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About This Item
Empirical Formula (Hill Notation):
C22H31FN4O3S
CAS Number:
Molecular Weight:
450.57
UNSPSC Code:
12352200
Quality Level
Assay
≥94% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
-10 to -25°C
Biochem/physiol Actions
Potent and selective SETD2 inhibitor with anti-cancer efficacy.
EPZ-719 is a potent and selective SETD2 inhibitor (Ki/IC50 = 3.3/8 nM), being > 8000-fold more selective towards SETD2 over 14 other histone methyltransferases, including the mono/di-H3K36 methylases SMYD2 and WHSC1/MMSET/NSD2. EPZ-719 downregulates cellular H3K36 trimethylation level (IC50 = 23 nM, A549 cells) and shows potent anti-proliferative activity against multiple myeloma cell lines (IC50 in 14 days = 25 nM/KMS34, 11 nM/KMS211) and good pharmacokinetic properties in mice.
EPZ-719 is a potent and selective SETD2 inhibitor (Ki/IC50 = 3.3/8 nM), being > 8000-fold more selective towards SETD2 over 14 other histone methyltransferases, including the mono/di-H3K36 methylases SMYD2 and WHSC1/MMSET/NSD2. EPZ-719 downregulates cellular H3K36 trimethylation level (IC50 = 23 nM, A549 cells) and shows potent anti-proliferative activity against multiple myeloma cell lines (IC50 in 14 days = 25 nM/KMS34, 11 nM/KMS211) and good pharmacokinetic properties in mice.
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