自噬
自噬是一个吞噬自身细胞质蛋白或细胞器并使其包被进入囊泡,并与溶酶体融合形成自噬溶酶体,降解其所包裹的内容物的过程。在哺乳动物细胞中,自噬主要有三种类型:微自噬、巨自噬和分子伴侣介导的自噬(CMA)。微自噬通过溶酶体的膜直接包裹待降解物质等,并在溶酶体内降解。巨自噬则由双层膜囊泡包裹待降解物质然后运送到溶酶体中降解。而在分子伴侣介导的自噬(CMA)过程中,分子伴侣识别待降解蛋白,去折叠后并转移目的蛋白至溶酶体内。
自噬通常发生在营养缺乏的情况下,也与发育、分化、神经退行性疾病、应激、感染和癌症等生理和病理过程有关。自噬机制的受损与肿瘤、神经退行性疾病、代谢相关疾病、免疫性疾病等发病过程密切相关。
自噬信号通路转导过程
巨自噬:(1)起始:UKL和Beclin 1蛋白复合物起始自噬泡的形成。(2)延伸:Atg5-Atg12-Atg16L复合物形成并与自噬泡融合;微管相关蛋白轻链3(LC3)由可溶解形式(LC3-I)转变为脂溶形式(LC3-II),与自噬泡结合形成自噬体。(3)融合与降解:自噬体捕获需降解或清除的蛋白质、细胞器等物质;自噬体与溶酶体融合形成自噬溶酶体,释放内容物降解,完成自噬。
线粒体自噬:属于选择性自噬,主要是降解细胞中损伤和不需要的线粒体。线粒体处于健康状态时,PINK 蛋白通过PARL的促进持续降解,而当线粒体功能障碍时, PINK蛋白会处于稳定状态,从细胞质中招募E3泛素连接酶Parkin,来诱导线粒体自噬。Parkin会诱导线粒体膜蛋白的聚泛素化,由此导致通过LC3-作用区域(LIR)与LC3结合的自噬受体蛋白的SQSTM1/p62,NBR1和Ambra1聚集。另外,在特定细胞中,BNIP3 和 BNIP3L/NIX(也存在LIR)可通过非泛素反应机制聚集自噬的相关因子,从而促进自噬体的形成。
自噬信号通路图
产品列表
按靶点分类:
*Autophagy
项目号 |
产品名称 |
规格 |
CAS |
包装 |
细胞 |
靶点 |
IC50 |
EC50 |
Ki |
kd |
ED50 |
LY294002
≥98%
154447-36-6
10mg,25mg,50mg
无细胞
p110α
0.5 μM
紫杉醇
99%
33069-62-4
10mg,50mg,250mg,1g,5g
人内皮细胞
Microtubule
0.1 pM
紫杉醇
分析标准品,≥99%
33069-62-4
10mg
人内皮细胞
Microtubule
0.1 pM
Wortmannin
98%
19545-26-7
5mg,10mg,25mg
无细胞
PI3K
3 nM
3-甲基腺嘌呤
98%
5142-23-4
50mg,250mg,1g,5g,25g
HeLa细胞
Vps34
25 μM
Nocodazole
≥99%
31430-18-9
10mg,50mg
Abl
0.21 μM
磷酸氯喹
≥99%
50-63-5
5g,10g,25g,100g,500g
ATM
Azithromycin
分析标准品
83905-01-5
25mg
PFK15
98% (HPLC)
4382-63-2
5mg,25mg
PFKFB3
207 nM
Spautin-1
98% (HPLC)
1262888-28-7
5mg,25mg
USP10
0.5779 μM
青藤碱盐酸盐
97%
6080-33-7
1g,5g
青藤碱盐酸盐
分析标准品,≥97%
6080-33-7
20mg
硫酸羟基氯喹
≥98%
747-36-4
250mg,1g,5g,25g
TLR9
Vorinostat
≥99.0%
149647-78-9
100mg,500mg,1g,5g
ABT-737
≥97%
852808-04-9
5mg,25mg,100mg
无细胞
Bcl-xL
78.7 nM
Y-27632 dihydrochloride
≥98%
129830-38-2
5mg,10mg,50mg,100mg
ROCK1
140 nM
Rapamycin
≥95%(HPLC)
53123-88-9
50mg,250mg,1g
HEK293细胞
mTOR
~0.1 nM
Rapamycin
≥98%(HPLC)
53123-88-9
10mg,25mg,50mg,250mg,1g
HEK293细胞
mTOR
~0.1 nM
Erlotinib HCl (OSI-744)
≥99%
183319-69-9
100mg,500mg,1g,5g
无细胞
EGFR
2 nM
Obatoclax Mesylate
≥97%
803712-79-0
5mg,10mg,50mg,100mg
无细胞
Bcl-2
0.22 μM
PI-103
≥98%
371935-74-9
10mg,50mg,100mg
无细胞
p110α
2 nM
盐酸吉西他滨
98%
122111-03-9
10mg,50mg,250mg,1g,5g,25g
PANC1细胞
DNA合成
50 nM
PP242
≥98%
1092351-67-1
5mg,10mg,50mg
无细胞
mTOR
8 nM
Temozolomide
≥98% (HPLC)
85622-93-1
250mg,500mg,1g,5g25g,100g
Metformin hydrochloride
