33
14
Cat. No. | Product Name | Target | Signaling Pathways |
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T36218 |
19R(20S)-EpDPA
|
||
19R(20S)-EpDPA is an oxylipin and a metabolite of docosahexaenoic acid .1,2It is formed from DHA by various cytochrome P450 (CYP) isoforms in a stereoselective manner.219R(20S)-EpDPA (30 nM) prevents calcium-induced increases in the spontaneous beating of isolated neonatal rat cardiomyocytes (NRCMs).3 1.Cinelli, M.A., Yang, J., Scharmen, A., et al.Enzymatic synthesis and chemical inversion provide both enantiomers of bioactive epoxydocosapentaenoic acidsJ. Lipid Res.59(11)2237-2252(2018) 2.Lucas... | |||
T63321 |
20S Proteasome activator 1
|
Proteasome | Proteases/Proteasome; Ubiquitination |
20S Proteasome activator 1 是一种 20S 蛋白酶激活剂,对胰蛋白酶样位点、胰凝乳蛋白酶样位点和半胱天冬酶位点的 IC50 分别为 0.3 μM、0.7 μM 和 1.8 μM。20S Proteasome activator 1 通过在细胞系统中翻译来防止致病性 α-synuclein A53T 突变体积累从而减少疾病发生的概率。20S Proteasome activator 1 可用于研究神经退行性疾病。 | |||
T62255 |
20S Proteasome-IN-4
|
||
20S Proteasome-IN-4 (Compound 7) 是一种能透过血脑屏障的、寄生虫选择性的、具有口服活性的20Sproteasome 抑制剂,对T. b. brucei20S 蛋白酶体的IC50为 6.3 nM。20S Proteasome-IN-4 可用于非洲人类锥虫病的研究。 | |||
T7814 |
Alloxan monohydrate
|
Proteasome | Proteases/Proteasome; Ubiquitination |
Alloxan Monohydrate 是一种能够引起糖尿病的致糖尿病药物。它作为蛋白酶体抑制剂,破坏胰腺中能够分泌胰岛素的B 细胞,导致实验动物患糖尿病。 | |||
T17011 |
TCH-165
|
Proteasome | Proteases/Proteasome; Ubiquitination |
TCH-165 是一种蛋白酶体组装的小分子调节剂,可增加游离 20S 水平,进而增强 IDP 蛋白水解。 | |||
T21854 |
Proteasome inhibitor IX
PS-IX,AM114 |
Proteasome | Proteases/Proteasome; Ubiquitination |
Proteasome inhibitor IX (PS-IX) 是 Chalcone 的一种衍生物,对20S 蛋白酶体的胰凝乳蛋白酶样活性有抑制作用,IC50约为 1 μM。它抑制 HCT116 p53+/+细胞生长,IC50为 1.49 μM,显示出有效的抗癌活性。 | |||
T10061 |
(1S,2S)-Bortezomib
Bortezomib,硼替佐米(1S,2S) |
Proteasome | Proteases/Proteasome; Ubiquitination |
(1S,2S)-Bortezomib (Bortezomib) 是 Bortezomib 的对映异构体。 Bortezomib 是一种可逆的选择性蛋白酶体抑制剂,对 20S 蛋白酶体的 Ki 为 0.6 nM。 | |||
T2016 |
MLN9708
Ixazomib Citrate |
Proteasome | Proteases/Proteasome; Ubiquitination |
MLN9708 (Ixazomib Citrate) 抑制 20S 蛋白酶体的糜蛋白酶样蛋白水解 (β5) 位点 (Ki50=0.93 nM, IC50=3.4 nM/)。 MLN9708 的生物活性形式是水溶液或血浆中的 MLN2238。 | |||
T2399 |
Bortezomib
Radiciol,NSC 681239,硼替佐米,MG 341,DPBA,Brotezamide,LDP 341 |
Apoptosis; NF-κB; Proteasome; Autophagy | Apoptosis; Autophagy; NF-κB; Proteases/Proteasome; Ubiquitination |
Bortezomib (LDP 341) 是一种 20S 蛋白酶体抑制剂 (Ki=0.6 nM),具有可逆性和选择性。Bortezomib 具有抗肿瘤活性,可以抑制 NF-κB,可破坏细胞周期、诱导细胞凋亡。 | |||
T2122 |
Ixazomib
艾沙佐米,MLN2238 |
Proteasome; Caspase; Autophagy | Apoptosis; Autophagy; Proteases/Proteasome; Ubiquitination |
Ixazomib (MLN2238) 含硼肽蛋白酶体抑制剂(PI),可抑制 20S 蛋白酶体的糜蛋白酶样蛋白水解 (β5) 位点,IC50为 3.4 nM,Ki 为 0.93 nM。它还抑制半胱天冬酶样 (β1) 和胰蛋白酶样 (β2) 蛋白水解位点,IC50值为 31和3500 nM。 | |||
