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阻害剤の選択性比較

カタログ番号 製品カタログ 溶解度(25°C)
DMSO アルコール
S1013 Bortezomib (PS-341) <1 mg/mL 76 mg/mL '<1 mg/mL
S2619 MG-132 <1 mg/mL 90 mg/mL ''25 mg/mL
S2853 Carfilzomib (PR-171) <1 mg/mL 50 mg/mL ''<1 mg/mL
S2181 Ixazomib Citrate (MLN9708) <1 mg/mL 100 mg/mL '<1 mg/mL
S2180 Ixazomib (MLN2238) <1 mg/mL 72 mg/mL ''9 mg/mL
S7504 Salinosporamide A (NPI-0052, Marizomib) ' mg/mL
S6851 RA-190 <1 mg/mL 100 mg/mL '''20 mg/mL
S7027 Lactacystin 10 mg/mL 20 mg/mL '''' mg/mL
S7172 ONX-0914 (PR-957) <1 mg/mL 100 mg/mL ''100 mg/mL
S7049 Oprozomib (ONX 0912) <1 mg/mL 100 mg/mL <1 mg/mL
S1157 Delanzomib (CEP-18770) <1 mg/mL 83 mg/mL 83 mg/mL
S1290 Celastrol <1 mg/mL 90 mg/mL '''<1 mg/mL
S7038 Epoxomicin <1 mg/mL 100 mg/mL ''100 mg/mL
S8279 Shikonin <1 mg/mL 57 mg/mL 23 mg/mL
S7933 VR23 5 mg/mL 31 mg/mL <1 mg/mL
S7462 PI-1840 <1 mg/mL 78 mg/mL 33 mg/mL
S3269 Acetylcorynoline -1 mg/mL 40 mg/mL -1 mg/mL

亜型選択性的な製品

Proteasome製品

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
S1013

Bortezomib (PS-341)

Bortezomib (PS-341, LDP-341, MLM341) is a potent 20S proteasome inhibitor with Ki of 0.6 nM. It exhibits favorable selectivity towards tumor cells over normal cells. Bortezomib (PS-341) inhibits NF-κB and induces ERK phosphorylation to suppress cathepsin B and inhibit the catalytic process of autophagy in ovarian cancer and other solid tumors.

S2619

MG-132

MG132 is a potent cell-permeable proteasome and calpain inhibitor with IC50s of 0.1 μM and 1.2 μM for the inhibition of proteasome and calpain, respectively. MG132 activates autophagy and induces apoptosis in tumor cells.

S2853

Carfilzomib (PR-171)

Carfilzomib (PR-171) is an irreversible proteasome inhibitor with IC50 of <5 nM in ANBL-6 cells, displayed preferential in vitro inhibitory potency against the ChT-L activity in the β5 subunit, but little or no effect on the PGPH and T-L activities. Carfilzomib activates prosurvival autophagy and induces cell apoptosis.

S2181

Ixazomib Citrate (MLN9708)

Ixazomib Citrate (MLN9708) immediately hydrolyzed to Ixazomib (MLN2238), the biologically active form, on exposure to aqueous solutions or plasma. Ixazomib (MLN2238) inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome with IC50/Ki of 3.4 nM/0.93 nM in cell-free assays, less potent to β1 and little activity to β2. Ixazomib (MLN2238) induces autophagy. Phase 3.

S2180

Ixazomib (MLN2238)

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 in cell-free assays, respectively, also inhibits the caspase-like (β1) and trypsin-like (β2) proteolytic sites, with IC50 of 31 and 3500 nM. Ixazomib (MLN2238) induces autophagy. Phase 3.

S7504

Salinosporamide A (NPI-0052, Marizomib)

Salinosporamide A (NPI-0052, Marizomib) is a novel marine derived proteasome inhibitor which inhibits CT-L β5, C-L β1, and T-L β2 proteasome activities in human erythrocyte-derived 20S proteasomes with IC50 of 3.5 nM, 430 nM, 28 nM.

S6851

RA-190

RA190, a bis-benzylidine piperidon, is a potent, selective and oral effective inhibitor of proteasome ubiquitin receptor RPN13/ADRM1 with anticancer activity. RA190 triggers ER stress response, p53/p21 signaling axis and autophagy in multiple myeloma cells.

