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JAK/Stat

Items 1-50 of 1052

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  1. A12694
    Pacritinib (SB1518)

    JAK2/FLT3 inhibitor

    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.
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  2. A17252
    Tofacitinib

    JAK3/2/1 inhibitor

    Tofacitinib is an orally available JAK3/2/1 inhibitor with IC50s of 1, 20, and 112 nM, respectively.
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  3. A10426
    Genistin (Genistoside)
    Genistin is an isoflavone found in a number of dietary plants like soy and kudzu. It was shown to stimulate estrogen-dependent breast cancer cell growth in vivo.
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  4. A10817
    S3I-201 (NSC 74859)

    Stat3 Inhibitor

    S3I-201 (NSC 74859) is a novel inhibitor of Stat3 that inhibits Stat3, Stat3 complex formation and Stat3-DNA binding activity in vitro (IC50 = 86 ?? 33 μM) and Stat3-dependent transcriptional activities.
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  5. A10043
    AEE788

    EGFR inhibitor

    AEE788 is an orally bioavailable multiple-receptor tyrosine kinase inhibitor that inhibits phosphorylation of the tyrosine kinases of EGFR, HER2 and VEGF2.
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  6. A10263
    Momelotinib (Cyt387)

    JAK inhibitor

    CYT387 is an inhibitor of Janus kinases JAK1 and JAK2, acting as an ATP competitor with IC50 values of 11 and 18 nM, respectively.
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  7. A16640
    Oclacitinib maleate

    JAK inhibitor

    Oclacitinib maleate (PF-03394197 maleate) is a novel JAK inhibitor. Oclacitinib maleate (PF-03394197 maleate) is most potent at inhibiting JAK1 (IC50=10 nM).
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  8. A13203
    AZD1208

    pan-Pim kinase inhibitor

    AZD1208 is orally available, small molecule inhibitor of PIM kinases with potential antineoplastic activity.
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  9. A14390
    INCB39110 (Itacitinib)

    JAK1 Inhibitor

    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.
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  10. A10241
    CP-690550 (Tofacitinib citrate)

    JAK3 inhibitor

    CP-690550 (Tofacitinib citrate) is an orally available, highly selective inhibitor of the Janus kinase (JAK) family of enzymes.
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  11. A10211
    Canertinib (CI-1033)

    HER2/ErbB2 inhibitor

    Canertinib (CI-1033) is an irreversible tyrosine-kinase inhibitor with activity against EGFR (IC50 0.8 nM), HER-2 (IC50 19 nM) and ErbB-4 (IC50 7 nM).
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  12. A21658
    Momelotinib Mesylate

    JAK1/JAK2 inhibitor

    Momelotinib Mesylate (CYT387 Mesylate) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, appr 10-fold selectivity versus JAK3.
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  13. A11158
    ARRY334543 (Varlitinib)

    EGFR inhibitor

    ARRY334543 is a potent, orally active small molecule inhibitor of EGFR and ErbB-2.
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  14. A11416
    Erlotinib

    EGFR inhibitor

    Erlotinib is an epidermal growth factor receptor inhibitor (EGFR inhibitor). Erlotinib HCl was approved. Erlotinib binds in a reversible fashion to the adenosine triphosphate (ATP) binding site of the receptor. For the signal to be transmitted, two EGFR molecules need to come together to form a homodimer. These then use the molecule of ATP to trans-phosphorylate each other on tyrosine residues, which generates phosphotyrosine residues, recruiting the phosphotyrosine-binding proteins to EGFR to assemble protein complexes that transduce signal cascades to the nucleus or activate other cellular biochemical processes. When erlotinib binds to EGFR, formation of phosphotyrosine residues in EGFR is not possible and the signal cascades are not initiated.
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  15. A10422
    Gefitinib (Iressa)

    EGFR Inhibitor

    Gefitinib is an EGFR inhibitor, which interrupts signaling through the epidermal growth factor receptor (EGFR) in target cells.
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  16. A11329
    Baricitinib (LY3009104)

    JAK Inhibitor

    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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  17. A18014
    Afatinib

    EGFR inhibitor

    Afatinib (BIBW 2992) is an irreversible EGFR family inhibitor with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively.
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  18. A10396
    Fludarabine (Fludara)

