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Guanosine triphosphate- 13C (GTP- 13C) dilithium is 13C-labeled Guanosine triphosphate (HY-113225). Guanosine triphosphate is a native nucleotide. The derivatives of GTP may be used as specific inhibitors against COVID-19.
Guanosine triphosphate-d14(GTP-d14) dilithium is deuterium labeled Guanosine triphosphate (HY-113225). Guanosine triphosphate is a native nucleotide. The derivatives of GTP may be used as specific inhibitors against COVID-19.
Guanosine triphosphate- 15N5 (GTP- 15N5) dilithium is 15N labeled Guanosine triphosphate (HY-113225). Guanosine triphosphate is a native nucleotide. The derivatives of GTP may be used as specific inhibitors against COVID-19.
Guanosine triphosphate- 13C10 (GTP- 13C10) dilithium is 13C-labeled Guanosine triphosphate (HY-113225). Guanosine triphosphate is a native nucleotide. The derivatives of GTP may be used as specific inhibitors against COVID-19.
GTP-14564 is a tyrosine kinase inhibitor targeting to internal tandem duplication (ITD) and FLT3. GTP-14564 inhibits FLT3 ligand-dependent growth in Ba/F3 leukemia cells .
Guanosine triphosphate- 15N5,d14 (GTP- 15N5,d14) dilithium is deuterium and 15N labeled Guanosine triphosphate (HY-113225). Guanosine triphosphate is a native nucleotide. The derivatives of GTP may be used as specific inhibitors against COVID-19.
Guanosine triphosphate- 13C10, 15N5 (tetraammonium) is the 13C and 15N labeled Guanosine triphosphate tetraammonium[1]. Guanosine triphosphate is a native nucleotide. The derivatives of GTP may be used as specific inhibitors against COVID-19[2].
GTPγS (tetralithium) is a G-protein activator that protects proteins from proteolytic degradation, stimulates GLUT4 translocation in a tyrosine kinase-dependent manner, stimulate phospholipases and induce actin polymerization. GTPγS (tetralithium) to couple with G- protein α, to study its effect on kinase activity. GTPγS (tetralithium) acts as a component of lysis buffer .
8-Br-GTP, a GTP analog, is a competitive FtsZ polymerization and GTPase activity (Ki of 31.8 μM) inhibitor. 8-Br-GTP can be used for nucleic acid modification .
5'-GTP trisodium salt hydrate is an activator of the signal transducing G proteins and also serves as an energy-rich precursor of mononucleotide units in the enzymatic biosynthesis of DNA and RNA.
Guanosine-5'-triphosphate disodium salt (5'-GTP trisodium salt) is an activator of the signal transducing G proteins and also serves as an energy-rich precursor of mononucleotide units in the enzymatic biosynthesis of DNA and RNA .
7-Methyl-guanosine-5'-triphosphate (m7GTP) sodium is a guanosine 5'-phosphate. 7-Methyl-guanosine-5'-triphosphate sodium phosphorothioate analog is a potent cap-dependent translation inhibitor .
ADT-007 is a potent and orally active pan-RAS inhibitor with strong anticancer effects. ADT-007 binds RAS in a nucleotide-free conformation to block GTP activation. ADT-007 potently and selectively inhibits the growth of cancer cells with mutated or hyper-activated wild-type RAS isozymes .
GDP-α-D-mannose disodium is the donor substrate for mannosyltransferases and the precursor of GDP-β-L-fucose. GDP-α-D-mannose disodium gives a competitive inhibition with respect to GTP (Ki 14.7 μM) and an uncompetitive inhibition with respect to mannose-1-P (Ki 115 μM) .
Guanylyl Imidodiphosphate (Guanosine 5'-[β,γ-imido]triphosphate) trisodium is a non-hydrolysable GTP analogue, an activator of ADP-ribosylation factor (ARF) and a potent stimulator of adenylate cyclase. Imidodiphosphate trisodium can be used in protein synthesis studies .
SOS1 activator 1 (Compound 64) is a potent activator of SOS1-mediated nucleotide exchange with a Kd of 44 nM. SOS1 is a guanine nucleotide exchange factor that catalyzes the exchange of GDP for GTP on RAS .
NF449 octasodium is a highly potent P2X1 receptor antagonist, with IC50s of 0.28, 0.69, and 120 nM for rP2X1, rP2X1+5, P2X2+3, respectively. NF449 octasodium is a Gsα-selective G Protein antagonist. NF449 octasodium suppresses the rate of GTP[γS] binding to Gsα-s, inhibits the stimulation of adenylyl cyclase activity, and blocks the coupling of β-adrenergic receptors to Gs .
KRA-533 is a potent KRAS agonist. KRA-533 binds to the GTP/GDP binding pocket in the KRAS protein to prevent GTP cleavage, resulting in the accumulation of constitutively active GTP-bound KRAS that triggers both apoptotic and autophagic cell death pathways in cancer cells.
dGTP (2'-Deoxyguanosine-5'-triphosphate), a guanosine nucleotide, can be used in deoxyribonucleic acid synthesis. Guanosine nucleotides (GDP, GTP, dGDP, and dGTP) are highly susceptible to oxidative damage to 8-oxo-GDP (8-O-GDP), 8-O-dGTP, 8-O-GTP, and 8-O-dGTP .
ZINC69391, a specific Rac1 inhibitor, interferes with Rac1-GEF interaction by masking Trp56 residue on Rac1 surface. ZINC69391 interferes with the interaction of Rac1 with Dock180 and reduces Rac1-GTP levels. ZINC69391 induces apoptosis, and shows antiproliferative and antimetastatic effects .
