Metabolism

Items 2001-2050 of 5995

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  1. HSP90 Antagonist

    17-AEP-GA is a selective antagonist of HSP90, demonstrating potent inhibition of glioblastoma cell proliferation, survival, migration, and invasion. This compound is valuable for research applications focused on cancer biology, particularly in elucidating the role of HSP90 in oncogenic processes and therapeutic interventions in glioblastoma.
  2. HSP90 Inhibitor

    HSP90i is a potent inhibitor of the heat shock protein 90 (HSP90), a key molecular chaperone involved in the stabilization and folding of client proteins. This compound demonstrates significant biological activity relevant to cancer research and therapeutic applications, particularly in the development of targeted therapies. HSP90i can also serve as an important intermediate for synthesizing ligand-mediated targeted protein degradation agents, such as dPDL1-4, facilitating advancements in targeted drug delivery systems.
  3. HSP Inhibitor

    STA-2842 is a selective inhibitor of heat shock protein HSP90, demonstrating potential therapeutic effects in the context of autosomal dominant polycystic kidney disease (ADPKD). By modulating signaling pathways activated by mutations in PKD1 or PKD2 genes, STA-2842 effectively reduces renal cyst formation and inhibits kidney growth. In preclinical models, this compound has shown promise in slowing the progression of ADPKD, making it a valuable tool for understanding disease mechanisms and developing targeted interventions.
  4. HSP Inhibitor

    17-GMB-APA-GA is a potent inhibitor of Heat Shock Protein 90 (HSP90), known for its role in protein folding and cellular stress responses. This compound is particularly useful in research focused on latent Toxoplasma gondii infections. Its ability to disrupt HSP90 function presents valuable opportunities for studying therapeutic strategies targeting this essential chaperone in infectious disease contexts.
  5. Hsp90 Inhibitor

    HSP90-IN-14 is a potent inhibitor of heat shock protein 90 (Hsp90), exhibiting a dissociation constant (Kd) of 0.26 μM. This compound demonstrates significant antiviral activity against influenza viruses, showing EC50 values of 2.6 μM for A/H3N2, 3.9 μM for A/H1N1, and 17 μM for influenza B in MDCK cell assays. HSP90-IN-14 is a valuable tool for research into Hsp90's role in viral infections and therapeutic interventions.
  6. Hsp70 Inhibitor

    YM-1 tosylate is a stable analog of MKT-077 that functions as an orally active inhibitor of Hsp70. This compound has been shown to induce cell death in HeLa cells, while also up-regulating p53 and p21 protein levels. YM-1 tosylate is valuable for research applications focused on cancer biology and cellular stress responses.
  7. HSP90 Inhibitor

    DDO-6691 is a potent inhibitor of heat shock protein 90 (HSP90), targeting its role in protein folding and stabilization. This compound demonstrates significant antiproliferative activity against various tumor cell lines, particularly HCT-116 colon cancer cells, with an IC50 of 1.08 μM. DDO-6691 also effectively inhibits tumor growth in the HCT-116 xenograft mouse model, highlighting its potential for cancer research and therapeutic applications.
  8. Combined with Hsp90

    AMP-PCP is a potent ATP analogue that selectively binds to the N-terminal domain of Hsp90 with a Kd value of 3.8 μM. This binding promotes the formation of the active homodimeric structure of Hsp90, enhancing its chaperone activity. AMP-PCP is valuable in research applications focused on understanding the molecular mechanisms of Hsp90 modulation and its role in protein folding and stability in various cellular contexts.
  9. HSP Inhibitor

    Monorden diacetate is an effective Hsp90 inhibitor that demonstrates significant potential in the development of new fungicides. By targeting the heat shock protein 90 (HSP90), it disrupts the molecular chaperone activity essential for the stability and function of various client proteins. This compound is valuable for research applications focused on fungal biology and disease management.
  10. HSP Induction Inhibitor

