AH081
AH081 is a CK1δ/ε PROTAC degrader. AH081 serves as the negative control of AH078 (HY-170859). AH081 exhibits inhibitory activity but no degradative activity against CK1δ/ε by using an inactive stereoisomer of the VHL ligand.
(Pink: CK1δ and CK1ε ligand (HY-148251); Blue: VHL ligand (HY-125845B); Black: linker).
For research use only. We do not sell to patients.
- Formula: C51H60F2N10O5S
- Molecular Weight:963.15
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
IC50 & Target
[1]|
CK1δ |
CK1ε |
In Vitro
AH081 (compound 38) (1-20 μM; 6 h) does not induce degradation of CK1α, CK1δ, or CK1ε in HEK293 cells at concentrations up to 20 μM, but exhibits enzymatic inhibition of CK1δ/ε at concentrations >3 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK293 cells
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Concentration:1-20 μM
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Incubation Time:6 h
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Result:Did not induce degradation of CK1δ, CK1ε, or CK1α at concentrations of 1, 3, 10, and 20 μM.
Caused dephosphorylation of DVL3 and phosphorylated VANGL2 at concentrations >3 μM.
Upregulated CK1δ and CK1ε protein levels at concentrations >3 μM.
Chemical Information
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Molecular Weight 963.15
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Formula C51H60F2N10O5S
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SMILES
O=C(NCC1=CC=C(C=C1)C2=C(N=CS2)C)[C@H]3N(C[C@H](C3)O)C([C@H](C(C)(C)C)NC(CCCCCCC(N4CCC(F)(CC4)CN5C(C6=C7C(NC=C7)=NC=C6)=C(N=C5)C8=NC=C(C=C8)F)=O)=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)
AH081 Related Classifications
HY-170859A Related Classifications
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