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阿拉丁小分子抑制劑、激動(dòng)劑、拮抗劑--NF-κB信號(hào)通路
閱讀：916 發(fā)布時(shí)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(dòng)物細(xì)胞類型中，并參與機(jī)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(gè)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(dòng)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(hào)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(hào)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、乙酰化、糖基化等）激活，并轉(zhuǎn)運(yùn)入胞核，在核內(nèi)單獨(dú)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(hào)通路中，則通過p100到p52的加工處理來激活信號(hào)通路。信號(hào)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(shí)，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(yùn)入胞核，誘導(dǎo)目的基因的表達(dá)。
NF-κB信號(hào)通路圖
產(chǎn)品列表
按靶點(diǎn)分類：
*HDAC
| 項(xiàng)目號(hào) | 產(chǎn)品名稱 | 規(guī)格 | CAS | 包裝 | 細(xì)胞 | 靶點(diǎn) | IC50 | Ki |
|---|---|---|---|---|---|---|---|---|
| V125336 | Vorinostat | ≥99.0% | 149647-78-9 | 100mg,500mg,1g,5g | 無細(xì)胞 | HDAC | ~10 nM | |
| E125068 | Entinostat (MS-275) | ≥98% | 209783-80-2 | 10mg,50mg,100mg,250mg | 無細(xì)胞 | HDAC1 | 0.51 μM | |
| HDAC3 | 1.7 μM | |||||||
| P125167 | Panobinostat (LBH589) | ≥98% | 404950-80-7 | 10mg,50mg | 無細(xì)胞 | HDAC | 5 nM | |
| T129665 | Trichostatin A | ≥98% | 58880-19-6 | 5mg,10mg,50mg | 無細(xì)胞 | HDAC | ~1.8 nM | |
| M126151 | Mocetinostat (MGCD0103) | ≥98% | 726169-73-9 | 5mg,25mg,50mg | 無細(xì)胞 | HDAC1 | 0.15 μM | |
| S135494 | 軟木肟酸 | 95% | 38937-66-5 | 1g,5g | HDAC1 | 0.25 μM | ||
| HDAC3 | 0.3 μM | |||||||
| B126780 | Belinostat (PXD101) | ≥98% | 414864-00-9 | 10mg,50mg,250mg | 無細(xì)胞 | HDAC | 27 nM | |
| R125265 | Romidepsin (FK228, Depsipeptide) | ≥99% | 128517-07-7 | 1mg,5mg | 無細(xì)胞 | HDAC1 | 36 nM | |
| HDAC3 | 47 nM | |||||||
| M127417 | MC1568 | ≥97%(HPLC) | 852475-26-4 | 10mg,25mg | 無細(xì)胞 | HD1-A | 100 nM | |
| T129677 | Tubastatin A HCl | ≥98% | 1310693-92-5 | 10mg,50mg,250mg | 無細(xì)胞 | HDAC6 | 15 nM | |
| G129672 | Givinostat (ITF2357) | ≥95% | 732302-99-7 | 5mg,10mg,50mg | 無細(xì)胞 | HD2 | 10 nM | |
| HD1B | 7.5 nM | |||||||
| HD1A | 16 nM | |||||||
| C127191 | CUDC-101 | ≥98% | 1012054-59-9 | 10mg,25mg,50mg,100mg,250mg | HDAC | 4.4 nM | ||
| EGFR | 2.4 nM | |||||||
| HER2 | 15.7 nM | |||||||
| P127910 | Pracinostat (SB939) | ≥98% | 929016-96-6 | 5mg,10mg,50mg | pan-HDAC | 40-140 nM | ||
| P126351 | PCI-34051 | ≥98% | 950762-95-5 | 10mg,50mg | 無細(xì)胞 | HDAC8 | 10 nM | |
| D127578 | Droxinostat | ≥96% | 99873-43-5 | 5mg,10mg,25mg | HDACs 6 | 2.47μM | ||
| HDACs 8 | 1.46 μM | |||||||
