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SirReal2, Sirt2 Inhibitor

SirReal2, Sirt2 Inhibitor

$119.00
A potent and selective Sirt2 inhibitor.
Catalog No. Unit Price Qty
M60289-2s 2 mg solid $119.00
M60289-2 2 mg in DMSO $119.00

Details

Product Information
Molecular Weight: 420.55
Formula: C22H20N4OS2
Purity: ≥98%
CAS#: 709002-46-0
Solubility: DMSO up to 100 mM
Chemical Name: 2-((4,6-dimethylpyrimidin-2-yl)thio)-N-(5-(naphthalen-1-ylmethyl)thiazol-2-yl)acetamide
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

Biological Activity:

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.


How to use: 

In vitro: SirReal2 was used at 10-20 μ M final concentration in vitro and in cellular assays.
In vivo: n/a 

Reference:
  • 1. Rumpf T, et al. Selective Sirt2 inhibition by ligand-induced rearrangement of the active site. (2015) Nat Commun. 6:6263. 

SirReal2_spec.pdf      


Products are for research use only. Not for human use. 

Description

Details

Product Information
Molecular Weight: 420.55
Formula: C22H20N4OS2
Purity: ≥98%
CAS#: 709002-46-0
Solubility: DMSO up to 100 mM
Chemical Name: 2-((4,6-dimethylpyrimidin-2-yl)thio)-N-(5-(naphthalen-1-ylmethyl)thiazol-2-yl)acetamide
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

Biological Activity:

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.


How to use: 

In vitro: SirReal2 was used at 10-20 μ M final concentration in vitro and in cellular assays.
In vivo: n/a 

Reference:
  • 1. Rumpf T, et al. Selective Sirt2 inhibition by ligand-induced rearrangement of the active site. (2015) Nat Commun. 6:6263. 

SirReal2_spec.pdf      


Products are for research use only. Not for human use. 

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