gtp

8-Br-GTP, an analog of GTP, functions as both a competitive inhibitor of FtsZ polymerization and GTPase activity (with a K i value of 31.8 μM). Moreover, it is capable of facilitating nucleic acid modification.

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).

Using specific antisera raised against synthetic peptides, we find that three distinct GTP-binding protein alpha subunits remain bound to the plasma membrane even after activation with nonhydrolyzable GTP analog. Trypsin cleaves each alpha subunit at a si

Guanosine 5'-triphosphate trisodium salt (5'-GTP trisodium salt) activates signal-transducing G proteins involved in cellular processes such as proliferation, differentiation, and activation of intracellular kinase cascades. It regulates proliferation and apoptosis through the hydrolysis by small GTPases Ras and Rho, and plays a role in vesicle docking, fusion, and formation via Rab. Additionally, GTP serves as an energy-rich precursor for the biosynthesis of DNA and RNA.

Mant-GTPγS, an effective GTP analog, displays strong competitive inhibition of adenylyl cyclase (AC). Additionally, it acts as a potent inhibitor of YdeH.

GTPγS tetralithium (Guanosine 5'-[γ-thio]triphosphate tetralithium) is a G-protein activator, a non-hydrolyzable GTP analog that protects proteins from proteolytic degradation.GTPγS tetralithium is involved in the detection of cells expressing recombinant receptors and endogenous receptors. GTPγS tetralithium is involved in the detection of GPCR signaling in cells expressing recombinant receptors as well as in cells and tissues expressing endogenous receptors, and can be assayed to measure agonist-induced desensitization of two human polymorphic α2B-adrenoceptor variants.

dGTP (2'-Deoxyguanosine-5'-triphosphate) is a guanosine nucleotide highly susceptible to oxidative damage, resulting in 8-O-GDP, 8-O-dGTP, 8-O-GTP, and 8-O-dGTP.

RAS GTPase inhibitor 1 is a RAS GTPase inhibitor with potential antitumor activity.

3'-O-Methylguanosine-5'-O-triphosphate (3'-O-methyl GTP), a methylated derivative of GTP, serves as a chain termination reagent in synthesizing early RNA polymerase II elongation intermediates.

5′-Guanylyl methylenediphosphonate (sodium) serves as a GTP analogue and acts as a specific, competitive inhibitor of the GTP reaction in protein synthesis [1].

Guanosine-5'-triphosphate disodium salt (5'-GTP disodium salt) is an enhancer of myogenic cell differentiation and serves as an energy source for translation and other critical cellular processes.

2’-O-Methylguanosine-5’-O-triphosphate (2’-methyl GTP) acts as an inhibitor targeting the hepatitis C virus (HCV) non-structural protein 5B (NS5B; with an IC50 of 3.5 µM), and serves as an active metabolite of the prodrug IDX184 through a 2’-methylguanosine intermediate transformation. Additionally, at a concentration of 50 µM, it promotes tubulin polymerization. Notably, levels of 2’-methyl GTP are reduced in the tumoral tissues of patients with hepatocellular carcinoma in comparison to the adjacent normal tissues.

Sp-Guanosine-5'-O-(1-thiotriphosphate) (Sp-GTP-α-S), an isomer of the sulfur-containing nucleotide derivative GTP-α-S, demonstrates the ability to bind tubulin and facilitate microtubule assembly in cell-free assays at a concentration of 20 mM.

5'-GTP trisodium salt hydrate, an activator of the signal-transducing G proteins, serves as a precursor of mononucleotide units in the enzymatic biosynthesis of DNA and RNA.

8-Bromoguanosine-5'-O-triphosphate, a derivative of guanosine 5'-triphosphate (GTP) - the energy substrate for protein synthesis and gluconeogenesis, acts as an inhibitor of the E. coli GTPase FtsZ with an inhibition constant (Ki) of 31.8 µM. Furthermore, at a concentration of 500 µM, it facilitates the assembly of porcine brain microtubules in a cell-free assay.

