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-180154
    EGFR/BRAFV600E-IN-6
    		Inhibitor
    EGFR/BRAFV600E-IN-6 (Compound 7c) is a dual EGFR/BRAFV600E inhibitor with IC50 values of 0.12 and 0.05 μM. EGFR/BRAFV600E-IN-6 can activate caspase-3/8/9, unregulate Bax expression and downregulate Bcl-2 levels. EGFR/BRAFV600E-IN-6 can induce apoptosis and shows antioxidant activity. EGFR/BRAFV600E-IN-6 can be used for the research of cancer, such as colon cancer.
    EGFR/BRAFV600E-IN-6
  • HY-147825
    EGFR/BRAFV600E-IN-1
    		Inhibitor
    EGFR/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.
    EGFR/BRAFV600E-IN-1
  • HY-144271
    RAF-IN-1
    		Inhibitor
    RAF-IN-1 is a RAF inhibitor. RAF-IN-1 suppresses RAF enzymatic activity and reduces cancer cell proliferation. RAF-IN-1 can be used for cancer research.
    RAF-IN-1
  • HY-179098
    Multi-target kinase-IN-8
    		Inhibitor
    Multi-target kinase-IN-8 (3d) is an anti-cancer agent. Multi-target kinase-IN-8 exhibits inhibitory activity against various protein kinases (B-Raf V600E (IC50 = 0.078 µg/mL), c-Met (IC50 = 0.405 µg/mL), Pim-1 (IC50 = 1.053 µg/mL), EGFR WT (IC50 = 0.177 µg/mL), VEGFR-2 (IC50 = 0.275 µg/mL)). Multi-target kinase-IN-8 can induce cell cycle arrest and promote early and late apoptosis. Multi-target kinase-IN-8 is commonly used in cancer research.
    Multi-target kinase-IN-8
  • HY-14716
    CCT239065
    		Inhibitor
    CCT239065 is an orally available, effective inhibitor of the mutant protein kinase V600EBRAF (RAF) with anti-tumor activity. CCT239065 inhibits downstream signaling of V600EBRAF in cancer cells, blocking DNA synthesis and suppressing proliferation.
    CCT239065
  • HY-153914
    B-Raf IN 14
    		Inhibitor
    B-Raf IN 14 (Comp 25) is a BRAF inhibitor with IC50 value of 11.08 μM, which can be used in cancer-related research.
    B-Raf IN 14
  • HY-N13009
    MO-2097
    		Inhibitor
    MO-2097 is a RAF-1/HIF-1α inhibitor. MO-2097 induces RAF-1 destabilization, leading to a reduction in EMT-associated transcription factors and mesenchymal markers. MO-2097 inhibits HIF-1a protein expression mediated by hnRNPA2B1 under hypoxic and mimetic hypoxia. MO-2097 induces mitochondrial ROS, which leads to apoptosis in cells. MO-2097 effectively suppresses colorectal cancer metastasis by inhibiting the RAF/MEK/ERK signaling pathway. MO-2097 attenuates tumor growth in a xenograft HCT116 cell mouse model. MO-2097 can be used for the study of colorectal cancer.
    MO-2097
  • HY-153490C
    ISIS 5132 sodium scrambled negative control
    		Inhibitor
    ISIS 5132 sodium scrambled negative control is the sequence scrambled negative control of ISIS 5132 sodium.
    ISIS 5132 sodium scrambled negative control
  • HY-180327
    NEPP11
    		Inhibitor
    NEPP11 is a cyclopentenone prostaglandin analogue. NEPP11 can inhibit glutamate-induced HT22 cell death in mouse hippocampus and prevent manganese-induced apoptosis in PC12 cells. NEPP11 can activate Nrf2 and maintain MEK1/2 and ERK1/2 activity by inhibiting c-Raf downregulation. NEPP11 exerts a neuroprotective effect in a mouse model of focal cerebral ischemia caused by permanent middle cerebral artery occlusion.
    NEPP11
  • HY-18507A
    AD57 hydrochloride
    		Inhibitor
    AD57 hydrochloride is an orally active multikinase inhibitor, inhibits RET, BRAF, S6K and Src.
    AD57 hydrochloride
  • HY-182749
    KRAS-IN-58
    		Inhibitor
    KRAS-IN-58 is a KRAS inhibitor with a IC50 of 0.223 μM against KRASG12D. KRAS-IN-58 binds to KRASG12C and KRASG12D proteins, and reduces the levels of phosphorylated Raf1, AKT and ERK in pancreatic cancer cells. KRAS-IN-58 can be used for the research of pancreatic cancer.
    KRAS-IN-58
  • HY-135216
    Antiproliferative agent-54
    		Inhibitor
    Antiproliferative agent-54 (Compound 6z) is the inhibitor for multiple kinases, such as ABL WT, B-RAF, EGFR, HCK, LYN A and SRC with IC50 of 6-50 nM. Antiproliferative agent-54 inhibits proliferation of several cancer cell, inhibits HUVEC and HepG2, with EC50 of 34 and 38 nM. Antiproliferative agent-54 exhibits good pharmacokinetic characteristics in rats.
