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JAK

Inhibitory Selectivity
Catalog No.Inhibitor Name JAK1JAK2JAK3Tyk2Other
A11041Ruxolitinib
***
****
A10241Tofacitinib Citrate
**
**
****
ROCK2,LCK
A10110AZD1480
****
A11082Fedratinib
****
FLT3,RET
A10095AT9283
****
****
***
Aurora B,Aurora A,Abl1
A10047AG-490
*
EGFR,ErbB2
A10263Momelotinib
***
***
*
A11795WP1066
*
STAT3
A11180TG101209
***
*
RET,FLT3
A10546Gandotinib
**
****
**
**
FLT3,FLT4,FGFR2
A11193NVP-BSK805 2HCl
**
****
***
***
A11329Baricitinib
***
***
**
A10104AZ 960
****
A12808CEP-33779
****
A12694Pacritinib
*
**
*
**
FLT3 (D835Y),FLT3
A14049WHI-P154
*
EGFR,Src,VEGFR
A12394XL019
*
****
*
*
PDGFRβ,FLT3,c-Kit
A14955S-Ruxolitinib
***
****
*
**
A13509ZM 39923 HCl
*
*
TGM2,EGFR
A14012Decernotinib
***
***
****
***
A14210Cerdulatinib
***
***
***
****
ARK5,MST1,Fms
A14232Filgotinib
***
**
*
*
A15911FLLL32
*
A11241BMS-911543
*
****
**
**
A14438Peficitinib
A13162GLPG0634 analogue
A12419Go6976
FLT3,PKCα,PKCβ1
A10247Curcumol
A11608WHI-P97
A13082PF-03394197 (oclacitinib)
***
***
**
**
A13457Pyridone 6 (JAK Inhibitor I)
***
****
****
A14132NSC 42834(JAK2 Inhibitor V, Z3)
A14390INCB39110 (Itacitinib)
A14405Solcitinib (GSK2586184)
A15134JANEX-1
*
A15362Cercosporamide
***
Mnk2, Mnk1
A15365TCS 21311
*
*
***
*
A15366ZM 449829
****
****
STAT-5, EGFR, CDK4
A15389NSC 33994
A16227ZM 39923
*
*
TGM2, EGFR

Notes:
1.Hover mouse over " * " to view the IC50 value.(A few compounds have proven potency but without published IC50 data.)
2.For more details about the compound, click on the product name of your interest.
3.The higher the number of " * " is, the more potent the inhibitor or activator is.
4."" refers to compounds which do inhibitory effects on the related isoform, but without specific value.



产品 1 到 50 共 51个

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Catalog No. Product Name Application Product Information
A10247 SALE

Curcumol

JAK2 抑制剂
Curcumol induces apoptosis via caspases-independent mitochondrial pathway in human lung adenocarcinoma ASTC-a-1 cells.
A15364

SD 1008

JAK2/STAT3 抑制剂
SD 1008 is reported to be a JAK2/STAT3 signaling pathway inhibitor which additionally inhibits Src. SD 1008 is noted to induce apoptosis in cell lines that express constitutively active tyrosine-phosphorylated STAT3.
A15365

TCS 21311

JAK3 抑制剂
TCS 21311 is a potent JAK3 inhibitor (IC50 = 8 nM). TCS 21311 is selective for JAK3 over JAK1, JAK2 and Tyk 2 (IC50 values are 1017, 2550 and 8055 nM respectively).
A15366

ZM 449829

JAK/STAT 抑制剂
JAK3 Inhibitor V is a potent, selective inhibitor of JAK3 (Janus tyrosine kinase 3) which binds competitively to the JAK3 ATP site.
A15389

NSC 33994

JAK2 抑制剂
NSC 33994 is novel inhibitor of JAK2 tyrosine kinase (Janus kinase 2 ). Janus kinase 2 (JAK2) plays a crucial role in the pathomechanism of myeloproliferative disorders and hematological malignancies.
A14438

Peficitinib (ASP015K, JNJ-54781532)

JAK 抑制剂?€?
Peficitinib is a novel potent JAK inhibitor, which demonstrated potent efficacy in adjuvant-induced arthritis model in rats.
A15911

FLLL32

JAK2 抑制剂
FLLL32 is a potent JAK2/STAT3 inhibitor with IC50 of <5 uM.
A11608

WHI-P97

JAK3 抑制剂
WHI-P97 is a rationally designed potent inhibitor of JAK-3.
A16224

NS-018

JAK2 抑制剂
NS-018 is an orally bioavailable, small molecule inhibitor of Janus-associated kinase 2 (JAK2) and Src-family kinases, with potential antineoplastic activity.
A16225

NS-018 hydrochloride

JAK2 抑制剂
NS-018 hydrochloride is a novel highly selective JAK2 inhibitor.
A16226

NS-018 maleate

JAK2 抑制剂
NS-018 maleate is an ATP-competitive small-molecule inhibitor of JAK2 with IC50 of 470nM in Ba/F3-JAK2V617F cells . have30-50-fold greater selectivity for JAK2 over other JAK-family kinases, such as JAK1, JAK3 and tyrosine kinase 2.
A16227

