1. MAPK/ERK Pathway
  2. Raf

Raf

Raf kinases are a family of three serine/threonine-specific protein kinases that are related to retroviral oncogenes. RAF is an acronym for Rapidly Accelerated Fibrosarcoma. Raf kinases participate in the RAS-RAF-MEK-ERK signal transduction cascade, also referred to as the mitogen-activated protein kinase (MAPK) cascade. Activation of RAF kinases requires interaction with RAS-GTPases. The three RAF kinase family members are: A-Raf, B-Raf, C-Raf (Raf-1). The B-Raf protein is involved in sending signals inside cells, which are involved in directing cell growth. It was shown to be faulty (mutated) in some human cancers. C-RAF or even Raf-1 is an enzyme that in humans is encoded by the RAF1 gene. The c-Raf protein is part of the ERK1/2 pathway as a MAP kinase kinase kinase (MAP3K) that functions downstream of the Ras subfamily of membrane associated GTPases. C-Raf is a member of the Raf kinase family of serine/threonine-specific protein kinases, from the TKL (Tyrosine-kinase-like) group of kinases.

Raf Related Products (32):

Cat. No. Product Name Effect Purity
  • HY-10201
    Sorafenib Inhibitor
    Sorafenib is a potent multikinase inhibitor with IC50s of 6 nM, 20 nM, and 22 nM for Raf-1, B-Raf, and VEGFR-3, respectively.
  • HY-12057
    Vemurafenib Inhibitor
    Vemurafenib is a novel and potent inhibitor of B-RAF kinase, with IC50 values of RAFV600E (31 nM) and c-RAF-1 (48 nM).
  • HY-10201A
    Sorafenib Tosylate Inhibitor
    Sorafenib tosylate is a potent multikinase inhibitor, with IC50s of 6 nM, 20 nM, and 22 nM for Raf-1, B-Raf, and VEGFR-3, respectively.
  • HY-14660
    Dabrafenib Inhibitor
    Dabrafenib is an ATP-competitive inhibitor of BRAF with IC50s of 5 nM and 0.6 nM for CRAF and BRAFV600E, respectively.
  • HY-14660A
    Dabrafenib Mesylate Inhibitor
    Dabrafenib (Mesylate) is a novel, potent, and selective Raf kinase inhibitor, and inhibits the kinase activity of B-RafV600Eand c-Raf with IC50 values of 0.6 and 5.0 nM, respectively.
  • HY-18957
    BGB-283 Inhibitor
    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.
  • HY-10320
    Doramapimod Inhibitor
    Doramapimod is a highly potent p38α inhibitor with an IC50 of 4 nM, also inhibits B-Raf with an IC50 of 83 nM and Abl with an IC50 of 14.6 μM.
  • HY-15605
    LGX818 Inhibitor
    LGX818 is an orally available mutated BRafV600E inhibitor (IC50=0.3 nM) with potential antineoplastic activity.
  • HY-15246
    MLN 2480 Inhibitor
    MLN 2480 is an orally active and selective inhibitor of pan-Raf kinase.
  • HY-12558
    LY3009120 Inhibitor
    LY3009120 is a pan RAF and RAF dimer inhibitor, and inhibits BRAFV600E, BRAFWT and CRAFWT with IC50 values of 5.8, 9.1 and 15 nM, respectively.
  • HY-51424
    PLX-4720 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.
  • HY-10542
    GW 5074 Inhibitor
    GW 5074 is a potent and selective c-Raf inhibitor with IC50 of 9 nM, and has no effect on the activities of JNK1/2/3, MEK1, MKK6/7, CDK1/2, c-Src, p38 MAP, VEGFR2 or c-Fms.
  • HY-12291
    HG6-64-1 Inhibitor
    HG6-64-1 is a potent and selective B-Raf and mutant B-Raf inhibitor; more information can be found in Patent WO 2011090738.
  • HY-11004
    AZ 628 Inhibitor
    AZ628 is a new pan-Raf inhibitor for BRAF, BRAFV600E, and c-Raf-1 with IC50 of 105 nM, 34 nM and 29 nM, also inhibits VEGFR2, DDR2, Lyn, Flt1, FMS, etc.
  • HY-18652
    Ro 5126766 Inhibitor
    Ro 5126766 (CH5126766) is a potent and selective dual RAF/MEK inhibitor. For SK-MEL-28, SK-MEL-2, MIAPaCa-2, and SW480 cell lines, the IC50 is determined by WST-8 assay is 65, 28, 40, and 46 nM, respectively.
  • HY-13343
    ZM 336372 Inhibitor
    ZM 336372 is a potent and selective c-Raf inhibitor with IC50 of 70 nM, 10-fold selectivity over B-RAF, no inhibition to PKA/B/C, AMPK, p70S6, etc.
  • HY-15767
    TAK-632 Inhibitor
    TAK-632 is a potent pan-RAF inhibitor with IC50 of 1.4, 2.4 and 8.3 nM for CRAF, BRAFV600E, BRAFWT, respectively.
  • HY-10248
    RAF265 Inhibitor
    RAF265 (CHIR-265) is a potent selective inhibitor of C-Raf/B-Raf/B-Raf V600E with IC50 of 3-60 nM, and exhibits potent inhibition on VEGFR2 phosphorylation with EC50 of 30 nM.
  • HY-14177
    B-Raf inhibitor 1 Inhibitor
    B-Raf inhibitor 1 is a potent and selective B-Raf inhibitor with cell IC50s of 0.31 uM and 2 nM for A375 proliferation and A375 p-ERK respectively.
  • HY-50864
    GDC-0879 Inhibitor
    GDC-0879 is a novel, potent, and selective B-Raf inhibitor with IC50 of 0.13 nM with activity against c-Raf as well; no inhibition known to other protein kinases.