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Catalog No.
Product Name
Application
Product Information
Citations
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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. -
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. -
Tyrosinase Inhibitor
2-Hydroxy-4-methoxybenzaldehyde is a potent inhibitor of the enzyme tyrosinase, which is crucial in melanin biosynthesis. This compound plays a significant role in research pertaining to pigmentation disorders and skin-related applications. Additionally, it can be utilized as a precursor for the synthesis of Urolithin M7, expanding its utility in biochemical studies. -
Aminopeptidase Inhibitor
Amastatin hydrochloride is a potent competitive inhibitor of aminopeptidases, exhibiting slow, tight binding kinetics. It demonstrates Ki values of 0.26 nM, 30 nM, and 52 nM against Aeromonas aminopeptidase, cytosolic leucine aminopeptidase, and microsomal aminopeptidase, respectively. This compound is valuable for research applications focusing on protein metabolism and post-translational modifications, as well as in studies exploring the role of aminopeptidases in various physiological and pathological processes. -
Calpain Inhibitor
Calpain Inhibitor V (Mu-Val-HPh-FMK) is an irreversible inhibitor of calpain, designed for effective cellular penetration. This compound exhibits notable anti-chlamydial activity and is utilized in research exploring calpain-mediated pathways and their implications in various diseases. Its application extends to studies focused on cellular signaling processes and the therapeutic potential of calpain modulation. -
DPP IV/CA Inhibitor
DPP IV/hCA II-IN-1 is a potent and selective inhibitor of dipeptidyl peptidase IV (DPP IV) and carbonic anhydrase (CA) enzymes. This compound exhibits a strong inhibitory effect on DPP IV with an IC50 value of 0.049 μM, while displaying varying Ki values for different carbonic anhydrase isoforms, including 0.0361 μM for CA II. Its dual-target inhibitory activity makes it a valuable tool for studying metabolic disorders and exploring therapeutic avenues in conditions involving DPP IV and CA dysregulation. -
DPP-4 Inhibitor
Gemigliptin tartrate is a selective and reversible inhibitor of dipeptidyl peptidase-4 (DPP-4), demonstrating an IC50 of 10.3 nM for human recombinant DPP-4. This compound exhibits significant anti-glycation properties, making it valuable for research into advanced glycation end products (AGEs) and their associated diabetic complications. Its specificity and efficacy position Gemigliptin tartrate as a useful tool in studies aimed at understanding and mitigating the effects of diabetes-related conditions. -
DPP-4 Inhibitor
Saxagliptin hydrochloride is a potent, selective, reversible inhibitor of dipeptidyl peptidase-4 (DPP-4), exhibiting an inhibition constant (Ki) of 0.6-1.3 nM. This compound is primarily employed in research focused on type 2 diabetes mellitus, as it enhances insulin secretion by increasing incretin levels, aiding in glucose regulation. Saxagliptin hydrochloride serves as a valuable tool for studying DPP-4's role in glucose homeostasis and potential therapeutic interventions in diabetes management. -
DPP-4 Inhibitor
Retagliptin is a selective, competitive inhibitor of dipeptidyl peptidase-4 (DPP-4) known for its oral bioavailability. It plays a crucial role in increasing incretin levels, which enhances insulin secretion and lowers glucagon levels in patients with type 2 diabetes mellitus (T2DM). This compound is valuable for research applications focused on the regulation of glucose homeostasis and the therapeutic potential in metabolic disorders. -
DPP-4 Inhibitor
Cofrogliptin is a potent oral dipeptidyl peptidase-4 (DPP-4) inhibitor. It exhibits long-acting antidiabetic efficacy, making it a promising candidate for the management of type 2 diabetes mellitus (T2DM). Cofrogliptin's mechanism of action enhances incretin levels, which supports insulin secretion and regulates glucose metabolism. This compound is valuable for research applications focused on diabetes treatment and metabolic disorders. -
