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-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
  • HY-141868
    SB-682330A
    SB-682330A is a Raf kinase inhibitor.
    SB-682330A
  • HY-175831
    BRAFV600E-IN-2
    		Inhibitor
    BRAFV600E-IN-2 is a BRAF V600E inhibitor with IC50 ≤10 nM. BRAFV600E-IN-2 has anti-tumor activity.
    BRAFV600E-IN-2
  • HY-149517
    EGFR/BRAFV600E-IN-2
    		Inhibitor
    EGFR/BRAFV600E-IN-2 (compound 3g) is a potential multi-target inhibitor of EGFR, BRAFV600E, and EGFRT790M, and an inducer of apoptosis. EGFR/BRAFV600E-IN-2 can activate caspase-3, 8, and Bax, and downregulate the anti-apoptotic protein Bcl2, inducing apoptosis. EGFR/BRAF V600E-IN-2 also has antioxidant activity and DPPH free radical scavenging potency.
    EGFR/BRAFV600E-IN-2
  • HY-12057S1
    Vemurafenib-d7
    		Inhibitor
    Vemurafenib-d7 is deuterium labeled Vemurafenib. Vemurafenib (PLX4032) is a first-in-class, selective, potent inhibitor of B-RAF kinase, with IC50s of 31 and 48 nM for RAFV600E and c-RAF-1, respectively. Vemurafenib induces cell autophagy.
    Vemurafenib-d<sub>7</sub>
  • HY-10201S4
    Sorafenib-d3 tosylate
    		Inhibitor
    Sorafenib-d3 (Donafenib-d3) tosylate is the deuterium labeled Sorafenib (HY-10201). Sorafenib is a potent and orally active Raf inhibitor with IC50s of 6 nM and 20 nM for Raf-1 and B-Raf, respectively. Sorafenib-d3tosylate 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-d3tosylate induces autophagy and apoptosis. Sorafenib-d3tosylate has anti-tumor activity. Sorafenib is a ferroptosis activator.
    Sorafenib-d<sub>3</sub> tosylate
  • HY-147854
    B-Raf IN 9
    		Inhibitor
    B-Raf IN 9 (compound 8b) is a potent B-Raf inhibitor, with an IC50 of 24.79 nM. B-Raf IN 9 induces apoptosis and shows cell cycle arrest at G2/M phase. B-Raf IN 9 exhibits potent antitumor activity against human prostate cancer PC-3 cell line, with an IC50 of 7.83 µM.
    B-Raf IN 9
  • HY-RS11620
    Raf1 Mouse Pre-designed siRNA Set A
    		Inhibitor

    Raf1 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Raf1 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Raf1 Mouse Pre-designed siRNA Set A
  • HY-175435
    CST905
    		Degrader
    CST905 is a potent PROTAC degrader of BRAF-V600E with a DC50 of 18 nM. CST905 is suitable for cancer research. (Structure Note: Pink: target protein ligand (HY-41747); Blue: E3 ligase ligand (HY-125845); Black: linker (HY-78378)).
    CST905
  • HY-146491
    VEGFR-2/BRAF-IN-1
    		Inhibitor
    VEGFR-2/BRAF-IN-1 (Compound 4b) is a dual VEGFR-2 and BRAF kinases inhibitor with IC50 values of 0.049, 0.063 and 0.005 µM against VEGFR-2, BRAFV600E and BRAFWT, respectively. VEGFR-2/BRAF-IN-1 induces apoptosis and arrests the cell cycle mainly in the G1/S phase.
    VEGFR-2/BRAF-IN-1
  • HY-113632
    Debromohymenialdisine
    Debromohymenialdisine (10Z-Debromohymenialdisine) is a pyrrole alkaloid. Debromohymenialdisine has moderate inhibitory activity with an IC50 value of 881 nM in the initial Raf/MEK-1/MAPK signaling cascade assay. Debromohymenialdisine can be used for the research of proliferation and differentiation.
    Debromohymenialdisine
  • HY-158027
    B-Raf IN 17
    		Inhibitor
    B-Raf IN 17 (Compound 8e) is a potent and orally active type II multi-kinase inhibitor. B-Raf IN 17 exhibits potent cellular-level suppression of BRAFWT, VEGFR-2, and FGFR-1 in A375 cell line, with IC50 values of 0.02, 0.18 and 1.65 μM, respectively. B-Raf IN 17 can be used for the research of cancer.
    B-Raf IN 17
  • HY-RS11621
    Raf1 Rat Pre-designed siRNA Set A
    		Inhibitor

    Raf1 Rat Pre-designed siRNA Set A contains three designed siRNAs for Raf1 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Raf1 Rat Pre-designed siRNA Set A
  • HY-147852
    B-Raf IN 7
    		Inhibitor
    B-Raf IN 7 (compound 6a) is a potent B-Raf inhibitor, with an IC50 of 110.23 nM. B-Raf IN 7 exhibits antitumor activity against colon carcinoma (HCT-116), mammary gland (MCF-7), hepatocellular carcinoma (HEPG-2), human cervical carcinoma (Hela) and human prostate cancer (PC-3) cells, with IC50 values of 7.50, 9.87, 10.57, 11.63 and 12.83 µM.
    B-Raf IN 7
  • HY-153858
    PHI-501
    		Inhibitor
    PHI-501 is a dual inhibitor targeting RAF/DDR. PHI-501 exhibits significant anti-proliferative effects in melanoma cell lines and significantly inhibits the colony formation of drug-resistant cells. PHI-501 strongly inhibits ERK and AKT phosphorylation. PHI-501 downregulates the gene sets in drug-resistant cells of TNFA-NFKB, IL6-JAK-STAT3, and KRAS signaling pathways as well as the epithelial-mesenchymal transition (EMT) signaling pathways. PHI-501 demonstrates significant anti-tumor effects in the SK-MEL3DR xenograft model. PHI-501 can be used for research on the problem of drug resistance in melanoma.
    PHI-501
  • HY-179012
    CDC20/HSP90-IN-1
    		Modulator
    CDC20/HSP90-IN-1 (Compound 2b) is a Cdc20/Hsp90 inhibitor with a Kd of 16.2 μM for Cdc20 and a Kd of 0.241 μM for Hsp90α. CDC20/HSP90-IN-1 exerts potent antitumor activity through reducing p53-mediated Cdc20, upregulating Bim, downregulating Cyclin B1 expression, and disturbing B-Raf and AKT pathways via destroying Hsp90 chaperone function. CDC20/HSP90-IN-1 overcomes Vemurafenib (HY-12057)-induced resistant melanoma.
    CDC20/HSP90-IN-1
  • HY-172877
    EGFR/BRAFV600E-IN-5
    		Inhibitor
    EGFR/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.
    EGFR/BRAFV600E-IN-5
  • HY-169869
    pan-Raf/RTK inhibitor 1
    		Inhibitor
    Pan-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.
    pan-Raf/RTK inhibitor 1
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Raf Isoform Comparison

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