DC7137 |
Filgotinib(GLPG0634)
Featured
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Filgotinib (GLPG0634) is a selective, orally available JAK1 inhibitor with anti-inflammatory and antiviral activities. Filgotinib can effectively inhibit the activities of JAK1, JAK2, JAK3 and TYK2 with IC50 values of 10 nM, 28 nM, 810 nM and 116 nM, respectively. Filgotinib also inhibits HIV-1 driven gene transcription and reduces proliferation of HIV-1 infected cells. Filgotinib can be used in the study of rheumatoid arthritis and inflammatory bowel disease. |
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DC10171 |
Hispidulin
Featured
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Hispidulin is a natural flavone with a broad spectrum of biological activities. Hispidulin is a Pim-1 inhibitor with an IC50 of 2.71 μM. |
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DC10626 |
HJC0152 |
HJC0152 is a signal transducer and activator of transcription 3 (STAT3) inhibitor with remarkably improved aqueous solubility. |
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DC10918 |
INCB053914 |
INCB053914 (INCB-053914) is a novel potent, and selective ATP-competitive, pan-PIM kinase inhibitor with IC50 of 0.24/30.0/0.12 nM for PIM1/2/3, respectively. |
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DC10555 |
inS3-54A18
Featured
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inS3-54A18 is a potent STAT3 inhibitor, with anti-cancer properties. |
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DC12378 |
Itacitinib(INCB039110)
Featured
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Itacitinib is a potent and selective inhibitor of JAK1, with >20-fold selectivity for JAK1 over JAK2 and >100-fold over JAK3 and TYK2; Itacitinib is used in the research of myelofibrosis. |
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DC11136 |
JAK2 inhibitor G5-7
Featured
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JAK2 inhibitor G5-7 is a small molecule, allosteric JAK2 inhibitor that selectively inhibits JAK2-mediated phosphorylation and activation of EGFR and STAT3 by binding to JAK2. |
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DC8077 |
WHI-P131(Janex 1)
Featured
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Janex 1 selectively inhibits the tyrosine kinase activity of JAK3 with an IC50 value of 78 µM without affecting the enzymatic activity of JAK1, JAK2, or other protein tyrosine kinases (IC50 ≥350 µM). |
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DC7665 |
Gandotinib(LY2784544)
Featured
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LY2784544 is a potent JAK2 inhibitor with IC50 of 3 nM, effective in JAK2V617F, 8- and 20-fold selective versus JAK1 and JAK3. Phase 2. |
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DC7195 |
JAK Inhibitor I(Merck 5, Pyridone 6)
Featured
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Merck 5 is a potent and reversible ATP-competitive inhibitor of the JAK kinases (JAK1, JAK2, JAK3, and Tyk2). It also blocks IL2 and IL4 dependent proliferation of CTLL cells and inhibits the phosphorylation of STAT5. |
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DC8474 |
Napabucasin (BBI608)
Featured
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Napabucasin (BBI608) is an orally-administered small molecule which can block cancer stem cell (CSC) self-renewal and induces cell death in CSCs as well as non-stem cancer cells. |
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DC10748 |
NSC31205
Featured
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NSC 31205 is a PIM2/1 inhibitor. |
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DC7216 |
NVP-BSK805 dihydrochloride
Featured
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NVP-BSK805 is a potent and selective ATP-competitive JAK2 inhibitor with IC50 of 0.5 nM; >20-fold selectivity towards JAK1, JAK3 and TYK2. |
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DC7478 |
Pacritinib |
Pacritinib (SB1518) is a potent and selective JAK2 (IC50 = 23 and 19 nM for JAK2WT and JAK2V617F, respectively) and FLT3 (IC(50) = 22 nM) inhibitor with selectivity against JAK1 and JAK3 (IC50= 1280 and 520 nM, respectively). |
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DC8168 |
Peficitinib(ASP015K,JNJ-54781532)
Featured
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Peficitinib(ASP015K,JNJ-54781532) is a novel potent JAK inhibitor, which demonstrated potent efficacy in adjuvant-induced arthritis model in rats. |
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DC11734 |
PF-06263276 |
PF-06263276 (PF06263276, PF 6263276) is a potent, selective pan JAK inhibitor with IC50 of 2.2, 23.1, 59.9 and 29.7 nM for JAK1, JAK2, JAK3, and TYK2, respectively. |
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DC10779 |
PF-06651600
Featured
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PF-06651600 is a potent JAK3-selective inhibitor with an IC50 of 33.1 nM. |
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DC12489 |
PF-06700841 free base
Featured
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PF-06700841 is an inhibitor of JAK1 and TYK2 kinases. PF-06700841 has been investigated for the treatment of psoriasis and lupus. |
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DC12488 |
PF-06700841 tosylate
Featured
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PF-06700841 is an inhibitor of JAK1 and TYK2 kinases. PF-06700841 has been investigated for the treatment of psoriasis and lupus. |
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DC9593 |
Pim1/AKK1-IN-1
Featured
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PIM/AKK1-IN-1 is a potent multi-kinase inhibitor with Kd values of 35 nM/53 nM/75 nM/380 nM for Pim1/AKK1/MST2/LKB1 respectively; also inhibits MPSK1 and TNIK. |
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DC10047 |
PIM-447 dihydrochloride
Featured
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PIM447 is novel pan-PIM kinase inhibitor, including Moloney Murine Leukemia (PIM) 1, 2, and 3 Kinase. |
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DC7236 |
Pimobendan
Featured
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Pimobendan is a selective inhibitor of PDE3 with IC50 of 0.32 μM. |
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DC9691 |
Piperlongumine
Featured
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Piperlongumine induces cell death and increases the level of reactive oxygen species (ROS) in cancer cells with both wild-type and normal p53. |
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DC8604 |
Pim-1 Inhibitor 2 |
PIM1-IN-2 is a highly effective and ATP-competitive inhibitor of Pim-1, demonstrating a Ki value of 91 nM. Unlike traditional inhibitors, it interacts with the ATP-binding kinase hinge region without relying on the formation of standard hydrogen bonds, showcasing a unique mechanism of action. This distinctive approach highlights its potential as a promising therapeutic agent. |
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DC4230 |
Ruxolitinib (INCB018424)
Featured
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Ruxolitinib is a potent ATP mimetic that inhibits both JAK1 and JAK2 with IC50 values of 2.7 and 4.5 nM, respectively and is relatively less selective for JAK3 (IC50 = 322 nM). |
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DC8309 |
Ruxolitinib Phosphate
Featured
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Ruxolitinib Phosphate is a potent and selective Janus kinase (JAK1, IC50 = 5.9 nM and JAK2, IC50 = 5.7 nM) inhibitor. |
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DC10823 |
SAR-20347
Featured
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SAR-20347 is an inhibitor of TYK2, JAK1, JAK2 and JAK3 with IC50s of 0.6, 23, 26 and 41 nM, respectively. |
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DC7160 |
SGI-1776
Featured
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SGI-1776 is a novel ATP competitive inhibitor of Pim1 with IC50 of 7 nM; 50- and 10-fold selective versus Pim2 and Pim3, also potent to Flt3 and haspin. |
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DC7983 |
SH-4-54
Featured
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SH-4-54 is a potent STAT inhibitor with KD of 300 nM and 464 nM for STAT3 and STAT5, respectively. |
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DC10105 |
SH5-07
Featured
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SH5-07 is a hydroxamic acid based Stat3 inhibitor with an IC50 of 3.9±0.6 μM in in vitro assay. |
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