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SGC-SMARCA-BRDVIII

Names

[ CAS No. ]:
1997319-84-2

[ Name ]:
SGC-SMARCA-BRDVIII

Biological Activity

[Description]:

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].

[Related Catalog]:

Research Areas >> Metabolic Disease
Signaling Pathways >> Epigenetics >> Epigenetic Reader Domain

[Target]

Kd: 35 nM (SMARCA2), 36 nM (SMARCA4), 13 nM (PB1(5))[1]


[In Vitro]

SGC-SMARCA-BRDVIII (compound 22) (1 μM; 14 days) blocks adipocyte differentiation in 3T3-L1 murine fibroblasts[1].

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C19H25N5O3

[ Molecular Weight ]:
371.43

[ Storage condition ]:
-20°C

Safety Information

[ Hazard Codes ]:
Xn


Related Compounds