T6041 |
Oprozomib
PR-047,奥泼佐米,ONX 0912 |
Proteasome; Autophagy | Autophagy; Proteases/Proteasome; Ubiquitination |
Oprozomib (PR-047) 是一种可口服的选择性肽环氧酮类蛋白酶体抑制剂,诱导多发性骨髓瘤细胞凋亡。它对蛋白酶体 (β5) 和免疫蛋白酶体 (LMP7) 的 IC50分别为 36 和 82 nM。 | |||
T1795 |
Carfilzomib
卡非佐米,PR-171 |
Apoptosis; Proteasome; Autophagy | Apoptosis; Autophagy; Proteases/Proteasome; Ubiquitination |
Carfilzomib (PR-171) 是一种蛋白酶体抑制剂,与 20S 蛋白酶体的糜蛋白酶不可逆结合。Carfilzomib 具有抗肿瘤活性,可以用于治疗多发性骨髓瘤。 | |||
T8397 |
Ixazomib citrate
枸橼酸艾沙佐米,MLN9708 |
Proteasome; Autophagy | Autophagy; Proteases/Proteasome; Ubiquitination |
Ixazomib citrate (MLN9708) 是 Ixazomib 的前药,是20S 蛋白酶体胰凝乳蛋白酶样蛋白水解β5位点的可逆抑制剂,IC50为3.4 nM 和Ki 为0.93 nM。 | |||
T21617 |
MG-115
Z-LL-Nva-CHO |
Proteasome | Proteases/Proteasome; Ubiquitination |
MG-115 (Z-LL-Nva-CHO) 是一种有效且可逆的蛋白酶体抑制剂,对20S 和26S 蛋白酶体的 Ki 值分别为 21 nM 和 35 nM。MG-115 特异性抑制蛋白酶体的胰凝乳蛋白酶样活性,诱导 p53 依赖性细胞凋亡。 | |||
T12579 |
RAMB4
PTP1B-IN-9 |
Proteasome | Proteases/Proteasome; Ubiquitination |
RAMB4 (PTP1B-IN-9) 是一种泛素-蛋白酶体系统(UPS)应激源,是通过抑制 20S 蛋白酶体催化活性物质上游泛素介导的蛋白质降解而产生。它能够在不影响 20S 蛋白酶体催化活性的情况下触发泛素蛋白酶体系统 (UPS) 应激反应。 | |||
T36352 |
Suc-Leu-Tyr-AMC
|
||
Suc-Leu-Tyr-AMC 是钙蛋白酶 I 和 II 以及木瓜蛋白酶(另一种半胱氨酸蛋白酶)的荧光底物,用于测量 20S 蛋白酶体的糜蛋白酶样肽酶活性(Ex-max:360 nm;Em-max:460 nm)。Suc-Leu-Tyr-AMC 也能被大肠杆菌的 Ti 蛋白酶裂解。 | |||
T6300 |
Degrasyn
WP1130 |
Apoptosis; JAK; Bcr-Abl; DUB; Autophagy | Angiogenesis; Apoptosis; Autophagy; Cell Cycle/Checkpoint; Chromatin/Epigenetic; Cytoskeletal Signaling; DNA Damage/DNA Repair; JAK/STAT signaling; Stem Cells; Tyrosine Kinase/Adaptors; Ubiquitination |
Degrasyn (WP1130) 是一种可渗透细胞的去泛素化酶(DUB)抑制剂,直接抑制USP9x,USP5,USP14和UCH37的DUB 活性。 它减弱抗细胞凋亡蛋白Bcr-Abl 和JAK2。 | |||
T8464 |
RA-9
|
Apoptosis; DUB | Apoptosis; Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Ubiquitination |
RA-9 是一种高选择性蛋白酶体相关的 DUBs 抑制剂,具有良好的毒性和抗癌活性。它阻断泛素依赖性蛋白降解而不影响 20S 蛋白酶体蛋白水解活性。它诱导卵巢癌细胞内质网应激反应,选择性诱导卵巢癌细胞株和供体原代培养细胞凋亡。 | |||
T77796 |
DL-Borneol
(endo)-Borneol,Borneol,(±)-Borneol |
GABA Receptor; Endogenous Metabolite | Membrane transporter/Ion channel; Metabolism; Neuroscience |
DL-Borneol ((endo)-Borneol) 是一种从中药中提取的小分子,是一种可口服的生物佐剂,可以改善药物向大脑的输送,常用作治疗心脑血管疾病的中药的辅助成分。 | |||
T37011 |
Boc-LRR-AMC
|
||
Boc-LRR-AMC is a fluorogenic substrate for the trypsin-like activity of the 26S proteasome or 20S proteolytic core. Upon enzymatic cleavage by the 26S proteasome or 20S proteolytic core, amino-4-methylcoumarin (AMC) is released and its fluorescence can be used to quantify 26S proteasome or 20S proteolytic core trypsin-like activity. AMC displays excitation/emission maxima of 340-360/440-460 nm, respectively. | |||
T82529 |
DPLG3
|
||
DPLG3是一种免疫蛋白酶体β5i亚基的特异性抑制剂,其对小鼠i-20S的IC50值为9.4 nM,可应用于免疫疾病相关研究领域。 | |||
