- Cat. No.
- A16231
APS-2-79
APS-2-79 is an antagonist of MEK phosphorylation by RAF through direct binding of the KSR active site.
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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.
APS-2-79 is an antagonist of MEK phosphorylation by RAF through direct binding of the KSR active site.
CE3F4 is a selective antagonist of exchange protein directly activated by cAMP (Epac1), with IC50s of 10.7 μM and 66 μM for Epac1 and Epac2(B), respectively.
ESI-08 is a potent and selective antagonist of exchange proteins directly activated by cAMP (EPACs). It inhibits both EPAC1 and EPAC2 with an IC₅₀ of 8.4 μM, effectively blocking cAMP-induced EPAC activation while sparing cAMP-mediated protein kinase A (PKA) signaling. By selectively disrupting EPAC-dependent pathways, ESI-08 serves as a valuable tool compound for dissecting cAMP signaling mechanisms and studying EPAC-related physiological and pathological processes.
HJC0197 is a selective antagonist of Epac1 and Epac2, exhibiting an IC50 of 5.9 μM for Epac2. This compound effectively inhibits cAMP-induced activation of Epac, demonstrating a capacity to block Epac1-mediated Rap1-GDP exchange activity at a concentration of 25 μM in the presence of a corresponding concentration of cAMP. HJC0197 serves as a valuable tool for investigating the role of Epac proteins in cellular signaling pathways and cAMP-mediated biological processes.
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.
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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K-Ras-IN-2 is a selective antagonist of the K-Ras protein. It has demonstrated significant biological activity in inhibiting K-Ras-driven signaling pathways, making it a valuable tool for researchers studying tumor biology and oncogenic signaling. This compound is particularly useful in cancer research applications focused on K-Ras-related malignancies.
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NY-0173 is an antagonist of exchange proteins directly activated by cAMP (EPAC), demonstrating IC50 values of 3.5 μM for EPAC2 and 4.0 μM for EPAC1. This reagent serves as a valuable tool for investigating the biological roles and pathways mediated by EPAC. Researchers can utilize NY-0173 to explore its impact on cellular processes influenced by EPAC signaling.