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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
Gene Data

Raf Kinase 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
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
7309 Vemurafenib
Potent BRAF and CRAF inhibitor

Degraders
Cat. No. Product Name / Activity
7427 CG 858
Selective BRAF-V600E protein Degrader
7745 CST 905
Potent and selctive BRAFV600E Degrader (PROTAC®)
7463 SJF 0628
Potent BRAF kinase Degrader

Controls
Cat. No. Product Name / Activity
7428 CG 858-Neg
Negative control for CG 858
7464 SJF 0661
Negative control for SJF 0628 (Cat. No. 7463)

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 :

    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