KZR-504是具有口服活性的、高度选择性的免疫原体低分子质量多肽2(LMP2)的抑制剂、其对LMP2和LMP7的IC50值分别为51nM,4.274μM。
货号:ajcx12686
CAS:1629052-78-3
分子式:C21H23N3O6
分子量：413.42
溶解度:Soluble in DMSO
纯度：98%
存储：Store at -20°C
库存：现货

Background:

KZR-504 is a highly selective and orally active inhibitor of immunoproteasome low molecular mass polypeptide 2 (LMP2), with IC50s of 51 nM, 4.274 μM for LMP2 and LMP7, respectively.

Evaluating the inhibition of LMP2, and antitargets LMP7 and β5, in mouse tissues reveals that KZR-504 (compound 12) is both selective and potent in vivo with >50% target inhibition achieved at >1 mg/kg in all tissues tested except brain[1].

[1]. Johnson HWB, et al. Discovery of Highly Selective Inhibitors of the Immunoproteasome Low Molecular Mass Polypeptide 2 (LMP2) Subunit. ACS Med Chem Lett. 2017 Mar 9;8(4):413-417.