S7027

Lactacystin

Lactacystin is a potent and selective inhibitor of the 20S proteasome.

S7172

ONX-0914 (PR-957)

ONX-0914 (PR-957) is a potent and selective immunoproteasome inhibitor with minimal cross-reactivity for the constitutive proteasome in a cell-free assay.

S7049

Oprozomib (ONX 0912)

Oprozomib (ONX 0912) is an orally bioavailable inhibitor for CT-L activity of 20S proteasome β5/LMP7 with IC50 of 36 nM/82 nM. Phase 1/2.

S1157

Delanzomib (CEP-18770)

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. Phase 1/2.

S1290

Celastrol

Celastrol (Tripterine) is a potent proteasome inhibitor for the chymotrypsin-like activity of a purified 20S proteasome with IC50 of 2.5 μM. Celastrol induces apoptosis and autophagy via the ROS/JNK signaling pathway. Celastrol inhibits dopaminergic neuronal death of Parkinson's disease through activating mitophagy.

S7038

Epoxomicin

Epoxomicin (BU-4061T, Aids010837) is a selective proteasome inhibitor with anti-inflammatory activity, inhibits primarily the CH-L activity of the 20S proteasome, while T-L and PGPH catalytic activities are also inhibited at 100- and 1000-fold reduced rate. Epoxomicin promotes apoptosis.

S8279

Shikonin

Shikonin, a potent and specific Pyruvate kinase M2 (PKM2) inhibitor, is a major component of zicao (purple gromwell, the dried root of Lithospermum erythrorhizon), a Chinese herbal medicine with various biological activities. It is also an inhibitor of TMEM16A chloride channel activity using cell-based fluorescent-quenching assay. Shikonin exerts an anti-inflammatory effect by inhibiting tumor necrosis factor-α (TNF-α) and prevents activation of nuclear factor-κB (NF-κB) pathway via proteasome inhibition.

S7933

VR23

VR23 is a potent proteasome inhibitor with IC50 of 1 nM, 50-100 nM, and 3 μM for trypsin-like proteasomes, chymotrypsin-like proteasomes, and caspase-like proteasomes, respectively.

S7462

PI-1840

PI-1840 is a reversible and selective chymotrypsin-like (CT-L) inhibitor with IC50 of 27 nM with little effects on the other two major proteasome proteolytic activities, trypsin-like (T-L) and postglutamyl-peptide-hydrolysis-like (PGPH-L).

S3269

Acetylcorynoline

Acetylcorynoline, a major alkaloid component derived from Corydalis bungeana which is a traditional Chinese medical herb, shows anti-inflammatory properties. Acetylcorynoline may decrease egl-1 expression to suppress apoptosis pathways and increase rpn5 expression to enhance the activity of proteasomes.

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
S1013

Bortezomib (PS-341)

Bortezomib (PS-341, LDP-341, MLM341) is a potent 20S proteasome inhibitor with Ki of 0.6 nM. It exhibits favorable selectivity towards tumor cells over normal cells. Bortezomib (PS-341) inhibits NF-κB and induces ERK phosphorylation to suppress cathepsin B and inhibit the catalytic process of autophagy in ovarian cancer and other solid tumors.

S2619

MG-132

MG132 is a potent cell-permeable proteasome and calpain inhibitor with IC50s of 0.1 μM and 1.2 μM for the inhibition of proteasome and calpain, respectively. MG132 activates autophagy and induces apoptosis in tumor cells.

S2853

Carfilzomib (PR-171)

Carfilzomib (PR-171) is an irreversible proteasome inhibitor with IC50 of <5 nM in ANBL-6 cells, displayed preferential in vitro inhibitory potency against the ChT-L activity in the β5 subunit, but little or no effect on the PGPH and T-L activities. Carfilzomib activates prosurvival autophagy and induces cell apoptosis.

S2181

Ixazomib Citrate (MLN9708)

Ixazomib Citrate (MLN9708) immediately hydrolyzed to Ixazomib (MLN2238), the biologically active form, on exposure to aqueous solutions or plasma. Ixazomib (MLN2238) inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome with IC50/Ki of 3.4 nM/0.93 nM in cell-free assays, less potent to β1 and little activity to β2. Ixazomib (MLN2238) induces autophagy. Phase 3.

