1. Signaling Pathways
  2. MAPK/ERK Pathway
  3. Raf

Raf

Raf kinases

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-114491
    Rineterkib
    Inhibitor 98.79%
    Rineterkib (compound B) is an orally available ERK1 and ERK2 inhibitor in the treatment of a proliferative disease characterized by activating mutations in the MAPK pathway. The activity is particularly related to the treatment of KRAS-mutant NSCLC, BRAF-mutant NSCLC, KRAS-mutant pancreatic cancer, KRAS-mutant colorectal cancer (CRC) and KRAS-mutant ovarian cancer. Rineterkib hydrochloride can also inhibit RAF.
    Rineterkib
  • HY-12846
    CCT196969
    Inhibitor 99.67%
    CCT196969 is a pan-Raf inhibitor, which inhibits B-Raf, BRafV600E and CRAF with IC50s of 0.1, 0.04, and 0.01 μM, respectively.
    CCT196969
  • HY-10320A
    Doramapimod hydrochloride
    Inhibitor 98.29%
    Doramapimod hydrochloride (BIRB 796 hydrochloride) is an anti-inflammatory compound with biological activity through inhibition of p38 MAPK. Doramapimod hydrochloride can significantly inhibit the activities of TNF-α and IL-1β induced by LPS, LTA and PGN. Doramapimod hydrochloride showed a stronger inhibitory effect on inflammation induced by all three bacterial toxins, which was more significant compared with the effects of other compounds. Doramapimod hydrochloride can be used in the research of autoimmune diseases.
    Doramapimod hydrochloride
  • HY-147405
    Tinlorafenib
    Inhibitor 98.21%
    Tinlorafenib (PF-07284890) is the orally active inhibitor for BRAF and CRAF with IC50s of 5.8 nM and 4.1 nM. Tinlorafenib (Compound 10) inhibits V600E mutated BRAF and V600K mutanted BRAF with IC50s of 4.25 nM and 2.7 nM. Tinlorafenib can cross the blood brain barrier. Tinlorafenib demonstrates CNS penetration and can be used in the research of BRAF-associated malignant and benign tumors of the CNS as well as extracranial malignancies.
    Tinlorafenib
  • HY-100510
    RAF709
    Inhibitor 99.92%
    RAF709 is a potent, selective, and efficacious RAF inhibitor with IC50s of 0.4 nM and 0.5 nM for BRAF and CRAF, respectively. Antitumor efficacy.
    RAF709
  • HY-18997
    PLX7904
    Inhibitor 98.72%
    PLX7904 is a potent and selective BRAF inhibitor, with IC50 of appr 5 nM against BRAFV600E in mutant RAS expressing cells.
    PLX7904
  • HY-10247
    BRAF inhibitor
    Inhibitor 98.07%
    BRAF inhibitor (Compound P-0850) is a B-Raf inhibitor with anti-tumor activity.
    BRAF inhibitor
  • HY-136567
    TBAP-001
    Inhibitor 98.97%
    TBAP-001 (Synthesis 13), extracted from patent WO2015075483A1, is a pan-RAF kinase inhibitor, with an IC50 of 62 nM in BRAF V600E kinase assay.
    TBAP-001
  • HY-12787
    L-779450
    Inhibitor 98.75%
    L-779450 is a potent and selective B-Raf kinase inhibitor with a Kd of 2.4 nM.
    L-779450
  • HY-77113
    B-Raf IN 11
    Inhibitor 99.46%
    B-Raf IN 11 is a B-RafV600E mutant kinase inhibitor with an IC50 of 76 nM, and exhibits an IC50 of 238 nM against wild-type B-Raf kinase. B-Raf IN 11 inhibits the kinase activities of B-RafV600E mutant and wild-type B-Raf kinase. B-Raf IN 11 is applicable to relevant research on colorectal cancer.
    B-Raf IN 11
  • HY-123673
    MCP110
    Inhibitor 99.82%
    MCP110 is an inhibitor of Ras/Raf-1 interaction. MCP110 blocks the interaction of Ras with Raf. MCP110 disrupts this interaction might can be used for the research of human tumors.
    MCP110
  • HY-111940
    LUT014
    Inhibitor
    LUT014 is a topical inhibitor targeting BRAF that cannot pass through the blood-brain barrier. LUT014 inhibits BRAF kinase and abnormally activates the MAPK/ERK signaling pathway, promoting the proliferation of epidermal keratinocytes, repairing skin barrier damage caused by radiation damage, and alleviating inflammatory responses. LUT014 is independent of RAS signaling and accelerates the repair and regeneration of damaged skin cells. LUT014 can be used to study radiation dermatitis, especially skin damage caused by breast cancer radiotherapy.
    LUT014
  • HY-107779
    BI-882370
    Inhibitor 98.55%
    BI-882370 is a potent and selective RAF kinase inhibitor that binds to the ATP binding site of the kinase positioned in the DFG-out (inactive) conformation of the BRAF kinase. BI-882370 (BI 882370) inhibits the oncogenic BRAFV600E-mutant, the WT BRAF and CRAF kinases with IC50s of 0.4, 0.8, and 0.6 nM, respectively. BI-882370 also inhibits SRC family kinases.
    BI-882370
  • HY-159534
    Flezurafenibum
    Inhibitor 99.85%
    Flezurafenibum (Flezurafenib) is a rapidly accelerated fibrosarcoma (Raf) kinase inhibitor, with antineoplastic effect.
    Flezurafenibum
  • HY-117737A
    RRD-251
    Inhibitor 99.87%
    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-12291
    HG6-64-1
    Inhibitor 99.69%
    HG6-64-1 (HMSL 10017-101-1) is a B-raf kinase modulator.HG6-64-1 modulates B-raf kinase activity, including the V600E mutant form and the drug-resistant gatekeeper mutation T529I. HG6-64-1 is a germinal center kinase inhibitor. HG6-64-1 induces cell cycle arrest and apoptosis. HG6-64-1 can be used for the research of diffuse large B-cell lymphoma (DLBCL).
    HG6-64-1
  • HY-P10438
    TAT-Braftide
    Inhibitor 99.52%
    TAT-Braftide is a peptide inhibitor designed to block the dimerization of BRAF, thereby inhibiting its kinase activity. The destruction of BRAF dimer by TAT-Braftide makes BRAF protein more susceptible to proteasome degradation, directly inhibits the activity of BRAF kinase, and reduces the activation of MAPK signaling pathway. Tat-braftide can be used for the role of RAF kinase in MAPK signaling pathway and for the study of BRAF mutant cancers.
    TAT-Braftide
  • HY-148059
    Uplarafenib
    Inhibitor 99.63%
    Uplarafenib (B-Raf IN 10) (Compound C09) is a BRAF inhibitor with an IC50 between 50 and 100 nM. Uplarafenib shows antitumor activity.
    Uplarafenib
  • HY-150023
    BI-1622
    Inhibitor 98.02%
    BI-1622 is an orally active, potent and highly selective HER2 (ERBB2) inhibitor, with an IC50 of 7 nM. BI-1622 shows greater than 25-fold selectivity over EGFR. BI-1622 shows high antitumor efficacy in vivo in xenograft mouse tumor models with engineered H2170 and PC9 cells and had a favorable agent metabolism and pharmacokinetics profile.
    BI-1622
  • HY-18507
    AD57
    Inhibitor 98.27%
    AD57 is an orally active multikinase inhibitor, inhibits RET, BRAF, S6K and Src, with greatly reduces mTOR activity.
    AD57
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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