Catalog No.
Product Name
Application
Product Information
Citations
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Hsp-Cdc Inhibitor
Hsp90-Cdc37-IN-2 is a selective inhibitor of the interaction between heat shock protein 90 (Hsp90) and cyclin 37 (Cdc37). This compound exhibits potent anti-proliferative activity against cancer cell lines A549, MCF-7, HOS, and HepG2, with IC50 values ranging from 0.41 to 0.94 μM. Hsp90-Cdc37-IN-2 effectively disrupts mitochondrial membrane potential, induces apoptosis, and causes cell cycle arrest at the G0/G1 phase in A549 cells, making it a valuable tool for cancer research and therapeutic investigations. -
Drug Metabolite
4-Hydroperoxy cyclophosphamide is an active metabolite of the precursor cyclophosphamide, primarily targeting DNA cross-linking. This compound induces T cell apoptosis through a caspase-independent mechanism and can activate the mitochondrial death pathway via reactive oxygen species (ROS) generation. It is valuable for research applications in studying mechanisms underlying rheumatoid arthritis and other autoimmune diseases. -
RAR/RXR Agonist
9-cis-Retinoic acid is a potent RAR/RXR agonist derived from vitamin A. It plays a critical role in inducing apoptosis and regulating the cell cycle, exhibiting significant anticancer, anti-inflammatory, and neuroprotective activities. This compound is valuable for research applications aimed at understanding retinoid signaling and its implications in various biological processes and diseases. -
Endogenous Metabolite
Crocin is an endogenous metabolite derived from the stigma of Crocus sativus, recognized for its role in inhibiting tumor cell proliferation and promoting apoptosis via the JAK signaling pathway. It exhibits significant anti-inflammatory and antioxidant properties, making it a valuable compound for research in cancer biology and therapeutic development. Crocin is utilized in studies focused on its potential as an antitumor agent and its broader implications in cellular health. -
Endogenous Metabolite
Phosphocreatine is an endogenous metabolite primarily known for its role in energy metabolism within vertebrate skeletal muscle. It enhances antioxidant activity and activates the TAK1 pathway, contributing to cardiac protection. Additionally, phosphocreatine normalizes mitochondrial function and mitigates oxidative stress through the Akt-mediated Nrf2/HO-1 pathway. Furthermore, it provides renal protection by inhibiting apoptosis and reactive oxygen species (ROS) generation via the ERK-mediated Nrf2/HO-1 pathway, making it a valuable tool for research in cellular stress responses and organ protection. -
RXR Antagonist
HX531 is an orally active antagonist of the retinoid X receptor (RXR), demonstrating an IC50 of 18 nM. This compound effectively upregulates the p53-p21Cip1 pathway while counteracting the anti-apoptotic effects of trans-retinoic acid (t-RA). HX531 is characterized by its potential applications in anti-obesity, anti-diabetic, and anti-melanoma research, making it a valuable tool for investigating metabolic and cancer-related pathways. -
Phospholipase C Activator
m-3M3FBS is a potent activator of phospholipase C (PLC). It effectively stimulates superoxide generation in human neutrophils and enhances intracellular calcium concentrations, leading to inositol phosphate production in diverse cell lines. Additionally, m-3M3FBS has been shown to induce apoptosis in monocytic leukemia cells, making it valuable for studying cellular signaling pathways and apoptosis mechanisms in research applications. -
Endogenous Metabolite
N1-Acetylspermidine hydrochloride is an acetyl derivative of polyamines, serving as a substrate for polyamine oxidase (PAO). It has been shown to promote apoptosis, particularly in conjunction with procyanidins, and demonstrates cleavage efficiency at apurinic sites in DNA. This compound has valuable applications in colorectal cancer research, facilitating investigations into polyamine metabolism and its implications in tumorigenesis. -
ChA Inhibitor
α-NETA is a potent noncompetitive inhibitor of choline acetyltransferase (ChA), exhibiting an IC50 value of 9 μM. Additionally, it displays strong antagonistic activity against aldehyde dehydrogenase 1A1 (ALDH1A1) with an IC50 of 0.04 µM and also targets chemokine-like receptor-1 (CMKLR1). While it shows some inhibitory effects on cholinesterase (ChE) and acetylcholinesterase (AChE) with higher IC50 values, α-NETA is notable for its anti-cancer properties, making it a valuable tool for research in cancer biology and neuropharmacology. -
CYP450 ω-Hydroxylase Inhibitor
