1. Signaling Pathways
  2. MAPK/ERK Pathway
  3. Raf

Raf

Raf kinases

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-116664
    DPQZ
    Inhibitor
    DPQZ is an anti-tubulin agent that inhibits cell separation and induces cell cycle arrest at the G2/M phase. In addition, DPQZ induces caspase-dependent apoptosis of HSC-3 cells by inhibiting Ras/Raf and activating MAP kinase. DPQZ can be used in the study of oral cancer.
    DPQZ
  • HY-15605R
    Encorafenib (Standard)
    Inhibitor
    Encorafenib (Standard) is the analytical standard of Encorafenib. This product is intended for research and analytical applications. Encorafenib (LGX818) is a highly potent BRAF inhibitor with selective anti-proliferative and apoptotic activity in cells expressing BRAFV600E (EC50=4 nM).
    Encorafenib (Standard)
  • HY-164530
    SKLB646
    Inhibitor
    SKLB646 is an orally active multi-target kinase inhibitor. SKLB646 shows significant inhibitory effects on SRC and VEGFR2 with IC50 values ??of 0.002 μmol/L and 0.012 μmol/L, respectively. SKLB646 also shows significant inhibitory effects on B-Raf and C-Raf with IC50 values ??of 0.022 μmol/L and 0.019 μmol/L, respectively. SKLB646 inhibits the activation of the SRC signaling pathway and blocks the MAPK signaling pathway by inhibiting Raf kinase. In addition, SKLB646 can inhibit the proliferation, migration and invasion of human umbilical vein endothelial cells (HUVEC) to inhibit tumor-induced angiopoietic formation. SKLB646 shows significant anti-proliferative and anti-survival activities against triple-negative breast cancer (TNBC) cell lines.
    SKLB646
  • HY-10201AR
    Sorafenib tosylate (Standard)
    Inhibitor
    Sorafenib tosylate (Standard) is the analytical standard of Sorafenib tosylate. This product is intended for research and analytical applications. Sorafenib tosylate (Bay 43-9006 tosylate) is a potent and orally active Raf inhibitor with IC50s of 6 nM and 20 nM for Raf-1 and B-Raf, respectively. Sorafenib tosylate is a multikinase inhibitor with IC50s of 90 nM, 15 nM, 20 nM, 57 nM and 58 nM for VEGFR2, VEGFR3, PDGFRβ, FLT3 and c-Kit, respectively. Sorafenib tosylate induces autophagy and apoptosis. Sorafenib Tosylate has anti-tumor activity. Sorafenib tosylate is a ferroptosis activator.
    Sorafenib tosylate (Standard)
  • HY-14660AR
    Dabrafenib Mesylate (Standard)
    Inhibitor
    Dabrafenib (Mesylate) (Standard) is the analytical standard of Dabrafenib (Mesylate). This product is intended for research and analytical applications. Dabrafenib Mesylate is a potent and selective Raf kinase inhibitor with IC50s of 0.6 and 5.0 nM for RafV600E and c-Raf, respectively.
    Dabrafenib Mesylate (Standard)
  • HY-51424S
    PLX-4720-d7
    Inhibitor
    PLX-4720-d7 is the deuterium labeled PLX-4720. PLX-4720 is a potent and selective inhibitor of?B-RafV600E?with?an 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.
    PLX-4720-d<sub>7</sub>
  • HY-10248R
    RAF265 (Standard)
    Inhibitor
    RAF265 (Standard) is the analytical standard of RAF265 (HY-10248). This product is intended for research and analytical applications. RAF265 is a potent and orally active RAF/VEGFR2 inhibitor.
    RAF265 (Standard)
  • HY-107779R
    BI-882370 (Standard)
    Inhibitor
    BI-882370 (Standard) is the analytical standard of BI-882370 (HY-107779). This product is intended for research and analytical applications. 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. BI-882370 (BI 882370) inhibits the oncogenic BRAFV600E-mutant, the WT BRAF and CRAF Kinases with IC50s of 0.4, 0.8, and 0.6 nM, respectively. BI-882370 also inhibits SRC family Kinases.
    BI-882370 (Standard)
  • HY-13308R
    Regorafenib Hydrochloride (Standard)
    Inhibitor
    Regorafenib (Hydrochloride) (Standard) is the analytical standard of Regorafenib (Hydrochloride). This product is intended for research and analytical applications. Regorafenib Hydrochloride (BAY 73-4506 hydrochloride) is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1 with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM, respectively.
    Regorafenib Hydrochloride (Standard)
  • HY-14177A
    Raf inhibitor 1 dihydrochloride
    Inhibitor 99.29%
    B-Raf inhibitor 1 dihydrochloride is a potent Raf kinase inhibitor with Kis of 1 nM, 1 nM, and 0.3 nM for B-RafWT, B-RafV600E, and C-Raf, respectively.
    Raf inhibitor 1 dihydrochloride
  • HY-18817
    AFG210
    Inhibitor
    AFG210 is a potent multi-target kinase inhibitor that primarily inhibits Abl kinase (IC50=330 nM), and also has inhibitory effects on other kinases such as B-Raf, C-Raf, FGFR-1, RET and VEGF receptors. AFG210 can be used to study chronic myeloid leukemia and other diseases with abnormal activation of Abl kinase.
    AFG210
  • HY-51424R
    PLX-4720 (Standard)
    Inhibitor
    PLX-4720 (Standard) is the analytical standard of PLX-4720. This product is intended for research and analytical applications. 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.
    PLX-4720 (Standard)
  • HY-N15264
    Azaspirene
    Inhibitor
    Azaspirene ((-)-Azaspirene) is an angiogenesis and Raf-1 activation inhibitor isolated from the fungus Neosartorya sp. Azaspirene inhibits vascular endothelial growth factor (VEGF)-induced human umbilical vein endothelial cell (HUVEC) migration and Raf-1 activation, but has no effect on the activation of kinase insert domain-containing receptor/fetal liver kinase 1 (VEGF receptor 2).
    Azaspirene
  • HY-10542R
    GW 5074 (Standard)
    Inhibitor
    GW 5074 (Standard) is the analytical standard of GW 5074 (HY-10542). This product is intended for research and analytical applications. 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.
    GW 5074 (Standard)
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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