T27558 |
HT1042
HT 1042,HT-1042 |
||
HT1042 is an inhibitor of the β5i component of the 20S proteasome complex, it is used to aid in the treatment of inflammatory diseases, autoimmune and hematologic malignancies. | |||
T37420 |
Ac-ANW-AMC
Ac-ANW-AMC,Ac-Ala-Asn-Trp-AMC |
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Ac-ANW-AMC is a fluorogenic substrate for the β5i/LMP7 subunit of the 20S immunoproteasome. [1] Upon cleavage, 7-amino-4-methylcoumarin (AMC) is released and its fluorescence can be used to quantify the activity of the β5i/LMP7 subunit of the 20S immunoproteasome. AMC displays excitation/emission maxima of 340-360/440-460 nm, respectively. Reference[1]. Winter, M.B., La Greca, F., Arastu-Kapur, S., et al. Immunoproteasome functions explained by divergence in cleavage specificity and regulation. ... | |||
T37421 |
Ac-PAL-AMC
|
||
Ac-PAL-AMC is a fluorogenic substrate for the β1i/LMP2 subunit of the 20S immunoproteasome. Upon cleavage, 7-amino-4-methylcoumarin (AMC) is released and its fluorescence can be used to quantify the activity of the β1i/LMP2 subunit of the 20S immunoproteasome. Ac-PAL-AMC is selective for the immunoproteasome over the constitutive proteasome. AMC displays excitation/emission maxima of 351/430 nm, respectively. | |||
T78847 | BC-05 | Others | Others |
BC-05为一CD13及20S蛋白酶体的口服有效抑制剂,分别对人CD13和20S蛋白酶体的IC50值为0.13 μM与1.39 μM。该化合物适用于进行多发性骨髓瘤相关研究。 | |||
T2154 |
MG-132
Z-LLL-al,Z-Leu-Leu-Leu-CHO |
Apoptosis; Proteasome; Autophagy | Apoptosis; Autophagy; Proteases/Proteasome; Ubiquitination |
MG-132 (Z-Leu-Leu-Leu-al) 是一种 26S 蛋白酶体抑制剂 (IC50=100 nM),具有细胞渗透性、可逆性。MG-132 可作为自噬激活剂,可诱导凋亡。 | |||
T73191 | LONP1-IN-2 | ||
LONP1-IN-2 是一种有效的选择性 LONP1抑制剂,对 LONP1 和 20S 蛋白酶体的IC50值分别为 0.187 μM 和 >10 μM。LONP1-IN-2可用于癌症研究。 | |||
TP1308 |
Suc-Leu-Leu-Val-Tyr-AMC
|
||
Suc-Leu-Leu-Val-Tyr-AMC is a fluorescent substrate for the 20S proteasome, other chymotrypsin-like proteases. | |||
T74878 |
Enzyme-IN-1
|
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Enzyme-IN-1(compound 1)为基于肽的N端亲核试剂(Ntn)水解酶抑制剂,特别针对20S蛋白酶体的糜胰蛋白酶样活性(CT-L)进行抑制,可能展现出抗炎特性。 | |||
T37418 |
Z-LLL-AMC
|
||
Z-LLL-AMC is a fluorogenic substrate for the chymotrypsin-like activity of the 26S proteasome or 20S proteolytic core. Chymotrypsin-like activity can be quantified by fluorescent detection of free AMC (also known as 7-amino-4-methylcoumarin), which is excited at 340-360 nm and emits at 440-460 nm. Z-LLL-AMC is typically used in cell lysates after experimental treatment. | |||
T37417 |
Z-LLE-AMC
|
||
