Carfilzomib - CAS 868540-17-4
Catalog number:
B0084-305419
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C40H57N5O7
Molecular Weight:
719.91
COA:
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Targets:
Proteasome
Description:
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
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Purity:
>98%
Synonyms:
PR-171
MSDS:
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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.
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