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A 196

Cat. No. 6167 Submit a Review Datasheet / COA / SDS
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Description: Potent and selective SUV420H1/H2 inhibitor
Chemical Name: 6,7-Dichloro-N-cyclopentyl-4-(4-pyridinyl)-1-phthalazinamine
Purity: ≥98% (HPLC)
Datasheet
Citations
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Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for A 196

A 196 is a potent and selective SUV420H1/H2 inhibitor (IC50 values are 25 and 144 nM respectively) that exhibits 100-fold selectivity over other histone methyltransferases and non-epigenetic targets. A 196 inhibits the di- and tri-methylation of H4K20me in multiple cell lines (IC50 < 1 μM).

To request the negative control for A 196, please fill out the SGC 2043 request form on the SGC website.

Licensing Information

This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the A-196 probe summary on the SGC website.

External Portal Information for A 196

Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of A196 is reviewed on the Chemical Probes website.

Compound Libraries for A 196

A 196 is also offered as part of the Tocriscreen Epigenetics Library. Find out more about compound libraries available from Tocris.

Technical Data for A 196

M. Wt 359.25
Formula C18H16Cl2N4
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 1982372-88-2
PubChem ID 117072548
InChI Key ABGOSOMRWSYAOB-UHFFFAOYSA-N
Smiles ClC1=CC2=C(C(C3=CC=NC=C3)=NN=C2NC4CCCC4)C=C1Cl

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for A 196

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 7.18 20

Preparing Stock Solutions for A 196

The following data is based on the product molecular weight 359.25. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.2 mM 13.92 mL 69.59 mL 139.18 mL
1 mM 2.78 mL 13.92 mL 27.84 mL
2 mM 1.39 mL 6.96 mL 13.92 mL
10 mM 0.28 mL 1.39 mL 2.78 mL

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References for A 196

References are publications that support the biological activity of the product.

Bromberg et al (2017) The SUV4-20 inhibitor A-196 verifies a role for epigenetics in genomic integrity. Nat.Chem.Biol. 13 317 PMID: 28114273

Scheer et al (2019) A chemical biology toolbox to study protein methyltransferases and epigenetic signaling. Nat.Commun. 10 19 PMID: 30604761

Brustel et al (2017) Histone H4K20 tri-methylation at late-firing origins ensures timely heterochromatin replication. EMBO J 36 2726 PMID: 28778956

If you know of a relevant reference for A 196, please let us know.

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Keywords: A 196, A 196 supplier, A196, methyltransferases, histones, inhibitors, inhibits, HMTs, MLL, leukemia, mll-rearranged, H4K20me, potent, selective, Other, Lysine, Methyltransferases, 6167, Tocris Bioscience

Citations for A 196

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