K2-B4-3e
K2-B4-3e is a BRD4 PROTAC degrader with a DC50 of 66 nM. K2-B4-3e binds to KLHDC2 to form a ternary complex with BRD4, inducing degradation dependent on the ubiquitin-proteasome system. K2-B4-3e is applicable for cancer-related research.
(Pink: BRD4 Target protein ligand; Blue: KLHDC2 ligand (HY-78695); Black: linker).
For research use only. We do not sell to patients.
- Formula: C53H64ClN9O7S
- Molecular Weight:1006.65
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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
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BRD4 66 nM (DC50) |
K2-B4-3e (0.000001-10 μM; 6 h) induces partial degradation of endogenous HiBiT-BRD4 in PC-3 cells, with a DC50 of 66 nM and a maximum degradation rate of 62% after 6 h[1].
K2-B4-3e (4 h) promotes the degradation of BRD family proteins in SKBR3 and U2OS cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Molecular Weight 1006.65
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Formula C53H64ClN9O7S
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SMILES
CCC(C1=CC2=C(N(C1=O)C3=CN(C(C=C3)=O)CC(OC)=O)CN(CC2)C(OCCC4CCN(CC4)CC5CCN(CC5)C(C[C@@H]6N=C(C7=C(N8C(C)=NN=C68)SC(C)=C7C)C9=CC=C(C=C9)Cl)=O)=O)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
[1]. Hickey CM, et al. Co-opting the E3 ligase KLHDC2 for targeted protein degradation by small molecules. Nature structural & molecular biology. 2024 Feb;31(2):311-322. [Content Brief]
[2]. Scott DC, et al. Principles of paralog-specific targeted protein degradation engaging the C-degron E3 KLHDC2. Nature communications. 2024 Oct 12;15(1):8829. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
K2-B4-3e Related Classifications
HY-157561 Related Classifications
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