A SIRT1 inhibitor
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(±)-EX-527

Item No. 10009798

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
6-chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide
CAS Number
49843-98-3
Molecular Formula
C13H13ClN2O
Formula Weight
248.7
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMSO: 20 mg/mlDMSO:PBS(pH7.2) (1:1): 0.5 mg/mlEthanol: 5 mg/ml
λmax
233, 291 nm
SMILES
ClC(C=C1)=CC2=C1NC3=C2CCCC3C(N)=O
InChi Code
InChI=1S/C13H13ClN2O/c14-7-4-5-11-10(6-7)8-2-1-3-9(13(15)17)12(8)16-11/h4-6,9,16H,1-3H2,(H2,15,17)
InChi Key
FUZYTVDVLBBXDL-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $36

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    10 mg

    $68

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    25 mg

    $153

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    50 mg

    $288

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    Product Description

    EX-527 is an inhibitor of sirtuin 1 (SIRT1; IC50 = 0.098 µM).1 It is selective for SIRT1 over SIRT2, and SIRT3 (IC50s = 19.6 and 48.7 µM, respectively) and the cytochrome P450 (CYP) isoforms CYP3A4, CYP2D6, CYP2C9, CYP2C19, and CYP1A2 at 1 µM. EX-527 (50 µM) induces cell cycle arrest at the G1 phase in MCF-7 cells.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Napper, A.D., Hixon, J., McDonagh, T., et al. Discovery of indoles as potent and selective inhibitors of the deacetylase SIRT1. J. Med. Chem. 48(25), 8045-8054 (2005).

    2. Peck, B., Chen, C.-Y., Ho, K.-K., et al. SIRT inhibitors induce cell death and p53 acetylation through targeting both SIRT1 and SIRT2. Mol. Cancer Ther. 9(4), 844-855 (2010).