    STAT inhibitor

    Fludarabine or fludarabine phosphate (Fludara) is a chemotherapy drug used in the treatment of hematological malignancies (cancers of blood cells such as leukemias and lymphomas) .Fludarabine inhibits DNA synthesis by interfering with ribonucleotide reductase and DNA polymerase. It is active against both dividing and resting cells.
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  19. A10838
    SGI-1776 (free base)

    PIM1 Inhibitor

    SGI-1776 free base is a novel ATP competitive inhibitor of Pim1 with IC50 of 7 nM in a cell-free assay, 50- and 10-fold selective versus Pim2 and Pim3, also potent to Flt3 and haspin. Phase 1.
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  20. A10110
    AZD1480

    JAK1/JAK2 Inhibitor

    AZD1480 is a novel potent small JAK2 inhibitor with an IC50 of 0.26 nM.
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  21. A13162
    Filgotinib (GLPG0634)

    JAK1 inhibitor

    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.
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  22. A11022
    AG-1478 (Tyrphostin AG-1478)

    EGFR Inhibitor

    AG-1478 (Tyrphostin AG-1478) is an inhibitor of EGFR kinase with an IC50 value of 3 nM.
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  23. A11028
    AV-412

    EGFR inhibitor

    AV-412 is an EGFR/HER2 inhibitor that binds to and inhibits the epidermal growth factor receptor (EGFR) and the human epidermal growth factor receptor 2 (HER2), which may result in the inhibition of tumor growth and angiogenesis.
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  24. A11945
    (Z)-SMI-4a

    Pim Inhibitor

    SIM-4a is a Pim kinase inhibitor that blocks mTORC1 activity via activation of AMPK. Mostly potent to Pim-2, does not significantly inhibit any other serine/threonine- or tyrosine-kinases.
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  25. A10638
    Neratinib (HKI-272)

    HER2 inhibitor

    Neratinib (HKI-272) is a tyrosine kinase inhibitor.
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  26. A12232
    STAT3-IN-1

    STAT3 inhibitor

    STAT3-IN-1 (compound 7d) is an excellent, selective and orally active STAT3 inhibitor, with IC50 values of 1.82 μM and 2.14 μM in HT29 and MDA-MB 231 cells, respectively. STAT3-IN-1 (compound 7d) induces tumor apoptosis.
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  27. A10047
    AG-490

    EGFR inhibitor

    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.
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  28. A11041
    INCB018424 (Ruxolitinib)

    JAK1/2 Inhibitor

    INCB018424 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;
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  29. A13681
    Osimertinib (AZD-9291)

    EGFR inhibitor

    Osimertinib (AZD-9291) is a third-generation EGFR inhibitor, showed promise in preclinical studies and provides hope for patients with advanced lung cancers that have become resistant to existing EGFR inhibitors.

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  30. A11752
    Lapatinib (free base)

    Lapatinib is a dual tyrosine kinase inhibitor which interrupts the HER2 growth receptor pathway. Lapatinib is a potent EGFR and ErbB2 inhibitor with IC50 of 10.8 and 9.2 nM in cell-free assays, respectively. Lapatinib induces ferroptosis and autophagic cell death.

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  31. A10315
    Diosgenin

    Pdia3/ERp57 activator, STAT3 inhibitor

    Diosgenin is a steroid sapogenin and the precursor for the semisynthesis of progesterone which in turn was used in early combined oral contraceptive pills.It is the product of hydrolysis by acids, strong bases, or enzymes of saponins, extracted from the tubers of Dioscorea wild yam, such as the Kokoro.
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  32. A14420
    LGB-321 HCl

    Pan-PIM kinase inhibitor

    LGB-321 HCl is a potent and selective ATP-competitive small molecule inhibitor of PIM kinases (Pan-PIM kinase inhibitor).
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  33. A10104
    AZ-960

    JAK2 inhibitor

    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.
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  34. A10706
    Pelitinib (EKB-569)

    EGFR inhibitor

    Pelitinib (EKB-569) is a 3-cyanoquinoline pan-ErbB tyrosine kinase inhibitor with potential antineoplastic activity.
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  35. A11795
    WP1066

    JAK2 Inhibitor

    WP1066 is a novel JAK2 inhibitor and it suppresses proliferation and induces apoptosis in eythroid human cells carrying the JAK2 V617F mutation.
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  36. A12733
    Stattic

    STAT3 inhibitor

    Stattic is a small molecule shown to selectively inhibit the activation of the Stat3 transcription factor by blocking phosphorylation and dimerization events.
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  37. A10005
    (-)-Epigallocatechin gallate