17-ODYA is a selective CYP450 ω-hydroxylase inhibitor, demonstrating potent inhibition (IC50<100 nM) of 20-hydroxyeicosatetraenoic acid (20-HETE) and related eicosanoids in rat renal cortical microsomes. This compound effectively prevents isoproterenol-induced apoptosis and necrosis in cultured cardiomyocytes. Additionally, 17-ODYA serves as a click chemistry reagent with an alkyne group, facilitating copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules, making it a valuable tool for various biochemical applications. -
Endogenous Metabolite
Linolelaidic acid is an omega-6 trans fatty acid that functions as an endogenous metabolite with critical roles in human physiology. This compound exhibits anti-inflammatory and anti-parasitic activities, and has been shown to induce apoptosis in various cell types. Linolelaidic acid is relevant for research applications in the study of infections and nutritional science, particularly concerning enteral and parenteral nutrition as well as infant formula development. -
AhR agonist
β-Naphthoflavone is a potent aryl hydrocarbon receptor (AHR) agonist that modulates various biological processes, including cell proliferation, differentiation, apoptosis, and metabolism. This compound exhibits antioxidant activity, primarily by enhancing the function of antioxidant enzymes. As a non-carcinogenic CYP1A inducer, β-Naphthoflavone is valuable for investigating the mechanisms underlying aristolochic acid-induced renal injury and other related research applications. -
RARα Antagonist
Ro 41-5253 is a selective antagonist of the retinoic acid receptor alpha (RARα). It effectively binds to RARα without promoting transcriptional activity or influencing RAR/RXR heterodimerization and DNA binding. This compound demonstrates significant inhibition of cancer cell proliferation and can induce apoptosis, highlighting its potential as an antitumor agent in cancer research applications. -
SCD1 Inhibitor
SSI-4 is a potent stearoyl-CoA desaturase (SCD1) inhibitor with an EC50 of 1.9 nM for mouse SCD1. By blocking the conversion of saturated fatty acids to monounsaturated fatty acids, SSI-4 effectively reduces oleic and palmitoleic acid production. It promotes lipid peroxidation, induces endoplasmic reticulum stress, and activates apoptotic pathways. Additionally, SSI-4 inhibits mTORC1 activity, suppresses B cell proliferation and antibody production, and induces autophagy. This compound is valuable for studies related to cancers such as acute myeloid leukemia and renal cell carcinoma, as well as influenza infections. -
Monoamine Oxidase Inhibitor
4-Hydroxyderricin is a selective inhibitor of Monoamine Oxidase B (MAO-B) with an IC50 of 3.43 μM, making it a valuable tool for studying neurological conditions. In addition to its primary mechanism, it exhibits mild inhibition of dopamine β-hydroxylase activity. This compound has demonstrated a range of biological activities, including antidepressant, anti-allergic, anti-diabetic, antioxidant, and antitumor effects. It has been shown to induce apoptosis and cell cycle arrest in hepatocellular carcinoma cells via modulation of the PI3K/AKT/mTOR pathway, as well as enhance osteoblast differentiation while inhibiting osteoclast formation, positioning it as a promising candidate for research into inflammatory diseases. -
Endogenous metabolite
6-Oxolithocholic acid is an endogenous bile acid metabolite primarily involved in bile acid metabolism and cholesterol synthesis regulation. It exhibits significant cytotoxic effects and can induce apoptosis in hepatocytes. This compound is valuable for research into the roles of bile acids in various health conditions, particularly in the context of digestive and liver diseases. -
α-mannosidases inhibitor
Kifunensine is a potent and selective inhibitor of class I α-mannosidases, originally isolated from *Actinomycete* species. It blocks the trimming of mannose residues from N-linked glycoproteins by inhibiting α-mannosidase I activity, thereby preventing proper glycoprotein maturation. Through this mechanism, Kifunensine disrupts endoplasmic reticulum–associated degradation (ERAD) pathways, leading to the accumulation of misfolded glycoproteins. It is widely used as a biochemical tool in studies of protein folding, quality control, and glycosylation. - NNK is a tobacco-specific nitrosamine derived from nicotine and is a well-established carcinogenic compound. It activates both ERK1/2 and PKCα signaling pathways, leading to phosphorylation of Bcl-2 at Ser70 and c-Myc at Thr58 and Ser62, thereby promoting cell survival and proliferation in human lung cancer cells. Due to its strong tumorigenic potential, NNK is widely used to induce lung cancer in experimental mouse models for studying carcinogenesis and evaluating anticancer therapeutics.
