利克飞龙 T6568

Product Introduction
Bioactivity


英文名: Licofelone

描述: Licofelone (ML-3000) 是一种 COX/LOX 双重抑制剂，IC50分别为 0.21和0.18 μM，有潜力研究骨关节炎，具有抗炎和抗增殖作用。它可诱导细胞凋亡，减少促炎性白三烯和前列腺素的产生。

体外活性: The dual COX/5-LOX inhibitor licofelone triggers apoptosis in a dose- and time-dependent manner in HCA-7 colon cancer cells.?Induction of apoptosis was related to the recruitment of the intrinsic mitochondrial apoptotic pathway, as shown by loss in mitochondrial membrane potential, cytochrome c release, caspase-9 and 3 activation and poly-(ADP-ribose)polymerase-1 cleavage.?Moreover, licofelone induced the cleavage of the full-length p21(Bax) into p18(Bax), a more potent inducer of the apoptotic process than the uncleaved form.?Pre-treatment of HCA-7 cells with the pan-caspase inhibitor z-VAD-fmk significantly blocked licofelone-induced apoptosis, confirming that this process occurred primarily in a caspase-dependent pathway.?Licofelone was able to affect the arachidonic acid (AA) cascade, as it blocked the activity of 5-LOX and COX enzymes, and it induced, through the phosphorylation of cytoplasmic phospholipase A(2) (cPLA(2)), the release of unesterified AA from HCA-7 membrane phospholipids.[1]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 25 mg/mL (65.81 mM)
Ethanol : 10 mg/mL (26.32 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble) (< 1 mM)


关键字: Lipoxygenase | LOX | Apoptosis | COX | Licofelone | Inhibitor | ML3000 | inhibit | ML 3000 | Cyclooxygenase

相关产品: Ezatiostat | Protosappanin B | 4-Thiothymidine | Sunitinib Malate | TTNPB | Epoxomicin | PARP-1-IN-3 | G5-7 | Embelin | EAD1 TFA(1644388-26-0 Free base)

相关库: Anti-Aging Compound Library | Anti-Cancer Compound Library | Bioactive Compounds Library Max | Ferroptosis Compound Library | Neuronal Signaling Compound Library | Human Metabolite Library | Inhibitor Library | Apoptosis Compound Library | Lipid Metabolism Compound Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途