Formulation: A solid
Formal Name: 4-[3-amino-6-(2-hydroxyphenyl)-4-pyridazinyl]-1-piperazinecarboxylic acid, 1,1-dimethylethyl ester
Purity: ≥98%
Formula Markup: C19H25N5O3
Formula Weight: 371,4
Shelf life (days): 1460
CAS Number: 1997319-84-2
Notes: SGC-SMARCA-BRDVIII is a pan-inhibitor of family VIII bromodomain-containing proteins (BRDs), which are components of switch/sucrose nonfermentable (SWI/SNF) chromatin remodeling complexes.{57472} It selectively binds to polybromo-1D (PBRM1) bromodomain 5, BRM, also known as SMARCA2, and BRG1, also known as SMARCA4 (Kds = 13, 35, and 36 nM, respectively), over PBRM1 bromodomain 2, PBRM1 bromodomain 3, and PBRM1 bromodomain 4 (Kds = 3,655, 1,963, and >10,000 nM, respectively). SGC-SMARCA-BRDVIII (1 µM) decreases lipid accumulation induced by the PPARγ agonist rosiglitazone (Item Nos. 71740 / 11884 / 71742) in 3T3-L1 mouse fibroblasts differentiated into adipocytes by a combination of the phosphodiesterase (PDE) inhibitor IBMX (Item No. 13347), the glucocorticoid dexamethasone (Item No. 11015), and insulin. It decreases expression of the genes encoding PPARγ, C/EBPα, and fatty acid binding protein 4 (FABP4), markers of adipocytes, in the same cells when used at a concentration of 0.5 µM. See the Structural Genomics Consortium (SGC) website for more information.
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