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-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-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/KDR/Flk-1, VEGFR3/Flt-4, PDGFRβ, FLT3 and c-Kit, respectively. Sorafenib induces autophagy and apoptosis. Sorafenib has anti-tumor activity. Sorafenib is a ferroptosis activator[1].
    Sorafenib-<sup>13</sup>C,d<sub>3</sub>
  • HY-10201S1
    Sorafenib-d4
    		Inhibitor
    Sorafenib-d4 is the deuterium labeled Sorafenib. Sorafenib is a multikinase inhibitor IC50s of 6 nM, 20 nM, and 22 nM for Raf-1, B-Raf, and VEGFR-3, respectively.
    Sorafenib-d<sub>4</sub>
  • 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[4].
    Dabrafenib-d<sub>9</sub>
  • HY-18507A
    AD57 hydrochloride
    		Inhibitor
    AD57 hydrochloride is an orally active multikinase inhibitor, inhibits RET, BRAF, S6K and Src.
    AD57 hydrochloride
  • HY-12847
    CCT241161
    		Inhibitor
    CCT241161 is an orally active pan-RAF inhibitor with IC50s of 3, 6, 10, 15 and 30 nM for LCK, CRAF, SRC, V600E-BRAF and BRAF, respectively. CCT241161 shows good activity to in BRAF and NRAS mutant melanomas. CCT241161 also exhibits anticancer cell proliferative activity.
    CCT241161
  • 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/Flt-1,2, 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-P10436
    Braftide
    		Inhibitor 99.68%
    Braftide is an allosteric inhibitor for BRAF kinase by targeting the dimer interface of BRAF kinase and inhibiting the formation of BRAF dimers. Braftide inhibits wild-type BRAF and oncogenic BRAFG469A with IC50 of 364 nM and 172 nM, respectively. Braftide inhibits MAPK signaling pathway, inhibits proliferation of KRAS mutant tumor cells (EC50 is 7.1 and 6.6 μM, for HCT116 and HCT-15), in combination of TAT sequence.
    Braftide
  • 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, VEGFR2/KDR/Flk-1, 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-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
  • HY-18957B
    Lifirafenib maleate
    		Inhibitor
    Lifirafenib (BGB-283) maleate is a novel and potent Raf Kinase and EGFR inhibitor with IC50 values of 23 and 29 nM for recombinant BRafV600E and EGFR, respectively.
    Lifirafenib maleate
  • HY-150639
    Everafenib
    		Inhibitor
    Everafenib is a potent and blood-brain barrier (BBB) penetrant BRAF inhibitor, also inhibits MAPK signaling. Everafenib has inhibitory activity against a panel of V600EBRAF melanoma cell lines with IC50 values of 2-10 nM, which is better than Dabrafenib (HY-14660) and Vemurafenib (HY-12057). Everafenib has efficacy in an intracranial mouse model of metastatic melanoma.
    Everafenib
  • HY-P10832
    ATWLPPRAANLLMAAS
    		Inhibitor
    ATWLPPRAANLLMAAS is a chimeric peptide with anti-angiogenic and potent anti-tumor effects. ATWLPPRAANLLMAAS can inhibit the proliferation, viability, migration, and invasion of human hepatocellular carcinoma cells, and induce apoptosis..
    ATWLPPRAANLLMAAS
  • HY-156554
    Raf inhibitor 3
    		Inhibitor
    Raf inhibitor 3 (Example 30) is a Raf inhibitor. Raf inhibitor 3 inhibits B-Raf and C-Raf with IC50 values less than 15 nM. Raf inhibitor 3 can be used for research of cancers.
    Raf inhibitor 3
  • HY-156590
    B-Raf IN 16
    		Inhibitor
    B-Raf IN 16 (Compound I) is a BRAF inhibitors that belongs a cyclic iminopyrimidine derivative. B-Raf IN 16 can be used for cancer research.
    B-Raf IN 16
  • HY-10331S1
    Regorafenib-13C,d3
    		Inhibitor
    Regorafenib-13C,d3 is the 13C- and deuterium labeled Regorafenib. Regorafenib (BAY 73-4506) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s 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-<sup>13</sup>C,d<sub>3</sub>
  • HY-120676
    B-Raf IN 18
    		Inhibitor
    B-Raf IN 18 (compound 26) is a B-Raf inhibitor, with IC50 of 3.8 nM. B-Raf IN 18 can be used in anti-cancer related research.
    B-Raf IN 18
Cat. No. Product Name / Synonyms Application Reactivity
Raf Isoform Comparison

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