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-138294
    RAS/RAS-RAF-IN-1
    Inhibitor 99.81%
    RAS/RAS-RAF-IN-1 is a potent RAS and RAS-RAF inhibitor. RAS/RAS-RAF-IN-1 has a KD of 5.0 μΜ-15 μΜ for cyclophilin A (CYPA) binding affinity. RAS/RAS-RAF-IN-1 has antitumor activity.
    RAS/RAS-RAF-IN-1
  • HY-15198
    KG5
    Inhibitor 99.79%
    KG5 is an orally active dual PDGFRβ and B-Raf allosteric inhibitor. KG5 also inhibits Flt3, KIT and c-Raf. KG5 has anticancer, antiangiogenic activities.
    KG5
  • HY-149380
    Vem-L-Cy5
    Inhibitor
    Vem-L-Cy5 (compound 3),modified with the NIR fluorophore cyanine-5 (Cy5),is a Vemurafenib (HY-12057)-based inhibitor of BRAF. Vem-L-Cy5 targets to BRAFV600E,and also inhibits MEK phosphorylation. Vem-L-Cy5 has cell permeability,and inhibits cell growth of many types of cancer.
    Vem-L-Cy5
  • HY-10331S
    Regorafenib-d3
    Inhibitor ≥98.0%
    Regorafenib-d3 is a deuterium labeled Regorafenib. Regorafenib is a multi-targeted receptor tyrosine kinase inhibitor.
    Regorafenib-d<sub>3</sub>
  • HY-P1039
    R18
    R18 is a peptide antagonists of 14-3-3, with a KD of 70-90 nM. R18 efficiently blocks the binding of 14-3-3 to the kinase Raf-1, a physiological ligand of 14-3-3, and effectively abolished the protective role of 14-3-3 against phosphatase-induced inactivation of Raf-1.
    R18
  • 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-10201S2
    Sorafenib-13C,d3
    Inhibitor 98.35%
    Sorafenib-13C,d3 is the 13C- and deuterium labeled Sorafenib. Sorafenib (Bay 43-9006) is a potent and orally active Raf inhibitor with IC50s of 6 nM and 20 nM for Raf-1 and B-Raf, respectively. Sorafenib 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 induces autophagy and apoptosis. Sorafenib has anti-tumor activity. Sorafenib is a ferroptosis activator.
    Sorafenib-<sup>13</sup>C,d<sub>3</sub>
  • HY-P10051A
    Cyclorasin 9A5 TFA
    Inhibitor 99.57%
    Cyclorasin 9A5 TFA is an 11-residue cell-permeable cyclic peptide that orthosterically inhibits the Ras-Raf protein interaction with an IC50 of 120 nM.
    Cyclorasin 9A5 TFA
  • 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 VEGFR1/2/3, 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-14660S
    Dabrafenib-d9
    Inhibitor
    Dabrafenib-d9 is the deuterium labeled Dabrafenib. Dabrafenib (GSK2118436A) is an ATP-competitive inhibitor of Raf with IC50s of 5 nM and 0.6 nM for C-Raf and B-RafV600E, respectively.
    Dabrafenib-d<sub>9</sub>
  • 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-159508
    Brimarafenib
    Inhibitor 99.35%
    Brimarafenib is a rapidly accelerated fibrosarcoma (Raf) kinase inhibitor wtih antineoplastic effect.
    Brimarafenib
  • 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
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