Catalog No.
Product Name
Application
Product Information
Citations
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PTBP1 Inhibitor
PT109 is a potent inhibitor of the protein-targeting poly(A)-binding protein 1 (PTBP1). By promoting the conversion of the pyruvate kinase isoform from PKM2 to PKM1, PT109 effectively suppresses the proliferation and migration of glioblastoma multiforme and facilitates its reprogramming into oligodendrocytes. Additionally, PT109 interacts with key signaling pathways, including JNK, SGK1, and GSK3β, conferring neuroprotective effects that enhance neurogenesis, foster synapse formation, and mitigate neuroinflammation. In models of Alzheimer's disease, PT109 demonstrates significant improvements in spatial learning, making it a valuable tool for researching metabolic reprogramming in glioblastoma and neuroprotection in neurodegenerative disorders. -
Phospholipase A Metabolite
Glycerophosphoinositol 4-phosphate (GroPIns-4-P) is a metabolite of phospholipase A that functions as an inhibitor of adenylyl cyclase. This compound plays a crucial role in regulating cAMP-dependent cellular activities and can stimulate the formation of membrane ruffles and stress fibers in serum-starved Swiss 3T3 cells by activating small GTPases Rac and Rho. Glycerophosphoinositol 4-phosphate is valuable for research involving cancer cell motility and invasiveness. -
PDE6D/CK1α Degrader
TMX-4113 is a degrader targeting phosphodiesterase 6D (PDE6D) and casein kinase 1α (CK1α). This compound exhibits significant biological activity in the degradation of these proteins, making it a valuable tool for investigating their roles in cancer research. TMX-4113 can facilitate studies aimed at elucidating the molecular mechanisms underlying tumor progression and treatment responses. -
RARγ Agonist
CD1530 is a selective agonist of retinoic acid receptor gamma (RARγ) with notable antibacterial properties. It effectively decreases the phosphorylation of Smad1/5/8 and overall Smad levels, leading to a reduction in β-catenin, MMP9 protein, and reactive oxygen species (ROS) levels. CD1530 is utilized in research focusing on orthopedic conditions, such as heterotopic ossification and Achilles tendon injuries, as well as muscle disorders related to fatty infiltration. -
TMA /TMAO Inhinbitor
3,3-Dimethyl-1-butanol is an orally active inhibitor of trimethylamine (TMA) and trimethylamine N-oxide (TMAO), acting via the suppression of the p65 NF-κB signaling pathway and the TGF-β1/Smad3 pathway. This compound exhibits significant potential in the study of cardiovascular diseases (CVD), making it a valuable reagent for researchers investigating the molecular mechanisms underlying these conditions. -
HSP60 Inhibitor
DCEM1 is a potent inhibitor of heat shock protein 60 (HSP60), disrupting its interaction with ClpP and thereby impeding the mitochondrial unfolded protein response. This compound has been shown to significantly inhibit β-catenin expression and ATP production in both PC-3 and TKO cell lines. DCEM1 is a valuable tool for investigating the role of HSP60 in prostate cancer research and understanding its impact on cellular metabolism and signaling pathways. -
LXR/RXR Agonist
UAB116 is an agonist of the Liver X Receptor (LXR) and Retinoid X Receptor (RXR). It exhibits significant biological activity by diminishing the metastatic phenotype in hepatoblastoma, primarily through inhibition of the Wnt/β-Catenin signaling pathway via upregulation of TRIM29. UAB116 effectively reduces cell proliferation, stemness, and invasiveness in metastatic hepatoblastoma cells, making it a valuable tool for research in cancer biology and therapeutic development. -
Hsp90 Inhibitor
BIIB021 mesylate is a potent inhibitor of the heat shock protein 90 (Hsp90). This orally active compound effectively inhibits the proliferation of chronic myeloid leukemia (CML) cells, demonstrating IC50 values of 513.99 nM for K562, 603.53 nM for K562/G, 110.08 nM for 32Dp210, and 148.07 nM for 32Dp210-T315I cell lines. BIIB021 promotes the degradation of the BCR-ABL protein and suppresses the β-catenin/c-Myc pathway, while also inducing autophagy in CML cells. This compound serves as a valuable tool for research focused on CML and Hsp90-related pathways. -