ZM39923

JAK1/3 抑制剂
ZM39923 is an JAK1/3 inhibitor with pIC50 of 4.4/7.1, almost no activity to JAK2 and modestly potent to EGFR; also found to be sensitive to transglutaminase.
A15363

Cucurbitacin I

JAK2/STAT3 抑制剂
Cucurbitacin I, Cucumis sativus L. has been found to suppress levels of phosphotyrosine Stat3 (signal transducer and activator of transcription 3) in v-Src-transformed NIH 3T3 cells.
A15362

Cercosporamide

Mnk2/JAK3 抑制剂
Cercosporamide, an usnic amide, was originally identified in Cercosporidium henningsii as a host-selective phytotoxin and broad-spectrum antifungal agent and is a potent inhibitor of MAP-kinase interacting kinase-2 (Mnk2; IC50 = 11 nM), JAK3 (IC50 = 31), and Mnk1 (IC50 = 116 nM).
A12694 SALE

Pacritinib (SB1518)

JAK2/FLT3 抑制剂
Pacritinib, also known as SB1518, is an orally bioavailable inhibitor of Janus kinase 2 (JAK2) and the JAK2 mutant JAK2V617F with potential antineoplastic activity. Pacritinib competes with JAK2 for ATP binding, which may result in inhibition of JAK2 activation, inhibition of the JAK-STAT signaling pathway, and so caspase-dependent apoptosis.
A14147

PRT 062070 (Cerdulatinib)

Dual Syk and JAK 抑制剂
PRT062070 is a novel, oral, dual spleen tyrosine kinase (Syk) and janus kinase (JAK) inhibitor. Cerdulatinib preferentially inhibited JAK1 and JAK3 dependent cytokine mediated signaling and functional responses in various cell types.
A14132

NSC 42834(JAK2 Inhibitor V, Z3)

JAK2 抑制剂
Z3 is a novel specific inhibitor of Jak2 tyrosine kinase.
A14232 SALE

Filgotinib

JAK 抑制剂
Filgotinib is a selective JAK1 inhibitor with IC50 of 10 nM, 28 nM, 810 nM, and 116 nM for JAK1, JAK2, JAK3, and TYK2, respectively.
A14405

Solcitinib (GSK2586184)

JAK1 抑制剂
Solcitinib is a Janus kinase 1 (JAK1) inhibitor.
A14012

Decernotinib

JAK3 抑制剂
Decernotinib is an oral, selective Janus kinase 3 (JAK3) inhibitor being developed by Vertex.
A13509

ZM 39923 HCl

JAK3 抑制剂
ZM 39923 HCl is an inhibitor of JAK3 (IC50 = 79 nM) that less potently inhibits epidermal growth factor receptor, JAK1, and cyclin-dependent kinase 4 (IC50s = 2.4, 40, and 10 M, respectively)
A14955

S-Ruxolitinib

JAK 抑制剂
S-Ruxolitinib is the chirality of INCB018424, is a potent and selective small-molecule Janus kinase 1 (JAK1) and JAK2 inhibitor.
A15056

CYT387 sulfate salt

JAK 抑制剂
CYT387 sulfate salt is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, ~10-fold selectivity versus JAK3.
A15134 SALE

JANEX-1

JAK3 抑制剂
Janex-1 is a cell-permeable, reversible, potent, ATP-competitive, and specific inhibitor of JAK3 (IC50 = 78 uM); has no effect on JAK1, JAK2, or Zap/Syk or SRC tyrosine kinases.
A15361

1,2,3,4,5,6-Hexabromocyclohexane

JAK2 抑制剂
1,2,3,4,5,6-Hexabromocyclohexane is a potent and specific inhibitor of JAK2 autophosphorylation.
A13162 SALE

GLPG0634

JAK1 抑制剂
GLPG0634 is an orally-available, selective inhibitor of JAK1 (Janus kinase 1) being developed by Galapagos for the treatment of rheumatoid arthritis and potentially other inflammatory diseases.
A13082

PF-03394197 (oclacitinib)

JAK1 抑制剂
PF-03394197 (oclacitinib) is a potent JAK1 inhibitor
A12394 SALE

XL019

JAK2 抑制剂
XL019 is an orally bioavailable inhibitor of Janus-associated kinase 2 (JAK2) with potential antineoplastic activity.
A12808 SALE

CEP33779

JAK2 抑制剂
CEP33779 is a selective JAK2 inhibitor with IC50 of 1.8 nM.
A12419

Go 6976

PKC 抑制剂
Go6976 is a potent PKC inhibitor with IC50 of 7.9 nM, 2.3 nM, and 6.2 nM for PKC (Rat brain), PKCα, and PKCβ1, respectively. Also a potent inhibitor of JAK2 and Flt3.
A13457 SALE

Pyridone 6 (JAK Inhibitor I)

JAK 抑制剂
JAK Inhibitor I is a potent, reversible, cell-permeable, and ATP-competitive inhibitor of JAK1, JAK2, and JAK3.
A14049

WHI-P 154

JAK3 抑制剂
WHI-P 154 is a JAK3 inhibitor with IC50 = 1.8uM. WHI-P 154 also Inhibits STAT1 activation, iNOS expression and NO production in macrophages in vitro.
A11962 SALE

