A-366

Name: A-366
Brand: MedChemExpress
SKU: HY-12583
Rating: 5.0 (6 reviews)

Cat. No.: HY-12583 Purity: 98.13%: Data Sheet
COA

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A-366, a chemical probe, 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 (K_i=17 nM) and shows subtype selectivity among subsets of the histaminergic and dopaminergic receptor families.

For research use only. We do not sell to patients.

CAS No. : 1527503-11-2

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	Get quote
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Customer Review

Based on 6 publication(s) in Google Scholar

6 Publications Citing Use of MCE A-366

Bio/Physico-chemical Assay

: A-366 purchased from MedChemExpress. Usage Cited in: Diabetes. 2025 Oct 1;74(10):1825-1838. [Abstract]; Insulin secretion, normalized by total content, of EndoC-βH1 cells treated with A-366 under different conditions.

: A-366 purchased from MedChemExpress. Usage Cited in: Diabetes. 2025 Oct 1;74(10):1825-1838. [Abstract]; Principal component (PC) analysis of the RNA-seq data shows the separation of samples along two axes corresponding to glucolipotoxicity (GL) treatment and A-366.

: A-366 purchased from MedChemExpress. Usage Cited in: Diabetes. 2025 Oct 1;74(10):1825-1838. [Abstract]; RRHO map comparing the differential expression of GL vs. Ctrl (x-axis) and A-366 vs. on drug (y-axes).

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View All Isoforms

EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D ASH1L/KMT2H SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 NSD3/WHSC1L1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

