Proteasome(蛋白酶体)

The proteasome is a large multisubunit complex of approximately 2.5 MDa that mediates a wide range of physiological and pathological cellular processes by selectively degrading unnecessary proteins in eukaryotes. The structure of a proteasome is comprised of the catalytic core particle (CP) and two terminal regulatory particles (RPs). The CP (also known as the 20S proteasome) is a barrel shaped multisubunit complex (approximately 750 kDa) consisting of four axially stacked heptameric rings (two outer α-rings and two inner β-rings) with 7 subunits in each ring, where three β subunits (β1, β2 and β5) contain catalytically active threonine residues and are associated with caspase-like, trypsin-like and chymotrypsin-like activities respectively.

Products for Proteasome

Cat.No. 产品名称 Information
GC11640 MDL 28170
Calpain Inhibitor III
A cell permeable, selective calpain inhibitor
GC17255 Gliotoxin
胶霉毒素,Aspergillin
An immunosuppressive mycotoxin with diverse biological effects
GC10342 Calpeptin A calpain inhibitor
GC10486 Salinosporamide A (NPI-0052, Marizomib)
马里佐米,salinosporamide A, MARIZOMIB, NPI-0052, (-)-Salinosporamide A
An orally bioactive proteasome inhibitor
GC15778 ONX-0914 (PR-957)
ONX-0914,PR-957
A selective inhibitor of the β5i (LMP7) subunit of the immunoproteasome
GC12784 Artemether (SM-224)
蒿甲醚; Dihydroqinghaosu methyl ether; Dihydroartemisinin methyl ether; SM224
An antiparasitic compound
GC13711 Gabexate mesylate
甲磺酸加贝酯; FOY
A serine protease inhibitor
GC12272 CEP-18770
CEP-18770
An inhibitor of chymotrypsin-like proteasome activity
GC16146 MLN2238
艾沙佐米; MLN2238
A 20S proteasome inhibitor and an active metabolite of MLN9708
GC13718 MLN9708
艾沙佐米柠檬酸盐,MLN-9708, MLN 9708
A prodrug form of MLN2238
GC15517 MG-262
PS-III,MG262,MG 262
A proteasome inhibitor with diverse biological activities
GC16747 Dihydroeponemycin
Dihydroeponemycin,uk101
Dihydroeponemycin 是抗肿瘤和抗血管生成天然产物eponemycin 的类似物，选择性靶向20S 蛋白酶体。 Dihydroeponemycin 共价修饰催化蛋白酶体亚基的一个子集，优先与 IFN-γ 诱导亚基 LMP2 和 LMP7 结合。 Dihydroeponemycin 介导的蛋白酶体抑制诱导纺锤样细胞形态变化和细胞凋亡。
GC13789 AM 114
PS-IX; AM114
AM 114 (PS-IX; AM114) 是查尔酮衍生物和 20S 蛋白酶体抑制剂的糜蛋白酶样活性，IC50 值为 ~1 μM. AM 114 表现出 HCT116 p53+/+ 细胞生长抑制活性，IC50 值为 1.49 μM. AM 114 具有强大的抗癌活性。
GC15447 Oprozomib (ONX-0912)
ONX-0912,ONX0912,ONX 0912,PR 047,Oprozomib
An orally available proteasome inhibitor
GC15089 Carfilzomib (PR-171)
卡非佐米; PR-171
A proteasome inhibitor
GC13865 PSI
Z-异亮氨酰-叔丁基谷氨酰-丙氨酸-亮氨酸缩醛,Z-Ile-Glu(OtBu)-Ala-Leu-CHO
PSI (Proteasome Inhibitor 1) 是一种有效的蛋白酶体抑制剂。
GC17644 Bortezomib (PS-341)
硼替佐米; PS-341; LDP-341; NSC 681239

Bortezomib (PS-341) 作为一种具有抗肿瘤活性的二肽硼酸蛋白酶体抑制剂,可通过靶向苏氨酸残基,有效抑制Ki为0.6 nM的20S蛋白酶体。
GC10178 MG-115
MG115,蛋白酶体抑制剂,Carbobenzoxy-L-leucyl-L-leucyl-L-norvalinal, Z-LL-Nva-CHO, Proteasome Inhibitor XII,MG115
MG-115 是一种有效的抑制剂，对 20S 和 26S 蛋白酶体的 Kis 分别为 21 nM 和 35 nM 。
GC10383 MG-132
MG132,蛋白酶体抑制剂,MG132,Z-LLL-al,Z-Leu-Leu-Leu-CHO
MG-132是一种强效、可逆和细胞渗透的蛋白酶体抑制剂，属于合成肽醛类。
GC12494 Epoxomicin
环氧酶素; BU-4061T
环氧霉素（Epoxomicin）是一种选择性蛋白酶体抑制剂，有效地抑制20S蛋白酶体的胰凝乳蛋白酶样（CH-L）活性，IC50约为40-80nM。
GC13123 Lactacystin (Synthetic)
蛋白酶体抑制剂

A selective inhibitor of the 20S proteasome
GC16581 Clasto-Lactacystin β-lactone
β-Clastolactacystin; Omuralide
A selective inhibitor of the 20S proteasome
GC15083 Celastrol
雷公藤红素; Celastrol
Celastrol是一种蛋白酶体抑制剂，有效且优先的抑制纯化的20S蛋白酶体，IC₅₀ 为2.5 μM。
GC12527 Calpain Inhibitor I, ALLN
ALLN钙蛋白酶抑制剂,Ac-LLnL-CHO, MG-101, MG101,N-Acetyl-L-leucyl-L-leucyl-L-norleucinal, N-Acetyl-Leu-Leu-Nle-al,Calpain Inhibitor I
A non-selective cysteine protease inhibitor
GC10102 Aclacinomycin A
阿克拉霉素,Jaclacin,Aclarubicin,Aclarubicin A
An anthracycline with antibiotic and anticancer activities
GC11974 Pepstatin A
抑肽素; Pepstatin A
胃抑素Pepstatin A是由放线菌类产生的一种特异性的、具有口服活性的天冬氨酸蛋白酶 (aspartic proteases) 抑制剂,能够抑制 hemoglobin-pepsin、hemoglobin-proctase、casein-pepsin、casein-proctase、casein-acid protease 和 hemoglobin-acid protease 的活性,IC50 值分别为 4.5 nM、6.2 nM、150 nM、290 nM、520 nM 和 260 nM；Pepstatin A可抑制 HIV protease 的活性.Pepstatin A (0-120 µM) 抑制了受体活化因子NF-κB配体(RANKL)-诱导的破骨细胞分化。