MAPK

Items 151-200 of 239

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Catalog No.
Product Name
Application
Product Information
Product Citation
  1. AP-1 transcription inhibitor

    PNRI-299 is a selective AP-1 transcription inhibitor with IC50 of 20 uM without affecting NF-kappaB transcription (up to 200 μM) or thioredoxin (up to 200 μM).
  2. MLKL inhibitor

    Necrosulfonamide is a pharmacological inhibitor of MLKL with IC50 values of 124 nM in human HT-29.
  3. SMYD3/ MEKK2 inhibitor

    EPZ031686 is a noncompetitive inhibitor for SMYD3 and MEKK2 with a Ki=1.2 and 1.1 nM respectively.
  4. pan RAF inhibitor

    LY3009120 is a pan RAF inhibitor which inhibits BRAFV600E, BRAFWT and CRAFWT with IC50s of 5.8, 9.1 and 15 nM, respectively.
  5. ERK1/2 inhibitor

    CC-90003 is an irreversible inhibitor of ERK1/2 with IC50s in the 10-20 nM range and shows good kinase selectivity in a 258-kinase biochemical assay.
  6. ERK inhibitor

    MK-8353 (SCH900353) is an orally bioavailable, selective, and potent ERK inhibitor that inhibits activated ERK1 and ERK2 in vitro, with IC50 values of 23.0 nM and 8.8 nM, respectively (IMAP kinase assay), and nonactivated ERK2, with an IC50 of 0.5 nM (MEK1-ERK2-coupled assay).
  7. ERK inhibitor

    AZD0364 is a pre-clinical ERK1/2 inhibitor with an IC50 of 0.6 nM for ERK2.
  8. BRAF inhibitor

    PLX8394 is a next-generation, orally available, small-molecule BRAF inhibitor with IC50 values of 3.8 nM, 14 nM and 23 nM for BRAF(V600E), WT BRAF and CRAF respectively. It has potential antineoplastic activity.
  9. pan-RAF inhibitor

    LXH254 is a type II ATP-competitive inhibitor that inhibits both B- and CRAF kinase activities at picomolar concentrations with a high degree of selectivity against a panel of 456 human kinases and in cell-based assays.
  10. raf kinase inhibitor

    RAF709 is a potent inhibitor of B/C RAF kinase with almost equivalent IC50 values of 0.4 nM for B-RAF and C-RAF, showing a high level of selectivity, demonstrating greater than 99% on-target binding to BRAF, BRAFV600E, and CRAF at 1 μM and very few off-targets with DDR1 (>99%), DDR2 (86%), FRK (92%), and PDGFRb (96%), the only kinases with binding >80% at 1 μM.
  11. ERK inhibitor

    LY3214996 is a selective and novel ERK1/2 inhibitor with IC50 of 5 nM for both enzymes in biochemical assays. It potently inhibits cellular phospho-RSK1 in BRAF and RAS mutant cancer cell lines.
  12. BRAF inhibitor

    Lifirafenib (BGB-283), also known as Beigene-283, potently inhibits RAF family kinases and EGFR activities in biochemical assays with IC50 values of 23, 29 and 495 nM for the recombinant BRAFV600E kinase domain, EGFR and EGFR T790M/L858R mutant.
  13. TAK1 inhibitor

    Takinib is a selective TAK1 inhibitor that induces apoptosis following TNF-α stimulation in cell models of rheumatoid arthritis and metastatic breast cancer.
  14. ERK2 inhibitor

    AG-126 is a ERK2 inhibitor that selectively inhibits the phosphorylation of ERK1 (p44) and ERK2 (p42) at 25-50 μM.
  15. dual BRAF inhibitor

    AZ304 is a potent dual BRAF inhibitor targeting the kinase domains of wild type BRAF, V600E mutant BRAF. AZ304 exerted potent inhibitory effects on both wild type and V600E mutant forms of the serine/threonine-protein kinase BRAF, with IC50 values of 79?nM and 38?nM, respectively.
  16. 4-Methylbenzylidene camphor(4-MBC; Enzacamene)is an organic camphor derivative that is used in the cosmetic industry for its ability to protect the skin against UV, specifically UV B radiation.
  17. oncometabolite

    Fumaric acid is a fundamental unit of nucleic acids.. It is a oncometabolite or an endogenous, cancer causing metabolite. High levels of this organic acid can be found in tumors or biofluids surrounding tumors. Its oncogenic action appears to due to its ability to inhibit prolyl hydroxylase-containing enzymes.
  18. Antiparasitic

    Rafoxanide is a salicylanilide used as an anthelmintic. It is used to treat fluke, hookworm and other infestations.
  19. Raf/VEGFR3 inhibitor

    Sorafenib (Bay 43-9006) is a potent, orally active multikinase inhibitor with IC50s of 6 nM, 20 nM, and 22 nM for Raf-1, B-Raf, and VEGFR-3, respectively.
  20. Cephradine monohydrate (Cefradine monohydrate) is a first generation cephalosporin, which is active against a wide range of Gram positive and Gram-negative bacteria.
  21. MEK1 inhibitor

    Cobimetinib hemifumarate is a novel selective MEK1 inhibitor, and the IC50 value against MEK1 is 4.2 nM.
  22. MAP4K4 inhibitor

    PF-06260933 is a potent, selective, orally available MAP4K4 inhibitor with IC50 of 3.7 nM.
  23. Xanthocillin is a marine agent extracted from Penicillium commune, induces autophagy through inhibition of the MEK/ERK pathway.
  24. DLK inhibitor

    GNE-8505 is an orally available inhibitor of Dual leucine zipper kinase (DLK).
  25. p38α MAPK inhibitor