S2180

Ixazomib (MLN2238)

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 in cell-free assays, respectively, also inhibits the caspase-like (β1) and trypsin-like (β2) proteolytic sites, with IC50 of 31 and 3500 nM. Ixazomib (MLN2238) induces autophagy. Phase 3.

S7504

Salinosporamide A (NPI-0052, Marizomib)

Salinosporamide A (NPI-0052, Marizomib) is a novel marine derived proteasome inhibitor which inhibits CT-L β5, C-L β1, and T-L β2 proteasome activities in human erythrocyte-derived 20S proteasomes with IC50 of 3.5 nM, 430 nM, 28 nM.

S6851

RA-190

RA190, a bis-benzylidine piperidon, is a potent, selective and oral effective inhibitor of proteasome ubiquitin receptor RPN13/ADRM1 with anticancer activity. RA190 triggers ER stress response, p53/p21 signaling axis and autophagy in multiple myeloma cells.

S7027

Lactacystin

Lactacystin is a potent and selective inhibitor of the 20S proteasome.

S7172

ONX-0914 (PR-957)

ONX-0914 (PR-957) is a potent and selective immunoproteasome inhibitor with minimal cross-reactivity for the constitutive proteasome in a cell-free assay.

S7049

Oprozomib (ONX 0912)

Oprozomib (ONX 0912) is an orally bioavailable inhibitor for CT-L activity of 20S proteasome β5/LMP7 with IC50 of 36 nM/82 nM. Phase 1/2.

S1157

Delanzomib (CEP-18770)

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. Phase 1/2.

S1290

Celastrol

Celastrol (Tripterine) is a potent proteasome inhibitor for the chymotrypsin-like activity of a purified 20S proteasome with IC50 of 2.5 μM. Celastrol induces apoptosis and autophagy via the ROS/JNK signaling pathway. Celastrol inhibits dopaminergic neuronal death of Parkinson's disease through activating mitophagy.

S7038

Epoxomicin

Epoxomicin (BU-4061T, Aids010837) is a selective proteasome inhibitor with anti-inflammatory activity, inhibits primarily the CH-L activity of the 20S proteasome, while T-L and PGPH catalytic activities are also inhibited at 100- and 1000-fold reduced rate. Epoxomicin promotes apoptosis.

S8279

Shikonin

Shikonin, a potent and specific Pyruvate kinase M2 (PKM2) inhibitor, is a major component of zicao (purple gromwell, the dried root of Lithospermum erythrorhizon), a Chinese herbal medicine with various biological activities. It is also an inhibitor of TMEM16A chloride channel activity using cell-based fluorescent-quenching assay. Shikonin exerts an anti-inflammatory effect by inhibiting tumor necrosis factor-α (TNF-α) and prevents activation of nuclear factor-κB (NF-κB) pathway via proteasome inhibition.

S7933

VR23

VR23 is a potent proteasome inhibitor with IC50 of 1 nM, 50-100 nM, and 3 μM for trypsin-like proteasomes, chymotrypsin-like proteasomes, and caspase-like proteasomes, respectively.

S7462

PI-1840

PI-1840 is a reversible and selective chymotrypsin-like (CT-L) inhibitor with IC50 of 27 nM with little effects on the other two major proteasome proteolytic activities, trypsin-like (T-L) and postglutamyl-peptide-hydrolysis-like (PGPH-L).

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
S3269

Acetylcorynoline

Acetylcorynoline, a major alkaloid component derived from Corydalis bungeana which is a traditional Chinese medical herb, shows anti-inflammatory properties. Acetylcorynoline may decrease egl-1 expression to suppress apoptosis pathways and increase rpn5 expression to enhance the activity of proteasomes.

Tags: Proteasome inhibition | ubiquitin-Proteasome system | ubiquitin-Proteasome pathway | Proteasome activity | Proteasome function | ubiquitin-Proteasome degradation | Proteasome assay | Proteasome structure | Proteasome purification | Proteasome inhibitors in cancer therapy | Proteasome cleavage | 20s Proteasome activity | 26s Proteasome structure | Proteasome inhibition assay | Proteasome inhibitor drugs | Proteasome inhibitor review | Proteasomal inhibitor | Proteasomal inhibitors