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

ONX-0914 (PR-957) Chemical Structure

CAS: 960374-59-8

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 2694.51 现货
5mg RMB 2367.48 现货
25mg RMB 7100.88 现货
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客户使用Selleck的ONX-0914 (PR-957)发表文献17

客户使用该产品的2个实验数据

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

相关信号通路图

Proteasome抑制剂选择性比较

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
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
LMP7 [1]
(Cell-free assay)
~10 nM
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
批次:

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

Water : Insoluble

摩尔浓度计算器

体内溶解度
批次:

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

摩尔浓度计算器

质量 浓度 体积 分子量

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

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,: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: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: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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