A-196

Name: A-196
Brand: MedChemExpress
SKU: HY-100201
Rating: 5.0 (11 reviews)

Cat. No.: HY-100201 Purity: 98.76%: Data Sheet
COA

SDS
Handling Instructions
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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.

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

CAS No. : 1982372-88-2

Size	Stock	Quantity

Free Sample (0.1 - 0.2 mg)	Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
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Customer Review

Based on 11 publication(s) in Google Scholar

Other Forms of A-196:

A-196 (Standard) Get quote

11 Publications Citing Use of MCE A-196

Bio/Physico-chemical Assay

Cell Proliferation/Viability Assay

: 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.

: A-196 purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 Oct 20:2025.10.20.683419.; 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.; 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.; 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.

: 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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View All Histone Methyltransferase Isoform Specific Products:

View All Isoforms

EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D ASH1L/KMT2H SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 NSD3/WHSC1L1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

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

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	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]
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]
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]
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]

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.

Molecular Weight

359.25

Formula

C₁₈H₁₆Cl₂N₄

CAS No.

1982372-88-2

Appearance

Solid

Color

Light brown to brown

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
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.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

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

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Purity & Documentation

Purity: 98.76%

Select Batch:

Data Sheet (278 KB) SDS (393 KB)

COA (253 KB) HNMR (258 KB) LCMS (113 KB)

Handling Instructions (2659 KB)

References

[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]

Complete Stock Solution Preparation Table

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

A-196 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.

Keywords:

A-1961982372-88-2A196A 196Histone MethyltransferaseInhibitorinhibitorinhibit

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A-196

Customer Review

Other Forms of A-196:

A-196 Related Antibodies

11 Publications Citing Use of MCE A-196

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Histone Methyltransferase Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

A-196 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

A-196 Related Classifications

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Customer Review

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