Z-LLE-AMC is a fluorogenic substrate for the caspase-like post-glutamate peptide hydrolase of the 26S proteasome or 20S proteolytic core. Caspase-like activity can be quantified by fluorescent detection of free AMC (also known as 7-amino-4-methylcoumarin), which is excited at 340-360 nm and emits at 440-460 nm. Z-LLE-AMC is typically used in cell lysates after experimental treatment. | |||
T35773 |
Gliotoxin-13C13
Gliotoxin-13C13 |
||
Gliotoxin-13C13is intended for use as an internal standard for the quantification of gliotoxin by GC- or LC-MS. Gliotoxin is an immunosuppressive mycotoxin produced by pathogenic strains ofAspergillusand other fungi with diverse biological activities.1,2,3,4,5,6,7,8It inhibits 20S proteasomal chymotrypsin activity (IC50= 10 μM), blocking the degradation of IκBα and preventing the activation of NF-κB.2,3Gliotoxin induces apoptosis in monocytes and dendritic cells and reduces phagocytosis by neutr... | |||
T36321 |
C6 Urea Ceramide
|
||
C6 urea ceramide is an inhibitor of neutral ceramidase.1 It increases total ceramide levels in wild-type mouse embryonic fibroblasts (MEFs) and in HT-29 colon cancer cells but not in MEFs lacking neutral ceramidase. It inhibits proliferation of, and induces apoptosis and autophagy in HT-29, but not non-cancerous RIE-1, cells when used at concentrations of 5 and 10 μM. C6 urea ceramide decreases total β-catenin, increases phosphorylated β-catenin, and induces colocalization of β-catenin with the ... |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T2799 |
(20S)-Protopanaxadiol
20-Epiprotopanaxadiol,20(S)-APPD,20 (S)-原人参二醇,原人参二醇 |
Apoptosis; Reactive Oxygen Species; P-gp | Apoptosis; Immunology/Inflammation; Membrane transporter/Ion channel; Metabolism; Neuroscience; NF-κB |
(20S)-Protopanaxadiol (20-Epiprotopanaxadiol) 是人参皂甙的代谢产物,是一种凋亡诱导剂,抑制Akt 活性并诱导多种肿瘤细胞凋亡。 | |||
T2810 |
(20S)-Protopanaxatriol
原人参三醇,20(S)-APPT,20 (S)-原人参三醇,g-PPT |
Apoptosis; Estrogen Receptor/ERR; Glucocorticoid Receptor; Estrogen/progestogen Receptor; Liver X Receptor | Apoptosis; Endocrinology/Hormones; Metabolism |
(20S)-Protopanaxatriol (g-PPT) 是人参皂苷的代谢物,通过糖皮质激素受体和雌激素受体起作用,同时为LXRα的抑制剂,具有广泛的抗癌活性。 | |||
TN5310 |
Pregn-5-ene-3β,17α,20S-triol
(3β,17α,20S)-Pregn-5-ene-3,17,20-triol |
||
Pregn-5-ene-3β,17α,20S-triol 是一种天然产物,可用于生命科学领域的相关研究。其产品编号为 TN5310,CAS号为 903-67-3。 | |||
TN2803 |
20S,24R-Epoxydammar-12,25-diol-3-one
|
Others | Others |
20S,24R-Epoxydammar-12,25-diol-3-one是一种天然产物,属于松科金钱松属,其产品编号为 TN2803,CAS号为 25279-15-6。20S,24R-Epoxydammar-12,25-diol-3-one可用作对照参考。 | |||
T2873 |
Ginsenoside Rg2
Chikusetsusaponin I,Panaxoside Rg2,人参皂苷Rg2,Prosapogenin C2,(20S)Ginsenoside Rg2,人参皂苷 Rg2 |
Beta Amyloid; GSK-3; NF-κB | Neuroscience; NF-κB; PI3K/Akt/mTOR signaling; Stem Cells |