    NSC-134754 is a dehydroemetine derivative that functions as a heat shock protein induction inhibitor. It specifically targets Hsp72 and Hsp27 at the post-transcriptional level, without affecting overall protein synthesis, HSF-1 transcriptional activity, or Hsp mRNA levels. Preclinical studies indicate that NSC-134754 exhibits minimal toxicity while enhancing the sensitivity of cancer cells to proteasome and Hsp90 inhibitors. This reagent is applicable in research involving multiple myeloma, prostate carcinoma, and colon carcinoma.
  11. HSP

    HSP90-IN-12 is a potent inhibitor of Heat Shock Protein 90 (HSP90), a chaperone protein essential for protein folding and stability. This compound exhibits significant anti-proliferative effects across various cancer cell lines, making it a valuable tool in cancer research. HSP90-IN-12 disrupts the regulation of HSP90-related proteins and effectively inhibits the HSP90-mediated refolding of luciferase in vitro, highlighting its potential for studying HSP90 dynamics and therapeutic applications in oncology.
  12. HSP90 Inhibitor

    MPC-0767 is a selective and potent inhibitor of heat shock protein 90 (HSP90). As an L-alanine ester proagent of MPC-3100, it exhibits enhanced chemical stability, making it suitable for in vivo applications. MPC-0767 is primarily utilized in research applications focused on cancer biology, as it disrupts the chaperone function of HSP90 and thereby influences the stability of various oncogenic client proteins.
  13. Hsp90-TPR2A Interaction Inhibitor

    Hsp90-IN-43 is a potent inhibitor of the Hsp90-TPR2A interaction, exhibiting an IC50 value of 360 nM and a Kd of 928 nM. This compound effectively inhibits the proliferation of BT474 breast cancer cells, making it a valuable tool for research in breast cancer biology. Its specific activity allows for deeper investigation into the role of Hsp90 in cancer progression and therapeutic response.
  14. Dye Tethered Hsp90 Inhibitor

    HS-131 is a dye-tethered inhibitor that targets heat shock protein 90 (Hsp90). This compound exhibits the ability to selectively bind to and inhibit Hsp90, facilitating the detection of oncogene-driven breast cancers across various molecular subtypes. HS-131 is a valuable research tool for studying the role of Hsp90 in cancer biology and for developing novel therapeutic strategies targeting breast cancer.
  15. Hsp90α/Hsp90β Inhibitor

    PU-11 is a selective inhibitor of Hsp90α and Hsp90β, targeting the ATP-binding pocket of these heat shock proteins. It exhibits IC50 values of 18.6 μM and 89.8 μM, along with Kd values of 2 μM for Hsp90α and 4.2 μM for Hsp90β, demonstrating a preference for Hsp90α due to the unique Ser52 residue. PU-11 is applicable in research related to neurodegenerative disorders, providing insights into the role of Hsp90 in cellular stress responses and protein homeostasis.
  16. HSP Inhibitor

    HSP90-IN-28 is a selective inhibitor of heat shock protein 90 (Hsp90), demonstrating an IC50 value of 0.46 μM for Hsp90α and approximately 48-fold selectivity over Hsp90β (IC50 = 22.28 μM). This compound is instrumental in research focused on cellular stress responses, cancer biology, and protein homeostasis. Its specificity makes HSP90-IN-28 an effective tool for studying the role of Hsp90 in various physiological and pathological processes.
  17. FKBP51-Hsp90 Inhibitor

    FKBP51-Hsp90-IN-2 is a selective inhibitor of the FKBP51-Hsp90 protein-protein interaction, demonstrating IC50 values of 0.4 µM for FKBP51 and 5 µM for FKBP52. This compound has been shown to enhance cellular energy metabolism and promote neurite growth. Its efficacy makes FKBP51-Hsp90-IN-2 a valuable tool in research focused on neurodegenerative diseases and cancer.
  18. MAO A/HSP90 Inhibitor

