ras-raf

RAS RAS-RAF-IN-1 is a potent inhibitor of RAS and RAS-RAF, exhibiting a KD of 5.0 μμ-15 μμ for cyclophilin A (CYPA) binding affinity and demonstrating antitumor activity[1].

Sulindac sulfide (cis-Sulindac sulfide) is a non-steroidal anti-inflammatory compound that has a high affinity for COX-1 and acts as an inhibitor in Ras activation of Raf-1. Sulindac sulfide is a non-competitive inhibitor of gamma-secretase with an IC50 value of 20.2 μM. It is an active metabolite of sulinic acid.

INU-152 is a pan-RAF inhibitor. INU-152 has potent anti-tumor activity in preclinical models of BRAFV600E mutant cancer. INU-152 inhibits all RAF isoforms and inhibits MAPK pathways in mutant BRAF cells. INU-152 exhibits minimal paradoxical pathway activa

Kobe0065 is a novel and effective small-molecule compound that inhibits the Ras-Raf interaction by structure-based drug design (SBDD); it displays potent activity, competitively inhibiting the binding of H-Ras·GTP to c-Raf-1 RBD with a Ki value of 46 ± 13 μM.

REDX05358 is a highly selective and potent pan RAF inhibitor with a potential therapeutic for BRAF and RAS mutant tumors. REDX05358 has improved therapeutic potential and predicted safety profile. REDX05358 demonstrates subnanomolar binding affinity for B

Balamapimod is a reversible inhibitor of Ras Raf MEK. It also has a potential anti-tumor activity.

The Survival of Motor Neurons (SMN) protein participates in RNA splicing. Decreases in SMN, typically a consequence of defects in the smn1 gene, result in the death of motor neurons and lead to the neurodegenerative disease, spinal muscular atrophy (SMA). Cuspin-1 is a small molecule upregulator of SMN that has been shown in vitro to increase levels of SMN in SMA patient fibroblasts by 50% at 18 μM. Its mechanism of action is thought to involve increased phosphorylation of ERK to initiate Ras-Raf-MEK signaling, which results in an increased rate of SMN translation.

Antitumor agent-60 is a potent antitumor agent that targets the RAS-RAF signaling pathway and binds to CRAF (Kd: 721.3 nM). antitumor agent-60 increases p53 and ROS levels in cancer cells, resulting in oval and irregular nuclei. antitumor agent-60 is sufficient to block the cell cycle in G2 M phase and induce apoptosis. Antitumor agent-60 is sufficient to block the cell cycle in G2 M phase and induce apoptosis. In the A549 tumor transplantation model, Antitumor agent-60 has the ability to inhibit tumor growth.

Cyclorasin 9A5 is a cell-permeable, 11-residue cyclic peptide that orthosterically disrupts the Ras-Raf protein interaction, demonstrating an inhibition concentration (IC50) of 120 nM [1].

Norartocarpetin is a potent tyrosinase inhibitor exhibiting significant antibrowning properties useful for food system research, with an IC50 of 0.47 μM. Furthermore, it demonstrates substantial anticancer activity specifically in lung carcinoma cells (NCI-H460), achieving an IC50 of 22 μM. The antiproliferative effects of Norartocarpetin are achieved through targeting the Ras Raf MAPK signaling pathway, inducing mitochondrial-mediated apoptosis, facilitating S-phase cell cycle arrest, and inhibiting cell migration and invasion in human lung carcinoma cells.

I194496 is an effective inhibitor of cystathionine γ-lyase (CSE) with an IC50 value of 0.79 mM. It inhibits the growth of human TNBC cells by dual targeting the PI3K Akt and Ras Raf ERK pathways. Additionally, I194496 suppresses the metastasis of human TNBC cells by downregulating the Anxa2 STAT3 and VEGF FAK Paxillin signaling pathways.

Pseudoginsenoside Rh2 has cytotoxicity, it induces mitochondrial apoptosis in A549 cells and is responsible for excessive activation of the Ras Raf ERK p53 pathway. (20Z) -Pseudoginsenoside Rh2 and (20E)-Pseudoginsenoside Rh2 have antioxidative activity.

Cobimetinib racemate (Cobimetinib (racemate)) (GDC-0973 racemate) is a selective inhibitor of MEK.Cobimetinib racemate is also known as a mitogen-activated protein kinase, is a key component of the RAS RAF MEK ERK pathway.

MCP110 is an inhibitor of the interaction of Ras with Raf-1 and can be used in studies about the treatment of human tumors.

Semilicoisoflavone B, an isoflavone extracted from Kohlrabi, has anticancer activity and induces apoptosis in oral cancer cells by inducing ROS production and down-regulating MAPK and Ras Raf MEK signaling.

APS-2-79 hydrochloride (APS-2-79 HCl) is a MAPK antagonist that modulating KSR-dependent MAPK signalling by antagonizing RAF heterodimerization as well as the conformational changes required for phosphorylation and activation of KSR-bound MEK.

Cyclorasin 9A5 TFA is a cell-penetrating cyclic peptide consisting of 11 residues that inhibits the interaction between Ras and Raf proteins, with an IC50 of 120 nM.

DPQZ is an anti-tubulin compound acting by inducing cell apoptosis in human oral cancer cells through Ras/Raf inhibition and MAP kinases activation.

Pan-RAF kinase inhibitor 1 is a potent inhibitor of the Pan-RAF kinase pair, which regulates MAPK signaling and affects the proliferation of RAS-mutated tumor cells. Pan-RAF kinase inhibitor 1 has shown research potential for the study of cancer diseases.

SHR902275 is a selective, potent, orally active RAF inhibitor targeting RAS mutant cancers, acting on cRAF (IC50: 1.6 nM), bRAFwt (IC50: 10 nM), and bRAFV600E (IC50: 5.7 nM). SHR902275 exhibits cell growth inhibitory effects in H358 cells (GI50: 1.5 nM), A375 cells (GI50: 0.17 nM), Calu6 cells (GI50: 0.4 nM), and SK-MEL2 cells (GI50: 0.32 nM).

Kobe2601 is a Kobe0065 and Kobe02602 water-soluble analog. It displays inhibitory activity towards Ras-Raf binding.

PLX7904 (PB04), also known as PB04, is a potent and selective paradox-breaker RAF inhibitor. It is able to efficiently inhibit activation of ERK1 2 in mutant BRAF melanoma cells but does not hyperactivate ERK1 2 in mutant RAS-expressing cells.

Deltarasin is a high affinity PDEδ-KRAS interaction inhibitor. Deltarasin can inhibit KRAS-PDEδ interactions by binding to a hydrophobic pocket on PDEδ, resulting in the impairment of cell growth, KRAS activity, and RAS RAF signaling in human pancreatic ductal adenocarcinoma cell lines. The anti-cancer cell activity of deltarasin can be enhanced by simultaneously blocking tumor protective autophagy

Pimasertib HCl is an orally bioavailable small-molecule inhibitor of MEK1 and MEK2 (MEK1 2) with potential antineoplastic activity. Pimasertib selectively binds to and inhibits the activity of MEK1 2, preventing the activation of MEK1 2-dependent effector proteins and transcription factors, which may result in the inhibition of growth factor-mediated cell signaling and tumor cell proliferation. MEK1 2 (MAP2K1 K2) are dual-specificity threonine tyrosine kinases that play key roles in the activation of the RAS RAF MEK ERK pathway and are often upregulated in a variety of tumor cell types.