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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.
PROTAC K-Ras Degrader-1 (Compound 518) is a cereblon-based PROTAC that selectively degrades K-Ras, achieving ≥70% degradation efficiency in SW1573 cells. It serves as a valuable tool for studying K-Ras-driven signaling pathways and potential therapeutic strategies in cancer research.
LC-2 is a first-in-class, VHL-based PROTAC designed to degrade endogenous KRAS G12C. Incorporating a MRTX849-derived covalent warhead, LC-2 binds KRAS G12C and recruits the VHL E3 ligase, inducing rapid and sustained degradation with DC₅₀ values between 0.25 and 0.76 μM. It effectively suppresses MAPK signaling in both homozygous and heterozygous KRAS G12C mutant cell lines, making it a valuable tool for targeted cancer research.
PROTAC SOS1 Degrader-1 (TFA) is a potent PROTAC molecule targeting SOS1, with a DC₅₀ of 98.4 nM. It exhibits antiproliferative activity in cancer cells harboring various KRAS mutations and demonstrates antitumor efficacy with low toxicity, making it a promising candidate for targeted cancer therapy research.
Synonyms: ASP-3082; KRAS G12D inhibitor 17
Setidegrasib is a PROTAC degrader specifically targeting the KRAS G12D mutation with a DC50 of 37 nM. This compound effectively induces the degradation of KRAS G12D protein, leading to the suppression of key signaling molecules such as p-ERK, p-AKT, and p-S6 in AsPC-1 cells. Setidegrasib demonstrates significant anti-tumor activity across various cancer xenograft models, making it a valuable tool for studying KRAS(G12D)-mutated solid tumors.
ACBI3 is a PROTAC designed to target KRAS, employing a unique mechanism to induce degradation of this oncogenic protein. It comprises a pan-KRAS degrader linked to an E3 ligase ligand through a specialized linker, facilitating the recruitment of the proteasome for degradation. ACBI3 has demonstrated significant biological activity by achieving durable modulation of signaling pathways and promoting tumor regression in KRAS mutant xenograft mouse models, making it a valuable tool for research into cancer therapeutics aimed at KRAS-driven malignancies.
PROTAC KRAS G12D degrader 1 functions as a selective PROTAC targeting the KRAS G12D mutant by promoting its degradation. This compound effectively inhibits the proliferation of KRAS G12D-mutant cell lines and suppresses phosphorylation of ERK, a critical pathway in cancer signaling. In vivo studies demonstrate its ability to impede tumor growth in mice with AsPC-1 xenografts, making it a valuable tool for research into KRAS G12D-driven cancers.
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.
PROTAC KRAS G12C degrader-1 is a Cereblon-based PROTAC targeting the KRAS G12C mutant. This compound promotes the formation of a dimer between Cereblon and KRAS G12C, leading to the degradation of GFP-tagged KRAS G12C in reporter cell systems. It serves as a valuable tool for research on targeted degradation strategies in KRAS-driven cancers.
PROTAC K-Ras Degrader-5 is a cereblon-based PROTAC specifically designed to target KRASG12D, achieving a DC50 of less than 100 nM. This reagent facilitates the recruitment of KRASG12D to the cereblon E3 ubiquitin ligase complex, leading to its ubiquitination and proteasomal degradation. As a result, it effectively reduces pERK levels and inhibits the proliferation of cancer cells. PROTAC K-Ras Degrader-5 also enhances caspase 3/7 activity and cleaved PARP levels, indicative of apoptosis, in pancreatic cancer models. This compound is a valuable tool for researching both pancreatic and colorectal cancer.
MCB-36 is a VHL-recruiting pan-KRAS PROTAC degrader that targets various KRAS mutants, including G12D, G12C, G12V, and wild-type forms, with an exceptionally high binding affinity (Kd ≈ 1 pM). This compound effectively lowers p-ERK levels, promoting apoptosis in KRAS-driven cancer cells while showing minimal impact on HRAS and NRAS protein levels. MCB-36 is particularly useful for investigating colorectal and lung cancers, as it demonstrates efficacy against KRASG12C inhibitor-resistant tumors and aids in remodeling the tumor immune microenvironment.
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.
PROTAC KRAS G12C degrader-2 is a bifunctional molecule that targets the KRAS G12C mutant protein for degradation via the proteasome. It features a cereblon inhibitor that modulates the activity of inhibitors of apoptosis proteins (IAPs) to facilitate the targeted destruction of KRAS. This reagent is valuable for research applications aimed at elucidating the role of KRAS in cancer biology and developing effective targeted therapies for KRAS-driven malignancies.
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.
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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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.
(R)-ACBI-4 is a selective PROTAC degrader targeting the GTP-loaded active state of KRAS (KRAS(on)). It exhibits notable anti-proliferative activity and effectively degrades various KRAS mutants, including KRASG12R, in cancer cell lines. This compound is utilized in research focused on understanding KRAS-driven oncogenesis and therapeutic interventions in KRAS-related cancers.
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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.
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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