[CAS NO. 1982372-88-2]  A-196

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PRODUCTS SPECIFICATIONS [1982372-88-2]

Catalog
SLK-S7983
Brand
Selleck
CAS
1982372-88-2

DESCRIPTION [1982372-88-2]

Overview

MDLMFCD29924807
Molecular Weight359.25
Molecular FormulaC18H16Cl2N4
SMILESClC1=CC2=C(C=C1Cl)C(C3=CC=NC=C3)=NN=C2NC4CCCC4

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

1 mg5 mg10 mg
1 mM2.7836 mL13.9179 mL27.8358 mL
5 mM0.5567 mL2.7836 mL5.5672 mL
10 mM0.2784 mL1.3918 mL2.7836 mL
50 mM---

Description

A-196 is a potent and selective inhibitor of and 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 nM144 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.