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BBDDL2059

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

M.Wt 512.67
Formula C27H36N4O4S
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

O=C(NCC1=C(SC)C=C(C)NC1=O)C2=CC(CNC(C=C)=O)=CC(N(CC)C3CCOCC3)=C2C

References

1. Yi Zhang, et al. Journal of Medicinal Chemistry, 2023

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