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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.
KRA-533 is a potent KRAS agonist that selectively binds to the GTP/GDP binding pocket of the KRAS protein. This interaction inhibits GTP cleavage, leading to the accumulation of constitutively active GTP-bound KRAS. Consequently, KRA-533 induces both apoptotic and autophagic cell death pathways in cancer cells, making it a valuable tool for research into cancer biology and therapeutic strategies targeting KRAS signaling.
I942 is a selective non-cyclic nucleotide (NCN) agonist of EPAC1. It effectively modulates proinflammatory cytokine signaling pathways associated with various cardiovascular diseases. This compound serves as a valuable tool in research focused on understanding EPAC1-related mechanisms and developing therapeutic strategies for inflammatory cardiovascular conditions.
(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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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.
Synonyms: 8-(4-Hydroxyphenylthio)-2'-O-Me-cAMP
8-pHPT-2'-O-Me-cAMP is a cAMP analog that acts as an Epac agonist, specifically enhancing the activity of the exchange protein activated by cyclic AMP (Epac). This compound is utilized in cardiac research to explore signaling mechanisms and cellular responses associated with cardiac function and pathophysiology. Its ability to modulate Epac pathways makes it a valuable tool for investigating the roles of cAMP in cardiac health and disease.
(+)-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.
