A-196

Catalog No.S7983

A-196 Chemical Structure

Molecular Weight(MW): 359.25

A-196 is a potent and selective inhibitor of SUV420H1 and SUV420H2 with IC50 values of 0.025 and 0.144 μM, respectively; more than 100-fold selective over other histone methyltransferases and non-epigenetic targets.

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Biological Activity

Description A-196 is a potent and selective inhibitor of SUV420H1 and SUV420H2 with IC50 values of 0.025 and 0.144 μM, respectively; more than 100-fold selective over other histone methyltransferases and non-epigenetic targets.
Targets
SUV420H1 [1]
(Cell-free assay)
SUV420H2 [1]
(Cell-free assay)
25 nM 144 nM
In vitro

In cells, A-196 induces a global decrease in H4K20me2 and H4K20me3 and a concomitant increase in H4K20me1, but has no effect on any of the other histone modifications. A-196 inhibits 53BP1 foci formation upon ionizing radiation and reduces NHEJ-mediated DNA-break repair but does not affect homology-directed repair. A-196 potently inhibits SUV420H1 and SUV420H2 at both 1 and 10 μM of A-196, but has no activity at either concentration against any of the other PKMTs in the panel, including the other H4K20-modifying enzyme, PR-SET7, and those that utilize H3K4, H3K9, H3K27, and H3K79 as substrates[1].

Protocol

Cell Research:

[1]

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  • Cell lines: U2OS cells 
  • Concentrations: 3 μM
  • Incubation Time: 48 h
  • Method:

    U2OS cells are seeded on 6-well plates with 3 μM A-196 or DMSO as a control, and incubated for 48 h. The cells are washed once in 1 X PBS and then lysis buffer (20 mM Tris-HCl pH 7.5, 0.5% Triton X-100, 150 mM NaCl, 1 mM EDTA, 10 mM MgCl2, PMSF, protease inhibitors, benzonase) is added to half the cells to create whole cell extract (WCE). The remaining cells are subjected to sequential cellular fractionation. First the cell pellet is resuspended in hypotonic buffer A (10 mM HEPES pH 7.5, 10 mM KCl, 1.5 mM MgCl2, 0.3 M sucrose, 1 mM DTT and protease inhibitors) and then 0.1% triton X-100 is added. The cells are incubated for 15 min on ice and pelleted by centrifugation at 1,500g. The supernatant is clarified by centrifugation at max speed and saved as the cytoplasmic fraction. The pellet is resuspended in buffer B (3 mM EDTA, 3 mM EGTA, 1 mM DTT and protease inhibitors) and incubated on ice for 40 min and then centrifuged at 1,500g for 5 min. The supernatant is clarified and saved as the nucleoplasmic fraction. The pellet is resuspended in lysis buffer and incubated for 5 min at room temperature before being resuspended in 4× loading dye. The final lysate contains the solubilized chromatin fraction.


    (Only for Reference)

Solubility (25°C)

In vitro DMSO 15 mg/mL (41.75 mM)
Ethanol 12 mg/mL (33.4 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 359.25
Formula

C18H16Cl2N4

CAS No. 1982372-88-2
Storage powder
Synonyms N/A

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Related Antibodies

Histone Methyltransferase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID