Protein Inhibitors - EX 527 (CAS: 49843-98-3)

EX 527 (CAS: 49843-98-3)

Catalog #：EBC51040

Biological Activity

Synonyms

EX-527, SEN0014196, Selisistat

Chemical Name

6-Chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide

Application

EX 527 is a potent inhibitor of the SIRT1 class III histone deacetylase enzyme, selective over SIRT2 and SIRT3.

CAS Number

49843-98-3

Purity

≥98.0%

Molecular Weight

248.71

Molecular Formula

C₁₃H₁₃ClN₂O

SMILES

O=C(C1C(NC2=C3C=C(Cl)C=C2)=C3CCC1)N

Target & IC50

SIRT1: IC50 = 98 nM
SIRT2: IC50 = 19.6 μM
SIRT3: IC50 = 48.7 μM

Shipping

Gel Pack

Storage

Store at 4° C

Preparing Stock Solutions

Molecular Structure

ConcentrationSolventMass	1 mg	5 mg	10 mg
1 mM	4.0211 ml	20.1037 ml	40.2075 ml
5 mM	0.8042 ml	4.0207 ml	8.0415 ml
10 mM	0.4021 ml	2.0104 ml	4.0208 ml
50 mM	0.0804 ml	0.4021 ml	0.8042 ml

Solubility
DMSO: 49 mg/mL (197.02 mM) Ethanol: 30 mg/mL (120.62 mM)

Product Description

Selisistat (EX-527) is an inhibitor of SIRT1 enzymatic activity (IC50, 98 nM), identified in a high-throughput screen using bacterially expressed human SIRT1. Selisistat (EX-527) inhibits SIRT1 in a concentration-dependent manner with an IC50 of 38 nM, in agreement with the activity on bacterially expressed SIRT1. Selisistat (EX-527) has much lower potency against SIRT2 (IC50, 19.6 μM) or SIRT3 (IC50, 48.7 μM) but does not inhibit class I/II HDAC activity at concentrations up to 100 μM. Selisistat (EX-527) exerts an inhibitory effect on SIRT1 activity without affecting SIRT1 expression on both mRNA and protein levels.