1. Epigenetics
  2. Histone Methyltransferase

A-366 

Cat. No.: HY-12583 Purity: 98.83%
Data Sheet SDS Handling Instructions

A-366 is a peptide-competitive inhibitor of G9a/GLP with an enzymatic IC50 of ~3 nM and >100-fold selectivity over other methyltransferases and other non-epigenetic targets.

For research use only. We do not sell to patients.
A-366 Chemical Structure

A-366 Chemical Structure

CAS No. : 1527503-11-2

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $72 In-stock
5 mg $65 In-stock
10 mg $110 In-stock
50 mg $440 In-stock
100 mg   Get quote  
200 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

A-366 is a peptide-competitive inhibitor of G9a/GLP with an enzymatic IC50 of ~3 nM and >100-fold selectivity over other methyltransferases and other non-epigenetic targets. IC50 value: 3 nM Target: HMTase in vitro: A-366 is a cell-active G9a/GLP small molecule inhibitor. The potency and selectivity of A-366 made it an ideal candidate to probe the cellular activities of G9a/GLP. A-366 reduced the total levels of H3K9me2 in a time and concentration dependent manner with a cellular EC50 of ~300 nM. A-366 has significantly less cytotoxic effects on the growth of tumor cell lines compared to other known G9a/GLP small molecule inhibitors despite equivalent cellular activity on methylation of H3K9me2. Additionally, the selectivity profile of A-366 has aided in the discovery of a potentially important role for G9a/GLP in maintenance of leukemia. Long term treatment of leukemia cell lines with A-366 results in differentiation and inhibition of growth in vivo: Mice treated with A-366 administered via osmotic mini-pump at 30 mg/kg/day for two weeks showed no overt toxicity. Furthermore, treatment of a flank xenograft leukemia model with A-366 resulted in growth inhibition consistent with the profile of H3K9me2 reduction observed.

References
Preparing Stock Solutions
Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
1 mM 3.0355 mL 15.1773 mL 30.3545 mL
5 mM 0.6071 mL 3.0355 mL 6.0709 mL
10 mM 0.3035 mL 1.5177 mL 3.0355 mL
References
Molecular Weight

329.44

Formula

C₁₉H₂₇N₃O₂

CAS No.

1527503-11-2

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Product Name:
A-366
Cat. No.:
HY-12583
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