Tyrphostin 8(4-Hydroxybenzylidenemalononitrile) is a potent GTPase inhibitor that inhibits EGFR kinase with an IC50 of 560 μM.Tyrphostin 8 inhibits protein serine threonine calmodulin phosphatases (IC50=21 μM), enhances transferrin receptor-mediated transcytosis in Caco-2 cells, and increases the hypoglycemic effect of oral insulin-transferrin. hypoglycemic effect.

2,4-Diamino-6-hydroxypyrimidine (DAHP) (DAHP) is a selective, specific inhibitor of GTP cyclohydrolase I, the rate limiting step for de novo pterin synthesis

Ac-Ala-OH (N-Acetyl-L-alanine) is a substrate for Guanine nucleotide-binding protein G(I)/G(S)/G(O) gamma-2 subunit, Myelin basic protein, GTP-binding nuclear protein Ran, Tropomyosin alpha 4 chain, HIV-1 Rev binding protein 2, Xaa-Pro dipeptidase, Thymosin beta-10, Actin-like protein 3, Alanine aminotransferase, Serine/threonine protein Phosphatase PP1-beta catalytic subunit,10 kDa heat shock protein (mitochondrial), Calmodulin and Beta-1-syntrophin.

2-Ketoglutaric acid is a key molecule in the tricarboxylic acid cycle,is also connected to glutamic acid and glutamine metabolisms through the transamination reactions.

CID-4785700 is a potent pan-GTPase inhibitor that inhibits Rab7 and inhibits the fungal histone acetyltransferase Rtt109 that binds to Asf1 and Vps75, and can be used in the study of lupus.

IMM-01 is a novel class of small-molecule agonists of the mammalian Diaphanous (mDia)-related formins, which act downstream of Rho GTPases to assemble actin filaments, and their organization with microfilaments to establish and maintain cell polarity during migration and asymmetric division. GTP-bound Rho activates mDia family members by disrupting the interaction between the DID and DAD autoregulatory domains, which releases the FH2 domain to modulate actin and microtubule dynamics[1].

G-Protein antagonist peptide acetate is a truncated substance P-related peptide, competes with receptor for G protein binding. G-Protein antagonist peptide acetate inhibits the activation of Gi or Go by M2 muscarinic cholinergic receptor (M2 mAChR) or of Gs by beta-adrenergic receptor in the reconstituted phospholipid vesicles, assayed by receptor-promoted GTP hydrolysis

AZD4747 is a selective and potent inhibitor of the mutant GTPase KRASG12C that crosses the blood-brain barrier and has potential antitumor activity for the study of pancreatic and colorectal adenocarcinoma.

RMC-7977 is a highly selective inhibitor of the active (GTP-bound) forms of KRAS, HRAS, and NRAS with anticancer activity for the study of solid tumors with KRAS G12C mutations.

Rac GTPase fragment is a peptide with the sequence H2N-Val-Phe-Asp-Glu-Ala-Ile-Arg-Ala-Val-OH, MW= 1019.15. Rac is a subfamily of the Rho family of GTPases, small signaling G proteins (more specifically a GTPase).

ddGTP (2′,3′-Dideoxyguanosine 5′-triphosphate) is a type of 2',3′-dideoxyribonucleoside 5'-triphosphate (ddNTP) that functions as a chain-elongating inhibitor of DNA polymerase in DNA sequencing.

gTPA2-OMe is a potential hole transport layer candidate for perovskite solar cells (PSCs).

7-Deaza-7-propargylamino-dGTP is a dGTP analogue specifically engineered for gene sequencing.

7-Deaza-7-propargylamino-ddGTP is a gene sequencing analog of dideoxyguanosine triphosphate (ddGTP).

