|Description||A cell-permeable, reversible, potent, ATP-competitive, and specific inhibitor of JAK3 (Janus family kinase 3; IC50 = 78 µM). Has no effect on JAK1, JAK2, or Zap/Syk or Src tyrosine kinases. Acts as a potent inhibitor of glioblastoma cell adhesion and migration. Also reported to block thrombin-induced platelet aggregation.|
|Synonyms||WHI-P131; Janex 1; WHI-P 131|
Filgotinib, also known as GLPG0634, is a potent and selective JAK1 inhibitor. Filgotinib displayed a selectivity of 30-fold for JAK1- over JAK2-dependent signal...
TYK2-IN-2 is an inhibitor of TYK2 with potential for the treatment of inflammatory and autoimmune diseases.
JAK2 Inhibitor IV
JAK2 Inhibitor IV is a potent and selective Janus Kinase 2 (JAK2) inhibitor that inhibits the activity of both the wild-type JAK2 and the V617F mutant (IC50 = 7...
WHI-P154 is a JAK3 inhibitor with IC50 = 1.8 μM. WHI-P154 displays no activity at JAK1 or JAK2. WHI-P154 also Inhibits STAT1 activation, iNOS expression and N...
TCS 21311 is a potent JAK3 inhibitor (IC50 = 8 nM) with selectivity for JAK3 over JAK1, JAK2 and TYK2 (IC50 = 1017, 2550 and 8055 nM, respectively). It also inh...
Tofacitinib (CP-690550,Tasocitinib) is a novel inhibitor of JAK3 with IC50 of 1 nM, 20- to 100-fold less potent against JAK2 and JAK1.It is currently approved f...
AC410 is a Janus kinase 2 (JAK2) inhibitor with Kd of 0.18 nM. AC410 is selective for JAK2 and Kd is 2.5 nM for JAK1 and 5nM for JAK3. Phase I for the treatment...
NSC-33994 is a selective inhibitor of JAK2 with IC50 of 60 nM.
ZM 449829 is a potent and selective inhibitor of Janus tyrosine kinase 3 (JAK3) which binds competitively to the JAK3 ATP site (pIC50 = 6.8, 5.0, 4.7, and < 5.0...
ZM 39923 hydrochloride
ZM 39923 hydrochloride is a potent and selective inhibitor of Janus tyrosine kinase 3 (JAK3) (pIC50 = 7.1, 5.6, 4.4, and < 5.0 for JAK3, EGFR, JAK1 and CDK4, re...
Gandotinib is a potent and selective JAK inhibitor, which effectively inhibited JAK2V617F-driven signaling and cell proliferation in Ba/F3 cells (IC50=20 and 55...
Ruxolitinib sulfate (INCB018424) is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM, >130-fold selectivity for JAK1...
SD 1008 is a JAK2/STAT3 signaling pathway inhibitor that inhibits activation of STAT3, JAK2 and Src. SD 1008 induces apoptosis in cell lines expressing constitu...
SAR-20347 is a small molecule inhibitor of TYK2, JAK1, JAK2 and JAK3 with IC50s of 0.6, 23, 26 and 41 nM, respectively. SAR-20347 dose dependently (1 nM-10 μM) ...
Itacitinib is a potent Janus kinase-1 inhibitor under the development of AstraZeneca and Incyte Corporation. Itacitinib can inhibit OCT2-mediated uptake of crea...
BMS-911543 is an orally available small molecule targeting a subset of Janus-associated kinase (JAK) with potential antineoplastic activity. JAK2 inhibitor BMS-...
Peficitinib, also known as ASP015K and JNJ-54781532, is a novel potent JAK inhibitor, which demonstrated potent efficacy in adjuvant-induced arthritis model in ...
SB1317 is a novel small molecule potent CDK/JAK2/FLT3 inhibitor. It dose-dependently inhibits signaling pathways downstream of CDKs, JAK2 and FLT3 in cancer cel...
CEP-33779 is a highly selective, orally active, small-molecule inhibitor of JAK2. CEP-33779 induced regression of established colorectal tumors, reduced angioge...