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.
CAS Number: 709002-46-0
Molecular Weight: 420.55
Chemical Name: 2-((4,6-dimethylpyrimidin-2-yl)thio)-N-(5-(naphthalen-1-ylmethyl)thiazol-2-yl)acetamide
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: ≥12 months 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
SirReal2 was used at 10-20 μ M final concentration in vitro and in cellular assays.
- 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.
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