システインプロテアーゼ
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 | ||
| S1115 | Odanacatib (MK-0822) | <1 mg/mL | 100 mg/mL | <1 mg/mL |
| S7379 | E-64 | 11 mg/mL | 71 mg/mL | <1 mg/mL |
| S3025 | PMSF | <1 mg/mL | 35 mg/mL | 15 mg/mL |
| S7393 | E-64d (Aloxistatin, Loxistatin) | <1 mg/mL | 68 mg/mL | ''68 mg/mL |
| S7420 | CA-074 methyl ester (CA-074 Me) | 5.7 mg/mL | 79 mg/mL | 79 mg/mL |
| S2847 | Cathepsin Inhibitor 1 | <1 mg/mL | 80 mg/mL | 50 mg/mL |
| S7396 | Calpeptin | <1 mg/mL | 72 mg/mL | 72 mg/mL |
| S7386 | MG-101 (ALLN) | <1 mg/mL | 76 mg/mL | 76 mg/mL |
| S7391 | Z-FA-FMK | <1 mg/mL | 77 mg/mL | 34 mg/mL |
| S7380 | Leupeptin Hemisulfate | 95 mg/mL | 95 mg/mL | 95 mg/mL |
| S7392 | Loxistatin Acid (E-64C) | 2 mg/mL | 62 mg/mL | '62 mg/mL |
| S3692 | N-Ethylmaleimide (NEM) | 25 mg/mL | 25 mg/mL | 25 mg/mL |
| S7424 | PD 151746 | <1 mg/mL | 47 mg/mL | 47 mg/mL |
| S5611 | 2-cyano-Pyrimidine | <1 mg/mL | <1 mg/mL | <1 mg/mL |
Cysteine Protease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 |
|---|---|---|---|
| S1115 |
Odanacatib (MK-0822)Odanacatib (MK 0822) is a potent, selective, and neutral inhibitor of cathepsin K (human/rabbit) with IC50 of 0.2 nM/1 nM, and demonstrated high selectivity versus off-target cathepsin B, L, S. Phase 3. |
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| S7379 |
E-64E-64 is an irreversible and selective cysteine protease inhibitor, and also inhibits papain, calpain, and cathepsins B and H, but not serine proteases or aspartic proteases. The IC50 for papain is 9 nM. |
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| S3025 |
PMSFPMSF is an irreversible serine/cysteine protease inhibitor. |
||
| S7393 |
E-64d (Aloxistatin, Loxistatin)Aloxistatin is an irreversible and membrane-permeable cysteine protease inhibitor with blood platelet aggregation inhibiting activity. |
||
| S7420 |
CA-074 methyl ester (CA-074 Me)CA-074 Me is a membrane-permeable derivative of CA-074 and acts as an irreversible cathepsin B inhibitor. |
||
| S2847 |
Cathepsin Inhibitor 1Cathepsin Inhibitor 1 is an inhibitor of Cathepsin (L, L2, S, K, B) with pIC50 of 7.9, 6.7, 6.0, 5.5 and 5.2, respectively. |
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| S7396 |
CalpeptinCalpeptin is a potent, cell-permeable calpain inhibitor with ID50 of 52 nM, 34 nM, 138 nM, and 40 nM for Calpain I (porcine erythrocytes), Calpain II (porcine kidney), Papainb, and Calpain I (human platelets), respectively. |
Western blotting detection of focal adhesion kinase (FAK) expression and its cleaved fragments with different treatments. DTX represents docetaxel, CPP represents calpeptin (a calpain inhibitor). The experiments were carried out 3 times, obtaining essentially similar results.
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| S7386 |
MG-101 (ALLN)MG-101 (ALLN) is a cell-permeable and potent inhibitor of cysteine proteases including calpains and lysosomal cathepsins. |
Proteins from different subcellular compartments were efficiently separated without relevant cross-contamination: tight junction-protein claudin-5 (→ plasma membrane) was almost exclusively isolated together with proteins from membranes and organelles, and actin was only present in the fraction containing cytoskeleton proteins. Stronger signals in the lanes with samples from cells treated with the inhibitor MG-101 are due to the general inhibition of intracellular protein degradation.
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| S7391 |
Z-FA-FMKZ-FA-FMK is an irreversible cysteine protease inhibitor, and also inhibits effector caspases. |
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| S7380 |
Leupeptin HemisulfateLeupeptin Hemisulfate is a reversible inhibitor of serine and cysteine proteases. It inhibits cathepsin B (Ki = 6 nM), calpain (Ki = 10 nM), trypsin (Ki = 35 nM), plasmin (Ki = 3.4 μM), and kallikrein (Ki = 19 μM), and has no effect against chymotrypsin, elastase, renin, or pepsin. |
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| S7392 |
Loxistatin Acid (E-64C)Loxistatin Acid (E-64C), a derivative of E-64, is an irreversible and membrane-permeant cysteine protease inhibitor. The cysteine protease cathepsin L is required for SARS-CoV-2 viral entry. |
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| S3692 |
N-Ethylmaleimide (NEM)N-Ethylmaleimide (NEM) is an organic compound that is derived from maleic acid. It is an irreversible inhibitor of all cysteine peptidases, with alkylation occurring at the active site thiol group. |
||
| S7424 |
PD 151746PD 151746 is a selective, cell-permeable calpain inhibitor with Ki of 0.26 μM for μ-Calpain, about 20-fold selectivity over m-calpain. |
(A) Quantification of mS100a7a15 mRNA expression of skin from normal and imiquimod-induced psoriatic mouse backs at 5 days. (B) Immunoblot of mS100a7a15, IL-1α and calpain-1 in skin extracts from normal and imiquimod-induced psoriatic mouse backs. (C) HE staining and immunohistochemical analysis of mS100a7a15, calpain-1 in skin tissues as described in fig 4A. The scale bars represent 100 μm. All data are representative of three independent experiments with n = 6 and are means ± SEM. P values were determined by two-tailed t test. *** P<0.001.
