglycerate mutase 1 (PGAM1) that induces apoptosis and suppresses cell migration by inhibiting the formation of invasive pseudopodia. It increases oxidative stress, activates the JNK/c-Jun pathway, and downregulates AKT and ERK signaling. HKB99 is a promising compound for the study of non-small cell lung cancer (NSCLC). -
Endoplasmic Reticulum Stress Inhibitor
Tauroursodeoxycholate (Tauroursodeoxycholic acid; TDUCA) dihydrate is an inhibitor of endoplasmic reticulum (ER) stress that significantly downregulates pro-apoptotic molecules, including caspase-3 and caspase-12. Additionally, it suppresses ERK signaling, contributing to its cytoprotective and anti-apoptotic effects. -
ADAM17 inhibitor
JG26 is a potent ADAM inhibitor with IC50 values of 12 nM for ADAM8, 1.9 nM for ADAM17, and 150 nM for ADAM10. It also inhibits MMP-12 with an IC50 of 9.4 nM. JG26 suppresses AngII-induced EGFR transactivation and ERK activation, upregulates ACE2 expression, inhibits CD23 shedding, and reduces SARS-CoV-2 infection. Additionally, JG26 demonstrates anti-metastatic effects in colorectal cancer and holds research potential in Hodgkin lymphoma and vascular diseases. -
HIV-1 protease/PTP1B inhibitor
Isosinensetin is a bioactive flavonoid compound with diverse pharmacological properties. It acts as a dual inhibitor of HIV-1 protease and protein tyrosine phosphatase 1B (PTP1B), with an IC₅₀ of 2.61 µM and a Kᵢ of 0.92 µM for PTP1B, indicating its potential in antiviral and metabolic disease research. Additionally, isosinensetin inhibits P-glycoprotein (P-gp) activity in MDR1-MDCKII cells, suggesting its utility in overcoming multidrug resistance. Isosinensetin exhibits multiple therapeutic effects, including anti-tumor, anti-viral, anti-inflammatory, and antioxidant activities. These properties support its application in the research of various conditions such as cancer, chronic inflammation, osteoporosis, diabetes, and infectious diseases. -
Phosphatase inhibitor
β-Glycerophosphate disodium salt pentahydrate is a bioactive endogenous metabolite and a widely used phosphatase inhibitor. It plays a critical role in promoting and sustaining osteoblast differentiation, supporting mineral metabolism, and modulating cellular signal transduction pathways. In tissue engineering and drug delivery, it is commonly utilized as a component in the formation of heat-sensitive hydrogels due to its thermoresponsive properties. Additionally, β-glycerophosphate disodium salt accelerates calcification in vascular smooth muscle cells, making it a valuable tool for studying vascular calcification and related pathologies. -
COX-1/HDAC/Tyrosinase Inhibitor
Gnetol is a bioactive phenolic compound isolated from the root of *Gnetum montanum* with diverse pharmacological properties. It potently inhibits cyclooxygenase-1 (COX-1) with an IC₅₀ of 0.78 μM and exhibits histone deacetylase (HDAC) inhibitory activity. Gnetol is also a strong tyrosinase inhibitor, with an IC₅₀ of 4.5 μM against murine tyrosinase, leading to suppression of melanin biosynthesis. In addition to its antioxidant, antiproliferative, anticancer, and hepatoprotective effects, Gnetol modulates metabolic enzymes in a concentration-dependent manner, including α-amylase, α-glucosidase, and adipogenesis pathways, making it a promising candidate for research in oncology, dermatology, and metabolic disorders. -
DPP4 Inhibitor
DPP4-In hydrochloride is a selective inhibitor of dipeptidyl peptidase 4 (DPP4), an enzyme that plays a critical role in glucose metabolism and immune regulation. By inhibiting DPP4, this compound can effectively increase the levels of active incretin hormones, which may contribute to improved glycemic control. DPP4-In hydrochloride is primarily utilized in diabetes research and can aid in the investigation of metabolic disorders and potential therapeutic strategies for type 2 diabetes. -
Tyrosinase Inhibitor
2-Ketoglutaric Acid Potassium is a reversible and orally active inhibitor of tyrosinase, exhibiting an IC50 value of 15 mM. As a key intermediate in the Krebs cycle, it plays a role in ATP and GTP production and serves as a major carbon skeleton for nitrogen-assimilatory reactions. In addition to its enzymatic inhibition, 2-Ketoglutaric Acid Potassium has demonstrated the ability to suppress abnormal intestinal permeability and the expression of TNFα, both in vitro and in vivo. Its therapeutic applications extend to alleviating symptoms of inflammatory bowel disease (IBD) and rebalance of gut microbiota. -
MMP Inhibitor
