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

Raf

Raf kinases

Raf

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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 Isoform Specific Products:

Raf Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-P10051
    Cyclorasin 9A5
    		Inhibitor
    Cyclorasin 9A5 is an 11-residue cell-permeable cyclic peptide that orthosterically inhibits the Ras-Raf protein interaction with an IC50 of 120 nM.
    Cyclorasin 9A5
  • HY-10966R
    SB-590885 (Standard)
    		Inhibitor
    SB-590885 (Standard) is the analytical standard of SB-590885 (HY-10966). This product is intended for research and analytical applications. SB-590885 is a potent B-Raf inhibitor with a Ki of 0.16 nM, and has 11-fold greater selectivity for B-Raf over c-Raf, without inhibition to other human kinases.
    SB-590885 (Standard)
  • HY-10331B
    Regorafenib mesylate
    		Inhibitor
    Regorafenib (BAY 73-4506) mesylate is an orally active and potent multi-targeted receptor tyrosine kinase inhibitor, with IC50 values of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/Flt-1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively. Regorafenib mesylate shows very robust antitumor and antiangiogenic activity.
    Regorafenib mesylate
  • HY-10542A
    (Z)-GW 5074
    		Inhibitor
    (Z)-GW 5074 is a compound which interacts with both mHTT (mutant huntingtin protein) and LC3, but not but not with the wild-type HTT protein. (Z)-GW 5074 inhibits c-Raf, shows no effect on autophagy, and is effective for neurodegenerative disorder.
    (Z)-GW 5074
  • HY-142452
    Pan-RAF kinase inhibitor 1
    Pan-RAF kinase inhibitor 1 is a potent inhibitor of Pan-RAF kinase. Pan-RAF kinase inhibitor 1 regulates MAPK signaling by inhibiting RAF kinase, thereby exerting an effect on the proliferation of RAS-mutant tumor cells. Pan-RAF kinase inhibitor 1 has the potential for the research of cancer diseases (extracted from patent WO2021110141A1, compound 16B).
    Pan-RAF kinase inhibitor 1
  • HY-159534
    Flezurafenibum
    		Inhibitor
    Flezurafenibum (Flezurafenib) is a rapidly accelerated fibrosarcoma (Raf) kinase inhibitor, with antineoplastic effect.
    Flezurafenibum
  • HY-159508
    Brimarafenibum
    		Inhibitor
    Brimarafenibum (Brimarafenib) is a rapidly accelerated fibrosarcoma (Raf) kinase inhibitor, wtih antineoplastic effect.
    Brimarafenibum
  • HY-108887
    Anticancer agent 124
    		Inhibitor
    Anticancer agent 124 is an orally active, highly selective and potent pan RAF inhibitor. Anticancer agent 124 inhibits MAPK signalling in BRAF V600E, NRAS and KRAS mutant tumor cells.
    Anticancer agent 124
  • HY-126298
    RAF mutant-IN-1
    		Inhibitor
    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-RAF 340D/Y341D, B-RAFV600E and B-RAFWT, respectively.
    RAF mutant-IN-1
  • HY-146303
    C-RAF kinase-IN-1
    		Inhibitor
    C-RAF kinase-IN-1 (compound 1l) is a potent inhibitor of C-RAF kinase with an IC50 of 0.193 μM. C-RAF kinase-IN-1 is a quinoline derivative. C-RAF kinase-IN-1 has the potential for the research of cancer diseases.
    C-RAF kinase-IN-1
  • HY-153490A
    ISIS 5132 sodium
    		Inhibitor
    ISIS 5132 sodium is a 20-base phosphorothioate oligonucleotide that specifically down-regulates c-raf expression.
    ISIS 5132 sodium
  • HY-115933
    EGFR/BRAF-IN-1
    		Inhibitor
    EGFR/BRAF-IN-1 (compound 21), a 2,3-dihydropyrazino[1,2-a]indole-1,4-dione derivative, is a potent EGFR/BRAF inhibitor with an IC50 of 45 nM for BRAFV600E. EGFR/BRAF-IN-1 inhibits cancer cell proliferation (GI50=35 nM). EGFR/BRAF-IN-1 shows good antioxidant activity.
