| Description | L48H37 is a chemically stable analog of Curcumin. It exhibits potent inhibitory properties against myeloid differentiation protein 2 (MD2), acting as a specific inhibitor. Its mechanism involves inhibiting the interaction and signaling transduction of LPS-TLR4/MD2. L48H37 is primarily utilized in sepsis and lung injury research [1]. |
| In vitro | L48H37抑制LPS诱导的小鼠巨噬细胞中特别是TNF-α和IL-6的产生及基因表达[1]。在肺癌细胞中，L48H37 (0-20 μM; 24小时)降低了A549和H460细胞的活性，其IC50值分别为5.3μM和2.3μM，这比姜黄素效果更佳。对正常人肺上皮细胞(BEAS-2B)的低细胞毒性，IC50为21μM[2]。L48H37 (1, 2或4 μM; 16小时)剂量依赖性抑制p‐Cdc2和Cdc2的表达，并增加p53的表达。同时，H460和A549细胞中切割型聚(ADP-核糖)聚合酶(PARP)的水平升高，而抗凋亡蛋白Bcl-2的水平降低[2]。L48H37 (4μM; 16小时)迅速剂量依赖性地诱导H460和A549细胞内ROS水平上升，通过增加DCF水平检测到[2]。细胞活性测定[2]细胞系：A549和H460细胞；BEAS-2B细胞浓度：0.625, 1.25, 2.5, 5, 7.5, 10和20μM孵育时间：24小时结果：以浓度依赖的方式抑制肺癌细胞生长。西方印迹分析[2]细胞系：A549和H460细胞浓度：0.625, 1.25, 2.5, 5, 7.5, 10和20μM孵育时间：24小时结果：在两种肺癌细胞中减少了p‐Cdc2、Cdc2和Bcl‐2的表达。 |
| In vivo | L48H37（腹腔注射；每日一次；11天；剂量为5 mg或10 mg/kg）在小鼠中抑制H460异种移植瘤生长，并展现出抗肿瘤活性[1]。动物模型：5周龄无胸腺BALB/cA nu/nu雌性小鼠（18-22 g）[2]。剂量：5 mg或10 mg/kg。给药方式：腹腔注射；每日一次；共11天。结果：与对照组相比，降低了肿瘤湿重。降低了p-STAT3水平，并增加了p-EIF2α与ATF4的水平。小鼠未显示出明显的结构变化。 |
| molecular weight | 483.55 |
| Molecular formula | C27H33NO7 |
| CAS | 343307-76-6 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 45 mg/mL (93.06 mM), Sonication is recommended. |
| References | 1. Yi Wang, et al. Curcumin Analog L48H37 Prevents Lipopolysaccharide-Induced TLR4 Signaling Pathway Activation and Sepsis via Targeting MD2. J Pharmacol Exp Ther. 2015 Jun;353(3):539-50 2. Chen Feng, et al. Curcumin analog L48H37 induces apoptosis through ROS-mediated endoplasmic reticulum stress and STAT3 pathways in human lung cancer cells. Mol Carcinog. 2017 Jul;56(7):1765-1777. |