Endogenous Metabolite
9,10-EpOME (9,10-Epoxyoctadecenoic acid) is a cytochrome P450-derived metabolite of linoleic acid. It is known to induce oxidative stress by activating the NF-κB and AP-1 transcription factors and facilitates the chemotaxis of human neutrophils. Additionally, 9,10-EpOME has been shown to induce mechanical and thermal pain in wild-type mice via the PKA pathway. This compound is useful for investigating mechanisms of inflammation and pain in research settings. -
Ferroptosis/DNA Damage Inducer
HJ03 is a potent inducer of ferroptosis that targets DNA damage pathways. It enhances intracellular reactive oxygen species (ROS) levels, facilitates Fe2+ accumulation, and promotes lipid peroxidation, ultimately leading to the induction of DNA adducts and interstrand crosslinks. By inhibiting DNA replication and transcription, HJ03 effectively arrests the cell cycle at the G2/M phase and triggers apoptosis. This reagent is valuable for investigating glioblastoma multiforme and colorectal cancer research. -
AHR Agonist
AHR Agonist 10 is a potent agonist of the aryl hydrocarbon receptor (AHR), exhibiting an EC50 of 2.01 nM. This compound significantly upregulates the expression of AHR downstream target genes, such as CYP1A1 and CYP1B1, while downregulating pro-inflammatory markers including CD36, IL-18, CCL5, CCL20, IL-6, and TNF-α. AHR Agonist 10 demonstrates low cytotoxicity (above 40 μM) in normal cells, making it suitable for use in psoriasis research and studies investigating AHR-dependent modulation of inflammatory responses. -
AHR Agonist
PY109 is a highly selective aryl hydrocarbon receptor (AHR) agonist that exhibits oral bioactivity. It demonstrates potent efficacy with EC50 values of 1.2 nM in human HepG2 cells and 1.4 nM in mouse Hepa-1c1c7 cells. PY109 significantly enhances the expression of CYP1A1 and interleukin-22 (IL-22), while inhibiting interleukin-17A (IL-17A) expression. This compound has been shown to effectively improve colitis in murine models, making it a valuable tool for research focused on inflammatory bowel diseases. -
Cathepsin L Inhibitor
Cathepsin L-IN-6 is a selective inhibitor of cathepsin L, exhibiting an IC50 value of 0.021 μM. It functions by directly binding to cathepsin L, effectively suppressing its enzymatic activity. Additionally, Cathepsin L-IN-6 inhibits pro-inflammatory cytokines IL-6 and IL-8, demonstrating significant anti-inflammatory properties. This compound is particularly relevant for research focused on acute lung injury and related inflammatory conditions. -
HSP90α Inhibitor
HSP90α-IN-1 is a selective inhibitor of HSP90α, with an IC50 value of 111 nM, demonstrating significant senolytic activity in diverse cellular senescence models. This compound is associated with the xanthinic family and plays a critical role in investigations aimed at addressing age-related inflammaging and associated diseases, including cancer. HSP90α-IN-1 is also being explored for its potential to promote healthy lifespan extension in various biological research contexts. -
PDE4 Inhibitor
Etazolate is a selective phosphodiesterase 4 (PDE4) inhibitor that exhibits anti-inflammatory properties by reducing interleukin-1 beta (IL-1β) levels. This compound demonstrates a dose-dependent effect on inflammation and edema, while also contributing to enhanced memory performance. Additionally, Etazolate's modulation of GABAA receptors suggests potential applications in research related to mood disorders, particularly in studying antidepressant-like effects. -
PKM2 Inhibitor
LIQ1 is a potent allosteric inhibitor of Pyruvate kinase M2 (PKM2), targeting Arg43 within the polyarginine pocket with an IC50 of 0.39 μM and a Kd of 4.5 μM. This flavonoid derivative effectively prevents the nuclear translocation of PKM2 and its interaction with HIF-1α, leading to the suppression of IL-1β transcription. LIQ1 is valuable for research involving endotoxemic conditions, particularly in studies of inflammation and metabolic regulation. -
