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A dual inhibitor of Cdk8 and Cdk19 (IC50s = 4.4 and 10.4 nM, respectively); selective for Cdk8 and Cdk19 over a panel of CDK/cyclin complexes at 1 µM; inhibits IFN-γ-induced phosphorylation of STAT1 in HCT116 colon cancer cells at 0.1-5 µM; inhibits proliferation of MOLM-16, MV4-11, and KG-1 cells (GI50s = <1 µM); reduces tumor growth in a KG-1 mouse xenograft model at 60 mg/kg
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A dipeptide; inhibits AAPH-induced lipid peroxidation at 10 mM; decreases LDH and PGE2 release from PC12 cells in an in vitro model of ischemia induced by oxygen-glucose deprivation at 1 mM; reduces infarct area and neurological deficit scores in a rat model of MCAO-induced cerebral ischemia-reperfusion injury; reduces mortality in a mouse model of subcutaneous S. aureus infection at 5 mg/animal
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A flavonoid with antioxidant and anticancer activities; scavenges superoxide anions in a cell-free assay at 100 µM; decreases EGFR and phosphorylated EGFR levels in, and reduces viability of, PC-9 and H1975 NSCLC cells at 25 and 50 µM; decreases intratumoral levels of EGFR and phosphorylated EGFR and reduces tumor growth in an H1975 mouse xenograft model at 1 mg/kg
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A BTK inhibitor (IC50s = 10-100 and C481S, respectively); selective for BTK over EGFR (IC50 = 1-10 µM); decreases the number of Ki67-positive cells in MEC-1 CLL mouse xenograft models using MEC-1 cells that express either wild-type BTK or BTKC481S
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N-4AIA is one of several aromatic amides of indomethacin reported to be potent and selective reversible inhibitors of COX-2.{8243} N-4AIA inhibits human recombinant and ovine COX-2 with IC50 values of 0.1 and 0.625 µM, respectively.{8243,8513} It is about 80 times less potent as an inhibitor of ovine COX-1 than ovine COX-2.
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A major metabolite of olaquindox; induces cell cycle arrest at the S phase and is toxic to Chang liver cells in a concentration- and time-dependent manner; has been used as a marker of olaquindox use in livestock applications
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A sesquiterpene with diverse biological activities; inhibits proliferation of, as well as halts the cell cycle at the G2/M phase and induces apoptosis in, DU145 and LNCaP prostate cancer cells at 50 and 100 µM; prevents irradiation-induced cutaneous and intestinal ulcers in mice at 60 mg/kg
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A peripherally restricted µ-opioid receptor antagonist (Ki = 10 nM; IC50s = 130.7 and 0.43 nM in rat brain membranes prepared with sodium chloride or water, respectively); selective for µ-opioid receptors over δ- and κ-opioid receptors (Kis = 630.95 and 31.62 nM, respectively); decreases spontaneous mechanical activity in ileum isolated from morphine-treated guinea pigs when administered at doses of 1 and 10 µM; does not inhibit heroin self-administration in rats; does not induce withdrawal syndrome in morphine-dependent rhesus monkeys when administered at doses up to 32 mg/kg
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A phospholipid; has been used in the generation of LNPs for the delivery of mRNA in vivo; has been used in the synthesis of various PEG-conjugates for incorporation into liposomes; LNPs containing 1,2-dierucoyl-sn-glycero-3-PE and encapsulating mRNA encoding hEPO increase serum hEPO levels in mice
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A racemic mixture of 8(R)-KAPA and 8(S)-KAPA; biosynthesized as the 8(S) form but racemizes in culture media in a pH-dependent manner, with a higher racemization rate under very low (pH E. coli and M. tuberculosis DAPA AT, which leads to accumulation of 8(R)-KAPA in M. tuberculosis cultures after exogenous application of racemic KAPA
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A form of tocopherol; has similar antioxidant activity to α-tocol, but lower activity than γ-tocol; increases microviscosity of PC rat liver liposomes by 70.6% when used at a molar ratio of 0.2 to PC; has been used as an internal standard for the quantification of tocols, tocopherols, and tocopheryl quinones by HPLC
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