Search Result

Results for "

Proteasome subunits

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Proteasome (20) Androgen Receptor (1) Apoptosis (4) Bacterial (4) E1/E2/E3 Enzyme (1) HIV (2) HSP (1) Keap1-Nrf2 (2) Ligands for Target Protein for PROTAC (1) Mitophagy (1) Parasite (1) PROTACs (2) Reactive Oxygen Species (1)
By Research Areas:	Cancer (10) Infection (3) Inflammation/Immunology (10) Metabolic Disease (1)

Inhibitors & Agonists

Fluorescent Dye

Peptides

Natural
Products

Targets Recommended: Proteasome

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-127102

GSK3494245 DDD01305143	Parasite Proteasome	Infection
GSK3494245 (DDD01305143) is a potent, orally active, and selective inhibitor of the chymotrypsin-like activity of the parasite *proteasome* binding in a site sandwiched between the β4 and β5 subunits (IC₅₀=0.16 μM for WT L. donovani proteasomes). GSK3494245 moderately inhibits chymotrypsin-like activity of human proteasome (IC₅₀: purified 26S=13 µM; enriched THP-1 extracts IC₅₀=40µM). GSK3494245 exhibits attractive biological and biosafety properties .

HY-P1259A

PR-39 TFA	Proteasome Bacterial	Inflammation/Immunology
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 .

HY-169144

Bortezomib analog	Proteasome	Cancer
Bortezomib analog (Compound 13), an analog of Bortezomib (HY-10227), is an active control of 20S proteasome subunit β5 ligand.

HY-169134

*PROTAC 20S proteasome* subunit β5 degrader 1**	PROTACs Apoptosis	Cancer
PROTAC 20S proteasome subunit β5 degrader 1 (compound 12f) is a targeted degrader of PROTAC for 20S proteasome subunit β5, with a DC₅₀ value of 0.11 μM in FaDu cells. PROTAC 20S proteasome subunit β5 degrader 1 disrupts the cell cycle, promotes apoptosis, and inhibits cell proliferation and migration in both FaDu and KM3/BTZ cells. PROTAC 20S proteasome subunit β5 degrader 1 can be used to study the resistance of pharyngeal cancer and multiple myeloma to Bortezomib (HY-10227) (Pink: Target protein ligand (HY-10227); Blue: E3 ligase ligand (HY-103596); Black: Linker (HY-169142)) .

HY-150590

20S Proteasome-IN-2	Proteasome	Cancer
20S Proteasome-IN-2 is a human 20S proteasome inhibitor. 20S Proteasome-IN-2 shows high selectivity to its β5 subunit with the IC₅₀ of 0.18 μM. 20S Proteasome-IN-2 displays anti-proliferative effect in vitro and in vivo, and arrests cell cycle at G2/M .

HY-169135

*PROTAC 20S proteasome* subunit β5 degrader 2**	PROTACs Proteasome	Cancer
PROTAC 20S proteasome subunit β5 degrader 2 is a PROTAC degrader for *20S proteasome* subunit β5, with a DC₅₀** of 0.16 μM. PROTAC 20S proteasome subunit β5 degrader 2 inhibits the proliferation of cancer cell FaDu with IC₅₀ of 0.23 μM. PROTAC 20S proteasome subunit β5 degrader 2 exhibits antitumor efficacy in mice models . (Pink: Ligand for target protein (HY-10227); Blue: Ligand for E3 ligase (HY-103596); Black: Linker (HY-Y1760))

HY-150591

20S Proteasome-IN-3	Proteasome	Cancer
20S Proteasome-IN-3 is a 20S proteasome β5 subunit inhibitor (IC₅₀=1.64 μM) . 20S Proteasome-IN-3 shows anti-tumor proliferation activity .

HY-108553

Dihydroeponemycin	Proteasome Apoptosis	Cancer
Dihydroeponemycin, an analogue of the antitumor and antiangiogenic natural product eponemycin, selectively targets the 20S proteasome. Dihydroeponemycin covalently modifies a subset of catalytic proteasomal subunits, binding preferentially to the IFN-gamma-inducible subunits LMP2 and LMP7. Dihydroeponemycin-mediated proteasome inhibition induces a spindle-like cellular morphological change and apoptosis .

