Home / Pharmacology / Enzymes / Transferases / Protein Arginine Methyltransferases / Protein Arginine Methyltransferase Inhibitors / EPZ 015666

EPZ 015666

Cat. No. 6516 1 Citation Submit a Review Datasheet / COA / SDS
Pricing Availability   Qty
Description: Potent and selective PRMT5 inhibitor
Chemical Name: N-[(2S)-3-(3,4-Dihydro-2(1H)-isoquinolinyl)-2-hydroxypropyl]-6-(3-oxetanylamino)-4-pyrimidinecarboxamide
Purity: ≥98% (HPLC)
Datasheet
Citations (1)
Reviews
Literature (1)
Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for EPZ 015666

EPZ 015666 is a potent and selective protein arginine methyltransferase 5 (PRMT5) inhibitor (IC50 = 22 nM, Ki = 5 nM). Displays selectivity for PRMT5 over a panel of 20 other protein methyltransferases. Exhibits dose-dependent antitumor effects in multiple mantle cell lymphoma (MCL) xenograft models. Orally bioavailable.

Compound Libraries for EPZ 015666

EPZ 015666 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Epigenetics Library. Find out more about compound libraries available from Tocris.

Technical Data for EPZ 015666

M. Wt 383.44
Formula C20H25N5O3
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1616391-65-1
PubChem ID 90241673
InChI Key ZKXZLIFRWWKZRY-KRWDZBQOSA-N
Smiles O[C@H](CN1CCC2=CC=CC=C2C1)CNC(C3=NC=NC(NC4COC4)=C3)=O

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 EPZ 015666

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 38.34 100
ethanol 19.17 50

Preparing Stock Solutions for EPZ 015666

The following data is based on the product molecular weight 383.44. 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
1 mM 2.61 mL 13.04 mL 26.08 mL
5 mM 0.52 mL 2.61 mL 5.22 mL
10 mM 0.26 mL 1.3 mL 2.61 mL
50 mM 0.05 mL 0.26 mL 0.52 mL

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

References for EPZ 015666

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

Duncan et al (2015) Structure and property guided design in the identification of PRMT5 tool compound EPZ015666. ACS Med.Chem.Lett. 7 162 PMID: 26985292

Chan-Penebre et al (2015) A selective inhibitor of PRMT5 with in vivo and in vitro potency in MCL models. Nat.Chem.Biol. 11 432 PMID: 25915199

If you know of a relevant reference for EPZ 015666, please let us know.

View Related Products by Target

View Related Products by Product Action

View all Protein Arginine Methyltransferase Inhibitors

Keywords: EPZ 015666, EPZ 015666 supplier, EPZ015666, GSK3235025, potent, selective, PRMT5, protein, arginine, methytransferase, 5, inhibitors, inhibits, Protein, Arginine, Methyltransferases, 6516, Tocris Bioscience

1 Citation for EPZ 015666

Citations are publications that use Tocris products. Selected citations for EPZ 015666 include:

Omar et al (2019) Therapeutic Targeting of RNA Splicing Catalysis through Inhibition of Protein Arginine Methylation. Cancer Cell 36 194-209.e9 PMID: 31408619

Do you know of a great paper that uses EPZ 015666 from Tocris? Please let us know.

Reviews for EPZ 015666

There are currently no reviews for this product. Be the first to review EPZ 015666 and earn rewards!

Have you used EPZ 015666?

Submit a review and receive an Amazon gift card.

$50/€35/£30/$50CAN/¥300 Yuan/¥5000 Yen for first to review with an image

$25/€18/£15/$25CAN/¥75 Yuan/¥2500 Yen for a review with an image

$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image

Submit a Review

Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.

Epigenetics Scientific Review

Epigenetics Scientific Review

Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.