SirReal1-O-propargyl (Synonyms: PROTAC Sirt2-binding moiety 1)

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SirReal1-O-propargyl is a selective and highly potent Sirtuin 2 (Sirt2) inhibitor, with an IC₅₀ of 2.4 μM. SirReal1-O-propargyl, the SirReal1-based moiety, binds to the cereblon ligand via a linker to form PROTAC to degrade Sirt2. SirReal1-O-propargyl is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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SirReal1-O-propargyl Chemical Structure

CAS No. : 1862237-99-7

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Description	SirReal1-O-propargyl is a selective and highly potent Sirtuin 2 (Sirt2) inhibitor, with an IC₅₀ of 2.4 μM. SirReal1-O-propargyl, the SirReal1-based moiety, binds to the cereblon ligand via a linker to form PROTAC to degrade Sirt2^[1]. SirReal1-O-propargyl is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
IC₅₀ & Target	IC50: 2.4 μM (Sirt2)^[1].
Molecular Weight	424.54
Formula	C₂₁H₂₀N₄O₂S₂
CAS No.	1862237-99-7
Appearance	Solid
Color	White to yellow
SMILES	O=C(NC1=NC=C(CC2=CC=CC(OCC#C)=C2)S1)CSC3=NC(C)=CC(C)=N3
Shipping	Room temperature in continental US; may vary elsewhere.
Storage	4°C, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Purity & Documentation	Data Sheet (266 KB) Handling Instructions (2659 KB)
References	[1]. Schiedel M, et al. Chemically Induced Degradation of Sirtuin 2 (Sirt2) by a Proteolysis Targeting Chimera (PROTAC) Based on Sirtuin Rearranging Ligands (SirReals). J Med Chem. 2018 Jan 25;61(2):482-491. [Content Brief]

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Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SirReal1-O-propargyl1862237-99-7PROTAC Sirt2-binding moiety 1Ligands for Target Protein for PROTACTarget Protein-binding MoietyInhibitorinhibitorinhibit

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SirReal1-O-propargyl (Synonyms: PROTAC Sirt2-binding moiety 1)

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