Thioureas
AdipoGen Caroverin
Chemical. CAS 23465-76-1. Formula C22H27N3O2. MW 365.47. Synthetic. Quinoxaline compound, originally developed as a spasmolytic drug. Acts as an N-type calcium channel blocker, competitive AMPA receptor antagonist, and non-competitive NMDA receptor antagonist. Antioxidant agent through partial prevention of the formation and the highly active scavenging of hydroxyl radicals. Used to treat inner ear diseases such as tinnitus. Shown to inhibit tumor-promoting factors and potentially useful as a chemotherapeutic agent.
AdipoGen Caroverin
Chemical. CAS 23465-76-1. Formula C22H27N3O2. MW 365.47. Synthetic. Quinoxaline compound, originally developed as a spasmolytic drug. Acts as an N-type calcium channel blocker, competitive AMPA receptor antagonist, and non-competitive NMDA receptor antagonist. Antioxidant agent through partial prevention of the formation and the highly active scavenging of hydroxyl radicals. Used to treat inner ear diseases such as tinnitus. Shown to inhibit tumor-promoting factors and potentially useful as a chemotherapeutic agent.
AdipoGen Efavirenz
Chemical. CAS 154598-52-4. Formula C14H9ClF3NO2. MW 315.7. Efavirenz is a non-nucleoside reverse transcriptase inhibitor NNRTI that exhibits antiviral and anticancer activities. Efavirenz binds to wild-type and mutant HIV-1 RTs Ki= 2.93nM and 3.85-56.5nM, respectively. It inhibits wild-type and mutant HIV-1 viral replication in MT-4 human T lymphoid cells IC95s = 1.5-1,500 nM. Efavirenz also prevents RNA plus-strand initiation with an IC50 value of 17nM. Efavirenz is an anti-HIV drug, commonly used in combination therapy for AIDS treatment. It is part of highly active antiretroviral therapy HAART for the treatment of a human immunodeficiency virus HIV type 1. In various cancer cell lines, Efavirenz inhibits cellular proliferation and increases activation of p53. CARD8 inflammasome senses HIV-1 protease activity. In HIV1-infected cells, CARD8 cannot detect the virus because the viral protease remains inactive as a subunit of unprocessed Gag-Pol polyprotein.
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 Efavirenz
Chemical. CAS 154598-52-4. Formula C14H9ClF3NO2. MW 315.7. Efavirenz is a non-nucleoside reverse transcriptase inhibitor NNRTI that exhibits antiviral and anticancer activities. Efavirenz binds to wild-type and mutant HIV-1 RTs Ki= 2.93nM and 3.85-56.5nM, respectively. It inhibits wild-type and mutant HIV-1 viral replication in MT-4 human T lymphoid cells IC95s = 1.5-1,500 nM. Efavirenz also prevents RNA plus-strand initiation with an IC50 value of 17nM. Efavirenz is an anti-HIV drug, commonly used in combination therapy for AIDS treatment. It is part of highly active antiretroviral therapy HAART for the treatment of a human immunodeficiency virus HIV type 1. In various cancer cell lines, Efavirenz inhibits cellular proliferation and increases activation of p53. CARD8 inflammasome senses HIV-1 protease activity. In HIV1-infected cells, CARD8 cannot detect the virus because the viral protease remains inactive as a subunit of unprocessed Gag-Pol polyprotein.
AdipoGen MnTBAP chloride
Chemical. CAS 55266-18-7. Formula C48H28MnN4O8Cl. MW 879.2. Cell permeable superoxide dismutase SOD mimetic. Potent inhibitor of peroxynitrite-induced oxidative reactions peroxynitrite scavenger, but not a scavenger of nitric oxide NO. Neuronal apoptosis inhibitor. Protects T cells from superoxide generation, caspase-dependent DNA loss and cell death. Lipopolysaccharide-induced TNF-alpha production inhibitor, by prevention of intracellular ROS generation and subsequent inactivation of p38 MAPK and SAPK/JNK. .
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-Val-Leu-Arg-AMC
Chemical. Formula C35H47N7O7 . C2HF3O2. MW 677.8 . 114.0. Proteasome subunit alpha type-1 Macropain substrate used for assaying the trypsin-like activity of the 20S proteasome. Cysteine proteinase falcipain-2 and falcipain-3 malarial hemoglobinases substrate. Cathepsin S substrate. Hydrolysis of this fluorogenic peptide substrate is monitored by observing fluorescence at an Excitation of 345nm and Emission at 445nm.
AdipoGen PP2
Chemical. CAS 172889-27-9. Formula C15H16ClN5. MW 301.8. Highly potent and selective Scr family tyrosine kinase inhibitor. Reduces cancer metastasis. Apoptotic. Antitumor compound. RIP2 inhbitor. Blocks TGF-beta-mediated cellular responses. Autophagy modulator.
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 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 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 Boc-Leu-Arg-Arg-AMC
Chemical. CAS 109358-46-5 free base. Formula C33H52N10O7 . C2H4O2. MW 700.8 . 60.1. Fluorogenic tri-peptide substrate for measuring the trypsin-like peptidase activity of the 20S proteasome. Substrate for the Kex2 endopeptidase from S. Cervisiae, which has substrate specificity toward the C-terminal side of LR, PR and RR sequences. Can be cleaved by Kallikrein 5 with a P1 site preference for basic residues R and K. Excitation 380nm. Emission 460nm. This substrate is useful for inhibitor screening and kinetic analysis.
AdipoGen Raptinal
Chemical. CAS 1176-09-6. Formula C28H18O2. MW 386.4. Rapid apoptosis inducer that initiates intrinsic pathway caspase-dependent apoptosis within minutes in multiple cell lines and in vivo systems. Exerts anticancer activity in vivo, likely through the induction of apoptosis. Induces cell death against various cancer and non-cancerous cell lines with 24 hour IC50 values between 0.7-3.4µM indicating activity across a wide range of cell lines. Activates the intrinsic pathway and requires functional mitochondria for apoptosis induction. Treated cells did not undergo mitochondrial-permeability-transition-pore MPTP formation, suggesting a mitochondrial outer membrane permeabilization MOMP model of cytochrome c release.
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.