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MAPK

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Items 1-50 of 670

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  1. A10001
    Sorafenib Tosylate (Nexavar)

    Raf inhibitor

    Sorafenib Tosylate (Nexavar) is a novel, small molecular inhibitor of several tyrosine protein kinases (VEGFR and PDGFR) and RAF/MEK/ERK cascade inhibitor with an IC50 of 6, 22, 38 nM for Raf-1, wt BRAF and V599E mutant BRAF.
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  2. A12505
    TCS ERK 11e (VX-11e)

    ERK2 inhibitor

    TCS ERK 11e (VX-11e) is a potent and selective extracellular signal-related kinase 2 (ERK2) inhibitor (Ki values are <2, 395, 540 and 852 nM for ERK2, GSK-3, Aurora Kinase A and Cdk2 respectively). Potently blocks proliferation of HT29 cells (IC50 = 48 nM).
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  3. A11221
    PD 169316

    p38 MAPK inhibitor

    PD 169316 (PD169316) is a selective inhibitor of p38 MAPK.1 that inhibits p38 MAPK with an IC50 of 89 nM.
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  4. A10151
    (E/Z)-BIX 02189

    MEK inhibitor

    BIX 02189 is a selective dual MEK5 and ERK5 (or BMK1) kinase inhibitor, with IC50 values of 1.5, 59, 580 and >6200 nM for MEK5, ERK5, TGFbR1 and other closely related kinases respectively.
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  5. A16334
    Necrosulfonamide

    MLKL inhibitor

    Necrosulfonamide is a pharmacological inhibitor of MLKL with IC50 values of 124 nM in human HT-29.
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  6. A10257
    AZD6244 (Selumetinib)

    MEK inhibitor

    AZD6244 (Selumetinib) also known as Selumetinib, ARRY142886, AZD-6244 & ARRY-142886 is MEK 1/2 inhibitor with GI50 values ranging from 14 to 50 nm.
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  7. A15050
    Cobimetinib (racemate)

    MEK inhibitor

    Cobimetinib is a potent, highly selective inhibitor of MEK1/2.
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  8. A10823
    SB 202190

    p38 MAPK Inhibitor

    SB202190 is a highly selective, potent and cell-permeable inhibitor of p38 MAP kinase.
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  9. A11582
    TAK-715

    p38 MAPK inhibitor

    TAK 715 an inhibitor of p38 MAPK (IC50 = 7.1 nM for p38 MAPKα), Wnt/beta-catenin signaling, and Inhibits 22 kinases by more than 80%, including CK 1δ/ε.
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  10. A14219
    URMC-099

    MLK inhibitor

    URMC-099 is an orally bioavailable, brain penetrant mixed lineage kinase (MLK) inhibitor with IC50 of 19 nM, 42 nM, 14 nM, and 150 nM, for MLK1, MLK2, MLK3, and DLK, respectively.
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  11. A12866
    Refametinib R enantiomer

    MEK1/2 inhibitor

    Refametinib, also known as RDEA119, BAY 86-9766, is an orally bioavailable selective MEK inhibitor with potential antineoplastic activity.
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  12. A15762
    BI-847325

    MEK/Aurora Inhibitor

    BI-847325 is an orally bioavailable, and selective dual MEK/Aurora kinase inhibitor with IC50 of 3 nM, 25 nM, 15 nM, 25 nM, and 4 nM for Xenopus laevis Aurora B, human Aurora A and Aurora C, as well as human MEK1 and MEK2, respectively. Phase 1.
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  13. A11352
    CC-401

    JNK inhibitor

    CC-401 is a second generation ATP-competitive anthrapyrazolone c-Jun N terminal kinase (JNK) inhibitor with potential antineoplastic activity.
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  14. A10957
    U0126-EtOH

    MEK inhibitor

    U0126-EtOH is an inhibitor of both MEK1 and MEK2 with an IC50 of 72 nM and 58 nM respectively.
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  15. A10002
    PLX-4720

    Raf inhibitor

    PLX-4720 is a potent and selective inhibitor of B-RafV600E with IC50 of 13 nM in a cell-free assay, equally potent to c-Raf-1(Y340D and Y341D mutations), and 10-fold selectivity for B-RafV600E than wild-type B-Raf.
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  16. A10250
    Regorafenib (BAY 73-4506)

