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Inhibitory Selectivity
| Catalog No. | Inhibitor Name | JAK1 | JAK2 | JAK3 | Tyk2 | Other |
|---|---|---|---|---|---|---|
| A11041 | Ruxolitinib | *** | **** | |||
| A10241 | Tofacitinib Citrate | ** | ** | **** | ROCK2,LCK | |
| A10110 | AZD1480 | **** | ||||
| A11082 | Fedratinib | **** | FLT3,RET | |||
| A10095 | AT9283 | **** | **** | *** | Aurora B,Aurora A,Abl1 | |
| A10047 | AG-490 | * | EGFR,ErbB2 | |||
| A10263 | Momelotinib | *** | *** | * | ||
| A11795 | WP1066 | * | STAT3 | |||
| A11180 | TG101209 | *** | * | RET,FLT3 | ||
| A10546 | Gandotinib | ** | **** | ** | ** | FLT3,FLT4,FGFR2 |
| A11193 | NVP-BSK805 2HCl | ** | **** | *** | *** | |
| A11329 | Baricitinib | *** | *** | ** | ||
| A10104 | AZ 960 | **** | ||||
| A12808 | CEP-33779 | **** | ||||
| A12694 | Pacritinib | * | ** | * | ** | FLT3 (D835Y),FLT3 |
| A14049 | WHI-P154 | * | EGFR,Src,VEGFR | |||
| A12394 | XL019 | * | **** | * | * | PDGFRβ,FLT3,c-Kit |
| A14955 | S-Ruxolitinib | *** | **** | * | ** | |
| A13509 | ZM 39923 HCl | * | * | TGM2,EGFR | ||
| A14012 | Decernotinib | *** | *** | **** | *** | |
| A14210 | Cerdulatinib | *** | *** | *** | **** | ARK5,MST1,Fms |
| A14232 | Filgotinib | *** | ** | * | * | |
| A15911 | FLLL32 | * | ||||
| A11241 | BMS-911543 | * | **** | ** | ** | |
| A14438 | Peficitinib | |||||
| A13162 | GLPG0634 analogue | |||||
| A12419 | Go6976 | FLT3,PKCα,PKCβ1 | ||||
| A10247 | Curcumol | |||||
| A11608 | WHI-P97 | |||||
| A13082 | PF-03394197 (oclacitinib) | *** | *** | ** | ** | |
| A13457 | Pyridone 6 (JAK Inhibitor I) | *** | **** | **** | ||
| A14132 | NSC 42834(JAK2 Inhibitor V, Z3) | |||||
| A14390 | INCB39110 (Itacitinib) | |||||
| A14405 | Solcitinib (GSK2586184) | |||||
| A15134 | JANEX-1 | * | ||||
| A15362 | Cercosporamide | *** | Mnk2, Mnk1 | |||
| A15365 | TCS 21311 | * | * | *** | * | |
| A15366 | ZM 449829 | **** | **** | STAT-5, EGFR, CDK4 | ||
| A15389 | NSC 33994 | |||||
| A16227 | ZM 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.
| 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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