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上海阿拉丁生化科技股份有限公司>>技術(shù)文章>>阿拉丁小分子抑制劑,、激動劑、拮抗劑--NF-κB信號通路

阿拉丁小分子抑制劑,、激動劑,、拮抗劑--NF-κB信號通路

閱讀:934        發(fā)布時間:2019-12-26


NF-κB

       NF-κB是一種控制DNA轉(zhuǎn)錄的蛋白質(zhì)復(fù)合物。NF-κB幾乎存在于所有動物細(xì)胞類型中,,并參與機體的炎癥反應(yīng),、免疫應(yīng)答,能調(diào)節(jié)細(xì)胞凋亡,、應(yīng)激反應(yīng),。 NF-κB網(wǎng)絡(luò)由五個家族成員蛋白單體(p65 / RelA,RelB,,cRel,,p50和p52)組成,它們形成同源二聚體或異二聚體,,其差異結(jié)合DNA并受兩種途徑調(diào)節(jié):經(jīng)典的NF-κB必需調(diào)節(jié)劑(NEMO)依賴性途徑和非經(jīng)典的NEMO非依賴性途徑,。NF-κB通路的過度激活,與人類許多疾病相關(guān),,如哮喘,、類風(fēng)濕性關(guān)節(jié)炎、炎癥性腸病,、心臟與腦部疾病的炎癥等,。此外,改變的NF-κB調(diào)節(jié)可能涉及其他疾病,,如動脈粥樣硬化和阿爾茨海默病和各種各樣的人類癌癥,。

NF-κB通路轉(zhuǎn)導(dǎo)過程

       NF-κB經(jīng)典信號通路中,通過IκB蛋白降解釋放NF-κB二聚體,。細(xì)胞受到胞外刺激后,,信號因子與細(xì)胞膜上的受體結(jié)合,激活I(lǐng)κB激酶(IKK),。IκB磷酸化后進(jìn)一步泛素化,,進(jìn)而釋放NF-κB二聚體,。NF-κB二聚體經(jīng)翻譯后修飾(磷酸化、乙?;?、糖基化等)激活,并轉(zhuǎn)運入胞核,,在核內(nèi)單獨或聯(lián)合其他轉(zhuǎn)錄因子,,促進(jìn)基因的表達(dá)。
       NF-κB非經(jīng)典信號通路中,,則通過p100到p52的加工處理來激活信號通路,。信號轉(zhuǎn)導(dǎo)通過受體子集(LTβR、CD40和BR3等),,激活激酶NIK,,進(jìn)而激活I(lǐng)KKα復(fù)合體,IKKα復(fù)合體再磷酸化NF-κB2 p100(C端殘基),。磷酸化后的NF-κB2 p100將自身泛素化,,再經(jīng)蛋白酶加工為NF-κB2 p52。此時,,在胞漿中失活的NF-κB2 p100/RelB已激活為NF-κB p52/RelB 復(fù)合體,,轉(zhuǎn)運入胞核,誘導(dǎo)目的基因的表達(dá),。

NF-κB信號通路圖

產(chǎn)品列表

按靶點分類:     

