GTP-dependent

(±)-Decursinol (3',4'-dihydro-3'-hydroxy-Xanthyletin) is a natural product from Angelica gigas.

Emivirine (MKC-442) is a potent and selective nonnucleoside reverse transcriptase inhibitor for human immunodeficiency virus type 1.

AZD0022 is a selective, reversible, and orally active KRAS G12D inhibitor exhibiting high affinity for both active (KRAS G12D-GTP) and inactive (KRAS G12D-GDP) proteins, whilst demonstrating selectivity for wild-type KRAS. AZD0022 exhibits tumour marker inhibition in PDAC and NSCLC models, making it suitable for investigating tumours such as advanced solid tumours, pancreatic cancer, and colorectal cancer.

Purine riboside-5'-O-triphosphate sodium is an active metabolite of Nebularine and acts as an inhibitor of DNA primase ATP and GTP polymerization activities, with IC50 values of 35 µM and 28 µM, respectively. It also inhibits calmodulin-dependent protein kinase II (CaMKII), with a Ki value of 590 µM.

Glycerophosphoinositol 4-phosphate (GroPIns-4-P) disodium is a metabolite of phospholipase A and an inhibitor of adenylate cyclase. This compound can regulate cAMP-dependent cellular functions and also induces membrane ruffling and stress fiber formation in serum-starved Swiss 3T3 cells by activating small GTPases Rac and Rho, respectively. It is useful for research on cancer cell motility and invasion.

Glycerophosphoinositol 4-phosphate (GroPIns-4-P) is a metabolite of phospholipase A and serves as an inhibitor of adenylyl cyclase. In its disodium form, it regulates cAMP-dependent cellular functions. It can also induce membrane ruffling and stress fiber formation in serum-starved Swiss 3T3 cells through the activation of small GTPases Rac and Rho, respectively. Glycerophosphoinositol 4-phosphate disodium is used in studies related to cancer cell motility and invasion.

Propylbenzilylcholine mustard (PrBCM) is an irreversible, covalently binding selective antagonist for muscarinic receptors in rat hearts, specifically targeting receptor subtypes with low agonist affinity. This compound can inactivate these receptors in vitro in a dose- and time-dependent manner, maintaining receptor selectivity across various ionic strengths and GTP-containing buffers. PrBCM is utilized in fundamental pharmacological studies of muscarinic receptor structure and function, with a focus on cardiac muscarinic receptor heterogeneity and cardiovascular pharmacology research.

Dolastatin 10 trifluoroacetate is a potent antimitotic polypeptide isolated from a marine animal and is developed as a potential antitumor agent. Dolastatin 10 is found to have an activity to inhibit tubulin polymerization (IC50: 1.2 μM). Besides that, it

RBC6 is a small-molecule inhibitor that targets the Ras-like GTPase Ral. RBC6 blocks the interaction between Ral and its downstream effector protein RALBP1, thereby disrupting Ral-mediated cellular signaling. RBC6 inhibits Ral-dependent cell migration in mouse embryonic fibroblasts, as well as anchorage-independent growth in various human cancer cell lines.

Cornigerine is a natural product analog of colchicine produced by Colchicum cornigerum that inhibited tubulin polymerization both with and without microtubule-associated proteins, inhibited the binding of radiolabeled colchicine to tubulin, and stimulated tubulin-dependent GTP hydrolysis.

GTP-14564 is a novel tyrosine kinase inhibitor that also inhibits wt-FLT3 and ITD-FLT3. GTP-14564 inhibits the growth of interleukin-3-independent Ba/F1 expressing ITD-FLT3 at 3 μ m, whereas a 30-fold higher concentration of GTP-14564 is required to inhibit the FLT3 ligand-dependent growth (wt-FLT3) of Ba/F3 expressing wild-type FLT3. F3 expressing wild-type FLT3 (wt-FLT3).

PROTAC SOS1 degrader-2, a potent degrader of PROTAC SOS1, effectively reduces the expression of pERK and RAS-GTP in a dose-dependent manner. It significantly inhibits tumor growth in vivo [1].

mP6 (Myr-FEEERA-OH), a myristoylated peptide, selectively inhibits Gα 13's interaction with integrin β 3 while preserving talin-dependent integrin function. Additionally, mP6 impedes the GTPase activity of Rac1, Rap1, and Rab7, effectively reducing the infection of CHO-A24 cells [1].

TNP-GTP, a fluorescent derivative of guanosine 5'-triphosphate (GTP), essential for protein synthesis and gluconeogenesis, exhibits an emission peak at 552 nm when excited at 410 nm in water. Its fluorescence intensity increases and emission peaks shift to 544 nm and 532 nm in 40% and 80% N,N-dimethylformamide, respectively, due to the solvent's lower polarity compared to water. As a potent inhibitor of glutamate dehydrogenase (Ki = 2.7 μM), TNP-GTP enhances fluorescence and shifts its emission to 545 nm upon binding to this enzyme, a process reversible by GTP addition. Additionally, it serves as an antagonist to purinergic P2X2 and P2X2/3 receptors (IC50s = 0.4 and 1.2 nM, respectively) and selectively inhibits rat soluble guanylyl cyclase (sGC; Ki = 11 nM) over bovine liver glutamate dehydrogenase (GDH; Ki = 2.7 µM) and the calmodulin-dependent B. pertussis adenylyl cyclase (AC) toxin, with inhibition constants of 20 µM and 320 µM in the presence of manganese and magnesium, respectively.

ARF1 (2-17) inhibits both ARF-dependent (i.e., PLD) and ARF-independent pathways (i.e., PLC-β). This compound also suppresses GTP-γ-S-stimulated PLD activity, phospholipase C-β (PLC-β), and exocytosis.

mP6 (Myr-FEEERA-OH) TFA, a myristoylated peptide, inhibits the interaction between Gα13 and integrin β3 without disrupting talin-dependent integrin functions. It effectively blocks GTP usage by Rac1, Rap1, and Rab7, thereby inhibiting CHO-A24 cell infection.