SOS1 agonist-1 (compound 79) is an agonist for the Son of sevenless homologue SOS1. SOS1 is a guanine nucleotide exchange factor that catalyzes the exchange of GDP to GTP on RAS and regulates RAS activation. SOS1 agonists increase nucleotide exchange on RAS, enhance cellular RAS-GTP levels, and trigger biphasic signaling changes in ERK1/2 phosphorylation. Play an anti-cancer role [1] .
GRP (14-27) (human, porcine, canine) is a bombesin receptor ligand. The specific binding of GRP (14-27) is inhibited by GTP and GDP, whereas GMP was without effect .
Kobe0065 is a novel and effective inhibitor of Ras-Raf interaction, competitively inhibiting the binding of H-Ras·GTP to c-Raf-1 RBD with a Ki value of 46±13 μM.
MLS000532223 is a high affinity, selective inhibitor of Rho family GTPases, with EC50 values ranging from 16 μM to 120 μM. MLS000532223 prevents GTP binding to several GTPases .
ASN04421891 is a potent GPR17 receptor modulator, with an EC50 of 3.67 nM in [35S]GTPγS binding assay. ASN04421891 can be used for neurodegenerative diseases research .
dGTP- 13C10 (2'-Deoxyguanosine-5'-triphosphate- 13C10) dilithium is 13C-labeled dGTP (HY-138616). dGTP (2'-Deoxyguanosine-5'-triphosphate), a guanosine nucleotide, can be used in deoxyribonucleic acid synthesis. Guanosine nucleotides (GDP, GTP, dGDP, and dGTP) are highly susceptible to oxidative damage to 8-oxo-GDP (8-O-GDP), 8-O-dGTP, 8-O-GTP, and 8-O-dGTP.
dGTP- 15N5 (2'-Deoxyguanosine-5'-triphosphate- 15N5) dilithium is 15N labeled dGTP (HY-138616). dGTP (2'-Deoxyguanosine-5'-triphosphate), a guanosine nucleotide, can be used in deoxyribonucleic acid synthesis. Guanosine nucleotides (GDP, GTP, dGDP, and dGTP) are highly susceptible to oxidative damage to 8-oxo-GDP (8-O-GDP), 8-O-dGTP, 8-O-GTP, and 8-O-dGTP.
dGTP-d14 (2'-Deoxyguanosine-5'-triphosphate-d14) dilithium is deuterium labeled dGTP (HY-138616). dGTP (2'-Deoxyguanosine-5'-triphosphate), a guanosine nucleotide, can be used in deoxyribonucleic acid synthesis. Guanosine nucleotides (GDP, GTP, dGDP, and dGTP) are highly susceptible to oxidative damage to 8-oxo-GDP (8-O-GDP), 8-O-dGTP, 8-O-GTP, and 8-O-dGTP.
MK-6892 is a potent, selective, and full agonist for the high affinity nicotinic acid (NA) receptor GPR109A. Ki and GTPγS EC50 of MK-6892 on the Human GPR109A is 4 nM and 16 nM, respectively.
Kobe2602 is a Ras-Raf interaction inhibitor. Kobe2602 inhibits the binding of H-Ras·GTP to c-Raf-1 RBD with a Ki of 149 μM. Kobe2602 has antitumor activity .
ASN04885796 (compound IV) is an GPR17 activator with an EC50 of 2.27 nM for GPR17 induced GTPγS binding. ASN04885796 has neuroprotective property and can be used for research of neurological diseases .
2'-Deoxyguanosine 5'-monophosphate disodium (5′-dGMP disodium) is a mononucleotide having guanine as the nucleobase. 2'-Deoxyguanosine 5'-monophosphate disodium is a nucleic acid guanosine triphosphate (GTP) derivative .
ASN02563583, a compound that regulates the activity of the GPR17 receptor, has a IC50 value of 0.64 nM in [35S]GTPγS binding assay. ASN02563583 can be used in the study of neurological diseases .
dGTP- 13C10, 15N5 (2'-Deoxyguanosine-5'-triphosphate- 13C10, 15N5) dilithium is 13C and 15N-labeled dGTP (HY-138616). dGTP (2'-Deoxyguanosine-5'-triphosphate), a guanosine nucleotide, can be used in deoxyribonucleic acid synthesis. Guanosine nucleotides (GDP, GTP, dGDP, and dGTP) are highly susceptible to oxidative damage to 8-oxo-GDP (8-O-GDP), 8-O-dGTP, 8-O-GTP, and 8-O-dGTP.
dGTP- 15N5,d14 (2'-Deoxyguanosine-5'-triphosphate- 15N5,d14) dilithium is deuterium and 15N labeled dGTP (HY-138616). dGTP (2'-Deoxyguanosine-5'-triphosphate), a guanosine nucleotide, can be used in deoxyribonucleic acid synthesis. Guanosine nucleotides (GDP, GTP, dGDP, and dGTP) are highly susceptible to oxidative damage to 8-oxo-GDP (8-O-GDP), 8-O-dGTP, 8-O-GTP, and 8-O-dGTP.
AZD1283 is a potent P2Y12 receptor antagonist with a binding IC50 of 11 nM and a GTPγS IC50 of 25 nM. AZD1283 has excellent antiplatelet aggregation potency. AZD1283 can be used to research thromboembolic disorders .
Mastoparan X is a GTP-binding regulatory protein (G protein)-activating peptide, and a tetradecapeptide from wasp venom. Mastoparan X acts function by the direct activation of G protein that couple to phospholipase C to cause secretion from various kinds of cells .
