The enzyme indoleamine 2,3-dioxygenase (IDO) has been implicated in mediating pathological immunosuppression associated with certain diseases, including cancer. Several naphthoquinones inhibit IDO in vitro and in cells, but at low (μM) potency.{16354} Importantly, naphthoquinones reduce tumor growth in wild type mice but not in IDO-deficient mice.{16354} CAY10581 is a naphthoquinone derivative that potently inhibits IDO (IC50 = 55 nM).{16354} It is a more potent inhibitor of IDO than annulin B or 1-methyl-d-tryptophan (1MT). CAY10581 acts as a reversible uncompetitive inhibitor of IDO and demonstrates minimal impact on cell viability at 100 μM after 24 hours.{16354}
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A naphthoquinone derivative that potently and reversibly inhibits indoleamine 2,3-dioxygenase (IC50 = 55 nM); a more potent inhibitor of IDO than annulin B or 1-methyl-d-tryptophan (1MT)
Formal name: (±)3,4-dihydro-3-hydroxy-2,2-dimethyl-4-[(phenylmethyl)amino]-2H-naphtho[2,3-b]pyran-5,10-dione
Synonyms:
Molecular weight: 363.4
CAS: 1018340-07-2
Purity: ≥97%
Formulation: A crystalline solid
Product Type|Biochemicals|Small Molecule Inhibitors||Research Area
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 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}
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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 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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