Catalog No.
Product Name
Application
Product Information
Citations
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Caspase-6 Fluorogenic Substrate
Ac-VEID-AFC is a fluorogenic substrate specifically designed for the detection of caspase-6 activity. Its cleavage by caspase-6 produces a fluorescent signal, making it a valuable tool for assessing apoptotic processes and related signaling pathways in various biological systems. This substrate is widely utilized in research applications focused on cell death, inflammation, and neurodegenerative diseases. -
Metacaspase Substrate
Ac-VRPR-AMC is a fluorogenic substrate specifically designed for the detection of metacaspase activity. This compound is utilized in biochemical assays to measure metacaspase activity, making it a valuable tool for research in apoptosis and programmed cell death. Its fluorescence properties enable sensitive detection, facilitating studies on metacaspase function in various biological systems. -
Caspase Substrate
Ac-LEVD-pNA is a chromogenic substrate that specifically targets caspase-4, facilitating the detection of its enzymatic activity. This compound is essential for studies related to apoptosis and cellular signaling pathways, providing a reliable assay tool for researchers investigating caspase-mediated processes in various biological contexts. -
Etoposide/Obatoclax/Caspase-3 Inhibitor
M190S is a selective inhibitor of Caspase-3, demonstrating significant protection against mitochondria-dependent apoptosis in both in vitro and in vivo models. This small molecule is poised to serve as an essential research tool for elucidating mechanisms of cell death and for the development of therapeutics that target mitochondria-dependent apoptotic pathways. M190S also exhibits favorable oral bioavailability and excellent brain permeability, enhancing its potential utility in neurological research applications. -
Caspase-1 Inhibitor
Ac-Tyr-Val-Lys-Asp-aldehyde is a reversible caspase-1 inhibitor, primarily targeting the caspase-1 enzyme. This compound plays a significant role in increasing GATA1 levels and enhancing erythroid differentiation. It is particularly useful in research applications pertaining to anemias associated with chronic diseases, chemotherapy-induced anemia, and Diamond-Blackfan anemia. -
Caspase-4 Inhibitor
Ac-LEVD-CHO is a potent inhibitor of caspase-4, designed to selectively target this key protease involved in the apoptotic pathway. This peptide, comprising the sequence Ac-Leu-Glu-Val-Asp-al, effectively blocks caspase-4 activity, making it valuable for studies investigating apoptosis and inflammation. It serves as a useful tool for researchers examining the role of caspases in various biological processes and potential therapeutic interventions in related diseases. -
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 Activator
5,7-Dihydroxychromone functions as a caspase activator and exhibits neuroprotective properties by activating the Nrf2/ARE signaling pathway. This compound effectively mitigates oxidative stress and apoptosis induced by 6-hydroxydopamine (6-OHDA) in SH-SY5Y cells. Additionally, 5,7-Dihydroxychromone reduces the expression of activated caspase-3, caspase-9, and cleaved PARP, making it a valuable tool for studying neuroprotection and apoptosis in cellular models. -
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. -
PTP/PTEN Inhibitor
bpV(phen) is a potent inhibitor of protein tyrosine phosphatases (PTPs) and PTEN, exhibiting IC50 values of 38 nM, 343 nM, and 920 nM for PTEN, PTP-β, and PTP-1B, respectively. This compound demonstrates significant anti-proliferative effects on the protozoan parasite Leishmania in vitro. Additionally, bpV(phen) enhances the secretion of various chemokines and pro-inflammatory cytokines while promoting a Th1-type immune response characterized by IL-12 and IFNγ production. It also induces apoptosis and exhibits anti-angiogenic and anti-tumor properties, making it valuable for research in cancer and inflammation biology. -
Thrombin Inhibitor
Hirudin is a potent thrombin inhibitor known for its anticoagulant properties. It exhibits significant anti-thrombotic activity and is implicated in therapeutic applications such as wound repair, anti-fibrosis, and anti-tumor responses. Additionally, Hirudin has been explored for its effects on diabetic complications and cerebral hemorrhage, making it a valuable reagent in various research contexts. -
Calpain Inhibitor
Z-LLY-FMK is a potent calpain inhibitor that exhibits significant effects on apoptosis across various cell systems. By inhibiting calpain activity, Z-LLY-FMK has been shown to mitigate intestinal apoptosis following common bile duct ligation and reduce parasite burden in mouse models challenged with Taenia crassiceps cysts. This reagent serves as a valuable tool for research into cysticercosis and the role of calpain in cellular processes. -
