SirReal1-O-propargyl

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.

Product information

CAS Number: 1862237-99-7

Molecular Weight: 424.54

Formula: C21H20N4O2S2

Synonym:

PROTAC Sirt2-binding moiety 1

Chemical Name: 2-[(4, 6-dimethylpyrimidin-2-yl)sulfanyl]-N-(5-{[3-(prop-2-yn-1-yloxy)phenyl]methyl}-1, 3-thiazol-2-yl)acetamide

Smiles: CC1C=C(C)N=C(N=1)SCC(=O)NC1=NC=C(CC2=CC(=CC=C2)OCC#C)S1

InChiKey: ISDMLEKZQIHDDE-UHFFFAOYSA-N

InChi: InChI=1S/C21H20N4O2S2/c1-4-8-27-17-7-5-6-16(10-17)11-18-12-22-20(29-18)25-19(26)13-28-21-23-14(2)9-15(3)24-21/h1,5-7,9-10,12H,8,11,13H2,2-3H3,(H,22,25,26)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO.

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

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.

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