JQEZ5


CAS No. : 1913252-04-6

1913252-04-6
Price and Availability of CAS No. : 1913252-04-6
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10mg $140 In-stock
25mg $270 In-stock
50mg $400 In-stock
100mg $580 In-stock
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Cat. No. : HY-100846
M.Wt: 542.68
Formula: C30H38N8O2
Purity: >98 %
Solubility: DMSO : 25 mg/mL (ultrasonic)
Introduction of 1913252-04-6 :

JQEZ5 is a potent and selective EZH2 lysine methyltransferase inhibitor. JQEZ5 SAM-competitively inhibits polycomb repressive complex 2 (PRC2) with an IC50 of 80 nM. JQEZ5 has anti-tumor effects[1]. IC50 & Target:EZH2[1] In Vitro:JQEZ5 inhibits enzymatic functionality of PRC2 with a biochemical IC50 of 80nM. JQEZ5 exhibits S-adenosyl methionine (SAM)-competitive inhibition of PRC2[1].
H661 cells treated with increasing concentrations of JQEZ5 demonstrate acutely reduced levels of H3K27me3 without affecting H3K27 mono- or di-methylation. JQEZ5 suppresses the proliferation of EZH2-overexpressing H661 and H522 cells after treatment for 4 days without affecting the proliferation of cell lines that were deemed insensitive to EZH2 knockdown[1]. In Vivo:JQEZ5 (75 mg/kg; intraperitoneal injection; daily; for 3 weeks) treatment exhibits rapid and pronounced tumor regression over the three week treatment course. And H3K27me3 levels are largely reduced with treatment further confirming the on-target effect of JQEZ5 in mice[1].

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