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KZR-616 , CAS No.1629677-75-3, Inhibitor of proteasome 20S subunit beta 2;Inhibitor of proteasome 20S subunit beta 5;Inhibitor of proteasome 20S subunit beta 8;Inhibitor of proteasome 20S subunit beta 9

Item Number
K611367
Grouped product items
SKUSizeAvailabilityPrice Qty
K611367-5mg
5mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$660.90
K611367-25mg
25mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$2,300.90
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proteasome 20S subunit beta 2 Inhibitor proteasome 20S subunit beta 5 Inhibitor proteasome 20S subunit beta 8 Inhibitor proteasome 20S subunit beta 9 Inhibitor

Basic Description

SynonymsZetomipzomib | KZR-616 | 1629677-75-3 | UNII-O4BT6C02M2 | O4BT6C02M2 | (2S,3R)-N-[(2S)-3-(cyclopenten-1-yl)-1-[(2R)-2-methyloxiran-2-yl]-1-oxopropan-2-yl]-3-hydroxy-3-(4-methoxyphenyl)-2-[[(2S)-2-[(2-morpholin-4-ylacetyl)amino]propanoyl]amino]propanamide | D-Erythro-
Specifications & PurityMoligand™
GradeMoligand™
Action TypeINHIBITOR
Mechanism of actionInhibitor of proteasome 20S subunit beta 2;Inhibitor of proteasome 20S subunit beta 5;Inhibitor of proteasome 20S subunit beta 8;Inhibitor of proteasome 20S subunit beta 9

Associated Targets(Human)

PSMB9 Tchem Proteasome subunit beta type-9 (2 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
PSMB5 Tclin Proteasome subunit beta type-5 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
PSMB2 Tclin Proteasome subunit beta type-2 (2 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
PSMB10 Tchem Proteasome subunit beta type-10 (2 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
PSMB1 Tclin Proteasome subunit beta type-1 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
PSMB8 Tclin Proteasome subunit beta type-8 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
PBMC (10003 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PSMB2 Tclin Proteasome Macropain subunit (1025 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PSMB5 Tclin Proteasome Macropain subunit MB1 (2451 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PSMB8 Tclin Proteasome subunit beta type-8 (743 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PSMB10 Tchem Proteasome subunit beta type-10 (258 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

Mus musculus (284745 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PRE7 Proteasome component C5 (37 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Psmb9 Proteasome subunit beta type-9 (16 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Psmb5 Proteasome subunit beta type-5 (29 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Psmb2 Proteasome subunit beta type-2 (16 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Mechanisms of Action

Mechanism of ActionAction Typetarget IDTarget NameTarget TypeTarget OrganismBinding Site NameReferences

Names and Identifiers

IUPAC Name (2S,3R)-N-[(2S)-3-(cyclopenten-1-yl)-1-[(2R)-2-methyloxiran-2-yl]-1-oxopropan-2-yl]-3-hydroxy-3-(4-methoxyphenyl)-2-[[(2S)-2-[(2-morpholin-4-ylacetyl)amino]propanoyl]amino]propanamide
INCHI InChI=1S/C30H42N4O8/c1-19(31-24(35)17-34-12-14-41-15-13-34)28(38)33-25(26(36)21-8-10-22(40-3)11-9-21)29(39)32-23(16-20-6-4-5-7-20)27(37)30(2)18-42-30/h6,8-11,19,23,25-26,36H,4-5,7,12-18H2,1-3H3,(H,31,35)(H,32,39)(H,33,38)/t19-,23-,25-,26+,30+/m0/s1
InChi Key GHYOCDFICYLMRF-UTIIJYGPSA-N
Canonical SMILES CC(C(=O)NC(C(C1=CC=C(C=C1)OC)O)C(=O)NC(CC2=CCCC2)C(=O)C3(CO3)C)NC(=O)CN4CCOCC4
Isomeric SMILES C[C@@H](C(=O)N[C@@H]([C@@H](C1=CC=C(C=C1)OC)O)C(=O)N[C@@H](CC2=CCCC2)C(=O)[C@]3(CO3)C)NC(=O)CN4CCOCC4
Alternate CAS 1629677-75-3
PubChem CID 117607904
MeSH Entry Terms (2 S,3 R)- N-(( S)-3-(Cyclopent-1-en-1-yl)-1-(( R)-2-methyloxiran-2-yl)-1-oxopropan-2-yl)-3-hydroxy-3-(4-methoxyphenyl)-2-(( S)-2-(2-morpholinoacetamido)propanamido)propenamide;KZR-616

Certificates

Certificate of Analysis(COA)

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Related Documents

 SDS

 Specification Sheet

References

1. Johnson HWB, Lowe E, Anderl JL, Fan A, Muchamuel T, Bowers S, Moebius DC, Kirk C, McMinn DL.  (2018)  Required Immunoproteasome Subunit Inhibition Profile for Anti-Inflammatory Efficacy and Clinical Candidate KZR-616 ((2 S,3 R)- N-(( S)-3-(Cyclopent-1-en-1-yl)-1-(( R)-2-methyloxiran-2-yl)-1-oxopropan-2-yl)-3-hydroxy-3-(4-methoxyphenyl)-2-(( S)-2-(2-morpholinoacetamido)propanamido)propenamide)..  J Med Chem,  61  (24): (11127-11143).  [PMID:30380863] [10.1021/op500134e]
2. Fang Y, Johnson H, Anderl JL, Muchamuel T, McMinn D, Morisseau C, Hammock BD, Kirk C, Wang J.  (2021)  Role of epoxide hydrolases and cytochrome P450s on metabolism of KZR-616, a first-in-class selective inhibitor of the immunoproteasome..  Drug Metab Dispos,  71  (13): (1755-70).  [PMID:34234005] [10.1124/dmd.120.000307]

Solution Calculators

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