ROC-0929 (compound 13a) 是一种有效且选择性的分泌型磷脂酶 A2 (sPLA2s) 抑制剂。其IC50值为 80 nM，特异性靶点为hGX。ROC-0929 抑制 ERK1/2 和 p-38 的磷酸化。分泌型磷脂酶 A2 (sPLA2s) 是富含二硫键的 Ca2+ 依赖性酶家族，可水解甘油磷脂的 sn-2 位以释放脂肪酸和溶血磷脂。ROC-0929具有研究炎症相关疾病的潜力。
| Cas No. | 1048660-43-0 |
| 分子式 | C30H31N3O6S |
| 分子量 | 561.65 |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | ROC-0929 (compound 13a) is a potent and selective inhibitor of secreted phospholipases A2 (sPLA2s) with an IC50 of 80 nM, specially targeting hGX. ROC-0929 inhibits the phosphorylation of ERK1/2 and p-38. Secreted phospholipases A2 (sPLA2s) are a family of disulfide-rich, Ca2+-dependent enzymes that hydrolyze the sn-2 position of glycero-phospholipids to release a fatty acid and a lysophospholipid. ROC-0929 has the potential for researching inflammation related diseases[1]. [1]. Oslund RC, et al. Highly specific and broadly potent inhibitors of mammalian secreted phospholipases A2. J Med Chem. 2008;51(15):4708-4714.
[2]. Hallstrand TS, et al. Endogenous secreted phospholipase A2 group X regulates cysteinyl leukotrienes synthesis by human eosinophils. J Allergy Clin Immunol. 2016;137(1):268-277.e8. |
