Thioureas
AdipoGen Desacetylcolchicine tartrate
Chemical. CAS 49720-72-1. Formula C20H23NO5 . C4H6O6. MW 357.4 . 150.1. Synthetic. Anticancer colchicine analog. Microtubule polymerization inhibitor. Prevents cell division.
AdipoGen Boc-AspOMe-FMK
Chemical. CAS 187389-53-3. Formula C11H18FNO5. MW 263.3. Synthetic. Cell permeable, irreversible, broad-spectrum caspase inhibitor. Inhibits non-caspase cysteine proteases, as well as cathepsins H and L. Can be used for in vitro and in vivo studies. Contains a methyl ester group, which facilitates uptake by cells and subsequently is removed by cytoplasmic esterases, leaving the functional inhibitor. Inhibits the pro-apoptotic effect of TNF-alpha IC50=39µM. Shown to reduce the activation of NF-kB, suppresses the phosphorylation of IkBalpha and inhibits TNF-induced expression of ICAM-1 and VCAM-1. Blocks hepatocyte apoptosis in vivo. Neuroprotective.
AdipoGen 4-Hydroxytamoxifen
Chemical. CAS 68392-35-8. Formula C26H29NO2. MW 387.51. 4-Hydroxytamoxifen is an active metabolite of the chemotherapeutic drug tamoxifen, a selective estrogen receptor modulator SERM that acts as an agonist or antagonist in various tissues. 4-Hydroxytamoxifen acts as a tissue-selective agonist-antagonist of the estrogen receptors ERalpha and ERbeta. 4-Hydroxytamoxifen is an isoform-specific inhibitor of orphan estrogen-receptor-related ERR nuclear receptors beta and gamma. 4-Hydroxytamoxifen exhibits anticancer chemotherapeutic activity, inducing autophagy and vacuole formation as well as KRAS degradation in various cancer cell lines. In cardiac myocytes, 4-hydroxytamoxifen decreases Ca2 amplitude, slowing relaxation and decreasing contractility. 4-Hydroxytamoxifen has also shown to be a potent inhibitor of the mitochondrial permeability transition MPT.
Biomatik Corporation Pepstatin A. Grade High Purity. Storage 4C. CAS 8913806
Pepstatin A. Grade High Purity. Storage 4C. CAS 8913806
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 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 Vandetanib
Chemical. CAS 443913-73-3. Formula C22H24BrFN4O2. MW 475.4. Vandetanib is an orally available, ATP mimetic small molecule tyrosine kinases inhibitor that targets vascular endothelial growth factor receptor-2 VEGFR-2, VEGFR-3 and epidermal growth factor receptor EGFR, REarranged during Transfection RET and slightly VEGFR-1. Inhibition of these tyrosine kinases blocks multiple intracellular signaling pathways involved in tumor growth, proliferation, progression and angiogenesis. It inhibits RET, VEGFR2, VEGFR3, VEGFR1, EGFR, PDGFRbeta, Tie-2, and FGFR1 in cell-free assays IC50s = 34, 40, 110, 1,600, 500, 1,100, 2,500, and 3,600 nM, respectively. It also binds to 142 additional kinases in a panel of 442 kinases Kds = 4.6-7,900 nM. Vandetanib 1 and 2.5 µM induces apoptosis, autophagy, ROS and cell cycle arrest at the G0/G1 phase and has anti-proliferative properties in several cancer cell lines and in in vivo cancer models.
eMolecules 28456-54-4 | 5,6-Dimethyl-2-thiouracil | MFCD00278872 | 25g
Ambeed | 9-Propyl-9H-purin-6-amine | 250mg | 592283558 | A121142 | 707-98-2 | MFCD18801082 | 177.211 | C8H11N5
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eMolecules 62-56-6 | Thiourea ACS Reagent Grade | Oakwood Chemicals | MFCD00008067 | 76.120 | CH4N2S | 99.000 | NC(N)=S | 100g | 486563126
Thiourea ACS Reagent Grade | Oakwood Chemicals | 62-56-6 | MFCD00008067 | 76.120 | CH4N2S | 99.000 | NC(N)=S | 100g | 486563126
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.
eMolecules 105-55-5 | 1,3-Diethyl-2-thiourea | Oakwood Chemicals | MFCD00004925 | 132.230 | C5H12N2S | 0.000 | CCNC(=S)NCC | 25g | 480149343
1,3-Diethyl-2-thiourea | Oakwood Chemicals | 105-55-5 | MFCD00004925 | 132.230 | C5H12N2S | 0.000 | CCNC(=S)NCC | 25g | 480149343
eMolecules 62-56-6 | Thiourea | Chem-Impex | MFCD00008067 | 76.120 | CH4N2S | 99.000 | NC(N)=S | 100kg | 112439619
Thiourea | Chem-Impex | 62-56-6 | MFCD00008067 | 76.120 | CH4N2S | 99.000 | NC(N)=S | 100kg | 112439619
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.