| P126975 | PCI-24781 (Abexinostat) | ≥97% | 783355-60-2 | 5mg,10mg,50mg | HDAC1 | 7 nM | ||
| R129686 | RGFP966 | ≥98% | 1396841-57-8 | 5mg,25mg,100mg | 無細(xì)胞 | HDAC3 | 0.08μM | |
| A127913 | AR-42 | ≥99% | 935881-37-1 | 2mg,5mg,10mg,50mg | HDAC | 30 nM | ||
| A124886 | Rocilinostat (ACY-1215) | ≥98% | 1316214-52-4 | 5mg,10mg,50mg | 無細(xì)胞 | HDAC6 | 5 nM | |
| S161023 | 2-丙戊酸鈉 | ≥98.0% | 1069-66-5 | 5g,25g,100g,500g | HDAC2 | |||
| C126432 | CI-994 | ≥98% | 112522-64-2 | 10mg,50mg,250mg | HDAC 1 | 0.9 μM | ||
| HDAC 2 | 0.9 μM | |||||||
| HDAC 3 | 1.2 μM | |||||||
| HDAC 8 | >20 μM | |||||||
| C126527 | CUDC-907 | ≥99% | 1339928-25-4 | 5mg,10mg,50mg | PI3Kα | 19 nM | ||
| HDAC1 | 1.7 nM | |||||||
| HDAC2 | 5 nM | |||||||
| HDAC1/2/3/10 | 1.8 nM | |||||||
| HDAC1/2/3/10 | 2.8 nM | |||||||
| S102954 | 丁酸鈉 | 98% | 156-54-7 | 25g,100g,250g,500g | HDAC | |||
| S102956 | 丁酸鈉 | 99%,用于生物學(xué) | 156-54-7 | 5g,25g,100g,500g | HDAC | |||
| C140600 | 姜黃素 | ≥65% | 458-37-7 | 5g,25g,100g | p300 histone acetylatransferase | ~25 μM | ||
| Histone deacetylase | ||||||||
| C110685 | 姜黃素 | 分析標(biāo)準(zhǔn)品 | 458-37-7 | 20mg | p300 histone acetylatransferase | |||
| Histone deacetylase | ||||||||
| M125894 | M344 | ≥97% | 251456-60-7 | 5mg,25mg,100mg | HDAC | 100 nM | ||
| R127721 | RG2833 | ≥98% | 1215493-56-3 | 5mg,10mg,25mg,50mg,100mg | HDAC1 | 60 nM | ||
| HDAC3 | 50 nM | |||||||
| S125104 | Scriptaid | ≥99% | 287383-59-9 | 1mg,5mg | HDAC | |||
| V298968 | 丙戊酸 | ≥98.0% | 99-66-1 | 25ml,100ml,500ml | ||||
| T125086 | Tasquinimod | ≥99% | 254964-60-8 | 5mg,10mg,50mg | ||||
| S161350 | 斯普利特麻一辛 | >98.0%(GC) | 5690-03-9 | 200mg,1g | HDAC4 | |||
| B151913 | 4-聯(lián)苯磺酰氯 | >98.0%(GC) | 1623-93-4 | 5g,25g,100g | HDAC | |||
| P115736 | 小白菊內(nèi)酯 | ≥98% | 20554-84-1 | 20mg | HDAC1 | |||
*NF-κB
| 項(xiàng)目號(hào) | 產(chǎn)品名稱 | 規(guī)格 | CAS | 包裝 | 細(xì)胞 | 靶點(diǎn) | IC50 |
|---|---|---|---|---|---|---|---|
| Q125550 | QNZ (EVP4593) | ≥98% | 545380-34-5 | 5mg,25mg,100mg | Jurkat T | NF-κB | 11 nM |
| TNF-α | 7 nM | ||||||
| C140600 | 姜黃素 | ≥65% | 458-37-7 | 5g,25g,100g | p300 histone acetylatransferase | ~25 μM | |
| Histone deacetylase | |||||||
| C110685 | 姜黃素 | 分析標(biāo)準(zhǔn)品 | 458-37-7 | 20mg | p300 histone acetylatransferase | ~25 μM | |
| Histone deacetylase | |||||||
| S115316 | 對氨基水楊酸鈉 | 98% | 6018-19-5 | 25g,50g,100g,250g,1kg | NF-κB | ||
| M134534 | JSH-23 | ≥98% (HPLC) | 749886-87-1 | 25mg,100mg | RAW 264.7細(xì)胞系 | NF-κB | 7.1 μM |
| C102139 | 咖啡酸苯乙酯 | 97% | 104594-70-9 | 25mg,250mg,1g,5g,25g,100g | NF-κB | ||
