Catalog No.
Product Name
Application
Product Information
Citations
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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. - Deltonin is a steroidal saponin isolated from *Dioscorea zingiberensis*, exhibiting notable antitumor activity. It exerts its effects by inhibiting the activation of key survival and proliferation pathways, specifically ERK1/2 and AKT signaling. Through this dual inhibition, Deltonin suppresses tumor cell growth and promotes apoptosis, making it a promising candidate for further investigation in cancer research and therapeutic development.
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PPAR agonist
Lobeglitazone is a novel thiazolidinedione-class compound and an orally active dual agonist of peroxisome proliferator-activated receptors (PPARs), with EC₅₀ values of 137.4 nM for PPARγ and 546.3 nM for PPARα. In addition to its metabolic effects, Lobeglitazone functions as an inhibitor of multiple pro-inflammatory and pro-fibrotic signaling pathways, including ERK, JNK, Smad, and NF-κB. Lobeglitazone exhibits a broad range of pharmacological activities, including anti-inflammatory, anti-diabetic, anti-fibrotic, and anti-atherosclerotic effects. These properties make it a promising candidate for therapeutic research in metabolic syndrome, type 2 diabetes, cardiovascular disease, and fibrosis-related conditions. -
Endogenous Metabolite
Gamma-linolenic acid (γ-linolenic acid, GLA) is an orally active omega-6 unsaturated fatty acid with broad pharmacological activities. It exhibits anti-inflammatory effects by inhibiting the NF-κB signaling pathway and suppressing the phosphorylation of ERK1/2 and JNK, key mediators of inflammatory responses. GLA also induces apoptosis in cancer cells, contributing to its anticancer potential. Additionally, it possesses antioxidant properties and has been shown to improve memory function, suggesting neuroprotective benefits. These multifunctional effects position gamma-linolenic acid as a promising compound for research in inflammation, oncology, and neurological disorders. -
PDE4/NF-κB inhibitor
Sappanone A is an orally active homoisoflavone isolated from Caesalpinia sappan L., exhibiting notable anti-inflammatory and antioxidant properties. It functions as an inhibitor of phosphodiesterase 4 (PDE4) and NF-κB, key regulators of inflammatory signaling. Additionally, Sappanone A activates the Nrf2 pathway, leading to increased expression of the cytoprotective enzyme heme oxygenase-1 (HO-1). Sappanone A also inhibits RANKL-induced osteoclastogenesis, suggesting potential benefits in bone metabolism disorders. With its multifaceted bioactivity, Sappanone A holds significant promise for research in inflammation-related diseases, cardiovascular conditions, and bone health. -
phospholipase A2/HDAC2 inhibitor
Rhamnetin is a naturally occurring flavonoid and quercetin derivative found in *Coriandrum sativum*. It functions as an inhibitor of secretory phospholipase A₂ and histone deacetylase 2 (HDAC2), contributing to its broad pharmacological profile. Rhamnetin exhibits notable antitumor, antioxidant, and anti-inflammatory activities, making it a promising compound for research in cancer, oxidative stress-related conditions, and inflammatory diseases. -
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. -
Endogenous Metabolite
Triacetin (Glyceryl triacetate) is an orally active synthetic triester of glycerol and acetic acid that serves as a bioavailable source of acetate. It freely crosses the blood–brain barrier and cellular membranes, making it particularly effective in targeting central nervous system malignancies. In glioma cells, Triacetin increases intracellular acetate levels, promotes histone acetylation, and induces cell cycle arrest and apoptosis. Additionally, Triacetin enhances the chemotherapeutic efficacy of Temozolomide (TMZ), supporting its potential as an adjuvant in glioma treatment strategies. -
PDE6D/IKZF1/IKZF3/CK1α Degrader
