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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。
ONX-0914 (PR-957) Chemical Structure
CAS: 960374-59-8
产品质控
批次：
S717202
DMSO]100 mg/mL]false]Ethanol]100 mg/mL]false]Water]Insoluble]false
纯度：
99.74%
99.74
ONX-0914 (PR-957)相关产品
| 相关靶点 | 20S proteasome | 点击展开 |
|---|---|---|
| 相关产品 | MG132 Epoxomicin (BU-4061T) Celastrol Oprozomib Delanzomib VR23 Marizomib (Salinosporamide A) PI-1840 | 点击展开 |
| 相关化合物库 | FDA药物库 天然产物库 已知活性药物库-I 蛋白酶抑制剂库 泛素化化合物库 | 点击展开 |
相关信号通路图
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息(PMID) |
|---|---|---|---|---|---|
| EBC1 | Antitumor assay | 15 mg/kg | 5 days | Antitumor activity against human EBC1 cells xenografted in CD-1 nude mouse assessed as tumor regression at 15 mg/kg, po qd administered for 5 days on and 2 days off up to 32 days | 25006746 |
| PBMC | Function assay | 100 nM | 3 to 72 hrs | Inhibition of 20S proteasome beta 5i in human PBMC cells assessed as induction of PSMB5 expression at 100 nM after 3 to 72 hrs by RT-PCR analysis | 31283222 |
| PBMC | Function assay | 100 nM | 3 to 72 hrs | Inhibition of 20S proteasome beta 5i in human PBMC cells assessed as induction of PSMB6 expression at 100 nM after 3 to 72 hrs by RT-PCR analysis | 31283222 |
| PBMC | Function assay | 100 nM | 3 to 72 hrs | Inhibition of 20S proteasome beta 5i in human PBMC cells assessed as induction of PSMB7 expression at 100 nM after 3 to 72 hrs by RT-PCR method | 31283222 |
| NCI-H727 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human NCI-H727 cells assessed as reduction in cell viability after 48 hrs by Hoechst 33342 staining based HCS assay, EC50=0.3μM | 29339252 | |
| PC3 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human PC3 cells assessed as reduction in cell viability after 48 hrs by Hoechst 33342 staining based HCS assay, EC50=0.33μM | 29339252 | |
| HuH7 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human HuH7 cells assessed as reduction in cell viability after 48 hrs by Hoechst 33342 staining based HCS assay, EC50=0.39μM | 29339252 | |
| Caco2 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human Caco2 cells assessed as reduction in cell viability after 48 hrs by Hoechst 33342 staining based HCS assay, EC50=1.3μM | 29339252 | |
| Raji | Function assay | Inhibition of proteasome subunit beta-2i in human Raji cells using BODIPY- epoxomicin by fluorescent densitometry, IC50=0.59μM | 25006746 | ||
| Raji | Function assay | Inhibition of proteasome subunit beta-1i in human Raji cells using BODIPY- epoxomicin by fluorescent densitometry, IC50=0.46μM | 25006746 | ||
| RPMI8226 | Function assay | Inhibition of proteasome subunit beta-1i in human RPMI8226 cells using BODIPY-NC001 by fluorescent densitometry, IC50=0.34μM | 25006746 | ||
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 25006746 | ||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 25006746 | ||
| Raji | Function assay | Inhibition of proteasome subunit beta-5i in human Raji cells using BODIPY-NC005 by fluorescent densitometry, IC50=0.0057μM | 25006746 | ||
| RPMI8226 | Function assay | Inhibition of proteasome subunit beta-2i in human RPMI8226 cells using BODIPY-epoxomicin by fluorescent densitometry, IC50=0.59μM | 25006746 | ||
| Raji | Function assay | Inhibition of 20s proteasome subunit beta-2c in human Raji cells using BODIPY- epoxomicin by fluorescent densitometry, IC50=1.1μM | 25006746 | ||
| RPMI8226 | Function assay | Inhibition of 20s proteasome subunit beta-2c in human RPMI8226 cells using BODIPY-epoxomicin by fluorescent densitometry, IC50=1.1μM | 25006746 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 29339252 | ||
| RD | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 29339252 | ||
| MG 63 (6-TG R) | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 29339252 | ||
| DAOY | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 30380863 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 30380863 | ||
| Rh41 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 30380863 | ||
| A20 | Function assay | Inhibition of LMP2 in mouse A20 cells by ELISA, IC50=0.328μM | 30380863 | ||
| A20 | Function assay | Inhibition of 20S proteosome beta 5 in mouse A20 cells by ELISA, IC50=0.401μM | 30380863 | ||
| MOLT4 | Function assay | Inhibition of 20S proteosome beta 5 in human MOLT4 cells by ELISA, IC50=0.422μM | 30380863 | ||
| A20 | Function assay | Inhibition of MECL1 in mouse A20 cells by ELISA, IC50=0.699μM | 30380863 | ||
| MOLT4 | Function assay | Inhibition of MECL1 in human MOLT4 cells by ELISA, IC50=0.902μM | 30380863 | ||
| A20 | Function assay | Inhibition of 20S proteosome beta 2 in mouse A20 cells by ELISA, IC50=0.913μM | 30380863 | ||
| MOLT4 | Function assay | Inhibition of 20S proteosome beta 2 in human MOLT4 cells by ELISA, IC50=0.927μM | 30380863 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | 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。 | ||
|---|---|---|---|
| 特性 | ONX-0914 是第一个高度选择性，小分子，免疫蛋白酶抑制剂。 | ||
| 靶点 |
|
| 体外研究(In Vitro) | ||||
| 体外研究活性 | ONX-0914作用于LMP7比作用于下一个最敏感的位点β5或LMP2选择性高20到40倍。ONX-0914在体外和体内抑制LMP7特异性的，MHC-I限制性的抗原，对组成型蛋白酶体具有最低的交叉反应性。ONX-0914选择性抑制LMP7，通过该活化的单核细胞和T细胞产生的干扰素-γ和IL-2，而导致白细胞介素-23（IL-23）的产生受抑制。LMP7受抑制导致90% IL-23的产生受抑制，及50%肿瘤坏死因子-α（TNF-α）和IL-6受抑制。[1] | |||
|---|---|---|---|---|
| 体内研究(In Vivo) | ||
| 体内研究活性 | ONX-0914处理风湿性关节炎和狼疮小鼠模型，逆转疾病的征兆，并降低细胞浸润，细胞因子产生，及自身抗体水平在良好的耐受剂量。ONX-0914处理小鼠的最大耐受剂量（MTD）为30 mg/kg体重。ONX-0914为LMP7选择性浓度时，抑制60％IFN-g释放，在更高浓度时，抑制90%。ONX-0914还抑制约50％IL-2产生。[1] | |
|---|---|---|
|
化学信息&溶解度
| 分子量 | 580.67 | 分子式 | C31H40N4O7 |
| CAS号 | 960374-59-8 | SDF | Download ONX-0914 (PR-957) SDF |
| Smiles | CC(C(=O)NC(CC1=CC=C(C=C1)OC)C(=O)NC(CC2=CC=CC=C2)C(=O)C3(CO3)C)NC(=O)CN4CCOCC4 | ||
| 储存条件(自收到货起) | |||
|
体外溶解度 |
DMSO : 100 mg/mL ( (172.21 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Ethanol : 100 mg/mL (172.21 mM) Water : Insoluble |
摩尔浓度计算器 |
|
体内溶解配方 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | |||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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