Steviol is the aglycon derivative of steviol glycosides, which are natural sweeteners isolated from S. rebaudiana. Steviol inhibits human organic anion transporters (hOATs) in uptake assays using murine cells from the S2 segment of proximal tubules. It is selective for hOAT1 and hOAT3 over hOAT2 and hOAT4 (IC50s = 11.4, 36.5, 1,000, and 285 μM, respectively).{34559} Uptake assays in mouse renal cortical slices yield similar results with IC50 values of 12.8 and 67.6 μM for hOAT1 and hOAT3, respectively.{34559} Due to the use of steviol glycosides as sweeteners, the safety of steviol is widely studied, including its genotoxicity and toxicokinetics.{34557,34558}
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An OAT inhibitor; selective for hOAT1 and hOAT3 over hOAT2 and hOAT4 (IC50s = 11.4, 36.5, 1,000, and 285 μM, respectively)
Formal name: (4α)-13-hydroxy-kaur-16-en-18-oic acid
Synonyms: Hydroxy Dehydrostevic Acid|NSC 226902
Molecular weight: 318.5
CAS: 471-80-7
Purity: ≥98%
Formulation: A crystalline solid
Product Type|Biochemicals|Natural Products||Product Type|Biochemicals|Transporter & Exchanger Modulators||Research Area
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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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 maintenance of embryonic stem cells in culture typically requires feeder cells and various exogenous factors found in serum. Murine embryonic stem (mES) cells can be maintained in the absence of feeder cells and serum but require the leukemia inhibitor factor (LIF) and bone morphogenic protein (BMP) to prevent differentiation and promote self-renewal. SC-1 is a small molecule activator of stem cell renewal that allows the propagation of OG2 mES cells for at least 10 passages in an undifferentiated state.{14533} The activity of SC-1 is mediated by the combined inhibition of RasGAP and ERK1 with Kd values of 98 and 212 nM, respectively.{14533} Inhibition of RasGAP increases Ras signaling via the PI3-kinase pathway which promotes self-renewal, whereas inhibition of ERK blocks differentiation.
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