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Ras inhibitors and related small GTPase modulators act on KRAS and on the Rac, Rho and Cdc42 proteins. Small GTPases of the Ras superfamily work as molecular switches. They cycle between an active form bound to guanosine triphosphate (GTP) and an inactive form bound to guanosine diphosphate (GDP). Oncogenic KRAS mutations such as G12C keep the protein in its signaling state. ARS-853 and KRas G12C inhibitor 4 target the mutant cysteine of KRAS G12C, while Kobe2602 interferes with binding of Ras to Raf. Salirasib, a farnesylcysteine mimetic, disrupts the membrane association of Ras. Rho-family tools include NSC 23766 and EHT 1864, which inhibit Rac, and CASIN, which targets Cdc42.
KY1220 is a compound that destabilizes both β-catenin and Ras, via targeting the Wnt/β-catenin pathway; with an IC50 of 2.1 μM in HEK293 reporter cells.
RGB-1 is a selective RNA G-quadruplex stabilizer that targets and reduces the expression of the NRAS proto-oncogene within breast cancer cells. This compound serves as a valuable tool for exploring the cellular mechanisms and functions of RNA G-quadruplex structures, while also aiding in the identification of novel mRNA sequences capable of forming G-quadruplexes. RGB-1 is particularly relevant for research focused on breast cancer therapeutics and the molecular basis of oncogene regulation.
VVD-849 is a RAS ligand that covalently binds to Cys242 in the RAS-binding domain of PI3K p110α, facilitating the interaction between RAS and PI3K. This compound exhibits partial inhibition of pAKT (S473) specifically in HER2-overexpressing tumors. VVD-849 is utilized in cancer research, particularly for studying the mechanisms underlying breast cancer progression and RAS-related signaling pathways.
MRTX849 acid serves as a ligand for KRAS G12C, facilitating the synthesis of the PROTAC LC-2. This first-in-class PROTAC effectively induces degradation of endogenous KRAS G12C, demonstrating potent biological activity with DC50 values ranging from 0.25 to 0.76 μM. It is applicable in research settings focused on targeted protein degradation and cancer therapeutics.
(Rac)-D3S-001 is a racemic mixture of the compound D3S-001, which serves as a potent modulator of specific biological pathways. This compound exhibits significant activity in regulating cellular processes, making it a valuable tool for investigating the underlying mechanisms of disease. It is particularly useful in pharmacological studies and in the development of therapeutic strategies targeting related biological systems.
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PPI stabilizer-1 is a KRAS dimerizing agent that effectively promotes the dimerization of KRAS with a dissociation constant (KD) of 3.8 µM. This compound has the ability to co-crystallize with GCP-KRASG12D, facilitating structural studies and elucidating the role of KRAS in cellular signaling. PPI stabilizer-1 is valuable for researching KRAS-driven cancers, providing insights into therapeutic strategies targeting this critical pathway.
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SOS2 Ligand 1 is a selective ligand that targets son of sevenless 2 (SOS2), exhibiting a KD value of 4.6 µM. This compound is valuable for studying the role of SOS2 in cellular signaling pathways and may facilitate research in cancer biology and related fields. Its specificity for SOS2 makes it a useful tool for investigating SOS2-mediated processes and potential therapeutic interventions.
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Palmostatin M is a Ras signaling modulator that specifically targets acyl-protein thioesterases 1 and 2 (APT1 and APT2), exhibiting an IC50 of 2.5 nM for APT1. By disrupting the depalmitoylation cycle of Ras, Palmostatin M effectively downregulates the Ras signaling pathway. This compound is particularly relevant for studies investigating cancer biology and the modulation of Ras-driven signaling networks.
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KRAS G12D modulator-1 is an effective modulator targeting the KRAS G12D mutation. It exhibits potent activity with IC50 values ranging from 1 to 10 μM against NEA-G12D, PPI-G12D, and phosphorylated ERK in AGS cells. This compound is suitable for research applications focused on cancer biology and the modulation of KRAS signaling pathways.
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Ras Modulator-1 is a selective modulator of the Ras protein, which plays a critical role in cell signaling pathways associated with growth and differentiation. This compound has been shown to influence the activity of Ras, making it a valuable tool for investigating cancer biology and therapeutic interventions targeting Ras-driven malignancies. Research applications include studying signal transduction mechanisms and evaluating potential treatments in oncogenic signaling pathways.
JH530 is a potent inducer of methuosis, specifically targeting triple-negative breast cancer (TNBC) cells. It triggers extensive intracellular vacuolization, leading to the inhibition of TNBC cell proliferation. With its demonstrated anti-tumor activity, JH530 serves as a valuable tool for cancer research applications.
ZCL279 is a small molecule modulator that selectively inhibits the interaction between Cdc42 and intersectin (ITSN). At lower concentrations (
LZTR1-KRAS modulator 1 is designed to modulate the interaction between KRAS and LZTR1, thereby enhancing the recruitment of the LZTR1-KRAS complex. This compound is crucial for studies investigating the regulation of KRAS signaling pathways and their implications in cellular processes. Its application can further elucidate the role of LZTR1 in cancer biology and potential therapeutic interventions targeting KRAS-driven tumors.
RasGRP3 ligand 1 is a specific ligand for RasGRP3 with a binding affinity characterized by a Ki of 1.75 nM. This compound effectively induces Ras activation, making it a valuable tool for investigating downstream signaling pathways in cancer research. Its targeted mechanism allows for detailed studies of RasGRP3's role in cellular processes associated with tumorigenesis.
(+)-Oxanthromicin is a K-Ras localization modulator that disrupts the localization of oncogenic mutant K-Ras from the plasma membrane in intact Madin-Darby canine kidney (MDCK) cells. This compound demonstrates significant antitumor efficacy, making it valuable for research into cancer biology and potential therapeutic strategies targeting K-Ras-mediated signaling pathways. Its ability to alter K-Ras localization positions it as a promising candidate in the development of targeted cancer therapies.
SML-10-70-1 is a K-Ras ligand that covalently modifies the K-Ras G12C mutant protein, providing a targeted approach in cancer research. This compound effectively inhibits the phosphorylation of ERK and Akt, key signaling pathways involved in cell proliferation. In vitro studies demonstrate that SML-10-70-1 significantly reduces the proliferation of cancer cell lines H23, H358, and A549, with IC50 values ranging from 26.6 to 47.6 μM, indicating its potential utility in therapeutic applications against K-Ras-driven malignancies.
pan-KRAS ligand 1 is a potent ligand designed for Target Protein applications within PROTAC technology. It facilitates the development of PROTAC pan-KRAS degrader 4, enabling targeted degradation of KRAS mutants. This compound is instrumental for researchers investigating KRAS-related oncogenic pathways and therapeutic strategies against cancer.
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