Ecliptasaponin A is a pentacyclic triterpenoid saponin that functions as a robust inhibitor of matrix metalloproteinases (MMPs). It demonstrates significant anti-tumor properties by activating the ASK1/JNK pathway, leading to apoptosis and autophagy in lung cancer cells. Additionally, Ecliptasaponin A exerts anti-inflammatory and anti-fibrotic effects by inhibiting the HMGB1/TLR4/NF-κB signaling pathway, impacting COX-2 and MMP-9 expression. Its chondroprotective effects are attributed to the downregulation of MMP13 and modulation of inflammatory factors, while it also promotes ovarian function by enhancing ESR1 receptor expression. -
HDAC6/Proteasome Inhibitor
AMC-3-030 is a selective inhibitor targeting histone deacetylase 6 (HDAC6) and the chymotrypsin-like activity of the proteasome, demonstrating IC50 values of 884 nM and 4.17 nM, respectively. This compound exhibits a proliferative inhibitory effect and has been shown to reduce levels of α-tubulin and β-actin. AMC-3-030 serves as a valuable tool for investigating mechanisms related to multiple myeloma and other related research applications. -
Calpain/Apoptosis Inhibitor
AK 295 is a selective calpain inhibitor that modulates apoptosis via a calpain-dependent mechanism. This compound exhibits potent neuroprotective effects and is effective in decreasing myocardial injury by inhibiting calpain activity. AK 295 is suitable for research applications related to infection, inflammation, and a variety of diseases, including cardiovascular conditions and neurological disorders such as stroke and viral myocarditis. -
γ-Secretase Inhibitor I
Z-LLNle-CHO is a γ-secretase inhibitor that effectively disrupts the Akt-mediated pro-survival signaling pathway, leading to caspase activation and ROS-dependent apoptosis. This compound is instrumental in cancer research, particularly in the studies of breast cancer and leukemia, where inhibiting γ-secretase activity may provide insights into therapeutic strategies. -
Aldose Reductase Inhibitor
WJ-39 is a potent orally active inhibitor of aldose reductase (AR), demonstrating significant therapeutic potential. This compound has been shown to mitigate tubular damage in diabetic nephropathy models by activating the PINK1/Parkin signaling pathway, thereby promoting mitophagy and reducing apoptosis. WJ-39 serves as a valuable tool for studying diabetic complications and the underlying mechanisms of kidney injury. -
Granzyme B/Caspase-8 Inhibitor
Ac-IETD-CHO is a potent, reversible inhibitor of granzyme B and caspase-8. By blocking these proteases, Ac-IETD-CHO effectively inhibits Fas-mediated apoptotic cell death, as well as preventing hemorrhage and liver failure. This compound is valuable for research in apoptosis, immune response, and the modulation of cytotoxic T lymphocyte-induced cell death. -
DHODH Inhibitor
Olorofim is a selective inhibitor of dihydroorotate dehydrogenase (DHODH), a crucial enzyme in the pyrimidine biosynthesis pathway. It demonstrates potent antifungal activity, particularly against Aspergillus fumigatus and other species within the Aspergillus genus. Olorofim is a valuable tool for research focused on fungal infections and the development of antifungal therapies. -
DHODH Inhibitor
DHODH-IN-33 is a selective inhibitor of dihydroorotate dehydrogenase (DHODH), exhibiting potent anti-cancer activity with IC50 values of 5.22 μM in A549 cells and 3.03 μM in 5637 cells. This compound induces autophagy-dependent ferroptosis characterized by mitochondrial dysfunction, lipid peroxidation, and reactive oxygen species (ROS) accumulation, while demonstrating minimal toxicity in vivo. DHODH-IN-33 is a valuable tool for researching therapeutic strategies targeting non-small cell lung cancer and bladder cancer through the autophagy-mediated degradation of DHODH. -
Tyrosinase Inhibitor
Deoxyarbutin is a potent tyrosinase inhibitor, primarily utilized in dermatological and cancer research. It promotes apoptosis in melanoma cells and enhances the vitality of mouse acinar cells, exhibiting significant skin whitening effects and anti-tumor activity. This compound is valuable for studies focused on skin disorders and melanoma treatment strategies. -
Mushroom Tyrosinase Inhibitor
Dihydroaltenuene B is a potent inhibitor of mushroom tyrosinase, exhibiting an IC50 of 38.33 µM. This compound interacts with active site residues, including His244, Met280, and Gly281, through hydrogen bonding with its 3-OH and 4'-OH groups. Dihydroaltenuene B serves as a valuable reagent for investigating tyrosinase-related enzymatic processes and offers potential applications in skin-whitening agents and studies on melanin biosynthesis inhibition. -
