Soluble in dimethyl sulfoxide, ethanol and dimethyl formamide.
form
powder
pka
16.12±0.40(Predicted)
color
white to beige
Stability
Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months
Safety Information
Symbol(GHS)
Signal word
Danger
Hazard statements
H301:Toxic if swalloed
H302:Harmful if swallowed
H319:Causes serious eye irritation
Precautionary statements
P264:Wash hands thoroughly after handling.
P264:Wash skin thouroughly after handling.
P301+P310:IF SWALLOWED: Immediately call a POISON CENTER or doctor/physician.
P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P337+P313:IF eye irritation persists: Get medical advice/attention.
Description
EX-527 is a potent and selective sirtuin 1 (SIRT1) inhibitor (IC50 38 nM) identified from a high throughput screen. EX-527 is more selective (200-500-fold) for SIRT1 than for SIRT2 or SIRT3 and has been shown to be a potent SIRT6 inhibitor using H3K56 deacetylation site based substrate. EX-527 does not inhibit class I/II HDAC activity at concentrations up to 100uM. Enhances p53 acetylation in response to DNA damaging agents. EX-527 is racemic; the active isomer (EX-243) gives similar results and potency whereas the other isomer (designated EX-242) is inactive.