EHMT2/G9a/KMT1C

EHMT1/GLP/KMT1D

Cellular Effect

Cell Line	Type	Value	Description	References
CWR22R	EC₅₀	> 10 μM Compound: Chemical probe: A-366	Antiproliferative against human 22RV1 cells after 5 days by Cell-Titer Glo assay Antiproliferative against human 22RV1 cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
Calu-1	EC₅₀	> 10 μM Compound: Chemical probe: A-366	Antiproliferative against human Calu-1 cells after 5 days by Cell-Titer Glo assay Antiproliferative against human Calu-1 cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
Calu-6	EC₅₀	> 10 μM Compound: Chemical probe: A-366	Antiproliferative against human Calu-6 cells after 5 days by Cell-Titer Glo assay Antiproliferative against human Calu-6 cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
DU-145	EC₅₀	> 10 μM Compound: Chemical probe: A-366	Antiproliferative against human DU-145 cells after 5 days by Cell-Titer Glo assay Antiproliferative against human DU-145 cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
Daoy	EC₅₀	> 10 μM Compound: Chemical probe: A-366	Antiproliferative against human Daoy cells after 7 days by Cell-Titer Glo assay Antiproliferative against human Daoy cells after 7 days by Cell-Titer Glo assay	[PMID: 26147105]
G-401	EC₅₀	> 10 μM Compound: Chemical probe: A-366	Antiproliferative against human G-401 cells after 7 days by Cell-Titer Glo assay Antiproliferative against human G-401 cells after 7 days by Cell-Titer Glo assay	[PMID: 26147105]
HL-60	EC₅₀	> 10 μM Compound: Chemical probe: A-366	Antiproliferative against human HL-60 cells after 5 days by Cell-Titer Glo assay Antiproliferative against human HL-60 cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
HT-1080	EC₅₀	> 10 μM Compound: Chemical probe: A-366	Antiproliferative against human HT-1080 cells after 5 days by Cell-Titer Glo assay Antiproliferative against human HT-1080 cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
IMR-32	EC₅₀	> 10 μM Compound: Chemical probe: A-366	Antiproliferative against human IMR-32 cells after 7 days by Cell-Titer Glo assay Antiproliferative against human IMR-32 cells after 7 days by Cell-Titer Glo assay	[PMID: 26147105]
K562	EC₅₀	> 10 μM Compound: Chemical probe: A-366	Antiproliferative against human K562 cells after 5 days by Cell-Titer Glo assay Antiproliferative against human K562 cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
KMS-11	EC₅₀	> 10 μM Compound: Chemical probe: A-366	Antiproliferative against human KMS-11 cells after 5 days by Cell-Titer Glo assay Antiproliferative against human KMS-11 cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
KMS-12-BM	EC₅₀	> 10 μM Compound: Chemical probe: A-366	Antiproliferative against human KMS-12-BM cells after 5 days by Cell-Titer Glo assay Antiproliferative against human KMS-12-BM cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
Kasumi 1	EC₅₀	> 10 μM Compound: Chemical probe: A-366	Antiproliferative against human Kasumi-1 cells after 5 days by Cell-Titer Glo assay Antiproliferative against human Kasumi-1 cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
L-363	EC₅₀	> 10 μM Compound: Chemical probe: A-366	Antiproliferative against human L-363 cells after 5 days by Cell-Titer Glo assay Antiproliferative against human L-363 cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
LN-229	EC₅₀	> 10 μM Compound: Chemical probe: A-366	Antiproliferative against human LN-229 cells after 5 days by Cell-Titer Glo assay Antiproliferative against human LN-229 cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
LNCaP	EC₅₀	> 10 μM Compound: Chemical probe: A-366	Antiproliferative against human LNCaP cells after 5 days by Cell-Titer Glo assay Antiproliferative against human LNCaP cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
MOLT-16	EC₅₀	> 10 μM Compound: Chemical probe: A-366	Antiproliferative against human MOLT-16 cells after 5 days by Cell-Titer Glo assay Antiproliferative against human MOLT-16 cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
MV4-11	EC₅₀	> 10 μM Compound: Chemical probe: A-366	Antiproliferative against human MV4-11 cells after 5 days by Cell-Titer Glo assay Antiproliferative against human MV4-11 cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
NCI-H1975	EC₅₀	> 10 μM Compound: Chemical probe: A-366	Antiproliferative against human NCI-H1975 cells after 5 days by Cell-Titer Glo assay Antiproliferative against human NCI-H1975 cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
NCI-H2009	EC₅₀	> 10 μM Compound: Chemical probe: A-366	Antiproliferative against human NCI-H2009 cells after 5 days by Cell-Titer Glo assay Antiproliferative against human NCI-H2009 cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
NCI-H358	EC₅₀	> 10 μM Compound: Chemical probe: A-366	Antiproliferative against human NCI-H358 cells after 5 days by Cell-Titer Glo assay Antiproliferative against human NCI-H358 cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
NCI-H441	EC₅₀	> 10 μM Compound: Chemical probe: A-366	Antiproliferative against human NCI-H441 cells after 5 days by Cell-Titer Glo assay Antiproliferative against human NCI-H441 cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
NCI-H522	EC₅₀	> 10 μM Compound: Chemical probe: A-366	Antiproliferative against human NCI-H522 cells after 5 days by Cell-Titer Glo assay Antiproliferative against human NCI-H522 cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
