Bioactivity | 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]. | ||||||||||||
Target | Kd: 35 nM (SMARCA2), 36 nM (SMARCA4), 13 nM (PB1(5)) | ||||||||||||
Invitro | SGC-SMARCA-BRDVIII (compound 22) (1 μM; 14 days) blocks adipocyte differentiation in 3T3-L1 murine fibroblasts[1]. | ||||||||||||
Name | SGC-SMARCA-BRDVIII | ||||||||||||
CAS | 1997319-84-2 | ||||||||||||
Formula | C19H25N5O3 | ||||||||||||
Molar Mass | 371.43 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [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. |