DPP-4 Inhibitor
Sitagliptin fenilalanil is a potent dipeptidyl peptidase-4 (DPP-4) inhibitor that plays a crucial role in the regulation of glucose metabolism. By blocking the activity of DPP-4, it increases levels of incretin hormones, which enhance insulin secretion in response to meals and reduce glucagon levels. This compound is primarily utilized in diabetes research to explore therapeutic strategies for improving glycemic control and understanding the mechanisms of insulin regulation. -
DPP IV Inhibitor
Diprotin B is an inhibitor of dipeptidyl peptidase IV (DPP IV). By exhibiting competitive inhibition, Diprotin B mimics substrate behavior due to its tripeptide structure, particularly the presence of a proline residue at the penultimate position. This compound is utilized in research to study the modulation of glucose metabolism and to explore potential therapeutic applications in diabetes and related metabolic disorders. -
DPP-4 Inhibitor
Fotagliptin benzoate is a potent Dipeptidyl Peptidase IV (DPP-4) inhibitor with an IC50 value of 2.27 nM. It demonstrates a favorable safety profile in both rat and canine models. This compound is primarily utilized in research related to Type 2 diabetes mellitus, providing insights into glucose metabolism and potential therapeutic interventions. -
DPP1 Inhibitor
Propyl-GSK-2793660 hydrochloride is an irreversible and covalent inhibitor of Dipeptidyl Peptidase I (DPP1). This compound demonstrates significant inhibition of DPP1 activity, making it a valuable tool for investigating mechanisms related to bronchiectasis. Its application in research may facilitate the understanding of DPP1's role in various biological processes and potential therapeutic avenues. -
DPP-4 Inhibitor
Fotagliptin is a potent Dipeptidyl Peptidase IV (DPP-4) inhibitor with an IC50 of 2.27 nM. This compound is characterized by its favorable safety profile in rodent and canine models. Fotagliptin is primarily utilized in research related to Type 2 diabetes mellitus, contributing to investigations aimed at understanding glycemic control and insulin secretion mechanisms. -
DPP-4 Inhibitor
Sitagliptin fenilalanil hydrochloride is a potent inhibitor of dipeptidyl peptidase-4 (DPP-4), an enzyme involved in glucose metabolism. By blocking DPP-4 activity, this compound enhances the levels of incretin hormones, which promotes insulin secretion and lowers glucagon levels, thereby improving glycemic control. It is primarily used in research applications related to diabetes mellitus and metabolic disorders. -
DPP-IV Inhibitor
PK44 phosphate is a potent inhibitor of dipeptidyl peptidase IV (DPP-IV) with an IC50 value of 15.8 nM. It plays a critical role in regulating glucose metabolism and has potential applications in the treatment of type 2 diabetes. PK44 phosphate may also be used in pharmacological studies to explore the therapeutic effects of DPP-IV inhibition. -
DPP-4 Inhibitor
Teneligliptin-d8 is a deuterium-labeled analog of Teneligliptin, a competitive and durable inhibitor of dipeptidyl peptidase-4 (DPP-4). This compound is utilized in research to study the pharmacokinetics and metabolic pathways of Teneligliptin. Its potent inhibition of DPP-4 makes it significant for investigating therapeutic strategies for type 2 diabetes and related metabolic disorders. -
DPP1 Inhibitor
AZD5248 is a selective inhibitor of dipeptidyl peptidase 1 (DPP1), a key enzyme involved in the regulation of peptide homeostasis. This compound demonstrates significant biological activity in the modulation of immune responses and is particularly relevant for research in chronic obstructive pulmonary disease (COPD) and other inflammatory lung disorders. Its ability to inhibit DPP1 makes it a valuable tool for investigating the therapeutic potential in respiratory diseases. -
DPP-4 Inhibitor