| S104176 | 水楊酸鈉 | AR,≥99.5% (NT) | 54-21-7 | 250g,500g,1kg,5kg | NF-κB | ||
| S104177 | 水楊酸鈉 | CP,99.5% | 54-21-7 | 100g,250g,500g,1kg | NF-κB | ||
| S104179 | 水楊酸鈉 | USP級(jí) | 54-21-7 | 250g,1kg | NF-κB | ||
| A106037 | 吡咯烷二硫代甲酸銨 | 99% | 5108-96-3 | 1g,5g,25g,100g,500g | NF-κB | ||
| A103738 | 吡咯烷二硫代甲酸銨鹽 | 95% | 5108-96-3 | 25g,100g | NF-κB | ||
| A101649 | 穿心蓮內(nèi)酯 | 98% | 5508-58-7 | 100mg,500mg,1g,5g | |||
| A101650 | 穿心蓮內(nèi)酯 | 分析標(biāo)準(zhǔn)品 | 5508-58-7 | 20mg | |||
| E140884 | 吳茱萸堿 | 98% | 518-17-2 | 1g,5g,25g | IkB kinase | ||
| E101966 | 吳茱萸堿 | 分析標(biāo)準(zhǔn)品,≥99% | 518-17-2 | 20mg | IkB kinase | ||
| I105220 | 3-吲哚甲醇 | 96% | 700-06-1 | 1g,5g,25g,100g,500g | NF-κB | ||
| IκBα | |||||||
| M111377 | 厚樸酚 | 分析標(biāo)準(zhǔn)品,>98% | 528-43-8 | 20mg | TNFα | ||
| M111378 | 厚樸酚 | ≥98%(HPLC) | 528-43-8 | 50mg,250mg,1g,5g | TNFα | ||
| P115736 | 小白菊內(nèi)酯 | ≥98% | 20554-84-1 | 20mg | HDAC1 | ||
| T107399 | 雷公藤甲素 | 分析標(biāo)準(zhǔn)品,≥98% | 38748-32-2 | 10mg,20mg | NF-κB | ||
| T107400 | 雷公藤甲素 | 98% | 38748-32-2 | 50mg | NF-κB | ||
| D104017 | 馬來酸二乙酯 | 96% | 141-05-9 | 25ml,100ml,500ml,2.5L | NF-κB | ||
*IκB/IKK
| 項(xiàng)目號(hào) | 產(chǎn)品名稱 | 規(guī)格 | CAS | 包裝 | 細(xì)胞 | 靶點(diǎn) | IC50 |
|---|---|---|---|---|---|---|---|
| B126947 | BX-795 | ≥97% | 702675-74-9 | 10mg,50mg,100mg | 無細(xì)胞 | PDK1 | 6 nM |
| B129693 | BAY 11-7082 | ≥98% | 19542-67-7 | 50mg,250mg,1g | 腫瘤細(xì)胞 | IκBα | 10 μM |
| I129698 | IKK-16 (IKK Inhibitor VII) | ≥99% | 873225-46-8 | 10mg,50mg | 無細(xì)胞 | IKK-2 | 40 nM |
| IKK complex | 70 nM | ||||||
| IKK-1 | 200 nM | ||||||
| T126861 | TPCA-1 | ≥98% | 507475-17-4 | 5mg,25mg,100mg | 無細(xì)胞 | IKK-2 | 17.9 nM |
| I129696 | IMD 0354 | ≥99% | 978-62-1 | 5mg,10mg,50mg | IKKβ | ||
| W124219 | 蟛蜞菊內(nèi)酯 | ≥98%(HPLC) | 524-12-9 | 1mg,5mg,25mg | IKK | ||
| B129704 | Bardoxolone Methyl | ≥98% | 218600-53-4 | 25mg,100mg | IKK | ||
| S126740 | SC-514 | ≥98% | 354812-17-2 | 10mg,50mg | IKK-2 | 3-12 μM | |
| A129982 | 5-氨基水楊酸 | ≥99% | 89-57-6 | 5g,25g,100g,500g | |||
| B168290 | Bay 11-7085 | 98% (HPLC) | 196309-76-9 | 10mg | IκBα | 10 μM | |
| M126461 | MRT67307 | ≥98% | 1190378-57-4 | 10mg,50mg | IKK? | 160 nM | |
| TBK1 | 19 nM | ||||||
| R109804 | 迷迭香酸 | 分析標(biāo)準(zhǔn)品,≥97% | 20283-92-5 | 10mg,20mg | IKK-β | ||
| R109805 | 迷迭香酸 | 97% | 20283-92-5 | 1g,5g | IKK-β | ||
| W167241 | WS3 | 98% (HPLC) | 1421227-52-2 | 5mg,25mg | IκB |
*
| 項(xiàng)目號(hào) | 產(chǎn)品名稱 | 規(guī)格 | CAS | 包裝 | 靶點(diǎn) | IC50 |
|---|---|---|---|---|---|---|
| M129713 | ML130 (Nodinitib-1) | ≥99% | 799264-47-4 | 5mg,10mg,25mg,50mg | 0.56 μM |