JAK
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.
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NS-018
Catalog No. A16224 JAK2 inhibitorNS-018 is an orally bioavailable, small molecule inhibitor of Janus-associated kinase 2 (JAK2) and Src-family kinases, with potential antineoplastic activity. Learn More -
ZM 39923 HCl
Catalog No. A13509 JAK3 inhibitorZM 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) Learn More -
S-Ruxolitinib
Catalog No. A14955 JAK inhibitorS-Ruxolitinib is the chirality of INCB018424, is a potent and selective small-molecule Janus kinase 1 (JAK1) and JAK2 inhibitor. Learn More -
CYT387 sulfate salt
Catalog No. A15056 JAK inhibitorCYT387 sulfate salt is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, ~10-fold selectivity versus JAK3. Learn More -
JANEX-1
Catalog No. A15134 JAK3 inhibitorJanex-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. Learn More -
1,2,3,4,5,6-Hexabromocyclohexane
Catalog No. A15361 JAK2 inhibitor1,2,3,4,5,6-Hexabromocyclohexane is a potent and specific inhibitor of JAK2 autophosphorylation. Learn More -
Cercosporamide
Catalog No. A15362 Mnk2/JAK3 inhibitorCercosporamide, 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). Learn More -
Cucurbitacin I
Catalog No. A15363 JAK2/STAT3 inhibitorCucurbitacin 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. Learn More -
SD 1008
Catalog No. A15364 JAK2/STAT3 inhibitorSD 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. Learn More -
TCS 21311
Catalog No. A15365 JAK3 inhibitorTCS 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). Learn More -
ZM 449829
Catalog No. A15366 JAK/STAT inhibitorJAK3 Inhibitor V is a potent, selective inhibitor of JAK3 (Janus tyrosine kinase 3) which binds competitively to the JAK3 ATP site. Learn More -
NSC 33994
Catalog No. A15389 JAK2 inhibitorNSC 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. Learn More -
Peficitinib (ASP015K, JNJ-54781532)
Catalog No. A14438 JAK inhibitorPeficitinib is a novel potent JAK inhibitor, which demonstrated potent efficacy in adjuvant-induced arthritis model in rats. Learn More -
INCB018424 (Ruxolitinib)
Catalog No. A11041 JAK1/2 InhibitorINCB018424 is a potent and selective inhibitor of Janus-associated kinase (JAK) 1 and 2, with IC50 to be 2.7, 4.5 and 332 nM for JAK1, JAK2 and JAK3 respectively; Learn More -
WHI-P97
Catalog No. A11608 -
FLLL32
Catalog No. A15911 -
NS-018 hydrochloride
Catalog No. A16225 JAK2 inhibitorNS-018 hydrochloride is a novel highly selective JAK2 inhibitor. Learn More -
NS-018 maleate
Catalog No. A16226 JAK2 inhibitorNS-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. Learn More -
ZM39923
Catalog No. A16227 JAK1/3 inhibitorZM39923 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. Learn More -
AZ-3
Catalog No. A19217 JAK1 inhibitorAZ-3 is a potent and selective JAK1 inhibitor with an IC50 of 34 nM. Learn More -
Delgocitinib
Catalog No. A19234 JAK inhibitorDelgocitinib is a novel and specific JAK inhibitor with IC50s of 2.8, 2.6, 13 and 58 nM for JAK1, JAK2, JAK3 and Tyk2, respectively. Learn More -
JAK1-IN-3
Catalog No. A19251 JAK1 inhibitorJAK1-IN-3 is a selective JAK1 inhibitor, with an IC50 of 73 nM, weakly inhibits JAK2, and shows little inhibition on JAK3 (IC50, >14.7, >30 μM, respectively). Learn More -
JAK-IN-5
Catalog No. A19792 JAK inhibitorJAK-IN-5 is an inhibitor of JAK extracted from patent US20170121327A1, compound example 283. Learn More -
Gusacitinib
Catalog No. A19883 SYK/JAK inhibitorGusacitinib (ASN-002) is a potent dual inhibitor of spleen tyrosine kinase (SYK) and janus kinase (JAK) with IC50 values of 5-46 nM. Learn More -
JAK-IN-3
Catalog No. A20220 JAK inhibitorJAK-IN-3 (compound 22) is a potent JAK inhibitor, with IC50 values of 3 nM, 5 nM, 34 nM and 70 nM for JAK3, JAK1, TYK2 and JAK2, respectively. Learn More -
JAK-IN-4
Catalog No. A20230 JAK inhibitorJAK-IN-4 is a prodrug of a JAK inhibitor, effective in murine collagen induced arthritis model. Learn More -
