For research use only. Not for therapeutic Use.
KZR-504 is a highly selective inhibitor of immunoproteasome low molecular mass polypeptide 2 (LMP2), with IC50s of 51 nM, 4.274 μM for LMP2 and LMP7, respectively. KZR-504 is of interest for the treatment of autoimmune disease[1].
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].
| Catalog Number | I019773 |
| CAS Number | 1629052-78-3 |
| Synonyms | N-[(2S)-3-hydroxy-1-[[(2S)-1-[(2R)-2-methyloxiran-2-yl]-1-oxo-3-phenylpropan-2-yl]amino]-1-oxopropan-2-yl]-6-oxo-1H-pyridine-2-carboxamide |
| Molecular Formula | C21H23N3O6 |
| Purity | ≥95% |
| InChI | InChI=1S/C21H23N3O6/c1-21(12-30-21)18(27)15(10-13-6-3-2-4-7-13)23-20(29)16(11-25)24-19(28)14-8-5-9-17(26)22-14/h2-9,15-16,25H,10-12H2,1H3,(H,22,26)(H,23,29)(H,24,28)/t15-,16-,21+/m0/s1 |
| InChIKey | QYDASSGXBXGRBS-CKJXQJPGSA-N |
| SMILES | CC1(CO1)C(=O)C(CC2=CC=CC=C2)NC(=O)C(CO)NC(=O)C3=CC=CC(=O)N3 |
| Reference | [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. |