    Antiproliferative agent-54
  • HY-149415
    Multi-kinase-IN-5
    		Inhibitor
    Multi-kinase-IN-5 (compound 15c) is a promising multi-kinase inhibitory agent. Multi-kinase-IN-5 inhibits a panel of protein kinases (RET, KIT, cMet, VEGFR1,2, FGFR1, PDGFR and BRAF), showing % inhibition of 74%, 31%, 62%, 40%, 73%, 74%, 59%, and 69%, respectively, and IC50 of 1.287, 0.117 and 1.185 μM against FGFR1, VEGFR, and RET kinases, respectively.
    Multi-kinase-IN-5
  • HY-180161
    B-Raf-IN-20
    		Inhibitor
    B-Raf-IN-20 (Compound Z-001) is a B-RAF inhibitor with an IC50 value of 37.80 nM. B-Raf-IN-20 binds to DFG-out/C-helix-in conformation in the B-RAF kinase. B-Raf-IN-20 has anti-cancer activity against non-small cell lung cancer.
    B-Raf-IN-20
  • HY-137488
    PROTAC BRAF-V600E degrader-2
    		Inhibitor
    PROTAC BRAF-V600E degrader-2 (compound 12) is a potent BRAF-V600E degrader with Kds of 14.4 nM and 9.5 nM for BRAF and BRAF-V600E, respectively. PROTAC BRAF-V600E degrader-2 selectively degraded the kinase domain of BRAF-V600E but not the wild-type BRAF. PROTAC BRAF-V600E degrader-2 inhibits melanoma cell growth.
    PROTAC BRAF-V600E degrader-2
  • HY-14979
    ML786
    		Inhibitor
    ML786 is a potent and orally bioavailable Raf inhibitor, with IC50s of 2.1, 4.2, and 2.5 nM for V600EΔB-Raf, wt B-Raf, and C-Raf, respectively. ML786 also inhibits Abl-1, DDR2, EPHA2, KDR, and RET (IC50=<0.5, 7.0, 11, 6.2, 0.8 nM). ML786 can be used for the research of cancers.
    ML786
  • HY-103086
    INU-152
    		Inhibitor
    INU-152 is a potent and selective B-Raf inhibitor. INU-152 reduces tumor cell proliferation, enhances autophagy, and induces apoptosis by inhibiting B-Raf activity. INU-152 exhibits significant cytotoxicity against cancer cells transformed with v-Ha-ras (Ras-NIH 3T3). INU-152 can be utilized in cancer research.
    INU-152
  • HY-182763
    EGFR/BRAFV600E-IN-7
    		Inhibitor
    EGFR/BRAFV600E-IN-7 is a dual EGFR and BRAFV600E kinase inhibitor with human IC50 values of 0.12 μM, 0.80 μM, 1.20 μM for EGFR and 0.05 μM, 0.22 μM, 0.78 μM for BRAFV600E.EGFR/BRAFV600E-IN-7 interacts with key ATP-binding site residues of EGFR and BRAFV600E, including hydrogen bonding with EGFR Met769 and BRAFV600E Cys532.EGFR/BRAFV600E-IN-7 induces apoptosis via caspase-3/8/9 activation, modulates Bax and Bcl-2 expression, scavenges free radicals, and exhibits antiproliferative activity against human cancer cell lines.EGFR/BRAFV600E-IN-7 displays drug-likeness with no PAINS/Brenk structural alerts per in silico predictions.EGFR/BRAFV600E-IN-7 can be used for the research of colon cancer, pancreatic cancer, lung cancer, breast cancer.
    EGFR/BRAFV600E-IN-7
  • HY-173164
    EGFR/BRAFV600E-IN-4
    		Inhibitor
    EGFR/BRAFV600E-IN-4 (Compound 10f) is a dual EGFR and BRAFV600E inhibitor with IC50 values of 61 nM and 43 nM, respectively. EGFR/BRAFV600E-IN-4 arrests cell cycle, induces apoptosis in both early and late stages and inhibits cancer cells growth in vitro, and has a broad anticancer activity.
    EGFR/BRAFV600E-IN-4
  • HY-147853
    B-Raf IN 8
    		Inhibitor
    B-Raf IN 8 (compound 7g) is a potent B-Raf inhibitor, with an IC50 of 70.65 nM. B-Raf IN 8 exhibits antitumor activity against hepatocellular carcinoma (HEPG-2), colon carcinoma (HCT-116), mammary gland (MCF-7) and human prostate cancer (PC-3) cells, with IC50 values of 9.78, 13.78, 18.52 and 29.85 µM.
    B-Raf IN 8
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Raf Isoform Comparison

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