About 32 results found for searched term "Proteasome" (0.074 seconds)
| Cat.No. | Name | Target |
|---|---|---|
| M51264 | Proteasome-activating peptide 1 | Others |
| Proteasome-activating peptide 1 is a peptide, which increases the chymotrypsin-like proteasomal catalytic activity and, consequently, proteolytic rates both in vitro and in culture. | ||
| M56779 | Proteasome inhibitor IX | Proteasome |
| Proteasome inhibitor IX (PS-IX; AM114) is a Chalcone derivative and a chymotrypsin-like activity of the 20S proteasome inhibitor with an IC50 value of ~1 μM. | ||
| M1686 | Bortezomib (PS-341) | Proteasome |
| Velcade; PS-341; LDP 341; MG 341; NSC 681239 | ||
| Bortezomib (PS-341) is a highly selective proteasome inhibitor with a ki value of 6nM. | ||
| M45166 | LWY713 | PROTAC |
| LWY713 is a PROTAC molecule targeting FLT3 with acetyl group as linker, which can selectively induce FLT3 degradation in CRBN and proteasome-dependent manner, with a DC50 of 0.64 nM and a Dmax of 94.8%, and possesses antitumor activity. | ||
| M1902 | MG132 | Proteasome |
| Z-Leu-Leu-Leu-al; MG-132 | ||
| MG132 is a specific and potent cell-permeable proteasome inhibitor (IC50 = 100 nM, Ki = 4 nM). | ||
| M2071 | ONX-0914 | Proteasome |
| PR-957 | ||
| Onx-0914 (PR-957) is a selective inhibitor of low molecular weight polypeptide 7 (LMP7), a chymotrypsin subunit of the immune proteasome. Onx-0914 blocks cytokine production and reduces the progression of experimental arthritis. Onx-0914 is a non-competitive irreversible inhibitor of mycobacterium proteasome (Ki=5.2 μM). Onx-0914 activates latent HIV-1 through HF-1-mediated p-TEFb activation. | ||
| M2122 | MLN9708 | Proteasome |
| ixazomib citrate | ||
| MLN9708 is a novel orally bioactive proteasome inhibitor, inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome with an IC50 value of 3.4 nM. | ||
| M2150 | Oprozomib | Proteasome |
| ONX 0912, PR-047 | ||
| Oprozomib (ONX 0912) is a novel orally proteasome inhibitor with potential antineoplastic activity. | ||
| M2152 | Carfilzomib | Proteasome |
| PR-171 | ||
| Carfilzomib (PR-171) is an irreversible proteasome inhibitor with an IC50 of <5 nM. Carfilzomib irreverently selectively binds to the active site containing n-terminal threonine of the 20S proteasome and proteolytic core particles of the 26S proteasome.*The compound is unstable in solutions, freshly prepared is recommended. | ||
| M2166 | Birinapant | IAP |
| TL32711 | ||
| Birinapant (TL32711) is a bivalent Smac analogue, which is a potent antagonist of XIAP and cIAP1 with Kd values of 45 nM and less than 1 nM, respectively. Birinapant (TL32711) induces autoubiquitination and proteasome degradation of cIAP1 and cIAP2 in intact cells, resulting in the formation of RIPK1: Caspase-8 complex, which activates and induces tumor cell death. | ||
| M2193 | Epoxomicin | Proteasome |
| BU 4061T | ||
| Epoxomicin (BU-4061T) is a cell-permeable, selective and irreversible proteasome inhibitor with an IC50 value of 4 nM. 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. | ||
| M2285 | MLN2238 | Proteasome |
| Ixazomib | ||
| 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. | ||
| M2431 | b-AP15 | Deubiquitinase |
| NSC 687852 | ||
| b-AP15 is a deubiquitinases inhibitor for 19S proteasomes activity of Ub-AMC cleavage with IC50 of 2.1 μM. *The compound is unstable in solutions, freshly prepared is recommended | ||
| M2583 | PD 169316 | p38 MAPK |
| PD 169316 is a cell-permeable, potent and selective p38 MAP kinase inhibitor that indirectly activates proteasome activity and has antiviral activity against Enterovirus71 with an IC50 value of 89 nM. | ||
| M2801 | Lactacystin | Proteasome |
| Lactacystin is a potent and selective inhibitor of the 20S proteasome. | ||
| M2807 | LDN-57444 | Deubiquitinase |
| LDN-57444 is a reversible, competitive proteasome inhibitor for Uch-L1 with IC50 of 0.88 μM, 28-fold selectivity over isoform Uch-L3. | ||
| M2995 | Salinosporamide A | Proteasome |
| (-)-Salinosporamide A; ML 858; NPI 0052; Marizomib | ||
| Salinosporamide A (NPI-0052, Marizomib) is a novel marine derived proteasome inhibitor which inhibits CT-L, C-L, and T-L proteasome activities in human erythrocyte-derived 20S proteasomes with EC50 of 3.5 nM, 430 nM, 28 nM. | ||
| M3161 | Betulinic acid | NF-κB |
| Lupatic acid; Betulic acid | ||
