详情描述
SirReal2 is a potent and selective Sirt2 inhibitor with IC50 ~140 nM, has minimal effect on Sirt1 and Sirt3-6. It occupies the extended C-site and induces a major rearrangement of Sirt2’s active site, so it selectively inhibits Sirt2 and functions as a molecular wedge to lock Sirt2 in an open conformation. SirReal2 can increase tubulin hyperacetylation in HeLa cells and induces destabilization of the checkpoint protein BubR1. It could be a useful chemical tool for sirtuin biology.
Product information
CAS Number: 709002-46-0
Molecular Weight: 420.55
Formula: C22H20N4OS2
Chemical Name: 2-((4,6-dimethylpyrimidin-2-yl)thio)-N-(5-(naphthalen-1-ylmethyl)thiazol-2-yl)acetamide
Smiles: CC1C=C(C)N=C(N=1)SCC(=O)NC1=NC=C(CC2=CC=CC3=CC=CC=C23)S1
InChiKey: MENNDDDTIIZDDN-UHFFFAOYSA-N
InChi: 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)
Technical Data
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO up to 100 mM
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥360 days if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
In Vitro:
SirReal2 was used at 10-20 μ M final concentration in vitro and in cellular assays.
References:
- Rumpf T, et al. Selective Sirt2 inhibition by ligand-induced rearrangement of the active site. (2015) Nat Commun. 6:6263.
Products are for research use only. Not for human use.