PC58538 is a cell division inhibitor, targeting to FtsZ. PC58538 shows moderate antibacterial activity, and inhibits cell division in vegetative cells of wild-type B. subtilis. PC58538 is also known to modulate the rate of GTP hydrolysis .
W123, a FTY720 analog, is a competitive sphingosine 1-phosphate type 1 (S1P1) receptor antagonist. W123 is measured by GTPγS activation, MAPK recruitment, cell migration, and ligand-induced receptor internalization .
Pelitrexol (AG 2037) is an inhibitor of glycinamide ribonucleotide formyltransferase (GARFT), a purine biosynthetic enzyme. Pelitrexol also inhibits mTORC1 by reducing GTP-bound Rheb level, a mTORC1 obligate activator. Pelitrexol shows robust tumor growth suppression in mice .
2-Ketoglutaric acid (Alpha-Ketoglutaric acid) is an intermediate in the production of ATP or GTP in the Krebs cycle. 2-Ketoglutaric acid also acts as the major carbon skeleton for nitrogen-assimilatory reactions. 2-Ketoglutaric acid is a reversible inhibitor of tyrosinase (IC50=15 mM) .
2-Ketoglutaric acid Sodium (Alpha-Ketoglutaric acid Sodium) is an intermediate in the production of ATP or GTP in the Krebs cycle. 2-Ketoglutaric acid Sodium also acts as the major carbon skeleton for nitrogen-assimilatory reactions. 2-Ketoglutaric acid Sodium is a reversible inhibitor of tyrosinase (IC50=15 mM) .
Calcium 2-oxoglutarate is an intermediate in the production of ATP or GTP in the Krebs cycle. Calcium 2-oxoglutarate also acts as the major carbon skeleton for nitrogen-assimilatory reactions. Calcium 2-oxoglutarate is a reversible inhibitor of tyrosinase (IC50=15 mM) .
GDP-α-D-mannose disodium is the donor substrate for mannosyltransferases and the precursor of GDP-β-L-fucose. GDP-α-D-mannose disodium gives a competitive inhibition with respect to GTP (Ki 14.7 μM) and an uncompetitive inhibition with respect to mannose-1-P (Ki 115 μM) .
GPR84 antagonist 3 (compound 42) is a potent GPR84 (G-protein-coupled receptor 84) antagonist. GPR84 antagonist 3 inhibits GTPγS, with a pIC50 of 8.28. GPR84 antagonist 3 has a favorable pharmacokinetic profile suitable .
TH1760 is an inhibitor of NUDIX-type 15 (NUDT15) with an IC50 value of 25 nM. TH1760 sensitizes cells to 6-thioguanine by enhancing the accumulation of 6-thio- (d) GTP in nucleic acids. TH1760 enhances the anti-leukemia effect of thiopurine .
2,4-Diamino-6-hydroxypyrimidine is a specific GTP cyclohydrolase I inhibitor (the rate-limiting enzyme in de novo pterin synthesis). 2,4-Diamino-6-hydroxypyrimidine blocks Tetrahydrobiopterin (BH4) synthesis and suppresses NO production .
Methylophiopogonanone B, homoisoflavonoid, is extracted from the root of Ophiopogon japonicas, shows high antioxidant ability . Methylophiopogonanone B increases GTP-Rho and acts via the Rho signaling pathway, inducing cell morphological change via actin cytoskeletal reorganization, including dendrite retraction and stress fiber formation .
RMC-0331 (RM-023) is a potent, selective and orally bioavailable SOS1 inhibitor. RMC-0331 is an in vivo tool compound that blocks RAS activation via disruption of the RAS-SOS1 interaction .
Farnesyl thiosalicylic acid amide (FTS-A) is an orally active derivative of farnesyl thiosalicylic acid (HY-14754). Farnesyl thiosalicylic acid amide reduces Ras-GTP levels and inhibits cell growth with IC50s of 20 and 10 μM for Panc-1 and U87 cells, respectively. Farnesyl thiosalicylic acid amide can be used for the research of cancer .
BI-3406 (compound I-6) is an orally active, highly potent and selective inhibitor of the interaction between KRAS and Son of Sevenless 1 (SOS1) with an IC50 of 6 nM. BI-3406 potently reduces the formation of GTP-loaded KRAS, and inhibits MAPK pathway signaling. BI-3406 has anticancer activity .
KRAS G12D inhibitor 14 is a potent KRAS G12D inhibitor with a KD of 33 nM for binding to KRAS G12D protein. KRAS G12D inhibitor 14 decreases the active form of KRAS G12D (KRAS G12D-GTP) but not KRAS G13D .
G-Protein antagonist peptide TFA is a truncated substance P-related peptide, competes with receptor for G protein binding. G-Protein antagonist peptide TFA 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 .
MLS-573151 (MLS000573151) is a selective GTPase Cdc42 inhibitor with an EC50 of 2 μM. MLS-573151 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 .
(4S)-PROTAC SOS1 degrader-1 is a potent PROTAC SOS1 degrader. (4S)-PROTAC SOS1 degrader-1 decreases the expression of pERK and RAS-GTP level in a dose-dependent manner. (4S)-PROTAC SOS1 degrader-1 significantly inhibits the tumor growth in vivo .
mP6 (Myr-FEEERA-OH) is a myristoylated peptide. mP6 inhibits the interaction of Gα13 with integrin β3 without disrupting talin-dependent integrin function. mP6 can block the GTP usage of Rac1, Rap1, and Rab7, effectively inhibiting the infection of CHO-A24 cells .
