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首页-小分子抑制剂&激动剂-Epigenetics-Histone Methyltransferase (HMTase)-EPIC-0307
EPIC-0307

Chemical Structure : EPIC-0307

CAS No.: 894949-88-3

EPIC-0307 (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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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

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.

物理化学性质&存储条件

分子量 416.54
分子式 C25H24N2O2S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

O=C(C(N1CC2=CC=C(C=C)C=C2)=C(CNCC3=CC=CS3)C4=C1C=C(C)C=C4)O

参考文献

1. Lei Xin, et al. Neuro Oncol. 2023 Jun 5;noad102.

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