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Histone Methytransferase

A-366 (1527503-11-2)

A-366 is a potent and selective G9a/GLP histone lysine methyltransferase inhibitor (IC₅₀ = 3.3 nM). It displays >1000-fold selectivity for G9a/GLP over 21 other methyltransferases. A-366 has been shown to inhibit H3K9 methylation in prostate cancer PC3 cells with an IC₅₀ of 100 nM.

Not Intended for Therapeutic Use. For research use only.

CAS: 1527503-11-2 Category

A-366 (1527503-11-2) Description

A-366 is a potent, peptide-competitive inhibitor of the lysine methyltransferase G9a (IC50 = 3.3 nM). It displays greater than 1,000-fold selectivity over 21 other methyltransferases. 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. It also blocks the interaction of the methyl lysine reader protein Spindlin1 with H3K4me3 by binding with a Spindlin1 Tudor domain (Kd = 111 nM).

 

A-366 (1527503-11-2) Specifications

Product Name A-366
Synonyms A 366; A366.
Chemical Name 5′-methoxy-6′-(3-pyrrolidin-1-ylpropoxy)spiro[cyclobutane-1,3′-indole]-2′-amine
Drug Class Inhibitor
Purity >98%
CAS Number 1527503-11-2
Molecular Formula C19H27N3O2
Molecular Weight 329.444 g/mol
Monoisotopic Mass 329.21 g/mol
MDL number MFCD28133403
InChIKey BKCDJTRMYWSXMC-UHFFFAOYSA-N
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)
SMILES COC1=C(C=C2C(=C1)C3(CCC3)C(=N2)N)OCCCN4CCCC4
Form Powder
Color white to beige
Solubility  DMSO: 10 mg/mL
Storage Temp.  Dry, dark and at 0 – 4 C for short term (days to weeks) or -20 C for long term (months to years).
Shelf life >3 years if stored properly
Handling Protect from air and light
Application G9a/GLP inhibitor

 


RIDADR NONH for all modes of transport

References:

  • 1.Inhibition of the G9a/GLP histone methyltransferase complex modulates anxiety-related behavior in mice. Wang DY, Kosowan J, Samsom J, Leung L, Zhang KL, Li YX, Xiong Y, Jin J, Petronis A, Oh G, Wong AHC. Acta Pharmacol Sin. 2018 May;39(5):866-874. doi: 10.1038/aps.2017.190. Epub 2018 Feb 8.
  • 2.CsrB, a noncoding regulatory RNA, is required for BarA-dependent expression of biocontrol traits in Rahnella aquatilis HX2. Mei L, Xu S, Lu P, Lin H, Guo Y, Wang Y. PLoS One. 2017 Nov 1;12(11):e0187492. doi: 10.1371/journal.pone.0187492. eCollection 2017.
  • 3.Isolation and Tissue Distribution of an Insulin-Like Androgenic Gland Hormone (IAG) of the Male Red Deep-Sea Crab, Chaceon quinquedens. Lawrence A, Green S, Chung JS. Mar Drugs. 2017 Aug 1;15(8). pii: E241. doi: 10.3390/md15080241.
  • 4.Largely Improved Near-Infrared Silicon-Photosensing by the Piezo-Phototronic Effect. Dai Y, Wang X, Peng W, Zou H, Yu R, Ding Y, Wu C, Wang ZL. ACS Nano. 2017 Jul 25;11(7):7118-7125. doi: 10.1021/acsnano.7b02811. Epub 2017 Jul 13.
  • 5.Characterization of occult hepatitis B virus infection among HIV positive patients in Cameroon. Gachara G, Magoro T, Mavhandu L, Lum E, Kimbi HK, Ndip RN, Bessong PO. AIDS Res Ther. 2017 Mar 8;14(1):11. doi: 10.1186/s12981-017-0136-0.