KZR-504( KZR 504 | KZR504 )

Catalog No. M12437 CAS No. 1629052-78-3

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

KZR-504
Note

Research use only, not for human use.
Brief Description

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

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.
In Vitro

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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.
Synonyms

KZR 504 | KZR504
Pathway

Proteasome/Ubiquitin
Target

Proteasome
Recptor

Proteasome
Research Area

——
Indication

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CAS Number

1629052-78-3
Formula Weight

413.43
Molecular Formula

C21H23N3O6
Purity

>98% (HPLC)
Solubility

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

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
Chemical Name

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

1. Johnson HWB, et al. ACS Med Chem Lett. 2017 Mar 9;8(4):413-417.

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