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.
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) | |
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 |