C-021 dihydrochloride is a potent CC chemokine receptor-4 (CCR4) antagonist. C-021 dihydrochloride potently inhibits functional chemotaxis in human and mouse with IC50s of 140 nM and 39 nM, respectively. C-021 dihydrochloride effectively prevents human CCL22-derived [ 35S]GTPγS from binding to the receptor with an IC50 of 18 nM .
BMS-986122 is a selective, potent positive allosteric modulator of the mu-opioid receptor (µ-OR). BMS-986122 shows potentiation of orthosteric agonist-mediated β-arrestin recruitment, adenylyl cyclase inhibition, and G protein activation. BMS-986122 potentiates DAMGO-mediated [ 35S]GTPγS binding in mouse brain membranes .
C-021 is a potent CC chemokine receptor-4 (CCR4) antagonist. C-021 potently inhibits functional chemotaxis in human and mouse with IC50s of 140 nM and 39 nM, respectively. C-021 effectively prevents human CCL22-derived [ 35S]GTPγS from binding to the receptor with an IC50 of 18 nM .
(±)-J-113397 is a potent and selective non-peptidyl ORL1 receptor antagonist with a Ki of 1.8 nM for cloned human ORL1. J-113397 inhibited nociceptin/orphanin FQ-stimulated GTPγS binding to CHO cells expressing ORL1 with an IC50 value of 5.3 nM. J-113397 can be used for researching the physiological roles of nociceptin/orphanin FQ .
RM-018 is a potent, functionally distinct tricomplex KRAS G12C active-state inhibitor. RM-018 retains the ability to bind and inhibit KRAS G12C/Y96D and could overcome resistance. RM-018 binds specifically to the GTP-bound, active [“RAS(ON)”] state of KRAS G12C .
LY487379 is a selective human mGluR2 positive allosteric modulator (PAM). LY487379 potentiates glutamate-stimulated [ 35S]GTPγS binding with EC50 values of 1.7 μM and >10 μM for mGlu2 and mGlu3 receptors respectively. LY487379 promotes cognitive flexibility and facilitates behavioral inhibition in a rat model. LY487379 can be used for schizophrenia research .
2-Ketoglutaric acid- 13C5 is the 13C labeled 2-Ketoglutaric acid[1]. 2-Ketoglutaric acid (Alpha-Ketoglutaric acid) is an intermediate in the production of ATP or GTP in the Krebs cycle. 2-Ketoglutaric acid also acts as the major carbon skeleton for nitrogen-assimilatory reactions. 2-Ketoglutaric acid is a reversible inhibitor of tyrosinase (IC50=15 mM)[2].
2-Ketoglutaric acid-d4 is the deuterium labeled 2-Ketoglutaric acid[1]. 2-Ketoglutaric acid (Alpha-Ketoglutaric acid) is an intermediate in the production of ATP or GTP in the Krebs cycle. 2-Ketoglutaric acid also acts as the major carbon skeleton for nitrogen-assimilatory reactions. 2-Ketoglutaric acid is a reversible inhibitor of tyrosinase (IC50=15 mM)[2].
2-Ketoglutaric acid-d6 is the deuterium labeled 2-Ketoglutaric acid[1]. 2-Ketoglutaric acid (Alpha-Ketoglutaric acid) is an intermediate in the production of ATP or GTP in the Krebs cycle. 2-Ketoglutaric acid also acts as the major carbon skeleton for nitrogen-assimilatory reactions. 2-Ketoglutaric acid is a reversible inhibitor of tyrosinase (IC50=15 mM)[2].
(4S)-PROTAC SOS1 degrader-1 (diTFA) is a potent PROTAC SOS1 degrader. (4S)-PROTAC SOS1 degrader-1 (diTFA) decreases the expression of pERK and RAS-GTP level in a dose-dependent manner. (4S)-PROTAC SOS1 degrader-1 (diTFA) significantly inhibits the tumor growth in vivo .
NIBR-0213 is a potent, orally active and selective S1P1 antagonist with efficacy in experimental autoimmune encephalomyelitis. NIBR-0213 displays potent and comparable potency on human and rat S1P1 (IC50 of 2.0 nM and 2.3 nM, respectively) in GTPγ 35S assays .
AMN082, a selective, orally active, and brain penetrant mGluR7 agonist, directly activates receptor signaling via an allosteric site in the transmembrane domain. AMN082 potently inhibits cAMP accumulation and stimulates GTPγS binding (EC50 values, 64-290 nM) at transfected mammalian cells expressing mGluR7. AMN082 shows selectivity over other mGluR subtypes and selected ionotropic glutamate receptors. Antidepressant effects .
ZCZ011 is a potent and brain penetrant cannabinoid 1 (CB1) receptor positive allosteric modulator. ZCZ011 potentiates binding of CP55,940 to the CB1 receptor, enhances anandamide (AEA)-stimulated GTPγS binding in mouse brain membranes. ZCZ011 increases β-arrestin recruitment and ERK phosphorylation in hCB1 cells. ZCZ011 can be used for researching neuropathic and inflammatory pain .
Trap-101 hydrochloride is a potent, selective and competitive antagonist of NOP receptors over classical opioid receptors. Trap-101 stimulates GTPγ 35S binding to CHOhNOP membranes with pKi values of 8.65, 6.60, 6.14 and <5 for NOP, μ-, κ-, and δ-opioid receptors, respectively. Trap-101 attenuates motor deficits in a rat model of parkinson's disease and can be used for the research of nervous system diseases .