Evogliptin hydrochloride is a potent and selective inhibitor of Dipeptidyl Peptidase-4 (DPP-4), primarily utilized to enhance glycemic control in the management of type 2 diabetes. Its mechanism involves significant and sustained hypoglycemic effects while also reducing inflammatory and fibrotic signals in hepatocytes through the induction of autophagy. This compound is relevant for research exploring metabolic disorders, including type 2 diabetes, renal impairment, osteoporotic changes, and chronic liver inflammation. -
DPP4 Inhibitor
Dutogliptin tartrate is a potent and selective dipeptidyl peptidase-4 (DPP4) inhibitor. It demonstrates significant biological activity in the modulation of incretin hormones, thereby enhancing insulin secretion and lowering glucose levels. This compound is primarily utilized in research focused on the management and treatment of type 2 diabetes mellitus, contributing to the understanding of glucose metabolism and the role of DPP4 in diabetic pathophysiology. -
DPP-4 Inhibitor
Anagliptin hydrochloride is a potent and selective inhibitor of dipeptidyl peptidase 4 (DPP-4), exhibiting an IC50 of 3.8 nM. It demonstrates reduced selectivity for DPP-8 and DPP-9, with IC50 values of 68 nM and 60 nM, respectively. This compound is utilized in research focused on glycemic control and has applications in studying Type 2 diabetes and related metabolic disorders. -
DPP9 Inhibitor
DPP9-IN-2 is a selective, potent inhibitor of Dipeptidyl Peptidase 9 (DPP9), exhibiting an IC50 of 12.9 nM. It demonstrates a selectivity index of 59 over DPP8 and shows minimal inhibitory effects on related peptidases, including DPP2, DPP4, FAP, and PREP. DPP9-IN-2 has been shown to induce pyroptosis in cancer cells and exhibits weak synergistic anti-HIV-1 activity when combined with non-nucleoside reverse transcriptase inhibitors. This compound is suitable for research related to cancer and infectious diseases. -
DPP-IV Inhibitor
NVP-DPP728 dihydrochloride is a selective and potent inhibitor of dipeptidyl peptidase IV (DPP-IV), with a Ki value of 11 nM. This compound plays a critical role in the regulation of glucose metabolism and is utilized in research related to diabetes mellitus. NVP-DPP728 dihydrochloride offers valuable insights into the therapeutic potential of DPP-IV inhibition in glycemic control and metabolic diseases. -
DPP-4 Inhibitor
ZY15557 is a novel competitive DPP-4 inhibitor with a Ki of 5.53 nM, demonstrating significant potency in inhibiting plasma DPP-4 activity. This orally active compound is useful in the investigation of type 2 diabetes and its potential therapeutic strategies. Research applications include studying glucose metabolism and insulin secretion modulation associated with DPP-4 inhibition. -
DPP-IV Inhibitor
RBx-0597 is a selective inhibitor of Dipeptidyl Peptidase IV (DPP-IV), exhibiting IC50 values of 32 nM, 31 nM, and 39 nM for human, mouse, and rat plasma DPP-IV, respectively. This compound shows promise in the investigation of type 2 diabetes by modulating glucose metabolism and incretin levels, making it a valuable tool for diabetes research and related metabolic studies. -
DPP-IV Inhibitor
O-Benzoylhydroxylamine is a selective inhibitor of Dipeptidyl Peptidase IV (DPP-IV), a key enzyme involved in glucose metabolism. By inhibiting DPP-IV, this compound exhibits significant anti-diabetic effects, making it valuable for research into diabetes management and related metabolic disorders. Its mechanisms and targets are critical for understanding the pathways influenced by DPP-IV inhibition. -
DPP4 Inhibitor
ASP4000 hydrochloride is a potent, selective inhibitor of dipeptidyl peptidase IV (DPP4), exhibiting an IC50 value of 2.25 nM against human recombinant DPP4. This compound demonstrates significant antihyperglycemic effects, making it valuable in studies related to type 2 diabetes research. Its oral bioavailability and competitive inhibition profile allow for potential applications in understanding DPP4's role in glucose metabolism and diabetes management. -
DPP4 Inhibitor
ZINC000003015356 is a DPP4 inhibitor that selectively blocks the activity of the dipeptidyl peptidase-4 enzyme. This inhibition enhances the availability of incretin hormones, which are crucial for glucose metabolism. ZINC000003015356 is primarily used in research related to diabetes and metabolic disorders, contributing to studies focused on glycemic control and potential therapeutic strategies. -
