Thioureas
AdipoGen Thapsigargin
Chemical. CAS 67526-95-8. Formula C34H50O12. Molecular Weight 650.75. Thapsigargin is a non-competitive, cell permeable inhibitor of calcium transport by SERCAs IC50 values are cell type-dependent and range from ~2-80 nM. Inhibition of SERCAs leads to an increase in intracellular calcium, which has been linked to cell activation, release of histamine from mast cells, and increased proliferation of certain types of cancer cells. Thapsigargin shows anti-inflammatory and anti-cancer effects.
AdipoGen Josamycin
Chemical. CAS 16846-24-5. Formula C42H69NO15. MW 827.99. Synthetic. A member of the leucomycin family of macrolide antibiotics produced by Streptomyces kitasatoensis. May overcome anticancer drug resistance by inhibiting the binding of vinblastine or cyclosporin A to P-glycoprotein Pgp. An antimicrobial against a wide variety of pathogens.
AdipoGen Budesonide
Chemical. CAS 51333-22-3. Formula C25H34O6. MW 430.5. Budesonide is a glucocorticoid and an agonist of glucocorticoid receptors EC50=45.7pM in a transactivation assay, selective for glucocorticoid over mineralocorticoid receptors. Budesonide is a synthetic anti-inflammatory agent that displays chemopreventive activity. It is used as an anti-inflammatory agent in the treatment of asthma, rhinitis and inflammatory bowel disease and is evaluated in prevention of lung cancer. It prevents formation of lung adenomas and adenocarcinomas in mice following inhalation or oral administration. It also reverses DNA hypomethylation and modulates expression of cancer related genes. Due to its potent activity, as an inhaled glucocorticoid, in reducing airway inflammation, Budesonide has potential as treatment for early COVID-19 infection.
AdipoGen KBU2046
Chemical. CAS 1143863-69-7. Formula C15H11FO2. MW 242.2. Highly selective metastasis inhibitor in vitro. Binds to and stabilizes Cdc37-HSP90beta heterocomplexes, consequently blocking its function and inhibiting cancer cell motility. Does not bind to Cdc37 or HSP90beta alone. Inhibits cancer metastasis in vivo in murine models of human prostate and breast cancer. Shown to exhibit a complete lack of cellular cytotoxicity and systemic toxicity.
AdipoGen RO-3306
Chemical. CAS 872573-93-8. Formula C18H13N3OS2. MW 351.5. Selective CDK 1 inhibitor Cdk1/B1 and Cdk1/A. Potential anti-cancer compound. Cell cycle arrest inducer at G1, S and G2/M . Apoptosis inducer in embryonic stem cells. Actively enhances downstream p53 signaling to promote apoptosis in AML cell lines. Suppresses phosphorylation of p53 at Ser315 and procaspase-8 at Ser387. Enhances Fas-mediated activation and processing of procaspase-8 in mitotic cells towards.
AdipoGen Ac-Arg-Leu-Arg-AMC
Chemical. CAS 929903-87-7 free base. Formula C30H46N10O6 . C2HF3O2. MW 642.8 . 114.0. Fluorogenic tri-peptide substrate for measuring the trypsin-like peptidase activity of the 20S proteasome. It is cleaved exclusively at the amide R-AMC bond to release fluorescent product. Shows low Km and high specific activity. Excitation 380nm. Emission 460nm. This substrate is useful for inhibitor screening and kinetic analysis.
AdipoGen Ixazomib MLN2238
Chemical. CAS 1072833-77-2. Formula C14H19BCl2N2O4. MW 361. Synthetic. Potent selective and reversible proteasome inhibitor all proteolytic subunits. Targets the chymotrypsin-like beta5 subunit of the constitutive 20S proteasome IC50=3.4nM. Cross-reacts and inhibits the trypsin-like beta2 subunit IC50=3.5µM and the caspase-like/peptidyl-glutamyl peptide-hydrolyzing PGPH beta1 subunit IC50=0.03µM. Anticancer compound effective in cell-based assays, in xenografts and against multiple myeloma in vivo. In vitro, induces cell cycle arrest and apoptosis in human cancer cell lines including multiple myeloma. Biologically active form of the prodrug MLN9708 AG-CR1-3671. Exhibits improved pharmacodynamics and antitumor activity compared to bortezomib in various B-cell lymphoma models, due to a greater tumor to blood ratio of proteasome inhibition that ultimately translates into improved tumor pharmacodynamic response and antitumor activity in several tumor xenograft models.