    MAO A/HSP90-IN-1 is a dual inhibitor targeting MAO A and HSP90, exhibiting IC50 values of 1.77 μM in glioblastoma GL26 cells and 0.019 μM for HSP90α. This compound effectively inhibits MAO A activity, disrupts HSP90 binding, and downregulates HER2 and phospho-Akt expression, leading to reduced growth of glioblastoma cells. Additionally, MAO A/HSP90-IN-1 decreases PD-L1 expression, which may hinder tumor immune escape and suppress T cell activation. This reagent serves as a valuable tool for research on brain tumor-related diseases.
  19. HSP90 Inhibitor

    HSP90-IN-29 is a selective inhibitor of heat shock protein 90 (HSP90), exhibiting a potent IC50 value of 30 nM. This benzoxazole derivative demonstrates significant antitumor activity, making it a valuable tool for cancer research. Its specific targeting of HSP90 allows for the exploration of its role in oncogenesis and the development of therapeutic strategies against malignancies.
  20. p38 Kinase/HSP Activator

    (±)-Iroxanadine serves as a p38 kinase and heat shock protein (HSP) activator, demonstrating vasculoprotective properties. This compound is pertinent for research into atherosclerosis and various vascular diseases, facilitating studies aimed at understanding the molecular mechanisms underlying these conditions. Its activation of key signaling pathways makes it a valuable tool for exploring therapeutic targets in cardiovascular research.
  21. Hsp90 Inhibitor

    HSP90-IN-35 is a selective Hsp90 inhibitor that exhibits potent antitumor activity, with an IC50 value for Her2 in the range of 0.05 to 0.5 μM. This compound is valuable for research applications focused on cancer biology and therapeutic development. Additionally, HSP90-IN-35 can be utilized in the synthesis of PROTACs, facilitating the exploration of targeted protein degradation strategies in cellular models.
  22. Hsp90 Inhibitor

    C086 is a potent inhibitor of Heat Shock Protein 90 (Hsp90), a crucial chaperone involved in protein folding and stability. This compound has been shown to inhibit cell cycle progression and induce apoptosis across various cell types. It also exhibits anti-metastatic properties, making it a valuable tool for research in cancer biology and therapeutic development targeting Hsp90.
  23. Hsp90 Activator

    Araloside C is an Hsp90 activator primarily derived from the natural saponin found in Aralia elata. This compound demonstrates significant anti-inflammatory properties and has shown protective effects against myocardial ischemia/reperfusion injury. Its ability to modulate Hsp90 activity makes it a valuable tool for research in cardiovascular protection and inflammation-related studies.
  24. HSP70 Inhibitor

    HSP70-IN-5 is a selective inhibitor of the heat shock protein 70 (HSP70). It demonstrates an IC₅₀ of 0.6 μM in HSP70/DnaJ-mediated luciferase reconstitution assays. This compound serves as a valuable biochemical probe for investigating the functional role of HSP70 and its co-chaperone DnaJ in diverse biological processes, including protein folding and stress response pathways.
  25. Aha1-Hsp90 Complex Inhibitor

    Hsp90-IN-34 is a potent inhibitor of the Aha1-Hsp90 chaperone complex, displaying a high affinity for Hsp90 and Aha1 with a dissociation constant (KDapp) of 23.5 µM. This compound interferes with the ATPase activity of Hsp90 by disrupting its interaction with Aha1, thereby influencing chaperone-mediated protein folding and stability. Hsp90-IN-34 is valuable for research into cancer biology and the modulation of protein homeostasis.
  26. HSP90 Inhibitor

    ML189 is a selective inhibitor of HSP90, a critical chaperone involved in protein folding and stability. By disrupting HSP90 activity, ML189 induces the degradation of client proteins, which can affect cellular proliferation and survival. This compound is primarily utilized in research related to infectious diseases, including candidiasis, and provides insights into the role of HSP90 in pathogen biology and therapeutic development.
  27. HSP90 Inhibitor

