Raf
RAF kinases act downstream of RAS and relay signals through the RAF-MEK-ERK/MAPK cascade to regulate cell growth, survival, and differentiation[1]. Mechanistically, RAF activation depends on phosphorylation, conformational control, membrane recruitment, and kinase-domain dimerization, which provides an allosteric mechanism for catalytic activity[1]. In cancer models, mutant BRAF tumors depend on RAF-MEK-ERK signaling, whereas ATP-competitive RAF inhibitors inhibit ERK signaling in mutant BRAF cells but enhance signaling in wild-type BRAF cells through RAF dimer transactivation[2]. Compared with related isoforms, BRAF has the highest basal kinase activity, while ARAF shows a cell-type-dependent role in MAPK activity and cell migration[3]. CRAF/RAF1 differs further because KRAS-mutant tumor subsets depend on CRAF growth functions, and kinase-dead but not dimer-defective CRAF rescues growth inhibition[4]. For experimental applications, RAF inhibitors therefore serve as pathway probes, but study design should distinguish mutant BRAF inhibition from wild-type RAF dimer activation[2][5].
References:
- [1]. Lavoie H, et al. Regulation of RAF protein kinases in ERK signalling. Nat Rev Mol Cell Biol. 2015 May;16(5):281-98. [Content Brief]
- [2]. Poulikakos PI, et al. RAF inhibitors transactivate RAF dimers and ERK signalling in cells with wild-type BRAF. Nature. 2010 Mar 18;464(7287):427-30. [Content Brief]
- [3]. Mooz J, et al. Dimerization of the kinase ARAF promotes MAPK pathway activation and cell migration. Sci Signal. 2014 Aug 5;7(337):ra73. [Content Brief]
- [4]. Venkatanarayan A, et al. CRAF dimerization with ARAF regulates KRAS-driven tumor growth. Cell Rep. 2022 Feb 8;38(6):110351. [Content Brief]
- [5]. Karoulia Z, et al. An Integrated Model of RAF Inhibitor Action Predicts Inhibitor Activity against Oncogenic BRAF Signaling. Cancer Cell. 2016 Sep 12;30(3):485-498. [Content Brief]
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Raf Related Products (120)
Related Products (120)
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Antibodies (2)
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EGFR/BRAFV600E-IN-5
0 ImagesCat. No.: HY-172877EGFR/BRAFV600E-IN-5 (Compound 7I) is a dual BRAFV600E/EGFR inhibitor with IC50 of 0.048 μM and 0.037 μM, respectively. EGFR/BRAFV600E-IN-5 has significant anti-melanoma activity with IC50 of 3.16 μM and 2.50 μM against MALME-3M and LOX-IMVI cell lines, respectively. EGFR/BRAFV600E-IN-5 exerts anti-tumor effects by inducing G1 arrest, inhibiting DNA synthesis, and activating the mitochondrial apoptosis pathway. EGFR/BRAFV600E-IN-5 can be used for melanoma research, especially for combined inhibition of BRAFV600E mutation and EGFR signaling pathway.
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pan-Raf/RTK inhibitor 1
0 ImagesCat. No.: HY-169869CAS No.: 1980821-53-1Pan-Raf/RTK inhibitor 1 (compound I-16) is a potent pan-Raf inhibitor with IC50 values of 3.49 nM (BRafV600E), 8.86 nM (ARaf), 5.78 nM (BRafWT), and 1.65 nM (CRaf). Pan-Raf/RTK inhibitor 1 exhibits antiproliferative activities against various cancer cell lines and can be utilized in cancer research.
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Ferroptosis inducer-3
0 ImagesCat. No.: HY-161760Ferroptosis inducer-3 (compound JB3) is an oral bioactive inhibitor of RAF1, with the IC50 of 226.9 nM. Ferroptosis inducer-3 can induce ferroptosis and plays an important role in cancer research.
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ISIS 5132
0 ImagesCat. No.: HY-153490CAS No.: 177075-18-2Synonyms: CGP 69846A; ISIS 9271ISIS 5132 is a 20-base phosphorothioate oligonucleotide that specifically down-regulates c-raf expression.
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Vemurafenib-d5
0 ImagesCat. No.: HY-12057SCAS No.: 1365986-90-8
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Regorafenib monohydrate (Standard)
0 ImagesSynonyms: BAY 73-4506 monohydrate (Standard)Regorafenib (monohydrate) (Standard) is the analytical standard of Regorafenib (monohydrate). This product is intended for research and analytical applications. Regorafenib (BAY 73-4506) monohydrate 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 monohydrate shows very robust antitumor and antiangiogenic activity.
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(Rac)-Zearalanone-d6
0 ImagesCat. No.: HY-N6678SCAS No.: 1795020-90-4(Rac)-Zearalanone-d6 is the d6-labeled (Rac)-Zearalanone (HY-N6678A). (Rac)-Zearalanone is an ATP-competitive HSP90 inhibitor with an EC50 of 2.3 μM. (Rac)-Zearalanone interferes with the binding of ATP to HSP90, impairs the chaperone function of HSP90, and promotes the degradation of client proteins. (Rac)-Zearalanone reduces intracellular accumulation of Raf-1, induces cleavage of caspase-3, and promotes Her2 degradation in a dose-dependent manner by disrupting the Her2-HSP90 interaction. (Rac)-Zearalanone can be used in the research of small cell lung cancer and breast cancer.
