Chemical Structure : BRD4 PROTAC 6b
CAS No.:
BRD4 PROTAC 6b
Catalog No.: PC-22990Not For Human Use, Lab Use Only.
BRD4 PROTAC 6b is a potent, specific PROTAC degrader of BRD4 protein, suppresses BLBC cell growth by targeting BRD4, but not BRD2 and BRD3, for cereblon (CRBN)-mediated ubiquitination and proteasomal degradation.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
BRD4 PROTAC 6b is a potent, specific PROTAC degrader of BRD4 protein, suppresses BLBC cell growth by targeting BRD4, but not BRD2 and BRD3, for cereblon (CRBN)-mediated ubiquitination and proteasomal degradation.
Compound 6b (0.1 μM) induced time-dependent BRD4 degradation and degraded most BRD4 protein within 12 hours.
Compound 6b effectively inhibit multiple BLBC cell lines, with a marked decline in KLF5, c-Myc, SKP2, Bcl-2, and Bcl-XL levels, and increased levels of Bim, p21, and p27.
Compound 6b causes growth inhibition and cell cycle arrest in BLBC cell lines.
Compound 6b promotes BRD4 ubiquitination and degradation dependent on CRBN
Compound 6b significantly suppressed HCC1806 xenograft and UM1 patient-derived xenograft tumor growth in nude mice.
Physicochemical Properties
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M.Wt
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708.68
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Formula
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C37H30F2N6O7
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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N-(4-(2,3-difluorophenoxy)-3-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)phenyl)-4-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)butanamide
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References
1. Yanjie Kong, et al. Oncogene. 2024 Aug 20. doi: 10.1038/s41388-024-03121-1.
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