A-395
Based on 4 publication(s) in Google Scholar
A-395, a chemical probe, 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.
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- Reinheit: 98.78%
- CAS. Nr.: 2089148-72-9
- Formel: C26H35FN4O2S
- Molecular Weight:486.65
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Publications Citing Use of MedChemExpress (MCE) A-395
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Biologische Aktivität
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EZH2 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| KARPAS-422 | IC50 |
62.9 nM
Compound: 7; A-395
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Growth inhibition of human KARPAS-422 cells assessed as cell growth incubated for 7 days by lactate dehydrogenase based WST-8 assay
Growth inhibition of human KARPAS-422 cells assessed as cell growth incubated for 7 days by lactate dehydrogenase based WST-8 assay
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[PMID: 34613724] |
| Pfeiffer | IC50 |
69 nM
Compound: 74; A-395
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Antiproliferative activity against human Pfeiffer cells incubated for 10 days by cellTiter-glo luminesence method
Antiproliferative activity against human Pfeiffer cells incubated for 10 days by cellTiter-glo luminesence method
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[PMID: 33283516] |
| Pfeiffer | IC50 |
69 nM
Compound: A-395
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Growth inhibition of human Pfeiffer cells incubated for 10 days by WST8 assay
Growth inhibition of human Pfeiffer cells incubated for 10 days by WST8 assay
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[PMID: 32580550] |
| RD | IC50 |
0.09 μM
Compound: 43c; A395
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Inhibition of H3K27me3 methylation in human RD cell incubated for 72 hrs
Inhibition of H3K27me3 methylation in human RD cell incubated for 72 hrs
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[PMID: 34351144] |
| RD | IC50 |
0.39 μM
Compound: 43c; A395
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Inhibition of H3K27me2 methylation in human RD cell incubated for 72 hrs
Inhibition of H3K27me2 methylation in human RD cell incubated for 72 hrs
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[PMID: 34351144] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 2089148-72-9
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Appearance Solid
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Molecular Weight 486.65
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Formel C26H35FN4O2S
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Color White to yellow
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SMILES
O=S(N1CCN(C2=CC=C([C@H]3CN(C4C(C(F)=CC=C5)=C5CC4)C[C@@H]3N(C)C)C=C2)CC1)(C)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (4)
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Journal Impact Factor
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Most Recent
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Nat Neurosci
Single-cell epigenomic reconstruction of developmental trajectories from pluripotency in human neural organoid systems. [Abstract]2024 Jul;27(7):1376-1386. PMID: 38914828 -
Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175 -
iScience
CD2 costimulation strength: A key regulator of T cell function and anti-tumor immunity that is epigenetically regulated. [Abstract]2025 Nov 10;28(12):113977. PMID: 41377664 -
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (205.49 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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.
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
This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 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.
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
This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protokoll
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (279 KB)
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SDS (393 KB)
- English - EN (393 KB)
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- Deutsch - DE (393 KB)
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- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
Verweise
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0549 mL | 10.2743 mL | 20.5486 mL | 51.3716 mL |
| 5 mM | 0.4110 mL | 2.0549 mL | 4.1097 mL | 10.2743 mL | |
| 10 mM | 0.2055 mL | 1.0274 mL | 2.0549 mL | 5.1372 mL | |
| 15 mM | 0.1370 mL | 0.6850 mL | 1.3699 mL | 3.4248 mL | |
| 20 mM | 0.1027 mL | 0.5137 mL | 1.0274 mL | 2.5686 mL | |
| 25 mM | 0.0822 mL | 0.4110 mL | 0.8219 mL | 2.0549 mL | |
| 30 mM | 0.0685 mL | 0.3425 mL | 0.6850 mL | 1.7124 mL | |
| 40 mM | 0.0514 mL | 0.2569 mL | 0.5137 mL | 1.2843 mL | |
| 50 mM | 0.0411 mL | 0.2055 mL | 0.4110 mL | 1.0274 mL | |
| 60 mM | 0.0342 mL | 0.1712 mL | 0.3425 mL | 0.8562 mL | |
| 80 mM | 0.0257 mL | 0.1284 mL | 0.2569 mL | 0.6421 mL | |
| 100 mM | 0.0205 mL | 0.1027 mL | 0.2055 mL | 0.5137 mL |
A-395 Related Classifications
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