EST1027
EST1027 is a CDK4 Molecular glue degrader. EST1027 degrades CDK4 by forming a CDK4-EST1027-RNF126 ternary complex. EST1027 can be used for research on cervical cancer.
For research use only. We do not sell to patients.
- CAS No.: 3036530-23-8
- Formula: C33H35F3N8O2
- Molecular Weight:632.68
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[1]|
CDK4 |
RNF126 |
In Vitro
EST1027 modifies cysteine 32 of RNF126[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:C33A cells
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Concentration:3 μM (24 h); 5 μM (after 1 h BTZ pretreatment); 5 μM (24 h)
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Incubation Time:24 h (3 μM); 1 h (BTZ pretreatment for 5 μM); 24 h (5 μM)
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Result:Reduced CDK4 levels by >50% in C33A cells at 3 μM after 24 h but did not reduce CDK6.
At 5 μM for 24 h, CDK4 was also reduced.
BTZ pretreatment attenuated CDK4 degradation, indicating proteasome dependence.
RNF126 knockdown completely attenuated CDK4 degradation.
RNF126 levels were also reduced.
Chemical Information
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CAS No. 3036530-23-8
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Molecular Weight 632.68
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Formula C33H35F3N8O2
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SMILES
O=C(C1=CC2=CN=C(NC3=NC=C(N4CCN(C(/C=C/C5=CC=C(C(F)(F)F)C=C5)=O)CC4)C=C3)N=C2N1C6CCCC6)N(C)C
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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)