3093556-90-9
Chemical Structure
K2-B4-5e
- CAS No.: 3093556-90-9
- Formula:C52H49ClN8O6S
- Molecular Weight:949.51
InChIKey: OKMMCOVMIZQGDT-WBCKFURZSA-N
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
Biological Activity: 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[1][2].
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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. | |||||||||||||||||||||
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- [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]
Keywords