97%
1115-70-4
5g,25g,100g,500g
Fasudil Hydrochloride
98%
105628-07-7
100mg,250mg,500mg,1g,5g
ROCK2
0.33 μM
他莫昔芬柠檬酸盐
99%
54965-24-1
1g,5g,25g
ER
Torin 1
≥97%
1222998-36-8
10mg,25mg,50mg
无细胞
mTORC1
2 nM
白藜芦醇
99%
501-36-0
1g,5g,25g,100g
COX
1.1 μM
白藜芦醇
分析标准品
501-36-0
100mg
COX
1.1 μM
Dexamethasone
98%
50-02-2
1g,5g,25g
Gemcitabine
≥99%
95058-81-4
50mg,100mg,250mg,1g,5g,25g
布雷非德菌素 A
≥98% (HPLC)
20350-15-6
5mg,25mg
HCT 116
ATPase
0.2 μM
格尔德霉素
≥98% (HPLC)
30562-34-6
10mg,50mg,250mg
SKBr3
p185
70 nM
Pifithrin-α (PFTα)
≥97%
63208-82-2
10mg,50mg
p53
氯硝柳胺
98%
50-65-7
50g,250g
无细胞
STAT3
0.7 μM
氯硝柳胺
分析标准品
50-65-7
100mg
无细胞
STAT3
0.7 μM
奥美拉唑
98%
73590-58-6
1g,5g,25g,100g
Amiodarone hydrochloride
≥98%
19774-82-4
1g,5g,25g,100g
Loperamide HCl
≥98%
34552-83-5
5g,25g
μ阿片受体
3.3 nM
地塞米松磷酸钠
≥99%
55203-24-2
50mg,250mg
卡马西平
≥98.0%
298-46-4
5g,25g,100g
钠离子通道
131 μM
盐酸可乐定
98%
4205-91-8
250mg,1g,5g,100g
α2肾上腺素能受体
0.02±0.01 mg/kg
Flubendazole
≥98%(HPLC)
31430-15-6
5g,25g,100g
Nimodipine
≥98%
66085-59-4
250mg,1g,5g
乙酸地塞米松
98%
1177-87-3
250mg,1g,5g,25g
尼群地平
≥95.0%
39562-70-4
25mg,100mg,500mg,1g
钙离子通道
95 nM
磺胺乙酰钠
分析标准品
127-56-0
250mg,25g
异钩藤碱
分析标准品,≥98%
6859-01-4
10mg,20mg
他莫西芬
≥99%
10540-29-1
1g,5g,25g
他莫西芬
分析标准品,≥99.0% (HPLC)
10540-29-1
50mg
Vincristine sulfate
98%
2068-78-2
25mg,100mg
微管
32 μM
硫酸长春新碱
分析标准品,>99%
2068-78-2
10mg
微管
32 μM
2-丙戊酸钠
≥98.0%
1069-66-5
5g,25g,100g,500g
HDAC
STF-62247
≥98%
315702-99-9
5mg,25mg,100mg
Sulfacetamide sodium salt monohydrate
-
6209-17-2
100g,500g
DHPS
9.5 μM
MG-132
≥98%
133407-82-6
5mg,25mg,100mg,1g
蛋白酶体
100 nM
Carprofen
>98.0%(HPLC)
53716-49-7
1g,5g,25g,100g
COX-2
3.9 μM
肝素钠
≥180 USP units/mg
9041-08-1
100KU,250KU,500KU,1000KU
肝素钠
185 USP units/mg
9041-08-1
1g,5g,25g
Olaparib (AZD2281, Ku-0059436)
≥98%
763113-22-0
10mg,25mg,100mg,250mg,1g
PARP-1
5 nM
盐酸阿霉素
98%
25316-40-9
25mg,100mg,250mg,500mg,1g,5g
TAK-242
≥98%
243984-11-4
5mg,10mg,50mg,100mg
NO
1.8 nM
ABT-199 (GDC-0199)
≥99%
1257044-40-8
10mg,50mg
Bcl-2
<0.01 nM
巴佛洛霉素A1
≥95.0 %
88899-55-2
1mg,5mg
V-ATPase
肝素钠
≥180 USP units/mg
9041-08-1
100KU,250KU,500KU,1000KU
肝素钠
185 USP units/mg
9041-08-1
1g,5g,25g
Olaparib (AZD2281, Ku-0059436)
≥98%
763113-22-0
10mg,25mg,100mg,250mg,1g
PARP-1
5 nM
盐酸阿霉素
98%
25316-40-9
25mg,100mg,250mg,500mg,1g,5g