FPFT-2216 is a “molecular glue” degrader that facilitates the proteasomal degradation of multiple target proteins, including phosphodiesterase 6D (PDE6D), zinc finger transcription factors Ikaros (IKZF1) and Aiolos (IKZF3), as well as casein kinase 1α (CK1α). By promoting selective ubiquitination through E3 ligase recruitment, FPFT-2216 modulates key regulatory pathways and holds promise for research in oncology and inflammatory diseases. -
Ferroptosis inhibitor
SRS11-92 is a potent ferroptosis inhibitor and structural analogue of Ferrostatin-1 (Fer-1). It effectively blocks Erastin-induced ferroptotic cell death in HT-1080 human fibrosarcoma cells, with an EC₅₀ of 6 nM. SRS11-92 serves as a valuable tool for studying ferroptosis and its therapeutic modulation in oxidative stress-related diseases and cancer. -
FFAR3 agonist
AR420626 is a selective agonist of free fatty acid receptor 3 (FFAR3, also known as GPR41), with an IC₅₀ of 117 nM. It demonstrates anti-inflammatory, antitumor, and antidiabetic activities. AR420626 improves neurogenic diarrhea by modulating neural pathways mediated by nicotinic acetylcholine receptors (nAChRs). In cancer models, it suppresses the growth of HepG2 xenografts and inhibits hepatoma cell proliferation through apoptosis induction. Additionally, AR420626 mitigates allergic asthma and eczema and enhances glucose uptake by activating FFAR3-mediated Ca²⁺ signaling, offering potential therapeutic benefits in metabolic disorders such as diabetes. -
PROTAC NCOA4 degrader
PROTAC NCOA4 Degrader-1 (Compound V3) is a highly potent PROTAC targeting NCOA4, with a DC₅₀ of 3 nM in HeLa cells. It functions as a ferroptosis inhibitor by reducing NCOA4 levels and lowering intracellular ferrous iron (Fe²⁺) concentrations. PROTAC NCOA4 Degrader-1 has demonstrated protective effects in a CCl₄-induced acute liver injury model, making it a valuable tool for studying ferroptosis and liver disease therapeutics. -
PROTAC HK2 Degrader
C-02 is a PROTAC molecule composed of the hexokinase inhibitor lonidamine linked to the cereblon ligand thalidomide. It selectively degrades hexokinase 2 in 786-O and PANC-1 cells at 20 µM. C-02 exhibits cytotoxicity across multiple cancer cell lines, with IC₅₀ values of 34.07 µM (786-O), 5.08 µM (4T1), 31.53 µM (PANC-1), 6.11 µM (HGC-27), and 21.65 µM (MCF-7), supporting its use in cancer metabolism research. -
PROTAC SGK3 degrader
SGK3-PROTAC1 is a PROTAC molecule designed to selectively degrade SGK3 by linking the 308-R SGK inhibitor to the VHL-binding ligand VH032. Through recruitment of the VHL E3 ligase, SGK3-PROTAC1 induces proteasomal degradation of SGK3, providing a targeted approach for studying SGK3 function in cellular signaling and disease. -
MAO/LSD1 Inhibitor
Tranylcypromine hemisulfate is an irreversible, nonselective inhibitor of monoamine oxidase (MAO) and also acts as a lysine-specific demethylase 1 (LSD1) inhibitor. This compound demonstrates notable antidepressant effects and is utilized in the treatment of depression. Additionally, tranylcypromine hemisulfate has been shown to suppress lesion growth and alleviate generalized hyperalgesia in mouse models of induced endometriosis, making it a valuable tool for research in both psychiatric and pain-related studies. -
5-LO Inhibitor
EP6 is a selective 5-Lipoxygenase (5-LO) inhibitor that exhibits potent anti-tumor activity. It effectively reduces the viability of various tumor cell lines while demonstrating a lack of mutagenic properties. This compound is valuable for research applications focused on cancer therapy and the modulation of inflammatory pathways. -
PROTAC Nampt Degrader
Nampt degrader-2 is a potent PROTAC designed to target and degrade nicotinamide adenine dinucleotide (NAD+) precursor NAMPT with an IC50 of 41.9 nM. By forming a ternary complex with NAMPT and VHL, it effectively induces degradation through the ubiquitin-proteasome system. This compound significantly reduces NAD+ levels and demonstrates remarkable antitumor activity, making it a valuable tool for cancer research and therapeutic exploration. -
PROTAC HSP90 Degrader