    VEGFR inhibitor

    Regorafenib (BAY 73-4506) is a multikinase inhibitor with IC50 of 17, 40 and 69 nM c-KIT, VEGFR2, B-Raf. Regorafenib (BAY 73-4506) is an orally bioavailable multikinase inhibitor targeting both the tumor and its vasculature.
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  17. A11441
    GDC-0973 (Cobimetinib)

    MEK1 inhibitor

    Cobimetinib (GDC-0973, RG7420) is a potent and highly selective MEK1 inhibitor with IC50 of 4.2 nM, showing more than 100-fold selectively for MEK1 over MEK2 and showed no significant inhibition when tested against a panel of more than 100 of serine-threonine and tyrosine kinases.
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  18. A10420
    GDC-0879

    B-Raf inhibitor

    GDC-0879 is a specific inhibitor of B-Raf kinase enzyme,targeting B-Raf (V600E) (IC50: 0.13 nM).
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  19. A11794
    Ulixertinib (BVD-523, VRT752271)

    ERK1/ERK2 inhibitor

    VRT752271 is a pyrrole inhibitors of ERK protein kinase.
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  20. A12749
    JNK-IN-8

    JNK Inhibitor

    JNK-IN-8 is the first irreversible JNK inhibitor for JNK1, JNK2 and JNK4 with IC50 of 4.7 nM, 18.7 nM and 1 nM, respectively
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  21. A21729
    BIX02189

    MEK5 inhibitor

    BIX02189 is a potent and selective MEK5 inhibitor with an IC50 of 1.5 nM. BIX02189 also inhibits ERK5 catalytic activity with an IC50 of 59 nM.
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  22. A11225
    Pluripotin (SC-1)

    ERK1/RasGAP Inhibitor

    The activity of Pluripotin (SC-1) is mediated by the combined inhibition of RasGAP and ERK1 with Kd values of 98 and 212 nM, respectively.
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  23. A10824
    Adezmapimod (SB-203580)

    p38 MAPK inhibitor

    SB 203580 is a specific inhibitor of p38α and p38β which suppresses downstream activation of MAPKAP kinase-2 and heat shock protein 27.
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  24. A10860
    SP600125

    JNK inhibitor

    SP600125 is a JNK inhibitor with IC50=40 nM for JNK-1 and JNK-2 and 90 nM for JNK-3.
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  25. A11321
    Skepinone-L

    p38 MAPK inhibitor

    Skepinone-L is a selective p38 mitogen-activated protein kinase inhibitor.
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  26. A10661
    NVP-BHG712

    EphB4 inhibitor

    NVP-BHG712 is a selective inhibitor of EphB4 kinase that exhibits selectivity for EphB4 over more than 40 other kinases in vitro, including FGFR3.
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  27. A11493
    MEK162 (ARRY-438162, Binimetinib)

    MEK1/2 inhibitor

    MEK162 (ARRY-438162) is a potent, selective, ATP uncompetitive inhibitor of MEK1/2.
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  28. A10212
    PD184352 (CI-1040)

    MEK1/2 inhibitor

    PD184352 (CI-1040) is an ATP non-competitive MEK1/2 inhibitor with IC50 of 17 nM in cell-based assays, 100-fold more selective for MEK1/2 than MEK5. Phase 2.
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  29. A10115
    AZD8330

    MEK Inhibitor

    AZD8330 is a novel, selective, non-ATP competitive MEK 1/2 inhibitor with IC50 of 7 nM. Phase 1.
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  30. A11040
    TAK-733

    MEK Inhibitor

    TAK-733 is an orally bioavailable small-molecule inhibitor of MEK1 and MEK2 (MEK1/2) with potential antineoplastic activity.
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  31. A13226
    LGX 818 (Encorafenib)

    Selective B-RAF Inhibitor

    LGX818 is an orally available Raf kinase inhibitor with potential antineoplastic activity.
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  32. A14119
    FR 180204

    ERK inhibitor

    FR 180204 is a novel and selective inhibitor of extracellular signal-regulated kinase (ERK), which may be a potential new therapy for rheumatoid arthritis.
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  33. A11381
    Dabrafenib (GSK2118436A)

    Raf inhibitor

    Dabrafenib is a potent and selective inhibitor of B-RAF protein kinase carrying V600E mutation, currently in clinical trial.
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  34. A11296
    AS 602801 (Bentamapimod)

    JNK inhibitor

    AS 602801 is a novel, orally active, Jun Kinase Inhibitor.
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  35. A10256
    Mirdametinib (PD0325901)

    MEK inhibitor

    PD0325901 is MEK inhibitor and non-competitive with ATP, Kiapp of 1 nM against activated MEK1 and MEK2.
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  36. A11029
    Trametinib (GSK1120212, JTP-74057)

    MEK Inhibitor

    Trametinib (GSK1120212, JTP-74057) strongly prevented the activities of MEK1 and MEK2 kinases rather than activities of other 98 kinases.

