| Identification | Back Directory | [Name]
1-Piperazinecarboxylic acid, 4-[3-amino-6-(2-hydroxyphenyl)-4-pyridazinyl]-, 1,1-dimethylethyl ester | [CAS]
1997319-84-2 | [Synonyms]
SGC-SMARCA-BRDVIII
1-Piperazinecarboxylic acid, 4-[3-amino-6-(2-hydroxyphenyl)-4-pyridazinyl]-, 1,1-dimethylethyl ester | [Molecular Formula]
C19H25N5O3 | [MOL File]
1997319-84-2.mol | [Molecular Weight]
371.43 |
| Chemical Properties | Back Directory | [Boiling point ]
599.6±50.0 °C(Predicted) | [density ]
1.270±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 25 mg/mL (67.31 mM; ultrasonic and warming and heat to 60°C) | [form ]
Solid | [pka]
8.82±0.51(Predicted) | [color ]
Off-white to yellow |
| Hazard Information | Back Directory | [Uses]
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]. | [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. |
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