709002-46-0
Chemical Structure
SirReal2
- CAS No.: 709002-46-0
- Formula:C22H20N4OS2
- Molecular Weight:420.55
IUPAC Name: 2-((4,6-dimethylpyrimidin-2-yl)thio)-N-(5-(naphthalen-1-ylmethyl)thiazol-2-yl)acetamide
InChIKey: MENNDDDTIIZDDN-UHFFFAOYSA-N
SMILES: O=C(NC1=NC=C(CC2=C3C=CC=CC3=CC=C2)S1)CSC4=NC(C)=CC(C)=N4
Biological Activity: SirReal2 is a potent, isotype-selective Sirt2 inhibitor with an IC50 value of 140 nM and has very little effect on the activities of Sirt3-5. SirReal2 leads to tubulin hyperacetylation in HeLa cells and induces destabilization of the checkpoint protein BubR1. SirReal2 combined with VS-5584 (HY-16585) suppresses tumor growth and extends the survival rate of mice in tumor xenograft model. SirReal2 is is promising for research of cancer, inflammation and neurodegeneration[1][2][3][4].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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SirReal2 | 99.0% | SirReal2 is a potent, isotype-selective Sirt2 inhibitor with an IC50 value of 140 nM and has very little effect on the activities of Sirt3-5. SirReal2 leads to tubulin hyperacetylation in HeLa cells and induces destabilization of the checkpoint protein BubR1. SirReal2 combined with VS-5584 (HY-16585) suppresses tumor growth and extends the survival rate of mice in tumor xenograft model. SirReal2 is is promising for research of cancer, inflammation and neurodegeneration. | ||||||||||||||||||||
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SirReal2 (Standard) | 99.80% | SirReal2 (Standard) is the analytical standard of SirReal2 (HY-100591). This product is intended for research and analytical applications. SirReal2 is a potent, isotype-selective Sirt2 inhibitor with an IC50 value of 140 nM and has very little effect on the activities of Sirt3-5. SirReal2 leads to tubulin hyperacetylation in HeLa cells and induces destabilization of the checkpoint protein BubR1. SirReal2 combined with VS-5584 (HY-16585) suppresses tumor growth and extends the survival rate of mice in tumor xenograft model. SirReal2 is is promising for research of cancer, inflammation and neurodegeneration. | ||||||||||||||||||||
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References
- [1]. Rumpf T, et al. Selective Sirt2 inhibition by ligand-induced rearrangement of the active site. Nat Commun. 2015 Feb 12;6:6263. [Content Brief]
- [2]. Schiedel M, et al. Structure-Based Development of an Affinity Probe for Sirtuin 2. Angew Chem Int Ed Engl. 2016;55(6):2252-2256. [Content Brief]
- [3]. Luo Y, et al. SIRT2 inhibitor SirReal2 enhances anti-tumor effects of PI3K/mTOR inhibitor VS-5584 on acute myeloid leukemia cells. Cancer Med. 2023 Sep;12(18):18901-18917. [Content Brief]
- [4]. Zhang M, et al. SIRT2 promotes murine melanoma progression through natural killer cell inhibition. Sci Rep. 2021 Jun 21;11(1):12988. [Content Brief]