TAK-242
≥98%
243984-11-4
5mg,10mg,50mg,100mg
NO
1.8 nM
ABT-199 (GDC-0199)
≥99%
1257044-40-8
10mg,50mg
Bcl-2
<0.01 nM
巴佛洛霉素A1
≥95.0 %
88899-55-2
1mg,5mg
V-ATPase
(+)-JQ1
98% (HPLC)
1268524-70-4
5mg,25mg
BRD41
77 nM
SB-203580
≥98%(HPLC)
152121-47-6
5mg,25mg,100mg,500mg
SAPK2a/p38
50 nM
SP600125
≥98%
129-56-6
25mg,100mg,500mg,1g,5g
JNK1
40 nM
CHIR-99021 (CT99021) HCl
≥98%
252917-06-9
5mg,25mg,100mg
GSK-3α
10 nM
CHIR-99021
≥98%
252917-06-9
5mg,25mg
GSK-3α
10 nM
Enzalutamide
≥98%
915087-33-1
25mg,100mg,250mg,1g,5g
LNCaP前列腺细胞
AR
36 nM
Sorafenib
≥99%
284461-73-0
250mg,1g
Raf-1
6 nM
U0126-EtOH
≥97%
1173097-76-1
25mg,100mg,500mg
MEK1
70 nM
MK-2206 2HCl
≥98%
1032350-13-2
10mg,50mg,100mg
Akt1
5 nM
Trametinib (GSK1120212)
≥98%
871700-17-3
10mg,50mg,100mg,250mg,500mg,1g
MEK1
2 nM
PD98059
≥98%
167869-21-8
10mg,50mg
MEK1
2-7 µM
Forskolin
≥98%
66575-29-9
10mg,50mg,100mg,500mg,1g
腺苷酸环化酶
41 nM
0.5 μM
Bortezomib (PS-341)
≥98%
179324-69-7
5mg,25mg,100mg,1g
20S 蛋白酶体
0.6 nM
奥沙利铂
99%
61825-94-3
25mg,100mg,500mg
人黑色素瘤细胞系
C32
0.98 μM
BAY 11-7082
≥98%
19542-67-7
50mg,250mg,1g
USP7
0.19 μM
Dorsomorphin 2HCl
≥98%
1219168-18-9
5mg,10mg,50mg
AMPK
109 nM
Necrostatin-1
≥99%
4311-88-0
10mg,50mg
RIP1
182 nM
Gefitinib (ZD1839)
≥99%
184475-35-2
50mg,250mg,1g,5g,25g,100g
NR6wtEGFR 细胞
EGFR
2-37 nM
Dorsomorphin
≥98%
866405-64-3
5mg,25mg,100mg
AMPK
109 nM
Everolimus
≥98%
159351-69-6
10mg,25mg,100mg
mTOR
5-6 nM
Acadesine
≥98%
2627-69-2
50mg,250mg,1g
Dasatinib
≥99%
302962-49-8
25mg,100mg,500mg,1g,5g
Abl
0.6 nM
Verteporfin
≥97%
129497-78-5
10mg,50mg
Dasatinib
≥99%
302962-49-8
25mg,100mg,500mg,1g,5g
Abl
0.6 nM
Verteporfin
≥97%
129497-78-5
10mg,50mg
DAPT
≥98%
208255-80-5
5mg,10mg,25mg,50mg
Aβ
115 nM
Ruxolitinib (INCB018424)
≥98%
941678-49-5
5mg,25mg,50mg,100mg
JAK1
3.3 nM
Etoposide
98%
33419-42-0
100mg,250mg,500mg,1g,5g
5-氮胞苷
98%
320-67-2
50mg,250mg,1g,5g,25g
Vemurafenib (PLX4032, RG7204)
≥98%
918504-65-1
10mg,25mg,50mg,100mg,500mg,1g,5g
RAFV600E
31 nM
SB 202190
99%
152121-30-7
5mg,25mg,100mg
p38α
50 nM
Panobinostat (LBH589)
≥98%
404950-80-7
10mg,50mg
6-乙基鹅去氧胆酸
98%
459789-99-2
50mg,250mg,1g
FXR
99 nM
CB-839
97%
1439399-58-2
100mg
肾脏
GLS1
23 nM
*FKBP
项目号 |
产品名称 |
规格 |
CAS |
包装 |
细胞 |
靶点 |
IC50 |
Rapamycin
≥95%(HPLC)
53123-88-9