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| S5611 |
2-cyano-Pyrimidine2-cyano-Pyrimidine is a cathepsin K inhibitor with an IC50 of 170 nM. |
| 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 |
|---|---|---|---|
| S1115 |
Odanacatib (MK-0822)Odanacatib (MK 0822) is a potent, selective, and neutral inhibitor of cathepsin K (human/rabbit) with IC50 of 0.2 nM/1 nM, and demonstrated high selectivity versus off-target cathepsin B, L, S. Phase 3. |
|
|
| S7379 |
E-64E-64 is an irreversible and selective cysteine protease inhibitor, and also inhibits papain, calpain, and cathepsins B and H, but not serine proteases or aspartic proteases. The IC50 for papain is 9 nM. |
||
| S3025 |
PMSFPMSF is an irreversible serine/cysteine protease inhibitor. |
||
| S7393 |
E-64d (Aloxistatin, Loxistatin)Aloxistatin is an irreversible and membrane-permeable cysteine protease inhibitor with blood platelet aggregation inhibiting activity. |
||
| S7420 |
CA-074 methyl ester (CA-074 Me)CA-074 Me is a membrane-permeable derivative of CA-074 and acts as an irreversible cathepsin B inhibitor. |
||
| S2847 |
Cathepsin Inhibitor 1Cathepsin Inhibitor 1 is an inhibitor of Cathepsin (L, L2, S, K, B) with pIC50 of 7.9, 6.7, 6.0, 5.5 and 5.2, respectively. |
||
| S7396 |
CalpeptinCalpeptin is a potent, cell-permeable calpain inhibitor with ID50 of 52 nM, 34 nM, 138 nM, and 40 nM for Calpain I (porcine erythrocytes), Calpain II (porcine kidney), Papainb, and Calpain I (human platelets), respectively. |
Western blotting detection of focal adhesion kinase (FAK) expression and its cleaved fragments with different treatments. DTX represents docetaxel, CPP represents calpeptin (a calpain inhibitor). The experiments were carried out 3 times, obtaining essentially similar results.
|
|
| S7386 |
MG-101 (ALLN)MG-101 (ALLN) is a cell-permeable and potent inhibitor of cysteine proteases including calpains and lysosomal cathepsins. |
Proteins from different subcellular compartments were efficiently separated without relevant cross-contamination: tight junction-protein claudin-5 (→ plasma membrane) was almost exclusively isolated together with proteins from membranes and organelles, and actin was only present in the fraction containing cytoskeleton proteins. Stronger signals in the lanes with samples from cells treated with the inhibitor MG-101 are due to the general inhibition of intracellular protein degradation.
|
|
| S7391 |
Z-FA-FMKZ-FA-FMK is an irreversible cysteine protease inhibitor, and also inhibits effector caspases. |
||
| S7380 |
Leupeptin HemisulfateLeupeptin Hemisulfate is a reversible inhibitor of serine and cysteine proteases. It inhibits cathepsin B (Ki = 6 nM), calpain (Ki = 10 nM), trypsin (Ki = 35 nM), plasmin (Ki = 3.4 μM), and kallikrein (Ki = 19 μM), and has no effect against chymotrypsin, elastase, renin, or pepsin. |
||
| S7392 |
Loxistatin Acid (E-64C)Loxistatin Acid (E-64C), a derivative of E-64, is an irreversible and membrane-permeant cysteine protease inhibitor. The cysteine protease cathepsin L is required for SARS-CoV-2 viral entry. |
||
| S3692 |
N-Ethylmaleimide (NEM)N-Ethylmaleimide (NEM) is an organic compound that is derived from maleic acid. It is an irreversible inhibitor of all cysteine peptidases, with alkylation occurring at the active site thiol group. |
||
| S7424 |
PD 151746PD 151746 is a selective, cell-permeable calpain inhibitor with Ki of 0.26 μM for μ-Calpain, about 20-fold selectivity over m-calpain. |
(A) Quantification of mS100a7a15 mRNA expression of skin from normal and imiquimod-induced psoriatic mouse backs at 5 days. (B) Immunoblot of mS100a7a15, IL-1α and calpain-1 in skin extracts from normal and imiquimod-induced psoriatic mouse backs. (C) HE staining and immunohistochemical analysis of mS100a7a15, calpain-1 in skin tissues as described in fig 4A. The scale bars represent 100 μm. All data are representative of three independent experiments with n = 6 and are means ± SEM. P values were determined by two-tailed t test. *** P<0.001.
|
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| S5611 |
2-cyano-Pyrimidine2-cyano-Pyrimidine is a cathepsin K inhibitor with an IC50 of 170 nM. |
