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-109574
    Raf inhibitor 2
    		Inhibitor 98.48%
    Raf inhibitor 2 is a potent raf kinase (IC50<1.0 μM) inhibitor, compound 32, extracted from patent EP1003721B1. Raf inhibitor 2 can be used for cancer research.
    Raf inhibitor 2
  • HY-18227
    B-Raf IN 1
    		Inhibitor 99.94%
    B-Raf IN 1 is a potent and selective B-Raf kinase inhibitor with an IC50 of 24 nM.
    B-Raf IN 1
  • HY-111940
    LUT014
    		Inhibitor
    LUT014 is a B-Raf inhibitor with an IC50 of 11.7 nM, and developed to reduce dose-limiting acneiform lesions associated EGFR Inhibitors treatment. Extracted from patent WO 2019026065A2 .
    LUT014
  • HY-117737A
    RRD-251
    		Inhibitor 99.94%
    RRD-251 is an inhibitor of retinoblastoma tumor suppressor protein (Rb)-Raf-1 interaction, with potent anti-proliferative, anti-angiogenic and anti-tumor activities.
    RRD-251
  • HY-109080A
    Belvarafenib TFA
    		Inhibitor ≥99.0%
    Belvarafenib TFA (HM95573 TFA) is a potent and pan RAF (Rapidly Accelerated Fibrosarcoma) inhibitor, with IC50s of 56 nM, 7 nM and 5 nM for B-RAF, B-RAFv600E and C-RAF respectively.
    Belvarafenib TFA
  • 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-18507
    AD57
    		Inhibitor 98.08%
    AD57 is an orally active multikinase inhibitor, inhibits RET, BRAF, S6K and Src, with greatly reduces mTOR activity.
    AD57
  • HY-10331S
    Regorafenib-d3
    		Inhibitor ≥98.0%
    Regorafenib-d3 is a deuterium labeled Regorafenib. Regorafenib is a multi-targeted receptor tyrosine kinase inhibitor[1].
    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-155736
    MAPK-IN-2
    		Inhibitor 98.54%
    MAPK-IN-2 (compound 3h) is a potent MAPK inhibitor with antineoplastic activity. MAPK-IN-2 inhibits cancer cell proliferation among serval cancer cell lines, and suppresses MAPK pathway with potant efficacy (EGFRWT IC50=281 nM, c-MET IC50=205 nM, B-RAFWT IC50=112 nM, and CDK4/6 IC50=95 and 184 nM, respectively). MAPK-IN-2 even shows a remarkable potency against mutated EGFR and B-RAF (EGFRT790M IC50=69 nM and B-RAFV600E IC50=83 nM).
    MAPK-IN-2
  • 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-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-153603
    B-Raf IN 15
    		Inhibitor ≥98.0%
    B-Raf IN 15 (Compound 7) is a BRAF inhibitor. B-Raf IN 15 inhibits BRAF WT and BRAF V600E with IC50s of 2.0 and 0.8 μM. B-Raf IN 15 can be used for the research of cancer.
    B-Raf IN 15
  • 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
Cat. No. Product Name / Synonyms Application Reactivity
Raf Isoform Comparison

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