ONX-0914 (PR-957)

目錄號：S7172 Purity: 99.74%

ONX-0914 (PR-957)是一種有效的，選擇性immunoproteasome抑制劑，無細(xì)胞試驗中對組成型蛋白酶體具有最低的交叉反應(yīng)性。

ONX-0914 (PR-957) Chemical Structure

CAS: 960374-59-8

規(guī)格	價格	庫存
10mM (1mL in DMSO)	2694.51	現(xiàn)貨
5mg	2367.48	現(xiàn)貨
25mg	7100.88	現(xiàn)貨
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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(diǎn)	20S proteasome	點(diǎn)擊展開
相關(guān)產(chǎn)品	MG132 Epoxomicin (BU-4061T) Celastrol Oprozomib Delanzomib VR23 Marizomib (Salinosporamide A) PI-1840	點(diǎn)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(diǎn)擊展開

細(xì)胞實(shí)驗數(shù)據(jù)示例

細(xì)胞系	實(shí)驗類型	給藥濃度	孵育時間	活性描述	文獻(xiàn)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
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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(xì)胞試驗中對組成型蛋白酶體具有最低的交叉反應(yīng)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(diǎn)

LMP7 ^[1]
(Cell-free assay)

~10 nM

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(diǎn)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(yīng)性。ONX-0914選擇性抑制LMP7，通過該活化的單核細(xì)胞和T細(xì)胞產(chǎn)生的干擾素-γ和IL-2，而導(dǎo)致白細(xì)胞介素-23（IL-23）的產(chǎn)生受抑制。LMP7受抑制導(dǎo)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(fēng)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(xì)胞浸潤，細(xì)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]

參考文獻(xiàn)
[1] Muchamuel T, et al. Nat Med, 2009, 15(7), 781-787.

參考文獻(xiàn)

[1] Muchamuel T, et al. Nat Med, 2009, 15(7), 781-787.

化學(xué)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)	3年-20°C粉狀	儲備液保存和期限建議分裝儲備液，避免反復(fù)凍融！	1年-80°C溶于溶劑
儲存條件(自收到貨起)	3年-20°C粉狀	儲備液保存和期限建議分裝儲備液，避免反復(fù)凍融！	1個月-20°C溶于溶劑

體外溶解度
批次：

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
批次：

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(shí)驗計算

摩爾濃度計算器

質(zhì)量	濃度	體積	分子量
=	×	×

稀釋計算器分子量計算器

動物體內(nèi)配方計算器（澄清溶液）

第一步：請輸入基本實(shí)驗信息（考慮到實(shí)驗過程中的損耗，建議多配一只動物的藥量）

給藥劑量 mg/kg 動物平均體重 g 每只動物給藥體積 μL 動物數(shù)量只

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(jìn)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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