PDE4 Inhibitor
PDE4-IN-8 is a potent inhibitor of phosphodiesterase 4 (PDE4), demonstrating an IC50 of 0.93 nM specifically for the PDE4B2 isoform. This compound exhibits selective inhibition, with minimal effects on cytokines such as IL-13 (IC50 = 4.04 nM), IL-4 (IC50 = 36.33 nM), and IFN-γ (IC50 = 2394 nM). PDE4-IN-8 is suitable for research applications focused on inflammation and other PDE4-related pathways in various biological contexts. -
PDE3A/PDE4B Inhibitor
PDE3/4-IN-4 is a potent and selective inhibitor of phosphodiesterase 3A (PDE3A) and phosphodiesterase 4B (PDE4B), exhibiting IC50 values of 10 nM and 9.4 nM, respectively. This compound modulates the cAMP/PKA/CREB signaling pathway, effectively inhibiting the pro-inflammatory cytokine IL-6 and reducing expression of inflammatory markers in liver tissue. PDE3/4-IN-4 demonstrates potential in mitigating liver fibrosis and limiting liver damage in models of cholestatic and sepsis-induced liver diseases. This reagent is suitable for research focused on liver injury and cholestatic liver disorders. -
Hsp90 Inhibitor
Pochonin D ((+)-Pochonin D) is a potent inhibitor of heat shock protein 90 (Hsp90) with demonstrated antiviral and anti-inflammatory activities. By targeting Hsp90, Pochonin D disrupts the proper folding, stabilization, and assembly of client proteins, including viral proteins, thereby impairing viral protein homeostasis and significantly reducing viral replication capacity. In addition, Pochonin D exhibits anti-inflammatory effects by attenuating inflammatory cell infiltration and suppressing the production of pro-inflammatory cytokines, such as TNF-α and IL-1β. These combined pharmacological properties highlight Pochonin D as a promising small-molecule tool for the study of human rhinovirus (HRV) infection and cancer-related pathways.
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PFKFB4 Inhibitor
5MPN is a selective inhibitor of 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase 4 (PFKFB4), exhibiting competitive inhibition at the fructose-6-phosphate binding site with a Ki of 8.6 μM. This compound does not affect PFK-1 or PFKFB3, allowing for targeted modulation of glucose metabolism in cancer cells. 5MPN has demonstrated the ability to suppress the proliferation of various human cancer cell lines, making it a valuable tool for research in cancer metabolism and therapeutic development. -
PTP1B Inhibitor
Caffeoyltryptophan is a competitive inhibitor of protein tyrosine phosphatase 1B (PTP1B), exhibiting an IC50 of 16.99 μM. Additionally, it demonstrates inhibitory effects on α-glucosidase, linoleic acid peroxidation, and hemolysis. This compound is primarily utilized in research related to type 2 diabetes, offering insights into metabolic regulation and potential therapeutic avenues. -
FXR Agonist
EDP-305 is a highly selective agonist of the farnesoid X receptor (FXR), exhibiting potent activity with EC50 values of 34 nM in chimeric FXR and 8 nM in full-length FXR. This compound demonstrates significant antifibrotic effects, making it a valuable tool for studying liver diseases. EDP-305 is relevant in research focused on primary biliary cholangitis (PBC) and non-alcoholic steatohepatitis (NASH). -
PFKFB3 Inhibitor
PFKFB3-IN-2 is a selective inhibitor of 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase 3 (PFKFB3). It demonstrates key biological activity by modulating glucose metabolism, making it relevant in cancer research and neurodegenerative disorders. This compound holds potential for applications in autoimmune diseases, inflammatory conditions, multiple sclerosis, metabolic disorders, and the study of angiogenesis. -
DPP-4 Inhibitor
Antidiabetic agent 2 is a potent DPP-4 inhibitor that effectively promotes glucose uptake. This compound also inhibits PTP-1B, α-amylase, and α-glucosidase, exhibiting IC50 values of 0.036, 0.042, 0.241, and 0.185 μM, respectively. By decreasing blood glucose levels, Antidiabetic agent 2 serves as a valuable tool for research focused on diabetes management and the modulation of glucose homeostasis. -