*HDAC

項目號產(chǎn)品名稱規(guī)格CAS包裝細(xì)胞靶點IC50Ki
V125336Vorinostat≥99.0%149647-78-9100mg,500mg,1g,5g無細(xì)胞HDAC~10 nM 
E125068Entinostat (MS-275)≥98%209783-80-210mg,50mg,100mg,250mg無細(xì)胞HDAC10.51 μM 
HDAC31.7 μM 
P125167Panobinostat (LBH589)≥98%404950-80-710mg,50mg無細(xì)胞HDAC5 nM 
T129665Trichostatin A≥98%58880-19-65mg,10mg,50mg無細(xì)胞HDAC~1.8 nM 
M126151Mocetinostat (MGCD0103)≥98%726169-73-95mg,25mg,50mg無細(xì)胞HDAC10.15 μM 
S135494軟木肟酸95%38937-66-51g,5g HDAC10.25 μM 
HDAC30.3 μM 
B126780Belinostat (PXD101)≥98%414864-00-910mg,50mg,250mg無細(xì)胞HDAC27 nM 
R125265Romidepsin (FK228, Depsipeptide)≥99%128517-07-71mg,5mg無細(xì)胞HDAC136 nM 
HDAC347 nM 
M127417MC1568≥97%(HPLC)852475-26-410mg,25mg無細(xì)胞HD1-A100 nM 
T129677Tubastatin A HCl≥98%1310693-92-510mg,50mg,250mg無細(xì)胞HDAC615 nM 
G129672Givinostat (ITF2357)≥95%732302-99-75mg,10mg,50mg無細(xì)胞HD210 nM 
HD1B7.5 nM 
HD1A16 nM 
C127191CUDC-101≥98%1012054-59-910mg,25mg,50mg,100mg,250mg HDAC4.4 nM 
EGFR2.4 nM 
HER215.7 nM 
P127910Pracinostat (SB939)≥98%929016-96-65mg,10mg,50mg pan-HDAC40-140 nM 
P126351PCI-34051≥98%950762-95-510mg,50mg無細(xì)胞HDAC810 nM 
D127578Droxinostat≥96%99873-43-55mg,10mg,25mg HDACs 62.47μM 
HDACs 81.46 μM 
P126975PCI-24781 (Abexinostat)≥97%783355-60-25mg,10mg,50mg HDAC1 7 nM
R129686RGFP966≥98%1396841-57-85mg,25mg,100mg無細(xì)胞HDAC30.08μM 
A127913AR-42≥99%935881-37-12mg,5mg,10mg,50mgHDAC30 nM 
A124886Rocilinostat (ACY-1215)≥98%1316214-52-45mg,10mg,50mg無細(xì)胞HDAC65 nM 
S1610232-丙戊酸鈉≥98.0%1069-66-55g,25g,100g,500g HDAC2  
C126432CI-994≥98%112522-64-210mg,50mg,250mg HDAC 10.9 μM 
HDAC 20.9 μM 
HDAC 31.2 μM 
HDAC 8>20 μM 
C126527CUDC-907≥99%1339928-25-45mg,10mg,50mg PI3Kα19 nM 
HDAC11.7 nM 
HDAC25 nM 
HDAC1/2/3/101.8 nM 
HDAC1/2/3/102.8 nM 
S102954丁酸鈉98%156-54-725g,100g,250g,500g HDAC  
S102956丁酸鈉99%,用于生物學(xué)156-54-75g,25g,100g,500g HDAC  
C140600姜黃素≥65%458-37-75g,25g,100g p300 histone acetylatransferase~25 μM 
Histone deacetylase 
C110685姜黃素分析標(biāo)準(zhǔn)品458-37-720mg p300 histone acetylatransferase
Histone deacetylase 
M125894M344≥97%251456-60-75mg,25mg,100mg HDAC100 nM 
R127721RG2833≥98%1215493-56-35mg,10mg,25mg,50mg,100mg HDAC160 nM 
HDAC350 nM 
S125104Scriptaid≥99%287383-59-91mg,5mg HDAC  
V298968丙戊酸≥98.0%99-66-125ml,100ml,500ml    
T125086Tasquinimod≥99%254964-60-85mg,10mg,50mg    
S161350斯普利特麻一辛>98.0%(GC)5690-03-9200mg,1g HDAC4  
B1519134-聯(lián)苯磺酰氯>98.0%(GC)1623-93-45g,25g,100g HDAC  
P115736小白菊內(nèi)酯≥98%20554-84-120mg HDAC1  

 

