JAK/Stat

Items 651-700 of 1052

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  1. JAK inhibitor

    JAK-IN-4 is a prodrug of a JAK inhibitor, effective in murine collagen induced arthritis model.
  2. Tyk2 inhibitor

    Tyk2-IN-5 (compound 6) is a highly potent, selective and orally active Tyk2 inhibitor and targets the JH2 domain, with a Ki of 0.086 nM for Tyk2 JH2 and an IC50 of 25 nM for IFNα.
  3. KAT3B inhibitor

    L002 is a novel potent, specific acetyltransferase p300 (KAT3B) inhibitor with an IC50 of 1.98 uM.
  4. Stat3 inhibitor

    SH5-07 is a hydroxamic acid based Stat3 inhibitor with an IC50 of 3.9 μM in in vitro assay.
  5. Stat3 inhibitor

    BP-1-102 is an orally available, small-molecule inhibitor of transcription factor Stat3, with an IC50 of 6.8 μM.
  6. TYK2/JAK1/JAK2/JAK3 inhibitor

    SAR-20347 is an inhibitor of TYK2, JAK1, JAK2 and JAK3 with IC50s of 0.6, 23, 26 and 41 nM, respectively.
  7. tyrosine kinase inhibitor

    RG13022 is a tyrosine kinase inhibitor; inhibits the autophosphorylation reaction of the EGF receptor with an IC50 of 4 μM.
  8. EGFR inhibitor

    EGFR-IN-7 (compound 34) is a selective and potent EGFR kinase inhibitor extracted from patent WO2019015655A1, has IC50s of 7.92 nM and 0.218 nM for EGFR (WT) and EGFR (mutant C797S/T790M/L858R) respectively, and shows anti-tumor activity.
  9. EGFR inhibitor

    Mutated EGFR-IN-2 (compound 91) is a mutant-selective EGFR inhibitor extracted from patent WO2017036263A1, which potently inhibits single-mutant EGFR (T790M) and double-mutant EGFR (including L858R/T790M (IC50=??1nM) and ex19del/T790M), and can suppress activity of single gain-of-function mutant EGFR (including L858R and ex19del) as well. Mutated EGFR-IN-2 shows anti-tumor antivity.
  10. TYK2 Inhibitor

    BMS-986165 is a Highly Potent and Selective Allosteric Inhibitor of TYK2. BMS-986165 Blocks Il-12, IL-23 and type I Interferon Signaling and Provides for Robust Efficacy in Preclinical Models of Inflammatory Bowel Disease.
  11. JAK1 inhibitor

    JAK1-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).
  12. EGFR inhibitor

    DBPR112 is an orally active Furanopyrimidine-Based Epidermal Growth Factor Receptor inhibitor with IC50s of 15 nM and 48 nM for EGFRWT and EGFRL858R/T790M, respectively.
  13. JAK3 covalent inhibitor

    JAK3 covalent inhibitor-1 is a potent and selective janus kinase 3 (JAK3) covalent inhibitor with an IC50 of 11 nM and shows 246-fold selectivity vs other JAKs.
  14. JAK2/STAT3 inhibitor

    Protosappanin A is an immunosuppressive ingredient of the medicinal herb Caesalpinia sappan L.
  15. JAK1 inhibitor

    JAK1-IN-7 is a Janus-associated kinase 1 (JAK1) inhibitor extracted from patent WO2018134213A1, Example 63, has an anti-inflammatory effect.
  16. TYK2 inhibitor

    Ropsacitinib (PF-06826647) is a selective TYK2 inhibitor, which binds to TYK2 catalytically active JH1 domain with an IC50 of 17 nM, used in the treatment of psoriasis.

  17. RTC-5 is an optimized phenothiazine with anti-cancer potency. RTC-5 demonstrates efficacy against a xenograft model of an EGFR driven cancer, its effects is attributed to concomitant negative regulation of PI3K-AKT and RAS-ERK signaling.
  18. JAK1 inhibitor

    AZ-3 is a potent and selective JAK1 inhibitor with an IC50 of 34 nM.
  19. JAK inhibitor

    Delgocitinib 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.
  20. Pim kinase inhibitor

    GNE-955 is a potent and orally active pan Pim kinase inhibitor with Kis of 0.018, 0.11, 0.08 nM for Pim1, Pim2, Pim3, respectively.
  21. JAK1 inhibitor

    JAK1-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).
  22. TYK2 inhibitor

    TyK2-IN-2 (Compoud 18) is a potent and selective TYK2 inhibitor with IC50s of 7 nM, 0.1 μM and 0.05 μM for TYK2 JH2, IL-23 and IFNα, respectively.
  23. HER2 inhibitor

