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 About 30 results found for searched term "Proteasome" (0.019 seconds)

Cat.No.  Name Information
M1686 Bortezomib (PS-341) Bortezomib (PS-341) is a highly selective proteasome inhibitor with a ki value of 6nM.
M1902 MG132 MG132 is a specific and potent cell-permeable proteasome inhibitor (IC50 = 100 nM, Ki = 4 nM).
M2071 ONX-0914 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 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 Oprozomib (ONX 0912) is a novel orally proteasome inhibitor with potential antineoplastic activity.
M2152 Carfilzomib 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 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 Epoxomicin is a cell-permeable, novel proteasome inhibitor with an IC50 value of 4 nM.
M2285 MLN2238 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 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 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 Lactacystin is a potent and selective inhibitor of the 20S proteasome.
M2807 LDN-57444 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 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 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 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 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 (Tripterin) 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 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 Ursolic acid (Prunol) is a natural triterpenoid carboxylic acid compound with preventive and anticancer activities. Ursolic acid also has proteasome agonist activity, EC50=14μmol/L.
M4985 VR23 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) 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 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 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.
M8473 RA-9 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 PTP1B-IN-9 is a ubiquitin-proteasome system (UPS)-stressor with anticancer activity.
M9577 RA190 hydrochloride RA190 HCl is a potent RPN13 and ADRM1 Inhibitor, inhibits proteasome function by covalently binding to cysteine 88 of ubiquitin receptor RPN13.
M10753 VLX1570 VLX1570 is a competitive inhibitor of proteasome deuteronase (DUBs), with IC50 of 10 μM.
M10767 M-3258 M3258 is an oral bioavailable, potent, reversible, and highly selective immunoproteasome subunit LMP7 (β5i) inhibitor. M3258 for LMP7 IC50 is 3.6 nM in cells IC50 3.4 nM.
M10883 RTS-V5 RTS-V5 is an inhibitor of HDAC/proteasomes, against HDAC1, HDAC2, HDAC3, HDAC6, HDAC8IC50They were 6.9, 18, 15, 0.27, 0.53 μM, respectively.

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