LY487379 hydrochloride is a selective human mGluR2 positive allosteric modulator (PAM). LY487379 hydrochloride potentiates glutamate-stimulated [ 35S]GTPγS binding with EC50 values of 1.7 μM and >10 μM for mGlu2 and mGlu3 receptors respectively. LY487379 hydrochloride promotes cognitive flexibility and facilitates behavioral inhibition in a rat model. LY487379 hydrochloride can be used for schizophrenia research .
MRS2365 is a potent and selective P2Y1 receptor (EC50=0.4 nM) /[ 35S]GTPγS binding/β-arrestin 2 recruitment agonist with an EC50 of 0.4 nM. MRS2365 relieves mechanical allodynia and increases mechanical sensitivity. MRS2365 shows little agonist or antagonist activity at the P2Y12 or P2Y13 receptors .
2'-Deoxyguanosine 5'-monophosphate- 13C10, 15N5 (disodium) is the 13C and 15N labeled 2'-Deoxyguanosine 5'-monophosphate disodium[1]. 2'-Deoxyguanosine 5'-monophosphate disodium (5′-dGMP disodium) is a mononucleotide having guanine as the nucleobase. 2'-Deoxyguanosine 5'-monophosphate disodium is a nucleic acid guanosine triphosphate (GTP) derivative[2].
2-Ketoglutaric acid- 13C (Alpha-Ketoglutaric acid- 13C) is a 13C labeled 2-Ketoglutaric acid (HY-W013636) . 2-Ketoglutaric acid (Alpha-Ketoglutaric acid) is an intermediate in the production of ATP or GTP in the Krebs cycle. 2-Ketoglutaric acid also acts as the major carbon skeleton for nitrogen-assimilatory reactions. 2-Ketoglutaric acid is a reversible inhibitor of tyrosinase (IC50=15 mM) .
CID44216842 (Cdc42-IN-1) 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 .
AMN082 free base, a selective, orally active, and brain penetrant mGluR7 agonist, directly activates receptor signaling via an allosteric site in the transmembrane domain. AMN082 free base potently inhibits cAMP accumulation and stimulates GTPγS binding (EC50 values, 64-290 nM) at transfected mammalian cells expressing mGluR7. AMN082 free base shows selectivity over other mGluR subtypes and selected ionotropic glutamate receptors. Antidepressant effects .
Z62954982 (ZINC08010136) is a potent, selective and cell-permeable Rac1 (IC50=12 μM) inhibitor that is 4 times more effective than NSC23766 (HY-15723A) (IC50=50 μM). Z62954982 disrupts the Rac1/Tiam1 complex and decreases cytoplasmic levels of active Rac1 (GTP-bound Rac1), without affecting the activity of other Rho GTPases (such as Cdc42 or RhoA) .
SX-517 is a dual CXCR2/1 antagonist, containing boronic acid. SX-517 inhibits CXCL1-induced Ca 2+ flux (IC50=38 nM), and antagonizes CXCL8-induced [(35)S]GTPγS binding (IC50=60 nM) and ERK1/2 phosphorylation. SX-517 has significant ability for inflammation suppression, in both humanized polymorphonuclear (PMN) cells and in murine model .
BBO-8520 is a direct small molecule covalent inhibitor targeting KRAS G12C with high oral availability. BBO-8520 has the characteristics of KRAS G12C (OFF) inhibitor and the function of blocking KRAS G12C (ON) signal. BBO-8520 inhibits cell proliferation by inhibiting KRAS G12C (ON) by binding GTP protein. BBO-8520 can block RAS-RAF1 interaction and return KRAS G12C to the inactive (OFF) state .
KRAS inhibitor-9, a potent KRAS inhibitor (Kd=92 μM), blocks the formation of GTP-KRAS and downstream activation of KRAS. KRAS inhibitor-9 binds to KRAS G12D, KRAS G12C and KRAS Q61H protein with a moderate binding affinity. KRAS inhibitor-9 causes G2/M cell cycle arrest and induces apoptosis. KRAS inhibitor-9 selectively inhibits the proliferation of NSCLC cells with KRAS mutation but not normal lung cells .
BC-LI-0186 is a potent and selective inhibitor of Leucyl-tRNA synthetase (LRS; LeuRS) and Ras-related GTP-binding protein D (RagD) interaction (IC50=46.11 nM). BC-LI-0186 competitively binds to the RagD interacting site of LRS (Kd=42.1 nM) and has on effects on LRS-Vps34, LRS-EPRS, RagB-RagD association, mTORC1 complex formation or the activities of 12 kinases. BC-LI-0186 can effectively suppress the activity of cancer-associated MTOR mutants and the growth of rapamycin-resistant cancer cells. BC-LI-0186 is a promising agent for lung cancer research .
MRTX1133 is a noncovalent, potent, and selective KRAS G12D inhibitor. MRTX1133 optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated KD against KRAS G12D of 0.2 pM. MRTX1133 prevents SOS1-catalyzed nucleotide exchange and/or formation of the KRAS G12D/GTP/RAF1 complex, thereby inhibiting mutant KRAS-dependent signal transduction. MRTX1133 selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tumor cells. MRTX1133 has single digit nanomolar activity in cellular assays and marked in vivo efficacy in tumor models harboring KRAS G12D mutations .
7-Methyl-guanosine-5'-triphosphate (m7GTP) sodium is a guanosine 5'-phosphate. 7-Methyl-guanosine-5'-triphosphate sodium phosphorothioate analog is a potent cap-dependent translation inhibitor .
GDP-mannose pyrophosphorylase (ManC) (GDP-MP) is a cytoplasmic protein that catalyzes the formation of GDP-mannose. GDP-mannose pyrophosphorylase (ManC) is the precursor for the mannose residues in glycoconjugates, using mannose 1-phosphate and GTP as substrates .
