A-196
Based on 11 publication(s) in Google Scholar
A-196 is a potent and selective inhibitor of SUV420H1 and SUV420H2 with IC50 values of 25 nM and 144 nM, respectively. A-196 inhibits SUV4-20 biochemically in a substrate-competitive manner. A-196 represents a first-in-class chemical probe of SUV4-20 to investigate the role of histone methyltransferases in genomic integrity.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.76%
- CAS 番号: 1982372-88-2
- 分子式: C18H16Cl2N4
- 分子量:359.25
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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Epigenetics Compound Library
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HY-L203
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Posttranslational Modification Library
HY-L226
MedChemExpress（MCE）の使用を引用している文献 A-196
More- Cancer Cell. 2024 Sep 26:S1535-6108(24)00350-7. [Abstract]
- Cancer Res. 2025 Oct 1. [Abstract]
- Nat Commun. 2026 Feb 12;17(1):1214. [Abstract]
- Nat Commun. 2025 Feb 10;16(1):1483. [Abstract]
- Proc Natl Acad Sci U S A. 2026 Feb 10;123(6):e2501052123. [Abstract]
- PLoS Pathog. 2020 Mar 24;16(3):e1008429. [Abstract]
- Mol Carcinog. 2023 Aug;62(8):1119-1135. [Abstract]
- Biochem Biophys Res Commun. 2023 Jun 30:663:41-46. [Abstract]
- bioRxiv. 2025 Oct 20:2025.10.20.683419. [Abstract]
- bioRxiv. 2025 March 14.
- bioRxiv. 2023 Apr 3.
Customer Validation & Images
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WB
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WB
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Cell Proliferation/Viability Assay
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Cell Proliferation/Viability Assay
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Bio/Physico-chemical Assay
Histone Methyltransferase アイソフォーム固有の製品をすべて表示
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生物活性
IC50: 25 nM (SUV420H1) and 144 nM (SUV420H2)[1].
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| LNCaP | IC50 |
0.211 μM
Compound: Chemical probe : A-196; 3
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Inhibition of H4K20me3 in human LNCaP cells incubated for 48 hrs by Western blotting analysis
Inhibition of H4K20me3 in human LNCaP cells incubated for 48 hrs by Western blotting analysis
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[PMID: 28114273] |
| LNCaP | IC50 |
0.511 μM
Compound: Chemical probe : A-196; 3
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Inhibition of H4K20me2 in human LNCaP cells incubated for 48 hrs by Western blotting analysis
Inhibition of H4K20me2 in human LNCaP cells incubated for 48 hrs by Western blotting analysis
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[PMID: 28114273] |
| LNCaP | IC50 |
0.799 μM
Compound: Chemical probe : A-196; 3
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Inhibition of H4K20me1 in human LNCaP cells incubated for 48 hrs by Western blotting analysis
Inhibition of H4K20me1 in human LNCaP cells incubated for 48 hrs by Western blotting analysis
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[PMID: 28114273] |
| PC-3 | IC50 |
>20 μM
Compound: Chemical probe : A-196; 3
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Antiproliferative activity against human PC-3 cells assessed as change in number of nuclei incubated for 72 hrs by Hoechst staining based high content microscopy
Antiproliferative activity against human PC-3 cells assessed as change in number of nuclei incubated for 72 hrs by Hoechst staining based high content microscopy
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[PMID: 28114273] |
| PC-3 | IC50 |
0.521 μM
Compound: Chemical probe : A-196; 3
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Inhibition of H4K20me3 in human PC-3 cells assessed as decrease in methylation level incubated for 72 hrs by Hoechst staining based high content microscopy
Inhibition of H4K20me3 in human PC-3 cells assessed as decrease in methylation level incubated for 72 hrs by Hoechst staining based high content microscopy
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[PMID: 28114273] |
| PC-3 | IC50 |
0.686 μM
Compound: Chemical probe : A-196; 3
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Inhibition of H4K20me1 in human PC-3 cells assessed as increase in methylation level incubated for 72 hrs by Hoechst staining based high content microscopy
Inhibition of H4K20me1 in human PC-3 cells assessed as increase in methylation level incubated for 72 hrs by Hoechst staining based high content microscopy
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[PMID: 28114273] |
| U2OS | IC50 |
>20 μM
Compound: Chemical probe : A-196; 3
