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首页 >  新闻动态 >  阿拉丁小分子抑制剂、激动剂、拮抗剂--NF-κB信号通路

阿拉丁小分子抑制剂、激动剂、拮抗剂--NF-κB信号通路

发布时间:2019-12-26

阿拉丁小分子抑制剂、激动剂、拮抗剂--NF-κB信号通路

NF-κB

       NF-κB是一种控制DNA转录的蛋白质复合物。NF-κB几乎存在于所有动物细胞类型中,并参与机体的炎症反应、免疫应答,能调节细胞凋亡、应激反应。 NF-κB网络由五个家族成员蛋白单体(p65 / RelA,RelB,cRel,p50和p52)组成,它们形成同源二聚体或异二聚体,其差异结合DNA并受两种途径调节:经典的NF-κB必需调节剂(NEMO)依赖性途径和非经典的NEMO非依赖性途径。NF-κB通路的过度激活,与人类许多疾病相关,如哮喘、类风湿性关节炎、炎症性肠病、心脏与脑部疾病的炎症等。此外,改变的NF-κB调节可能涉及其他疾病,如动脉粥样硬化和阿尔茨海默病和各种各样的人类癌症。

NF-κB通路转导过程

       NF-κB经典信号通路中,通过IκB蛋白降解释放NF-κB二聚体。细胞受到胞外刺激后,信号因子与细胞膜上的受体结合,激活IκB激酶(IKK)。IκB磷酸化后进一步泛素化,进而释放NF-κB二聚体。NF-κB二聚体经翻译后修饰(磷酸化、乙酰化、糖基化等)激活,并转运入胞核,在核内单独或联合其他转录因子,促进基因的表达。
       NF-κB非经典信号通路中,则通过p100到p52的加工处理来激活信号通路。信号转导通过受体子集(LTβR、CD40和BR3等),激活激酶NIK,进而激活IKKα复合体,IKKα复合体再磷酸化NF-κB2 p100(C端残基)。磷酸化后的NF-κB2 p100将自身泛素化,再经蛋白酶加工为NF-κB2 p52。此时,在胞浆中失活的NF-κB2 p100/RelB已激活为NF-κB p52/RelB 复合体,转运入胞核,诱导目的基因的表达。

NF-κB信号通路图

产品列表

按靶点分类:     

*HDAC

项目号产品名称规格CAS包装细胞靶点IC50Ki
V125336Vorinostat≥99.0%149647-78-9100mg,500mg,1g,5g无细胞HDAC~10 nM
E125068Entinostat (MS-275)≥98%209783-80-2 10mg,50mg,100mg,250mg无细胞HDAC10.51 μM
HDAC31.7 μM
P125167Panobinostat (LBH589)≥98%404950-80-710mg,50mg无细胞HDAC5 nM
T129665Trichostatin A≥98%58880-19-65mg,10mg,50mg无细胞HDAC~1.8 nM
M126151Mocetinostat (MGCD0103)≥98%726169-73-95mg,25mg,50mg无细胞HDAC10.15 μM
S135494软木肟酸95%38937-66-51g,5g
HDAC10.25 μM
HDAC30.3 μM
B126780Belinostat (PXD101)≥98%414864-00-910mg,50mg,250mg无细胞HDAC27 nM
R125265Romidepsin (FK228, Depsipeptide)≥99%128517-07-71mg,5mg无细胞HDAC136 nM
HDAC347 nM
M127417MC1568≥97%(HPLC)852475-26-410mg,25mg无细胞HD1-A100 nM
T129677Tubastatin A HCl≥98%1310693-92-510mg,50mg,250mg无细胞HDAC615 nM
G129672Givinostat (ITF2357)≥95%732302-99-75mg,10mg,50mg无细胞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无细胞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无细胞HDAC30.08μM
A127913AR-42≥99%935881-37-12mg,5mg,10mg,50mgHDAC30 nM
A124886Rocilinostat (ACY-1215)≥98%1316214-52-45mg,10mg,50mg无细胞HDAC65 nM
S1610232-丙戊酸钠≥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丁酸钠98%156-54-725g,100g,250g,500g
HDAC

