Results for Activators & Inhibitors ( 70851 )
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2-O-(α-D-Glucopyranosyl)glycerol (Legacy Tebubio ref. 282T38376). 2-O-(α-D-Glucopyranosyl)glycerol (2-alphaGG) is present in certain bacteria and plants that thrive in harsh environments and may extend the lifespan of budding yeast and erythrosporidium by enhancing their osmotic response.
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ADTL-EI1712 (Legacy Tebubio ref. 282T38377). ADTL-EI1712 is a dual inhibitor of ERK1 and ERK5 (IC50s = 40.43 and 64.5 nM, respectively).1It reduces ERK1 and ERK5 activity by 93.5% and 89.4%, respectively, but also inhibits ERK2 activity by 92.7%, in a panel of 100 kinases at 1 μM. ADTL-EI1712 inhibits proliferation of HL-60 and MKN74, but not HeLa, cancer cells (IC50s = 1.26, 2.55, and >50 μM, respectively). It reduces tumor growth and intratumor phosphorylation of ERK1/2 and ERK5 in an MKN74 mouse xenograft model when administered at a dose of 50 mg/kg per day.
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Dnp-PLAYWAR (trifluoroacetate salt) (Legacy Tebubio ref. 282T38378). Dnp-PLAYWAR is a fluorogenic substrate for matrix metalloproteinase-8 (MMP-8) and MMP-26. The activity of MMP-8 and MMP-26 can be quantified by measuring tryptophan fluorescence that is unquenched upon peptide hydrolysis that removes the N-terminal dinitrophenol (Dnp) group.
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4-tert-Octylphenol diethoxylate (Legacy Tebubio ref. 282T38379). 4-tert-Octylphenol diethoxylate is a degradation product of the multi-purpose surfactant, Triton X. A known environmental contaminant, 4-tert-octylphenol diethoxylate is reported to be an endocrine disruptor in animal and human research studies, producing weak estrogenic effects.
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CAY17c (Legacy Tebubio ref. 282T38381). CAY17c is an inhibitor of bromodomain-containing protein 4 (BRD4; IC50= 0.71 μM), as well as class I histone deacetylases (HDACs; IC50s = 0.046, 0.058, 0.075, and 0.167 μM for HDAC1, -2, -3, and -8, respectively) and class IIb HDACs (IC50s = 0.073 and 0.923 μM for HDAC6 and HDAC10, respectively).1It is selective for these enzymes over BRD2, -3, and -T (IC50s = >20 μM for all), as well as over HDAC4, -5, -7, -9, and -11 (IC50s = >10 μM for all). CAY17c inhibits the proliferation of HCT116, SW620, and DLD-1 colorectal cancer cells (IC50s = 0.45, 1.78, and 2.11 μM, respectively), as well as induces apoptosis and autophagy in HCT116 cells. It reduces tumor growth in an HCT116 mouse xenograft model when administered at doses of 15 and 30 mg/kg.