Ras Activator

ML-098 (CID-7345532) is an activator of the GTP-binding protein Rab7 with an EC₅₀ of 77.6 nM.

Geranylgeranyl pyrophosphate triammonium is a type of isoprenoid metabolic intermediate, mainly synthesized through the mevalonate pathway. Geranylgeranyl pyrophosphate triammonium is a key precursor in various biological synthesis processes, especially as a necessary substrate for post-translational modification of proteins - geranylgeranyl phosphorylation. Geranylgeranyl pyrophosphate triammonium regulates various cellular processes and disease progression through protein geranylgeranyl phosphorylation, such as activating the YAP signaling pathway, promoting cell proliferation and inhibiting apoptosis; promoting IL-2 production and STAT5 phosphorylation; and influencing metabolic homeostasis and cancer, etc.

8-pCPT-2′-O-Me-cAMP (8-CPT-2'-O-Me-cAMP) sodium, an analog of cAMP, is an activator of exchange proteins activated by cAMP (Epac). 8-pCPT-2′-O-Me-cAMP sodium activates Epac1 (EC₅₀ = 2.2 μM), but not PKA (EC₅₀ >10 μM). 8-pCPT-2′-O-Me-cAMP sodium stimulates Epac-mediated Ca²⁺ release in pancreatic β-cells in vitro. 8-pCPT-2′-O-Me-cAMP sodium is a Rap1 activator. 8-pCPT-2′-O-Me-cAMP sodium enhances the retinal pigment epithelium barrier against the pathological choroidal endothelial cell invasion that occurs in macular degeneration.

ML-099 (CID-888706) is a pan Ras-related GTPases activator that can activate Rac1, cell division cycle 42, Ras, Rab7, and Rab-2A.

Methylophiopogonanone B is a homoisoflavonoid compound. Methylophiopogonanone B can be isolated from O. japonicus root. Methylophiopogonanone B promotes Rho activation and Tubulin depolymerization. Methylophiopogonanone B significantly increases GTP-Rho, but not GTP-Rac or GTP-CDC42. Methylophiopogonanone B induces cell morphological change via melanocyte dendrite retraction and stress fiber formation. Methylophiopogonanone B exhibits strong antioxidant activity. Methylophiopogonanone B can be used in the research of cervical cancer.

N-Acetylneuraminic acid (Standard) is the analytical standard of N-Acetylneuraminic acid. This product is intended for research and analytical applications. N-Acetylneuraminic acid (NANA; Lactaminic acid), a nonphenolic structure, is the predominant form of sialic from Collocalia esculenta. N-Acetylneuraminic acid plays a biological role in myocardial injury, melanoma and viral or bacterial infection. N-Acetylneuraminic acid inhibits melanogenesis by reducing tyrosinase activity and triggers myocardial injury in vitro and in vivo by activation of the Rho/Rho-associated signaling pathway through binding to RhoA and Cdc42. N-Acetylneuraminic acid may prevent high fat diet (HFD)-induced inflammation and oxidative stress, thereby prevents hyperlipidemia-associated inflammation and oxidative stress. N-Acetylneuraminic acid is promising for research in the field of melanoma, coronary artery, obesity-related diseases and hyperlipidemia.

Mevalonolactone is an intermediate metabolite in the eukaryotic mevalonate pathway, serving as the stable δ-lactone form of mevalonate with oral activity. Mevalonolactone exhibits binding affinity for ZNF384 (K_a = 12.6 μM) and inhibitory activity against aconitase (aconitase). Mevalonolactone promotes the nuclear localization of ZNF384 and enhances its binding to the GGPPS promoter. Mevalonolactone induces insulin resistance, disrupts glucose and lipid metabolism, enhances the isoprenylation of K-Ras, and inhibits the activation of the insulin signaling pathway. Mevalonolactone inhibits polypeptide synthesis of HMG-CoA reductase in isolated rat hepatocytes, promotes its degradation, and reduces its enzymatic activity. Mevalonolactone impairs mitochondrial function in rat brains. Mevalonolactone promotes the development of metabolically unhealthy obesity. Mevalonolactone can be used in research related to metabolically abnormal obesity, mevalonic aciduria, HMGCR-related limb-girdle myopathy, and statin-induced myopathy.

VUBI1 (SOS1 activator 1) is a benzimidazole derivative and SOS1 activator with a K_d of 44 nM. VUBI1 can significantly activate RAS-GTP and regulate the phosphorylation of ERK. VUBI1 also can serve as a target ligand for synthesizing PROTACs, such as PROTAC SOS1 degrader-1 (HY-145737), to induce SOS1 degradation. VUBI1 can be used in the study of cancer.

CX-5011 is a CK2 inhibitor. CX-5011 also induces Rac1 activation. CX-5011 induces apoptosis and induces cancer cell death.

