General
Preferred name
BORTEZOMIB
Synonyms
LDP-341,PS-341 ()
NSC681239 ()
Velcade ()
Brotezamide ()
DPBA ()
LDP 341 ()
MG 341 ()
NSC 681239 ()
Radiciol ()
Bortezomib (Velcade) ()
S1013 ()
B1875 ()
PS-341 ()
LDP-341 ()
Bortezomib (PS-341) ()
Velcade, LDP-341, MLM341, NSC 681239,PS-341 ()
Bortezomib accord ()
Bortezomib hydrate ()
NSC-681239 ()
P&D ID
PD003632
CAS
179324-69-7
Tags
covalent binder
nuisance
natural product
drug
available
Approved by
PMDA
EMA
FDA
First approval
2003
Drug Status
investigational
approved
Drug indication
Mantle cell lymphoma
Multiple myeloma
Non-hodgkin lymphoma
Max Phase
Phase 4
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION Bortezomib is a dipeptide (Phe-Leu), with a pyrazinoic acid protecting the N-terminus and a boronic acid replacing the C-terminal carboxylic acid. The boron atom is believed to interact with and inactivate the catalytic site on β subunits which form the active core of the proteasome, preferentially binding β5 active site . Bortezomib is the first-in-class proteasome inhibitor to be approved for clinical use.
Proteasome activity is reviewed in .

The compound also has antimalarial activity. The Malaria tab on this ligand page provides additional curator comments of relevance to the Guide to MALARIA PHARMACOLOGY. (GtoPdb)
DESCRIPTION inhibitor of 26S proteasome (Informer Set)
DESCRIPTION Potent and selective PIKfyve inhibitor (Tocris Bioactive Compound Library)
Cell lines
404
Organisms
1
Compound Sets
40
AdooQ Bioactive Compound Library
A10160
Axon Medchem Screening Library
1810
Bioprocess diversity set
Cayman Chemical Bioactives
10008822
CeMM library of unique drugs (CLOUD)
ChEMBL Approved Drugs
CHEMBL325041
ChEMBL Drugs
CHEMBL325041
Concise Guide to Pharmacology 2017/18
6391
Concise Guide to Pharmacology 2019/20
6391
Concise Guide to Pharmacology 2021/22
6391
Concise Guide to Pharmacology 2023/24
6391
CovalentInDB
CI006008
CovBinderInPDB
CBR000902
CBR001076
CBR001077
CBR001078
CBR001079
CBR002868
CBR002869
CBR002870
CBR002871
CBR002872
CBR002873
CBR002874
CBR002875
CBR002876
CBR002877
CBR002878
CBR002879
CBR002880
CBR002881
CBR002882
CBR002883
CBR002884
CBR002885
CBR002886
CBR002887
CBR002888
CBR002889
CBR002890
CBR002891
CBR002892
CBR002893
CBR002894
CBR002895
CBR002896
CBR002897
CBR002902
CBR002903
CBR002904
CBR002905
CBR002906
CBR002907
CBR002908
CBR002909
CBR002910
CBR002911
CBR002912
CBR002913
CBR002914
CBR002915
CBR002916
CBR002917
CBR002918
CBR002919
CBR003404
CBR003405
CBR003406
CBR003407
CBR003408
CBR003409
CBR003780
CBR003781
CBR003782
CBR003783
CBR003784
CBR003785
CBR003883
CBR003884
CBR003885
CBR003886
CBR003887
CBR003888
CBR004773
CBR004774
CBR004775
CBR004776
CBR004777
CBR004778
CBR004832
CBR004833
CBR004834
CBR004835
CBR004836
CBR004837
CBR005180
CBR005181
CBR005182
CBR005183
CBR005184
CBR005185
CBR005186
CBR005187
CBR005188
CBR005189
CBR005190
CBR005191
CBR005359
CBR005360
CBR005361
CBR005362
CBR005363
CBR005364
CBR005414
CBR005415
CBR005416
CBR005417
CBR005418
CBR005419
CBR005433
CBR005434
CBR005435
CBR005436
CBR005437
CBR005438
CBR005449
CBR005450
CBR005451
CBR005452
CBR005453
CBR005454
CBR005552
CBR006473
CBR006474
CBR006475
CBR006476
CBR006477
CBR006478
CBR006479
CBR006480
CBR006481
CBR006482
CBR006483
CBR006484
CBR006485
CBR006649
CBR006650
CBR006651
CBR006652
CBR006653
CBR006654
CBR006673
CBR006674
CBR006675
CBR006676
CBR006677
CBR006678
CBR007102
CBR007103
CBR007104
CBR007105
CBR007106
CBR007107
CBR007294
CBR007295
CBR007296
CBR007297
CBR007298
CBR007299
Drug Repurposing Hub
DrugBank
DB00188
DrugBank Approved Drugs
DB00188
DrugCentral
391
DrugCentral Approved Drugs
391
DrugMAP
DMNO38U
DrugMAP Approved Drugs
DMNO38U
Enamine BioReference Compounds
EU-OPENSCREEN Bioactive Compound Library
EOS101809
Guide to Pharmacology
6391
Informer Set
411737
LINCS compound set
10241-101
LSP-MoA library (Laboratory of Systems Pharmacology)
CHEMBL325041
MedChem Express Bioactive Compound Library
HY-10227
Natural product-based probes and drugs
NCATS Inxight Approved Drugs
69G8BD63PP
NIH Approved Oncology Drugs
Novartis Chemogenetic Library (NIBR MoA Box)
NPC Screening Collection
Nuisance compounds in cellular assays
Other bioactive compounds
Reference compounds for characterizing cellular injury in high-content cellular morphology assays
ReFrame library
Selleckchem Bioactive Compound Library
Bortezomib
TargetMol Bioactive Compound Library
T2399
Tocris Bioactive Compound Library
7282
Welcome Trust Cancer Drugs
104
External IDs
59
Properties
(calculated by RDKit )
Molecular Weight
384.2
Hydrogen Bond Acceptors
6
Hydrogen Bond Donors
4
Rotatable Bonds
9
Ring Count
2
Aromatic Ring Count
2
cLogP
0.36
TPSA
124.44
Fraction CSP3
0.37
Chiral centers
2.0
Largest ring
6.0
QED
0.46
Structural alerts
1
Protein disruption
Proteosome inhibition
Nuisance compounds in cellular assays
Related compounds
Custom attributes
(extracted from source data)
Target
PSMB1
PSMB2
PSMB5
PSMD1
PSMD2
Proteasome
26S proteosome
20S proteasome
PSMA1, PSMA2, PSMA3, PSMA4, PSMA5, PSMA6, PSMA7, PSMA8, PSMB1, PSMB10, PSMB11, PSMB2, PSMB3, PSMB4, PSMB5, PSMB6, PSMB7, PSMB8, PSMB9, PSMD1, PSMD2, RELA
Autophagy,Cathepsin B,Cysteine Protease,ERK,NF-¦ÊB,Proteasome
Compound status
FDA
Biological process
Protein degradation
MOA
Proteasome inhibitor
Inhibitor
Proteasome Inhibitors
Apoptosis Inducers
Caspase 3 Activators
NF-kappaB (NFKB) Activation Inhibitors
NFkB pathway inhibitor, proteasome inhibitor
Pathway
Proteases/Proteasome
Ubiquitination
NF-¦ÊB
Apoptosis
Autophagy
Metabolic Enzyme/Protease
NF-κB
Member status
virtual
Indication
multiple myeloma, mantle cell lymphoma (MCL)
Therapeutic Indication
Anticancer
Therapeutic Class
Anticancer Agents
Source data