Ethyl Caffeoylquinate
Ethyl-3,5-di-O-caffeoylquinate is a derivative of ethyl caffeoylquinate, primarily targeting α-glucosidase and PTP1B enzymes. This compound demonstrates potential as an inhibitor of these critical enzymes, making it valuable for research in metabolic disorders and diabetes management. Isolated from the flower buds of Lonicera macranthoides, it also serves as an isomer of chlorogenic acid (ethyl dicaffeoylquinate), expanding its relevance in phytochemical studies and pharmacological applications. -
Phosphatase Inhibitor
Chrysophanol triglucoside is an anthraquinone with a specific inhibitory action on protein tyrosine phosphatase 1B (PTP1B) and α-glucosidase, demonstrating IC50 values of 80.17 µM and 197.06 µM, respectively. This compound is derived from Cassia obtusifolia and has potential applications in diabetes research, particularly in the study of glucose metabolism and insulin signaling pathways. -
Prenylated Flavonoid
Parvisoflavone B is a prenylated flavonoid that selectively inhibits protein tyrosine phosphatase 1B (PTP1B) with an IC50 of 42.6 μM and α-glucosidase with an IC50 of 12.19 μM. This compound is derived from the root bark of Erythrina mildbraedii and exhibits significant biological activity relevant to metabolic disorders. Parvisoflavone B is utilized in research exploring mechanisms related to type 2 diabetes and obesity, making it a valuable tool for studying these conditions. -
Carbonic Anhydrase/Alkaline Phosphatase Inhibitor
ALP/Carbonic Anhydrase-IN-1 is a dual inhibitor of carbonic anhydrase (CA) and alkaline phosphatase (ALP), selectively targeting key isoforms. It demonstrates IC50 values of 0.44 µM for CA-II, 1.61 µM for CA-IX, 0.51 µM for CA-XII, and 0.107 µM for ALP, indicating potent inhibitory activity. This compound is useful in exploring the roles of carbonic anhydrase and alkaline phosphatase in various biological processes and disease models. -
Bipyridine Herbicide
Morfamquat dichloride is a bipyridine herbicide that primarily targets the reticuloendothelial system. It induces significant lysosomal membrane damage and enzyme leakage, disrupting the function of the hepatocyte Golgi apparatus and associated glucose metabolic pathways. Research has shown that Morfamquat dichloride increases the activities of acid phosphatase and β-glucuronidase, resulting in toxic effects in mice; however, pre-administration of vitamin E has been observed to mitigate these toxic effects. This compound is relevant for studies investigating herbicide mechanisms and the associated biochemical responses in metabolic systems. -
PTP1B/hMAO-A Inhibitor
Cassiaside B2 is an inhibitor of protein tyrosine phosphatase 1B (PTP1B) and human monoamine oxidase A (hMAO-A). This compound exhibits significant antiallergic properties and functions as a 5-HT2C receptor agonist. It serves as a valuable tool for understanding the modulation of these targets in various biological pathways and contributes to research in neuropharmacology and allergy-related studies. -
PFKFB3 Inhibitor
(E/Z)-3PO is a selective inhibitor of PFKFB3, a key regulator of glycolysis. This compound effectively inhibits glycolysis, reduces the extracellular acidification rate, and suppresses angiogenesis by impairing endothelial cell migration and capillary tube formation. Research applications of (E/Z)-3PO include investigations into cancer, acute lung injury, pulmonary fibrosis, and atherosclerosis, making it a valuable tool for exploring therapeutic strategies in these diseases. -
Endogenous Metabolite
Glycodeoxycholic Acid is an endogenous metabolite that plays a significant role in hepatic physiology. It has been shown to induce hepatocyte necrosis and initiate autophagy, particularly in conditions such as obstructive cholestasis. This compound is essential for studying liver pathology and can be utilized in research focused on cholestatic liver diseases and cellular response mechanisms. -
Hsp110-STAT3 Interaction Inhibitor