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Antiproliferative activity against human U2OS cells assessed as change in number of nuclei incubated for 72 hrs by Hoechst staining based high content microscopy
Antiproliferative activity against human U2OS cells assessed as change in number of nuclei incubated for 72 hrs by Hoechst staining based high content microscopy
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[PMID: 28114273] |
| U2OS | IC50 |
0.262 μM
Compound: Chemical probe : A-196; 3
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Inhibition of H4K20me2 in human U2OS cells incubated for 48 hrs by Western blotting analysis
Inhibition of H4K20me2 in human U2OS cells incubated for 48 hrs by Western blotting analysis
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[PMID: 28114273] |
| U2OS | IC50 |
0.37 μM
Compound: Chemical probe : A-196; 3
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Inhibition of H4K20me3 in human U2OS cells incubated for 48 hrs by Western blotting analysis
Inhibition of H4K20me3 in human U2OS cells incubated for 48 hrs by Western blotting analysis
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[PMID: 28114273] |
| U2OS | IC50 |
0.502 μM
Compound: Chemical probe : A-196; 3
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Inhibition of H4K20me3 in human U2OS cells assessed as decrease in methylation level incubated for 72 hrs by Hoechst staining based high content microscopy
Inhibition of H4K20me3 in human U2OS cells assessed as decrease in methylation level incubated for 72 hrs by Hoechst staining based high content microscopy
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[PMID: 28114273] |
| U2OS | IC50 |
0.736 μM
Compound: Chemical probe : A-196; 3
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Inhibition of H4K20me1 in human U2OS cells incubated for 48 hrs by Western blotting analysis
Inhibition of H4K20me1 in human U2OS cells incubated for 48 hrs by Western blotting analysis
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[PMID: 28114273] |
| U2OS | IC50 |
1.91 μM
Compound: Chemical probe : A-196; 3
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Inhibition of H4K20me1 in human U2OS cells assessed as increase in methylation level incubated for 72 hrs by Hoechst staining based high content microscopy
Inhibition of H4K20me1 in human U2OS cells assessed as increase in methylation level incubated for 72 hrs by Hoechst staining based high content microscopy
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[PMID: 28114273] |
A-196 (0-5 μM; 48 hours; U2OS cells) treatment results in an increase in H4K20me1 (EC50 value of 735 nM) and a decrease in both H4K20me2 and H4K20me3 (EC50 values of 262 and 370 nM, respectively)[1].
A-196 (10 μM; 72 hours; Wild-type, Suv4-20h double knockout and inhibitortreated mouse embryonic fibroblast cells) inhibits both SUV4-20 enzymes in cells in multiple tissue types without overt toxicity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:U2OS cells
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Concentration:0 μM, 0.075 μM, 0.15 μM, 0.3 μM, 0.6 μM, 1.25 μM, 2.5 μM, 5 μM
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Incubation Time:48 hours
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Result:Increased in H4K20me1 and decreased in both H4K20me2 and H4K20me3.
化学情報
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CAS 番号 1982372-88-2
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性状 Solid
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分子量 359.25
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分子式 C18H16Cl2N4
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Color Light brown to brown
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SMILES
ClC1=C(Cl)C=C(C(C2=CC=NC=C2)=NN=C3NC4CCCC4)C3=C1
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (11)
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Journal Impact Factor
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Most Recent
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Cancer Cell
2024 Sep 26:S1535-6108(24)00350-7. PMID: 39366375 -
Cancer Res
Targeting SUV4-20H Epigenetic Enzymes Enhances Topoisomerase II Poisoning in Prostate Cancer. [Abstract]2025 Oct 1. PMID: 41032740 -
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 -
Nat Commun
2025 Feb 10;16(1):1483. PMID: 39929827
A-196 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 10;16(1):1483. [Abstract]
Western blot (left) and densitometry analyses (right) of indicated proteins in primary hepatocytes (n = 3 per group). Primary hepatocytes isolated from 12-week-old C57BL/6 male mice were treated with A-196 for 72 h.
