1. Epigenetics
  2. Histone Methyltransferase
  3. A-395

A-395 

Cat. No.: HY-101512 Purity: 99.31%
Handling Instructions

A-395 est un antagoniste des interactions protéine-protéine complexe répressif polycombique 2 (PRC2) qui inhibe puissamment le complexe trimérique PRC2 (EZH2-EED-SUZ12) avec un IC50 de 18 nM.

A-395 is an antagonist of polycomb repressive complex 2 (PRC2) protein-protein interactions that potently inhibits the trimeric PRC2 complex (EZH2-EED-SUZ12) with an IC50 of 18 nM.

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

A-395 Chemical Structure

A-395 Chemical Structure

CAS No. : 2089148-72-9

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Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 118 In-stock
Estimated Time of Arrival: December 31
5 mg USD 110 In-stock
Estimated Time of Arrival: December 31
10 mg USD 190 In-stock
Estimated Time of Arrival: December 31
25 mg USD 450 In-stock
Estimated Time of Arrival: December 31
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Description

A-395 is an antagonist of polycomb repressive complex 2 (PRC2) protein-protein interactions that potently inhibits the trimeric PRC2 complex (EZH2-EED-SUZ12) with an IC50 of 18 nM[1].

IC50 & Target

IC50: 18 nM (Trimeric PRC2 complex)[1]

In Vitro

The embryonic ectoderm development (EED) protein is an essential subunit of Polycomb repressive complex 2 (PRC2). A-395 antagonizes of the H3K27me3 binding functions of EED. A-395 binds to EED in the H3K27me3-binding pocket, thereby preventing allosteric activation of the catalytic activity of PRC2. A-395 is capable of competing for H3K27me3 peptide binding to EED, with an IC50 of 7 nM. A-395, but not the close chemical analog A-395N, modulates activity of PRC2 in cells by potently reducing the H3K27 methyl mark in a highly selective manner. A-395 treatment inhibits both H3K27me2 and H3K27me3, with IC50 values of 390 nM and 90 nM, respectively. Furthermore, A-395 treatment results in growth inhibition of human tumor cell lines sensitive to SAM-competitive EZH2 inhibitors[1].

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

In Vivo

The embryonic ectoderm development (EED) protein is an essential subunit of Polycomb repressive complex 2 (PRC2). A-395 antagonizes of the H3K27me3 binding functions of EED. A-395 binds to EED in the H3K27me3-binding pocket, thereby preventing allosteric activation of the catalytic activity of PRC2. A-395 is capable of competing for H3K27me3 peptide binding to EED, with an IC50 of 7 nM. A-395, but not the close chemical analog A-395N, modulates activity of PRC2 in cells by potently reducing the H3K27 methyl mark in a highly selective manner. A-395 treatment inhibits both H3K27me2 and H3K27me3, with IC50 values of 390 nM and 90 nM, respectively. Furthermore, A-395 treatment results in growth inhibition of human tumor cell lines sensitive to SAM-competitive EZH2 inhibitors[1].

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

Molecular Weight

486.65

Formula

C₂₆H₃₅FN₄O₂S

CAS No.
SMILES

O=S(N1CCN(C2=CC=C([[email protected]]3CN(C4C(C(F)=CC=C5)=C5CC4)C[[email protected]@H]3N(C)C)C=C2)CC1)(C)=O

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 : 100 mg/mL (205.49 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0549 mL 10.2743 mL 20.5486 mL
5 mM 0.4110 mL 2.0549 mL 4.1097 mL
10 mM 0.2055 mL 1.0274 mL 2.0549 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: ≥ 0.83 mg/mL (1.71 mM); Clear solution

  • 2.

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

    Solubility: ≥ 0.83 mg/mL (1.71 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 0.83 mg/mL (1.71 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Kinase Assay

The embryonic ectoderm development (EED) protein is an essential subunit of Polycomb repressive complex 2 (PRC2). A-395 antagonizes of the H3K27me3 binding functions of EED. A-395 binds to EED in the H3K27me3-binding pocket, thereby preventing allosteric activation of the catalytic activity of PRC2. A-395 is capable of competing for H3K27me3 peptide binding to EED, with an IC50 of 7 nM. A-395, but not the close chemical analog A-395N, modulates activity of PRC2 in cells by potently reducing the H3K27 methyl mark in a highly selective manner. A-395 treatment inhibits both H3K27me2 and H3K27me3, with IC50 values of 390 nM and 90 nM, respectively. Furthermore, A-395 treatment results in growth inhibition of human tumor cell lines sensitive to SAM-competitive EZH2 inhibitors[1].

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

Cell Assay
[1]

1,000 multiple myeloma cells are seeded in each well of 96-well cell culture plates and treated with A-395 (0.001-100 μM) or DMSO control for 10 d before the cell proliferation assay. Cell proliferation assays are conducted with the CellTiter-Glo Luminescent Cell Viability Assay[1].

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

Animal Administration
[1]

Mice[1]

SCID mice are inoculated with the human Pfeiffer cell line and these xenografts are grown to size match at ∼200 mm3. Mice are subsequently treated with vehicle control, A-395 and A-395N at 300 mg/kg s.c. two times per week for 5 weeks or GSK126 at 50 mg/kg i.p. once per day for 36 d. Tumor volume is measured at different intervals and is represented by the average ± s.d. (eight mice per group)[1].

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

References

Purity: 99.31%

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Keywords:

A-395A395A 395Histone MethyltransferaseInhibitorinhibitorinhibit

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A-395
Cat. No.:
HY-101512
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