Finasteride-d9 is intended for use as an internal standard for the quantification of finasteride (Item No. 14938) by GC- or LC-MS. Finasteride is a 4-azasteroid competitive inhibitor of 5α-reductase type II (IC50 = 4.2 nM) and a derivative of testosterone.{23862} It is 100-fold selective for 5α-reductase type II over type I. Finasteride (10 µM) does not affect the growth of androgen-refractory PC3 prostate cancer cells but increases the protein levels of Nrf2 and heme oxygenase-1 (HO-1).{23866} It decreases prostatic diameter and volume, as well as dihydrotestosterone, but not testosterone, serum levels in dogs with spontaneous benign prostatic hypertrophy when administered at doses of 0.1 and 0.5 mg/kg.{48477} Finasteride reduces testosterone-induced type I procollagen and TGF-β1 protein levels in cultured human scalp dermal fibroblasts in a model of androgenic alopecia when applied at a concentration of 0.1 μM.{23865} Formulations containing finasteride have been used in the treatment of benign prostatic hyperplasia and androgenic alopecia in men.
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An internal standard for the quantification of finasteride by GC- or LC-MS
Formal name: (4aR,4bS,6aS,7S,9aS,9bS,11aR)-4a,6a-dimethyl-N-(2-(methyl-d3)propan-2-yl-1,1,1,3,3,3-d6)-2-oxo-2,4a,4b,5,6,6a,7,8,9,9a,9b,10,11,11a-tetradecahydro-1H-indeno[5,4-f]quinoline-7-carboxamide
Synonyms:
Molecular weight: 381.6
CAS: 1131342-85-2
Purity: ≥99% deuterated forms (d1-d9)
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 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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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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