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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PROTAC BRAF-V600E degrader-2
0 ImagesCat. No.: HY-137488CAS No.: 2417296-82-1PROTAC BRAF-V600E degrader-2 is a PROTAC degrader targeting BRAF-V600E. The Kd values of PROTAC BRAF-V600E degrader-2 for BRAF and BRAF-V600E are 14.4 nM and 9 nM, respectively. PROTAC BRAF-V600E degrader-2 selectively degrades BRAF-V600E but does not degrade wild-type BRAF. PROTAC BRAF-V600E degrader-2 inhibits the MEK/ERK kinase cascade and suppresses the growth of melanoma cells. PROTAC BRAF-V600E degrader-2 can be used in studies related to melanoma and colon cancer.
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EGFR/BRAFV600E-IN-4
0 ImagesCat. No.: HY-173164EGFR/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.
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B-Raf IN 8
0 ImagesCat. No.: HY-147853CAS No.: 1215313-19-1B-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.
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BRAFV600E/ABL2-IN-1
0 ImagesCat. No.: HY-178382BRAFV600E/ABL2-IN-1 is a BRAFV600E (IC50 = 0.088 μM)/ABL2 (IC50 = 0.3 μM) dual inhibitor. BRAFV600E/ABL2-IN-1 can diminish P-glycoprotein expression. BRAFV600E/ABL2-IN-1 effectively inhibits p-CrkL (Abl2 signaling) and p-ERK1/2 (BRAFV600E pathway) in A375-R melanoma cells. BRAFV600E/ABL2-IN-1 causes cell cycle arrest. BRAFV600E/ABL2-IN-1 significantly increases the percentage of late apoptotic cells. BRAFV600E/ABL2-IN-1 can be used for the study of melanoma.
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SJ-C1044
0 ImagesSJ-C1044 is an orally available pan-RAF inhibitor with immunomodulatory and anti-tumor activities. SJ-C1044 inhibits wild-type BRAF, wild-type CRAF, and BRAF (V600E) with IC50 values ??of 331, 257, and 187 nM, respectively. SJ-C1044 inhibits tumor cell proliferation by inhibiting kras activation and MEK-ERK phosphorylation. In addition, SJ-C1044 also has a certain inhibitory effect on VEGFR2, TIE2, and CSF1R, with IC50 values ??of 100, 23, and 235 nM, respectively. SJ-C1044 improves the tumor immune microenvironment by inhibiting angiogenesis and regulating macrophage function. SJ-C1044 can be used in the study of colorectal cancer.
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XL-281
0 ImagesCat. No.: HY-19343CAS No.: 870603-16-0Synonyms: BMS-908662
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RAF-IN-4
0 ImagesCat. No.: HY-177946CAS No.: 1445582-05-7RAF-IN-4 (Compound 120) is a Raf Kinase inhibitor. RAF-IN-4 shows IC50 values of 134.3, 118.6 and 276.7 nM for B-Raf, B-Raf (V600E) and C-Raf. RAF-IN-4 can inhibit the proliferation of cancer cells by blocking the Raf signaling pathway. RAF-IN-4 can be used for research of cancer, such as lung cancer and breast cancer.
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SKLB646
0 ImagesCat. No.: HY-164530CAS No.: 1970149-05-3SKLB646 is an orally active multi-target kinase inhibitor. SKLB646 shows significant inhibitory effects on SRC and VEGFR2 with IC50 values ??of 0.002 μmol/L and 0.012 μmol/L, respectively. SKLB646 also shows significant inhibitory effects on B-Raf and C-Raf with IC50 values ??of 0.022 μmol/L and 0.019 μmol/L, respectively. SKLB646 inhibits the activation of the SRC signaling pathway and blocks the MAPK signaling pathway by inhibiting Raf kinase. In addition, SKLB646 can inhibit the proliferation, migration and invasion of human umbilical vein endothelial cells (HUVEC) to inhibit tumor-induced angiopoietic formation. SKLB646 shows significant anti-proliferative and anti-survival activities against triple-negative breast cancer (TNBC) cell lines.
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Sorafenib tosylate (Standard)
0 ImagesSynonyms: Bay 43-9006 tosylate (Standard)Sorafenib (tosylate) (Standard) (Bay 43-9006 (tosylate) (Standard)) is the analytical standard of Sorafenib (tosylate) (HY-10201A). This product is intended for research and analytical applications. Sorafenib (Bay 43-9006) tosylate 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 tosylate induces cell cycle arrest, autophagy, apoptosis, and PARP cleavage, reduces Bcl-2, Bcl-XL, cyclin D1 levels, and activates Bak and Bax. Sorafenib tosylate inhibits tumor growth and metastasis in mouse and rat models. Sorafenib tosylate 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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B-Raf-IN-21
0 ImagesCat. No.: HY-184875CAS No.: 342434-07-5B-Raf-IN-21 is a B-Raf kinase inhibitor with a Kd of 4.8 nM and an IC50 of 6 nM. B-Raf-IN-21 can be used for the research of stroke.
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PROTAC B-Raf degrader 1 (Standard)
0 ImagesCat. No.: HY-111758RCAS No.: 2364367-27-9PROTAC B-Raf degrader 1 (Standard) is the analytical standard of PROTAC B-Raf degrader 1 (HY-111758). This product is intended for research and analytical applications. PROTAC 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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CG 858-Neg
0 ImagesCat. No.: HY-180329CAS No.: 2417296-83-2CG 858-Neg (compound 13) is a negative control for Thalidomide (HY-14658)-derived PROTAC degraders, targeting BRAF and BRAFV600E with Ki values of 9.5 nM and 14.4 nM, respectively. CG 858-Neg inhibits downstream ERK phosphorylation and suppresses BRAFV600E-driven melanoma (e.g., A375 cells, IC50=492 nM) and colorectal cancer (e.g., HT-29 cells, IC50=459 nM) cells. CG 858-Neg can be used in research related to melanoma and colorectal cancer.
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BRAF ligand-1
0 ImagesCat. No.: HY-41747CAS No.: 2413037-31-5
