Search Result
Results for "
GTP/GDP
" in MedChemExpress (MCE) Product Catalog:
7
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-173632
-
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Ras
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Cancer
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AMG410 is a non-covalent and selective pan-KRAS inhibitor with IC50 values of 1-4 nM for KRAS G12D, KRAS G12V, and KRAS G13D. AMG410 shows greater than 100-fold selectivity against both HRAS and NRAS. AMG410 is a dual GTP(on)- and GDP(off)-state inhibitor (Kd(GDP-state) of 1 nM; Kd(GTP-state) of 22 nM). AMG410 blocks KRAS signaling in a cycling state-independent manner and also blocks proliferation in wildtype KRAS-amplified tumor cells. AMG410 can be used for the study of colorectal, pancreatic, and lung cancers .
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- HY-145928
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Divarasib
Maximum Cited Publications
6 Publications Verification
GDC-6036
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Ras
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Cancer
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Divarasib (GDC-6036) is an orally active, selective KRAS G12C inhibitor with an IC50 of <0.01 μM. Divarasib covalently binds Cys12 in GDP-bound KRAS G12C, occupies the switch II pocket, blocks GTP binding and SOS-mediated reactivation, and inhibits oncogenic KRAS signaling. Divarasib induces tumor shrinkage and robust tumor growth inhibition in KRAS G12C-positive models and cancer cells. Divarasib can be used for the research of non-small cell lung cancer, colorectal adenocarcinoma, pancreatic ductal adenocarcinoma, and other KRAS G12C-mutated solid tumors .
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- HY-159852
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PI3K
Ras
Akt
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Cancer
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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 .
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- HY-138188
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KRA-533
1 Publications Verification
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Ras
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Cancer
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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.
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- HY-13963
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ZCL278
3 Publications Verification
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Ras
Dengue Virus
VSV
Arenavirus
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Infection
Neurological Disease
Metabolic Disease
Cancer
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ZCL278 is a selective Cdc42 inhibitor with Kds of 6.4 μM in fluorescence titration and 11.4 μM in surface plasmon resonance (SPR) measurement. ZCL278 is able to disrupt the Cdc42-ITSN interaction as well as GTP/GDP binding. ZCL278 has inhibitory effects on various enveloped viruses, but is ineffective against non-enveloped viruses. ZCL278 can be used for the studies of arsenic neurotoxicity and HER2-positive gastric cancer (GC) .
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- HY-136379
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Cdc42-IN-1
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Ras
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Cancer
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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 .
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- HY-N7389A
-
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Endogenous Metabolite
Drug Intermediate
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Metabolic Disease
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GDP-D-mannose disodium consists of GDP-α-D-mannose (HY-N7389B) and GDP-β-D-mannose. GDP-α-D-mannose serves as a donor substrate for mannosyltransferases and acts as a precursor of GDP-β-L-fucose. GDP-α-D-mannose exerts competitive inhibition on GTP (with a Ki value of 14.7 μM) and non-competitive inhibition on mannose-1-P (with a Ki value of 115 μM). GDP-D-mannose disodium is metabolized to GDP-L-fucose (HY-134433) via GMDS (Gmd) and TSTA3 (WcaG) .
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- HY-134885
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RM-023
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SHP2
SOS1
Ras
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Cancer
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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 .
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- HY-18674
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Ras
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Cancer
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K-Ras-IN-1 is the inhibitor for K-Ras by occupying the binding site of son of sevenless (Sos), preventing the interaction between Sos and K-Ras, inhibiting the Sos-catalyzed GDP to GTP exchange process. K-Ras-IN-1 is promising for research of pancreatic, colon and lung cancer .
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- HY-P5979
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LRRK2
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Neurological Disease
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LRRKtide is a polypeptide substrate. LRRKtide is a specific phosphorylation substrate of LRRK2, a kinase associated with Parkinson's disease, and its phosphorylation site is a threonine residue. LRRKtide can be used for characterization of the catalytic properties of LRRK2, as well as studies on kinase activity and inhibition. LRRKtide is applicable to research related to Parkinson's disease .