Y-27632 hydrochloride hydrate is a ROCK inhibitor with K_i values of 220 nM and 300 nM for ROCK1 and ROCK2, respectively. Y-27632 hydrochloride hydrate exerts anti-inflammatory and immunomodulatory effects in systemic lupus erythematosus models by inhibiting the ROCK/NF-κB pathway. Y-27632 hydrochloride hydrate enhances autophagy by inhibiting the AKT/mTOR pathway, thereby inducing apoptosis apoptosis in oral squamous cell carcinoma. Y-27632 hydrochloride hydrate induces the formation of tunneling nanotubes in ARPE-19 cells and significantly enhances mitochondrial transfer through these channels. Y-27632 hydrochloride hydrate promotes neurite outgrowth in PC12 cells by activating the Rac1/NOX1/ROS/AKT/PAK1 signaling cascade.

Mulberroside C is one of the main bioactive components in white mulberry (Morus alba L.). Mulberroside C exhibits antiplatelet, antiviral and neutrophil-regulating activities, and binds to EV-A71 VP1 with a K_d value of 1.289 nM. Mulberroside C reduces the phosphorylation level of ERK, promotes the phosphorylation of IP3RI at the Ser¹⁷⁵⁶ site, and decreases calcium influx and calcium mobilization. Mulberroside C inhibits the expression of P-selectin (P-selectin). Mulberroside C upregulates the cyclic nucleotide signaling pathway in human platelets. Mulberroside C binds to IL-23R, upregulates the expression of G-CSF, GM-CSF and RASGRP1, and activates the RAS/ERK signaling pathway. Mulberroside C promotes neutrophil maturation, accelerates the recovery of leukopenia, and enhances the antibacterial activity of neutrophils. Mulberroside C inhibits the replication of hepatitis C virus in replicon cells. Mulberroside C prevents the uncoating and genome release of EV-A71, and inhibits the synthesis of viral proteins and RNA. Mulberroside C can be used in studies related to thrombosis-mediated cardiovascular diseases, chemotherapy- and radiotherapy-induced leukopenia, hepatitis C virus infection, and hand, foot and mouth disease.

CX-5011 free base is a potent CK2 inhibitor. CX-5011 free base also is a Rac-1 activator. CX-5011 free base induces methuosis and promotes macropinocytosis. CX-5011 free base induces apoptosis. CX-5011 free base decreases the expression of rpS6 phosphorylation.

8-Br-2'-O-Me-cAMP is an analogue of the signal molecule cyclic AMP (cAMP). 8-Br-2'-O-Me-cAMP is an agonist of exchange factors activated by cAMP (Epac), while it doesn't activate PKA as cAMP do. 8-Br-2'-O-Me-cAMP can be used in cardiovascular disease research.

RAS activator compound 1 (Compound 7c) is a RAS activator targeting the guanine nucleotide exchange factor (GEF) son of sevenless homologue 1 (SOS1). RAS activator compound 1 can activate the nucleotide exchange process and increase levels of active RAS-GTP in HeLa cells. RAS activator compound 1 can be used for research of RAS-driven tumor.

8-pCPT-2′-O-Me-cAMP (8-CPT-2'-O-Me-cAMP), an analog of cAMP, is an activator of exchange proteins activated by cAMP (Epac). 8-pCPT-2′-O-Me-cAMP activates Epac1 (EC₅₀ = 2.2 μM), but not PKA (EC₅₀ >10 μM). 8-pCPT-2′-O-Me-cAMP stimulates Epac-mediated Ca²⁺ release in pancreatic β-cells in vitro. 8-pCPT-2′-O-Me-cAMP is a Rap1 activator. 8-pCPT-2′-O-Me-cAMP enhances the retinal pigment epithelium barrier against the pathological choroidal endothelial cell invasion that occurs in macular degeneration.

α,δ-NAG is an orally active glutaminase-resistant less-hydrolyzable L-Glutamine derivative. α,δ-NAG is a G protein-coupled receptor (GPCR) allosteric modulator. α,δ-NAG suppresses neutrophilic airway inflammation by activating the GPCR/ERK/MKP-1 pathway. α,δ-NAG can be used for the researches of inflammation and immunology, such as asthma.

8-pMeOPT-2'-O-Me-cAMP is an analogue of the signal molecule cAMP and a potent stimulator of exchange factors activated by cAMP (Epac), while it doesn't activate PKA as cAMP does.

LZTR1-KRAS modulator 1 is a KRAS-LZTR1 interaction modulator that can enhance the recruitment of the LZTR1-KRAS complex.

8-CPT-cAMP-AM (8-(4-Chlorophenylthio)-cAMP-AM) is an Epac/PKA activator. 8-CPT-cAMP-AM potentiates glucose-dependent first- and second-phase insulin secretion, induces β-cell depolarization, modulates intracellular calcium via influx and ryanodine-sensitive store mobilization, and facilitates calcium-induced calcium release resistant to PKA inhibition. 8-CPT-cAMP-AM can be used for the research of cardiac hypertrophy, diabetic cardiomyopathy, and melanoma.

RasGRP3 ligand 1 (compound 96) is a RasGRP3 ligand with a K_i of 1.75 nM. RasGRP3 ligand 1 can induce Ras activation and can be used for cancer research.