Raf Kinases

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.

Products
Background
Literature
Gene Data

Inhibitors

Cat No Product Name / Activity
4836 AZ 628
Potent Raf kinase inhibitor
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
5036 ML 786 dihydrochloride
Potent Raf kinase inhibitor; orally bioavailable
6015 RAF 265
Raf kinase and VEGFR-2 inhibitor
2650 SB 590885
Potent B-Raf inhibitor
1321 ZM 336372
Potent, selective c-Raf inhibitor

Other

Cat No Product Name / Activity
5475 Kobe 0065
H-Ras-cRaf1 interaction inhibitor; inhibits Raf signaling

Related Targets

    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.

    Literature for Raf Kinases

    Tocris offers the following scientific literature for Raf Kinases to showcase our products. We invite you to request* or download your copy today!

    *Please note that Tocris will only send literature to established scientific business / institute addresses.


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    Raf Kinase Gene Data

    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