Proteasome

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Cat. No.	Product Name	Field of Application
DC11860	FV-162	A potent, orally bioavailable, irreversible proteasome inhibitor with potent antimyeloma activity (IC50<60 nM).
DC1027	Bortezomib (Velcade,MG-341,PS-341) Featured	Bortezomib is a potent 20S proteasome inhibitor with Ki of 0.6 nM.
DC1002	Carfilzomib (PR-171) Featured	Carfilzomib is an irreversible proteasome inhibitor with an IC50 of 5 nM in ANBL-6 and RPMI 8226 cells,showed potent activity against COVID-19(SARS-COV-2).
DCAPI1155	Celastrol Featured	Celastrol is a potent proteasome inhibitor for the chymotrypsin-like activity of a purified 20S proteasome with IC50 of 2.5 μM.
DC8481	Delanzomib(CEP-18770) Featured	Delanzomib(CEP-18770) is a novel orally-active inhibitor of the chymotrypsin-like activity of the proteasome that down-modulates the nuclear factor-kappaB (NF-kappaB) activity.
DC12332	KZR-504	KZR-504 is a highly selective and orally active inhibitor of immunoproteasome low molecular mass polypeptide 2 (LMP2), with IC50s of 51 nM, 4.274 μM for LMP2 and LMP7, respectively.
DC7702	MG-101 Featured	MG-101 is a calpain inhibitor (IC50 = 0.09 μM) that activates p53-dependent apoptosis in tumor cell lines.
DC7816	MG-132 Featured	MG-132 is an inhibitor of proteasome with IC50 of 100 nM, and also inhibits calpain with IC50 of 1.2 μM.
DC5086	Ixazomib(MLN2238) Featured	MLN2238 inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome with IC50 and Ki of 3.4 nM and 0.93 nM, respectively, also inhibits the caspase-like (β1) and trypsin-like (β2) proteolytic sites, with IC50 of 31 and 3500 nM.
DC5089	Ixazomib Citrate (MLN-9708) Featured	MLN-9708 is a proteasome inhibitor, which inhibits the activity of the proteasome, blocking the targeted proteolysis normally performed by the proteasome.
DC4243	ONX-0914	ONX 0914 is an immunoproteasome inhibitor with potential treatment applications in autoimmune disorders, such as rheumatoid arthritis, inflammatory bowel disease and lupus.
DC2010	Oprozomib (ONX-0912) Featured	Oprozomib (ONX 0912) selectively inhibits CT-L activity of 20S proteasome β5/LMP7 with IC50 of 36 nM/82 nM.
DC8283	PD 150606 Featured	PD 150606 is a selective, cell-permeable non-peptide calpain inhibitor (Ki values for ν and m-calpains are 0.21 and 0.37 μM respectively).
DC8747	PD 151746 Featured	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.
DC9611	PI-1840 Featured	PI-1840 is a potent and selective inhibitor for chymotrypsin-like (CT-L) (IC50 value = 27 ± 0.14 nM) over trypsin-like and peptidylglutamyl peptide hydrolyzing (IC50 values >100 μM) activities of the proteasome.
DC10304	RA190 Featured	RA190, a bis-benzylidine piperidon, inhibits proteasome function by covalently binding to cysteine 88 of ubiquitin receptor RPN13.
DC11125	TCH-165 Featured	TCH-165 is a specific small molecule modulator of proteasome assembly, regulates the dynamic equilibrium between the 20S and 26S proteasome complexes, favoring 20S-mediated protein degradation.
DC8448	VR23 Featured	VR-23 is a Quinoline-Sulfonyl Hybrid Proteasome Inhibitor That Selectively Kills Cancer via Cyclin E–Mediated Centrosome Amplification
DC28847	(1S,2S)-Bortezomib	(1S,2S)-Bortezomib is an enantiomer of Bortezomib. Bortezomib is a cell-permeable, reversible, and selective proteasome inhibitor, and potently inhibits 20S proteasome (Ki of 0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is an anti-cancer agent and the first therapeutic proteasome inhibitor to be used in humans.
