EPIC-0307 | PRADX-EZH2 inhibitor | Probechem Biochemicals

Chemical Structure : EPIC-0307

EPIC-0307 (EPIC 0307)

Catalog No.: 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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Biological Activity

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.

Physicochemical Properties

M.Wt	416.54
Formula	C25H24N2O2S
Appearance	Solid
CAS No.
Storage	Solide Powder -20°C 12 Months; 4°C 6 Months	In Solvent -80°C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	6-methyl-3-(((thiophen-2-ylmethyl)amino)methyl)-1-(4-vinylbenzyl)-1H-indole-2-carboxylic acid

References

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

EPIC-0307 (EPIC 0307)

Biological Activity

Physicochemical Properties

References

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