The pro-angiogenic factor HIF-1α is targeted for destruction in non-hypoxic environments by the hydroxylation of a specific proline residue, P564, by the oxygen-sensing enzyme HIF-α prolyl hydroxylase (HIF-PH).{8840} Inhibitors of prolyl 4-hydroxylase are potentially useful in controlling excess collagen deposition in pathological fibrosis. 1,4-DPCA is a competitive inhibitor of prolyl 4-hydroxylase in embryonic chick tendon cells and of collagen hydroxylation in human foreskin fibroblasts with an IC50 value of 3.6 and 2.4 µM, respectively.{9009} β-oxocarboxylic acids such as 1,4-DPCA have also been found to inhibit the asparaginyl-hydroxylase, factor inhibiting HIF (FIH), with an IC50 value of 60 µM.{14775}
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A competitive inhibitor of HIF prolyl 4-hydroxylase (IC50 = 2.4-3.6 µM)
Formal name: 4,4α-dihydro-4-oxo-1,10-phenanthroline-3-carboxylic acid
Synonyms: 1,4-dihydrophenonthrolin-4-one-3-Carboxylic acid
Molecular weight: 240.2
CAS: 331830-20-7
Purity: ≥98%
Formulation: A crystalline solid
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 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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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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