Guanylyl Imidodiphosphate (Guanosine 5'-[β,γ-imido]triphosphate) trisodium is a non-hydrolysable GTP analogue, an activator of ADP-ribosylation factor (ARF) and a potent stimulator of adenylate cyclase. Imidodiphosphate trisodium can be used in protein synthesis studies .
Mastoparan X is a GTP-binding regulatory protein (G protein)-activating peptide, and a tetradecapeptide from wasp venom. Mastoparan X acts function by the direct activation of G protein that couple to phospholipase C to cause secretion from various kinds of cells .
G-Protein antagonist peptide TFA is a truncated substance P-related peptide, competes with receptor for G protein binding. G-Protein antagonist peptide TFA 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 .
GRP (14-27) (human, porcine, canine) is a bombesin receptor ligand. The specific binding of GRP (14-27) is inhibited by GTP and GDP, whereas GMP was without effect .
mP6 (Myr-FEEERA-OH) is a myristoylated peptide. mP6 inhibits the interaction of Gα13 with integrin β3 without disrupting talin-dependent integrin function. mP6 can block the GTP usage of Rac1, Rap1, and Rab7, effectively inhibiting the infection of CHO-A24 cells .
Guanosine-5'-triphosphate disodium salt (5'-GTP trisodium salt) is an activator of the signal transducing G proteins and also serves as an energy-rich precursor of mononucleotide units in the enzymatic biosynthesis of DNA and RNA .
GDP-α-D-mannose disodium is the donor substrate for mannosyltransferases and the precursor of GDP-β-L-fucose. GDP-α-D-mannose disodium gives a competitive inhibition with respect to GTP (Ki 14.7 μM) and an uncompetitive inhibition with respect to mannose-1-P (Ki 115 μM) .
5'-GTP trisodium salt hydrate is an activator of the signal transducing G proteins and also serves as an energy-rich precursor of mononucleotide units in the enzymatic biosynthesis of DNA and RNA.
2'-Deoxyguanosine 5'-monophosphate disodium (5′-dGMP disodium) is a mononucleotide having guanine as the nucleobase. 2'-Deoxyguanosine 5'-monophosphate disodium is a nucleic acid guanosine triphosphate (GTP) derivative .
2-Ketoglutaric acid (Alpha-Ketoglutaric acid) is an intermediate in the production of ATP or GTP in the Krebs cycle. 2-Ketoglutaric acid also acts as the major carbon skeleton for nitrogen-assimilatory reactions. 2-Ketoglutaric acid is a reversible inhibitor of tyrosinase (IC50=15 mM) .
2-Ketoglutaric acid Sodium (Alpha-Ketoglutaric acid Sodium) is an intermediate in the production of ATP or GTP in the Krebs cycle. 2-Ketoglutaric acid Sodium also acts as the major carbon skeleton for nitrogen-assimilatory reactions. 2-Ketoglutaric acid Sodium is a reversible inhibitor of tyrosinase (IC50=15 mM) .
Calcium 2-oxoglutarate is an intermediate in the production of ATP or GTP in the Krebs cycle. Calcium 2-oxoglutarate also acts as the major carbon skeleton for nitrogen-assimilatory reactions. Calcium 2-oxoglutarate is a reversible inhibitor of tyrosinase (IC50=15 mM) .
GDP-α-D-mannose disodium is the donor substrate for mannosyltransferases and the precursor of GDP-β-L-fucose. GDP-α-D-mannose disodium gives a competitive inhibition with respect to GTP (Ki 14.7 μM) and an uncompetitive inhibition with respect to mannose-1-P (Ki 115 μM) .
Methylophiopogonanone B, homoisoflavonoid, is extracted from the root of Ophiopogon japonicas, shows high antioxidant ability . Methylophiopogonanone B increases GTP-Rho and acts via the Rho signaling pathway, inducing cell morphological change via actin cytoskeletal reorganization, including dendrite retraction and stress fiber formation .
RHEB is an important small GTPase that acts as an allosteric activator of the mTORC1 complex, a key nutrient sensor that controls cell growth and biomass production. In response to signals such as nutrients and growth factors, RHEB activates the MTOR kinase within mTORC1 by inducing conformational changes. RHEB Protein, Human (GST) is the recombinant human-derived RHEB protein, expressed by E. coli , with N-GST labeled tag. The total length of RHEB Protein, Human (GST) is 184 a.a., with molecular weight of ~45.0 kDa.
RHEB is an important small GTPase that acts as an allosteric activator of the mTORC1 complex, a key nutrient sensor that controls cell growth and biomass production. In response to signals such as nutrients and growth factors, RHEB activates the MTOR kinase within mTORC1 by inducing conformational changes. RHEB Protein, Human (sf9, N-His) is the recombinant human-derived RHEB protein, expressed by P. pastoris , with N-His labeled tag. The total length of RHEB Protein, Human (sf9, N-His) is 181 a.a., with molecular weight of ~21 kDa.
COPII associated small GTPase; COPII-associated small GTPase; GTP binding protein SAR1a; GTP-binding protein SAR1a; Masra 2; Masra2; SAR 1; SAR1 gene homolog A; SARA 1; Sara; SARA1
The SAR1A protein critically facilitates intracellular transport from the endoplasmic reticulum to the Golgi apparatus. Through SAR1A-GTP-dependent assembly, it organizes endoplasmic reticulum exit sites (ERES), forming a scaffold that defines these sites. SAR1A Protein, Human (GST) is the recombinant human-derived SAR1A protein, expressed by E. coli , with N-GST labeled tag. The total length of SAR1A Protein, Human (GST) is 198 a.a., with molecular weight of ~49.4 kDa.
