阿拉丁小分子抑制剂、激动剂、拮抗剂--JAK/STAT信号通路

发布人：上海阿拉丁生化科技股份有限公司

发布日期:2020/5/13 15:34:50

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

R126338

Ruxolitinib (INCB018424)

≥98%

941678-49-5

5mg,25mg,50mg,100mg

无细胞

JAK1

3.3 nM

JAK2

2.8 nM

E129454

Tofacitinib (CP-690550) Citrate

≥99%

540737-29-9

10mg,50mg,250mg

JAK1

112 nM

JAK2

20 nM

JAK3

1 nM

A126326

AZD1480

≥98%

935666-88-9

5mg,25mg,100mg

无细胞

JAK2

0.26 nM

T126330

Fedratinib (SAR302503, TG101348)

≥98%

936091-26-8

5mg,25mg,100mg

无细胞

JAK2

3 nM

J126663

JANEX-1

98%

202475-60-3

5mg,10mg,50mg

JAK3

78 μM

W125855

WHI-P97

≥98%

211555-05-4

10mg,50mg

JAK-3

0.09 μM

C127224

CYT387

≥98%

1056634-68-4

5mg,10mg,50mg,100mg

JAK1

11 nM

JAK2

18 nM

T122330

Tofacitinib

≥98% (HPLC)

477600-75-2

5mg,25mg,100mg,500mg,1g

无细胞

JAK3

1 nM

W129459

WP1066

≥98%

857064-38-1

10mg,50mg

HEL细胞

JAK2

2.30 μM

STAT3

2.43 μM

T127523

TG101209

98%

936091-14-4

5mg,25mg,100mg

无细胞

JAK2

6 nM

Flt3

25 nM

RET

17 nM

L126490

LY2784544

≥98%

1229236-86-5

5mg,10mg,50mg

JAK2

3 nM

N129609

NVP-BSK805 2HCl

≥97%

1092499-93-8

5mg,10mg,50mg

JAK2

0.5 nM

B127687

Baricitinib

≥99%

1187594-09-7

5mg,10mg,50mg

无细胞

JAK1

5.9 nM

JAK2

5.7 nM

A129464

AZ 960

≥99%

905586-69-8

2mg,5mg,10mg

JAK2

＜3 nM

＜0.45 nM

C129474

CEP-33779

≥99%

1257704-57-6

5mg,10mg,50mg

JAK2

1.8 nM

W125072

WHI-P154

≥98%

211555-04-3

10mg,50mg

JAK3

1.8 μM

X127151

XL019

≥99%

945755-56-6

5mg,25mg

JAK2

2.2 nM

S129613

S-Ruxolitinib (INCB018424)

≥99%

941685-37-6

5mg,10mg,50mg

JAK1

3.3 nM

JAK2

2.8 nM

Z129618

ZM 39923 HCl

≥98%

1021868-92-7

10mg,50mg,250mg

JAK1

4.4

JAK3

7.1

R171967

Ruxolitinib phosphate salt

97%

1092939-17-7

100mg

JAK

C114054

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

S129625

S3I-201

≥99%

501919-59-1

5mg,10mg,50mg

STAT3

86 μM

F122998

氟达拉滨

98%

21679-14-1

50mg,250mg,1g,5g

STAT1

S129623

Stattic

≥98%

19983-44-9

25mg,100mg

STAT3

5.1 μM

N130841

氯硝柳胺

98%

50-65-7

50g,250g

无细胞

STAT3

0.7 μM

N114456

氯硝柳胺

分析标准品

50-65-7

100mg

无细胞

STAT3

0.7 μM

N129550

Nifuroxazide

≥98%

965-52-6

50mg,100mg

STAT1/3/5

3 µM

A107818

青蒿琥酯

98%

88495-63-0

5g,25g

小细胞肺癌细胞系H69

STAT3

< 5 μM

C101974

隐丹参酮

98%

35825-57-1

50mg,250mg

无细胞

STAT3

4.6 μM

C101973

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

E129310

Erlotinib HCl (OSI-744)

≥99%

183319-69-9

100mg,500mg,1g,5g

无细胞

EGFR

2 nM

G125799

Gefitinib (ZD1839)

≥99%

184475-35-2

50mg,250mg,1g,5g,25g,100g

NR6wtEGFR和NR6W细胞

Tyr1173

37 nM

Tyr992

37nM

Tyr1173

26 nM

Tyr992

57 nM

L129338

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

ErbB2

9.2 nM

A129323

Afatinib

≥99%

439081-18-2

5mg,10mg,50mg

无细胞

EGFR(wt)

0.5 nM

EGFR(L858R)

0.4 nM

EGFR(L858R/T790M)

10 nM

ErbB2（HER2）

14 nM

ErbB4（HER4）

1 nM

N126132

Neratinib (HKI-272)

≥99%

698387-09-6

5mg,25mg,100mg

无细胞

HER2

59 nM

EGFR

92 nM

P125741

PD153035

≥98%

153436-54-5

10mg,50mg,250mg

EGFR

5.2 pM

T162509

酪氨酸激酶抑制剂 AG 494

>98.0%(HPLC)(N)

133550-35-3

20mg,100mg

EGFR

1.2 μM

EGF

6 μM

C125447

Canertinib (CI-1033)

