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Products are for research use only. Not for human use. We do not sell to patients.
(UNC-1999; UNC 1999)
UNC1999 Chemical Structure
|Product name: UNC1999|
|Cat. No.: HY-15646|
UNC1999 is a potent, orally bioavailable and selective inhibitor of EZH2 and EZH1 with IC50 of 2 nM and 45 nM, respectively.
IC50 Value: 2 nM(EZH2); 45 nM(EZH1)
UNC1999 was the first orally bioavailable EZH2 inhibitor that has high in vitro potency for wild-type and mutant EZH2 as well as EZH1, UNC1999 was highly selective for EZH2 and EZH1 over a broad range of epigenetic and non-epigenetic targets, competitive with the cofactor SAM and non-competitive with the peptide substrate. This inhibitor potently reduced H3K27me3 levels in cells and selectively killed diffused large B cell lymphoma cell lines harboring the EZH2Y641N mutant. Importantly, UNC1999 was orally bioavailable in mice, making this inhibitor a valuable tool for investigating the role of EZH2 and EZH1 in chronic animal studies. We also designed and synthesized UNC2400, a close analogue of UNC1999 with potency >1,000-fold lower than that of UNC1999 as a negative control for cell-based studies .
|M.Wt||569.74||Storage||Please store the product under the recommended conditions in the Certificate of Analysis.|
|Solvent & Solubility||
10 mM in DMSO
|1 mg||5 mg||10 mg|
|1 mM||1.7552 mL||8.7759 mL||17.5519 mL|
|5 mM||0.3510 mL||1.7552 mL||3.5104 mL|
|10 mM||0.1755 mL||0.8776 mL||1.7552 mL|