Chemical Structure : YTHu78
CAS No.:
YTHu78
Catalog No.: PC-24854Not For Human Use, Lab Use Only.
YTHu78 is a potent, selective CRBN ligand-based KDM5B PROTAC degrader, effectively induce KDM5B degradation in MV-4-11 and MM.1S cell lines, exhibits comparable degradation efficacy toward KDM5B and KDM5A.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
YTHu78 is a potent, selective CRBN ligand-based KDM5B PROTAC degrader, effectively induce KDM5B degradation in MV-4-11 and MM.1S cell lines, exhibits comparable degradation efficacy toward KDM5B and KDM5A.
YTHu78 effectively induces KDM5B protein degradation at a concentration of 0.74 μM in MV-4-11 cell line using Western blot analysis, YTHu78 depletes KDM5B in a time-dependent manner, with maximal degradation achieved after 12 h of treatment at a concentration of 5 μM.
YTHu78 utilizes a CRBN-mediated proteasome pathway for KDM5B degradation.
YTHu78 treatment induces apoptosis in MV-4-11 cells.
YTHu78 exhibits notable antiproliferative activity in HL60, MM.1S (IC50=1.036 uM), and OCI-AML3 cell lines.
Physicochemical Properties
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M.Wt
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632.64
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Formula
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C33H28N8O6
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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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2-(2,6-dioxopiperidin-3-yl)-4-((3-(4-((4-((4-oxo-3,4-dihydropyrido[3,4-d]pyrimidin-2-yl)oxy)-1H-pyrazol-1-yl)methyl)phenyl)propyl)amino)isoindoline-1,3-dione
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References
1. Xiaowen Liu, et al. Eur J Med Chem. 2025 Jun 19:296:117883.
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