JAK/STAT
JAK/STAT(Janus激酶/信号转导子和转录激活子)信号通路将来自细胞外的化学信号传递给细胞核,导致与免疫、增殖、分化、凋亡和肿瘤发生等相关基因的DNA转录和表达。此信号通路是众多细胞因子信号转导的共同途径,其活性在炎性疾病和血液恶性肿瘤等疾病治疗研究中具有重要意义。JAK-STAT信号级联由三个主要成分组成:由酪氨酸激酶相关受体、酪氨酸激酶JAK和转录因子STAT三个成分组成。
JAK/STAT通路转导过程
细胞因子,如干扰素、白细胞介素和生长因子等配体,与细胞表面受体结合,引起受体分子二聚化。与受体偶联的JAK相互接近并通过交互的酪氨酸磷酸化而被激活。活化后的JAK使受体的酪氨酸磷酸化,为具有SH2结构域的STAT创建结合位点。STAT结合至受体后,在JAK作用下,STAT酪氨酸705(Tyr 705)被磷酸化。STAT就会从受体上脱离,形成同/异二聚体。STAT二聚体进入细胞核后,会结合特定的调节序列以激活或抑制靶基因的转录。
JAK/STAT信号通路图
产品列表
按靶点分类:
*JAK
项目号 |
产品名称 |
规格 |
CAS |
包装 |
细胞 |
靶点 |
IC50 |
Ki |
Ruxolitinib (INCB018424)
≥98%
941678-49-5
5mg,25mg,50mg,100mg
无细胞
JAK1
3.3 nM
Tofacitinib (CP-690550) Citrate
≥99%
540737-29-9
10mg,50mg,250mg
JAK1
112 nM
AZD1480
≥98%
935666-88-9
5mg,25mg,100mg
无细胞
JAK2
0.26 nM
Fedratinib (SAR302503, TG101348)
≥98%
936091-26-8
5mg,25mg,100mg
无细胞
JAK2
3 nM
JANEX-1
98%
202475-60-3
5mg,10mg,50mg
JAK3
78 μM
WHI-P97
≥98%
211555-05-4
10mg,50mg
JAK-3
0.09 μM
CYT387
≥98%
1056634-68-4
5mg,10mg,50mg,100mg
JAK1
11 nM
Tofacitinib
≥98% (HPLC)
477600-75-2
5mg,25mg,100mg,500mg,1g
无细胞
JAK3
1 nM
WP1066
≥98%
857064-38-1
10mg,50mg
HEL细胞
JAK2
2.30 μM
TG101209
98%
936091-14-4
5mg,25mg,100mg
无细胞
JAK2
6 nM
LY2784544
≥98%
1229236-86-5
5mg,10mg,50mg
JAK2
3 nM
NVP-BSK805 2HCl
≥97%
1092499-93-8
5mg,10mg,50mg
JAK2
0.5 nM
Baricitinib
≥99%
1187594-09-7
5mg,10mg,50mg
无细胞
JAK1
5.9 nM
AZ 960
≥99%
905586-69-8
2mg,5mg,10mg
JAK2
<3 nM
<0.45 nM
CEP-33779
≥99%
1257704-57-6
5mg,10mg,50mg
JAK2
1.8 nM
WHI-P154
≥98%
211555-04-3
10mg,50mg
JAK3
1.8 μM
XL019
≥99%
945755-56-6
5mg,25mg
JAK2
2.2 nM
S-Ruxolitinib (INCB018424)
≥99%
941685-37-6
5mg,10mg,50mg
JAK1
3.3 nM
ZM 39923 HCl
≥98%
1021868-92-7
10mg,50mg,250mg
JAK1
4.4
Ruxolitinib phosphate salt
97%
1092939-17-7
100mg
JAK
莪术醇
分析标准品,≥98%
4871-97-0
20mg
*STAT
项目号 |
产品名称 |
规格 |
CAS |
包装 |
细胞 |
靶点 |
IC50 |
S3I-201
≥99%
501919-59-1
5mg,10mg,50mg
STAT3
86 μM
氟达拉滨
98%
21679-14-1
50mg,250mg,1g,5g
STAT1
Stattic
≥98%
19983-44-9
25mg,100mg
STAT3
5.1 μM
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
Nifuroxazide
≥98%
965-52-6
50mg,100mg
STAT1/3/5
3 µM
青蒿琥酯
98%
88495-63-0
5g,25g
小细胞肺癌细胞系H69
STAT3
< 5 μM
隐丹参酮
98%
35825-57-1
50mg,250mg
无细胞
STAT3
4.6 μM
隐丹参酮
分析标准品,≥98%
35825-57-1
20mg
无细胞
STAT3
4.6 μM
*EGFR
项目号 |
产品名称 |
规格 |
CAS |
包装 |
细胞 |
靶点 |
IC50 |
Ki |
Erlotinib HCl (OSI-744)
≥99%
183319-69-9
100mg,500mg,1g,5g
无细胞
EGFR
2 nM
Gefitinib (ZD1839)
≥99%
184475-35-2
50mg,250mg,1g,5g,25g,100g
NR6wtEGFR和NR6W细胞
Tyr1173
37 nM
二对甲苯磺酸拉帕替尼(GW-572016)
≥98%
388082-77-7
25mg,100mg,250mg,500mg,1g
无细胞
EGFR
10.8 nM
Afatinib
≥99%
439081-18-2
5mg,10mg,50mg
无细胞