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ferroptosis inducer
Solasonine is a naturally occurring steroidal glycoalkaloid isolated from *Solanum melongena* (eggplant), known for its anti-infective, anticancer, and neurogenesis-promoting properties. It acts as a ferroptosis inducer by disrupting the glutathione redox system through inhibition of glutathione peroxidase 4 (GPX4). By promoting ferroptotic cell death in hepatocellular carcinoma (HCC) cells, Solasonine serves as a valuable compound for investigating ferroptosis mechanisms and developing novel anticancer strategies. -
Fluorescent Dye
BODIPY 581/591 C11 is a boron-dipyrromethene (BODIPY) derivative with excellent photostability and minimal fluorescence artifacts. It is widely used to study lipid peroxidation and antioxidant activity in living cells, and to detect ferroptosis through its reaction with hydroxyl radicals. The dye exhibits a fluorescence shift upon oxidation: the reduced form emits at 591 nm (Ex: 581 nm), while the oxidized form emits at 510 nm (Ex: 500 nm). -
TrxR-1 inhibitor
Manumycin A is a polyketide antibiotic that functions as an inhibitor of thioredoxin reductase 1 (TrxR-1). It exhibits anti-tumor activity by inhibiting breast cancer cell growth, potentially through LC3-mediated mechanisms. Manumycin A also downregulates pro-inflammatory cytokine release in TNF-α-stimulated human monocytes, indicating anti-inflammatory potential. Additionally, it inhibits the Ras/Raf/ERK1/2 signaling pathway and hnRNP H1 in castration-resistant prostate cancer cells, thereby suppressing exosome biogenesis and secretion. - Pyridoxal 5′-phosphate monohydrate is the active coenzyme form of vitamin B6 and is essential for the function of numerous enzymes. It serves as a key cofactor for aromatic L-amino acid decarboxylase, which catalyzes the final step in the biosynthesis of the neurotransmitters dopamine and serotonin. Pyridoxal 5′-phosphate is the primary intracellular phosphorylated form of vitamin B6 and is interconvertible with other forms, including pyridoxine 5′-phosphate (PNP) and pyridoxamine 5′-phosphate (PMP).
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Endogenous Metabolite
ATP (Adenosine 5'-triphosphate) dimagnesium is a key molecule in cellular energy storage and metabolism. It supplies metabolic energy for ion pumps and other enzymatic processes and functions as a coenzyme in numerous cellular reactions. Additionally, ATP dimagnesium acts as an important endogenous signaling molecule involved in immune and inflammatory responses. -
PCSK9 inhibitor
PF-06446846 hydrochloride is an orally active and highly selective inhibitor of the translation of proprotein convertase subtilisin/kexin type 9 (PCSK9). It inhibits PCSK9 expression by inducing ribosomal stalling at approximately codon 34 during translation. -
BRD4/NAMPT inhibitor
BRD4/NAMPT-IN-1 (Compound A2) is a dual inhibitor of NAMPT and BRD4, with IC₅₀ values of 35 nM and 58 nM, respectively. It suppresses the growth and migration of hepatocellular carcinoma cells and induces apoptosis. In the HCCLM3 xenograft mouse model, BRD4/NAMPT-IN-1 exhibits potent anticancer activity without apparent toxicity. - Ganodermanontriol, a sterol isolated from *Ganoderma lucidum*, exerts anti-inflammatory effects in tert-butyl hydroperoxide (t-BHP)-damaged hepatic cells by upregulating heme oxygenase-1 (HO-1) expression. It demonstrates hepatoprotective activity.
