E3 ligase Ligand 2

An active metabolite of thalidomide and a PROTAC synthetic intermediate

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1g

￥325.00

260.00

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2g

￥487.00

390.00

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100mg

￥1100.00

880.00

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500mg

￥2725.00

2180.00

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货号: ajce49938
CAS: 5054-59-1
别名: 2-(2,6-二氧代-哌啶-3-基)-4-羟基-异吲哚-1,3-二酮,Cereblon ligand 2; E3 ligase Ligand 2
分子式: C13H10N2O5
分子量: 274.23
纯度: >98%
溶解度: DMSO : ≥ 36.5 mg/mL (133.10 mM)
储存: Store at -20°C
库存: 现货

Background

E3 ligase ligand 2 is an active metabolite of thalidomide and an intermediate in the synthesis of proteolysis-targeting chimeras (PROTACs) containing thalidomide, a ligand for the E3 ubiquitin ligase cereblon (CRBN), used in targeted protein degradation.^1,2 E3 ligase ligand 2 is formed from thalidomide via hydroxylation. It decreases the production of TNF-α induced by 12-O-tetradecanoylphorbol 13-acetate in THP-1 cells when used at a concentration of 30 ?M.³ E3 ligase ligand 2 (333 ?M) completely inhibits the proliferation of human umbilical vein endothelial cells (HUVECs). It inhibits VEGF- and FGF2-induced angiogenesis by 14% in a chicken chorioallantoic membrane (CAM) assay in utero when administered at a dose of 100 ?g/embryo.¹

1.Marks, M.G., Shi, J., Fry, M.O., et al.Effects of putative hydroxylated thalidomide metabolites on blood vessel density in the chorioallantoic membrane (CAM) assay and on tumor and endothelial cell proliferationBiol. Pharm. Bull.25(5)597-604(2002) 2.Robb, C.M., Contreras, J.I., Kour, S., et al.Chemically induced degradation of CDK9 by a proteolysis targeting chimera (PROTAC)Chem. Commun. (Camb.)53(54)7577-7580(2017) 3.Nakamura, T., Noguchi, T., Kobayashi, H., et al.Mono- and dihydroxylated metabolites of thalidomide: Synthesis and TNF-α production-inhibitory activityChem. Pharm. Bull. (Tokyo)54(12)1709-1714(2006)