SRT1720, inhibitor

SRT1720

Cat. Num. AAA575261

• Purity: 99.93%
• Synonyms: SRT1720; SRT 1720 Hydrochloride; inhibitor

• Purity/Purification: 99.93%
• Form/Format: POWDER

• CAS: 1001645-58-4
• Formula: C25H24ClN7OS
• Solubility: DMSO 36 mg/ml (71.1 mM); Ethanol <1 mg/mL ; Water <1mg/mL
• Receptor (IC50): SIRTl 0.16 uM(EC50)
• Biological Activity: SRT1720 hydrochloride is a selective activator of human SIRTI.
• Smiles: Cl.O=C(Nc1ccccc1-c1cn2c(CN3CCNCC3)csc2n1)c1cnc2ccccc2n1
• Kinase Assay: SIRTI- fluorescence polarization assay: In the SIRT1 FP assay, SIRT1 activity ismonitored using a 20 amino acid peptide (Ac-Glu-Glu-Lys(biotin)-Gly-Gln-Ser-Thr-Ser-Ser-His-Ser-Lys(Ac)-Nle-Ser-Thr-Glu-Gly-Lys(MRL2l- or Tamra)-Glu-Glu-NH2)derived from the sequence of p53. The peptide is N-terminally linked to biotin andC-terminally modified with a fluorescent tag. The reaction for monitoring enzymeactivity is a coupled enzyme assaywhere the first reaction is the deacetylationreaction catalyzed by SIRT1 and the second reaction is cleavage by trypsin at thenewly exposed lysine residue. The reaction is stopped and streptavidin is added inorder to accentuate the mass differences between substrate and product. Thesensitivity of the FP assay allows identification of SRT1720. The fluorescencepolarization reaction conditions are as follows: 0.5 prM peptide substrate, 150 prMBNAD+, 0-10 nM SIRTL, 25 mM Tris-acetate pH 8, L37 mM Na-Ac, 2.7 mM K-Ac, lmMMg-Ac,0.05%o Twben-20,0.t%o Pluronic FL27,l-0 mM CaCl2,5 mM DTT,0.025%BSA, and 0.15 mM nicotinamide. The reaction is incubated at 37°C and stopped byaddition of nicotinamide, and trypsin is added to cleave the deacetylated substrate.This reaction is incubated at 37°C in the presence of L pM streptavidin. Fluorescentpolarization is determined at excitation (650 nm) and emission (680 nm)wavelengths.
• Cell Assay: Transwell Insert Assays are utilized to measure migration. In vitro angiogenesis isassessed by Matrigel capillary-like tube structure formation assay. For endothelialtube formation assay, human vascular endothelial cells (HUVECs) are obtained from Clonetics and maintained in endothelial cell growth medium-2 containing 5% FBS. After three passages, HUVEC cell viability is measured with the trypan blue exclusion assay,and < 5% of cell death is observed with SRT1720 treatment.(Only for reference).
• Preparation and Storage: 2 years -80°C in solvent.; 3 years -20°C powder.

Structure