PROTAC CCR9 Degrader 1
PROTAC CCR9 Degrader 1 is a PROTAC-based degrader targeting CCR9. PROTAC CCR9 Degrader 1 induces ubiquitination, proteasomal degradation of CCR9 and reduces intracellular CCR9 levels by recruiting the VHL E3 ligase. PROTAC CCR9 Degrader 1 has a Ki value of 78.0 nM against human CCR9. PROTAC CCR9 Degrader 1 modulates GPCR activity by binding to the intracellular allosteric binding site of CCR9. PROTAC CCR9 Degrader 1 can be used in research related to Crohn's disease.
(Pink: CCR9 ligand (HY-15724); Blue: VHL ligand (HY-125845); Black: linker (HY-W016735)).
For research use only. We do not sell to patients.
- Formula: C55H66ClN9O12S2
- Molecular Weight:1144.75
-
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]
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
All PROTACs Isoforms
More
Biological Activity
|
CCR9 78.0 nM (Ki) |
VHL |
PROTAC CCR9 Degrader 1 (compound 13) binds to the intracellular allosteric binding site (IABS) of CCR9 in live HEK293T cells, with a Ki value of 151 nM[1].
PROTAC CCR9 Degrader 1 (0.1-10000 nM) induces concentration-dependent degradation of cell surface CCR9 in HEK293T cells, reaching DCmax at 10 nM, with a hook effect occurring at concentrations >10 nM[1].
PROTAC CCR9 Degrader 1 exhibits selectivity for CCR9 over CCR2 and CCR7, with no cytotoxicity[1].
PROTAC CCR9 Degrader 1 (the PROTAC shown in Figure 8) moderately degrades CCR9 in cell-based assays, and exhibits excellent selectivity over CCR2 and CCR7[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:HEK293T cells
-
Concentration:0.1, 1, 10, 25, 100, 500, 1000, 2500 nM
-
Incubation Time:48 h
-
Result:Showed no cytotoxicity in cells.
Selectively induced a reduction in CCR9
levels, without affecting the levels of the related chemokine receptors CCR2 and CCR7.
Chemical Information
-
Molecular Weight 1144.75
-
Formula C55H66ClN9O12S2
-
SMILES
CC(N=CS1)=C1C(C=C2)=CC=C2CNC([C@@H]3C[C@@H](O)CN3C([C@@H](NC(COCC4=CN=NN4CCOCCOCCOC5=[N+]([O-])C=CC(C(C6=CC(Cl)=CC=C6NS(C7=CC=C(C(C)(C)C)C=C7)(=O)=O)=O)=C5)=O)C(C)(C)C)=O)=O
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[1]. Huber ME, et al. A Chemical Biology Toolbox Targeting the Intracellular Binding Site of CCR9: Fluorescent Ligands, New Drug Leads and PROTACs. Angew Chem Int Ed Engl. 2022;61(12):e202116782. [Content Brief]
[2]. Frost A, et al. Allosteric PROTACs: Expanding the Horizon of Targeted Protein Degradation. J Am Chem Soc. 2026;148(3):2823-2837. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PROTAC CCR9 Degrader 1 Related Classifications
HY-181287 Related Classifications
Powered by Bioz