1. MAPK/ERK Pathway
  2. Raf

Raf

Raf kinases are a family of three serine/threonine-specific protein kinases that are related to retroviral oncogenes. RAF is an acronym for Rapidly Accelerated Fibrosarcoma. Raf kinases participate in the RAS-RAF-MEK-ERK signal transduction cascade, also referred to as the mitogen-activated protein kinase (MAPK) cascade. Activation of RAF kinases requires interaction with RAS-GTPases. The three RAF kinase family members are: A-Raf, B-Raf, C-Raf (Raf-1). The B-Raf protein is involved in sending signals inside cells, which are involved in directing cell growth. It was shown to be faulty (mutated) in some human cancers. C-RAF or even Raf-1 is an enzyme that in humans is encoded by the RAF1 gene. The c-Raf protein is part of the ERK1/2 pathway as a MAP kinase kinase kinase (MAP3K) that functions downstream of the Ras subfamily of membrane associated GTPases. C-Raf is a member of the Raf kinase family of serine/threonine-specific protein kinases, from the TKL (Tyrosine-kinase-like) group of kinases.

Raf Related Products (131):

Cat. No. Product Name Effect Purity
  • HY-14660
    Dabrafenib Inhibitor
    Dabrafenib (GSK2118436A) is an ATP-competitive inhibitor of Raf with IC50s of 5 nM and 0.6 nM for C-Raf and B-RafV600E, respectively[4].
  • HY-12057
    Vemurafenib Inhibitor 99.83%
    Vemurafenib (PLX4032) is a first-in-class, selective, potent inhibitor of B-RAF kinase, with IC50s of 31 and 48 nM for RAFV600E and c-RAF-1, respectively[1][4]. Vemurafenib induces cell autophagy[5].
  • HY-10320
    Doramapimod Inhibitor 99.98%
    Doramapimod (BIRB 796) is an orally active, highly potent p38 MAPK inhibitor, which has an IC50 for p38α=38 nM, for p38β=65 nM, for p38γ=200 nM, and for p38δ=520 nM. Doramapimod has picomolar affinity for p38 kinase (Kd=0.1 nM). Doramapimod also inhibits B-Raf with an IC50 of 83 nM[1][2].
  • HY-10201
    Sorafenib Inhibitor 99.92%
    Sorafenib (Bay 43-9006) is a potent and orally active Raf inhibitor with IC50s of 6 nM and 20 nM for Raf-1 and B-Raf, respectively. Sorafenib is a multikinase inhibitor with IC50s of 90 nM, 15 nM, 20 nM, 57 nM and 58 nM for VEGFR2, VEGFR3, PDGFRβ, FLT3 and c-Kit, respectively. Sorafenib induces autophagy and apoptosis. Sorafenib has anti-tumor activity. Sorafenib is a ferroptosis activator[1].
  • HY-10331
    Regorafenib Inhibitor 99.93%
    Regorafenib (BAY 73-4506) is an orally active and potent multi-targeted receptor tyrosine kinase inhibitor, with IC50 values of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively. Regorafenib shows very robust antitumor and antiangiogenic activity[1].
  • HY-120676
    B-Raf IN 18 Inhibitor
    B-Raf IN 18 (compound 26) is a B-Raf inhibitor, with IC50 of 3.8 nM. B-Raf IN 18 can be used in anti-cancer related research[1].
  • HY-19343
    XL-281 Inhibitor
    XL-281 (BMS-908662) is an orally active inhibitor for RAF kinase, with IC50s of 2.6, 4.5 and 6 nM, for CRAF, B-RAF, and B-RAFV600E, respectively. XL-281 exhibits antitumor activity[1].
  • HY-P10436
    Braftide Inhibitor
    Braftide is an allosteric inhibitor for BRAF kinase by targeting the dimer interface of BRAF kinase and inhibiting the formation of BRAF dimers. Braftide inhibits wild-type BRAF and oncogenic BRAFG469A with IC50 of 364 nM and 172 nM, respectively. Braftide inhibits MAPK signaling pathway, inhibits proliferation of KRAS mutant tumor cells (EC50 is 7.1 and 6.6 μM, for HCT116 and HCT-15), in combination of TAT sequence[1].
  • HY-148059
    Uplarafenib Inhibitor 99.15%
    Uplarafenib (B-Raf IN 10) (Compound C09) is a BRAF inhibitor with an IC50 between 50 and 100 nM. Uplarafenib shows antitumor activity[1].