    MW150 (MW01-18-150SRM) is a selective, CNS penetrant, and orally active inhibitor of p38α MAPK with a Ki of 101 nM.
  26. MEK5 inhibitor

    GW284543, also known as UNC10225170;, is a potent and selective MEK5 inhibitor with the potential for cancer treatment.
  27. ERK5 inhibitor

    ERK5-IN-2 is an orally active, sub-micromolar, selective ERK5 inhibitor with IC50s of 0.82 μM, 3 μM for ERK5 and ERK5 MEF2D, respectively.
  28. Raf nhibitor

    RAF mutant-IN-1 is a RAF kinase inhibitor, extracted from patent WO2019107987A1, with IC50 values of 21 nM, 30 nM and 392 nM for C-RAF340D/Y341D, B-RAFV600E and B-RAFWT, respectively.
  29. RAF/ERK1/2 inhibitor

    ERK-IN-1 (compound B) is a RAF and ERK1/2 inhibitor in the treatment of a proliferative disease characterized by activating mutations in the MAPK pathway.
  30. p38α inhibitor

    p38α inhibitor 1 is a p38α inhibitor extracted from patent WO 2008076265 A1.
  31. RET/RAF/SRC/S6K inhibitor

    AD80, a multikinase inhibitor, inhibits RET, RAF,SRCand S6K, with greatly reduced mTOR activity.
  32. MNK1 and MNK2 inhibitor

    ETC-206 is a selective MNK1 and MNK2 inhibitor with IC50s of 64 nM and 86 nM, respectively.
  33. B-Raf inhibitor

    LUT014 is a B-Raf inhibitor with an IC50 of 11.7 nM, and developed to reduce dose-limiting acneiform lesions associated EGFR Inhibitors treatment. Extracted from patent WO 2019026065A2 .
  34. ERK2 inhibitor

    ERK2 IN-1 is a selective ERK2 inhibitor with an IC50 of 7 nM.
  35. MLKL inhibitor

    GW806742X is a Mixed Lineage Kinase Domain-Like protein (MLKL) inhibitor which binds the MLKL pseudokinase domain with a Kd value of 9.3 μM and has anti-necroptosis activity. GW806742X has activity against VEGFR2.
  36. ERK1/2 inhibitor

    ERK1/2 inhibitor 1 is a potent, orally bioavailable ERK1/2 inhibitor, showing 60% inhibition at 1 nM and an IC50 of 3.0 nM against ERK1 and ERK2, respectively.
  37. p38-α MAPK inhibitor

    5,6,7-Trimethoxyflavone is a novel p38-α MAPK inhibitor with an anti-inflammatory effect. 5,6,7-Trimethoxyflavone is isolated from several plants including Zeyhera tuberculosa, Callicarpa japonica, and Kickxia lanigera.
  38. RAF inhibitor

    BI-882370 is a potent and selective RAF kinase inhibitor that binds to the ATP binding site of the kinase positioned in the DFG-out (inactive) conformation of the BRAF kinase.
  39. Guggulsterone is a plant sterol derived from the gum resin of the tree Commiphora wightii. Guggulsterone inhibits the growth of a wide variety of tumor cells and induces apoptosis through down regulation of antiapoptotic gene products (IAP1, xIAP, Bfl-1/A1, Bcl-2, cFLIP and survivin), modulation of cell cycle proteins (cyclin D1 and c-Myc), activation of caspases and JNK, inhibition of Akt.
  40. p38 MAPK inhibitor

    AZD7624 is an inhaled p38 inhibitor, with potent anti-inflammatory activity.
  41. ERK1/2 kinases inhibitor

    KO-947 is a potent and selective inhibitor of ERK1/2 kinases with potential clinical utility in MAPK pathway dysregulated tumors.
  42. ERK5 inhibitor

    AX-15836 is a potent and selective ERK5 inhibitor with an IC50 of 8 nM.
  43. MAP4K4 inhibitor

    DMX-5804 is a potent, orally active and selective MAP4K4 inhibitor, with an IC50 of 3 nM, a pIC50 of 8.55 for human MAP4K4, less potent on MINK1/MAP4K6 (pIC50, 8.18), and TNIK/MAP4K7 (pIC50, 7.96).
  44. MNK1 and MNK2 inhibitor

    SLV-2436 is a highly potent and ATP-competitive inhibitor of MNK1 and MNK2 with IC50s of 10.8 ?nM and 5.4 nM, respectively.
  45. Nrf2 activator

    TBHQ (tert-Butylhydroquinone) is a widely used Nrf2 activator, protects against Doxorubicin (DOX)-induced cardiotoxicity through activation of Nrf2.
  46. MNK1/MNK2 inhibitor

    Tomivosertib (eFT508) is a potent, highly selective, and orally bioavailable MNK1 and MNK2 inhibitor, with IC50s of 1-2 nM against both isoforms.
  47. TNIK inhibitor

    NCB-0846 is an orally available TNIK inhibitor with an IC50 of 21?nM.
  48. p38 MAPK inhibitor

    ITX5061 is a type II inhibitor of p38 MAPK and also an antagonist of scavenger receptor B1 (SR-B1).
  49. Raf/EGFR inhibitor

    Lifirafenib (BGB-283) is a novel and potent Raf Kinase and EGFR inhibitor with IC50 values of 23 and 29 nM for recombinant BRafV600E and EGFR, respectively.
  50. MAPK14 inhibitor

    p38-α MAPK-IN-1 is an inhibitor of MAPK14 (p38-α), with IC50 of 2300 nM in EFC displacement assay, and 5500 nM in HTRF assay.

Items 151-200 of 239

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