Aconitase catalyzes the stereospecific isomerization of citrate to isocitrate in the first step of the citric acid cycle. It acts as an iron regulatory protein (IRP), controlling the translation of proteins involved in iron metabolism when iron is scarce and resumes aconitase activity when iron is abundant. Aconitase is now recognized as a regulator of iron-induced glutamate production.{17857} Oxalomalic acid, formed by the condensation of oxaloacetate with glyoxylate in vivo, inhibits both aconitase and NADP-dependent isocitrate dehydrogenase in the conversion of citrate to isocitrate at concentrations as low as 1 mM.{17849} At 5 mM, oxalomalic acid inhibition of aconitase leads to a decrease in the binding activity of IRP1 and a decrease in glutamate secretion in cultured lens epithelial cells, retinal pigment epithelial cells, and neurons.{17850,17851}
Formed by the condensation of oxaloacetate with glyoxylate; inhibits aconitase activity at 1 mM, which interferes with IRP1 binding and decreases glutamate secretion in lens and retinal pigment epithelial cells
Formal name: 3-carboxy-3-deoxy-2-pentulosaric acid, trisodium salt
Synonyms:
Molecular weight: 275
CAS: 89304-26-7
Purity: ≥95%
Formulation: A crystalline solid
Product Type|Biochemicals|Small Molecule Inhibitors||Research Area
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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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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