SAR-20347
Catalog No. A20380 TYK2/JAK1/JAK2/JAK3 inhibitorSAR-20347 is an inhibitor of TYK2, JAK1, JAK2 and JAK3 with IC50s of 0.6, 23, 26 and 41 nM, respectively. Learn More -
JAK3-IN-1
Catalog No. A20734 JAK3 inhibitorJAK3-IN-1 is a potent JAK3 inhibitor with IC50 of 4.8 nM, also inhibits JAK1 (IC50 = 896 nM) and JAK2 (IC50 = 1050 nM). Learn More -
TG-89
Catalog No. A22361 -
BD750
Catalog No. A22300 JAK3/STAT5 inhibitorBD750, an effective immunosuppressant and a JAK3/STAT5 inhibitor, inhibits IL-2-induced JAK3/STAT5-dependent T cell proliferation, with IC50 values of 1.5 μM and 1.1 μM in mouse and human T cells, respectively. Learn More -
Solcitinib (GSK2586184)
Catalog No. A14405 -
Pacritinib (SB1518)
Catalog No. A12694 JAK2/FLT3 inhibitorPacritinib, 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. Learn More -
Curcumol
Catalog No. A10247 JAK2 inhibitorCurcumol induces apoptosis via caspases-independent mitochondrial pathway in human lung adenocarcinoma ASTC-a-1 cells. Learn More -
Cyt387 (Momelotinib)
Catalog No. A10263 JAK inhibitorCYT387 is an inhibitor of Janus kinases JAK1 and JAK2, acting as an ATP competitor with IC50 values of 11 and 18 nM, respectively. Learn More -
CP-690550 (Tofacitinib citrate)
Catalog No. A10241 JAK3 inhibitorCP-690550 (Tofacitinib citrate) is an orally available, highly selective inhibitor of the Janus kinase (JAK) family of enzymes. Learn More -
PF-03394197 (oclacitinib)
Catalog No. A13082 JAK1 inhibitorPF-03394197 (oclacitinib) is a potent JAK1 inhibitor Learn More -
GLPG0634
Catalog No. A13162 JAK1 inhibitorGLPG0634 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. Learn More -
AG-490
Catalog No. A10047 EGFR inhibitorAG 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. Learn More -
PRT 062070 (Cerdulatinib)
Catalog No. A14147 Dual Syk and JAK inhibitorPRT062070 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. Learn More -
NSC 42834(JAK2 Inhibitor V, Z3)
Catalog No. A14132 -
AT9283
Catalog No. A10095 Aurora/JAK inhibitorAT9283 inhibits aurora kinase A and B and targets other tyrosine and serine/threonine kinases associated with myeloid cell proliferation. Learn More -
Decernotinib
Catalog No. A14012 JAK3 inhibitorDecernotinib is an oral, selective Janus kinase 3 (JAK3) inhibitor being developed by Vertex. Learn More -
Filgotinib
Catalog No. A14232 JAK inhibitorFilgotinib is a selective JAK1 inhibitor with IC50 of 10 nM, 28 nM, 810 nM, and 116 nM for JAK1, JAK2, JAK3, and TYK2, respectively. Learn More -
INCB39110 (Itacitinib)
Catalog No. A14390 JAK1 InhibitorINCB39110 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. Learn More -
AZD1480
Catalog No. A10110 JAK InhibitorAZD1480 is a novel potent small JAK2 inhibitor with an IC50 of 0.26 nM. Learn More -
Tofacitinib
Catalog No. A17252 JAK3/2/1 inhibitorTofacitinib is an orally available JAK3/2/1 inhibitor with IC50s of 1, 20, and 112 nM, respectively. Learn More -
JAK1-IN-4
Catalog No. A18821 JAK1 inhibitorJAK1-IN-4 is a potent and selective JAK1 inhibitor, with IC50s of 85 nM, 12.8 μM and >30 μM for JAK1, JAK2, and JAK3, respectively. JAK1-IN-4 inhibits STAT3 phosphorylation in NCI-H 1975 cells (IC50, 227 nM). Learn More -
PF-06263276
Catalog No. A12572 pan-JAK inhibitorPF-06263276 (PF 6263276) is a potent and selective pan-JAK inhibitor, with IC50s of 2.2 nM, 23.1 nM, 59.9 nM and 29.7 nM for JAK1, JAK2, JAK3 and TYK2, respectively. Learn More -
Ruxolitinib sulfate
Catalog No. A11467 JAK1/2 inhibitorRuxolitinib sulfate (INCB018424 sulfate) is the first potent, selective JAK1/2 inhibitor to enter the clinic with IC50s of 3.3 nM/2.8 nM, and has > 130-fold selectivity for JAK1/2 versus JAK3. Learn More -
JAK2-IN-4
Catalog No. A12182 JAK2/JAK3 inhibitorJAK2-IN-4 (compound 16h) is a selective JAK2/JAK3 inhibitor, with IC50 values of 0.7 nM and 23.2 nM for JAK2 and JAK3, respectively. Learn More