ChemicalBook CAS DataBase List 49843-98-3

49843-98-3

Name	6-CHLORO-2,3,4,9-TETRAHYDRO-1H-CARBAZOLE-1-CARBOXAMIDE
CAS	49843-98-3
Molecular Formula	C13H13ClN2O
MDL Number	MFCD03009471
Molecular Weight	248.71
MOL File	49843-98-3.mol

Synonyms

CS-1862 (S)-EX-527 Selisistat SEN0014196 EX 527, >=98% EX 527; EX527 EX 527 (Selisistat) EX 527 (SEN0014196) SIRT1 Inhibitor III Selisistat - EX 527 Selisistat (SEN0014196 SELISISTAT;EX 527;EX527;SEN0014196 EX-527; EX-527; EX-527; SELISISTAT. 6-CHLORO-2,3,4,9-TETRAHYDRO-1H-CARBAZOLE-1-CARBOXAMIDE 1H-Carbazole-1-carboxamide, 6-chloro-2,3,4,9-tetrahydro- 6-Chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide &gt (S)-6-chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide 6-CHLORO-2,3,4,9-TETRAHYDRO-1H-CARBAZOLE-1-CARBOXAMIDE, >95% 6-CHLORO-2,3,4,9-TETRAHYDRO-1H-CARBAZOLE-1-CARBOXAMIDE USP/EP/BP Selisistat 6-Chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxaMide 6-Chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide EX-527 Selisistat

Chemical Properties

Melting point	179.0 to 183.0 °C
Boiling point	531.7±38.0 °C(Predicted)
density	1.388
storage temp.	Store at +4°C
solubility	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 Data

Hazard Codes	Xn
Risk Statements	22-36 less more
Safety Statements	26 less more
RIDADR	UN 2811 6.1 / PGIII
WGK Germany	3
HS Code	2933998090

Hazard Information

Description

EX-527 (49843-98-3) is a selective SIRT1 inhibitor (IC50=98 nM). Does not inhibit other HDACs or SIRT family members. Increases p53 acetylation following DNA damage. Cell permeable.

Uses

A selective inhibitor of SIRT1 over SIRT2 and SIRT3

Definition

ChEBI: 6-chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide is a member of the class of carbazoles that is 2,3,4,9-tetrahydro-1H-carbazole which is substituted at position 1 by an aminocarbohyl group and at position 6 by a chlorine. It is a member of carbazoles, a monocarboxylic acid amide and an organochlorine compound.

General Description

A cell-permeable indole compound that acts as a potent and highly selective inhibitor of SIRT1 (IC₅₀ = 98 nM). It inhibits other sirtuin family deacetylases only at much higher concentrations (IC₅₀ = 19.6 and 48.7 μM for SIRT2 and SIRT3, respectively) and shows no inhibitory effect against class I and II HDACs or NAD glycohydrolase even at concentrations as high as 100 μM. Shown to be orally bioavailable with a serum half-life of 136 minutes in mice in vivo.

Biological Activity

Selective inhibitor of SIRT1 that does not inhibit histone deacetylase (HDAC) or other sirtuin deacetylase family members (IC 50 values are 98, 19600, 48700, > 100000 and > 100000 nM for SIRT1, SIRT2, SIRT3, HDAC and NADase respectively). Enhances p53 acetylation in response to DNA damaging agents.

Biochem/physiol Actions

Primary TargetSIRT1

storage

Store at +4°C

References

1) Napper et al. (2005), Discovery of indoles as potent and selective inhibitors of the deacetylase SIRT1; J. Med. Chem., 48 8045 2) Solomon et al. (2006) Inhibition of SIRT1 catalytic activity increases p53 acetylation but does not alter cell survival following DNA damage; Mol. Cell, 26 28 3) Gertz et al. (2013) EX-527 inhibits Sirtuins by exploiting their unique NAD+-dependent deacetylation mechanism; Proc. Natl. Acad. Sci. USA, 110 e2772

Spectrum Detail

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