Carfilzomib - CAS 868540-17-4
Catalog number:
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
Molecular Weight:
Carfilzomib is a tetrapeptide epoxyketone and an analog of epoxomicin, acting as a selective proteasome inhibitor, such as the chymotrypsin-like β5 subunit of the constitutive 20S proteasome (IC50 = 5.2 nM) and the β5i subunit of the immunoproteasome 20Si (LMP7; IC50 = 14 nM).
Ordering Information
Catalog Number Size Price Stock Quantity
B0084-305419 250 mg $198 In stock
Bulk Inquiry
Publictions citing BOC Sciences Products
  • >> More
1. Enantioselective synthesis of adamantylalanine and carboranylalanine and their incorporation into the proteasome inhibitor bortezomib
Gerjan de Bruin, Elliot D. Mock, Sascha Hoogendoorn, Herman S. Overkleeft*. Chem. Commun., 2016, 52, 4064—4067
The ubiquitin proteasome system (UPS) is responsible for the degradation of 80–90% of the proteins in eukaryotic cells. E1–E2–E3 enzymes canmodify a protein destined for degradation with a poly-ubiquitin chain, which is recognized by the 19S cap of the 26S proteasome. The 19S cap removes the ubiquitin chain and unfolds the protein, which is then translocated in the 20S core particle (CP), where proteolysis takes place. The hollow cylindrical shaped CP is composed out of four heptameric rings: two outer a-rings and two inner b-rings. The catalytic activities residues within the b-subunits: β1 (caspase-like, cleaves after acidic residues), β2 (trypsin-like, cleaves after basic residues) andβ5 (chymotrypsin-like, cleaves after hydrophobic residues). Next to the constitutively expressed cCP (β1c, β2c andβ5c) subunits, immune cells also express b-subunits with slightly altered substrate specificities (iCP: β1i, β2i andβ5i). Two proteasome inhibitors (PIs) are currently used in the clinic for the treatment of multiple myeloma (MM) and mantle cell lymphoma, namely bortezomib (Btz) and carfilzomib (Cfz), and several PIs are being evaluated in clinical trials. PIs can provide useful information on the substrate specificity of eachβ-subunit. The S1 and S3 pockets mainly determine the substrate specificities for each b-subunit.
2. Exploring dual electrophiles in peptide-based proteasome inhibitors: carbonyls and epoxides
Bo-Tao Xin, Gerjan de Bruin, Martijn Verdoes, Herman S. Overkleeft*. Org. Biomol. Chem.,2014, 12,5710–5718
Carfilzomib is a member of the family of peptide epoxyketone proteasome inhibitors. The first compound identified in this class is the natural product; epoxomicin. Epoxomicin features an epoxyketone electrophilic trap, also referred to as the warhead, which renders this compound highly selective towards the proteasome catalytic sites. Proteasome catalytic activities are characterized by an N-terminal threonine in which the hydroxyl acts as the nucleophile with the amine as catalytic base. Such catalytic sites are rare in nature and peptide epoxyketones appear ideally suited to react with the 1,2-amino-alcohol moiety in these N-terminal threonine residues. In the inhibition mechanism, the carbonyl of the epoxyketone warhead is first attacked by the N-terminal threonineγ-hydroxyl (Fig. 2) after which the α-amine attacks the epoxide ring, resulting in morpholine ring formation.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related Proteasome Products

CAS 110044-82-1 MG-101

(CAS: 110044-82-1)

MG-101, also known as Calpain Inhibitor I and ALLN, is a calpain inhibitor (IC50 = 0.09 μM) that activates p53-dependent apoptosis in tumor cell lines. Activiti...

CAS 960374-59-8 ONX-0914

(CAS: 960374-59-8)

ONX 0914 is an immunoproteasome inhibitor with potential treatment applications in autoimmune disorders, such as rheumatoid arthritis, inflammatory bowel diseas...

