20S proteasome 选择性抑制剂

目录号 产品名 产品描述 Selective / Pan IC50 / Ki
S1013 Bortezomib (PS-341)

Bortezomib (PS-341)是有效的蛋白酶抑制剂,Ki为0.6 nM。它对肿瘤细胞表现出良好的选择性。

Selective 20S proteasome, Ki: 0.6 nM
S4432 Ixazomib Citrate (MLN9708)

Ixazomib citrate (MLN9708, Ninlaro) is a prodrug of Ixazomib (MLN2238), which is a selective, orally bioavailable inhibitor of 20S proteasome that inhibits the chymotrypsin-like proteolytic (β5) site with IC50 of 3.4 nM and Ki of 0.93 nM, respectively. Ixazomib (MLN2238) also inhibits caspase-like (β1) and trypsin-like (β2) proteolytic sites with IC50 of 31 nM and 3500 nM, respectively.

Selective 20S proteasome β2 site, IC50: 3500 nM; 20S proteasome β1 site, IC50: 31 nM; 20S proteasome β5 site, Ki: 0.93 nM; 20S proteasome β5 site, IC50: 3.4 nM
S2180 Ixazomib (MLN2238)

MLN2238抑制20S proteasome的糜蛋白酶样蛋白水解(β5)位点,无细胞试验中IC50Ki分别为3.4 nM和0.93 nM,也抑制胱天蛋白酶样(β1)和胰蛋白酶样(β2)蛋白水解位点,IC50分别为31和3500 nM。Phase 3。

Selective 20S proteasome, IC50: 3.4 nM; 20S proteasome, Ki: 0.93 nM
S2181 Ixazomib Citrate (MLN9708) Analogue

Ixazomib Citrate (MLN9708)在水溶液或血浆中立即水解为具有具有生物活性的MLN2238。MLN2238抑制20S proteasome的胰凝乳蛋白酶等蛋白水解位点(β5),无细胞试验中IC50/Ki为3.4 nM/0.93 nM,对β1作用效果稍弱,对β2几乎没有抑制活性。Phase 3。

Selective 20S proteasome, IC50: 3.4 nM; 20S proteasome, Ki: 0.93 nM
S7504 Salinosporamide A (NPI-0052)

Salinosporamide A (NPI-0052, ML858, Marizomib, MRZ) 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.

Selective T-L β2, IC50: 28 nM; CT-L β5, IC50: 3.5 nM; C-L β1, IC50: 430 nM
S1157 Delanzomib (CEP-18770)

Delanzomib (CEP-18770)是一种口服有效的,具有胰凝乳蛋白酶样活性的蛋白酶体抑制剂,IC50为3.8 nM,只最低限度地抑制蛋白酶体的胰蛋白酶和肽谷氨酰基活性。Phase 1/2。

Selective Chymotrypsin-like proteasome, IC50: 3.8 nM
S7172 ONX-0914 (PR-957)

ONX-0914 (PR-957)是一种有效的,选择性immunoproteasome抑制剂,无细胞试验中对组成型蛋白酶体具有最低的交叉反应性。

Selective LMP7, IC50: ~10 nM
S7462 PI-1840

PI-1840 是一种可逆的选择性的chymotrypsin-like (CT-L)抑制剂,IC50为 27 nM,对其他两个主要的蛋白酶体(trypsin-like (T-L)和 postglutamyl-peptide-hydrolysis-like (PGPH-L))蛋白水解活动没有作用。

Selective Chymotrypsin-like proteasome, IC50: 27 nM
S7049 Oprozomib (ONX 0912)

Oprozomib (ONX 0912)是一种口服生物有效的抑制剂,抑制20S proteasome(20S蛋白酶体)β5/LMP7的CT-L活性,IC50为36 nM/82 nM。Phase 1/2。

Selective 20S proteasome LMP7, IC50: 82 nM; 20S proteasome β5, IC50: 36 nM
S1290 Celastrol (NSC 70931)

Celastrol是一种有效的蛋白酶抑制剂,有效且优先抑制胰凝乳蛋白酶样的纯化的20S proteasome 的活性,IC50为2.5 μM。

Selective 20S proteasome, IC50: 2.5 μM
S7038 Epoxomicin (BU-4061T)

Epoxomicin是一种选择性蛋白酶体抑制剂,具有抗炎活性,首要抑制20S蛋白酶体的CH-L活性,也抑制T-L和PGPH催化活性。

Selective