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LMP7 inhibitor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (5) Autophagy (1) Bacterial (2) Drug Derivative (1) Endogenous Metabolite (1) HIV (2) NF-κB (1) Proteasome (17) Reference Standards (1)
By Research Areas:	Cancer (5) Cardiovascular Disease (1) Infection (2) Inflammation/Immunology (14)
Click Chemistry:	Azide (1)

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Click Chemistry

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-13821

Epoxomicin 20+ 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-13207

ONX-0914 Maximum Cited Publications 24 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-12113

Oprozomib 3 Publications Verification ONX 0912; PR-047	Proteasome Autophagy Apoptosis	Cancer
Oprozomib (PR-047) is an orally bioavailable and selective peptide epoxyketone proteasome inhibitor with IC₅₀s of 36 and 82 nM for proteasome (β5) and immunoproteasome (LMP7), respectively. Oprozomib (ONX 0912) induces apoptosis in MM cells .

HY-111790

M3258 5 Publications Verification	Proteasome Apoptosis	Cancer
M3258 is an orally bioavailable, potent, reversible and highly selective immunoproteasome subunit LMP7 (β5i) inhibitor. M3258 exerts high biochemical (IC₅₀=3.6 nM) and cellular (IC₅₀=3.4 nM) potency against the LMP7 subunit. M3258 shows strong antitumor efficacy in multiple myeloma xenograft models. M3258 leads to a significant and prolonged suppression of tumor LMP7 activity and ubiquitinated protein turnover and the induction of apoptosis in multiple myeloma cells .

HY-P11306

Biotin-(Oaa)3-epoxomicin	Proteasome NF-κB	Inflammation/Immunology
Biotin-(Oaa)₃-epoxomicin is a biotin-labeled form of Epoxomicin (HY-13821), prepared by conjugating Epoxomicin with biotin via three hydrophilic oxaacetyl amino acid (Oaa) linkers. Biotin-(Oaa)₃-epoxomicin is primarily used in proteomic studies for the capture, identification and target validation of proteasome complexes, to determine the intracellular targets of epoxomicin. Epoxomicin acts as a proteasome inhibitor and NF-κB inhibitor, which effectively blocks inflammatory responses in mouse ear edema assays. It inhibits proteasome activity via covalent binding to catalytic subunits including LMP7, X, MECL1 and Z, with the strongest inhibitory effect on chymotrypsin-like activity, and does not interfere with non-proteasomal proteases such as trypsin and papain .

HY-123587

PR-924	Proteasome Apoptosis	Cancer
PR-924 is a selective tripeptide epoxyketone immunoproteasome subunit LMP-7 inhibitor with an IC₅₀ of 22 nM. PR-924 covalently modifies proteasomal N-terminal threonine active sites. PR-924 inhibits growth and triggers apoptosis in multiple myeloma (MM) cells. PR-924 has antitumor activities .

HY-101786

KZR-504 5 Publications Verification	Proteasome	Inflammation/Immunology
KZR-504 is a highly selective inhibitor of immunoproteasome low molecular mass polypeptide 2 (LMP2), with IC₅₀s of 51 nM, 4.274 μM for LMP2 and LMP7, respectively. KZR-504 is of interest for the treatment of autoimmune disease .

HY-114419

Zetomipzomib 4 Publications Verification 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 4 Publications Verification 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-114170

ML604440 3 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-13207A

ONX-0914 TFA Maximum Cited Publications 24 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 .

HY-157033

LMP7-IN-2	Proteasome	Inflammation/Immunology
LMP7-IN-2 is a LMP7 inhibitor. LMP7-IN-2 can be used for associated inflammatory diseases and disorders .

HY-142920

LMP7-IN-1	Proteasome	Inflammation/Immunology
LMP7-IN-1, a Boronic acid derivative, is a potent and selective immunoproteasome subunit LMP7 (β5i) inhibitor with an IC₅₀ of 1.83 nM (WO2021143923A1; compound 20) .

HY-162754

LMP7/LMP2-IN-1	Proteasome	Inflammation/Immunology
LMP7/LMP2-IN-1 (Compound 19) is the orally active inhibitor for immunoproteasome subunits *LMP7* and LMP2 with IC₅₀ of 257 and 10 nM. LMP7/LMP2-IN-1 reduces the generation of antibody, downregulates the cells in spleen germinal center B and in plasma in NP-OVA-immunized mice, and can be used in research about autoimmune diseases .

