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

A-196 

Cat. No.: HY-100201 Purity: 99.73%
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

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 71 In-stock
Estimated Time of Arrival: December 31
1 mg USD 50 In-stock
Estimated Time of Arrival: December 31
5 mg USD 90 In-stock
Estimated Time of Arrival: December 31
10 mg USD 120 In-stock
Estimated Time of Arrival: December 31
50 mg USD 480 In-stock
Estimated Time of Arrival: December 31
100 mg USD 850 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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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].

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

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 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 31 mg/mL (86.29 mM)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

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 provided by MCE.
References
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Product Name:
A-196
Cat. No.:
HY-100201
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