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5-Methyldeoxycytidine
5-Methyl-2'-deoxycytidine (5mdC) is an endogenous substrate of DNA methyltransferases, including mammalian 5-C-MTase, and binds to DNA in a manner dependent on DNA stem-loop structure formation. It directs de novo DNA methylation by serving as a methylation mark, promoting methylation of adjacent CpG sites in single-stranded DNA via cis-acting mechanisms. 5mdC regulates DNA methylation patterns by recruiting methyltransferases to specific chromatin regions, influencing chromatin condensation and gene expression. In plant cells, its distribution correlates with cell proliferation and differentiation stages, with lower methylation levels in proliferating cells and higher levels in differentiated cells. -
NNMT inhibitor
NNMTi is a potent nicotinamide N-methyltransferase (NNMT) inhibitor with an IC₅₀ of 1.2 μM. It selectively binds to residues within the NNMT substrate-binding site. NNMTi promotes myoblast differentiation in vitro and enhances the fusion and regenerative capacity of muscle stem cells (muSCs) in aged mice, making it a promising compound for research into muscle regeneration and age-related muscle decline. -
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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COX/LOX inhibitor
Phenidone is an orally active dual inhibitor of cyclooxygenase (COX) and lipoxygenase (LOX) pathways, exhibiting anti-inflammatory and immunomodulatory effects. It has been shown to ameliorate paralysis in rat models of experimental autoimmune encephalomyelitis (EAE), a model for multiple sclerosis. Phenidone also acts as a potent hypotensive agent in spontaneously hypertensive rats. Additionally, it has a long-standing application as a photographic developer due to its redox properties. -
HO-1 inhibitor
Tin protoporphyrin IX dichloride (SnPPIX) is a potent inhibitor of heme oxygenase-1 (HO-1), an enzyme involved in cellular stress responses and tumor progression. SnPPIX has been shown to sensitize pancreatic ductal adenocarcinoma (PDAC) tumors to chemotherapy in mouse models, enhancing therapeutic efficacy and supporting its potential use as a chemosensitizing agent in cancer treatment. -
20-HETE synthase inhibitor
HET0016 is a potent and selective inhibitor of 20-hydroxyeicosatetraenoic acid (20-HETE) synthase, with IC50 values of 17.7 nM, 12.1 nM, and 20.6 nM for CYP4A1-, CYP4A2-, and CYP4A3-mediated 20-HETE synthesis, respectively. It also acts as a selective cytochrome P450 (CYP450) inhibitor and has been shown to suppress angiogenesis and tumor growth, making it a valuable compound for cancer and vascular research. - Enrofloxacin monohydrochloride (BAY Vp 2674 monohydrochloride) is a broad-spectrum antibiotic with demonstrated efficacy against *Mycoplasma bovis*, exhibiting a MIC₉₀ of 0.312 μg/mL. In addition to its antibacterial properties, it also shows inhibitory activity against vaccinia virus (VV), indicating potential antiviral applications.
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PAF activator
C16-PAF (PAF (C16)) is a phospholipid mediator and a potent platelet-activating factor that functions as a ligand for the PAF G-protein-coupled receptor (PAFR). It exhibits anti-apoptotic effects by inhibiting caspase-dependent cell death through PAFR activation. C16-PAF is a strong activator of the MAPK and MEK/ERK signaling pathways and is known to induce increased vascular permeability. -
LOX inhibitor
LXG6403 is a highly potent and irreversible lysyl oxidase (LOX) inhibitor that efficiently suppresses cellular LOX activity in MDA-MB-231 cells with an IC50 of 1.3 μM. It exhibits over 3-fold selectivity for LOX over LOXL2 and shows no inhibitory activity against LOXL1, making it a valuable tool for studying LOX-specific functions in cancer and fibrosis research. -
PPAR agonist
Lobeglitazone sulfate is a novel thiazolidinedione and an orally active agonist of peroxisome proliferator-activated receptors (PPARs), with EC50 values of 137.4 nM for PPARγ and 546.3 nM for PPARα. It also acts as an inhibitor of the ERK/JNK/Smad/NF-κB signaling pathways. Lobeglitazone sulfate exhibits anti-inflammatory, anti-diabetic, anti-fibrotic, and anti-atherosclerotic activities, supporting its potential in the treatment of metabolic and inflammatory diseases. -
