The constitutive androstane receptor (CAR) is a nuclear receptor that functions as a sensor of toxic compounds and enhances their elimination.{27663} CITCO is an agonist of human CAR (EC50 = 49 nM).{28128} It induces nuclear translocation of human CAR in hepatocytes, followed by increased expression of CAR-regulated genes, including several cytochrome P450 isoforms.{28128} CITCO less potently activates human pregnane X receptor (EC50 = 3 µM) and has no detectable activity on other nuclear receptors at 10 µM.{28128} It is selective for human CAR, whereas TCPOBOP (Item No. 14140) is selective for mouse CAR.{27663} CITCO does activate alternative splice variants of human CAR that are also found in liver cells.{28132} It is commonly used to study the action of human CAR in hepatocytes.{28130,28131}
An agonist of human CAR (EC50 = 49 nM); induces nuclear translocation of human CAR in hepatocytes, followed by increased expression of CAR-regulated genes
Formal name: O-[(3,4-dichlorophenyl)methyl]oxime 6-(4-chlorophenyl)-imidazo[2,1-b]thiazole-5-carboxaldehyde
Synonyms:
Molecular weight: 436.7
CAS: 338404-52-7
Purity: ≥95%
Formulation: A crystalline solid
Product Type|Biochemicals|Receptor Pharmacology|Agonists||Research Area|Toxicology|Drug Metabolism|Cytochrome P450
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}
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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.
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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}
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The maintenance of embryonic stem cells in culture typically requires feeder cells and various exogenous factors found in serum. Murine embryonic stem (mES) cells can be maintained in the absence of feeder cells and serum but require the leukemia inhibitor factor (LIF) and bone morphogenic protein (BMP) to prevent differentiation and promote self-renewal. SC-1 is a small molecule activator of stem cell renewal that allows the propagation of OG2 mES cells for at least 10 passages in an undifferentiated state.{14533} The activity of SC-1 is mediated by the combined inhibition of RasGAP and ERK1 with Kd values of 98 and 212 nM, respectively.{14533} Inhibition of RasGAP increases Ras signaling via the PI3-kinase pathway which promotes self-renewal, whereas inhibition of ERK blocks differentiation.
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