HY-157035

Proteasome β2c/i-IN-1	Proteasome	Others
Proteasome β2c/i-IN-1 (compound 37) is a subunit-selective human proteasome β2c and β2i inhibitor .

HY-P1259

PR-39	Proteasome Bacterial	Inflammation/Immunology
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 .

HY-157034

LU-002i	Proteasome	Others
LU-002i is a subunit-selective human proteasome β2c and β2i inhibitor with an IC₅₀ value of 220 nM for β2i .

HY-157034A

LU-002i TFA	Proteasome	Others
LU-002i TFA is a subunit-selective human proteasome β2c and β2i inhibitor with an IC₅₀ value of 220 nM for β2i .

HY-169158

Bortezomib analog 1	Ligands for Target Protein for PROTAC	Cancer
Bortezomib analog 1 is an analog of Bortezomib (HY-10227). Bortezomib analog 1 and can be used to synthesize PROTAC 20S proteasome subunit β5 degrader 1 (HY-169134) .

HY-162965

Immunoproteasome activator 1	Proteasome	Cancer
Immunoproteasome activator 1 (compound A) is a selective immunoproteasome activator that increases the presentation of individual MHC-I–bound peptides by over 100-fold. Immunoproteasome activator 1 binds to the proteasome structural subunit PSMA1 and promotes the association of the proteasome activator PA28α/β (PSME1/PSME2) with immunoproteasomes .

HY-123051

Ac-WLA-AMC	Proteasome	Inflammation/Immunology
Ac-WLA-AMC is a specific 20S constitutive proteasome β5 fluorogenic substrate .

HY-13821

Epoxomicin 10+ Cited Publications BU-4061T	Proteasome Apoptosis	Inflammation/Immunology Cancer
Epoxomicin (BU-4061T) is an epoxyketone-containing natural product and a potent, selective and irreversible *proteasome* inhibitor. Epoxomicin covalently binds to the LMP7, X, MECL1, and Z catalytic subunits of the *proteasome* and potently inhibits primarily the chymotrypsin-like activity. Epoxomicin can cross the blood-brain barrier. Epoxomicin has strongly antitumor and anti-inflammatory activity .

HY-114170

ML604440 2 Publications Verification	Proteasome	Inflammation/Immunology
ML604440 is a specific and cell-permeable Proteasome β1i (LMP2) subunit inhibitor. ML604440 can be used in experimental colitis, EAE and autoimmune disease research. ML604440 shows synergistic effects and advantageous when combined with LMP7 inhibitor .

HY-136563

RA375	Proteasome Apoptosis Reactive Oxygen Species	Cancer
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 .

HY-114419

Zetomipzomib KZR-616	Proteasome	Inflammation/Immunology
Zetomipzomib (KZR-616), a first-in-class inhibitor of the immunoproteasome, selectively targets the LMP7 (IC₅₀: 39/57 nM=hLMP7/mLMP7) and LMP2 (IC₅₀: 131/179 nM=hLMP7/mLMP7) subunits of the immunoproteasome. Zetomipzomib has the potential for the research of multiple autoimmune diseases .

HY-114419A

Zetomipzomib maleate KZR-616 maleate	Proteasome	Inflammation/Immunology
Zetomipzomib (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=hLMP2/mLMP2) subunits of the immunoproteasome. Zetomipzomib maleate has the potential for the research of multiple autoimmune diseases .

HY-149127

Rosolutamide ASC-JM17; ALZ-003	Keap1-Nrf2 Androgen Receptor HSP Mitophagy	Metabolic Disease
Rosolutamide (ASC-JM17), a curcumin analog, is an orally active, potent Nrf1 and Nrf2 activator. Rosolutamide activates Nrf1, Nrf2 and heat shock factor 1 (Hsf1), thereby activating the expression of proteasome subunits, antioxidant enzymes and molecular chaperones. Rosolutamide degrades the polyglutamine (polyQ) androgen receptor (AR) via the ubiquitin-proteasome pathway and improves motor function in mouse models of spinal and bulbar muscular atrophy (SBMA). Rosolutamide improves mitochondrial function and promotes autophagy, decreases mutant protein aggregates, and attenuates intracellular/mitochondrial reactive oxygen species (ROS) levels .