AdipoGen Budesonide
Chemical. CAS 51333-22-3. Formula C25H34O6. MW 430.5. Budesonide is a glucocorticoid and an agonist of glucocorticoid receptors EC50=45.7pM in a transactivation assay, selective for glucocorticoid over mineralocorticoid receptors. Budesonide is a synthetic anti-inflammatory agent that displays chemopreventive activity. It is used as an anti-inflammatory agent in the treatment of asthma, rhinitis and inflammatory bowel disease and is evaluated in prevention of lung cancer. It prevents formation of lung adenomas and adenocarcinomas in mice following inhalation or oral administration. It also reverses DNA hypomethylation and modulates expression of cancer related genes. Due to its potent activity, as an inhaled glucocorticoid, in reducing airway inflammation, Budesonide has potential as treatment for early COVID-19 infection.
AdipoGen KBU2046
Chemical. CAS 1143863-69-7. Formula C15H11FO2. MW 242.2. Highly selective metastasis inhibitor in vitro. Binds to and stabilizes Cdc37-HSP90beta heterocomplexes, consequently blocking its function and inhibiting cancer cell motility. Does not bind to Cdc37 or HSP90beta alone. Inhibits cancer metastasis in vivo in murine models of human prostate and breast cancer. Shown to exhibit a complete lack of cellular cytotoxicity and systemic toxicity.
AdipoGen TPEN
Chemical. CAS 16858-02-9. Formula C26H28N6. MW 424.5. TPEN is a cell permeable metal ion chelator. TPEN is a chelator that has a high affinity for zinc Zn2, next to other transition metals Zn2 >Fe2 >Mn2 and is used in zinc treatment studies to limit intra- and extracellular concentrations of the mineral. TPEN has lower affinity for Ca2 and Mg2 and can also form complexes with other soft metal ions such as Cd2. In addition to a heavy metal chelator, TPEN is also known to be an apoptosis inducer. Depletion of zinc by TPEN induces apoptosis in several cell lines. TPEN shows anticancer activity through induction of caspase-dependent apoptosis, via reactive oxygen species ROS signaling mechanism and inhibiting cell autophagy. TPEN also inhibits RNA binding protein Lin28 and has been shown to be useful in extracting Abeta depostis from Alzheimers disease brain tissue.
AdipoGen TPEN
Chemical. CAS 16858-02-9. Formula C26H28N6. MW 424.5. TPEN is a cell permeable metal ion chelator. TPEN is a chelator that has a high affinity for zinc Zn2, next to other transition metals Zn2 >Fe2 >Mn2 and is used in zinc treatment studies to limit intra- and extracellular concentrations of the mineral. TPEN has lower affinity for Ca2 and Mg2 and can also form complexes with other soft metal ions such as Cd2. In addition to a heavy metal chelator, TPEN is also known to be an apoptosis inducer. Depletion of zinc by TPEN induces apoptosis in several cell lines. TPEN shows anticancer activity through induction of caspase-dependent apoptosis, via reactive oxygen species ROS signaling mechanism and inhibiting cell autophagy. TPEN also inhibits RNA binding protein Lin28 and has been shown to be useful in extracting Abeta depostis from Alzheimers disease brain tissue.
AdipoGen Salidroside
Chemical. CAS 10338-51-9. Formula C14H20O7. MW 300.3. Synthetic. Glycoside isolated from plants, most commonly from members of the genus Rhodiola, with many biological activities. Shown to have neuroprotective, antioxidant, antiviral, antidepressant, cardioprotective, anti-inflammatory and anticancer activity. Ameliorates insulin resistance.
AdipoGen Salidroside
Chemical. CAS 10338-51-9. Formula C14H20O7. MW 300.3. Synthetic. Glycoside isolated from plants, most commonly from members of the genus Rhodiola, with many biological activities. Shown to have neuroprotective, antioxidant, antiviral, antidepressant, cardioprotective, anti-inflammatory and anticancer activity. Ameliorates insulin resistance.
AdipoGen 1-Methyltryptamine
Chemical. CAS 7518-21-0. Formula C11H14N2. MW 174.24. Synthetic. Deacetylase inhibitor.
AdipoGen C646
Chemical. CAS 328968-36-1. Formula C24H19N3O6. MW 445.4. Reversible cell permeable p300/CBP histone acetyltransferase HAT inhibitor. Specific inhibition to p300 86% compared to N-acetyltransferase, PCAF, GCN5, Rtt109, Sas or MOZ histone acetyltransferases <10%. Cell growth inhibitor in melanoma and non-small-cell-lung NSCL human cancer cell lines.