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My Cart> Small Molecule Compounds > Inhibitors & Antagonists & Agonists > Epigenetics > A366CAS：1527503-11-2
Molecular Formula：C19H27N3O2
Molecular Weight：329.44
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：Light yellow to yellow Solid
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| CAS | 1527503-11-2 |
| Name | A366 |
| Molecular Formula | C19H27N3O2 |
| Molecular Weight | 329.44 |
| Solubility | Soluble in DMSO ≥5mg/mL(Need ultrasonic) |
| Purity | ≥98% |
| Appearance | Light yellow to yellow Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC | EINECS 808-907-0 |
| MDL | MFCD28133403 |
| SMILES | COC1=CC2=C(N=C(N)C23CCC3)C=C1OCCCN4CCCC4 |
| Target Point | Histone Methyltransferase |
| Passage | Epigenetics |
| Background | A-366 is a potent and selective G9a/GLP histone methyltransferase inhibitor. |
| Biological Activity | A-366 is a potent， highly selective， peptide-competitive histone methyltransferase G9a inhibitor with IC50s of 3.3 and 38 nM for G9a and GLP (EHMT1)， respectively. A-366 shows >1000-fold selectivity over 21 other methyltransferases. A-366 is also a potent， nanomolar inhibitor of the Spindlin1-H3K4me3-interaction (IC50=182.6 nM). A-366 displays high affinity at human histamine H3 receptor (Ki=17 nM) and shows subtype selectivity among subsets of the histaminergic and dopaminergic receptor families[1-4]. |
| Data Literature Source | [1]. Reiner D，et al. Epigenetics meets GPCR: inhibition of histone H3 methyltransferase (G9a) and histamine H3 receptor for Prader-Willi Syndrome. Sci Rep. 2020;10(1):13558. Published 2020 Aug 11. [2]. Wagner T，et al. Identification of a small-molecule ligand of the epigenetic reader protein Spindlin1 via a versatile screening platform. Nucleic Acids Res. 2016;44(9):e88. [3]. Sweis RF，et al. Discovery and development of potent and selective inhibitors of histone methyltransferase g9a. ACS Med Chem Lett. 2014;5(2):205-209. Published 2014 Jan 2. [4]. Pappano WN，et al. The Histone Methyltransferase Inhibitor A-366 Uncovers a Role for G9a/GLP in the Epigenetics of Leukemia. PLoS One. 2015;10(7):e0131716. Published 2015 Jul 6. |
| Unit | Bottle |
| Specification | 5mg 10mg |
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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