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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
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 Aloxistatin(E64d) <1 mg/mL 68 mg/mL '''68 mg/mL
S7394 MDL-28170 <1 mg/mL 76 mg/mL '''''10 mg/mL
S0722 Cruzain-IN-1 <1 mg/mL 60 mg/mL ''''<1 mg/mL
S0194 Balicatib <1 mg/mL 82 mg/mL '''3 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
S7381 Pepstatin A <1 mg/mL 57 mg/mL ''1 mg/mL
S5611 2-cyano-Pyrimidine <1 mg/mL <1 mg/mL <1 mg/mL
S3012 Pazopanib <1 mg/mL 87 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.

S7379

E-64

E-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. E-64 induces oxidative stress and apoptosis in Filarial Parasite.

S3025

PMSF

PMSF is an irreversible serine/cysteine protease inhibitor.

S7393

Aloxistatin(E64d)

Aloxistatin is an irreversible and membrane-permeable cysteine protease inhibitor with blood platelet aggregation inhibiting activity.

S7394

MDL-28170

MDL-28170 (Calpain Inhibitor III) is a potent and selective calpain inhibitor of calpain that penetrates the blood-brain barrier and inhibits brain cysteine protease activity after systemic administration. MDL-28170 is also an inhibitor of γ-secretase.

S0722

Cruzain-IN-1

Cruzain-IN-1 is a selective inhibitor of trypanosomal cysteine proteases and a covalent and reversible Cruzain inhibitor with IC50 of 10 nM.

S0194

Balicatib

Balicatib (AAE-581) is a potent and selective inhibitor of the osteoclastic enzyme cathepsin K.

S7420

CA-074 methyl ester (CA-074 Me)

CA-074 methyl ester (CA-074 Me, Cathepsin B Inhibitor IV) is a membrane-permeable derivative of CA-074 and acts as an irreversible cathepsin B inhibitor.

S2847

Cathepsin Inhibitor 1

Cathepsin 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

Calpeptin

Calpeptin 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. Calpeptin attenuates apoptosis and intracellular inflammatory changes in muscle cells.

S7386

MG-101 (ALLN)

MG-101 (ALLN, Calpain inhibitor-1) is a cell-permeable and potent inhibitor of cysteine proteases including calpains and lysosomal cathepsins.

S7391

Z-FA-FMK

Z-FA-FMK is an irreversible cysteine protease inhibitor, and also inhibits effector caspases.

S7380

Leupeptin Hemisulfate

Leupeptin 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, NSC 694279, EP 475), 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. N-Ethylmaleimide (NEM) inactivates endogenous deubiquitinating enzymes (DUBs). N-Ethylmaleimide (NEM) specifically inhibits phosphate transport in mitochondria.

S7424

PD 151746

PD 151746 is a selective, cell-permeable calpain inhibitor with Ki of 0.26 μM for μ-Calpain, about 20-fold selectivity over m-calpain.

S7381

Pepstatin A

Pepstatin A (Pepstatin) is a potent aspartic protease inhibitor, and also inhibits HIV replication. Pepstatin A is also an inhibitor of cathepsins D and cathepsins E. Pepstatin A inhibits autophagy by suppressing lysosomal proteases.

S5611

2-cyano-Pyrimidine

2-cyano-Pyrimidine is a cathepsin K inhibitor with an IC50 of 170 nM.

S3012

Pazopanib

Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms/CSF1R with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively. Pazopanib induces cathepsin B activation and autophagy.

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-64

E-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. E-64 induces oxidative stress and apoptosis in Filarial Parasite.

S3025

PMSF

PMSF is an irreversible serine/cysteine protease inhibitor.

S7393

Aloxistatin(E64d)

Aloxistatin is an irreversible and membrane-permeable cysteine protease inhibitor with blood platelet aggregation inhibiting activity.

S7394

MDL-28170

MDL-28170 (Calpain Inhibitor III) is a potent and selective calpain inhibitor of calpain that penetrates the blood-brain barrier and inhibits brain cysteine protease activity after systemic administration. MDL-28170 is also an inhibitor of γ-secretase.

S0722

Cruzain-IN-1

Cruzain-IN-1 is a selective inhibitor of trypanosomal cysteine proteases and a covalent and reversible Cruzain inhibitor with IC50 of 10 nM.

S0194

Balicatib

Balicatib (AAE-581) is a potent and selective inhibitor of the osteoclastic enzyme cathepsin K.

S7420

CA-074 methyl ester (CA-074 Me)

CA-074 methyl ester (CA-074 Me, Cathepsin B Inhibitor IV) is a membrane-permeable derivative of CA-074 and acts as an irreversible cathepsin B inhibitor.

S2847

Cathepsin Inhibitor 1

Cathepsin 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

Calpeptin

Calpeptin 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. Calpeptin attenuates apoptosis and intracellular inflammatory changes in muscle cells.

S7386

MG-101 (ALLN)

MG-101 (ALLN, Calpain inhibitor-1) is a cell-permeable and potent inhibitor of cysteine proteases including calpains and lysosomal cathepsins.

S7391

Z-FA-FMK

Z-FA-FMK is an irreversible cysteine protease inhibitor, and also inhibits effector caspases.

S7380

Leupeptin Hemisulfate

Leupeptin 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, NSC 694279, EP 475), 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. N-Ethylmaleimide (NEM) inactivates endogenous deubiquitinating enzymes (DUBs). N-Ethylmaleimide (NEM) specifically inhibits phosphate transport in mitochondria.

S7424

PD 151746

PD 151746 is a selective, cell-permeable calpain inhibitor with Ki of 0.26 μM for μ-Calpain, about 20-fold selectivity over m-calpain.

S7381

Pepstatin A

Pepstatin A (Pepstatin) is a potent aspartic protease inhibitor, and also inhibits HIV replication. Pepstatin A is also an inhibitor of cathepsins D and cathepsins E. Pepstatin A inhibits autophagy by suppressing lysosomal proteases.

S5611

2-cyano-Pyrimidine

2-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
S3012

Pazopanib

Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms/CSF1R with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively. Pazopanib induces cathepsin B activation and autophagy.

2020, 5;31(5):892-908 e11

2020, 10(3):240-253

2020, 27;12(5)pii: E1087