For research use only. Not for therapeutic Use.
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].
Catalog Number | I045144 |
CAS Number | 1048660-43-0 |
Synonyms | N-(benzenesulfonyl)-2-[1-benzyl-2-(2-methylpropyl)-3-oxamoylindol-4-yl]oxypropanamide |
Molecular Formula | C30H31N3O6S |
Purity | ≥95% |
InChI | InChI=1S/C30H31N3O6S/c1-19(2)17-24-27(28(34)29(31)35)26-23(33(24)18-21-11-6-4-7-12-21)15-10-16-25(26)39-20(3)30(36)32-40(37,38)22-13-8-5-9-14-22/h4-16,19-20H,17-18H2,1-3H3,(H2,31,35)(H,32,36) |
InChIKey | REUKAAAAEHWGGM-UHFFFAOYSA-N |
SMILES | CC(C)CC1=C(C2=C(N1CC3=CC=CC=C3)C=CC=C2OC(C)C(=O)NS(=O)(=O)C4=CC=CC=C4)C(=O)C(=O)N |
Reference | [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. |