    Antioxidant, antiangiogenic, antitumor agent

    (-)-Epigallocatechin gallate is a potent anti-oxidant polyphenol flavonoid isolated from green tea.
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  38. A10141
    (E/Z)-BIBW2992 (E/Z-Afatinib)

    EGFR inhibitor

    BIBW2992 (Afatinib) is tyrosine kinase inhibitor (TKI) that irreversibly inhibits human epidermal growth factor receptor 2 (Her2) and epidermal growth factor receptor (EGFR) kinases.
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  39. A13082
    PF-03394197 (oclacitinib)

    JAK1 inhibitor

    PF-03394197 (oclacitinib) is a potent JAK1 inhibitor
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  40. A10116
    AZD8931 (Sapitinib)

    pan-EGFR/pan-erbB inhibitor

    AZD8931 is an oral, equipotent inhibitor of ErbB1, ErbB2 and ErbB3 receptor signaling.
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  41. A10095
    AT9283

    Aurora/JAK inhibitor

    AT9283 inhibits aurora kinase A and B and targets other tyrosine and serine/threonine kinases associated with myeloid cell proliferation.
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  42. A15955
    DM1-SMCC

    potent EGFR inhibitor

    DM1-SMCC is DM1 with a reactive linker SMCC, which can react with antibody to make antibody drug conjugate.
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  43. A13457
    Pyridone 6 (JAK Inhibitor I)

    JAK inhibitor

    JAK Inhibitor I is a potent, reversible, cell-permeable, and ATP-competitive inhibitor of JAK1, JAK2, and JAK3.
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  44. A11558
    SU-5402

    VEGFR/FGFR/EGFR inhibitor?€?

    SU-5402 is a potent and selective vascular endothelial growth factor receptor (VEGFR) and fibroblast growth factor receptor (FGFR) inhibitor (IC50 values are 0.02, 0.03, 0.51 and > 100 μM at VEGFR2, FGFR1, PDGFRβ and EGFR respectively).
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  45. A10242
    CP-724714

    HER2/ErbB2 inhibitor

    CP-724714 is an orally available, small molecule, potent HER-2 tyrosine kinase inhibitor that inhibits HER2 kinase (IC50 3.8 ng/ml) .
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  46. A11051
    Dacomitinib (PF299804, PF299)

    EGFR inhibitor

    Dacomitinib (PF299804, PF299) is a potent, orally available, irreversible inhibitor of tyrosine kinase human epidermal growth factor receptors (HER) 1 (EGFR), HER2, and HER4.

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  47. A13044
    Poziotinib

    EGFR inhibitor

    Poziotinib is an orally bioavailable, quinazoline-based pan epidermal growth factor receptor (EGFR or HER) inhibitor with potential antineoplastic activity.
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  48. A10362
    Erlotinib HCl

    EGFR inhibitor

    Erlotinib hydrochloride is a reversible tyrosine kinase inhibitor, which acts on the epidermal growth factor receptor (EGFR).
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  49. A10678
    OSI-420

    EGFR Inhibitor

    OSI-420 (Desmethyl Erlotinib,CP-473420) is an orally active EGFR tyrosin kinase inhibitor, which inhibits receptor tyrosine kinases (TKs) by inhibition of the intercellular domain .
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  50. A10053
    Tyrphostin AG 879

    HER2 inhibitor

    Tyrphostin AG 879 is an inhibitor of the tyrosine kinase activity of nerve growth factor (NGF) TrkA.
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Items 1-50 of 1052

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  1. Inhibitor 931items
  2. Antagonist 1item
  3. Activator 1item
Target
  1. HDAC 1item
  2. HDAC1 1item
  3. HDAC2 1item
  4. HDAC3 1item
  5. HDAC4 1item
  6. HDAC5 1item
  7. HDAC6 1item
  8. HDAC7 1item
  9. HDAC8 1item
  10. HDAC9 1item
  11. HDAC10 1item
  12. EGFR/ErbB1/HER1 15items
  13. ErbB2/HER2 7items
  14. ErbB4/HER4 1item
  15. JAK 3items
  16. JAK1 48items
  17. JAK2 60items
  18. JAK3 54items
  19. Tyk2 39items
  20. STAT3 5items
  21. STAT5 1item
  22. IKKβ 1item
  23. SYK 3items
  24. CDK2 2items
  25. FLT3 3items
  26. ERK2 1item