A366
Cat.No:IA4090 Solarbio
CAS:1527503-11-2
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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A366CAS:1527503-11-2
Storage:Powder:2-8℃,2 years;Insolvent(Mother Liquid):-20℃,6 months;-80℃,1 year
Purity:≥98%
Appearance:Light yellow to yellow Solid
Qty:
Size:
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]. |
In Vitro | A-366(0.01-10 μM; 14 days)induces differentiation and affects viability in MV4;11 cells[4].A-366(0.3-3 μM; 72 hours)reduces the total levels of H3K9me2 in a time and concentration dependent manner with a cellular EC50 of ~300 nM in PC-3 prostate adenocarcinoma cells. A-366(0.01-10 μM; 4 days; HL-60 cells)results in a dose-dependent differentiation and a corresponding decrease in proliferation. DNA content analysis of A-366-treated HL-60 cells showed an accumulation of cells in G1 consistent with cytostasis[4]. |
In Vivo | A-366(30 mg/kg; osmotic mini-pump; daily for 14 days)treatment of MV4;11 xenografts elicits growth inhibition[4]. |
Animal Experiment | Animal Model: 6-8 week old SCID-beige female mice(MV4;11 xenografts);Dosage: 30 mg/kg;Administration: By osmotic mini-pump; daily for 14 days[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 |
A-366是一种有效的、选择性的G9a/GLP组蛋白甲基转移酶抑制剂。
Remark:These protocols are for reference only. Solarbio does not independently validate these methods.
Note:
1. The products are all for scientific research use only. Do not use it for medical, clinical diagnosis or treatment, food and cosmetics, etc. Do not store them in ordinary residential areas.
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3. The experimental results may be affected by many factors, after-sale service is limited to the product itself and does not involve other compensation.
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