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. -
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. -
cACE/NEP Inhibitor
AD012 is a dual inhibitor of the enzymes neprilysin (NEP) and angiotensin-converting enzyme (cACE). Designed from the C-domain selective ACE inhibitor, lisinopril-tryptophan, AD012 demonstrates significant antihypertensive and cardioprotective properties. This compound is valuable for research in cardiovascular health and the treatment of hypertension. -
NEP Inhibitor
GW 796406 is a potent neprilysin (NEP) inhibitor with an IC50 value of approximately 1.1-2.5 nM, exhibiting a higher selectivity compared to ACE, which has an IC50 of around 1.6-4.7 nM. This compound is valuable for exploring mechanisms involved in cardiovascular diseases and may aid in the development of therapeutics targeting NEP-related pathways. GW 796406's specificity and efficacy make it a useful tool for researchers studying cardiovascular health and related disorders. -
ACE/NEP Inhibitor
RB-105 is a potent dual inhibitor of angiotensin-converting enzyme (ACE) and neutral endopeptidase (NEP), with Ki values of 4.2 nM and 1.7 nM, respectively. By inhibiting ACE, RB-105 decreases angiotensin II production and enhances bradykinin levels, while NEP inhibition further elevates natriuretic peptide levels, resulting in a synergistic increase in bradykinin. This compound exhibits significant antihypertensive and natriuretic effects in both spontaneously hypertensive and normotensive rat models, making RB-105 a valuable reagent for studies on hypertension and related cardiovascular conditions. -
NEP/ACE Inhibitor
Aladotril, a dual inhibitor of neutral endopeptidase (NEP) and angiotensin-converting enzyme (ACE), exhibits potential in ameliorating cardiac hypertrophy without reducing blood pressure. This compound is valuable for research focused on heart failure and the mechanisms of cardiac remodeling following myocardial infarction. Its unique properties make it an important tool for studying cardiovascular health and therapeutic interventions. -
ACE/ECE-1/NEP Inhibitor
CGS 35601 is a potent inhibitor of endothelin-converting enzyme-1 (ECE-1), neutral endopeptidase 24.11 (NEP), and angiotensin-converting enzyme (ACE), exhibiting IC50 values of 55 nM, 2 nM, and 22 nM, respectively. This compound effectively suppresses pressor responses induced by big endothelin-1 and angiotensin I, while simultaneously enhancing the circulation of atrial natriuretic peptide (ANP). CGS 35601 serves as a valuable tool in cardiovascular research, particularly in delineating the regulatory mechanisms of cardiovascular function in animal models. -
Angiotensin-Converting Enzyme/Neprilysin Inhibitor
Alatrioprilat is an orally active inhibitor of angiotensin-converting enzyme (ACE) and neprilysin, with an IC50 of 19.6 nM for ACE and 6.1 nM for neprilysin. This compound is significant in the metabolism of hormonal peptides, particularly in the degradation of nitric oxide and atrial natriuretic factor (ANF). Alatrioprilat is applicable in cardiovascular disease research, offering insights into therapeutic strategies for conditions influenced by these pathways. -
Glutamine Synthetase Inhibitor
JFD01307SC is a selective inhibitor of glutamine synthetase, which plays a crucial role in the conversion of L-glutamate to glutamine. By mimicking L-glutamate, JFD01307SC effectively targets and modulates the enzymes involved in glutamine biosynthesis. This compound is primarily utilized in research related to tuberculosis and other metabolic disorders, providing valuable insights into the therapeutic potential of glutamine metabolism modulation. -
DPP4 Inhibitor
Evogliptin tartrate is an orally active DPP4 inhibitor that exhibits significant and sustained hypoglycemic effects in murine models. It not only lowers blood glucose levels but also attenuates the production of inflammatory and fibrotic signals in hepatocytes by inducing autophagy. This compound is suitable for research applications related to type 2 diabetes, osteoporosis, renal impairment, and chronic liver inflammation. -
DHODH Inhibitor
DHODH-IN-8 is a selective inhibitor of dihydroorotate dehydrogenase (DHODH) in both human and Plasmodium falciparum, exhibiting IC50 values of 0.13 μM and 47.4 μM, respectively. Additionally, it demonstrates Kis of 0.016 μM for human DHODH and 5.6 μM for the parasite's enzyme. This compound shows significant antimalarial activity, making it a valuable tool for research into malaria treatment and the inhibition of the pyrimidine biosynthesis pathway.
