Cas No.: | 1997319-84-2 |
Chemical Name: | SGC-SMARCA-BRDVIII |
Synonyms: | SGC-SMARCA-BRDVIII; SGCSMARCABRDVIII; SGC SMARCA BRDVIII; |
SMILES: | O=C(N1CCN(C2=CC(C3=CC=CC=C3O)=NN=C2N)CC1)OC(C)(C)C |
Formula: | C19H25N5O3 |
M.Wt: | 371.43 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Publication: | [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. |
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]. |
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. |