DC29221	PTP1B-IN-9 Featured	PTP1B-IN-9 is a ubiquitin-proteasome system (UPS)-stressor. PTP1B-IN-9 inhibits ubiquitin-mediated protein degradation upstream of the 20S proteasomal catalytic activites. PTP1B-IN-9 triggers a ubiquitin-proteasome-system (UPS)-stress response without affecting 20S proteasome catalytic activities. Anticancer activity.
DC39096	MDL-28170 Featured	MDL-28170 (Calpain Inhibitor III) is a potent and selective calpain inhibitor of calpain that penetrates the blood-brain barrier and inhibits brain cysteine protease activity after systemic administration. MDL-28170 is also an inhibitor of γ-secretase.
DC40228	(Rac)-Calpain Inhibitor XII	(Rac)-Calpain Inhibitor XII is a reversible and selective inhibitor of calpain I (μ-calpain, Ki=19 nM), with lower affinities for calpain II (m-calpain, Ki=120 nM) and cathepsin B (Ki=750 nM). (Rac)-Calpain Inhibitor XII has been used to study the role of calpains in diverse processes, including neutrophil chemotaxis, neuronal signaling, and cardiac response to injury.
DC41571	Acetyl-Calpastatin(184-210)(human)	Acetyl-Calpastatin(184-210)(human) is a potent, selective and reversible calpain inhibitor with Ki values of 0.2 nM and 6 μM for μ-calpain and cathepsin L, respectively.
DC41572	Acetyl-Calpastatin(184-210)(human) TFA	Acetyl-Calpastatin(184-210)(human) TFA is a potent, selective and reversible calpain inhibitor with Ki values of 0.2 nM and 6 μM for μ-calpain and cathepsin L, respectively.
DC41697	PR-39	PR-39, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric proteasome inhibitor. PR-39 reversibly binds to the α7 subunit of the proteasome and blocks degradation of NF-κB inhibitor IκBα by the ubiquitin-proteasome pathway. PR-39 stimulates angiogenesis, inhibits inflammatory responses and significant reduces myocardial infarct size in mice.
DC41698	PR-39 TFA	PR-39 TFA, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric proteasome inhibitor. PR-39 TFAreversibly binds to the α7 subunit of the proteasome and blocks degradation of NF-κB inhibitor IκBα by the ubiquitin-proteasome pathway. PR-39 TFA stimulates angiogenesis, inhibits inflammatory responses and significant reduces myocardial infarct size in mice.
DC45262	18α-Glycyrrhetinic acid	18α-Glycyrrhetinic acid, a diet-derived compound, is an inhibitor of NF-kB and an activator of proteasome, which serves as pro-longevity and anti-aggregation factor in a multicellular organism. 18α-Glycyrrhetinic acid induces apoptosis.
DC45912	KZR-616 maleate	KZR-616 maleate, a first-in-class immunoproteasome inhibitor, selectively targets the LMP7 (IC50: 39/57 nM=hLMP7/mLMP7) and LMP2 (IC50: 131/179 nM=hLMP7/mLMP7) subunits of the immunoproteasome. KZR-616 maleate has the potential for the research of multiple autoimmune diseases.
DC46341	RA375	RA375 is a RPN13 (26S proteasome regulatory subunit) inhibitor. RA375 activates UPR signaling, ROS production and apoptosis. RA375 exhibits ten-fold greater activity against cancer lines than RA190, reflecting its nitro ring substituents and the addition of a chloroacetamide warhead.
DC46920	Dazcapistat	Dazcapistat is a potent calpain inhibitor, with IC50s of <3 μM for calpain 1, calpain 2 and calpain 9, respectively (patent WO2018064119A1, compound 405).

Proteasome

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