K2-B4-5e
K2-B4-5e is a BRD4 PROTAC degrader with a DC50 of 6.2 nM. K2-B4-5e triggers the degradation of BRD4 and BRD2 mediated by KLHDC2 in a ubiquitin-proteasome system-dependent manner. K2-B4-5e induces BRD4 degradation in mouse cells. K2-B4-5e can be used in research related to prostate cancer, breast cancer and osteosarcoma.
(Pink: BRD4 ligand (HY-78695); Blue: KLHDC2 E3 ligase ligand; Black: linker).
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- CAS No.: 3093556-90-9
- Formule: C52H49ClN8O6S
- Masse moléculaire:949.51
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
[1]|
BRD4 6.2 nM (DC50) |
BRD2 |
In Vitro
K2-B4-5e (0.000001-10 μM; 2-6 h) potently degrades HiBiT-tagged endogenous BRD4 in CRISPR-edited cells with a DC50 of 6.2 nM and 93% maximal degradation at 6 hours, and this degradation is dependent on the ubiquitin-proteasome system and KLHDC2[1].
K2-B4-5e degrades endogenous BRD2 in cell lines, and this degradation is dependent on KLHDC2 but not DCAF16[1].
K2-B4-5e (1 μM; 24 h) degrades HiBiT-BRD4 in mouse A20 cells, demonstrating cross-species activity consistent with high KLHDC2 sequence conservation between mice and humans[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. 3093556-90-9
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Masse moléculaire 949.51
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Formule C52H49ClN8O6S
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SMILES
O=C(C[C@@H]1N=C(C2=C(N3C(C)=NN=C13)SC(C)=C2C)C4=CC=C(C=C4)Cl)NC5=CC=C(C=C5)C6=CC=C(C=C6)C(N7CCC8=C(N(C(C(CC(C)C)=C8)=O)C9=CN(C(C=C9)=O)CC(OC)=O)C7)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[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-B4-5e Related Classifications
HY-157491 Related Classifications
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