RAB11B protein is an important small GTPase in the Rab family, coordinating intracellular membrane transport by regulating vesicle processes. It cycles between GDP and GTP forms, recruiting effectors to control activities such as vesicle formation and movement. RAB11B Protein, Human (HEK293, His) is the recombinant human-derived RAB11B protein, expressed by HEK293 , with N-His labeled tag. The total length of RAB11B Protein, Human (HEK293, His) is 214 a.a., with molecular weight of ~25-30 kDa.
The AK3L1 protein actively maintains cellular nucleotide homeostasis by catalyzing the interconversion of nucleoside phosphates. This multifunctional enzyme efficiently phosphorylates AMP and dAMP using ATP as a phosphate donor, and selectively phosphorylates AMP when utilizing GTP. AK3L1 Protein, Human (sf9) is the recombinant human-derived AK3L1 protein, expressed by Sf9 insect cells , with tag free. The total length of AK3L1 Protein, Human (sf9) is 222 a.a., with molecular weight of ~27 kDa.
The SPG3A/ATL1 protein is a GTPase that promotes membrane tethering by forming trans homomers, thereby achieving homotypic fusion of the endoplasmic reticulum (ER) membrane. It makes a crucial contribution to the biogenesis of the endoplasmic reticulum tubular network and shaping the structural organization of cells. SPG3A/ATL1 Protein, Human (sf9, GST) is the recombinant human-derived SPG3A/ATL1 protein, expressed by Sf9 insect cells , with N-GST labeled tag. The total length of SPG3A/ATL1 Protein, Human (sf9, GST) is 447 a.a., with molecular weight of ~66 kDa.
The AK3L1 protein actively maintains cellular nucleotide homeostasis by catalyzing the interconversion of nucleoside phosphates. This multifunctional enzyme efficiently phosphorylates AMP and dAMP using ATP as a phosphate donor, and selectively phosphorylates AMP when utilizing GTP. AK3L1 Protein, Human (sf9, His-GST) is the recombinant human-derived AK3L1 protein, expressed by Sf9 insect cells , with N-His, N-GST labeled tag. The total length of AK3L1 Protein, Human (sf9, His-GST) is 222 a.a., with molecular weight of ~46 kDa.
The PCK2 protein serves as a key enzyme in cellular metabolism by catalyzing the conversion of oxaloacetate (OAA) to phosphoenolpyruvate (PEP), representing the rate-limiting step in the metabolic pathway responsible for generating glucose from lactate and other precursors derived from the citric acid cycle. This enzymatic activity plays a critical role in gluconeogenesis, a fundamental process that contributes to the maintenance of glucose homeostasis in the body. Through the transformation of OAA to PEP, PCK2 facilitates the synthesis of glucose, a vital energy source, and orchestrates a crucial step in the intricate interplay of metabolic pathways involved in cellular energy balance and glucose production. PCK2 Protein, Human (sf9, His-GST) is the recombinant human-derived PCK2 protein, expressed by Sf9 insect cells , with C-His, N-GST labeled tag. The total length of PCK2 Protein, Human (sf9, His-GST) is 608 a.a., with molecular weight of ~94.9 kDa.
CDC42 is a plasma membrane-associated small GTPase that regulates cellular responses by cycling between an active GTP-bound state and an inactive GDP-bound state. It participates in epithelial cell polarization, regulates the attachment of spindle microtubules to kinetochores, affects cell migration, and plays a key role in the formation of filopodia. CDC42 Protein, Human (GST) is the recombinant human-derived CDC42 protein, expressed by E. coli , with N-GST labeled tag. The total length of CDC42 Protein, Human (GST) is 188 a.a., with molecular weight of ~44 kDa.
Guanosine triphosphate- 13C (GTP- 13C) dilithium is 13C-labeled Guanosine triphosphate (HY-113225). Guanosine triphosphate is a native nucleotide. The derivatives of GTP may be used as specific inhibitors against COVID-19.
Guanosine triphosphate-d14(GTP-d14) dilithium is deuterium labeled Guanosine triphosphate (HY-113225). Guanosine triphosphate is a native nucleotide. The derivatives of GTP may be used as specific inhibitors against COVID-19.
Guanosine triphosphate- 15N5 (GTP- 15N5) dilithium is 15N labeled Guanosine triphosphate (HY-113225). Guanosine triphosphate is a native nucleotide. The derivatives of GTP may be used as specific inhibitors against COVID-19.
Guanosine triphosphate- 13C10 (GTP- 13C10) dilithium is 13C-labeled Guanosine triphosphate (HY-113225). Guanosine triphosphate is a native nucleotide. The derivatives of GTP may be used as specific inhibitors against COVID-19.
Guanosine triphosphate- 15N5,d14 (GTP- 15N5,d14) dilithium is deuterium and 15N labeled Guanosine triphosphate (HY-113225). Guanosine triphosphate is a native nucleotide. The derivatives of GTP may be used as specific inhibitors against COVID-19.
