PROTAC SMARCA2/4 degrader-27
PROTAC SMARCA2/4 degrader-27 is a VHL-recruiting PROTAC degrader targeting SMARCA2 and SMARCA4, derived from structure-guided modification of PROTAC SMARCA2/4 degrader-28 (HY-162835). PROTAC SMARCA2/4-degrader-27 forms a cooperative ternary complex with CRL2VHL E3 ligase to induce ubiquitination and degradation. PROTAC SMARCA2/4-degrader-27 induces a novel protein-protein interaction between VHL and SMARCA2/SMARCA4, thereby stabilizing ternary complex formation and promoting proteasomal degradation of target proteins. PROTAC SMARCA2/4-degrader-27 exhibits enhanced cell permeability and stronger ternary complex formation ability, leading to improved degradation activity. PROTAC SMARCA2/4-degrader-27 can be used in cancer-related research[1].
(Pink: SMARCA2 and SMARCA4 ligand (HY-44012); Blue: VHL ligand (HY-125905); Black: linker (HY-159678)).
For research use only. We do not sell to patients.
- CAS No.: 2375564-54-6
- Formula: C49H58FN9O6S
- Molecular Weight:920.10
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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
Biological Activity
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SMARCA2 |
SMARCA4 |
PROTAC SMARCA2/4 degrader-27 (PROTAC 2) forms a stable ternary complex with the purified SMARCA2 bromodomain and CRL2VHL E3 ligase, which is characterized by linker-mediated π-stacking interaction with VHL Y98 and a well-defined buried interface surface area[1].
PROTAC SMARCA2/4 degrader-27 forms a stable ternary complex with the purified SMARCA4 bromodomain and CRL2VHL E3 ligase, which is similar to its binding mode with SMARCA2, and maintains the linker-mediated π-stacking interaction with VHL Y98[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2375564-54-6
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Molecular Weight 920.10
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Formula C49H58FN9O6S
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SMILES
O=C(C1(CC1)F)N[C@@H](C(C)(C)C)C(N2[C@@H](C[C@H](C2)O)C(NCC3=C(C=C(C4=C(C)N=CS4)C=C3)OCCC5=CC=C(C=C5)CN6CCN(C7=C(N)N=NC(C8=C(C=CC=C8)O)=C7)CC6)=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)
PROTAC SMARCA2/4 degrader-27 Related Classifications
HY-162834 Related Classifications
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