For research use only. Not for therapeutic Use.
INY-03-041 is a potent, highly selective and PROTAC-based pan-AKT degrader consisting of the ATP-competitive AKT inhibitor Ipatasertib (HY-15186) conjugated to Lenalidomide (HY-A0003, Cereblon ligand). INY-03-041 inhibits AKT1, AKT2 and AKT3 with IC50s of 2.0, 6.8 and 3.5 nM, respectively[1].
INY-03-041 (10-1000 nM; 0-24 hours) induces potent degradation of all three AKT isoforms in MDA-MB-468 cells[1].
INY-03-041 exhibits potent in vitro inhibition of S6K1 (IC50 =37.3 nM) and PKG1 (IC50 = 33.2 nM)[1].
INY-03-041 displays enhanced anti-proliferative effects compared with Ipatasertib (HY-15186) in MDA-MB-468 and HCC1937 cells[1].
INY-03-041 (250 nM, 12 h) promotes sustained AKT degradation and inhibition of downstream signaling effects for up to 96 h, even after compound washout[1].
| Catalog Number | I045984 |
| CAS Number | 2503017-97-6 |
| Synonyms | 3-[7-[10-[[(2S)-2-(4-chlorophenyl)-3-[4-[(5R,7R)-7-hydroxy-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl]piperazin-1-yl]-3-oxopropyl]amino]decyl]-3-oxo-1H-isoindol-2-yl]piperidine-2,6-dione |
| Molecular Formula | C44H56ClN7O5 |
| Purity | ≥95% |
| InChI | InChI=1S/C44H56ClN7O5/c1-29-25-37(53)40-39(29)41(48-28-47-40)50-21-23-51(24-22-50)43(56)34(31-14-16-32(45)17-15-31)26-46-20-9-7-5-3-2-4-6-8-11-30-12-10-13-33-35(30)27-52(44(33)57)36-18-19-38(54)49-42(36)55/h10,12-17,28-29,34,36-37,46,53H,2-9,11,18-27H2,1H3,(H,49,54,55)/t29-,34-,36?,37-/m1/s1 |
| InChIKey | GQGZWBDNMCIYSF-OZDCPDTESA-N |
| SMILES | CC1CC(C2=C1C(=NC=N2)N3CCN(CC3)C(=O)C(CNCCCCCCCCCCC4=C5CN(C(=O)C5=CC=C4)C6CCC(=O)NC6=O)C7=CC=C(C=C7)Cl)O |
| Reference | [1]. You I, et al. Discovery of an AKT Degrader with Prolonged Inhibition of Downstream Signaling. Cell Chem Biol. 2020 Jan 16;27(1):66-73.e7. [2]. Maira SM, et al. Identification and characterization of NVP-BKM120, an orally available pan-class I PI3-kinase inhibitor. Mol Cancer Ther. 2012 Feb;11(2):317-28. |