S102956丁酸钠99%,用于生物学156-54-75g,25g,100g,500g
HDAC

C140600姜黄素≥65%458-37-75g,25g,100g
p300 histone acetylatransferase~25 μM
Histone deacetylase
C110685姜黄素分析标准品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)5690-03-9 200mg,1g
HDAC4

B1519134-联苯磺酰氯>98.0%(GC)1623-93-45g,25g,100g
HDAC

P115736小白菊内酯≥98%20554-84-120mg
HDAC1

 

*NF-κB

项目号产品名称规格CAS包装细胞靶点IC50
Q125550QNZ (EVP4593)≥98%545380-34-55mg,25mg,100mgJurkat TNF-κB11 nM
TNF-α7 nM
C140600姜黄素≥65%458-37-75g,25g,100g
p300 histone acetylatransferase~25 μM
Histone deacetylase
C110685姜黄素分析标准品458-37-720mg
p300 histone acetylatransferase~25 μM
Histone deacetylase
S115316对氨基水杨酸钠98%6018-19-525g,50g,100g,250g,1kg
NF-κB
M134534JSH-23≥98% (HPLC)749886-87-125mg,100mgRAW 264.7细胞系NF-κB7.1 μM
C102139咖啡酸苯乙酯97%104594-70-925mg,250mg,1g,5g,25g,100g
NF-κB
S104176水杨酸钠AR,≥99.5% (NT)54-21-7250g,500g,1kg,5kg
NF-κB
S104177水杨酸钠CP,99.5%54-21-7100g,250g,500g,1kg
NF-κB
S104179水杨酸钠USP级54-21-7250g,1kg
NF-κB
A106037吡咯烷二硫代甲酸铵99%5108-96-31g,5g,25g,100g,500g
NF-κB
A103738吡咯烷二硫代甲酸铵盐95%5108-96-325g,100g
NF-κB
A101649穿心莲内酯98%5508-58-7100mg,500mg,1g,5g


A101650穿心莲内酯分析标准品5508-58-720mg


E140884吴茱萸碱98%518-17-21g,5g,25g
IkB kinase
E101966吴茱萸碱分析标准品,≥99%518-17-220mg
IkB kinase
I1052203-吲哚甲醇96%700-06-11g,5g,25g,100g,500g
NF-κB
IκBα
M111377厚朴酚分析标准品,>98%528-43-820mg
TNFα
M111378厚朴酚≥98%(HPLC)528-43-850mg,250mg,1g,5g
TNFα
P115736小白菊内酯≥98%20554-84-120mg
HDAC1
T107399雷公藤甲素分析标准品,≥98%38748-32-210mg,20mg
NF-κB
T107400雷公藤甲素98%38748-32-250mg
NF-κB
D104017马来酸二乙酯96%141-05-925ml,100ml,500ml,2.5L
NF-κB

 

*IκB/IKK

项目号产品名称规格CAS包装细胞靶点IC50
B126947BX-795≥97%702675-74-910mg,50mg,100mg无细胞PDK16 nM
B129693BAY 11-7082≥98%19542-67-750mg,250mg,1g肿瘤细胞IκBα10 μM
I129698IKK-16 (IKK Inhibitor VII)≥99%873225-46-810mg,50mg无细胞IKK-240 nM
IKK complex70 nM
IKK-1200 nM
T126861TPCA-1≥98%507475-17-45mg,25mg,100mg无细胞IKK-217.9 nM
I129696IMD 0354≥99%978-62-15mg,10mg,50mg
IKKβ
W124219蟛蜞菊内酯≥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-氨基水杨酸≥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迷迭香酸分析标准品,≥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

 

*NOD1

项目号产品名称规格CAS包装靶点IC50
M129713ML130 (Nodinitib-1)≥99%799264-47-45mg,10mg,25mg,50mgNOD10.56 μM


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