Chemical Structure : BBDDL2059
CAS No.:
2691174-27-1
BBDDL2059
(BBDDL 2059)
Catalog No.: PC-20858Not For Human Use, Lab Use Only.
BBDDL2059 (BBDDL 2059) is a potent, selective and covalent inhibitor of EZH2 with IC50 of 1.5 nM (EZH2-Y641F), targeting the Cys663 of EZH2.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
BBDDL2059 (BBDDL 2059) is a potent, selective and covalent inhibitor of EZH2 with IC50 of 1.5 nM (EZH2-Y641F), targeting the Cys663 of EZH2.
BBDDL2059 demonstrates excellent cellular potency with IC50 values of 0.064 and 0.022 μM in inhibition of KARPAS-422 and Pfeiffer cell growth, respectively.
BBDDL2059 shows no significant inhibitionagainst a panel of 10 methyltransferases at 10 uM, including DNA methyltransferase DNMT1, arginine methyltransferases (PRMT1, PRMT4, and PRMT5), and protein lysine methyltransferases (G9a, GLP, MLL1, and MLL4).
BBDDL2059 (0.05-1 uM) effectively reduced the H2K27me3 mark in a concentration- and time- dependent manner but had no effect on the total H3 and EZH2 in KARPAS-422 cells.
Physicochemical Properties
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M.Wt
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512.67
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Formula
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C27H36N4O4S
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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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O=C(NCC1=C(SC)C=C(C)NC1=O)C2=CC(CNC(C=C)=O)=CC(N(CC)C3CCOCC3)=C2C
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References
1. Yi Zhang, et al. Journal of Medicinal Chemistry, 2023
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