HY-123587A

(R)-PR-924	Apoptosis	Cancer
(R)-PR-924 is the isomer of PR-924 (HY-123587), and can be used as an experimental control. PR-924 is a selective tripeptide epoxyketone immunoproteasome subunit LMP-7 inhibitor with an IC₅₀ of 22 nM. PR-924 covalently modifies proteasomal N-terminal threonine active sites. PR-924 inhibits growth and triggers apoptosis in multiple myeloma (MM) cells. PR-924 has antitumor activities .

HY-112946

LU-001i	Proteasome	Inflammation/Immunology
LU-001i is a highly specific proteasome β1i (LMP2) inhibitor. LU-001i alone has no significant immunomodulatory effect, but when combined with the LMP7 inhibitor (PRN1126), it can exert anti-inflammatory and immunomodulatory effects. LU-001i can be used for the study of autoimmune diseases .

HY-113526

AR-12463	Drug Derivative Endogenous Metabolite	Cardiovascular Disease
AR-12463 is a derivative of Trapidil (HY-B1016). AR-12463 inhibits the conversion of [14C]acetate to cholesterol. AR-12463 significantly reduces the elevation of total cholesterol in rabbit serum and prevents cholesterol incorporation into tissues. AR-12463 can be used to study atherosclerosis.

HY-179394

Immunoproteasome-IN-2	Proteasome	Inflammation/Immunology
Immunoproteasome-IN-2 is selective immunoproteasome inhibitor with IC₅₀ = 232.3 nM for *LMP7, IC₅₀* = 9384.9 nM for β5. Immunoproteasome-IN-2 exhibits ancillary inhibitory activity against LMP2 and MECL-1 subunits. Immunoproteasome-IN-2 demonstrates anti-inflammatory efficacy in a mouse model of arthritis and shows a favorable safety profile in toxicological studies with reduced hepatotoxicity and hematotoxicity. Immunoproteasome-IN-2 has *LMP7/β5* selectivity directly correlated with lower systemic toxicity. Immunoproteasome-IN-2 can be employed for research in arthritis .

HY-101786R

KZR-504 (Standard)	Reference Standards Proteasome	Inflammation/Immunology
KZR-504 (Standard) is the analytical standard of KZR-504 (HY-101786). This product is intended for research and analytical applications. KZR-504 is a highly selective inhibitor of immunoproteasome low molecular mass polypeptide 2 (LMP2), with IC₅₀s of 51 nM, 4.274 μM for LMP2 and LMP7, respectively. KZR-504 is of interest for the treatment of autoimmune disease .

Cat. No.	Product Name	Target	Research Area

HY-P11306

Biotin-(Oaa)3-epoxomicin	Proteasome NF-κB	Inflammation/Immunology
Biotin-(Oaa)₃-epoxomicin is a biotin-labeled form of Epoxomicin (HY-13821), prepared by conjugating Epoxomicin with biotin via three hydrophilic oxaacetyl amino acid (Oaa) linkers. Biotin-(Oaa)₃-epoxomicin is primarily used in proteomic studies for the capture, identification and target validation of proteasome complexes, to determine the intracellular targets of epoxomicin. Epoxomicin acts as a proteasome inhibitor and NF-κB inhibitor, which effectively blocks inflammatory responses in mouse ear edema assays. It inhibits proteasome activity via covalent binding to catalytic subunits including LMP7, X, MECL1 and Z, with the strongest inhibitory effect on chymotrypsin-like activity, and does not interfere with non-proteasomal proteases such as trypsin and papain .

Epoxomicin 20+ Cited Publications BU-4061T	Microorganisms Classification of Application Fields Ketones, Aldehydes, Acids Inflammation/Immunology Disease Research Fields Source Classification	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 .

Cat. No.	Product Name		Classification

HY-112946

LU-001i		Azide
LU-001i is a highly specific proteasome β1i (LMP2) inhibitor. LU-001i alone has no significant immunomodulatory effect, but when combined with the LMP7 inhibitor (PRN1126), it can exert anti-inflammatory and immunomodulatory effects. LU-001i can be used for the study of autoimmune diseases .

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LMP7 inhibitor

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