プロテアソーム
シグナル伝達経路
研究分野
- 阻害剤の選択性比較
- 溶解度
| 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 |
| 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 |
| 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阻害剤(12)
| 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. |
Immunoblot analysis of cell lysates from the indicated cell lines treated with GNE-6776 (2 μ M for 18 h), either alone or in combination with a UAE1 inhibitor MLN-7243 (5 μ M for 45 min) or the proteasome inhibitor bortezomib (5 μ M for 45 min) as indicated.
|
|
| 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. |
Western blot of IκBζ expression in BMDMs treated with DI and stimulated with LPS for 1 h. MG132 or bafilomycin A (BafA) were added 30 min before LPS stimulation.
|
|
| 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.
|
|
| 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. |
Dependence of SPRI signal on receptor concentration: (a) ONX 0914 inhibitor, (b) inhibitor 5. 20Si concentration: 2.8 μg/mL, pH 7.4
|
|
| 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. |
||
| 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). |
