EX527 Chemical Properties

Boiling point:

531.7±38.0 °C(Predicted)

Density 

1.388

storage temp. 

Store at -20°C

solubility 

Soluble in DMSO

pka

16.12±0.40(Predicted)

form 

Powder

color 

Light yellow to yellow

EX527 Usage And Synthesis

Uses

(S)-Selisistat ((S)-EX-527) is a potent and selective SIRT1 inhibitor, with an IC50 of 98 nM.

Definition

ChEBI: (S)-selisistat is a 6-chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide that has S configuration It is the active enantiomer. It has a role as a Sir1 inhibitor. It is an enantiomer of a (R)-selisistat.

in vivo

IC 50

SIRT1: 98 nM (IC₅₀)

References

[1] Solomon JM, et al. Inhibition of SIRT1 catalytic activity increases p53 acetylation but does not alter cell survival following DNA damage. Mol Cell Biol. 2006 Jan;26(1):28-38. DOI:10.1128/MCB.26.1.28-38.2006
[2] Jia Y, et al. SIRT1 is a regulator in high glucose-induced inflammatory response in RAW264.7 cells. PLoS One. 2015 Mar 20;10(3):e0120849. DOI:10.1371/journal.pone.0120849
[3] Wang X, et al. Resveratrol attenuates microvascular inflammation in sepsis via SIRT-1-Induced modulation of adhesion molecules in ob/ob mice. Obesity (Silver Spring). 2015 Jun;23(6):1209-17. DOI:10.1002/oby.21086
[4] Napper AD, et al. Discovery of indoles as potent and selective inhibitors of the deacetylase SIRT1. J Med Chem. 2005 Dec 15;48(25):8045-54. DOI:10.1021/jm050522v

EX527(848193-68-0)Related Product Information

• Aluminum oxide
• 6-CHLORO-2,3,4,9-TETRAHYDRO-1H-CARBAZOLE-1-CARBOXAMIDE
• EX-527 (R-enantioMer)