| Identification | Back Directory | [Name]
KZR-504 | [CAS]
1629052-78-3 | [Synonyms]
KZR-504
D-erythro-3-Pentulose, 4,5-anhydro-1,2-dideoxy-2-[[(2S)-2-[[(1,6-dihydro-6-oxo-2-pyridinyl)carbonyl]amino]-3-hydroxy-1-oxopropyl]amino]-4-C-methyl-1-phenyl- | [Molecular Formula]
C21H23N3O6 | [MDL Number]
MFCD31746873 | [MOL File]
1629052-78-3.mol | [Molecular Weight]
413.43 |
| Chemical Properties | Back Directory | [Boiling point ]
828.9±65.0 °C(Predicted) | [density ]
1.362±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C, protect from light, stored under nitrogen | [solubility ]
Soluble in DMSO | [form ]
Solid | [pka]
9.07±0.10(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
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]. | [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[1]. | [storage]
Store at -20°C, protect from light, stored under nitrogen | [References]
[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. DOI:10.1021/acsmedchemlett.6b00496 |
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