Latanoprost (free acid)-d4 (Lat-FA-d4) contains four deuterium atoms at the 3, 3, 4, and 4 positions. It is intended for use as an internal standard for the quantification of Lat-FA by GC- or LC-mass spectrometry. Latanoprost is an F-series prostaglandin (PG) analog which has been approved for use as an ocular hypotensive drug.{1107} It is the isopropyl ester of a PGF2α analog containing an aromatic group (17-phenyl) in the ω-chain. As an isopropyl ester, latanoprost acts as a prodrug which is converted to Lat-FA by endogenous esterase enzymes. Lat-FA is a potent FP receptor agonist with an EC50 value of 3.6 nM for human FP receptors, which is twice the potency of PGF2α and more than 200 times more potent latanoprost.{8322} The efficacy of PG analog esters for the treatment of glaucoma correlates closely with the FP receptor binding affinity of the free acid.{3802} However, Lat-FA is more irritating and less effective than the prodrug latanoprost when applied directly to the eyes of human glaucoma patients.{5358}
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An internal standard for the quantification of latanoprost (free acid) by GC- or LC-MS.
Formal name: 9α,11α,15R-trihydroxy-17-phenyl-18,19,20-trinor-prost-5Z-en-1-oic-3,3,4,4-d4 acid
Synonyms: 17-phenyl-13,14-dihydro trinor Prostaglandin F2α-d4|Lat-FA-d4|PhXA 85-d4
Molecular weight: 394.5
CAS: 1224443-47-3
Purity: ≥99% deuterated forms (d1-d4)
Formulation: A solution in methyl acetate
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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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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