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ONX-0914 (PR-957)
ONX-0914 (PR-957)是一種有效的，選擇性immunoproteasome抑制劑，無細胞試驗中對組成型蛋白酶體具有最低的交叉反應性。
ONX-0914 (PR-957) Chemical Structure
CAS: 960374-59-8
產(chǎn)品質(zhì)控
批次：
S717202
DMSO]100 mg/mL]false]Ethanol]100 mg/mL]false]Water]Insoluble]false
純度：
99.74%
99.74
ONX-0914 (PR-957)相關(guān)產(chǎn)品
| 相關(guān)靶點 | 20S proteasome | 點擊展開 |
|---|---|---|
| 相關(guān)產(chǎn)品 | MG132 Epoxomicin (BU-4061T) Celastrol Oprozomib Delanzomib VR23 Marizomib (Salinosporamide A) PI-1840 | 點擊展開 |
| 相關(guān)化合物庫 | FDA藥物庫 天然產(chǎn)物庫 已知活性藥物庫-I 蛋白酶抑制劑庫 泛素化化合物庫 | 點擊展開 |
相關(guān)信號通路圖
細胞實驗數(shù)據(jù)示例
| 細胞系 | 實驗類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻信息 |
|---|---|---|---|---|---|
| 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 | ||
| 點擊查看更多細胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | ONX-0914 (PR-957)是一種有效的，選擇性immunoproteasome抑制劑，無細胞試驗中對組成型蛋白酶體具有最低的交叉反應性。 | ||
|---|---|---|---|
| 特性 | ONX-0914 是第一個高度選擇性，小分子，免疫蛋白酶抑制劑。 | ||
| 靶點 |
|
| 體外研究(In Vitro) | ||||
| 體外研究活性 | ONX-0914作用于LMP7比作用于下一個最敏感的位點β5或LMP2選擇性高20到40倍。ONX-0914在體外和體內(nèi)抑制LMP7特異性的，MHC-I限制性的抗原，對組成型蛋白酶體具有最低的交叉反應性。ONX-0914選擇性抑制LMP7，通過該活化的單核細胞和T細胞產(chǎn)生的干擾素-γ和IL-2，而導致白細胞介素-23（IL-23）的產(chǎn)生受抑制。LMP7受抑制導致90% IL-23的產(chǎn)生受抑制，及50%腫瘤壞死因子-α（TNF-α）和IL-6受抑制。[1] | |||
|---|---|---|---|---|
| 體內(nèi)研究(In Vivo) | ||
| 體內(nèi)研究活性 | ONX-0914處理風濕性關(guān)節(jié)炎和狼瘡小鼠模型，逆轉(zhuǎn)疾病的征兆，并降低細胞浸潤，細胞因子產(chǎn)生，及自身抗體水平在良好的耐受劑量。ONX-0914處理小鼠的最大耐受劑量（MTD）為30 mg/kg體重。ONX-0914為LMP7選擇性濃度時，抑制60％IFN-g釋放，在更高濃度時，抑制90%。ONX-0914還抑制約50％IL-2產(chǎn)生。[1] | |
|---|---|---|
化學信息&溶解度
| 分子量 | 580.67 | 分子式 | C31H40N4O7 |
| CAS號 | 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 | ||
| 儲存條件(自收到貨起) | |||
|
體外溶解度 |
DMSO : 100 mg/mL ( (172.21 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO) Ethanol : 100 mg/mL (172.21 mM) Water : Insoluble |
摩爾濃度計算器 |
|
體內(nèi)溶解度 現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑 |
動物體內(nèi)配方計算器 | ||||
實驗計算
動物體內(nèi)配方計算器（澄清溶液）
第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）
mg/kg
g
μL
只
第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計算結(jié)果：
工作液濃度： mg/ml；
DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；
體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。
體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。
注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。
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