Hsp110-STAT3 PPI-IN-1 is a potent inhibitor of the Hsp110-STAT3 protein-protein interaction. This compound exhibits antiproliferative activity against the HPAEC cell line, demonstrating an IC50 value of 22.67 μM. It serves as a valuable tool for investigating the role of Hsp110-STAT3 interactions in various biological processes and therapeutic applications. -
Drug Metabolite
OR-1855 is an active metabolite of Levosimendan that primarily targets myometrial contractility. It demonstrates anti-inflammatory properties by inhibiting IL-1β-induced reactive oxygen species (ROS) formation and NAD(P)H oxidase-dependent superoxide radical generation in human umbilical vein endothelial cells (HUVECs). Furthermore, OR-1855 suppresses IL-1β-induced phosphorylation of key signaling molecules, including p38 MAPK, ERK1/2, c-Jun, and JNK. This compound is valuable for research focused on inflammation and related biological processes. -
HMG-CoA Inhibitor
HMG499 is a potent and selective inhibitor of HMG-CoA reductase, exhibiting an IC50 of 0.41 μM. This compound effectively reduces serum cholesterol levels and mitigates the statin-induced accumulation of HMGCR, making it a valuable tool for research in lipid metabolism and atherosclerosis. HMG499 is relevant for studies investigating cholesterol regulation and cardiovascular disease pathways. -
Cathepsin Inhibitor
LV-320 is a potent uncompetitive inhibitor of cathepsin ATG4B, exhibiting an IC50 of 24.5 μM and a Kd of 16 μM. This compound effectively inhibits the enzymatic activity of ATG4B, thereby obstructing autophagic flux in cellular environments. Due to its stability and low toxicity, LV-320 is suitable for in vivo applications, making it a valuable tool for research on autophagy-related pathways. -
Nampt Inhibitor
GPP78 is a potent inhibitor of nicotinamide adenine dinucleotide (NAD) biosynthesis via the enzyme Nampt, demonstrating an IC50 of 3.0 nM. It exhibits cytotoxicity in the neuroblastoma SH-SY5Y cell line, with an IC50 of 3.8 nM, primarily by inducing autophagy. GPP78 serves as a valuable tool in cancer and inflammatory research, highlighting its potential therapeutic applications in oncology. -
RXR Agonist
Bexarotene-d4 is a deuterium-labeled analog of Bexarotene, functioning as a selective retinoid X receptor (RXR) agonist. This compound is primarily utilized in the treatment of cutaneous T-cell lymphoma, demonstrating significant biological activity in modulating RXR signaling pathways. Its isotopic labeling facilitates research applications in pharmacokinetics and metabolism studies of RXR-targeted therapies. -
HMG-CoA Reductase Inhibitor
Atorvastatin hemicalcium trihydrate is an orally active inhibitor of HMG-CoA reductase, primarily utilized in the management of dyslipidemia by effectively lowering blood lipid levels. Additionally, it demonstrates inhibitory effects on human smooth muscle cell proliferation and invasion, with IC50 values of 0.39 μM and 2.39 μM, respectively. This compound is valuable for research focused on atherosclerosis, cardiovascular diseases, and cell growth regulation. -
HSP90 Inhibitor
KW-2478 hydrochloride is a potent HSP90 inhibitor with an IC50 value of 3.8 nM. It exhibits significant anti-proliferative effects by inducing apoptosis in chronic myeloid leukemia (CML) and liver cancer cells. KW-2478 hydrochloride disrupts the BCR/ABL and MAPK signaling pathways, resulting in elevated levels of p27 and p21, along with reduced cyclin B1 expression. Additionally, it downregulates STAT3 expression, making it a valuable tool for cancer research, particularly in the contexts of CML and liver malignancies. -
PKM2 Inhibitor
Vitamin K5 is a specific inhibitor of pyruvate kinase M2 (PKM2), exhibiting IC50 values of 28, 191, and 120 μM against PKM2, PKM1, and PKL, respectively. It demonstrates notable biological activity by inducing apoptosis in colon 26 cells, making it relevant for cancer research. Furthermore, Vitamin K5 possesses antimicrobial properties and may be employed in studies related to infection. Its applications also extend to the preservation of pharmaceuticals, foods, and beverages. -
Nampt Inhibitor
