Thioureas
AdipoGen PTACH
Chemical. CAS 848354-66-5. Formula C20H26N2O2S2. MW 390.56. Synthetic. Non-hydroxamate HDAC inhibitor HDACi IC50 32, 48 and 41nM for HDAC4, HDAC1 and HDAC6, respectively. Cell-permeable prodrug that is intracellularly converted to a potent HDAC inhibitor. Predicted to exhibit a similar HDAC binding mode as that of SAHA, interacting with the active-site zinc targeting group. Shown to exhibit comparable antiproliferative and apoptotic activity as SAHA against various cancer cell lines. Inhibits growth of various cancer cells in vitro EC50 = 1.1 - 9.1mM. Also reactivates latent HIV-1 gene expression.
AdipoGen Aluminon
Chemical. CAS 569-58-4. Formula C22H14O9 . 3NH3. MW 422.3 . 51.1. Synthetic. Aluminon, the triammonium salt of aurintricarboxylic acid, is a dye commonly used to detect the presence of the aluminium ion in an aqueous solution. In addition to its use in qualitative inorganic analysis, aluminon has applications in pigment production. It forms brilliantly colored lake pigments with aluminum, chromium, iron and beryllium. Spectral data AL-Complex Absorbance at ~525nm. Aurintricarboxylic acid readily polymerizes in aqueous solution, forming a stable free radical that inhibits protein-nucleic acid interactions. It is a potent inhibitor of RNA-directed DNA polymerase and topoisomerase II. Angiogenesis inhibitor. It stimulates tyrosine phosphorylation processes including the Jak2/STAT5 pathway in NB2 lymphoma cells, ErbB4 in neuroblastoma cells, and MAP kinases, Shc proteins, phosphatidylinositide 3-kinase and phospholipase C in PC12 cells.
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 4-Methylumbelliferone
Chemical. CAS 90-33-5. Formula C10H8O3. MW 176.17. 4-Methylumbelliferone 4-MU is a selective inhibitor of hyaluronan HA by depletion of UDP-glucuronic acid, the common substrate for HA synthesis and downregulation of hyaluronan synthase 2 and 3, MMP2 and MMP9. Since hyaluronan HA is a major component of the extracellular matrix that is synthesized in excess in cancer tissues, 4-MU has been shown to have anti-cancer activity and is involved in angiogenesis, invasion and metastasis of cancer. Fluorescent pH indicator, that is highly fluorescent in alkaline solution. Exhibits a blue fluorescence at pH7. The fluorescence intensity is pH dependent and increases to a maximum at pH10 plateau above pH10. The fluorescence at pH10.3 is approximately 100 times as intense as at pH7. Spectral data lambdaex=360nm lambdaem=448nm pH > 9.
AdipoGen 6-Dimethylaminopurine
Chemical. CAS 938-55-6. Formula C7H9N5. MW 163.18. Synthetic. A puromycin analog that acts as a protein kinase inhibitor. Selectively induces premature mitosis in mammalian cells. Inhibits TNF-alpha upregulation of ICAM-1, lipolysis, and the activation of JNK/SAPK. Inhibits p34cdc2/cyclin B IC50 = 300 µM. Induces apoptosis in S-phase-arrested HeLa cells ~5 mM.
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 4-Methylumbelliferone
Chemical. CAS 90-33-5. Formula C10H8O3. MW 176.17. 4-Methylumbelliferone 4-MU is a selective inhibitor of hyaluronan HA by depletion of UDP-glucuronic acid, the common substrate for HA synthesis and downregulation of hyaluronan synthase 2 and 3, MMP2 and MMP9. Since hyaluronan HA is a major component of the extracellular matrix that is synthesized in excess in cancer tissues, 4-MU has been shown to have anti-cancer activity and is involved in angiogenesis, invasion and metastasis of cancer. Fluorescent pH indicator, that is highly fluorescent in alkaline solution. Exhibits a blue fluorescence at pH7. The fluorescence intensity is pH dependent and increases to a maximum at pH10 plateau above pH10. The fluorescence at pH10.3 is approximately 100 times as intense as at pH7. Spectral data lambdaex=360nm lambdaem=448nm pH > 9.
AdipoGen CTPB
Chemical. CAS 586976-24-1. Formula C31H43ClF3NO2. MW 554.1. Potent activator of p300 HAT histone acetyltransferase activity, which has an important role in regulation of gene expression. Does not show PCAF p300/CBP-associated factor HAT activities. Membrane-impermeable that requires a carrier to pass the membrane barrier of cells.
AdipoGen YC-1
Chemical. CAS 170632-47-0. Formula C19H16N2O2. MW 304.4. Nitric oxide NO independent, superoxide-sensitive soluble guanylyl cyclase sGC activator. Induces concentration-dependent increase in cGMP levels. Inhibits platelet adhesion to collagen. Thombosis inhibitor. Non-specific phosphodiesterase inhibitor. Na channel blocker. Anticancer compound. HIF-alpha inhibitor. Blocks angiogenesis. Tumor growth inhibitor. Apoptosis inducer. NK cell differentiation enhancer. TRAIL sensitizer.
AdipoGen PJ-34
Chemical. CAS 344458-15-7. Formula C17H17N3O2 . HCl. MW 295.2 . 36.5. Potent, water soluble polyADP-ribose polymerase PARP inhibitor. Inhibits peroxynitrite-induced cell necrosis. Shows significant, dose-dependent anti-inflammatory effects in a variety of local inflammation models. Provides cardioprotection by decreasing myocardial infarct size. Shows protective effects in models of stroke. Suppresses cell growth in liver cancer cells.
AdipoGen Alsterpaullone
Chemical. CAS 237430-03-4. Formula C16H11N3O3. MW 293.3. Potent CDK1/cyclin B IC50 = 35 nM inhibitor. Anti-tumor compound Potent inhibitor of CDK2/cyclin A, CDK2/cyclin E IC50 = 200 nM, CDK5/p25 IC50 = 40 nM, CDK5/p35 IC50 = 40 nM. GSK-3beta glycogen synthase kinase-3beta inhibitor. Apoptosis inhibitor. Apoptosis inducer. Angiogenesis inhibitor.
AdipoGen Z-Leu-Leu-Leu-BOH2 MG-262
Chemical. CAS 179324-22-2. Formula C25H42BN3O6. MW 491.4. Highly potent and selective cell permeable inhibitor of the proteasome. Inhibits the chymotrypsin-like and caspase-like peptidase activity of the proteasome. Calpain and cathepsin inhibitor. Autophagy activator. Similar structure as MG-132 AG-CP3-0011 but much higher potency.
AdipoGen Z-Leu-Arg-Gly-Gly-AMC
Chemical. CAS 167698-68-2 free base. Formula C34H44N8O8 . C2HF3O2. MW 692.8 . 114.0. Fluorogenic tetrapeptide substrate for ubiquitin C-terminal hydrolases UCHs, e.g. UCHL3 and isopeptidase T. LRGG is the preferred substrate sequence of the human deSUMOylating enzymes SENP6 and SENP7. Excitation 380nm. Emission 460nm.
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.