Guanosine triphosphate- 13C10, 15N5 (tetraammonium) is the 13C and 15N labeled Guanosine triphosphate tetraammonium[1]. Guanosine triphosphate is a native nucleotide. The derivatives of GTP may be used as specific inhibitors against COVID-19[2].
dGTP- 13C10 (2'-Deoxyguanosine-5'-triphosphate- 13C10) dilithium is 13C-labeled dGTP (HY-138616). dGTP (2'-Deoxyguanosine-5'-triphosphate), a guanosine nucleotide, can be used in deoxyribonucleic acid synthesis. Guanosine nucleotides (GDP, GTP, dGDP, and dGTP) are highly susceptible to oxidative damage to 8-oxo-GDP (8-O-GDP), 8-O-dGTP, 8-O-GTP, and 8-O-dGTP.
dGTP- 15N5 (2'-Deoxyguanosine-5'-triphosphate- 15N5) dilithium is 15N labeled dGTP (HY-138616). dGTP (2'-Deoxyguanosine-5'-triphosphate), a guanosine nucleotide, can be used in deoxyribonucleic acid synthesis. Guanosine nucleotides (GDP, GTP, dGDP, and dGTP) are highly susceptible to oxidative damage to 8-oxo-GDP (8-O-GDP), 8-O-dGTP, 8-O-GTP, and 8-O-dGTP.
dGTP-d14 (2'-Deoxyguanosine-5'-triphosphate-d14) dilithium is deuterium labeled dGTP (HY-138616). dGTP (2'-Deoxyguanosine-5'-triphosphate), a guanosine nucleotide, can be used in deoxyribonucleic acid synthesis. Guanosine nucleotides (GDP, GTP, dGDP, and dGTP) are highly susceptible to oxidative damage to 8-oxo-GDP (8-O-GDP), 8-O-dGTP, 8-O-GTP, and 8-O-dGTP.
dGTP- 13C10, 15N5 (2'-Deoxyguanosine-5'-triphosphate- 13C10, 15N5) dilithium is 13C and 15N-labeled dGTP (HY-138616). dGTP (2'-Deoxyguanosine-5'-triphosphate), a guanosine nucleotide, can be used in deoxyribonucleic acid synthesis. Guanosine nucleotides (GDP, GTP, dGDP, and dGTP) are highly susceptible to oxidative damage to 8-oxo-GDP (8-O-GDP), 8-O-dGTP, 8-O-GTP, and 8-O-dGTP.
dGTP- 15N5,d14 (2'-Deoxyguanosine-5'-triphosphate- 15N5,d14) dilithium is deuterium and 15N labeled dGTP (HY-138616). dGTP (2'-Deoxyguanosine-5'-triphosphate), a guanosine nucleotide, can be used in deoxyribonucleic acid synthesis. Guanosine nucleotides (GDP, GTP, dGDP, and dGTP) are highly susceptible to oxidative damage to 8-oxo-GDP (8-O-GDP), 8-O-dGTP, 8-O-GTP, and 8-O-dGTP.
2-Ketoglutaric acid- 13C5 is the 13C labeled 2-Ketoglutaric acid[1]. 2-Ketoglutaric acid (Alpha-Ketoglutaric acid) is an intermediate in the production of ATP or GTP in the Krebs cycle. 2-Ketoglutaric acid also acts as the major carbon skeleton for nitrogen-assimilatory reactions. 2-Ketoglutaric acid is a reversible inhibitor of tyrosinase (IC50=15 mM)[2].
2-Ketoglutaric acid-d4 is the deuterium labeled 2-Ketoglutaric acid[1]. 2-Ketoglutaric acid (Alpha-Ketoglutaric acid) is an intermediate in the production of ATP or GTP in the Krebs cycle. 2-Ketoglutaric acid also acts as the major carbon skeleton for nitrogen-assimilatory reactions. 2-Ketoglutaric acid is a reversible inhibitor of tyrosinase (IC50=15 mM)[2].
2-Ketoglutaric acid-d6 is the deuterium labeled 2-Ketoglutaric acid[1]. 2-Ketoglutaric acid (Alpha-Ketoglutaric acid) is an intermediate in the production of ATP or GTP in the Krebs cycle. 2-Ketoglutaric acid also acts as the major carbon skeleton for nitrogen-assimilatory reactions. 2-Ketoglutaric acid is a reversible inhibitor of tyrosinase (IC50=15 mM)[2].
2'-Deoxyguanosine 5'-monophosphate- 13C10, 15N5 (disodium) is the 13C and 15N labeled 2'-Deoxyguanosine 5'-monophosphate disodium[1]. 2'-Deoxyguanosine 5'-monophosphate disodium (5′-dGMP disodium) is a mononucleotide having guanine as the nucleobase. 2'-Deoxyguanosine 5'-monophosphate disodium is a nucleic acid guanosine triphosphate (GTP) derivative[2].
2-Ketoglutaric acid- 13C (Alpha-Ketoglutaric acid- 13C) is a 13C labeled 2-Ketoglutaric acid (HY-W013636) . 2-Ketoglutaric acid (Alpha-Ketoglutaric acid) is an intermediate in the production of ATP or GTP in the Krebs cycle. 2-Ketoglutaric acid also acts as the major carbon skeleton for nitrogen-assimilatory reactions. 2-Ketoglutaric acid is a reversible inhibitor of tyrosinase (IC50=15 mM) .
RAN; ARA24; OK/SW-cl.81; GTP-binding nuclear protein Ran; Androgen receptor-associated protein 24; GTPase Ran; Ras-like protein TC4; Ras-related nuclear protein
MRTX1133 is a noncovalent, potent, and selective KRAS G12D inhibitor. MRTX1133 optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated KD against KRAS G12D of 0.2 pM. MRTX1133 prevents SOS1-catalyzed nucleotide exchange and/or formation of the KRAS G12D/GTP/RAF1 complex, thereby inhibiting mutant KRAS-dependent signal transduction. MRTX1133 selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tumor cells. MRTX1133 has single digit nanomolar activity in cellular assays and marked in vivo efficacy in tumor models harboring KRAS G12D mutations .
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