2. PROTAC PI3K/Akt/mTOR
  3. PROTACs Akt
  4. INY-03-041 trihydrochloride

INY-03-041 trihydrochloride 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 trihydrochloride inhibits AKT1, AKT2 and AKT3 with IC50s of 2.0, 6.8 and 3.5 nM, respectively.

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

INY-03-041 trihydrochloride Chemical Structure

INY-03-041 trihydrochloride Chemical Structure

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Based on 1 publication(s) in Google Scholar

Other Forms of INY-03-041 trihydrochloride:

INY-03-041 trihydrochloride Related Antibodies

Top Publications Citing Use of Products

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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Akt Akt1 Akt2 Akt3

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

INY-03-041 trihydrochloride 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 trihydrochloride inhibits AKT1, AKT2 and AKT3 with IC50s of 2.0, 6.8 and 3.5 nM, respectively[1].

IC50 & Target

Akt1

2.0 nM (IC50)

Akt3

3.5 nM (IC50)

Akt2

6.8 nM (IC50)

Cereblon

 

In Vitro

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

INY-03-041 trihydrochloride Related Antibodies

Western Blot Analysis[1]

Cell Line: MDA-MB-468 cells
Concentration: 0, 10, 50, 100, 250, 500, and 1000 nM
Incubation Time: 0, 2, 4, 6, 8. 10, 12, and 24 h
Result: Induced 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.
Molecular Weight

907.80

Formula

C44H59Cl4N7O5
Appearance

Solid

Color

Off-white to light yellow

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Purity & Documentation
References
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INY-03-041 trihydrochloride Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

INY-03-041 trihydrochloridePROTACsAktPKBProtein kinase BCRBNMDA-MB-468HCC1937 cellsZR-75-1 cellsPC3 cellsInhibitorinhibitorinhibit

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INY-03-041 trihydrochloride
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