    EGFR/BRAF-IN-1
  • HY-146432
    Antitumor agent-60
    		Inhibitor
    Antitumor agent-60 (compound 20) is a potent antitumor agent, targeting RAS-RAF signaling pathway and binding to CRAF with a Kd value of 3.93 μM. Antitumor agent-60 induces apoptosis by blocking cell cycle at G2/M phase. Antitumor agent-60 enhances the level of p53 and ROS. Antitumor agent-60 causes oval and irregular nucleus in cancer cells. Antitumor agent-60 can suppress the growth of tumor to some extent in A549 xenograft model.
    Antitumor agent-60
  • HY-13810
    PF-04880594
    		Inhibitor
    PF-04880594 is a potent and selective RAF inhibitor. PF-04880594 inhibits both wild-type and mutant BRAF and CRAF. PF-04880594 shows antitumor activity.
    PF-04880594
  • HY-142820
    B-Raf IN 5
    		Inhibitor
    B-Raf IN 5 (compound 3b) is a potent inhibitor of protein kinase B-Raf with an IC50 of 2.0 nM. B-Raf IN 5 is devoid of binding to the secondary target PXR and resists rapid metabolism. B-Raf IN 6 has the potential for the research of cancer disease.
    B-Raf IN 5
  • HY-17598R
    Rafoxanide (Standard)
    		Inhibitor
    Rafoxanide (Standard) is the analytical standard of Rafoxanide. This product is intended for research and analytical applications. Rafoxanide is a poent, orally active halogenated salicylaniline agent with antiparasitic activity. Rafoxanide interferes with energy metabolism in trematodes by uncoupling oxidative phosphorylation. Rafoxanide is also found to be a potent inhibitor of the BRAF V600E mutant protein, which is important in colorectal cancer. Rafoxanide can be used for the control of infestation with Hemonchus species or Fasciola species in sheep and cattle as well as Oestrus ovis in sheep. Rafoxanide can also be used for cancer research.
    Rafoxanide (Standard)
  • HY-150250
    B-Raf IN 13
    		Inhibitor
    B-Raf IN 13 is a BRAF inhibitor with an IC50 of 3.55 nM in BRAF V600E enzyme assay. B-Raf IN 13 has anticaner effects (WO2020261156A1, Example 74).
    B-Raf IN 13
  • HY-18652A
    Avutometinib potassium
    		Inhibitor
    Avutometinib (CH5126766) (potassium) is a RAF/MEK clamp that potently inhibits RAF/MEK kinase activity and induces dominant negative RAF-MEK complexes preventing phosphorylation of MEK by ARAF, BRAF and CRAF. Avutometinib (potassium) shows anti-proliferative potency across tumor cell lines carrying KRAS mutations including PDAC cell lines. Avutometinib (potassium) induces tumor inhibition and increases survival in a KRAS/p53 pancreatic cancer mouse model. Avutometinib (potassium) is promising for research of low-grade-serous-ovarian-carcinoma (LGSOC), ovarian cancer and pancreatic ductal adenocarcinoma (PDAC).
    Avutometinib potassium
  • HY-164492
    LSN3074753
    		Inhibitor
    LSN3074753, an analog of LY3009120 (HY-12558), is a pan-RAF and Raf dimer inhibitor. LSN3074753 demonstrates activity against tumor cells with MAPK pathway activation driven by BRAF monomer or RAF dimers including BRAF- or KRAS-mutant colorectal cancer. LSN3074753 combined with Cetuximab (HY-P9905) shows additive and synergistic effects for colorectal cancer PDX models, particularly those with KRAS or BRAF mutation.
    LSN3074753
  • HY-146492
    VEGFR-2/BRAF-IN-2
    		Inhibitor
    VEGFR-2/BRAF-IN-2 (Compound 4a) is a dual VEGFR-2 and BRAF kinases inhibitor with IC50 values of 0.111, 0.089 and 0.071 µM against VEGFR-2, BRAFV600E and BRAFWT, respectively. VEGFR-2/BRAF-IN-2 induces apoptosis and arrests the cell cycle mainly in the G1 phase.
    VEGFR-2/BRAF-IN-2
Cat. No. Product Name / Synonyms Application Reactivity
Raf Isoform Comparison

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