50mg,250mg,1g
HEK293细胞
mTOR
~0.1 nM
Rapamycin
≥98%(HPLC)
53123-88-9
10mg,25mg,50mg,250mg,1g
HEK293细胞
mTOR
~0.1 nM
Everolimus
≥98%
159351-69-6
10mg,25mg,100mg
mTOR
5-6 nM
他克莫司
分析标准品,≥98%
104987-11-3
10mg
-
-
-
他克莫司
≥98%(HPLC)
104987-11-3
50mg,1g
-
-
-
他克莫司一水合物
≥80.0%(HPLC)
109581-93-3
10mg,50mg,250mg,1g
-
-
-
Ascomycin
≥97.0%
104987-12-4
25mg,100mg,500mg
-
-
-
*LRRK2
项目号 |
产品名称 |
规格 |
CAS |
包装 |
靶点 |
IC50 |
LRRK2-IN-1
≥99%
1234480-84-2
10mg,50mg,100mg
LRRK2 (G2019S)
6 nM
GSK2578215A
98% (HPLC)
1285515-21-0
5mg,10mg,25mg,50mg,100mg
LRRK2 (G2019S)
8.9 nM
IKK-16 (IKK Inhibitor VII)
≥99%
873225-46-8
10mg,50mg
IKK2
40 nM
LRRK2-IN-1
≥99%
1234480-84-2
10mg,50mg,100mg
LRRK2 (G2019S)
6 nM
GSK2578215A
98% (HPLC)
1285515-21-0
5mg,10mg,25mg,50mg,100mg
LRRK2
~10 nM
*CXCR
项目号 |
产品名称 |
规格 |
CAS |
包装 |
细胞 |
靶点 |
IC50 |
单宁酸
AR
1401-55-4
10g,25g,100g,250g,500g
-
CXCR4
-
Reparixin
≥98%
266359-83-5
5mg,25mg,100mg
-
CXCR1
-
Plerixafor 8HCl (AMD3100 8HCl)
≥99%
155148-31-5
5mg,10mg,50mg
-
CXCR4
44 nM
Plerixafor
≥98%
110078-46-1
10mg,50mg,250mg
无细胞
CXCR4
44 nM
danirixin
97%
954126-98-8
100mg
-
CXCL8
12.5 nM
*Mitophagy
项目号 |
产品名称 |
规格 |
CAS |
包装 |
细胞 |
靶点 |
IC50 |
M129496
3-甲基腺嘌呤
98%
5142-23-4
50mg,250mg,1g,5g,25g
PtdIns3Kγ
60 μM
O126162
Olaparib (AZD2281, Ku-0059436)
≥98%
763113-22-0
10mg,25mg,100mg,250mg,1g
PARP-1
5 nM
D107159
盐酸阿霉素
98%
25316-40-9
25mg,100mg,250mg,
S131899
SB-203580
≥98%(HPLC)
152121-47-6
5mg,25mg,100mg,500mg
SAPK2a/p38
50 nM
M107827
Metformin hydrochloride
97%
1115-70-4
5g,25g,100g,500g
U127670
U0126-EtOH
≥97%
1173097-76-1
25mg,100mg,500mg,
MEK1
70 nM
D137736
Dexamethasone
98%
50-02-2
1g,25g,100g
A129749
Acadesine
≥98%
2627-69-2
50mg,250mg,1g
R126338
Ruxolitinib (INCB018424)
≥98%
941678-49-5
5mg,25mg,50mg,100mg
JAK1
3.3 nM
E121713
Etoposide
98%
33419-42-0
100mg,250mg,500mg,1g,5g
B102375
布雷非德菌素 A
≥98% (HPLC)
20350-15-6
5mg,25mg
HCT 116
ATPase
0.2 μM
V125336
Vorinostat
≥99%
149647-78-9
100mg,500mg,1g,5g
R107315
白藜芦醇
99%
501-36-0
1g,5g,25g,100g
COX
1.1 μM
R107314
白藜芦醇
分析标准品
501-36-0
100mg
COX
1.1 μM
A126970
17-AAG
98%
75747-14-7
25mg,100mg
HSP90
5 nM
M118674
褪黑素
98%
73-31-4
250mg,1g,5g,25g,100g
*Mitophagy
项目号 |
产品名称 |
规格 |
CAS |
包装 |
靶点 |
IC50 |
M126461
MRT67307
≥98%
1190378-57-4
10mg,50mg
IKKε
160 nM