A potent inhibitor of G9a
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A-366

Item No. 16081

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)Epigenetic Chemical Probe Guide (PDF)
Technical Information
Formal Name
5'-methoxy-6'-[3-(1-pyrrolidinyl)propoxy]-spiro[cyclobutane-1,3'-[3H]indol]-2'-amine
CAS Number
1527503-11-2
Molecular Formula
C19H27N3O2
Formula Weight
329.4
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlEthanol: 30 mg/mlEthanol:PBS(pH 7.2) (1:1): 0.5 mg/ml
λmax
222, 283 nm
SMILES
NC1=NC2=CC(OCCCN3CCCC3)=C(OC)C=C2C14CCC4
InChi Code
InChI=1S/C19H27N3O2/c1-23-16-12-14-15(21-18(20)19(14)6-4-7-19)13-17(16)24-11-5-10-22-8-2-3-9-22/h12-13H,2-11H2,1H3,(H2,20,21)
InChi Key
BKCDJTRMYWSXMC-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $94

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    10 mg

    $174

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    50 mg

    $728

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    Product Description

    A-366 is a potent, peptide-competitive inhibitor of the lysine methyltransferase G9a (IC50 = 3.3 nM).1 It displays greater than 1,000-fold selectivity over 21 other methyltransferases.1 A-366 significantly reduces the cellular levels of dimethylation on histone 3 at lysine 9 (H3K9Me2) in PC3 cells without reducing total histone 3, H3K27Me3, or H3K36Me2.1 It also blocks the interaction of the methyl lysine reader protein Spindlin1 with H3K4me3 by binding with a Spindlin1 Tudor domain (Kd = 111 nM).2 See the Structural Genomics Consortium (SGC) website for more information.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Sweis, R.F., Pliushchev, M., Brown, P.J., et al. Discovery and development of potent and selective inhibitors of histone methyltransferase G9a. ACS Med. Chem. Lett. 5(2), 205-209 (2014).

    2. Wagner, T., Greschik, H., Burgahn, T., et al. Identification of a small-molecule ligand of the epigenetic reader protein Spindlin1 via a versatile screening platform. Nucleic Acids Res. (2016).