Typical mitochondrial uncouplers are lipophilic weak acids that increase proton transport into the mitochondrial matrix through an ATP synthase-independent pathway, thereby uncoupling nutrient oxidation from ATP production. These chemicals are used to determine rate of cellular respiration and have antioxidant effects that protect from ischemia-reperfusion injury. Most proton transporter uncouplers, however, exhibit off-target activity that can lead to undesired effects, including plasma membrane depolarization, mitochondrial inhibition, and cytotoxicity. BAM15 is a mitochondrial protonophore uncoupler that does not depolarize the plasma membrane and protects mice from acute renal ischemic-reperfusion injury.{28818} In comparison to FCCP (Item No. 15218), 1-10 µM BAM15 was shown to increase oxygen flux with equal potency as the classic uncoupler, while displaying a higher maximum rate of mitochondrial respiration and less cytotoxicity.{28818}
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A mitochondrial protonophore uncoupler that does not depolarize the plasma membrane and protects mice from acute renal ischemic-reperfusion injury
Formal name: N5,N6-bis(2-fluorophenyl)-[1,2,5]oxadiazolo[3,4-b]pyrazine-5,6-diamine
Synonyms:
Molecular weight: 340.3
CAS: 210302-17-3
Purity: ≥98%
Formulation: A crystalline solid
Product Type|Biochemicals|Small Molecule Inhibitors|Oxidative Phosphorylation||Research Area|Cell Biology|Mitochondrial Biology
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 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 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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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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