    ML229 is a high-affinity inhibitor of HSP90, a chaperone protein crucial for the stability and function of various client proteins. This compound demonstrates significant biological activity in modulating heat shock protein activity, making it a valuable tool for investigating the role of HSP90 in various cellular processes. ML229 has potential applications in the research of infectious diseases, including candidiasis, as it can interfere with the growth and survival of pathogenic organisms reliant on HSP90 for their virulence.
  28. HSP90 Inhibitor

    BIIB-028 is an orally active inhibitor of heat shock protein 90 (Hsp90), primarily targeting its ATP-binding site. By disrupting Hsp90 function, BIIB-028 promotes the degradation of client proteins essential for cancer cell survival and proliferation. This compound is valuable for research in cancer biology and therapeutic development aimed at targeting Hsp90.
  29. Hsp70 Inhibitor

    JG-48 is an inhibitor of the heat shock protein 70 (Hsp70), a molecular chaperone involved in protein folding and stabilization. This compound effectively reduces tau protein levels in various tauopathy models, making it a valuable tool for studying neurodegenerative diseases. Its specific targeting of Hsp70 provides insights into the role of protein aggregation in tau-related pathologies.
  30. NMT1/2 Inhibitor

    IMP-1088 is a highly potent dual inhibitor of human N-myristoyltransferases NMT1 and NMT2, exhibiting IC50 values of less than 1 nM for both isoforms and a Kd of under 210 pM for NMT1. This compound effectively inhibits rhinovirus replication by blocking the N-myristoylation of the virus-encoded protein VP0, thereby preventing the virus from completing its lifecycle. In addition, IMP-1088 offers protective effects to host cells by mitigating the cytotoxic consequences associated with viral infections, making it a valuable tool for research into antiviral therapies.
  31. Endogenous Metabolite

    Cysteinylglycine is an endogenous dipeptide resulting from the linkage of cysteine and glycine. It serves as a crucial metabolic intermediate, primarily produced by the degradation of glutathione. Cysteinylglycine functions in redox processes by reducing ferric iron to ferrous iron, generating reactive oxygen species (ROS), and inducing oxidative stress, which can lead to lipid peroxidation and DNA damage. Its potential as a biomarker makes it valuable for assessing ischemic heart disease, breast cancer, and other pathological conditions.
  32. NMT Inhibitor

    DDD85646 is a potent inhibitor of N-myristoyltransferase (NMT), specifically targeting the enzyme from Trypanosoma brucei with an IC50 of 2 nM and human NMT with an IC50 of 4 nM. This compound demonstrates significant potential for therapeutic applications in treating human African trypanosomiasis by disrupting lipid modifications essential for parasite survival. Its oral bioavailability further enhances its applicability in drug development for infectious diseases caused by trypanosomes.
  33. Lipoxygenase Inhibitor

    β-Boswellic acid, a potent inhibitor of 5-lipoxygenase (5-LO), is derived from the gum resin of Boswellia serrata. This compound exhibits significant anticancer, antioxidant, anti-inflammatory, and anti-arthritic properties. Its mechanism involves direct interaction with 5-LO or inhibition of its translocation, leading to reduced synthesis of DNA, RNA, and protein in human leukemia HL-60 cells, with IC50 values ranging from 0.6 to 7.1 μM. β-Boswellic acid holds potential for research into diabetes and inflammatory disorders, particularly those related to arthritis.
  34. CYP1A Inducer

    β-Apo-8'-carotenal is a potent inducer of CYP1A, acting through the aryl hydrocarbon receptor (AhR) pathway. This carotenoid has demonstrated the ability to induce DNA strand breaks and lipid peroxidation in cancer cells, making it a valuable tool for research into cancer biology and metabolic disorders. Its role as a provitamin A compound further emphasizes its potential applications in studies related to cellular metabolism and disease mechanisms.
  35. Ser/Thr Protease Inhibitor

    Antipain dihydrochloride is a potent Ser/Thr protease inhibitor derived from Actinomycetes. It is known to inhibit N-methyl-N'-nitro-N-nitrosoguanidine (MNNG)-induced transformation, leading to an increase in chromosomal aberrations. Additionally, Antipain dihydrochloride has been shown to restrict uterine DNA synthesis and functionality in murine models, making it a valuable tool for studying proteolytic processes and their implications in cellular biology and genetics.
  36. Herbicide