7-Deaza-7-propargylamino-3’-azidomethyl-dGTP is a widely used deoxyguanosine triphosphate (dGTP) analog in next generation sequencing (NGS).

Rp-dGTPαS, an enantiomer of the dNTPαS nucleotide, serves as the substrate for SAMHD1, a critical regulator of cellular dNTP levels that curtails the replication of viruses (HIV-1, etc.) in CD4+ myeloid lineage and resting T cells. The SAMHD1 tetrameric complex facilitates the hydrolysis of Rp-dGQTPαS into 2'-deoxynucleosides and triphosphates [1].

7-Deaza-dGTP tetralithium is utilized for the amplification of GC-rich DNA sequences [1].

2′,3′-Dideoxyguanosine 5′-triphosphate (ddGTP) trisodium, a member of the 2',3'-dideoxyribonucleoside 5'-triphosphates (ddNTPs), functions as a chain-elongating inhibitor of DNA polymerase, pivotal for DNA sequencing. It operates either as an inhibitor or a substrate for DNA polymerase α [1] [2] [3].

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

TBB (NSC-231634)(NSC-231634) is a highly selective, ATP GTP-competitive inhibitor of casein kinase-2 (CK2).

QS11 is a GTPase activating protein of ADP-ribosylation factor 1 (ARFGAP1) inhibitor. Modulates ARF-GTP levels and synergizes with the Wnt/β-catenin signaling pathway to upregulate β-catenin nuclear translocation. Also reduces in vitro migration of metastatic human breast cancer cells.

BI-3406 is an orally active, highly potent and selective between KRAS and Son of Sevenless 1 (SOS1) interaction inhibitor(IC50 : 6 nM),with anticancer activity.

Azathioprine (BW 57-322), an immunosuppressive agent, inhibits purine synthesis and GTP-binding protein Rac1 activation.

RBC8 is a specific GTPases RalA/RalB inhibitor by inhibiting the binding of Ral to its effector RALBP1, no inhibition on the GTPases RhoA and Ras.

MLS-573151 is a selective inhibitor of GTPase Cdc42(EC50 of 2 μM). It is inactive against other GTPases family members, such as Rab2, Rab7, H-Ras, Rac1, Rac 2 and RhoA wild-type. MLS-573151 acts by blocking the binding of GTP to Cdc42.

ML-097 (CID-2160985) is a universal activator of Ras-related GTPases.

CID44216842 (KUC103479N-02) is a potent Cdc42-selective guanine nucleotide binding lead inhibitor. The EC50s for Cdc42 WT and Cdc42Q61L mutant are 1.0 and 1.2 μM in GTP binding assay, respectively. The EC50s for Cdc42 WT and Cdc42Q61L mutant are 0.3 and 0.5 μM in GDP binding assay, respectively. Use as a molecular probe.

MLS000532223 is a selectiveRho family GTPases inhibitor(EC50 : 16 μM to 120 μM).

