JNJ-0966 is an inhibitor of matrix metalloproteinase-9 (MMP-9) zymogen activation (IC50 = 440 nM).{54517} It is selective for MMP-9 over MMP-1, MMP-2, and MMP-3 zymogen activation at 10 μM and does not inhibit the catalytic activity of MMP-1, -2, -3, -9, or -14. It inhibits invasion of HT-1080 cells in a MatrigelTM assay (IC50 = 1 μM). JNJ-0966 (10 and 30 mg/kg, twice per day) reduces disease severity in a mouse model of experimental autoimmune encephalomyelitis (EAE).
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An inhibitor of MMP-9 zymogen activation (IC50 = 440 nM); selective for MMP-9 over MMP-1, MMP-2, and MMP-3 zymogen activation at 10 μM; inhibits invasion of HT-1080 cells in a MatrigelTM assay (IC50 = 1 μM); reduces disease severity in a mouse model of EAE at 10 and 30 mg/kg, twice per day
Formal name: N-[2-[(2-methoxyphenyl)amino]-4′-methyl[4,5′-bithiazol]-2′-yl]-acetamide
Synonyms:
Molecular weight: 360.5
CAS: 315705-75-0
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 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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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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