SML1514
SirReal2
≥98% (HPLC)
동의어(들):
2-(4,6-Dimethyl-pyrimidin-2-ylsulfanyl)-N-(5-naphthalen-1-ylmethyl-thiazol-2-yl)-acetamide, SirReal 2
조직 및 계약 가격을 보려면 로그인를 클릭합니다.
크기 선택
보기 변경
제품정보 (DICE 배송 시 비용 별도)
실험식(Hill 표기법):
C22H20N4OS2
CAS 번호:
Molecular Weight:
420.55
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77
Quality Level
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 20 mg/mL, clear
storage temp.
−20°C
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
Application
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
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.
SirReal2 is a potent and selective inhibitor of Sirt2.
저장 등급
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Asad Ali Shah et al.
Biological & pharmaceutical bulletin, 39(10), 1739-1742 (2016-10-12)
SIRT2 is a member of the human sirtuin family of proteins and possesses nicotinamide adenine dinucleotide (NAD)-dependent lysine deacetylase activity. SIRT2 has been involved in various cellular processes including gene transcription, genome constancy, and the cell cycle. In addition, SIRT2
Norio Kudo et al.
Philosophical transactions of the Royal Society of London. Series B, Biological sciences, 373(1748) (2018-04-25)
SIRT2 is a member of the human sirtuin family of proteins and possesses NAD+-dependent lysine deacetylase/deacylase activity. SIRT2 has been implicated in carcinogenesis in various cancers including leukaemia and is considered an attractive target for cancer therapy. Here, we identified