1-Piperazinecarboxylic acid, 4-[3-amino-6-(2-hydroxyphenyl)-4-pyridazinyl]-, 1,1-dimethylethyl ester

Biological Activity

SGC-SMARCA-BRDVIII is a potent and selective inhibitor of SMARCA2/4 and PB1(5), with Kds of 35 nM, 36 nM, and 13 nM, respectively. SGC-SMARCA-BRDVIII also inhibits PB1(2) and PB1(3), with Kds of 3.7 and 2.0 μM, respectively. SGC-SMARCA-BRDVIII can block adipogenesis of 3T3-L1 murine fibroblasts[1][2]. SGC-SMARCA-BRDVIII (compound 22) (1 μM; 14 days) blocks adipocyte differentiation in 3T3-L1 murine fibroblasts[1].

storage

Store at -20°C

References

[1]. Wanior M, et, al. Pan-SMARCA/PB1 Bromodomain Inhibitors and Their Role in Regulating Adipogenesis. J Med Chem. 2020 Dec 10;63(23):14680-14699. [2]. Mélin L, et, al. Design and Synthesis of LM146, a Potent Inhibitor of PB1 with an Improved Selectivity Profile over SMARCA2. ACS Omega. 2021 Aug 9;6(33):21327-21338.