*NF-κB

項目號產(chǎn)品名稱規(guī)格CAS包裝細(xì)胞靶點IC50
Q125550QNZ (EVP4593)≥98%545380-34-55mg,25mg,100mgJurkat TNF-κB11 nM
TNF-α7 nM
C140600姜黃素≥65%458-37-75g,25g,100g p300 histone acetylatransferase~25 μM
Histone deacetylase
C110685姜黃素分析標(biāo)準(zhǔn)品458-37-720mg p300 histone acetylatransferase~25 μM
Histone deacetylase
S115316對氨基水楊酸鈉98%6018-19-525g,50g,100g,250g,1kg NF-κB 
M134534JSH-23≥98% (HPLC)749886-87-125mg,100mgRAW 264.7細(xì)胞系NF-κB7.1 μM
C102139咖啡酸苯乙酯97%104594-70-925mg,250mg,1g,5g,25g,100g NF-κB 
S104176水楊酸鈉AR,≥99.5% (NT)54-21-7250g,500g,1kg,5kg NF-κB 
S104177水楊酸鈉CP,99.5%54-21-7100g,250g,500g,1kg NF-κB 
S104179水楊酸鈉USP級54-21-7250g,1kg NF-κB 
A106037吡咯烷二硫代甲酸銨99%5108-96-31g,5g,25g,100g,500g NF-κB 
A103738吡咯烷二硫代甲酸銨鹽95%5108-96-325g,100g NF-κB 
A101649穿心蓮內(nèi)酯98%5508-58-7100mg,500mg,1g,5g   
A101650穿心蓮內(nèi)酯分析標(biāo)準(zhǔn)品5508-58-720mg   
E140884吳茱萸堿98%518-17-21g,5g,25g IkB kinase 
E101966吳茱萸堿分析標(biāo)準(zhǔn)品,≥99%518-17-220mg IkB kinase 
I1052203-吲哚甲醇96%700-06-11g,5g,25g,100g,500g NF-κB 
IκBα 
M111377厚樸酚分析標(biāo)準(zhǔn)品,>98%528-43-820mg TNFα 
M111378厚樸酚≥98%(HPLC)528-43-850mg,250mg,1g,5g TNFα 
P115736小白菊內(nèi)酯≥98%20554-84-120mg HDAC1 
T107399雷公藤甲素分析標(biāo)準(zhǔn)品,≥98%38748-32-210mg,20mg NF-κB 
T107400雷公藤甲素98%38748-32-250mg NF-κB 
D104017馬來酸二乙酯96%141-05-925ml,100ml,500ml,2.5L NF-κB 

 

*IκB/IKK

項目號產(chǎn)品名稱規(guī)格CAS包裝細(xì)胞靶點IC50
B126947BX-795≥97%702675-74-910mg,50mg,100mg無細(xì)胞PDK16 nM
B129693BAY 11-7082≥98%19542-67-750mg,250mg,1g腫瘤細(xì)胞IκBα10 μM
I129698IKK-16 (IKK Inhibitor VII)≥99%873225-46-810mg,50mg無細(xì)胞IKK-240 nM
IKK complex70 nM
IKK-1200 nM
T126861TPCA-1≥98%507475-17-45mg,25mg,100mg無細(xì)胞IKK-217.9 nM
I129696IMD 0354≥99%978-62-15mg,10mg,50mg IKKβ 
W124219蟛蜞菊內(nèi)酯≥98%(HPLC)524-12-91mg,5mg,25mg IKK 
B129704Bardoxolone Methyl≥98%218600-53-425mg,100mg IKK 
S126740SC-514≥98%354812-17-210mg,50mg IKK-23-12 μM
A1299825-氨基水楊酸≥99%89-57-65g,25g,100g,500g   
B168290Bay 11-708598% (HPLC)196309-76-910mg IκBα10 μM
M126461MRT67307≥98%1190378-57-410mg,50mg IKK?160 nM
TBK119 nM
R109804迷迭香酸分析標(biāo)準(zhǔn)品,≥97%20283-92-510mg,20mg IKK-β 
R109805迷迭香酸97%20283-92-51g,5g IKK-β 
W167241WS398% (HPLC)1421227-52-25mg,25mg IκB 

 

*

項目號產(chǎn)品名稱規(guī)格CAS包裝靶點IC50
M129713ML130 (Nodinitib-1)≥99%799264-47-45mg,10mg,25mg,50mg0.56 μM


 

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