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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) | ||
|---|---|---|---|---|
| 水 | 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 (MLN9708) | <1 mg/mL | 100 mg/mL | <1 mg/mL |
| S2180 | Ixazomib (MLN2238) | <1 mg/mL | 72 mg/mL | 9 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 |
| S7933 | VR23 | <1 mg/mL | 31 mg/mL | <1 mg/mL |
| S7462 | PI-1840 | <1 mg/mL | 78 mg/mL | 33 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) is a potent 20S proteasome inhibitor with Ki of 0.6 nM. It exhibits favorable selectivity towards tumor cells over normal cells. |
Effect of different proteasome inhibitors on dysferlin expression and on membrane resealing in cultured primary myoblasts. Primary myoblasts from patient 2 harboring a homozygous Arg555Trp DYSF mutation that were treated with the indicated amounts of bortezomib for 24 hours. Western blots of protein extracts were stained with anti-dysferlin antibodies and with anti–a-tubulin antibody as loading control.
|
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| S2619 |
MG-132MG132 is a potent cell-permeable proteasome and calpain inhibitor with IC50s of 0.1 and 1.2 μM for the inhibition of proteasome and calpain, respectively. |
MDA-MB-231 cells were treated with 10 uM MG132 and incubated under normoxia or hypoxia for 4 h. Endogenous interaction between LATS2 and SIAH2 was analysed by immunoprecipitation.
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| 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. |
Validation of activity and specificity of chemical inhibitors of; ATM, ATR, and DNAPK. H460 cells were treated with 1 uM camptothecin (CPT) or 20 ug/ml bleomycin for 1 h in the presence of the indicated inhibitors: DNAPK-i1—NU7026, DNAPK-i2—NU7441. MSH6,
|
|
| S2181 |
Ixazomib (MLN9708)Ixazomib Citrate (MLN9708) immediately hydrolyzed to MLN2238, the biologically active form, on exposure to aqueous solutions or plasma. 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. Phase 3. |
LAT2 is degraded by proteasomes after treatment with alkylphospholipids. (A): 3-h treatment of NB4 cells before exposure to the proteasome inhibitor MG132 (10 M) prevented the reduction of LAT2 induced by 25 M ODPC. (B)(C): a similar effect was observed after exposure (30 min) of NB4 cells to the proteasome inhibitor MLN9708 (5 M) followed by treatment with 25 M ODPC (B) or 25 M perifosine (C).
|
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| S2180 |
Ixazomib (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 in cell-free assays, respectively, also inhibits the caspase-like (β1) and trypsin-like (β2) proteolytic sites, with IC50 of 31 and 3500 nM. Phase 3. |
Primary myoblasts from patient 2 harboring a homozygous Arg555Trp DYSF mutation that were treated with the indicated amounts of MLN2238 for 24 hours.
|
|
| 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. |
The oprozomib-mediated inhibition of 20S proteasome activity exhibits slow-binding kinetics. (A) The effect of varying concentrations of oprozomib on the relative fluorescence increase due to the 20S proteasome-catalyzed hydrolysis of Suc-LLVY-AMC. Otherwise experimental conditions and comments are as in Fig. 3A above. (B) Plot of the pseudo-first order rate constant kobs calculated from curve fitting of progress curves to an equation describing slow-binding kinetics vs. the oprozomib concentration for the oprozomib-mediated inhibition of 20S proteasome activity. The solid straight line was linear-least squares calculated and yielded an apparent second order rate constant kon of (3.8 ± 0.2) × 103 M−1·s−1 from the slope. The calculated intercept was zero within its SE, consistent with slow-binding irreversible inhibition.
|
|
| 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. |
Effect of CoCl2, CEP-18770 and ONX-0914 on the expression and activity of HIF-1α. As depicted in one representative of the three performed western blots, the evaluated compounds have a profound effect on HIF-1α expression, as well on its function as it is assessed by the expression of its transcriptional target LDH-A (a).
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|
| S1290 |
CelastrolCelastrol is a potent proteasome inhibitor for the chymotrypsin-like activity of a purified 20S proteasome with IC50 of 2.5 μM. |
SK-BR-3, A549, HCT-116 and BT-474 cells were incubated with or without X66 for 1 h before exposed to GM, celastrol or MG132 for 8 h. Cell lysates were analyzed by Western blot with indicated antibodies. |
|
| S7038 |
EpoxomicinEpoxomicin 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 did not inhibit the EV71-induced PMLIII and IV degradation. Cell lysates were prepared from 293T cells infected or mock-infected with EV71 at a multiplicity of infection (MOI) of 5 for 24 or 48 h in the presence or absence of epoxomicin (1 µM). At 24 h post-infection (p.i.) (left panels) or 48 h p.i. (right panels), 60 μg of protein extracted from each treatment were separated on SDS-PAGE and analyzed by performing a Western blot analysis using antibodies specific for PMLIII and IV (top panels), VP1 (middle panels), and GAPDH, which served as an internal loading control (bottom panels). PMLIII and IV were quantified by performing densitometry and are presented relative to the mock infection, which was set as 1.0. VP1 was quantified and is presented relative to that in the EV71-infected 293T cells at 24 h p.i. (left panels) or 48 h p.i. (right panels). The density value of VP1 without epoxomicin is set as 1.0. The experiment was performed three times, and representative results are shown.