PROTAC HSP90 Degrader BP3 is a selective agent designed for targeted degradation of Heat Shock Protein 90 (HSP90) through a CRBN-dependent mechanism. This compound effectively degrades HSP90 in MCF-7 breast cancer cells, with a DC50 value of 0.99 µM, and demonstrates significant inhibition of cell growth. Additionally, BP3 features an alkyne group that enables it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc), making it a versatile tool for advanced chemical biology applications. -
IDH1 Inhibitor
GSK321 is a potent and selective inhibitor of mutant isocitrate dehydrogenase 1 (IDH1), showing IC50 values of 2.9, 3.8, 4.6, and 46 nM for the R132G, R132C, R132H, and wild-type IDH1 variants, respectively, with over 100-fold selectivity for IDH2. This compound effectively reduces intracellular levels of α-Hydroxyglutaric acid (2-HG), disrupts the myeloid differentiation block, and promotes granulocytic differentiation in leukemic blasts and stem-like cells. GSK321 is valuable for research on acute myeloid leukemia (AML) and various other malignancies. -
AHR Agonist
Indole-3-pyruvic acid is an orally active agonist of the aryl hydrocarbon receptor (AHR). This compound exhibits antioxidant properties and is valuable for research into inflammation and anxiety-related pathways. Its role as an AHR modulator makes it a significant tool for studying the physiological effects of this receptor in various biological contexts. -
Endogenous Metabolite
Ergothioneine is an endogenous metabolite that acts as a potent antioxidant. It functions primarily as a specific inhibitor of p38 MAPK and Akt, which are critical signaling pathways involved in cellular stress responses. Ergothioneine is utilized in research focused on neuroprotection, cell apoptosis, and oxidative stress, making it a valuable compound for investigations into cellular resilience and health. -
PPARγ Agonist
Ciglitazone is a potent and selective agonist of the peroxisome proliferator-activated receptor gamma (PPARγ), with an EC50 of 3 μM. It effectively inhibits the proliferation and differentiation of Th17 cells and serves as a hypoglycemic agent in obese-hyperglycemic animal models. Additionally, Ciglitazone promotes apoptosis through the activation of p38 MAPK and facilitates the nuclear translocation of apoptosis-inducing factor (AIF) in opossum kidney (OK) renal epithelial cells, making it a valuable tool for research in metabolic and renal diseases. -
Secondary Metabolite
Atranorin is a secondary metabolite derived from lichens that acts as an AKT inhibitor. This compound demonstrates a wide range of biological activities, including antibacterial, anti-inflammatory, antioxidant, anti-glycation, analgesic, and anti-tumor effects. Notably, Atranorin has IC50 values of 117 μM for scavenging DPPH free radicals and less than 10 μM for ABTS radicals, highlighting its potent antioxidant capacity. Additionally, Atranorin promotes wound healing and can be utilized in research focused on myelodysplastic syndromes, tumors, and various inflammatory conditions. -
Kinases PROTAC
DB1113 is a bifunctional compound designed for targeted protein degradation of various kinases. It effectively induces degradation of ABL1, ABL2, BLK, CDK4, CDK11B, EPHA3, MAPK7, RIPK1, and others, facilitating the investigation of kinase-related signaling pathways. DB1113 is suitable for research focusing on diseases or disorders associated with dysregulated kinase activity, providing a valuable tool for exploring therapeutic interventions in cancer and other conditions. -
RNA RIBOTAC Degrader
Dovitinib-RIBOTAC TFA is a targeted RNA RIBOTAC degrader that specifically binds to and degrades pre-miR-21. This compound demonstrates significant anti-tumor activity and effectively inhibits breast cancer metastasis. It serves as a valuable tool for research involving RNA-targeted degradation and its implications in cancer biology. -
PROTAC IDO1 Degrader