EGFR(wt)
0.5 nM
Neratinib (HKI-272)
≥99%
698387-09-6
5mg,25mg,100mg
无细胞
HER2
59 nM
PD153035
≥98%
153436-54-5
10mg,50mg,250mg
EGFR
5.2 pM
酪氨酸激酶抑制剂 AG 494
>98.0%(HPLC)(N)
133550-35-3
20mg,100mg
EGFR
1.2 μM
Canertinib (CI-1033)
≥98%
267243-28-7
10mg,50mg,250mg
EGFR
1.5 nM
Lapatinib
≥99%
231277-92-2
25mg,100mg,250mg,500mg,1g,5g
无细胞
EGFR
10.2 nM
AG-490 (Tyrphostin B42)
≥98%
133550-30-8
20mg,50mg,250mg,1g
无细胞
EGFR
0.1 μM
CP-724714
≥99%
537705-08-1
5mg,10mg,25mg,50mg
HER2/ErbB2
10 nM
Dacomitinib (PF299804, PF299)
≥99%
1110813-31-4
5mg,10mg,50mg,250mg
无细胞
EGFR
6 nM
WZ4002
≥98%
1213269-23-8
10mg,50mg,100mg
BaF3细胞系
EGFR(L858R)
2 nM
AZD8931 (Sapitinib)
≥98%
848942-61-0
5mg,10mg,50mg
EGFR
4 nM
CUDC-101
≥98%
1012054-59-9
10mg,25mg,50mg,100mg,250mg
HDAC
4.4 nM
AG-1478 (Tyrphostin AG-1478)
≥98%
153436-53-4
5mg,10mg,25mg,50mg
无细胞
EGFR
3 nM
PD153035 HCl
≥98%(HPLC)
183322-45-4
10mg,50mg,250mg
EGFR
29 pM
5.2 pM
Pelitinib
≥98%
257933-82-7
5mg,25mg,100mg
EGFR
38.5 nM
AC480 (BMS-599626)
≥98%
714971-09-2
5mg,25mg,100mg
HER1
20 nM
AEE788 (NVP-AEE788)
≥97%
497839-62-0
5mg,25mg,100mg
EGFR
2 nM
AP26113
≥98%
1197958-12-5
5mg,10mg,25mg,50mg,100mg
ALK
OSI-420
≥99%
183320-51-6
5mg,10mg,50mg
EGFR
2 nM
WZ3146
≥98%
1214265-56-1
5mg,25mg,100mg
EGFR(L858R)
2 nM
ARRY-380
≥98%
937265-83-3
5mg,10mg,50mg
HER2
8 nM
WZ8040
≥98%
1214265-57-2
5mg,25mg,50mg
EGFRT790M
AST-1306 TsOH
≥98%
1050500-29-2
5mg,10mg,50mg
EGFR
0.5 nM
CO-1686 (AVL-301)
≥99%
1374640-70-6
5mg,10mg,50mg,100mg
无细胞
EGFRL858R/T790M
21.5 nM
金雀异黄酮
分析标准品,≥98%
446-72-0
20mg,1g,5g
NIH-3T3细胞
EGF
12μM
金雀异黄酮
97%
446-72-0
100mg,500mg,1g,5g,25g
NIH-3T3细胞
EGF
12μM
Varlitinib
≥96%
845272-21-1
5mg,10mg,50mg
ErbB1(EGFR)
7 nM
Icotinib
≥99%
610798-31-7
5mg,10mg,50mg
EGFR
5 nM
TAK-285
≥98%
871026-44-7
5mg,10mg,50mg
HER2和EGFR(HER1)
17 nM
WHI-P154
≥98%
211555-04-3
10mg,50mg
JAK3
1.8 μM
Daphnetin
>90.0%(HPLC)
486-35-1
50mg,250mg,1g
EGFR
7.67 μM
PD168393
≥98%
194423-15-9
10mg,50mg,250mg
EGFR
0.70 nM
Tyrphostin 9
≥98%
10537-47-0
25mg,100mg,500mg
EGFR
460 μM
Tyrphostin 23
≥98%
118409-57-7
10mg,50mg,250mg
EGFR
35 μM
Olmutinib
97%
1353550-13-6
100mg
EGFR
(-)-表没食子儿茶素没食子酸酯
分析标准品
989-51-5
20mg,100mg,500mg
(-)-表没食子儿茶素没食子酸
98%
989-51-5
100mg,500mg,2.5g
Erlotinib
≥98%
183321-74-6
100mg,500mg,1g,5g
EGFR
2 nM
Norcantharidin
98%
29745-04-8
1g,5g,25g
c-Met
Butein
≥98.0%(HPLC)
487-52-5
100mg,1g
*Pim
项目号 |
产品名称 |
规格 |
CAS |
包装 |
细胞 |
靶点 |
IC50 |
SGI-1776 free base
≥98%
1025065-69-3
5mg,10mg,50mg
无细胞
Pim1
7 nM
SMI-4a
≥98%
438190-29-5
10mg,50mg
Pim1
17 nM
AZD1208
≥98%
1204144-28-4
5mg,25mg,100mg
Pim1
0.4 nM