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  37. A10705
    PD98059

    MEK Inhibitor

    PD98059 is an equipotent antagonist of the aryl hydrocarbon receptor and inhibitor of mitogen-activated protein kinase kinase.
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  38. A10148
    Doramapimod (BIRB-796)

    p38 MAPK inhibitor

    Doramapimod (BIRB 796) is a small molecule inhibitor of p38 MAPK,which plays a critical role in regulating the production of proinflammatory cytokines.
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  39. A16079
    (E/Z)-Locostatin ((E/Z)-UIC-1005)

    RKIP/Raf1 inhibitor

    Locostatin is a cell permeable, potent inhibitor of Raf kinase inhibitor protein (RKIP)/Raf1 kinase interaction and an inhibitor of cell migration.
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  40. A10982
    VX-702

    p38 MAPK inhibitor

    VX-702 is an orally bioavailable inhibitor of p38 MAP kinase that inhibits platelet agonist induced p38 activation (IC50= 4 to 20 nM).
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  41. A10739
    PLX4032 (Vemurafenib)

    Raf inhibitor

    PLX4032 (Vemurafenib) also known as RG7204, Vemurafenib, R7204; RO5185426. PLX4032 is a B-raf inhibitor with an IC50 of 44 nM.
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  42. A13323
    TAK-632

    pan-RAF inhibitor

    TAK-632 is a potent pan-RAF inhibitor with favorable in vitro activity (BRAF(V600E) IC50, 2.4 nM; BRAF(wt), 8.3 nM; CRAF, 1.4 nM; pMEK (A375) IC50, 12 nM; pMEK (HMVII), 49 nM; V/B ratio.
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  43. A11078
    PH-797804

    p38 MAPK inhibitor

    PH-797804 is a diarylpyridinone inhibitor of p38 mitogen-activated protein (MAP) kinase.
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  44. A14019
    Avutometinib (RO5126766, CH5126766)

    Raf/MEK dual inhibitor

    Avutometinib (RO5126766, CH5126766), is a protein kinase inhibitor specific for the Raf and MEK mitogen-activated protein kinases (MAPKs) with potential anti-neoplastic activity.

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  45. A21450
    Trametinib (DMSO solvate)

    MEK inhibitor

    Trametinib DMSO solvate (GSK-1120212 (DMSO solvate);JTP-74057 (DMSO solvate)) is a potent MEK inhibitor that specifically inhibits MEK1/2, with an IC50 value of about 2 nM.
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  46. A12824
    SCH772984

    ERK Inhibitor

    SCH772984 is a novel, specific inhibitor of ERK1/2 with IC50 of 4 nM and 1 nM, respectively.
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  47. A12408
    ML-3043

    p38 MAPK inhibitor

    ML-3043 is a p38 MAPK inhibitor (IC50 = 0.38 μM). Inhibits the release of IL-1β and TNF-α in a peripheral blood mononuclear cell (PBMC) assay (IC50 values are 0.039 and 0.16 μM respectively).
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  48. A12502
    TC13172

    MLKL inhibitor

    TC13172 is a mixed lineage kinase domain-like protein (MLKL) inhibitor with an EC50 value of 2 nM for HT-29 cells.
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  49. A12526
    Losmapimod (GW856553X)

    p38 MAPK inhibitor

    Losmapimod, also know as GW856553 or GW856553X, is a drug developed by GlaxoSmithKline which acts as a selective inhibitor of the enzyme family known as p38 mitogen-activated protein kinases.
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  50. A12739
    PF-04880594

    RAF inhibitor

    PF-04880594 is an inhibitor of RAF with IC50 values of 0.19 nM/0.13 nM and 0.39 nM for BRAF/BRAFV599E and c-RAF, respectively.
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