Chemical Structure : EPIC-0307
货号: PC-20906Not For Human Use, Lab Use Only.
EPIC-0307 is a selective small-molecule inhibitor of PRADX-EZH2 interaction, inhibits GBM cell lines with IC50 of 12.13-17.69 uM, enhances temozolomide (TMZ) sensitivity to glioblastoma.
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EPIC-0307 is a selective small-molecule inhibitor of PRADX-EZH2 interaction, inhibits GBM cell lines with IC50 of 12.13-17.69 uM, enhances temozolomide (TMZ) sensitivity to glioblastoma.
EPIC-0307 shows no activity against NEAT1, MEG3, MALATI, HOXA11AS, KCNQ10T1, HOTAIR, XIST, H19, that reportedly bind to EZH2.
EPIC-0307 upregulates P21 and PUMA expressions, leading to cell cycle arrest and apoptosis.
EPIC-0307 enhances the sensitization of GBM cells to TMZ via modulation of DNA damage and repair in MGMT-negative cells.
TMZ (5 mg/kg) + EPIC-0307 (7.5 mg/kg) by gavage for 2 weeks, EPIC-0307 increases the TMZ sensitivity in MGMT-negative tumors in vivo.
EPIC-0307 inhibits TMZ-induced DNA DSB repair by downregulating CHK1, CHK2, RAD50, RAD51, and MRE11.
分子量 | 416.54 | |
分子式 | C25H24N2O2S | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
1. Lei Xin, et al. Neuro Oncol. 2023 Jun 5;noad102.
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