    Metazachlor is a chloroacetamide herbicide that targets the synthesis of very long chain fatty acids. By inhibiting this biosynthetic pathway, Metazachlor disrupts cell division and tissue differentiation during the germination and emergence of weed seeds. This mechanism effectively impedes the normal growth and development of various weed species, making it a valuable tool for agricultural research and weed management studies.
  37. Herbicide

    Napropamide is an amide herbicide primarily targeting DNA synthesis and cell division in various plant species. It is effective in controlling weeds in fruits, vegetables, tobacco, and ornamental plants. Napropamide demonstrates moderate to high field persistence, with a half-life ranging from 24 to 131 days, and is susceptible to photodegradation. This compound is valuable for agricultural research focused on weed management and herbicide efficacy.
  38. Endogenous Metabolite

    Guanine hydrochloride is a purine derivative that serves as a vital component of nucleic acids, including DNA and RNA. With its fused pyrimidine-imidazole ring system and conjugated double bonds, it plays important roles in cellular metabolism and genetic information transfer. This compound can potentially function as a significant nitrogen reservoir, making it valuable for various biochemical research applications, including studies of nucleic acid structure and metabolism.
  39. Endogenous Metabolite

    Cysteinylglycine TFA is a dipeptide formed by the linkage of cysteine and glycine, serving as an important endogenous metabolite. This compound plays a crucial role in the redox cycling of iron by reducing trivalent iron to divalent iron, leading to the generation of reactive oxygen species (ROS) and inducing oxidative stress, lipid peroxidation, and DNA damage. Cysteinylglycine TFA has potential applications as a biomarker for various conditions, including ischemic heart disease and breast cancer, making it valuable for research in metabolic and oxidative stress-related studies.
  40. Plant Growth Regulator/Herbicide

    Maleic hydrazide is a systemic plant growth regulator and herbicide that functions by inhibiting the synthesis of nucleic acids and proteins. This compound is utilized in agricultural research to regulate plant growth and development, making it valuable for studies exploring herbicide efficacy and crop management strategies. Its ability to affect plant physiology contributes to the understanding of plant response mechanisms to stress and growth regulation.
  41. AhR Antagonist

    3'-Methoxy-4'-nitroflavone is a specific antagonist of the aryl hydrocarbon receptor (AhR). This compound inhibits the metabolism of the endogenous ligand FICZ by blocking CYP1, thereby increasing FICZ accumulation. It effectively reverses the anti-apoptotic effects of TCDD and attenuates the activation of Akt and Erk1/2 kinases, as well as TGFα expression induced by TCDD. 3'-Methoxy-4'-nitroflavone is valuable for research into breast tumor promotion, rheumatoid arthritis, multiple sclerosis, and inflammatory bowel disease.
  42. PDE1C/PDE4B Inhibitor

    Sudachitin is a potent inhibitor of phosphodiesterase 1C (PDE1C) and phosphodiesterase 4B (PDE4B), exhibiting IC50 values of 5.0 μM and 15.0 μM, respectively. It enhances the expression of Sirt1 and PGC-1α in skeletal muscle, thereby influencing energy metabolism and promoting mitochondrial biogenesis. Sudachitin demonstrates beneficial effects on lipid metabolism, improves glucose tolerance and insulin sensitivity, and stimulates energy expenditure and fatty acid β-oxidation. Additionally, it activates the p38MAPK signaling pathway, influences apoptosis, and exhibits significant anti-inflammatory properties by reducing TNF-α, NO, and iNOS expression in macrophages. This compound is suitable for research in metabolic syndrome, type 2 diabetes, and psoriasis.
  43. 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.
  44. 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.
  45. 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.
  46. 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.
  47. 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.
  48. 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.
  49. 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.
  50. 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.

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