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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
54 Results for "
GTP activation
" in MedChemExpress (MCE) Product Catalog:
Products (54)
54 Results for "GTP activation" in MCE Product Catalog:
12
12 Publications Verification
Synonyms: NAV-2729
Grassofermata is a dual Arf1/Arf6 activation inhibitor. ADP ribosylation factors (Arfs) are members of the Arf family of GTP-binding proteins of the Ras superfamily.
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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 .
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2 Cited Publications
Cat. No.: HY-N2438
CAS No.: 74805-91-7
Category:
Ophiopogon japonicus (L. f.) Ker-Gawl. Flavonoids Other Diseases Phenols Polyphenols Plants Liliaceae Extract Disease Research Fields Other Flavonoids
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1 Cited Publications
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Nexinhib20 is an inhibitor that targets the interactions of Rab27a-JFC1 (IC50: 2.6 μM) and Rac-1-GTP. Nexinhib20 can inhibit neutrophil exocytosis, adhesion, and β2 integrin activation, and has anti-inflammatory activity. Nexinhib20 can be used in the research of diseases such as systemic inflammation and myocardial ischemia-reperfusion injury .
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1-Oleoyl-sn-glycero-3-phosphocholine (18:1 Lyso PC), a lysophospholipid, is a GPR82 inhibitor. 1-Oleoyl-sn-glycero-3-phosphocholine abrogates constitutive Gi-coupled GPR82 activity, shifts active/inactive equilibrium to inactive, suppresses Gi protein activation, increases cAMP production, and decreases GTPγS binding to Gαi proteins. 1-Oleoyl-sn-glycero-3-phosphocholine contributes to adipocyte lipolysis regulation.1-Oleoyl-sn-glycero-3-phosphocholine exhibits reduced serum levels in mouse models of steatohepatitis, linked to hepatic Lpcat 1-4 up-regulation .
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1 Cited Publications
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 .
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1 Cited Publications
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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 .
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1 Cited Publications
Cat. No.: HY-W040055
CAS No.: 2009-64-5
Synonyms: D-(+)-Neopterin; D-erythro-Neopterin
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1 Cited Publications
Synonyms: SR57746A; SR57746 hydrochloride
Target:
5-HT Receptor Dopamine Receptor Trk Receptor PKC ERK Akt JNK
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Xaliproden (SR57746) hydrochloride (SR57746A) is an orally active, highly selective 5-HT1A receptor agonist. Xaliproden hydrochloride activates pertussis toxin-sensitive G protein-coupled signaling cascades, as well as the PKC, ERK1/ERK2, Akt and p21 Ras/MEK-1 pathways. Xaliproden hydrochloride also downregulates the JNK/p66/c-Jun signaling pathway, induces phosphorylation of the shc adaptor protein, regulates extracellular dopamine and 5-HT levels, and induces [ 35S]GTPγS labeling in rat brain structures rich in 5-HT1A receptors. Xaliproden hydrochloride exerts neurotrophic, neuroprotective, renoprotective, anti-inflammatory, anti-apoptotic, anti-fibrotic and analgesic effects. Xaliproden hydrochloride also enhances NGF-induced neurite outgrowth, promotes motor neuron survival, attenuates renal tubular injury and inhibits chemotherapy-induced mechanical allodynia, without activating or altering NGF-induced TrkA receptor activation. Xaliproden hydrochloride can be used in the research of motor neuron disease, diabetic nephropathy, chemotherapy-induced peripheral neuropathy, amyotrophic lateral sclerosis, Alzheimer's disease, acute tonic nociceptive pain, inflammatory pain, depression and anxiety .
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1 Cited Publications
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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 .
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1 Cited Publications
Cat. No.: HY-P10495A
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1 Cited Publications
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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 .
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1 Cited Publications
Cat. No.: HY-P1376A
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Cat. No.: HY-159852
CAS No.: 2971769-60-3
BBO-10203 is a potent inhibitor of PI3Kα and KRAS G12C, selectively and covalently binding to Cys242 in the RAS-Binding Domain of PI3Kα, and inhibiting both the GTP-bound and GDP-bound states of KRAS G12C with an IC50 of 0.031 nM and an EC50 of 0.02 nM. BBO-10203 disrupts the interaction between RAS isoforms and PI3Kα, leading to the inhibition of RAS-mediated PI3Kα activation, and reduces pERK expression, cell growth, and induces G1 arrest and apoptosis. BBO-10203 can be used for the research of breast cancer, colorectal cancer, and non-small cell lung cancer .
Synonyms: Guanosine 5'-[γ-thio]triphosphate tetralithium
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GTPγS (Guanosine 5'-[γ-thio]triphosphate) 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 .
Synonyms: Gpp(NH)p lithium
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Guanylyl imidodiphosphate lithium (Gpp (NH) p lithium) is a non-hydrolyzable GTP analog. Guanylyl imidodiphosphate lithium increases adenylate cyclase activity. Guanylyl imidodiphosphate lithium binds to and irreversibly activates G proteins .
Cat. No.: HY-100767
CAS No.: 148892-91-5
Synonyms: Guanosine 5'-[β,γ-imido]triphosphate trisodium
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 .
RMC-4998 is an orally active inhibitor targeting the active or GTP-bound state of the KRAS G12C mutant. RMC-4998 can form a ternary complex with intracellular CYPA and the activated KRAS G12C mutant, with an IC50 value of 28 nM. RMC-4998 can inhibit ERK signaling in KRAS G12C mutant cancer cells and induce apoptosis. RMC-4998 can be used for tumor research .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