Tyrosinase Inhibitor
Aloesin is a potent tyrosinase inhibitor known for its diverse biological activities, including anti-inflammatory effects and ultraviolet protection. Additionally, it exhibits antibacterial properties and has been shown to induce apoptosis in various cancer cell lines, making it a valuable compound for research in ovarian cancer and related studies. Its multifunctional profile provides a broad spectrum of applications in both dermatological and oncology research. -
LonP1/ CT-L proteasome inhibitor
BT317 is a selective inhibitor of mitochondrial Lon peptidase I (LonP1) and the caspase-like (CT-L) activity of the proteasome. This compound has been shown to increase the production of reactive oxygen species (ROS), leading to apoptosis in astrocytoma cells. BT317 exhibits significant antitumor activity, making it a valuable reagent for research in cancer biology and therapeutic applications targeting gliomas. -
Proteasome Inhibitor
YSY01A is a potent proteasome inhibitor that promotes apoptosis in cancer cells, demonstrating IC50 values of 51.0 nM in HEK293T, 9.2 nM in A549, 5.2 nM in MCF-7, 8.9 nM in MGC-803, and 35.4 nM in PC-3M cell lines. This compound effectively disrupts constitutive STAT3 signaling by downregulating gp130 and JAK2 in human A549 lung cancer cells. YSY01A serves as a valuable tool for research in cancer therapy and apoptosis mechanisms. -
PTPN2/1 Dual Inhibitor
PTPN2/1-IN-4 is a potent dual inhibitor of PTPN1 and PTPN2, exhibiting IC50 values of 12.8 nM and 5.8 nM, respectively. This compound effectively modulates the IFNγ-JAK-STAT signaling pathway, resulting in enhanced CD8+ T-cell infiltration into tumors. PTPN2/1-IN-4 demonstrates significant anticancer activity, inhibiting tumor growth both as a standalone treatment and in combination with anti-PD-1 antibodies in B16-OVA syngeneic mouse models, making it a valuable tool for cancer research. -
Proteasome Inhibitor
Ub4ix is a potent proteasome inhibitor that selectively protects K48-linked ubiquitin chains from deubiquitinating enzymes (DUBs), thereby preventing the degradation of ubiquitin-tagged proteins. This compound has demonstrated significant biological activity, including the reduction of cell viability and induction of apoptosis in HeLa cells, with an IC50 value of 1.6 μM. Ub4ix is a valuable tool for research applications focused on understanding protein homeostasis and the role of the proteasome in cellular processes. -
uPA Inhibitor
UCD38B hydrochloride is a competitive inhibitor of urokinase-type plasminogen activator (uPA) with an IC50 value of 7 μM. This compound exhibits cell permeability and specifically targets intracellular uPA, leading to its mistrafficking into perinuclear mitochondria. This mistrafficking results in a reduction of mitochondrial membrane potential and ultimately promotes the release of apoptotic inducible factor (AIF), thereby inducing apoptosis. UCD38B hydrochloride is useful in research applications focused on cancer biology and therapeutic strategies targeting apoptosis. -
Proteasome Inhibitor
Baceridin is a proteasome inhibitor characterized as a cyclic hexapeptide. Isolated from the culture medium of Epiphytic Bacillus, it disrupts proteasome function, leading to inhibition of cell cycle progression and induction of apoptosis in tumor cells via a p53-independent mechanism. This compound is valuable for cancer research applications, particularly in studies exploring proteasome inhibition and its effects on tumor biology. -
Tubulin/MMP Inhibitor
Tubulin/MMP-IN-2 is a dual inhibitor targeting both tubulin and matrix metalloproteinases (MMPs). It effectively inhibits tubulin polymerization, leading to induced apoptosis in cancer cells. Additionally, Tubulin/MMP-IN-2 demonstrates inhibitory activity against MMP-2, MMP-3, and MMP-9, with IC50 values of 24.95 μM, 31.60 μM, and 22.37 μM, respectively. This compound is valuable for research focused on cancer biology and therapeutic development. -
γ-secretase Inhibitor
Nirogacestat dihydrobromide is a selective, noncompetitive inhibitor of γ-secretase, with a reported IC50 of 6.2 nM. This compound effectively inhibits Notch signaling, making it a valuable tool for studying Notch receptor-dependent cancers while minimizing gastrointestinal toxicity. It is particularly useful in research focused on the role of γ-secretase in cancer biology and therapeutic development. -
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. -
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.
