For research use only. Not for therapeutic Use.
VHL Ligand 14 (Compound 11) is a VHL ligand for design of PROTAC estrogen receptor α (ERα) degraders, with a binding affinity IC50 of 196 nM[1].
VHL Ligand 14 (5-10 μM) supports the stability of PROTAC ER degrader, promotes the ER degradation[1].
Catalog Number | I040021 |
CAS Number | 2010986-87-3 |
Synonyms | (2S,4R)-1-[(2S)-2-acetamido-3,3-dimethylbutanoyl]-4-hydroxy-N-[(1S)-1-[4-(4-methyl-1,3-thiazol-5-yl)phenyl]ethyl]pyrrolidine-2-carboxamide |
Molecular Formula | C25H34N4O4S |
Purity | ≥95% |
InChI | InChI=1S/C25H34N4O4S/c1-14(17-7-9-18(10-8-17)21-15(2)26-13-34-21)27-23(32)20-11-19(31)12-29(20)24(33)22(25(4,5)6)28-16(3)30/h7-10,13-14,19-20,22,31H,11-12H2,1-6H3,(H,27,32)(H,28,30)/t14-,19+,20-,22+/m0/s1 |
InChIKey | JAHUHEDUDMTTTF-COWZOJLOSA-N |
SMILES | CC1=C(SC=N1)C2=CC=C(C=C2)C(C)NC(=O)C3CC(CN3C(=O)C(C(C)(C)C)NC(=O)C)O |
Reference | [1]. Hu J, et al., Discovery of ERD-308 as a Highly Potent Proteolysis Targeting Chimera (PROTAC) Degrader of Estrogen Receptor (ER). J Med Chem. 2019 Feb 14;62(3):1420-1442. |