1. Epigenetics
  2. Histone Methyltransferase

A-366 

Cat. No.: HY-12583 Purity: 98.47%
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 USD 86 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
5 mg USD 78 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
10 mg USD 132 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
50 mg USD 528 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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    A-366 purchased from MCE. Usage Cited in: Theranostics. 2018 Apr 15;8(10):2884-2895.

    Plk1 levels are decreased companied with p53K373me2 decline in HCT116 cells treated with BRD9539.
    • Biological Activity

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    • 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.

    Solvent & Solubility
    In Vitro: 

    10 mM in DMSO

    Preparing
    Stock Solutions
    Concentration Solvent 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
    *Please refer to the solubility information to select the appropriate solvent.
    References
    Molecular Weight

    329.44

    Formula

    C₁₉H₂₇N₃O₂

    CAS No.

    1527503-11-2

    SMILES

    COC1=CC2=C(N=C(N)C23CCC3)C=C1OCCCN4CCCC4

    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

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

    Cat. No.: HY-12583