PROTAC IDO1 Degrader-1 is a novel compound targeting indoleamine 2,3-dioxygenase 1 (IDO1) through the engagement of Cereblon E3 ligase, facilitating its ubiquitination and subsequent degradation. With a reported DC50 of 2.84 μM, this degrader enhances the anti-tumor efficacy of HER2 CAR-T cells, making it a valuable tool for research in cancer immunotherapy and targeted degradation methods. Its ability to modulate IDO1 levels opens avenues for investigations into metabolic regulation and tumor microenvironment interactions. -
Natural Retinoid
9-cis-Retinal is a natural retinoid that serves as a crucial signaling molecule in visual processes. It is produced from dietary 9-cis-β-carotene through enzymatic cleavage. This compound exhibits high-affinity binding to cellular retinol-binding proteins CRBP-I and CRBP-II, with dissociation constants of 8 nM and 5 nM, respectively. 9-cis-Retinal plays a significant role in promoting differentiation and maturation of rod photoreceptors in retinal organoid models, making it valuable for research in vision science and photoreceptor development. -
RAR Agonist
EC23 is a retinoid analogue that acts as a retinoic acid receptor (RAR) agonist. This compound prompts neuronal differentiation, making it a valuable tool for studying neurodevelopmental processes and related disorders. Its stability enhances its suitability for various biological assays and research applications in the field of neurobiology. -
Anti-aging Peptide
Acetyltetrapeptide 11 is a bioactive peptide recognized for its anti-aging properties. It functions by promoting collagen synthesis and enhancing skin elasticity, making it valuable in cosmetic formulations aimed at reducing signs of aging. Its application extends to skincare products where it aids in rejuvenating and revitalizing the skin. -
Human Endogenous Metabolite
Estradiol (β-Estradiol) is a steroid hormone and the major female sex hormone. Estradiol can up-regulate the expression of neural markers of human endometrial stem cells (hEnSCs) and promote their neural differentiation. Estradiol can be used for the research of cancers, neurodegenerative diseases and neural tissue engineering. -
SIRT Inhibitor
Nicotinamide is a form of vitamin B3 or niacin. Nicotinamide Hydrochloride inhibits SIRT2 activity (IC50: 2 μM). Nicotinamide also inhibits SIRT1. Nicotinamide increases cellular NAD+, ATP, ROS levels. Nicotinamide inhibits tumor growth and improves survival. Nicotinamide also has anti-HBV activity. -
Endogenous Glucocorticoids
Corticosterone (17-Deoxycortisol) is an orally active and adrenal cortex-produced glucocorticoid, which plays an important role in regulating neuronal functions of the limbic system (including hippocampus, prefrontal cortex, and amygdala). Corticosterone increases the Rab-mediated AMPAR membrane traffic via SGK-induced phosphorylation of GDI. Corticosterone also interferes with the maturation of dendritic cells and shows a good immunosuppressive effect. -
Monounsaturated Fatty Acid
Oleic acid (9-cis-Octadecenoic acid) is an abundant monounsaturated fatty acid. Oleic acid is a Na+/K+ ATPase activator. -
omega-3 Fatty Acid
Docosahexaenoic Acid (DHA) is an omega-3 fatty acid abundantly present brain and retina. It can be obtained directly from fish oil and maternal milk. -
Endogenous Metabolite
ATP (Adenosine 5'-triphosphate) is a central component of energy storage and metabolism in vivo. ATP provides the metabolic energy to drive metabolic pumps and serves as a coenzyme in cells. ATP is an important endogenous signaling molecule in immunity and inflammation. ATP can activate the NLRP3 inflammasome and induce IL-1β and chemokines secretion. ATP has anti-bacterial infection effects and can protect mice against bacterial infection in mice. -
Mitochondrial ROS Indicator
MitoSOX Red is a live cell fluorescent probe that specifically targets mitochondria and is cell membrane permeable. MitoSOX Red enters mitochondria and is oxidized by superoxide but not by other ROS or RNS generating systems. The oxidized MitoSOX Red then binds to nucleic acids in mitochondria/nucleus, producing strong red fluorescence. MitoSOX Red can be used as a fluorescent indicator to specifically detect superoxide. In addition, superoxide dismutase (SOD) can prevent the oxidation of MitoSOX Red. Excitation/emission wavelength: 510/580 nm.
