KZR-504

Research use only, not for human use.

KZR-504 (KZR504) is a potent, highly selective inhibitor of immunoproteasome low molecular polypeptide-2 (LMP-2) subunit with IC50 of 51 nM.

KZR-504 (KZR504) is a potent, highly selective inhibitor of immunoproteasome low molecular polypeptide-2 (LMP-2) subunit with IC50 of 51 nM; displays >100-fold selectivity over β1, LMP7, β5, MECL1 and β2 subunits; shows little to no effect on cytokine production in human peripheral blood mononuclear cells (PBMCs) stimulated with LPS, and can be administered at a selective dose in vivo.

——

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.

KZR 504 | KZR504

Proteasome/Ubiquitin

Proteasome

Proteasome

——

——

1629052-78-3

413.43

C21H23N3O6

>98% (HPLC)

In Vitro:?DMSO : 170 mg/mL (411.20 mM)

O=C(C1=CC=CC(N1)=O)N[C@@H](CO)C(N[C@@H](CC2=CC=CC=C2)C([C@]3(C)OC3)=O)=O

N-((S)-3-hydroxy-1-(((S)-1-((S)-2-methyloxiran-2-yl)-1-oxo-3-phenylpropan-2-yl)amino)-1-oxopropan-2-yl)-6-oxo-1,6-dihydropyridine-2-carboxamide

(-20℃)

With Ice Pack

≥ 2 years