ONC212 is an agonist of the orphan G protein-coupled receptor GPR132 (EC50 = ~400 nM in a PathHunter® β-arrestin assay).{52749} It inhibits cell growth in a panel of 62 human leukemia cell lines, including acute myeloid leukemia (AML), acute lymphoblastic leukemia (ALL), chronic myelogenous leukemia (CML), and hairy cell leukemias, with GI50 values ranging from less than 78 to 456 nM. ONC212 also reduces cell growth in a panel of 58 lymphoma cell lines (GI50s = In vivo, ONC212 (50 mg/kg) reduces tumor volume in HT-29 and HCT116 mouse xenograft models.{52750}
Available on backorder
A GPR132 agonist (EC50 = ~400 nM in a PathHunter® β-arrestin assay); inhibits cell growth in a panel of 62 human leukemia cell lines (GI50s = 50s = <78-261 nM); reduces tumor volume in HT-29 and HCT116 mouse xenograft models at 50 mg/kg
Formal name: 2,4,6,7,8,9-hexahydro-7-(phenylmethyl)-4-[[4-(trifluoromethyl)phenyl]methyl]-imidazo[1,2-a]pyrido[3,4-e]pyrimidin-5(1H)-one
Synonyms:
Molecular weight: 440.5
CAS: 1807861-48-8
Purity: ≥98%
Formulation: A crystalline solid
1,2-Dipalmitoyl-sn-glycero-3-PC (DPPC) is a zwitterionic glycerophospholipid commonly used in the formation of lipid monolayers, bilayers, and liposomes for use in a variety of applications.{14480,24261,14478,14479} It has been used in the formation of proteoliposomes for implantation of γ-glutamyl transpeptidase into human erythrocyte membranes.{14478} Incorporation of glycosphingolipid antigens into DPPC-containing liposomes increases the immunogenicity of the antigens in mice.{14479}
Available on backorder
The nuclear factor-κB (NF-κB) regulates the expression of numerous genes involved in immunity and inflammation, cellular stress responses, growth, and apoptosis. Resveratrol, a polyphenolic trans-stilbene, is a known inhibitor of the activation of NF-κB and exhibits activity against a wide variety of cancer cells. CAY10512 is a substituted trans-stilbene analog of resveratrol that is 100-fold more potent as measured by antioxidant activity. The IC50 value for inhibition of TNFα-induced activation of NF-κB by CAY10512 is 0.15 µM compared to 20 µM by resveratrol.{14545}
Available on backorder
The tetracycline repressor (TetR) is a transcriptional regulator which normally binds tightly to its palindromic tetO operator DNA, blocking gene expression.{17508} Tet causes the repressor to dissociate from the DNA, allowing transcription to occur. A novel reverse TetR (revTetR) requires tetracycline as a co-repressor to bind tetO and block transcription.{17509,17510} Anhydrotetracycline (hydrochloride) is a powerful effector in both the tetracycline repressor (TetR) and reverse TetR (revTetR) systems, binding the Tet repressor 35-fold more strongly than Tet.{17508,17511} Moreover, anhydrotetracycline poorly binds the 30S ribosomal subunit, compared to Tet,{17512} so it does not act as a general inhibitor of translation and is a poor antibiotic. Perhaps related to this, the concentration of anhydrotetracycline that inhibits eukaryotic cell growth is more than a 1,000-fold above the dose that alters transcription through TetR.{17508}
Available on backorder
The PtdIn phosphates play an important role in the generation and transduction of intracellular signals.{8344,4096,14518} PtdIns-(3,4,5)-P3-biotin is an affinity probe which allows the PIP3 to be detected through an interaction with the biotin ligand. This design allows PtdIns-(3,4,5)-P3-biotin to serve as a general probe for any protein with a high affinity binding interaction with inositol-(3,4,5)-triphosphate phospholipids, such as phosphatidylinositol 3-kinase, PTEN, or PH-domain-containing proteins.
Available on backorder