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

A-366 

Cat. No.: HY-12583 Purity: 98.02%
COA Handling Instructions

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.

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
Solution
10 mM * 1 mL in DMSO USD 94 In-stock
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 94 In-stock
Solid
1 mg USD 40 In-stock
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 2 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 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].

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].

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

Appearance

Solid

Formula

C19H27N3O2
CAS No.
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)

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.
In Vivo:
  • 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

  • 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

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 98.02%

COA (246 KB) RP-HPLC (211 KB)

Handling Instructions (2659 KB)
References
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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.

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Keywords:

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

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