Akt RIMTAC-1
Akt RIMTAC-1 is a Akt RIMTAC degrader (a PROTAC-like agent) with a DC50 of 3.52 μM. Akt RIMTAC-1 forms a ternary complex with AKT and RIPK1, and recruits the VHL E3 ligase complex to mediate ubiquitination and proteasomal degradation. Akt RIMTAC-1 does not alter AKT1 mRNA levels (pink: AKT ligand-5 (HY-187501); blue: RIPK1-ligand-4 (HY-187391); black: Linker (HY-23166)).
For research use only. We do not sell to patients.
- Formula: C53H54ClF4N11O6S
- Molecular Weight:1084.58
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
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Biological Activity
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VHL |
RIPK1 |
Akt RIMTAC-1 (Compound 14) (0.125-5 μM; 18-48 h) induces concentration- and time-dependent degradation of endogenous AKT in HEK-293T cells via the ubiquitin-proteasome system, with a DC50 of 3.52 μM and Dmax of 54.5% after 24 h treatment[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK-293T cells (endogenous AKT)
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Concentration:0.125-5 μM (Western blot; qRT-PCR); 5 μM (proteasome inhibitor co-treatment); 1 μM (NEDD8-activating enzyme inhibitor co-treatment); 5 μM (AKT kinase inhibitor co-treatment); 5 μM (RIPK1 kinase inhibitor co-treatment); 50 μM (prolyl hydroxylase inhibitor co-treatment)
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Incubation Time:18 h (Western blot); 24 h (Western blot; qRT-PCR; co-treatments); 48 h (Western blot)
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Result:Induced substantial endogenous AKT degradation in HEK-293T cells, with a concentration-dependent DC50 of 3.52 μM and a maximum degradation (Dₘₐₓ) of 54.5% after 24 h treatment.
Achieved ~50% AKT degradation at 18 h and maximal degradation at 48 h with 5 μM treatment.
Showed co-treatment with proteasome inhibitor, NEDD8-activating enzyme inhibitor, AKT kinase inhibitor, RIPK1 kinase inhibitor, or prolyl hydroxylase inhibitor significantly restored AKT protein levels.
Confirmed AKT mRNA levels remained unchanged across tested concentrations via qRT-PCR.
Chemical Information
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Molecular Weight 1084.58
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Formula C53H54ClF4N11O6S
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SMILES
ClC1=CC=C(C=C1)[C@@H](NC(C2(N)CCN(CC2)C3=NC=NC4=C3C=CN4)=O)CCN5CCN(CC5)C(CCOCCC(NC6=NC7=C(S6)C=C(C=C7)C8=CC=C(C(NC(CC9=CC=CC(OC(F)(F)F)=C9)=O)=C8)F)=O)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Akt RIMTAC-1 Related Classifications
HY-187500 Related Classifications
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