Ara-G is an analog of the nucleoside guanosine and an active metabolite of nelarabine .1,2 Ara-G accumulates in T lymphoblasts and malignant T-lymphoid cells, where it is phosphorylated to produce ara-GTP and incorporated into the DNA.3,1 Ara-G inhibits DNA replication by 92% after 30 minutes when used at a concentration of 50 μM in CEM cells, which are used as a model for human T lymphoblasts.1 It also halts the cell cycle at the sub-G1 phase and induces apoptosis in CEM cells.3 Syngeneic bone marrow containing 6C3HED tumor cells treated with ara-G (100 mM) ex vivo prior to transplantation increases survival of lethally irradiated mice and induces reconstitution of lymphoid, myeloid, and erythroid cell linages.4References1. Leanza, L., Miazzi, C., Ferraro, P., et al. Activation of guanine-β-D-arabinofuranoside and deoxyguanosine to triphosphates by a common pathway blocks T lymphoblasts at different checkpoints. Exp. Cell Res. 316(20), 3443-3453 (2010).2. Lambe, C.U., Averett, D.R., Paff, M.T., et al. 2-Amino-6-methoxypurine arabinoside: An agent for T-cell malignancies. Cancer Res. 55(15), 3352-3356 (1995).3. Rodriguez, C.O., Jr., Stellrecht, C.M., and Gandhi, V. Mechanisms for T-cell selective cytotoxicity of arabinosylguanine. Blood 102(5), 1842-1848 (2003).4. Kurtzberg, J. Guanine arabinoside as a bone marrow-purging agent. Ann. N.Y. Acad. Sci 685(1), 225-236 (1993). Ara-G is an analog of the nucleoside guanosine and an active metabolite of nelarabine .1,2 Ara-G accumulates in T lymphoblasts and malignant T-lymphoid cells, where it is phosphorylated to produce ara-GTP and incorporated into the DNA.3,1 Ara-G inhibits DNA replication by 92% after 30 minutes when used at a concentration of 50 μM in CEM cells, which are used as a model for human T lymphoblasts.1 It also halts the cell cycle at the sub-G1 phase and induces apoptosis in CEM cells.3 Syngeneic bone marrow containing 6C3HED tumor cells treated with ara-G (100 mM) ex vivo prior to transplantation increases survival of lethally irradiated mice and induces reconstitution of lymphoid, myeloid, and erythroid cell linages.4 References1. Leanza, L., Miazzi, C., Ferraro, P., et al. Activation of guanine-β-D-arabinofuranoside and deoxyguanosine to triphosphates by a common pathway blocks T lymphoblasts at different checkpoints. Exp. Cell Res. 316(20), 3443-3453 (2010).2. Lambe, C.U., Averett, D.R., Paff, M.T., et al. 2-Amino-6-methoxypurine arabinoside: An agent for T-cell malignancies. Cancer Res. 55(15), 3352-3356 (1995).3. Rodriguez, C.O., Jr., Stellrecht, C.M., and Gandhi, V. Mechanisms for T-cell selective cytotoxicity of arabinosylguanine. Blood 102(5), 1842-1848 (2003).4. Kurtzberg, J. Guanine arabinoside as a bone marrow-purging agent. Ann. N.Y. Acad. Sci 685(1), 225-236 (1993).

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

BC-LI-0186 (4-(2,3-dimethyl-5-oxo-4-propan-2-ylpyrazol-1-yl)-N-(2-phenoxyethyl)benzenesulfonamide) is a potent and selective inhibitor of the interaction of Leucyl-tRNA synthetase (LRS) and Ras-related GTP-binding protein D (RagD) with IC50 of 46.11 nM. BC-LI-0186 competitively binds the RagD interaction site of LRS with Kd of 42.1 nM and has no effect on LRS-vps34, LRS-eprs, RagB-RagD association, mTORC1 complex formation. BC-LI-0186 potently inhibits the activity of tumor-associated MTOR mutants and the growth of rapamycin-resistant cancer cells. BC-LI-0186 can be used for lung cancer-related research.

KRAS inhibitor-9 (DUN09716) is a potent KRAS inhibitor with Kd of 92 μM that blocks the formation of GTP-KRAS and downstream activation of KRAS. KRAS inhibitor-9 causes G2/M cell cycle arrest and induces apoptosis. KRAS inhibitor-9 selectively inhibits the proliferation of NSC-LC cells with KRAS mutation but not normal lung cells

KRA-533, a potent KRAS agonist, directly targets the GTP/GDP binding pocket within the KRAS protein, inhibiting GTP cleavage. This inhibition leads to the buildup of constitutively active GTP-bound KRAS, which subsequently activates both apoptotic and autophagic cell death pathways specifically in cancer cells.

1. Methylophiopogonanone B (MOPB) induces cell morphological change and Rho activation via melanocyte dendrite retraction and stress fiber formation.

pan activator of Ras-related GTPases