5-Butyl-4-[2,3-difluoro-4-(phenylmethoxy)phenyl]-6-phenyl-2-pyrimidinamine is an inhibitor of microsomal prostaglandin E synthase-1 (mPGES-1; IC50s = 66 and 2,730 nM for the human and mouse enzymes, respectively).{52747} It is selective for mPGES-1 over COX-1 but does inhibit COX-2 at 20 µM. It also inhibits LPS-induced prostaglandin E2 (PGE2; Item No. 14010) production in mouse peritoneal cells (IC50 = 12 nM). In vivo, 5-butyl-4-[2,3-difluoro-4-(phenylmethoxy)phenyl]-6-phenyl-2-pyrimidinamine (25 mg/kg) reduces carrageenan-induced paw edema in rats.
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An mPGES-1 inhibitor (IC50s = 66 and 2,730 nM for human and mouse enzymes, respectively); selective for mPGES-1 over COX-1 but does inhibit COX-2 at 20 µM; inhibits LPS-induced PGE2 production in mouse peritoneal cells (IC50 = 12 nM); reduces carrageenan-induced paw edema in rats at 25 mg/kg
Formal name:
Synonyms:
Molecular weight: 445.5
CAS: 2253745-78-5
Purity: ≥98%
Formulation: A solution in methyl acetate
Cyclin-dependent kinases (CDKs) are key regulators of cell cycle progression and are therefore promising targets for cancer therapy. (R)-Roscovitine is a potent inhibitor of Cdk2/cyclin E with an IC50 value of 0.1 µM.{14988} It also inhibits Cdk7/cyclin H, Cdk5/p35, and cell division cycle (cdc)/cyclin B with IC50 values of 0.49, 0.16, and 0.65 µM, respectively.{14987,14988,14991} (R)-Roscovitine inhibits the growth of rapidly proliferating cells with an average IC50 value of 15.2 µM against a panel of 19 human tumor cell lines.{14988} In murine models of polycystic kidney disease, (R)-roscovitine effectively inhibited disease progression at doses of 50-100 mg/kg.{14564}
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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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Cyclin-dependent kinases (CDKs) are key regulators of cell cycle progression and are therefore promising targets for cancer therapy. (R)-Roscovitine is a potent inhibitor of Cdk2/cyclin E with an IC50 value of 0.1 µM.{14988} It also inhibits Cdk7/cyclin H, Cdk5/p35, and cell division cycle (cdc)/cyclin B with IC50 values of 0.49, 0.16, and 0.65 µM, respectively.{14987,14988,14991} (R)-Roscovitine inhibits the growth of rapidly proliferating cells with an average IC50 value of 15.2 µM against a panel of 19 human tumor cell lines.{14988} In murine models of polycystic kidney disease, (R)-roscovitine effectively inhibited disease progression at doses of 50-100 mg/kg.{14564}
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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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