EPZ015666 (GSK3235025), PRMT5 Inhibitor


Catalog No. size PriceQuantity
M60254-2S 2 mg solid $129
M60254-10S 10 mg solid $529

Description

Product Information
Molecular Weight: 383.44
Formula: C20H25N5O3
Purity: ≥98%
CAS#: 1616391-65-1
Solubility: DMSO and EtOH up to 100 mM
Chemical Name: (S)-N-(3-(3,4-dihydroisoquinolin-2(1H)-yl)-2-hydroxypropyl)-6-(oxetan-3-ylamino)pyrimidine-4-carboxamide
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

Biological Activity:

EPZ015666 is a potent, selective and orally bioavailable Protein arginine methyltransferase-5 (PRMT5) Inhibitor with Ki of 5 nM. It has >20,000-fold selectivity over other PMTs. It showed competitive inhibition with respect to the peptide substrate, not SAM. Treatment of MCL cell lines with EPZ015666 led to inhibition of SmD3 methylation and cell death, with IC50 values in the nanomolar range. Oral dosing with EPZ015666 demonstrated dose-dependent antitumor activity in multiple MCL xenograft models. EPZ015666 represents a validated chemical probe for further study of PRMT5 biology and arginine methylation in cancer and other diseases.

How to Use:


In vitro:
 EPZ015666 was used at 5 µM final concentration in various in vitro assays.
In vivo:
 EPZ015666 was dosed to MCL (Z-138, and Maver-1) xenograft animal models orally at 200 mg/Kg once per day.

Reference:

  • 1. Chan-Penebre E, et al. A selective inhibitor of PRMT5 with in vivo and in vitro potency in MCL models. (2015) Nat Chem Biol. In press. 


Products are for research use only. Not for human use.

Payment & Security

American Express Apple Pay Diners Club Discover Elo Google Pay JCB Mastercard PayPal Shop Pay Venmo Visa

Your payment information is processed securely. We do not store credit card details nor have access to your credit card information.

Estimate shipping

You may also like

Recently viewed