    TAS0728 is a potent, selective, oral active, irreversible and covalent-binding HER2 inhibitor, binds to HER2 at C805, inhibits its kinase activity, with an IC50 of 13 nM.
  24. PIM1/3 inhibitor

    PIM1-IN-1 is a potent and highly selective PIM1/3 inhibitor, with IC50s of 7, 5530 and 70 nM for PIM1, PIM2, and PIM3, respectively, inhibits the phosphorylation of BAD, a downstream target of PIM, with an EC50 of 262 nM.
  25. SDZ281-977 is an antiproliferative agent. It acts by binding to the ??colchicine binding site?? on tubulin and inhibiting tubulin polymerization in vitro.
  26. EGFR/HER2 dual inhibitor

    Pyrotinib (SHR-1258) is a potent and selective EGFR/HER2 dual inhibitor with IC50s of 13 and 38 nM, respectively.
  27. STAT inhibitor

    Nitidine chloride, a natural benzophenanthridine alkaloid, has been shown to inhibit cancer growth via induction of cell apoptosis and suppression of cancer angiogenesis.
  28. Epidermal Growth Factor Receptor Peptide (985-996) exists on the cell surface and is activated by the binding of its specific ligands, including epidermal growth factor and transforming growth factor.
  29. EGFR inhibitor

    Compound 56 is a cell-permeable, reversible, and ATP-competitive inhibitor of tyrosine kinase activity of EGFR.
  30. JAK inhibitor

    S-Ruxolitinib is the chirality of INCB018424, is a potent and selective small-molecule Janus kinase 1 (JAK1) and JAK2 inhibitor.
  31. EGFR inhibitor

    Afatinib is an irreversible EGFR/HER2 inhibitor with an IC50 of 14 nM for in vitro potency against HER2.
  32. JAK inhibitor

    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.
  33. Pim Inhibitor

    CX-6258 hydrochloride hydrate is a potent, orally efficacious Pim 1/2/3 kinase(IC50=5 nM/25 nM/16 nM) inhibitor with excellent biochemical potency and kinase selectivity.
  34. JAK inhibitor

    CYT387 sulfate salt is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, ~10-fold selectivity versus JAK3.
  35. EGFR inhibitor

    Erlotinib mesylate is a directly acting inhibitor of human EGFR tyrosine kinase with an IC50 of 2 nM.
  36. EGFR Inhibitor

    Gefitinib hydrochloride is an EGFR inhibitor, which interrupts signaling through the epidermal growth factor receptor (EGFR) in target cells. Therefore, it is only effective in cancers with mutated and overactive EGFR.
  37. JAK3 inhibitor

    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.
  38. VEGFR/EGFR inhibitor

    Vandetanib is a potent inhibitor of VEGFR2 with IC50 of 40 nM.
  39. JAK2 inhibitor

    1,2,3,4,5,6-Hexabromocyclohexane is a potent and specific inhibitor of JAK2 autophosphorylation.
  40. Mnk2/JAK3 inhibitor

    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).
  41. JAK2/STAT3 inhibitor

    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.
  42. JAK2/STAT3 inhibitor

    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.
  43. JAK3 inhibitor

    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).
  44. JAK3 inhibitor

    JAK3 Inhibitor V is a potent, selective inhibitor of JAK3 (Janus tyrosine kinase 3) which binds competitively to the JAK3 ATP site.
  45. PIM-1 Inhibitor

    PIM-1 inhibitor 2 is a potent Pim-1 kinase inhibitor (Ki = 91 nM).
  46. Pim-1 Kinase Inhibitor

    TCS PIM-1 1 is a potent and selective ATP-competitive Pim-1 kianse inhibitor with IC50 of 50 nM, displays good selectivity over Pim-2 and MEK1/MEK2(IC50s >20,000 nM).
  47. JAK2 inhibitor

    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.
  48. HER2 inhibitor

    D-69491 (SU11464) is a small-molecule HER2 inhibitor, which was under development for the treatment of tumours with high expression of HER2, such as breast, ovarian, lung and pancreatic carcinomas.
  49. EGFR inhibitor

    AV-412 (MP412) is an EGFR inhibitor with IC50s of 0.75, 0.5, 0.79, 2.3, 19 nM for EGFR, EGFRL858R, EGFRT790M, EGFRL858R/T790M and ErbB2, respectively.
  50. EGFR/Cdk2 inhibitor

    WHI-P180 is a potent EGFR and Cdk2 inhibitors with IC50 of 4.0 and 1.0 uM, respectively.

Items 651-700 of 1052

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