2. Epigenetics
  3. Histone Methyltransferase Epigenetic Reader Domain
  4. A-366

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.

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A-366 Chemical Structure

A-366 Chemical Structure

CAS No. : 1527503-11-2

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 94 In-stock
Solution
10 mM * 1 mL in DMSO USD 94 In-stock
Solid
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5 mg USD 86 In-stock
10 mg USD 145 In-stock
50 mg USD 460 In-stock
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Customer Review

Based on 3 publication(s) in Google Scholar

A-366 Related Antibodies

Top Publications Citing Use of Products

View All Histone Methyltransferase Isoform Specific Products:

View All Isoforms
EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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][2][3][4].

IC50 & Target

EHMT2/G9a/KMT1C

 

EHMT1/GLP/KMT1D

 

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

A-366 Related Antibodies

Cell Viability Assay[4]

Cell Line: MV4;11 cells
Concentration: 0.01-10 μM
Incubation Time: 14 days
Result: Resulted in inhibited proliferation and a decrease in viability corresponding to the dose response observed for CD11b staining.
In Vivo

A-366 (30 mg/kg; osmotic mini-pump; daily for 14 days) treatment of MV4;11 xenografts elicits growth inhibition[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 6-8 week old SCID-beige female mice (MV4;11 xenografts)[4]
Dosage: 30 mg/kg
Administration: By osmotic mini-pump; daily for 14 days
Result: A modest 45% tumor growth inhibition resulting from A-366 treatment in this model.
Molecular Weight

329.44

Formula

C19H27N3O2
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (151.77 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (7.59 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (7.59 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

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(per animal)

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Dosing volume
(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 98.01%

COA (246 KB) RP-HPLC (245 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.0355 mL 15.1773 mL 30.3545 mL 75.8864 mL
5 mM 0.6071 mL 3.0355 mL 6.0709 mL 15.1773 mL
10 mM 0.3035 mL 1.5177 mL 3.0355 mL 7.5886 mL
15 mM 0.2024 mL 1.0118 mL 2.0236 mL 5.0591 mL
20 mM 0.1518 mL 0.7589 mL 1.5177 mL 3.7943 mL
25 mM 0.1214 mL 0.6071 mL 1.2142 mL 3.0355 mL
30 mM 0.1012 mL 0.5059 mL 1.0118 mL 2.5295 mL
40 mM 0.0759 mL 0.3794 mL 0.7589 mL 1.8972 mL
50 mM 0.0607 mL 0.3035 mL 0.6071 mL 1.5177 mL
60 mM 0.0506 mL 0.2530 mL 0.5059 mL 1.2648 mL
80 mM 0.0379 mL 0.1897 mL 0.3794 mL 0.9486 mL
100 mM 0.0304 mL 0.1518 mL 0.3035 mL 0.7589 mL
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A-366 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

A-3661527503-11-2A366A 366Histone MethyltransferaseEpigenetic Reader Domainselectivepeptide-competitivemethyltransferaseH3K4me3interactionMV4;11cellsepigeneticsleukemiaInhibitorinhibitorinhibit

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