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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
17 Results for "
immunoproteasome LMP7
" in MedChemExpress (MCE) Product Catalog:
Products (17)
17 Results for "immunoproteasome LMP7" in MCE Product Catalog:
26
26 Publications Verification
Synonyms: PR-957
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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 (Ki=5.2 μM). ONX-0914 reactivates latent HIV-1 through p-TEFb activation mediated by HSF-1 .
26
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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 (Ki=5.2 μM). ONX-0914 TFA reactivates latent HIV-1 through p-TEFb activation mediated by HSF-1 .
5
5 Cited Publications
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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 .
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5 Cited Publications
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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 .
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4 Cited Publications
Synonyms: ONX 0912; PR-047
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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 .
4
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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 .
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4 Cited Publications
Synonyms: KZR-616 maleate
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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 .
Cat. No.: HY-P11307
CAS No.: 1334608-28-4
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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 .
Cat. No.: HY-P10002
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Cat. No.: HY-142920
CAS No.: 2671040-07-4
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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) .
Cat. No.: HY-162754
CAS No.: 3053755-09-9
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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 .
Cat. No.: HY-123587A
Purity: 98.50%
(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 .
Cat. No.: HY-113526
CAS No.: 100557-04-8
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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.
Cat. No.: HY-179394
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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 .
Cat. No.: HY-111790R
CAS No.: 2285330-15-4
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M3258 (Standard) is the analytical standard of M3258 (HY-111790). This product is intended for research and analytical applications. 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 .
Cat. No.: HY-101786R
CAS No.: 1629052-78-3
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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 .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
