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].

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.

Kobe 2602 is an inhibitor of Ras that exhibits anticancer chemotherapeutic activities.

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

Balamapimod, also known as MKI-822, is a small-molecule Ras/Raf/MEK inhibitor that directly targets deregulated MAPK signaling cascades and is being actively explored to suppress aberrant protein kinase activity implicated in oncogenic transformation, inflammatory signaling, and pathological cell proliferation, with demonstrated therapeutic relevance for stroke, osteoporosis, rheumatoid arthritis, polycystic kidney disease, colonic polyps, and other inflammation-driven disorders through pathway-level inhibition.

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.

XSJ-10 is an HDAC inhibitor containing a RAS/RAF protein interference unit, with IC50 values of 0.05 μM in PANC-1 cells and 0.04 μM in HT-29 cells. It effectively induces cancer cell apoptosis and tumor inhibition by strongly suppressing the RAS-RAF-MEK-ERK signaling pathway and HDAC3 acetylation levels.

Pan-RAS-IN-5 (compound 7A) is a molecular glue that facilitates the formation of a ternary complex with cyclophilin A (CYPA) and RAS(ON) protein. This complex inhibits the binding of RAF downstream of RAS, demonstrating antitumor activity.

Erufosine is an inhibitor of the PI3K/Akt and Ras/Raf/MAPK signaling pathways. It suppresses the activity of breast cancer cell lines MCF-7 and MDA-MB 231 with an IC50 of 40.95/40.8 μM, respectively. Erufosine reduces phosphorylation of PI3K(p85), Akt (PKB), and cRaf, making it applicable in research on breast cancer and myeloid leukemia.

Envometinib (Compound B) is a dual MEK inhibitor that operates through deep cyclic inhibition (DCI). It exhibits antitumor activity across various in vivo models and is applicable in researching RAS and RAF mutated cancers, such as colorectal cancer and melanoma.

Eras-4001 is a small-molecule pan-KRAS inhibitor capable of targeting both wild-type KRAS and various mutant forms simultaneously. Eras-4001 inhibits signaling between KRAS and effector proteins such as RAF, thereby blocking the activity of the RAS/MAPK pathway. In preliminary studies, this compound has demonstrated high affinity for KRAS (nano-molar IC₅₀) and induced tumor regression in multiple KRAS-mutant tumor models, indicating potential value for antitumor therapy.

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.

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

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

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

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

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.

Tunlametinib is a highly selective, orally bioavailable small molecule inhibitor of MEK1 and MEK2 kinases with a reported IC50 value of 1.9 nM for MEK1. Tunlametinib exerts its antitumor effects by blocking the oncogenic RAS-RAF-MEK-ERK signaling pathway, thereby inducing tumor cell cycle arrest and promoting apoptosis, Tunlametinib demonstrates strong inhibitory activity against various RAS/RAF-mutant cancer cells such as those harboring BRAF V600E or KRAS G12C mutations, shows synergistic effects in combination with BRAF/KRASG12C/SHP2 inhibitors and Docetaxel, and is used in targeted therapy for RAS/RAF-driven cancers including melanoma, colorectal cancer, and non-small cell lung cancer (NSCLC).

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.

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.

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).

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.

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.