≥98%

267243-28-7

10mg,50mg,250mg

EGFR

1.5 nM

ErbB2

9.0 nM

L126696

Lapatinib

≥99%

231277-92-2

25mg,100mg,250mg,500mg,1g,5g

无细胞

EGFR

10.2 nM

ErbB2

9.8 nM

A126525

AG-490 (Tyrphostin B42)

≥98%

133550-30-8

20mg,50mg,250mg,1g

无细胞

EGFR

0.1 μM

C129397

CP-724714

≥99%

537705-08-1

5mg,10mg,25mg,50mg

HER2/ErbB2

10 nM

D129347

Dacomitinib (PF299804, PF299)

≥99%

1110813-31-4

5mg,10mg,50mg,250mg

无细胞

EGFR

6 nM

W127713

WZ4002

≥98%

1213269-23-8

10mg,50mg,100mg

BaF3细胞系

EGFR(L858R)

2 nM

EGFR(T790M)

8 nM

A129380

AZD8931 (Sapitinib)

≥98%

848942-61-0

5mg,10mg,50mg

EGFR

4 nM

ErbB2

3 nM

ErbB3

4 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

A126582

AG-1478 (Tyrphostin AG-1478)

≥98%

153436-53-4

5mg,10mg,25mg,50mg

无细胞

EGFR

3 nM

P129384

PD153035 HCl

≥98%(HPLC)

183322-45-4

10mg,50mg,250mg

EGFR

29 pM

5.2 pM

P125444

Pelitinib

≥98%

257933-82-7

5mg,25mg,100mg

EGFR

38.5 nM

B126145

AC480 (BMS-599626)

≥98%

714971-09-2

5mg,25mg,100mg

HER1

20 nM

HER2

30 nM

A126830

AEE788 (NVP-AEE788)

≥97%

497839-62-0

5mg,25mg,100mg

EGFR

2 nM

HER2/ErbB2

6 nM

A127691

AP26113

≥98%

1197958-12-5

5mg,10mg,25mg,50mg,100mg

ALK

EGFR

O125033

OSI-420

≥99%

183320-51-6

5mg,10mg,50mg

EGFR

2 nM

W127717

WZ3146

≥98%

1214265-56-1

5mg,25mg,100mg

EGFR(L858R)

2 nM

EGFR(E746_A750)

2 nM

A126334

ARRY-380

≥98%

937265-83-3

5mg,10mg,50mg

HER2

8 nM

W126471

WZ8040

≥98%

1214265-57-2

5mg,25mg,50mg

EGFRT790M

A129426

AST-1306 TsOH

≥98%

1050500-29-2

5mg,10mg,50mg

EGFR

0.5 nM

ErbB2

3 nM

C124905

CO-1686 (AVL-301)

≥99%

1374640-70-6

5mg,10mg,50mg,100mg

无细胞

EGFRL858R/T790M

21.5 nM

EGFRWT

303.3 nM

G106672

金雀异黄酮

分析标准品,≥98%

446-72-0

20mg,1g,5g

NIH-3T3细胞

EGF

12μM

胰岛素

19 μM

G106673

金雀异黄酮

97%

446-72-0

100mg,500mg,1g,5g,25g

NIH-3T3细胞

EGF

12μM

胰岛素

19 μM

V129433

Varlitinib

≥96%

845272-21-1

5mg,10mg,50mg

ErbB1(EGFR)

7 nM

ErbB2(HER2)

2 nM

I129405

Icotinib

≥99%

610798-31-7

5mg,10mg,50mg

EGFR

5 nM

T126234

TAK-285

≥98%

871026-44-7

5mg,10mg,50mg

HER2和EGFR(HER1)

17 nM

HER2和EGFR(HER1)

23 nM

W125072

WHI-P154

≥98%

211555-04-3

10mg,50mg

JAK3

1.8 μM

D155111

Daphnetin

>90.0%(HPLC)

486-35-1

50mg,250mg,1g

EGFR

7.67 μM

PKA

9.33 μM

PKC

25.01 μM

P129447

PD168393

≥98%

194423-15-9

10mg,50mg,250mg

EGFR

0.70 nM

T129439

Tyrphostin 9

≥98%

10537-47-0

25mg,100mg,500mg

EGFR

460 μM

PDGFR

0.5μM

T129445

Tyrphostin 23

≥98%

118409-57-7

10mg,50mg,250mg

EGFR

35 μM

O173511

Olmutinib

97%

1353550-13-6

100mg

EGFR

E107403

(-)-表没食子儿茶素没食子酸酯

分析标准品

989-51-5

20mg,100mg,500mg

E107404

(-)-表没食子儿茶素没食子酸

98%

989-51-5

100mg,500mg,2.5g

E126633

Erlotinib

≥98%

183321-74-6

100mg,500mg,1g,5g

EGFR

2 nM

N159736

Norcantharidin

98%

29745-04-8

1g,5g,25g

c-Met

EGFR

B135922

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

S126376

SGI-1776 free base

≥98%

1025065-69-3

5mg,10mg,50mg

无细胞

Pim1

7 nM

T125988

SMI-4a

≥98%

438190-29-5

10mg,50mg

Pim1

17 nM

A127698

AZD1208

≥98%

1204144-28-4

5mg,25mg,100mg

Pim1

0.4 nM

Pim2

5 nM

Pim3

1.9 nM