| Betulinic acid is a natural pentacyclic triterpenoid compound, which is an inhibitor of eukaryotic cell topoisomerase I with IC50 value of 5 μM. It has anti-inflammatory, anti-malaria, anti-AIDS and anti-tumor activities. Betulinic acid(Betulinic acid) is also an agonist of 20S proteasome. EC50=5.5μmol/L, Betulinic acid can specifically enhance cT-L activity of 20S proteasome. | ||
| M3456 | Chlorpromazine hydrochloride | Potassium Channel |
| Sonazine | ||
| Chlorpromazine hydrochloride is an antagonist of D2, 5HT2A, potassium and sodium channels. The Ki of Chlorpromazine Hydrochloride to D2 and 5HT2A were 363 nM and 8.3 nM, respectively. Chlorpromazine also excites the 20S proteasome. *The compound is unstable in solutions, freshly prepared is recommended | ||
| M3476 | CEP-18770 | Proteasome |
| Delanzomib | ||
| CEP-18770 is an orally active inhibitor of the chymotrypsin-like activity of proteasome with IC50 of 3.8 nM, with only marginal inhibition of the tryptic and peptidylglutamyl activities of the proteosome. | ||
| M3884 | Celastrol | Proteasome |
| Tripterin; Tripterine; CEL | ||
| Celastrol (Tripterin) is a potent antioxidant and anti-inflammatory agent, as well as a proteasome inhibitor which potently and preferentially inhibits the chymotrypsin-like activity of a purified 20S proteasome with IC50 of 2.5 μM. | ||
| M4240 | Shikonin | TNF Receptor |
| C.I. 75535; Isoarnebin 4; CAS# 54952-43-1 | ||
| Shikonin (C.I. 75535, Anchusin, Anchusa acid, Alkanna Red, Isoarnebin 4, NSC 252844) is an effective and specific inhibitor of Pyruvate kinase M2 (PKM2). Shikonin is the main ingredient of Lithosia, a Chinese herb with a variety of biological activities. Shikonin acts as an anti-inflammatory by inhibiting tumor necrosis factor-α (TNF-α), Proteasome can inhibit the activation of nuclear factor-κB (NF-κB) signaling pathway. | ||
| M4522 | Ursolic acid | Autophagy |
| Prunol; Urson; Malol; Bungeolic acid | ||
| Ursolic acid (Prunol) is a natural triterpenoid carboxylic acid compound with preventive and anticancer activities. Ursolic acid also has proteasome agonist activity, EC50=14 μmol/L. | ||
| M4551 | Trigonelline hydrochloride | Anti-infection |
| Trigonelline chloride | ||
| Trigonelline chloride is an alkaloid with potential antidiabetic activity that can be isolated from Trigonella foenum-graecum L or Leonurus artemisia. Trigonelline chloride is a potent Nrf2 inhibitor that blocks Nrf2-dependent proteasome activity, thereby enhancing apoptosis in pancreatic cancer cells. | ||
| M4814 | K-7174 dihydrochloride | Proteasome |
| K7174 2HCl | ||
| K-7174 dihydrochloride is a novel, orally active proteasome and GATA inhibitor, inhibits the expression of vascular cell adhesion molecule-1 (VCAM-1) induced by either IL-1β or TNF-α. | ||
| M4985 | VR23 | Proteasome |
| VR23 is a small molecule that potently inhibited the activities of trypsin-like proteasomes (IC50 = 1 nM), chymotrypsin-like proteasomes (IC50 = 50-100 nM), and caspase-like proteasomes (IC50 = 3 μM). | ||
| M5385 | Acetylcysteine (NAC) | ROS |
| N-Acetyl-L-cysteine; NAC; N-acetylcysteine; N-Acetyl-Cysteine | ||
| Acetylcysteine (NAC; N-acetyl-l-cysteine) is a ROS inhibitor that antagonizes the activity of several proteasome inhibitors. It is also an inhibitor of the tumor necrosis factor TNF. | ||
| M5939 | Rolipram | PDE |
| ZK-62711, SB 95952 | ||
| A selective inhibitor of PDE4, Rolipram, inhibits immunopurified PDE4B and PDE4D activity with IC50 of 130 nM and 240 nM, respectively. It has anti-inflammatory activity. Rolipram also increased cAMP levels and activated PKA, which in turn increased proteasome activity and inhibited tau aggregation. | ||
| M7796 | Fluspirilene | Calcium Channel |
| Fluspirilene is a non-competitive L-type calcium channel antagonist (IC50 = 0.03μM). It is also a dopamine receptor antagonist and can be used as a precursor structure for the development of 20S proteasome agonists. | ||
| M50170 | ARV-393 | PROTAC |
| ARV-393 is an orally active PROTAC degrader targeting BCL6 for studies related to diffuse large B-cell lymphoma. ARV-393 utilizes the ubiquitin-proteasome system to target the degradation of BCL6. | ||
| M8473 | RA-9 | Others |
| RA-9 is a cell permeable and potent inhibitor of the ubiquitin-proteasome system (UPS) that targets deubiquitinating enzymes (DUB) without affecting 20S proteasome catalytic-core activity. | ||
| M9570 | PTP1B-IN-9 | Proteasome |
| PTP1B-IN-9 is a ubiquitin-proteasome system (UPS)-stressor with anticancer activity. | ||
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