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
6854 LY 3009120
Potent pan-Raf kinase 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
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

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.

    External sources of pharmacological information for Raf Kinases :

      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