Raf kinases, a family of three serine/threonine kinases, are part of the Ras-MAPK signaling cascade and phosphorylate MEK. Upon growth factor stimulation, Raf-1 (c-Raf) is activated by GTP-bound Ras and recruited to the cell membrane. This activation process is tightly regulated.
Inhibitors |
Cat. No. | Product Name / Activity |
---|---|
4836 | AZ 628 |
Potent Raf kinase inhibitor | |
7223 | Dabrafenib mesylate |
Potent and selective B-Raf, CDK16 and NEK9 inhibitor; anticancer; also targets human proteins in the SARS-CoV-2 interactome | |
4453 | GDC 0879 |
Potent B-Raf inhibitor | |
1381 | GW 5074 |
Potent, selective c-Raf1 kinase inhibitor | |
5260 | KG 5 |
PDGFRβ, B-Raf, c-Raf, FLT3 and KIT inhibitor | |
6854 | LY 3009120 |
Potent pan-Raf kinase inhibitor | |
6015 | RAF 265 |
Raf kinase and VEGFR-2 inhibitor | |
2650 | SB 590885 |
Potent B-Raf inhibitor | |
6814 | Sorafenib |
Potent Raf-1 inhibitor; also inhibits VEGFR-2, VEGFR-3, PDGFR-β, Flt-3 and cKIT | |
1321 | ZM 336372 |
Potent, selective c-Raf inhibitor |
Raf kinases, a family of three serine/threonine kinases, are part of the Ras-MAPK signaling cascade and phosphorylate MEK. Upon growth factor stimulation, Raf-1 (or c-Raf) is activated by GTP-bound Ras and recruited to the cell membrane. This activation process is tightly regulated by a number of factors including phosphatases (e.g. PP1, PP2A, PP5), kinases (e.g. Src, ERK, Akt, PKC) and proteins that bind directly to Raf-1 (e.g. RKIP, 14-3-3ζ, KSR, Hsp90).
Raf-1 is also thought to be able to dimerize with wild type B-Raf in a Ras-dependent process. B-Raf is commonly mutated and thereby activated in many human cancers, the most frequent mutation being the V600E mutation of the kinase domain. Whilst wild type B-Raf and Raf-1 are strongly activated by growth factor signals via Ras and Src, a-Raf is only modestly activated and has low basal activity. All three isoforms of Raf are considered to be oncogenic.
Tocris offers the following scientific literature for Raf Kinases to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Gene | Species | Gene Symbol | Gene Accession No. | Protein Accession No. |
---|---|---|---|---|
c-Raf/Raf1 | Human | RAF1 | NM_002880 | P04049 |
Mouse | Raf1 | NM_007658 | P48964 | |
Rat | Raf1 | NM_012639 | P11345 | |
a-Raf | Human | ARAF | NM_001654 | P10398 |
Mouse | Araf | NM_009703 | P04627 | |
Rat | Araf | NM_022532 | P14056 | |
b-Raf | Human | BRAF | NM_004333 | P15056 |
Mouse | Braf | NM_139294 | P28028 | |
Rat | Braf | AF352172 | Q99MC6 |