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A-366

Item № 16081
CAS № 1527503-11-2
Purity ≥98%
product image
                (CAS 1527503-11-2)
SIZE PRICE QUANTITY SUBTOTAL
CART TOTAL
     5 mg $68.00 0.00
     10 mg $129.00 0.00
     50 mg $544.00 0.00

Pricing updated 2019-06-26. Prices are subject to change without notice.

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.

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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
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

Warning - this product is not for human or veterinary use.

Shipping & Storage
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
Stability
≥ 2 years
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Additional Information

View the Cayman Structure Database for chemical structure definitions for many Cayman products

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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 Research (2016).

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