2. Epigenetics
  3. Histone Methyltransferase
  4. A-196

A-196 

Cat. No.: HY-100201 Purity: 99.73%
COA Handling Instructions

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.

A-196 Chemical Structure

A-196 Chemical Structure

CAS No. : 1982372-88-2

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Solid + Solvent
10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 71 In-stock
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50 mg USD 480 In-stock
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Customer Review

Based on 4 publication(s) in Google Scholar

A-196 Related Antibodies

Top Publications Citing Use of Products

View All Histone Methyltransferase Isoform Specific Products:

View All Isoforms
EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D SETDB1/KMT2G SETD2/KMT3A SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1].

IC50 & Target

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

A-196 Related Antibodies

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

Appearance

Solid

Formula

C18H16Cl2N4
CAS No.
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)

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

  • 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

  • 3.

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

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

*All of the co-solvents are available by MedChemExpress (MCE).
Purity & Documentation

Purity: 99.73%

COA (252 KB) LCMS (136 KB)

Handling Instructions (2659 KB)
References
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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.

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
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The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

A-1961982372-88-2A196A 196Histone MethyltransferaseInhibitorinhibitorinhibit

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