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MEK1/C-Raf-IN-1
0 ImagesCat. No.: HY-157750CAS No.: 946128-76-3MEK1/C-Raf-IN-1 (Compound 14d) is a MEK1/C-Raf inhibitor with IC50 values of 97 and 23 nM, respectively. MEK1/C-Raf-IN-1 has antitumor activity.
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RAF-IN-2
0 ImagesCat. No.: HY-177279CAS No.: 258851-00-2
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EBI-907
0 ImagesCat. No.: HY-117707CAS No.: 1581764-31-9EBI-907 is an orally active and highly potent B-RafV600E inhibitor. EBI-907 demonstrates excellent A375 and Colo-205 cellular antiproliferative activity with IC50 values of 13 nM and 14 nM, respectively. EBI-907 can also cause tumor regression in a B-RafV600E-dependent Colo-205 tumor xenograft model of mice. EBI-907 is promising for research of melanoma and B-RafV600E associated cancers.
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BRAF V600E/CRAF-IN-2
0 ImagesCat. No.: HY-146443CAS No.: 2499499-62-4BRAF V600E/CRAF-IN-2 (Compound 9c) is a potent inhibitor of BRAF V600E/CRAF with IC50s of 0.888 and 0.229 μM, respectively. BRAF V600E/CRAF-IN-2 triggers apoptosis and cell cycle arrest at G0/G1 phase in HCT-116 colon cancer cell. BRAF V600E/CRAF-IN-2 has the potential for the research of cancer diseases.
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Cucurbitacin IIa (Standard)
0 ImagesCat. No.: HY-N1988RCAS No.: 58546-34-2Synonyms: Hemslecin A (Standard)Cucurbitacin IIa (Hemslecin A) (Standard) is the analytical standard for Cucurbitacin IIa (HY-N1988). This product is used for research and analytical applications. Cucurbitacin IIa is an orally active, blood-brain barrier-penetrating EGFR inhibitor with an IC50 of 1.455 nM for human EGFR. Cucurbitacin IIa induces caspase-3 dependent cell apoptosis, downregulates survivin expression, enhances autophagy levels, disrupts the actin cytoskeleton through actin aggregation, blocks the cell cycle at the G2/M phase, and inhibits the EGFR-MAPK signaling pathway to exert anti-inflammatory activity. Cucurbitacin IIa can be used in research on inflammatory-related diseases, depression, and non-small cell lung cancer and other cancers.
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BRAF V600E Recombinant Human Active Protein Kinase
0 ImagesCat. No.: HY-E70649BRAF is a member of the Raf kinase family of growth signal transduction protein kinases. BRAF has multiple mutants. BRAF V600E is commonly found in melanoma. BRAF V600E Recombinant Human Active Protein Kinase is a recombinant BRAF V600E protein that can be used to study BRAF V600E-related functions.
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KRAS-IN-55
0 ImagesCat. No.: HY-181883KRAS-IN-55 is a pan-KRAS inhibitor with IC50 values of 4.3, 9.6 and 1.6 nM against KRASG12C, KRASG12D and KRASG12V, respectively. KRAS-IN-55 induces the formation of a new binding pocket on KRAS, thereby forming a high-affinity ternary complex with cyclophilin A (CYPA), inhibiting the interactions of KRAS with downstream effectors RAF and PI3K, and blocking oncogenic MAPK and PI3K signaling pathways. KRAS-IN-55 is applicable to cancer research such as colorectal cancer and non-small cell lung cancer.
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BRAF V600E/CRAF-IN-1
0 ImagesCat. No.: HY-146442CAS No.: 2499499-56-6
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Erufosine
0 ImagesCat. No.: HY-171777CAS No.: 202867-33-2Synonyms: ErPC3; ErucylphosphohomocholineErufosine is an inhibitor of PI3K/Akt and Ras/Raf/MAPK signaling pathways. Erufosine inhibits the activity of breast cancer cell lines MCF-7 and MDA-MB 231 (IC50: 40.95/40.8 μM). Erufosine reduces the phosphorylation of PI3K (p85), Akt (PKB), and cRaf. Erufosine can be used in the study of breast cancer and myeloid leukemia.
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EGFR/BRAFV600E-IN-1
0 ImagesCat. No.: HY-147825CAS No.: 2492429-45-3EGFR/BRAFV600E-IN-1 (Compound 23) is a potent EGFR and BRAFV600E dual inhibitor with IC50s of 0.08 and 0.15 µM, respectively. EGFR/BRAFV600E-IN-1 induces apoptosis and cell cycle arrest in both pre-G1 and G2/M phases. EGFR/BRAFV600E-IN-1 exhibits antiproliferative activity againist A-549, MCF-7, Panc-1, HT-29 with IC50s of 1.2, 0.79, 1.3, and 1.23 µM, respectively.
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rel-Lifirafenib
0 ImagesCat. No.: HY-18957ACAS No.: 1446090-77-2Synonyms: rel-BGB-283rel-Lifirafenib (rel-BGB-283) is the relative configuration of Lifirafenib (HY-18957). Lifirafenib is a potent Raf Kinase and EGFR inhibitor.
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PQ-1
0 ImagesCat. No.: HY-14584CAS No.: 955995-48-9PQ-1 is a gap junction enhancer.
