Raf
RAF kinases act downstream of RAS and relay signals through the RAF-MEK-ERK/MAPK cascade to regulate cell growth, survival, and differentiation[1]. Mechanistically, RAF activation depends on phosphorylation, conformational control, membrane recruitment, and kinase-domain dimerization, which provides an allosteric mechanism for catalytic activity[1]. In cancer models, mutant BRAF tumors depend on RAF-MEK-ERK signaling, whereas ATP-competitive RAF inhibitors inhibit ERK signaling in mutant BRAF cells but enhance signaling in wild-type BRAF cells through RAF dimer transactivation[2]. Compared with related isoforms, BRAF has the highest basal kinase activity, while ARAF shows a cell-type-dependent role in MAPK activity and cell migration[3]. CRAF/RAF1 differs further because KRAS-mutant tumor subsets depend on CRAF growth functions, and kinase-dead but not dimer-defective CRAF rescues growth inhibition[4]. For experimental applications, RAF inhibitors therefore serve as pathway probes, but study design should distinguish mutant BRAF inhibition from wild-type RAF dimer activation[2][5].
References:
- [1]. Lavoie H, et al. Regulation of RAF protein kinases in ERK signalling. Nat Rev Mol Cell Biol. 2015 May;16(5):281-98. [Content Brief]
- [2]. Poulikakos PI, et al. RAF inhibitors transactivate RAF dimers and ERK signalling in cells with wild-type BRAF. Nature. 2010 Mar 18;464(7287):427-30. [Content Brief]
- [3]. Mooz J, et al. Dimerization of the kinase ARAF promotes MAPK pathway activation and cell migration. Sci Signal. 2014 Aug 5;7(337):ra73. [Content Brief]
- [4]. Venkatanarayan A, et al. CRAF dimerization with ARAF regulates KRAS-driven tumor growth. Cell Rep. 2022 Feb 8;38(6):110351. [Content Brief]
- [5]. Karoulia Z, et al. An Integrated Model of RAF Inhibitor Action Predicts Inhibitor Activity against Oncogenic BRAF Signaling. Cancer Cell. 2016 Sep 12;30(3):485-498. [Content Brief]
-
Raf Related Products (120)
Related Products (120)
-
Antibodies (2)
-
CCT239065
0 ImagesCat. No.: HY-14716CAS No.: 1163719-51-4
-
B-Raf IN 14
0 ImagesCat. No.: HY-153914CAS No.: 326918-98-3B-Raf IN 14 (Comp 25) is a BRAF inhibitor with IC50 value of 11.08 μM, which can be used in cancer-related research.
-
MO-2097
0 ImagesCat. No.: HY-N13009CAS No.: 2744300-63-6MO-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.
-
RAF1 YDYD Recombinant Human Active Protein Kinase
0 ImagesCat. No.: HY-E70765Ras-associated factor -1 (RAF1) belongs to the RAF protein kinases family, also known as C-Raf. RAF1 participates in Ras-RAF-MEK-ERk signaling pathway (MAPK signaling pathway), and transmits extracellular signals into the nucleus through cell membrane receptors, thereby mediating the expression of intracellular specific proteins and participating in the regulation of cell proliferation, differentiation, apoptosis, autophagy and other functions. RAF1 YDYD is a mutant of RAF1. RAF1 YDYD Recombinant Human Active Protein Kinase is a recombinant RAF1 YDYD protein that can be used to study RAF1 YDYD-related functions.
-
ISIS 5132 sodium scrambled negative control
0 ImagesCat. No.: HY-153490CISIS 5132 sodium scrambled negative control is the sequence scrambled negative control of ISIS 5132 sodium.
-
AD57 hydrochloride
0 ImagesCat. No.: HY-18507ACAS No.: 2320261-72-9
-
Antiproliferative agent-54
0 ImagesCat. No.: HY-135216CAS No.: 1240322-54-6Antiproliferative 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.
-
ML786
0 ImagesCat. No.: HY-14979CAS No.: 1237586-97-8
-
INU-152
0 ImagesCat. No.: HY-103086CAS No.: 1380228-30-7INU-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.
-
BJ-2302
0 ImagesCat. No.: HY-182614CAS No.: 1631056-29-5BJ-2302 is a Src kinase inhibitor with an IC50 of 3.23 μM, and inhibits cathepsin S (CTSS) activity.BJ-2302 binds to Src, suppresses PI3K/AKT and Ras/Raf/ERK pathways, and reduces CTSS and MMP-9 expression.BJ-2302 inhibits cancer cell invasion, metastasis, proliferation, and tumor growth.BJ-2302 does not induce cytotoxicity in normal breast epithelial cells.BJ-2302 can be used for the research of breast cancer and triple-negative breast cancer.
-
Lifirafenib maleate
0 ImagesCat. No.: HY-18957BCAS No.: 1854985-74-2Synonyms: BGB-283 maleateLifirafenib (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.
-
ATWLPPRAANLLMAAS
0 ImagesCat. No.: HY-P10832CAS No.: 1228447-26-4ATWLPPRAANLLMAAS 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..
-
Raf inhibitor 3
0 ImagesCat. No.: HY-156554CAS No.: 1662682-11-2Raf 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.
-
Regorafenib N-oxide and N-desmethyl (M5)-d3-1
0 ImagesCat. No.: HY-W709612Synonyms: N-Desmethyl regorafenib N-oxide-d3-1Regorafenib N-oxide and N-desmethyl (M5)-d3-1 (N-Desmethyl regorafenib N-oxide-d3-1) is the deuterium labeled Regorafenib N-oxide and N-desmethyl (M5) (HY-108226). Regorafenib N-oxide and N-desmethyl (M5) (N-Desmethyl regorafenib N-oxide) is an active metabolite of Sorafenib (HY-10201) and can be metabolized by CYP3A4.
-
Regorafenib-13C,d3
0 ImagesCat. No.: HY-10331S1Synonyms: BAY 73-4506-13C,d3
-
CP-724714 succinate
0 ImagesCat. No.: HY-14674ACAS No.: 543681-31-8CP-724714 succinate is an orally active and selective HER2 tyrosine kinase inhibitor with an IC50 of 10 nM. CP-724714 succinate inhibits HER2 receptor autophosphorylation and blocks the downstream Ras-Raf-Mek-Erk signaling pathway, thereby inducing cell cycle arrest and apoptosis in tumor cells. CP-724714 succinate exhibits antiviral activity and inhibits various porcine diarrheal coronaviruses, including SADS-CoV (IC50 of 0.91 μM). CP-724714 succinate is an inhibitor of the hepatic transport receptors OATP1B1/MDR1/BSEP, and can enter hepatocytes via active uptake and trigger the accumulation of drugs and bile acids within hepatocytes. CP-724714 succinate can be used in research related to HER2-overexpressing breast cancer and porcine diarrheal coronavirus infection.
-
Doramapimod (Standard)
0 ImagesSynonyms: BIRB 796 (Standard)Doramapimod (Standard) is the analytical standard of Doramapimod. This product is intended for research and analytical applications. Doramapimod (BIRB 796) is an orally active, highly potent p38 MAPK inhibitor, which has an IC50 for p38α=38 nM, for p38β=65 nM, for p38γ=200 nM, and for p38δ=520 nM. Doramapimod has picomolar affinity for p38 kinase (Kd=0.1 nM). Doramapimod also inhibits B-Raf with an IC50 of 83 nM.
-
CRBN ligand-186
0 ImagesCat. No.: HY-174249CAS No.: 3084710-09-5