Ginsenoside Rg2 (Chikusetsusaponin I) 是一种人参的主要活性成分。它能够降低Aβ1-42积聚,抑制脂多糖介导的VCAM-1和ICAM-1表达的增加。 | |||
TN5993 |
16-Desoxycucurbitacin V
3β,20S,25-Trihydroxycucurbita-5,23-dien-11-one |
||
16-Desoxycucurbitacin V 是一种天然产物,可用于生命科学领域的相关研究。其产品编号为 TN5993,CAS号为 2081098-85-1。 | |||
T83572 |
(20S)-Protopanaxadiol-3-one
|
||
(20S)-Protopanaxadiol-3-one为Melia azedarach与Betula pendula中检出的一种天然化合物。 | |||
T3402 |
20(S)-Ginsenoside Rg3
20(S)-人参皂苷 Rg3,人参皂苷 Rg3,20(S)-Ginsenoside-Rg3,Rg3,20S-Ginsenoside Rg3,Ginsenoside Rg3,S-Ginsenoside Rg3 |
EGFR; Beta Amyloid; Potassium Channel; NF-κB; COX; Sodium Channel; Endogenous Metabolite | Angiogenesis; Immunology/Inflammation; JAK/STAT signaling; Membrane transporter/Ion channel; Metabolism; Neuroscience; NF-κB; Tyrosine Kinase/Adaptors |
20(S)-Ginsenoside Rg3 (Rg3) 是红参的主要成分,通过抑制肿瘤细胞的粘附和侵袭来抑制肿瘤细胞肺转移。它抑制Na+和hKv1.4通道,IC50分别为 32.2±4.5 和 32.6±2.2 μM。它还抑制Aβ,NF-κB 活性和COX-2表达,抑制人脐静脉内皮细胞的增殖并具有抗血管生成活性。 | |||
T3028 |
Tripterin
Celastrol,Tripterine,雷公藤红素 |
Apoptosis; Mitophagy; Proteasome; Autophagy | Apoptosis; Autophagy; Proteases/Proteasome; Ubiquitination |
Tripterin (Celastrol) 属于天然产物,是一种蛋白酶体抑制剂,抑制 20S 蛋白酶体的胰凝乳蛋白酶样活性 (IC50=2.5 μM)。Tripterin 具有抗炎、抗感染和免疫调节的作用。 | |||
T16012 |
Marizomib
NPI-0052,Salinosporamide A,ML858 |
Proteasome | Proteases/Proteasome; Ubiquitination |
Marizomib (ML858) 是一种新型不可逆的脑渗透性泛蛋白酶体 (proteasome) 抑制剂,对 20S 蛋白酶体的 CT-L (β5)、CT-T-laspase 样 (C-L, β1) 和胰蛋白酶样 (T-L, β2) 具有抑制作用, IC50 分别为 3.5, 28, 430 nM。 | |||
T6830 |
Epoxomicin
BU-4061T,BU-4061T,Aids010837,环氧酶素 |
Apoptosis; Proteasome | Apoptosis; Proteases/Proteasome; Ubiquitination |
Epoxomicin (BU-4061T,Aids010837) 是一种含环氧酮的天然产物,可穿越血脑屏障,并具有很强的抗肿瘤和抗炎活性。它是一种选择性不可逆的蛋白酶体抑制剂,抑制类胰凝乳蛋白酶的活性。 | |||
T3786 |
Tomatine
lycopersicin,番茄素,番茄碱 |
Apoptosis; Proteasome | Apoptosis; Proteases/Proteasome; Ubiquitination |
Tomatine (lycopersicin) 是从番茄植物中发现的一种糖苷生物碱。它促进神经母细胞瘤细胞中核凋亡诱导因子的上调,还抑制20S 蛋白酶体活性。它以 RIP1 激酶和 caspase 非依赖性的方式引发神经毒性。 | |||
T15702 |
Lactacystin
|
Proteasome | Proteases/Proteasome; Ubiquitination |
Lactacystin is an antibiotic Streptomyces spp. the metabolite and is an effective and selective proteasome inhibitor (IC50: 4.8 μM for 20S proteasome). Lactacystin inhibits cell growth and induces neurite outgrowth and also inhibits the lysosomal enzyme cathepsin A. | |||
T10238 |
Aclacinomycin A hydrochloride
盐酸阿柔比星,Aclarubicin hydrochloride |
Proteasome | Proteases/Proteasome; Ubiquitination |
Aclacinomycin A (Aclarubicin) hydrochloride is a fluorescent molecule and the first described non-peptidic inhibitor showing discrete specificity for the CTRL (chymotrypsin-like) activity of the 20S proteasome. Aclacinomycin A hydrochloride is also a dual inhibitor of topoisomerase I and II. |