HY-13207

ONX-0914 Maximum Cited Publications 15 Publications Verification PR-957	Proteasome Bacterial HIV	Infection Inflammation/Immunology
ONX-0914 (PR-957) is a selective inhibitor of low-molecular mass polypeptide-7 (LMP7), the chymotrypsin-like subunit of the immunoproteasome. ONX-0914 blocks cytokine production and attenuates progression of experimental arthritis. ONX-0914 is a noncompetitive irreversible inhibitor of the mycobacterial proteasome (K_i=5.2 μM). ONX-0914 reactivates latent HIV-1 through p-TEFb activation mediated by HSF-1 .

HY-160876

BC-1901S	Keap1-Nrf2 E1/E2/E3 Enzyme	Inflammation/Immunology
BC-1901S is a proteasome-independent NRF2 activator and stabilizer. BC-1901S binds to DCAF1 (E3 ligase subunit) and disrupts NRF2/DCAF1 interaction, and activates NRF2 by inhibiting NRF2 ubiquitination in a KEAP1-independent manner. BC-1901S shows anti-inflammatory effect in a murine model of LPS-induced acute lung injury .

HY-13207A

ONX-0914 TFA Maximum Cited Publications 15 Publications Verification PR-957 TFA	Proteasome Bacterial HIV	Infection Inflammation/Immunology
ONX-0914 (PR-957) TFA is a selective inhibitor of low-molecular mass polypeptide-7 (LMP7), the chymotrypsin-like subunit of the immunoproteasome. ONX-0914 TFA blocks cytokine production and attenuates progression of experimental arthritis. ONX-0914 TFA is a noncompetitive irreversible inhibitor of the mycobacterial proteasome (K_i=5.2 μM). ONX-0914 TFA reactivates latent HIV-1 through p-TEFb activation mediated by HSF-1 .

Ac-WLA-AMC	Fluorescent Dyes/Probes
Ac-WLA-AMC is a specific 20S constitutive proteasome β5 fluorogenic substrate .

Cat. No.	Product Name	Target	Research Area

HY-P1259A

PR-39 TFA	Proteasome Bacterial	Inflammation/Immunology
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 .

HY-123051

Ac-WLA-AMC	Proteasome	Inflammation/Immunology
Ac-WLA-AMC is a specific 20S constitutive proteasome β5 fluorogenic substrate .

HY-P1259

PR-39	Proteasome Bacterial	Inflammation/Immunology
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 .

Epoxomicin 10+ Cited Publications BU-4061T	Structural Classification Microorganisms Classification of Application Fields Ketones, Aldehydes, Acids Source classification Inflammation/Immunology Disease Research Fields	Proteasome Apoptosis
Epoxomicin (BU-4061T) is an epoxyketone-containing natural product and a potent, selective and irreversible *proteasome* inhibitor. Epoxomicin covalently binds to the LMP7, X, MECL1, and Z catalytic subunits of the *proteasome* and potently inhibits primarily the chymotrypsin-like activity. Epoxomicin can cross the blood-brain barrier. Epoxomicin has strongly antitumor and anti-inflammatory activity .

Inquiry Online

Your information is safe with us. * Required Fields.

MCE Japan Authorized Agent ナミキ商事株式会社コスモ・バイオ株式会社
Salutation			Country or Region *
Applicant Name *			Organization Name *
Department *
Email Address *			Product Name *
Cat. No.			Requested quantity *
Phone Number *
Remarks

Inquiry Online

Inquiry Information

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent:

Name
Email *

	Sorry, but the email address you supplied was invalid.

Proteasome subunits

Inhibitors & Agonists

Fluorescent Dye

Peptides

NaturalProducts

Natural
Products