Daporinad hydrochloride is a potent non-competitive inhibitor of nicotinamide phosphoribosyltransferase (Nampt), with a Ki of 0.3 nM. It induces cellular effects such as depletion of NAD+ and ATP levels, suppression of the mTORC1 and MAPK/ERK signaling pathways, and activation of TFEB, leading to enhanced autophagy. Additionally, Daporinad hydrochloride disrupts the endoplasmic reticulum calcium pool, impairing T cell activation through diminished mitogen-induced calcium signaling. This compound is valuable for research in myeloma, liver cancer, and immunosuppression, with effects including cell cycle arrest and apoptosis in various cancer cell lines. -
HSP90 Inhibitor
HSP90-IN-10 is a selective inhibitor of the heat shock protein 90 (HSP90) chaperone. It demonstrates significant antiproliferative activity against HCC1954 breast cancer cells, with an IC50 value of 6 µM, while sparing normal epithelial cells from growth inhibition. Additionally, HSP90-IN-10 promotes apoptosis, making it a valuable tool for research into cancer therapies targeting the HSP90 pathway. -
TrxR1 Inhibitor
LW-216 is a potent inhibitor of Thioredoxin Reductase 1 (TrxR1), known to induce apoptosis in cancer cells. This compound exhibits significant anti-tumor activity, making it a valuable tool for research in cancer biology and therapeutic development. Its mechanism of action and biological effects position LW-216 as an important reagent for studying redox regulation and cell death pathways in oncological contexts. -
NAMPT Inhibitor
Nampt-IN-8 is a selective inhibitor of Nicotinamide Adenine Dinucleotide Phosphate (NAMPT) with an IC50 value of 0.183 μM. This compound effectively induces apoptosis in cultured cells and enhances reactive oxygen species (ROS) production. It is a valuable tool for research on metabolic regulation and cellular stress responses, particularly in studies related to cancer and neurodegenerative diseases. -
PPARγ Agonist
GW7845 is a non-thiazolidinedione, tyrosine-derived agonist of PPARγ that exhibits oral bioactivity. It effectively inhibits voltage-dependent calcium channels (VDCC), relaxing pressurized arteries with an IC50 of 3 μM when using Ba2+ as the charge carrier. Additionally, GW7845 induces apoptosis in a manner that is dependent on mitochondria and the apoptosome, leading to rapid mitochondrial membrane depolarization and the release of cytochrome c in primary pro-B cells and BU-11 cells. This compound is useful for research into metabolic disorders and cardiovascular health. -
RXR Agonist
HX630 is a potent retinoic acid X receptor (RXR) agonist that effectively induces apoptosis and exhibits significant anti-tumor activity. It is particularly valuable in the study of Cushing's disease and related tumorigenic processes. Research applications include elucidating the mechanisms of RXR activation and its therapeutic potential in cancer treatments. -
Drug Metabolite
3-O-Methyltolcapone-d4 is a deuterium-labeled metabolite of Tolcapone, which serves as a selective and potent inhibitor of catechol-O-methyltransferase (COMT) with an IC50 of 773 nM. This compound is utilized in research focused on cancer and neurological disorders, including Parkinson's disease and neuroblastoma, due to its ability to inhibit α-synuclein and Aβ42 oligomerization, promote oxidative stress, and induce apoptosis in cancer cells. 3-O-Methyltolcapone-d4 provides a valuable tool for studying the metabolic pathways of Tolcapone and its therapeutic implications. -
Hsp90 Inhibitor
CPUY201112 is a potent inhibitor of heat shock protein 90 (Hsp90), exhibiting a Kd of 27 nM. This compound induces p53-mediated apoptosis in MCF-7 cells, leading to cell cycle arrest. CPUY201112 is a valuable tool for cancer research, particularly in studies focusing on apoptosis pathways and cell cycle regulation. -
PARP/NAMPT Inhibitor
PARP1/NAMPT-IN-2 is a potent dual inhibitor of PARP1 and NAMPT, exhibiting IC50 values of 0.8 nM and 18 nM, respectively. This compound effectively inhibits cell proliferation and migration, while inducing apoptosis in breast cancer cells. PARP1/NAMPT-IN-2 is particularly relevant for investigating therapeutic strategies in triple-negative breast cancer research.