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| S7933 |
VR23VR23 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-1840PI-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 |
|---|---|---|---|
| S1013 |
Bortezomib (PS-341)Bortezomib (PS-341) is a potent 20S proteasome inhibitor with Ki of 0.6 nM. It exhibits favorable selectivity towards tumor cells over normal cells. |
Effect of different proteasome inhibitors on dysferlin expression and on membrane resealing in cultured primary myoblasts. Primary myoblasts from patient 2 harboring a homozygous Arg555Trp DYSF mutation that were treated with the indicated amounts of bortezomib for 24 hours. Western blots of protein extracts were stained with anti-dysferlin antibodies and with anti–a-tubulin antibody as loading control.
|
|
| S2619 |
MG-132MG132 is a potent cell-permeable proteasome and calpain inhibitor with IC50s of 0.1 and 1.2 μM for the inhibition of proteasome and calpain, respectively. |
MDA-MB-231 cells were treated with 10 uM MG132 and incubated under normoxia or hypoxia for 4 h. Endogenous interaction between LATS2 and SIAH2 was analysed by immunoprecipitation.
|
|
| 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. |
Validation of activity and specificity of chemical inhibitors of; ATM, ATR, and DNAPK. H460 cells were treated with 1 uM camptothecin (CPT) or 20 ug/ml bleomycin for 1 h in the presence of the indicated inhibitors: DNAPK-i1—NU7026, DNAPK-i2—NU7441. MSH6,
|
|
| S2181 |
Ixazomib (MLN9708)Ixazomib Citrate (MLN9708) immediately hydrolyzed to MLN2238, the biologically active form, on exposure to aqueous solutions or plasma. 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. Phase 3. |
LAT2 is degraded by proteasomes after treatment with alkylphospholipids. (A): 3-h treatment of NB4 cells before exposure to the proteasome inhibitor MG132 (10 M) prevented the reduction of LAT2 induced by 25 M ODPC. (B)(C): a similar effect was observed after exposure (30 min) of NB4 cells to the proteasome inhibitor MLN9708 (5 M) followed by treatment with 25 M ODPC (B) or 25 M perifosine (C).
|
|
| S2180 |
Ixazomib (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 in cell-free assays, respectively, also inhibits the caspase-like (β1) and trypsin-like (β2) proteolytic sites, with IC50 of 31 and 3500 nM. Phase 3. |
Primary myoblasts from patient 2 harboring a homozygous Arg555Trp DYSF mutation that were treated with the indicated amounts of MLN2238 for 24 hours.
|
|
| 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. |
The oprozomib-mediated inhibition of 20S proteasome activity exhibits slow-binding kinetics. (A) The effect of varying concentrations of oprozomib on the relative fluorescence increase due to the 20S proteasome-catalyzed hydrolysis of Suc-LLVY-AMC. Otherwise experimental conditions and comments are as in Fig. 3A above. (B) Plot of the pseudo-first order rate constant kobs calculated from curve fitting of progress curves to an equation describing slow-binding kinetics vs. the oprozomib concentration for the oprozomib-mediated inhibition of 20S proteasome activity. The solid straight line was linear-least squares calculated and yielded an apparent second order rate constant kon of (3.8 ± 0.2) × 103 M−1·s−1 from the slope. The calculated intercept was zero within its SE, consistent with slow-binding irreversible inhibition.
|
|
| 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. |
Effect of CoCl2, CEP-18770 and ONX-0914 on the expression and activity of HIF-1α. As depicted in one representative of the three performed western blots, the evaluated compounds have a profound effect on HIF-1α expression, as well on its function as it is assessed by the expression of its transcriptional target LDH-A (a).
|
|
| S1290 |
CelastrolCelastrol is a potent proteasome inhibitor for the chymotrypsin-like activity of a purified 20S proteasome with IC50 of 2.5 μM. |
SK-BR-3, A549, HCT-116 and BT-474 cells were incubated with or without X66 for 1 h before exposed to GM, celastrol or MG132 for 8 h. Cell lysates were analyzed by Western blot with indicated antibodies. |
|
| S7038 |
EpoxomicinEpoxomicin 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 did not inhibit the EV71-induced PMLIII and IV degradation. Cell lysates were prepared from 293T cells infected or mock-infected with EV71 at a multiplicity of infection (MOI) of 5 for 24 or 48 h in the presence or absence of epoxomicin (1 µM). At 24 h post-infection (p.i.) (left panels) or 48 h p.i. (right panels), 60 μg of protein extracted from each treatment were separated on SDS-PAGE and analyzed by performing a Western blot analysis using antibodies specific for PMLIII and IV (top panels), VP1 (middle panels), and GAPDH, which served as an internal loading control (bottom panels). PMLIII and IV were quantified by performing densitometry and are presented relative to the mock infection, which was set as 1.0. VP1 was quantified and is presented relative to that in the EV71-infected 293T cells at 24 h p.i. (left panels) or 48 h p.i. (right panels). The density value of VP1 without epoxomicin is set as 1.0. The experiment was performed three times, and representative results are shown.
|
|
| S7933 |
VR23VR23 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-1840PI-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). |
