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Datasheet of EPZ020411 HCl
Description: EPZ020411 is a potent inhibitor of PRMT6 in biochemical (IC50 = 10 nM) and cellular (IC50 = 600 nM) assays. EPZ020411 is selective against the related enzymes PRMT3, PRMT4, PRMT5, and PRMT7 in a biochemical assay, and relatively selective against PRMT1 and PRMT8. In biochemical (IC50s = 100 and 200 nM, respectively) and cellular assays (for PRMT1). Even though EPZ020411 is selective within the PRMT family, there is no information on other relevant human methyltransferases.EPZ020411 is not greatly selective for PRMT6 over PRMT1 or PRMT8 in vitro. PRMT6 is the only PRMT known to methylate the H3R2 position, and EPZ020411 can be used as a probe to assess the functionality of this post-translational modification. While this compound shows poor bioavailability following oral dosing (<5%), subcutaneous (SC) dosing results in significant plasma levels, making this compound suitable for in vivo studies of the H3R2 mark using SC dosing.
.Chemical Information Catalog
DC9822
Purity of current batch:
>98%
Molecular Weight (MW)
479.3
Molecular Formula
C25H38N4O3.HCl
CAS No.
1700663-41-7
Solubility (25°C)
DMSO
Storage
Store at -20°C (desiccating conditions).
Handling: Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to 24 months. Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.