- Cat. No.
- A15925
ML-098
Synonyms: CID-7345532
ML-098 is an activator of the GTP-binding protein Rab7 (EC50 = 77.6 nM).
Search by product name, CAS, target or catalog number. Press Down Arrow to reach product suggestions, Tab to move between links, and Escape to close suggestions.
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.
Synonyms: CID-7345532
ML-098 is an activator of the GTP-binding protein Rab7 (EC50 = 77.6 nM).
Synonyms: CID-888706
ML-099 (CID-888706) is a pan Ras-related GTPase activator that promotes the activation of multiple small GTPases, including Rac1, Cdc42, Ras, Rab7, and Rab2A. It serves as a useful tool for studying the regulation and function of Ras-related GTPase signaling pathways.
Synonyms: SOS1 activator 1
VUBI1 (SOS1 Activator 1) is a benzimidazole-derived small molecule that acts as a potent activator of the guanine nucleotide exchange factor SOS1, with a dissociation constant (Kᴅ) of 44 nM. It promotes RAS activation by enhancing RAS-GTP formation and modulates downstream ERK phosphorylation, thereby influencing RAS–MAPK signaling. In addition, VUBI1 serves as a functional ligand for the development of PROTAC-based degraders, such as PROTAC SOS1 Degrader-1, to induce targeted SOS1 degradation. VUBI1 is a valuable compound for studying RAS pathway regulation and its role in cancer biology.
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.
Methylophiopogonanone B is a homoisoflavonoid that serves as a Ras activator. Isolated from the root of Ophiopogon japonicus, it exhibits potent antioxidant properties. This compound enhances GTP-Rho levels and activates the Rho signaling pathway, thereby inducing morphological changes in cells, such as actin cytoskeletal reorganization, dendrite retraction, and stress fiber formation. It is a valuable reagent for research into cellular signaling and structural dynamics.
Synonyms: CID-2160985
ML-097 is a potent activator of Ras-related GTPases, specifically targeting Rac1, CDC42, Ras, and Rab7. It plays a critical role in modulating cellular signaling pathways associated with proliferation, migration, and cytoskeletal organization. This compound is valuable for research applications focusing on cancer biology, neurobiology, and cellular communication mechanisms.
Synonyms: 8-CPT-2'-O-Me-cAMP sodium
8-pCPT-2′-O-Me-cAMP sodium is an analog of cyclic AMP that serves as a selective activator of exchange proteins activated by cAMP (Epac). This compound demonstrates effective activation of Epac1 with an EC50 value of 2.2 μM, while showing minimal activity towards protein kinase A (EC50 >10 μM). In vitro studies highlight its role in stimulating Epac-mediated Ca2+ release in pancreatic β-cells, and it functions as an activator of Rap1. Additionally, 8-pCPT-2′-O-Me-cAMP sodium has been shown to strengthen the barrier of retinal pigment epithelium against pathological choroidal endothelial cell invasion, contributing to research on macular degeneration.
Synonyms: 8-Hexylamino-cAMP
8-HA-cAMP is a membrane-permeable analogue of cyclic adenosine monophosphate (cAMP) that acts as an activator of cAMP-dependent protein kinase (PKA). Its structure confers metabolic stability against mammalian phosphodiesterases that respond to cyclic nucleotides. This compound is useful in studying PKA signaling pathways and their associated biological processes.
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.
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.
Synonyms: 8-(4-Chlorophenylthio)-cAMP-AM
8-CPT-cAMP-AM is a membrane-permeant analogue of cyclic adenosine monophosphate (cAMP) that acts as an activator of cAMP- and cGMP-dependent protein kinases. It also stimulates exchange protein directly activated by cAMP (Epac), making it a valuable tool for investigating cAMP signaling pathways. This compound is useful in research applications studying cellular processes influenced by cAMP, such as cell proliferation, differentiation, and effects on various physiological responses.
RAS Activator Compound 1 is a specific activator targeting the guanine nucleotide exchange factor, son of sevenless homologue 1 (SOS1). This compound effectively facilitates the nucleotide exchange process, leading to increased levels of active RAS-GTP in HeLa cells. RAS Activator Compound 1 is valuable for research focused on RAS-driven tumors, providing insights into the mechanisms of RAS activation and its role in cancer biology.
Out of stock
All 3 sizes
Synonyms: 8-CPT-2'-O-Me-cAMP
8-pCPT-2′-O-Me-cAMP is a selective activator of exchange proteins activated by cAMP (Epac), specifically targeting Epac1 with an EC50 of 2.2 μM. This compound does not activate protein kinase A (PKA) with an EC50 greater than 10 μM. 8-pCPT-2′-O-Me-cAMP effectively stimulates Epac-mediated Ca2+ release in pancreatic β-cells in vitro, and it plays a role as a Rap1 activator. Additionally, it enhances the barrier function of retinal pigment epithelium against choroidal endothelial cell invasion, potentially providing insights into therapeutic mechanisms for macular degeneration.
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.
Out of stock
All 3 sizes
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.
Out of stock
All 3 sizes
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.
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.
Out of stock
All 3 sizes
Sp-8-Br-2'-O-Me-cAMPS is a cAMP analog that serves as a potent activator of the exchange protein directly activated by cyclic AMP (EPAC). This compound is valuable for studying the role of EPAC in various biological pathways, particularly those related to metabolism. Its ability to modulate EPAC activity makes it an important tool for investigating signaling mechanisms and their implications in metabolic processes.
Goralatide is a Ra activator that modulates the thermal sensitivity of hematopoietic progenitor cells. It enhances the disparity in thermal sensitivity between leukemia progenitor cells and normal hematopoietic progenitor cells, thereby increasing the efficacy of hyperthermia therapy. This compound is relevant for research in cancer treatment strategies, particularly those involving targeted thermal therapies.
Sp-8-pCPT-2'-O-Me-cAMPS is a selective activator of the exchange protein directly activated by cyclic AMP (EPAC). This compound enhances EPAC-mediated signaling pathways, playing a significant role in the regulation of various physiological processes. It is valuable for research into endocrine metabolism and related signaling mechanisms.
Out of stock
All 3 sizes
2-AHA-cAMP is a cAMP analogue that acts as an activator of cAMP-dependent protein kinase. The molecule features a free terminal primary amino group, enabling its coupling to gels or fluorescent dyes for enhanced experimental versatility. Its application extends to various research areas including signaling pathways and protein interaction studies, making it a valuable reagent for biophysical and biochemical investigations.
Out of stock
All 3 sizes