  • HY-137487
    PROTAC BRAF-V600E degrader-1 Inhibitor 98.02%
    PROTAC BRAF-V600E degrader-1 is a potent PROTAC BRAF-V600E degrader with Kd value of 2.4 nM and 2 nM for BRAF and BRAF-V600E, respectively. PROTAC BRAF-V600E degrader-1 degrades BRAF-V600E via the ubiquitin-proteasome system (UPS). PROTAC BRAF-V600E degrader-1 can inhibit melanoma cell growth[1].
  • HY-153603
    B-Raf IN 15 Inhibitor
    B-Raf IN 15 (Compound 7) is a BRAF inhibitor. B-Raf IN 15 inhibits BRAF WT and BRAF V600E with IC50s of 2.0 and 0.8 μM. B-Raf IN 15 can be used for the research of cancer[1].
  • HY-153490A
    ISIS 5132 sodium Inhibitor
    ISIS 5132 sodium is a 20-base phosphorothioate oligonucleotide that specifically down-regulates c-raf expression.
  • HY-115933
    EGFR/BRAF-IN-1 Inhibitor
    EGFR/BRAF-IN-1 (compound 21), a 2,3-dihydropyrazino[1,2-a]indole-1,4-dione derivative, is a potent EGFR/BRAF inhibitor with an IC50 of 45 nM for BRAFV600E. EGFR/BRAF-IN-1 inhibits cancer cell proliferation (GI50=35 nM). EGFR/BRAF-IN-1 shows good antioxidant activity[1].
  • HY-146432
    Antitumor agent-60 Inhibitor
    Antitumor agent-60 (compound 20) is a potent antitumor agent, targeting RAS-RAF signaling pathway and binding to CRAF with a Kd value of 3.93 μM. Antitumor agent-60 induces apoptosis by blocking cell cycle at G2/M phase. Antitumor agent-60 enhances the level of p53 and ROS. Antitumor agent-60 causes oval and irregular nucleus in cancer cells. Antitumor agent-60 can suppress the growth of tumor to some extent in A549 xenograft model[1].
  • HY-153341
    CFT1946 Degrader 99.84%
    CFT1946 is an orally active, CRBN-based and mutant-selective bifunctional degradation activating compound (BiDAC) degrader of BRAFV600E with a DC50 of 14 nM in A375 cells. CFT1946 is capable of degrading BRAF V600E (Class I), G469A (Class II), G466V (Class III) mutations, and the p61-BRAFV600E splice variant. CFT1946 can be used in tumor research[1][2].
  • HY-N10503
    Norartocarpetin 98.92%
    Norartocarpetin is a tyrosinase inhibitor. Norartocarpetin has strong tyrosinase inhibitory activity with an IC50 value of 0.47 μM. Norartocarpetin as an antibrowning agent can be used for the research of food systems. Norartocarpetin also has a significant anticancer activity in lung carcinoma cells (NCI-H460) with an IC50 value of 22 μM. Norartocarpetin has antiproliferative effects are mediated via targeting Ras/Raf/MAPK signalling pathway, mitochondrial mediated apoptosis, S-phase cell cycle arrest and suppression of cell migration and invasion in human lung carcinoma cells[1][2].
  • HY-13810
    PF-04880594 Inhibitor
    PF-04880594 is a potent and selective RAF inhibitor. PF-04880594 inhibits both wild-type and mutant BRAF and CRAF. PF-04880594 shows antitumor activity[1].
  • HY-142820
    B-Raf IN 5 Inhibitor
    B-Raf IN 5 (compound 3b) is a potent inhibitor of protein kinase B-Raf with an IC50 of 2.0 nM. B-Raf IN 5 is devoid of binding to the secondary target PXR and resists rapid metabolism. B-Raf IN 6 has the potential for the research of cancer disease[1].
  • HY-15246
    Tovorafenib Inhibitor 99.89%
    Tovorafenib (TAK-580, MLN 2480) is an orally active and selective inhibitor of pan-Raf kinase.
  • HY-P1039A
    R18 TFA 98.48%
    R18 TFA is a peptide antagonists of 14-3-3, with a KD of 70-90 nM. R18 efficiently blocks the binding of 14-3-3 to the kinase Raf-1, a physiological ligand of 14-3-3, and effectively abolished the protective role of 14-3-3 against phosphatase-induced inactivation of Raf-1[1].