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. -
DNA gyrase inhibitor/Hsp90 antagonist
Novobiocin (Albamycin) is a potent and orally active antibiotic that functions as a DNA gyrase inhibitor and a heat shock protein 90 (Hsp90) antagonist. It holds potential for research into highly β-lactam-resistant pneumococcal infections and has demonstrated antiviral activity against orthopoxviruses. -
PCSK9 inhibitor
AZD0780 (PCSK9-IN-12) is a heteroaryl compound with high binding affinity for proprotein convertase subtilisin/kexin type 9 (PCSK9), exhibiting a Kd value of <200 nM. It is a valuable tool for research in cholesterol metabolism and PCSK9-related therapeutic pathways. - 7-Hydroxyflavone is an orally active flavonoid isolated from *Clerodendrum phlomidis*, exhibiting notable anti-inflammatory activity. It protects renal cells from nicotine-induced cytotoxicity through activation of the ERK/Nrf2/HO-1 signaling pathway. Additionally, 7-Hydroxyflavone inhibits PKM2 with an IC50 of 2.12 μM, and suppresses COX-2 and 5-LOX with IC50 values of 27 μg/mL and 33 μg/mL, respectively.
- Gondoic acid (cis-11-Eicosenoic acid) is a monounsaturated long-chain fatty acid found in various plant oils and nuts. It exhibits anti-inflammatory activity by reducing reactive oxygen species (ROS) production and inhibiting the PKCθ/ERK/STAT3 signaling pathway. Gondoic acid is also utilized as a raw material in medical applications and as a moisturizing agent in cosmetic formulations.
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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. -
EGFR/PI3K Inhibitor
MTX-531 is an orally active small molecule that inhibits EGFR (IC50 = 14.7 nM) and multiple PI3K isoforms, with IC50 values of 6.4 nM (PI3Kα), 233 nM (PI3Kβ), 8.3 nM (PI3Kγ), and 1.1 nM (PI3Kδ), demonstrating potent antitumor activity. Additionally, MTX-531 functions as a weak PPARγ agonist (IC50 = 2.5 µM), which may mitigate PI3K inhibitor-induced hyperglycemia. -
Vitamin B6 Derivative
Pyridoxal 5′-phosphate hydrate (PLP) is the biologically active form of vitamin B6 and serves as an essential cofactor for over 100 enzymatic reactions, particularly those involved in amino acid metabolism. It plays a critical role in the function of aromatic L-amino acid decarboxylase, the enzyme responsible for catalyzing the final step in the synthesis of key neurotransmitters such as dopamine and serotonin. PLP is the principal coenzyme form generated through intracellular phosphorylation of vitamin B6 precursors and is interconvertible with other phosphorylated forms, including pyridoxine 5′-phosphate (PNP) and pyridoxamine 5′-phosphate (PMP). -
Hsp90/HSV inhibitor
AT-533 is a potent inhibitor of heat shock protein 90 (Hsp90) and herpes simplex virus (HSV), exhibiting strong antitumor and antiviral activities. It suppresses tumor growth and angiogenesis by disrupting the HIF-1α/VEGF/VEGFR-2 signaling axis, a critical pathway in tumor vascularization and progression. Additionally, AT-533 inhibits key downstream signaling cascades, including Akt/mTOR/p70S6K, ERK1/2, and FAK pathways. In endothelial cells, specifically human umbilical vein endothelial cells (HUVECs), AT-533 effectively inhibits tube formation, cell migration, and invasion, highlighting its anti-angiogenic properties. These combined effects position AT-533 as a promising candidate for cancer therapy and angiogenesis-related disease research. -
POLRMT inhibitor
IMT1 is a first-in-class, specific, and noncompetitive inhibitor of human mitochondrial RNA polymerase (POLRMT). It induces a conformational change in POLRMT, preventing substrate binding and inhibiting transcription in a dose-dependent manner in vitro. IMT1 decreases deoxynucleoside triphosphate levels and citric acid cycle intermediates, leading to significant depletion of cellular amino acid levels. IMT1 holds potential for the treatment of diseases associated with mitochondrial transcription disorders.