TG-02 (SB1317)

FLT3 抑制剂
TG-02 is a novel small molecule potent CDK/JAK2/FLT3 inhibitor.
A14210 SALE

Cerdulatinib

multi-targeted tyrosine kinase 抑制剂
Cerdulatinib (PRT-062070) is an oral active, multi-targeted tyrosine kinase inhibitor with IC50 of 12 nM/6 nM/8 nM/0.5 nM and 32 nM for JAK1/JAK2/JAK3/TYK2 and Syk, respectively.
A14390 SALE

INCB39110 (Itacitinib)

JAK1 抑制剂
INCB39110 is a potent JAK1 tyrosine kinase inhibitor, which is currently in Phase II trials for the treatment of rheumatoid arthritis, myelofibrosis, rheumatoid arthritis and plaque psoriasis.
A15014

Baricitinib phosphate

JAK 抑制剂
Baricitinib phosphate is a selective JAK1 and JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM, ~70 and ~10-fold selective versus JAK3 and Tyk2, no inhibition to c-Met and Chk2.
A15937

CHZ868

JAK2 抑制剂
CHZ868 is a potent and selective type II JAK inhibitor which demonstrates activity in JAK inhibitor persistent cells, murine MPN models, and MPN patient samples.
A11241 SALE

BMS-911543

JAK 抑制剂
BMS-911543 is an orally available small molecule targeting a subset of Janus-associated kinase (JAK) with potential antineoplastic activity.
A11795 SALE

WP1066

JAK 抑制剂
WP1066 is a novel JAK2 inhibitor and it suppresses proliferation and induces apoptosis in eythroid human cells carrying the JAK2 V617F mutation.
A10110 SALE

AZD1480

JAK 抑制剂
AZD1480 is a novel potent small JAK2 inhibitor with an IC50 of 0.26 nM.
A10095 SALE

AT9283

Aurora/JAK 抑制剂
AT9283 inhibits aurora kinase A and B and targets other tyrosine and serine/threonine kinases associated with myeloid cell proliferation.
A10546

LY2784544 (Gandotinib)

JAK 抑制剂
LY2784544 is identified as being highly selective for JAK2-V617F and has advanced into human clinical trials for the treatment of several myeloproliferative disorders.
A10047 SALE

AG-490

EGFR 抑制剂
AG 490 is a selective inhibitor of EGF receptor tyrosine kinase (IC50 values are 2 and 13.5 μM for EGFR and ErbB2 respectively). Also inhibits JAK2 with no activity to Lck, Lyn, Btk, Syk and Src.
A10241 SALE

CP-690550 (Tofacitinib citrate)

JAK3 抑制剂
CP-690550 (Tofacitinib citrate) is an orally available, highly selective inhibitor of the Janus kinase (JAK) family of enzymes.
A10263 SALE

Cyt387 (Momelotinib)

JAK 抑制剂
CYT387 is an inhibitor of Janus kinases JAK1 and JAK2, acting as an ATP competitor with IC50 values of 11 and 18 nM, respectively.
A11082 SALE

TG-101348 (Fedratinib, SAR302503)

JAK2 抑制剂
TG-101348 is an orally bioavailable, ATP-competitive and selective inhibitor of Janus-associated kinase 2 with potential antineoplastic activity.
A10104 SALE

AZ-960

JAK2抑制剂
AZ-960 is a potent, selective and ATP competitive JAK2 inhibitor that inhibits JAK2 kinase with a Ki of 0.45 nM in vitro and induces growth arrest and apoptosis in adult T-cell leukemia (ATL) cell.
A11180

TG101209

JAK2 抑制剂

TG101209, a novel JAK2 inhibitor, has significant in vitro activity in multiple myeloma and displays preferential cytotoxicity for CD45+ myeloma cells.
A11193 SALE

NVP-BSK805

JAK 抑制剂

NVP-BSK805 is a potent and selective inhibition of polycythemia by the quinoxaline JAK2 inhibitor that potently suppressed recombinant human erythropoietin-induced polycythemia and extramedullary erythropoiesis in mice and rats.
A11329 SALE

Baricitinib (LY3009104)

JAK 抑制剂
Baricitinib, also known as INCB028050 or LY3009104, is a selective orally bioavailable JAK1/JAK2 inhibitor with nanomolar potency against JAK1 (5.9 nM) and JAK2 (5.7 nM).

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Target
  1. Aurora A (1)
  2. Aurora B (1)
  3. CDK (1)
  4. CDK4 (1)
  5. EGFR (2)
  6. ErbB2 (1)
  7. FLT3 (3)
  8. JAK1 (18)
  9. JAK2 (36)
  10. JAK3 (17)
  11. Mnk1 (1)
  12. Mnk2 (1)
  13. PKCα (1)
  14. PKCβ (1)
  15. RET (1)
  16. STAT1 (1)
  17. STAT3 (3)
  18. STAT5 (1)
  19. Syk (2)
  20. Tyk2 (5)
Mechanism of action
  1. Inhibitor (51)

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