ME0328

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

ME0328 是一种有效的选择性 PARP 抑制剂，对 PARP3 的 IC50 为 0.89 μM，选择性约为 PARP1 的 7 倍。

ME0328 is an inhibitor of PARP-3 (IC50 = 0.89 μM). ME0328 displays selectivity for PARP-3 over PARP-1, PARP-2 and other ARDT enzymes (IC50 values are 6.3, 10.8 and >30 μM respectively). ME0328 also enhances CRISPR-Cas9-mediated HER2 mutation frequency, resulting in increased reduction in proliferation of HER2-positive breast cancer cells.(In Vitro):ME0328 is a potent and selective inhibitor of ARTD3/PARP3 that is active in cells. In in vitro histone H1 modification assay, ME0328 inhibits the transferase activity of ARTD3 with an IC50 of 0.89±0.28 μM. In human A549 cells, ME0328 and ME0355 (at 10 μM) delay the resolution of γH2AX-containing foci that serve as markers for DNA double strand break repair following γ-irradiation (2 Gy). In silico and in vitro physicochemical and metabolic profiling indicated that ME0328 is soluble, cell permeable, and metabolically stable in human liver microsomes and rat hepatocytes.

ME0328 is a potent and selective inhibitor of ARTD3/PARP3 that is active in cells. In in vitro histone H1 modification assay, ME0328 inhibits the transferase activity of ARTD3 with an IC50 of 0.89±0.28 μM. In human A549 cells, ME0328 and ME0355 (at 10 μM) delay the resolution of γH2AX-containing foci that serve as markers for DNA double strand break repair following γ-irradiation (2 Gy). In silico and in vitro physicochemical and metabolic profiling indicated that ME0328 is soluble, cell permeable, and metabolically stable in human liver microsomes and rat hepatocytes.

——

ME0328 | ME 0328 | ME-0328

Proteasome/Ubiquitin

Tyrosinase

PARP1| PARP3

Others-Field

——

1445251-22-8

321.37

C19H19N3O2

>98% (HPLC)

DMSO : 75 mg/mL. 233.38 mM;H2O : < 0.1 mg/mL

C[C@H](NC(=O)CCC1=NC2=CC=CC=C2C(=O)N1)C1=CC=CC=C1

3-(4-oxo-1H-quinazolin-2-yl)-N-[(1S)-1-phenylethyl]propanamide

(-20℃)

With Ice Pack

≥ 2 years