Adefovir-d4 is intended for use as an internal standard for the quantification of adefovir (Item No. 18650) by GC- or LC-MS. Adefovir is an active metabolite of the antiviral nucleoside analog adefovir dipivoxil (Item No. 28373).{56174} Adefovir is formed from adefovir dipivoxil by gastrointestinal carboxylesterase 2 (CES2).{56175} It inhibits cytopathogenicity induced by herpes simplex virus 1 (HSV-1) and HSV-2 (EC50 = 7 µg/ml for both in E6SM cells), HIV-1 and HIV-2 (EC50s = 1.8 and 2.5 µg/ml, respectively, in CEM cells), and varicella zoster virus (VZV; EC50 = 10 µg/ml in human embryonic lung fibroblasts).{56176} Adefovir (50 mg/kg, p.o.) reduces increases in lymph node viral DNA and serum IgG levels in a mouse model of AIDS induced by infection with the retroviral complex LP-BM5.{56177} It also inhibits tumor growth induced by Moloney sarcoma virus (MSV) infection in mice at the same dose.{56178}
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An internal standard for the quantification of adefovir by GC- or LC-MS
Formal name: P-[[2-(6-amino-9H-purin-9-yl)ethoxy-1,1,2,2-d4]methyl]-phosphonic acid
Synonyms: PMEA-d4
Molecular weight: 277.2
CAS: 1190021-70-5
Purity: ≥99% deuterated forms (d1-d4)
Formulation: A solid
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 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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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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