1. Epigenetics
  2. Histone Methyltransferase

EPZ015866 (Synonyms: GSK591; GSK3203591)

Cat. No.: HY-100235 Purity: 98.71%
Data Sheet SDS Handling Instructions

EPZ015866 (GSK591) is a potent selective inhibitor of the arginine methyltransferase PRMT5. It maintained excellent selectivity against other PMT enzymes observed with EPZ015666 [1].

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EPZ015866 Chemical Structure

EPZ015866 Chemical Structure

CAS No. : 1616391-87-7

Size Price Stock Quantity
10 mM * 1 mL in DMSO $121 In-stock
5 mg $110 In-stock
10 mg $180 In-stock
25 mg $370 In-stock
50 mg $620 In-stock
100 mg $950 In-stock
200 mg   Get quote  
500 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

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  • References

Description

EPZ015866 (GSK591) is a potent selective inhibitor of the arginine methyltransferase PRMT5. It maintained excellent selectivity against other PMT enzymes observed with EPZ015666 [1]. IC50:61 nM-904 nM in Maver-1 cells [2] target: PRMT5 in vitro: A375 cells treated for 18 h with 1 μM EPZ015666 showed stabilization of PRMT5 in cellular thermal shift analysis in whole-cell lysates. [2] In vivo: EPZ015666 or vehicle (0.5% methylcellulose in water) was administered orally BID at a dose volume of 10 mL/kg for 21 d (Granta-519 was dosed for 18 d). [2]

References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 2.6283 mL 13.1413 mL 26.2826 mL
5 mM 0.5257 mL 2.6283 mL 5.2565 mL
10 mM 0.2628 mL 1.3141 mL 2.6283 mL
Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

380.48

Formula

C₂₂H₂₈N₄O₂

CAS No.

1616391-87-7

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Product Name:
EPZ015866
Cat. No.:
HY-100235
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