Catalog No.
Product Name
Application
Product Information
Citations
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Caspase-9 Fluorogenic Substrate
Ac-LEHD-AMC is a fluorogenic substrate specifically designed for the detection of caspase-9 activity. Upon hydrolysis by caspase-9, Ac-LEHD-AMC releases the AMC fluorophore, which emits fluorescence detectable at an excitation wavelength of 341 nm and an emission wavelength of 441 nm. This substrate is ideal for quantifying caspase-9 activity in various biological samples, facilitating research in apoptosis and related signaling pathways. -
Caspase-3 Activator
Raptinal is a potent activator of caspase-3, directly initiating the intrinsic pathway of caspase-dependent apoptosis. By rapidly inducing cell death in cancer cells through the direct activation of effector caspase-3, Raptinal effectively bypasses the need for initiator caspase-8 and caspase-9 activation. This unique mechanism makes Raptinal a valuable tool for research in cancer therapy and apoptosis studies. -
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. -
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. -
Pre-mRNA Splicing Activity Modulator
Hinokiflavone is a naturally occurring biflavonoid isolated from plants, recognized as a novel modulator of pre-mRNA splicing. It exhibits diverse biological activities, including anti-inflammatory, antitumor, and antiviral effects. Mechanistically, Hinokiflavone acts as a potent inhibitor of matrix metalloproteinases (MMPs) and suppresses the virulence of methicillin-resistant Staphylococcus aureus (MRSA) by targeting caseinolytic protease P (ClpP) with an IC₅₀ of 34.36 µg/mL. In cancer models, Hinokiflavone triggers apoptosis through a reactive oxygen species (ROS)-dependent, mitochondria-mediated pathway and suppresses tumor cell migration and invasion. Additionally, it functions as a SUMO protease inhibitor, effectively blocking sentrin-specific protease 1 (SENP1) activity. - CMC2.24 (TRB-N0224) is an orally active tricarbonylmethane compound that exhibits antitumor activity in pancreatic cancer models by inhibiting Ras activation and downstream ERK1/2 signaling. It is also a potent inhibitor of zinc-dependent matrix metalloproteinases (MMPs), with IC₅₀ values ranging from 2.0 to 69 μM. Additionally, CMC2.24 has therapeutic potential in osteoarthritis, where it restores cartilage homeostasis and reduces chondrocyte apoptosis through modulation of the NF-κB/HIF-2α pathway.
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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. - Triolein is a symmetric triacylglycerol composed of three oleic acid molecules esterified to glycerol. It exhibits strong antioxidant and anti-inflammatory properties and has been shown to reduce the upregulation of matrix metalloproteinase-1 (MMP-1), a key enzyme involved in tissue remodeling and inflammation. These activities make triolein a compound of interest in research related to inflammatory diseases and oxidative stress.
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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. - Papain is a cysteine protease belonging to the peptidase C1 family, derived from the latex of the papaya (*Carica papaya*). It is widely used across various industries, including food processing (as a meat tenderizer), pharmaceuticals (for wound debridement and anti-inflammatory formulations), textiles (for fabric treatment), and cosmetics (for exfoliation and skin care products).
- Hydrangenol is an orally active antiphotoaging compound isolated from *Hydrangea serrata* leaves. It prevents wrinkle formation by downregulating matrix metalloproteinases (MMPs) and inflammatory cytokines, while upregulating moisturizing factors and antioxidant gene expression, making it a promising agent for skin health and anti-aging research.
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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. -
mGluR5 allosteric modulator
CDPPB is a selective, orally active allosteric modulator of the metabotropic glutamate receptor 5 (mGluR5). It enhances AKT and ERK1/2 signaling and upregulates BDNF mRNA expression. CDPPB also inhibits caspase-3 activation and mitigates mitochondrial dysfunction, demonstrating therapeutic potential in improving cognitive impairment, depression, and Huntington’s disease. -
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. -
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. -
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. -
DPPH Scavenger
2,4,7-Trihydroxy-9,10-dihydrophenanthrene is a dihydrophenanthrene derivative primarily targeting DPPH radicals. It exhibits significant antioxidant activity, with an IC50 value of 16.2 μM in DPPH radical-scavenging assays. This compound is useful in research applications focused on antioxidant mechanisms and the study of natural products derived from Pholidota chinensis Lindl. -
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. -
DHODH Inhibitor
DHODH-IN-20 is a potent inhibitor of dihydroorotate dehydrogenase (DHODH), an iron-containing flavin-dependent enzyme located in the inner mitochondrial membrane of human cells. By inhibiting DHODH, this compound exhibits significant anti-tumor activity, making it a valuable tool in the study of cancer biology. DHODH-IN-20 is particularly relevant for research focused on acute myelogenous leukemia, offering insights into potential therapeutic strategies. -
HsDHODH Inhibitor
DHODH-IN-3 is a selective inhibitor of Human Dihydroorotate Dehydrogenase (HsDHODH), demonstrating a potent inhibitory effect with an IC50 value of 261 nM. By targeting the ubiquinone binding sites within the enzyme, DHODH-IN-3 exhibits a competitive inhibition profile, characterized by a Kiapp of 32 nM. This compound shows promise for therapeutic applications in malaria research, potentially contributing to the development of novel treatments. -
DHODH Inhibitor
DHODH-IN-12 is a derivative of Leflunomide that functions as a dihydroorotate dehydrogenase (DHODH) inhibitor. This compound displays weak inhibitory activity against DHODH, making it a valuable tool for studying the modulation of pyrimidine metabolism. Its applications include investigations into immunological diseases and the development of therapeutics targeting nucleotide synthesis pathways. The pKa of 5.07 further informs its solubility and stability characteristics in biological systems. -
hDHODH Inhibitor
hDHODH-IN-2 is a selective inhibitor of human dihydroorotate dehydrogenase (hDHODH), functioning as an analogue of Leflunomide's active metabolite. This compound exhibits anti-inflammatory properties, making it relevant for research into autoimmune diseases and other inflammatory conditions. Its mechanism of action targets pyrimidine synthesis, effectively reducing the production of lymphocytes involved in inflammatory responses.
