Referencia número: HY-100201

A-196

11 Cited Publications

Revisión del cliente

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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Pureza: 98.76%
No. CAS: 1982372-88-2
Fòrmula: C₁₈H₁₆Cl₂N₄
Peso molecular:359.25

Almacenamiento:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

A-196 Chemical Structure

No. CAS: 1982372-88-2

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Publications (11)
Solvente y solubilidad
- In Vitro
- In Vivo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

IC₅₀ & Target

IC50: 25 nM (SUV420H1) and 144 nM (SUV420H2)^[1].

Ver todos los productos específicos de isoformas Histone Methyltransferase :

Cellular Effect

Cell Line	Type	Value	Description	References
LNCaP	IC₅₀	0.211 μM Compound: Chemical probe : A-196; 3	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	[PMID: 28114273]
LNCaP	IC₅₀	0.511 μM Compound: Chemical probe : A-196; 3	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	[PMID: 28114273]
LNCaP	IC₅₀	0.799 μM Compound: Chemical probe : A-196; 3	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	[PMID: 28114273]
PC-3	IC₅₀	>20 μM Compound: Chemical probe : A-196; 3	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	[PMID: 28114273]
PC-3	IC₅₀	0.521 μM Compound: Chemical probe : A-196; 3	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	[PMID: 28114273]
PC-3	IC₅₀	0.686 μM Compound: Chemical probe : A-196; 3	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	[PMID: 28114273]
U2OS	IC₅₀	>20 μM Compound: Chemical probe : A-196; 3	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	[PMID: 28114273]
U2OS	IC₅₀	0.262 μM Compound: Chemical probe : A-196; 3	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	[PMID: 28114273]
U2OS	IC₅₀	0.37 μM Compound: Chemical probe : A-196; 3	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	[PMID: 28114273]
U2OS	IC₅₀	0.502 μM Compound: Chemical probe : A-196; 3	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	[PMID: 28114273]
U2OS	IC₅₀	0.736 μM Compound: Chemical probe : A-196; 3	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	[PMID: 28114273]
U2OS	IC₅₀	1.91 μM Compound: Chemical probe : A-196; 3	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	[PMID: 28114273]

In Vitro

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.

Western Blot Analysis^[1]

Cell Line:

U2OS cells
Concentration:

0 μM, 0.075 μM, 0.15 μM, 0.3 μM, 0.6 μM, 1.25 μM, 2.5 μM, 5 μM
Incubation Time:

48 hours
Result:

Increased in H4K20me1 and decreased in both H4K20me2 and H4K20me3.

Chemical Information

No. CAS 1982372-88-2
Appearance Solid
Peso molecular 359.25
Fòrmula C₁₈H₁₆Cl₂N₄
Color Light brown to brown
SMILES

ClC1=C(Cl)C=C(C(C2=CC=NC=C2)=NN=C3NC4CCCC4)C3=C1
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (11)

All WBBio/Physico-chemical AssayCell Proliferation/Viability Assay

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Journal Impact Factor

Cancer Cell

Midkine as a driver of age-related changes and increase in mammary tumorigenesis. [Abstract]

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

Non-catalytic mechanisms of KMT5C regulating hepatic gluconeogenesis. [Abstract]

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.
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
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.
bioRxiv

2025 March 14.
bioRxiv

2023 Apr 3.

Solvente y solubilidad

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.7836 mL

13.9179 mL

27.8358 mL

5 mM

0.5567 mL

2.7836 mL

5.5672 mL

10 mM

0.2784 mL

1.3918 mL

2.7836 mL

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.

Calculadora de molaridad

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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: ≥ 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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 1 mg/mL (2.78 mM); Clear solution

This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (278 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Bromberg KD, et al. The SUV4-20 inhibitor A-196 verifies a role for epigenetics in genomic integrity. Nat Chem Biol. 2017 Mar;13(3):317-324. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

A-196

11 Cited Publications

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A-196

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Reprogramming Compound Library

Chemical Probe Library

Anti-Blood Cancer Compound Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Methylation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) A-196

Ver todos los productos específicos de isoformas Histone Methyltransferase

Actividad biológica

Chemical Information

Publications (11)

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

A-196

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Reprogramming Compound Library

Chemical Probe Library

Anti-Blood Cancer Compound Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Methylation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) A-196

Ver todos los productos específicos de isoformas Histone Methyltransferase

Actividad biológica

Chemical Information

Publications (11)

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

A-196 Related Classifications

HY-100201 Related Classifications