Vigabatrin is an irreversible GABA transaminase (GABA-T) inhibitor.{55297} It inhibits rat brain GABA-T when used at a concentration of 0.1 mM. Vigabatrin is selective for rat brain GABA-T over P. fluorescens GABA-T at 10 mM and is 100-fold selective over rat brain glutamic acid decarboxylase (GAD). Vigabatrin (1,500 mg/kg) decreases brain GABA-T activity without affecting GAD activity in mice.{55298} It reduces the incidence of myoclonus in a mouse model of audiogenic seizures.{55299} Vigabatrin also increases the electroconvulsive threshold in mouse model of maximal electroshock-induced seizures and reduces the number of clonic convulsions induced by pentylenetetrazol (PTZ; Item No. 18682) in mice.{55300} Formulations containing vigabatrin have been used in the treatment of seizures and infantile spasms.
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A structural analog of the inhibitory neurotransmitter GABA that irreversibly inhibits its catabolism by GABA transaminase; produces a dose-dependent increase in extracellular GABA, and has been shown to result in increasing seizure suppression
Formal name: 4-amino-5-hexenoic acid
Synonyms: γ-Vinyl GABA
Molecular weight: 129.2
CAS: 68506-86-5
Purity: ≥95%
Formulation: A crystalline solid
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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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 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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