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SirReal2
产品别名
709002-46-0
SirReal2
2-(4,6-Dimethyl-pyrimidin-2-ylsulfanyl)-N-(5-naphthalen-1-ylmethyl-thiazol-2-yl)-acetamide
SirReal 2
结构式
基本信息
Empirical Formula【经验(实验)分子式】 | C22H20N4OS2 |
Molecular weight | 420.55 |
PubChem Substance ID【PubChem化学物质编号】 | 329825931 |
NACRES | NA.77 |
Application【应用】 | Sirtuin-rearranging ligand 2 (SirReal2) has been used as a positive control to evaluate in vivo sirtuin 2 (SIRT2) inhibition by RK-9123016 and NPD11033. |
Biochem/physiol Actions【生化/生理作用】 | SirReal2 is a potent and selective inhibitor of Sirt2, an NAD-dependent lysine deacetylase that has been implicated in the pathogenesis of cancer, inflammation, and neurodegeneration. SirReal2 has an IC50 value of 140 nM and is >1000-fold selective for Sirt2 over Sirt1 and Sirt3. SirReal2 is believed to act through a ligand-induced structural rearrangement of the active site, binding at an adjacent pocket to lock Sirt2 in an open conformation. SirReal2 caused to tubulin hyperacetylation in HeLa cells and destabilization of the checkpoint protein BubR1, consistent with Sirt2 inhibition. |
产品性质
Quality Level【质量水平】 | 100 |
Assay【测定】 | ≥98% (HPLC) |
form【形式】 | powder |
color【颜色】 | white to beige |
solubility【溶解性】 | DMSO: 20 mg/mL, clear |
storage temp.【储存温度】 | −20℃ |
SMILES string | CC1=NC(SCC(NC2=NC=C(S2)CC3=CC=CC4=C3C=CC=C4)=O)=NC(C)=C1 |
InChI | 1S/C22H20N4OS2/c1-14-10-15(2)25-22(24-14)28-13-20(27)26-21-23-12-18(29-21)11-17-8-5-7-16-6-3-4-9-19(16)17/h3-10,12H,11,13H2,1-2H3,(H,23,26,27) |
InChI key | MENNDDDTIIZDDN-UHFFFAOYSA-N |
packaging【包装】 | 5, 25 mg in glass bottle |
安全信息
Storage Class Code【储存分类代码】 | 13 - Non Combustible Solids |
WGK | WGK 3 |