NCI-H661	EC₅₀	> 10 μM Compound: Chemical probe: A-366	Antiproliferative against human NCI-H661 cells after 5 days by Cell-Titer Glo assay Antiproliferative against human NCI-H661 cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
NCI-H929	EC₅₀	> 10 μM Compound: Chemical probe: A-366	Antiproliferative against human NCI-H929 cells after 5 days by Cell-Titer Glo assay Antiproliferative against human NCI-H929 cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
OPM-2	EC₅₀	> 10 μM Compound: Chemical probe: A-366	Antiproliferative against human OPM-2 cells after 5 days by Cell-Titer Glo assay Antiproliferative against human OPM-2 cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
PA-1	EC₅₀	> 10 μM Compound: Chemical probe: A-366	Antiproliferative against human PA-1 cells after 7 days by Cell-Titer Glo assay Antiproliferative against human PA-1 cells after 7 days by Cell-Titer Glo assay	[PMID: 26147105]
RPMI-8226	EC₅₀	> 10 μM Compound: Chemical probe: A-366	Antiproliferative against human RPMI-8226 cells after 5 days by Cell-Titer Glo assay Antiproliferative against human RPMI-8226 cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
RS4-11	EC₅₀	> 10 μM Compound: Chemical probe: A-366	Antiproliferative against human RS4-11 cells after 5 days by Cell-Titer Glo assay Antiproliferative against human RS4-11 cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
SK-BR-3	EC₅₀	> 10 μM Compound: Chemical probe: A-366	Antiproliferative against human SK-BR-3 cells after 5 days by Cell-Titer Glo assay Antiproliferative against human SK-BR-3 cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
SK-N-MC	EC₅₀	> 10 μM Compound: Chemical probe: A-366	Antiproliferative against human SK-N-MC cells after 7 days by Cell-Titer Glo assay Antiproliferative against human SK-N-MC cells after 7 days by Cell-Titer Glo assay	[PMID: 26147105]
Sf9	IC₅₀	11 nM Compound: A-366	Inhibition of N-terminal GST tagged human recombinant EHMT1 (794 to 1294 residues) expressed in baculovirus infected Sf9 insect cells assessed as reduction in conversion of SAH to AMP using histone H3 as substrate and SAH as cosubstrate incubated for 30 mins by AMP Glo detection assay Inhibition of N-terminal GST tagged human recombinant EHMT1 (794 to 1294 residues) expressed in baculovirus infected Sf9 insect cells assessed as reduction in conversion of SAH to AMP using histone H3 as substrate and SAH as cosubstrate incubated for 30 mins by AMP Glo detection assay	[PMID: 31350126]
Sf9	IC₅₀	13 nM Compound: A-366	Inhibition of N-terminal GST tagged human recombinant EHMT2 (785 to 1210 residues) expressed in baculovirus infected Sf9 insect cells assessed as reduction in conversion of SAH to AMP using histone H3 as substrate and SAH as cosubstrate incubated for 30 mins by AMP Glo detection assay Inhibition of N-terminal GST tagged human recombinant EHMT2 (785 to 1210 residues) expressed in baculovirus infected Sf9 insect cells assessed as reduction in conversion of SAH to AMP using histone H3 as substrate and SAH as cosubstrate incubated for 30 mins by AMP Glo detection assay	[PMID: 31350126]
THP-1	EC₅₀	> 10 μM Compound: Chemical probe: A-366	Antiproliferative against human THP-1 cells after 5 days by Cell-Titer Glo assay Antiproliferative against human THP-1 cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
U2OS	EC₅₀	> 10 μM Compound: Chemical probe: A-366	Antiproliferative against human U2OS cells after 7 days by Cell-Titer Glo assay Antiproliferative against human U2OS cells after 7 days by Cell-Titer Glo assay	[PMID: 26147105]
ZR-75-30	EC₅₀	> 10 μM Compound: Chemical probe: A-366	Antiproliferative against human ZR-75-30 cells after 7 days by Cell-Titer Glo assay Antiproliferative against human ZR-75-30 cells after 7 days by Cell-Titer Glo assay	[PMID: 26147105]

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.

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.

1527503-11-2

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
10 mM	0.3035 mL	1.5177 mL	3.0355 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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

mg/kg

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Dosing volume
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μL

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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: 98.13%

Select Batch:

Data Sheet (277 KB) SDS (393 KB)

COA (246 KB) HNMR (260 KB) RP-HPLC (226 KB)

Handling Instructions (2659 KB)

References

[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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

Complete Stock Solution Preparation Table

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

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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A-366

Customer Review

A-366 Related Antibodies

6 Publications Citing Use of MCE A-366

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Histone Methyltransferase Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

A-366 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

A-366 Related Classifications

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