B-Raf
B-Raf is a serine/threonine protein kinase encoded by BRAF and functions as a central signal transducer in the RAS-RAF-MEK-ERK signaling cascade that regulates cell proliferation, differentiation, and survival[1][2]. Mechanistically, activated B-Raf phosphorylates MEK, leading to ERK activation and propagation of mitogenic signaling, making B-Raf a critical regulator of MAPK pathway output[2]. Dysregulation of this pathway is strongly linked to oncogenesis, and somatic BRAF mutations are among the most common kinase alterations identified in human cancer, particularly melanoma, colorectal cancer, thyroid cancer, and non-small-cell lung cancer[1][3]. In disease models, the canonical BRAF V600E mutation constitutively activates kinase signaling and promotes tumor cell growth independent of normal upstream regulatory inputs[2][3]. Compared with the related RAF isoforms A-Raf and C-Raf (RAF1), B-Raf displays stronger basal kinase activity and is the most potent activator of MEK-ERK signaling, making it a dominant MAPK pathway driver in many BRAF-mutant tumors[2]. For experimental applications, selective B-Raf inhibitors have been widely used to suppress oncogenic MAPK signaling and to investigate pathway dependence in cancer models[4]. The development of mutation-selective inhibitors, including compounds targeting BRAF V600E, established B-Raf as a validated therapeutic and mechanistic target and continues to support research on signaling regulation, drug resistance, and combination treatment strategies[4][5].
References:
- [1]. Davies H, et al. Mutations of the BRAF gene in human cancer. Nature. 2002 Jun 27;417(6892):949-54. [Content Brief]
- [2]. Wan PT, et al. Mechanism of activation of the RAF-ERK signaling pathway by oncogenic mutations of B-RAF. Cell. 2004 Mar 19;116(6):855-67. [Content Brief]
- [3]. B-Raf gene information from NCBI.
- [4]. Tsai J, et al. Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity. Proc Natl Acad Sci U S A. 2008 Feb 26;105(8):3041-6. [Content Brief]
- [5]. Bollag G, et al. Vemurafenib: the first drug approved for BRAF-mutant cancer. Nat Rev Drug Discov. 2012 Nov;11(11):873-86. [Content Brief]
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B-Raf Related Products (96)
Related Products (96)
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Antibodies (3)
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Lifirafenib
0 ImagesSynonyms: BGB-283Lifirafenib (BGB-283) is a novel and potent Raf Kinase and EGFR inhibitor with IC50 values of 23 and 29 nM for recombinant BRafV600E and EGFR, respectively.
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SJF-0628
0 ImagesSJF-0628 is a PROTAC degrader of BRAF mutants, with a DC50 of 6.8 nM against BRAFV600E. SJF-0628 induces the ubiquitination and degradation of BRAF mutants in various cancer cell lines. SJF-0628 reduces pMEK and pErk levels. SJF-0628 exhibits antitumor activity. SJF-0628 can be used in research on colorectal cancer, melanoma, lung cancer, and triple-negative breast cancer.
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TAK-632
0 ImagesTAK-632 is a potent pan-RAF inhibitor with IC50 of 1.4, 2.4 and 8.3 nM for CRAF, BRAFV600E, BRAFWT, respectively.
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PROTAC BRAF-V600E degrader-1
0 ImagesPROTAC BRAF-V600E degrader-1 is a BRAF-V600E-selective PROTAC degrader and inhibitor. PROTAC BRAF-V600E degrader-1 induces degradation of BRAF-V600E via the cellular ubiquitin proteasome system, sparing wild-type BRAF. PROTAC BRAF-V600E degrader-1 suppresses the MEK/ERK kinase cascade in melanoma cells. PROTAC BRAF-V600E degrader-1 impairs growth of melanoma cells in culture. PROTAC BRAF-V600E degrader-1 can be used for the research of melanoma, colon cancer.
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Sorafenib (Standard)
0 ImagesSynonyms: Bay 43-9006 (Standard)Sorafenib (Standard) (Bay 43-9006 (Standard)) is the analytical standard of Sorafenib (HY-10201). This product is intended for research and analytical applications. Sorafenib (Bay 43-9006) is a potent oral active multikinase inhibitor. Sorafenib blocks autophosphorylation and activity of receptor tyrosine kinases (VEGFR-2, VEGFR-3) and RAF family kinases, thereby suppressing the RAF/MEK/ERK and PI3K/Akt pathways, inhibiting STAT3 phosphorylation, and selectively inhibiting the MAPK pathway in cancer cells. Sorafenib induces cell cycle arrest, autophagy, apoptosis, and PARP cleavage, reduces Bcl-2, Bcl-XL, cyclin D1 levels, and activates Bak and Bax. Sorafenib inhibits tumor growth and metastasis in mouse and rat models. Sorafenib can be used for cancer research, such as colon, breast, non-small-cell lung cancer (NSCLC), ovarian, pancreatic, melanoma, colorectal and hepatocellular carcinoma.
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Mosperafenib
0 ImagesSynonyms: RG6344; RO7276389; B-Raf IN 2BRAF inhibitor. RG6344 can be used for the study of BRAF V600-mutant solid tumors, such as colorectal cancer (CRC).
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PROTAC B-Raf degrader 1
0 ImagesPROTAC B-Raf degrader 1 is a PROTAC degrader targeting B-Raf, which recruits the ubiquitin-proteasome system to accelerate B-Raf degradation and reduce the expression of downstream Mcl-1. PROTAC B-Raf degrader 1 inhibits cancer cell proliferation, arrests cell cycle and induces apoptosis. PROTAC B-Raf degrader 1 can be used in breast cancer-related research.
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Tinlorafenib
0 ImagesSynonyms: PF-07284890; ARRY-461Tinlorafenib (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.
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N-Feruloyloctopamine
0 ImagesSynonyms: N-trans-FeruloyloctopamineN-trans-feruloyloctopamine is a natural hydroxycinnamic acid amide compound derived from garlic outer skin, possessing tyrosinase inhibition, FGF2 inhibition, anti-melanogenic, and anti-tumor activities. N-trans-feruloyloctopamine inhibits tyrosinase activity and downregulates tyrosinase mRNA and protein expression (IC50 = 5.3 μM), and inhibits melanogenesis in α-MSH-stimulated B16F10 cells. N-trans-feruloyloctopamine inhibits Akt and p38 MAPK phosphorylation, binds to E-cadherin to block EMT, reduces Slug, inhibits hepatocellular carcinoma invasion, and induces hepatocellular carcinoma cell apoptosis. N-trans-feruloyloctopamine can be used in research related to hepatocellular carcinoma, pigmentation disorders, and UVB-induced skin damage.
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Omzirafenib
0 ImagesCat. No.: HY-111940CAS No.: 2274819-46-2Synonyms: LUT014Omzirafenib (LUT014) is a topical inhibitor targeting BRAF that cannot pass through the blood-brain barrier. Omzirafenib 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. Omzirafenib is independent of RAS signaling and accelerates the repair and regeneration of damaged skin cells. Omzirafenib can be used to study radiation dermatitis, especially skin damage caused by breast cancer radiotherapy.
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BRAF inhibitor
0 ImagesCat. No.: HY-10247CAS No.: 918505-61-0BRAF inhibitor (Compound P-0850) is a B-Raf inhibitor with anti-tumor activity.
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BI-882370
0 ImagesBI-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.
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HG6-64-1
0 ImagesSynonyms: HMSL 10017-101-1HG6-64-1 (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).