DPP-IV Inhibitor
H-Pro-Pro-Gln-OH is an oligopeptide that acts as a potent inhibitor of dipeptidyl peptidase-IV (DPP-IV). This compound exhibits significant biological activity in modulating insulin secretion and glucose metabolism, making it a valuable tool for diabetes research. Its effective inhibition of DPP-IV may contribute to therapeutic strategies in managing type 2 diabetes and related metabolic disorders. -
DPP-8/9 Inhibitor
DPP-8/9 probe-1 is a selective inhibitor targeting Dipeptidyl Peptidase DPP8/9, designed for use in fluorescence microscopy. This fluorescent probe features a nitrobenzoxadiazole (NBD) tag, demonstrating high affinity for DPP8/9 with an IC50 of 15 nM, while showing minimal activity against related S9 family members (IC50 of 210 nM). DPP-8/9 probe-1 enables visualization of active DPP8/9 in vitro, making it a valuable tool for studying the biological functions and pathways associated with this enzyme in research settings. -
DPP1 Inhibitor
Florensocatib hydrate is a potent inhibitor of dipeptidyl peptidase I (DPP1) with an IC50 value of 1.6 nM. This compound exhibits favorable bioavailability and pharmacokinetic properties, making it suitable for studies investigating inflammatory diseases and related pathophysiological processes. Its ability to modulate DPP1 activity provides a valuable tool for understanding disease mechanisms and exploring potential therapeutic strategies. -
DPP-IV Inhibitor
AMG-222 is a dipeptidyl peptidase IV (DPP-IV) inhibitor that reversibly binds to the enzyme, thereby inhibiting its activity. This compound demonstrates a saturable and concentration-dependent binding to human plasma proteins, achieving a binding rate of 80.8% at 1 nM and decreasing to 29.4% at concentrations above 100 nM. AMG-222 is primarily utilized in diabetes research, aiding studies focused on glucose metabolism and insulin regulation. -
DPP4 Inhibitor
BMS-767778 is a selective DPP4 inhibitor, exhibiting high affinity with Ki values of 0.94 nM for DPP4, and 4.9 nM and 3.2 nM for DPP8 and DPP9, respectively, demonstrating over 3,000-fold selectivity against these related enzymes. This compound also inhibits CYP-3A4 with an IC50 of 5.2 μM. BMS-767778 has been shown to significantly lower blood glucose levels in high-fat diet-induced ob/ob mouse models, indicating its potential for diabetes mellitus research applications. -
DPP-4 Inhibitor
DPP-4-IN-1 is a potent inhibitor of dipeptidyl peptidase 4 (DPP-4) with an IC50 of 49 nM. This compound, structurally analogous to Alogliptin, plays a crucial role in regulating glucose metabolism and enhancing insulin secretion. DPP-4-IN-1 is essential for diabetes research, facilitating investigations into therapeutic strategies for managing hyperglycemia. -
DPP-4 Inhibitor
Denagliptin tosylate is a tosyate salt of Denagliptin, functioning as a potent dipeptidyl peptidase IV (DPP-4) inhibitor. This small molecule effectively enhances incretin levels, contributing to improved glycemic control in type 2 diabetes models. Its applications in research include investigating mechanisms of insulin secretion and glucose metabolism, making it a valuable tool for diabetes-related studies. -
DPP-4 Inhibitor
DPP-4-IN-9 is a potent inhibitor of dipeptidyl peptidase 4 (DPP-4) with an IC50 of 8.22 nM. This compound exhibits significant antihyperglycemic activity, making it a valuable tool for research in diabetes and metabolic disorders. DPP-4-IN-9 is suitable for studies aimed at understanding the role of DPP-4 in glucose metabolism and the development of therapeutic agents targeting this pathway. -
DPP1 Inhibitor
Florensocatib is a potent inhibitor of Dipeptidyl Peptidase I (DPP1), a key enzyme involved in the processing of pro-inflammatory cytokines. This compound exhibits significant biological activity, making it a valuable tool for research in bronchiectasis and related inflammatory diseases. Its selective inhibition of DPP1 provides insights into therapeutic strategies aimed at modulating immune responses.