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Proc Natl Acad Sci U S A
Evaluation of targeted and immune combination therapies in a rat model of hormone receptor-positive breast cancer. [Abstract]2026 Feb 10;123(6):e2501052123. PMID: 41642991 -
PLoS Pathog
BRD4 inhibition exerts anti-viral activity through DNA damage-dependent innate immune responses. [Abstract]2020 Mar 24;16(3):e1008429. PMID: 32208449
A-196 purchased from MedChemExpress. Usage Cited in: PLoS Pathog. 2020 Mar 24;16(3):e1008429. [Abstract]
Inhibition of lysine methyltransferase by A196 (0-1000 nM), EPZ-6438 and GSK503 decreased the rate of PRV-GFP-positive cells, thus suggesting that histone methylation is essential for PRV infection
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Mol Carcinog
PRMT1 inhibition promotes ferroptosis sensitivity via ACSL1 upregulation in acute myeloid leukemia. [Abstract]2023 Aug;62(8):1119-1135. PMID: 37144835 -
Biochem Biophys Res Commun
Epigenetic regulation of DHRS2 by SUV420H2 inhibits cell apoptosis in renal cell carcinoma. [Abstract]2023 Jun 30:663:41-46. PMID: 37119764 -
bioRxiv
Oncogenic and immunomodulatory functions of SUV420H1 in HPV-negative head and neck squamous cell carcinoma. [Abstract]2025 Oct 20:2025.10.20.683419. PMID: 41473330
A-196 purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 Oct 20:2025.10.20.683419. [Abstract]
Top: Western blotting for H4K20me3 levels in HN-SCC-151, HN13 and HN-6 cells treated with control DMSO or incremental concentrations of the SUV420H1 inhibitor A-196 (0-5 μM) for 6 days. Nuclear extracts were obtained and 5 μg were loaded. H3 was used as a loading control. Bottom: Densitometry for H4K20me3 bands, normalized by H3 band intensity. Data are shown as mean ± SEM from n=2 independent biological replicates.
A-196 purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 Oct 20:2025.10.20.683419. [Abstract]
CCK8 assays in 5 HPV-negative HNSCC cell lines treated with control DMSO or A-196 at 0.5 μM, 1 μM and 2.5 μM for 12 days.
A-196 purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 Oct 20:2025.10.20.683419. [Abstract]
Colony forming assays (CFAs) in 5 HPV-negative HNSCC cell lines treated with control DMSO or A-196 at 0.5 μM, 1 μM and 2.5 μM for 12 days.
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溶剤 & 溶解度
DMSO : 12.5 mg/mL (34.79 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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: ≥ 1 mg/mL (2.78 mM); Clear solution
This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 1 mg/mL (2.78 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 1 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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.
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.
純度とドキュメンテーション
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データシート (278 KB)
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SDS (393 KB)
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- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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取扱説明書 (2659 KB)
参考文献
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 | 2.7836 mL | 13.9179 mL | 27.8358 mL | 69.5894 mL |
| 5 mM | 0.5567 mL | 2.7836 mL | 5.5672 mL | 13.9179 mL | |
| 10 mM | 0.2784 mL | 1.3918 mL | 2.7836 mL | 6.9589 mL | |
| 15 mM | 0.1856 mL | 0.9279 mL | 1.8557 mL | 4.6393 mL | |
| 20 mM | 0.1392 mL | 0.6959 mL | 1.3918 mL | 3.4795 mL | |
| 25 mM | 0.1113 mL | 0.5567 mL | 1.1134 mL | 2.7836 mL | |
| 30 mM | 0.0928 mL | 0.4639 mL | 0.9279 mL | 2.3196 mL |
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