1. PROTAC
    PI3K/Akt/mTOR
  2. PROTAC
    Akt
  3. INY-03-041

INY-03-041 

Cat. No.: HY-133120
Handling Instructions

INY-03-041 is a potent, highly selective and PROTAC-based pan-AKT degrader consisting of the ATP-competitive AKT inhibitor GDC-0068 conjugated to Lenalidomide. INY-03-041 inhibits AKT1, AKT2 and AKT3 with IC50s of 2.0 nM, 6.8 nM and 3.5 nM, respectively.

For research use only. We do not sell to patients.

INY-03-041 Chemical Structure

INY-03-041 Chemical Structure

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Description

INY-03-041 is a potent, highly selective and PROTAC-based pan-AKT degrader consisting of the ATP-competitive AKT inhibitor GDC-0068 conjugated to Lenalidomide. INY-03-041 inhibits AKT1, AKT2 and AKT3 with IC50s of 2.0 nM, 6.8 nM and 3.5 nM, respectively[1].

IC50 & Target[1]

Akt1

2.0 nM (IC50)

Akt2

6.8 nM (IC50)

Akt3

3.5 nM (IC50)

Cereblon

 

In Vitro

INY-03-041 (10-1000 nM; 2-24 hours; MDA-MB-468 cells) treatment induces potent degradation of all three AKT isoforms in a dose-dependent manner after a 12-h treatment, with maximal degradation observed between 100 and 250 nM. At concentrations of 500 nM and greater, AKT degradation is diminished. Treatment with 250 nM of INY-03-041 over time reveals partial degradation of all AKT isoforms within 4 h and progressive loss of AKT abundance out to 24 h[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 GDC-0068 in MDA-MB-468 and HCC1937 cells[1].

Western Blot Analysis[1]

Cell Line: MDA-MB-468 cells
Concentration: 10 nM, 50 nM, 100 nM, 250 nM, 500 nM, 1000 nM
Incubation Time: 2 hours, 4 hours, 6 hours, 8 hours, 10 hours, 12 hours, 24 hours
Result: Induced potent degradation of all three AKT isoforms in MDA-MB-468 cells.
Molecular Weight

798.41

Formula

C₄₄H₅₆ClN₇O₅

SMILES

O=C(C(N(CC1=C2C=CC=C1CCCCCCCCCCNC[[email protected]](C3=CC=C(Cl)C=C3)C(N4CCN(C5=C([[email protected]](C)C[[email protected]]6O)C6=NC=N5)CC4)=O)C2=O)CC7)NC7=O

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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

INY-03-041PROTACAktProteolysis-targeting chimeraPKBProtein kinase BAKT1AKT2AKT3LenalidomideGDC-0068anti-proliferativeInhibitorinhibitorinhibit

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INY-03-041
Cat. No.:
HY-133120
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