CAS 179461-52-0 PD 151746

PD 151746
(CAS: 179461-52-0)

PD 151746 is a selective, cell-permeable calpain inhibitor with Ki of 0.26 μM for μ-Calpain, about 20-fold selectivity over m-calpain.

CAS 935888-69-0 Oprozomib

(CAS: 935888-69-0)

Oprozomibm, also known as ONX 0912 and PR 047, is an orally bioavailable proteasome inhibitor with potential antineoplastic activity. ONX 0912 inhibits the act...

(CAS: 856849-35-9)

AM 114 is an inhibitor of chymotrypsin-like activity of the 20S proteasome. In addition, AM-114 shows anticancer activity, It can inhibit cell growth in human c...

CAS 1617495-03-0 RA190

(CAS: 1617495-03-0)

RA190, a bis-benzylidine piperidon, is a novel potent and selective inhibitor of proteasome ubiquitin receptor RPN13/ADRM1. RA190 stabilized targets of human pa...

CAS 1401223-22-0 PI-1840

(CAS: 1401223-22-0)

PI-1840 potently inhibits proteasomal CT-L activity with IC50 of 0.37 μM in intact human MDA-MB-468 cancer cells, and inhibits proliferation/survival of human M...

CAS 1072833-77-2 MLN-2238

(CAS: 1072833-77-2)

MLN-2238 is the biologically active form of MLN9708. MLN2238 has an improved pharmacodynamic profile and antitumor activity compared with bortezomib in both OCI...

CAS 329-98-6 PMSF

(CAS: 329-98-6)

PMSF is an irreversible serine/cysteine protease inhibitor.

CAS 133407-82-6 MG-132

(CAS: 133407-82-6)

MG-132 is a potent Proteasome inhibitor with potential anticancer activity. MG-132 induces MCPIP1 expression; induces C6 glioma cell apoptosis via oxidative str...

CAS 868540-17-4 Carfilzomib

(CAS: 868540-17-4)

Carfilzomib is a tetrapeptide epoxyketone and an analog of epoxomicin, acting as a selective proteasome inhibitor, such as the chymotrypsin-like β5 subunit of t...

CAS 1211877-36-9 MG-132(S,R,S)

(CAS: 1211877-36-9)

MG-132(S,R,S) is a reversible, cell permeable and selective tripeptide aldehyde proteasome inhibitor (IC50 = 0.22 μM), the most potent stereoisomer of MG-132. I...

Ixazomib citrate
(CAS: 1239908-20-3)

The citrate salt form of Ixazomib which is a proteasome inhibitor. It is considered a rollover Phase II trial against multiple myeloma, amyloidosis and lymphoma...

(CAS: 1624602-30-7)

VR23 is a potent and selective inhibitor of trypsin-like proteasomes (IC50 = 1 nmol/L), chymotrypsin-like proteasomes (IC50 = 50-100 nmol/L), and caspase-like p...

CAS 134381-21-8 Epoxomicin

(CAS: 134381-21-8)

Epoxomicin is a potent anti-tumor agent isolated from Actinomycetes that is used as a selective and irreversible inhibitor of the 20S proteasome. It inhibits pr...

CAS 847499-27-8 Delanzomib

(CAS: 847499-27-8)

Delanzomib, also known as CEP-18770, is An orally bioavailable synthetic P2 threonine boronic acid inhibitor of the chymotrypsin-like activity of the proteasom...

CAS 179324-69-7 Bortezomib (PS-341)

Bortezomib (PS-341)
(CAS: 179324-69-7)

Bortezomib (PS-341) is a potent 20S proteasome inhibitor with Ki of 0.6 nM.

CAS 921625-62-9 Cysteine Protease inhibitor

Cysteine Protease inhibitor
(CAS: 921625-62-9)

Cysteine Protease inhibitor is a inhibitor of cysteine protease.

Chemical Structure

CAS 868540-17-4 Carfilzomib

Quick Inquiry

Verification code

Featured Items