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- HY-176785S
-
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Ras
Apoptosis
p38 MAPK
Caspase
TNF Receptor
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Cancer
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MCB-294 is a dual-state pan-KRAS inhibitor that selectively inhibits KRAS over NRAS and HRAS. MCB-294 capable of binding both the active (GTP-bound) and inactive (GDP-bound) forms of KRAS with Kds of approximately 1 pM and 10 nM, respectively. MCB-294 broadly impairs the growth of hTERT-HPNE cells expressing G12D, G12C, G12V, G12S, G13D, and wild-type KRAS, with IC50s of approximately 700 nM. MCB-294 induces irreversible apoptosis in KRAS-mutated tumors. MCB-294 effectively suppress KRAS G12C inhibitor-resistant cancer cells and remodel the tumor immune microenvironment. MCB-294 can be used for the study of pancreatic cancer, colorectal cancer and lung cancer .
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- HY-N0097R
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DL-Guanosine (Standard); Vernine (Standard)
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Reference Standards
HSV
Endogenous Metabolite
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Infection
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Guanosine (Standard) is the analytical standard of Guanosine. This product is intended for research and analytical applications. Guanosine (DL-Guanosine) is a purine nucleoside comprising guanine attached to a ribose (ribofuranose) ring via a β-N9-glycosidic bond. Guanosine possesses anti-HSV activity.
In Vitro: Guanosine can be phosphorylated to become guanosine monophosphate (GMP), cyclic guanosine monophosphate (cGMP), guanosine diphosphate (GDP), and guanosine triphosphate (GTP). These forms play important roles in various biochemical processes such as synthesis of nucleic acids and proteins, photosynthesis, muscle contraction, and intracellular signal transduction (cGMP).
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- HY-138616S3
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2'-Deoxyguanosine-5'-triphosphate-13C10 dilithium
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Isotope-Labeled Compounds
DNA/RNA Synthesis
Nucleoside Antimetabolite/Analog
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Infection
Cancer
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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.
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- HY-145928B
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GDC-6036 adipate
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Ras
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Cancer
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Divarasib (GDC-6036) adipate is an orally active, selective KRASG12C inhibitor with an IC50 of <0.01 μM. Divarasib adipate covalently binds Cys12 in GDP-bound KRASG12C, occupies the switch II pocket, blocks GTP binding and SOS-mediated reactivation, and inhibits oncogenic KRAS signaling. Divarasib adipate induces tumor shrinkage and robust tumor growth inhibition in KRASG12C-positive models and cancer cells. Divarasib adipate can be used for the research of non-small cell lung cancer, colorectal adenocarcinoma, pancreatic ductal adenocarcinoma, and other KRASG12C-mutated solid tumors .
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- HY-138616S4
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2'-Deoxyguanosine-5'-triphosphate-13C10,15N5 dilithium
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Isotope-Labeled Compounds
DNA/RNA Synthesis
Nucleoside Antimetabolite/Analog
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Infection
Cancer
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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.
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- HY-135865
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Ras
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Cancer
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KRAS inhibitor-7 is a potent KRAS G12C inhibitor, extracted from patent WO2017087528A1, compound B .
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- HY-176170
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SOS1
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Cancer
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SOS1-IN-19 (Compound 10i) is a potent inhibitor of SOS1 (Son of Sevenless 1) with an IC50 value of 165.2 nM. SOS1-IN-19 blocks KRAS activation by preventing GDP/GTP exchange in KRAS signaling pathway. SOS1-IN-19 is promising for research of KRAS-driven cancers (e.g., NSCLC and colorectal cancer) .
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- HY-N7389B
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Endogenous Metabolite
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Metabolic Disease
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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) .
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- HY-P5072
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Bombesin Receptor
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Metabolic Disease
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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 .
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- HY-135864
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Ras
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Cancer
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KRAS inhibitor-6 is a potent KRAS G12C inhibitor, extracted from patent WO2017087528A1, compound A .
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- HY-18165
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LPL Receptor
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Cancer
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XL541 is a potent, selective S1P1 antagonist. XL541 inhibits GDP-GTP exchange. XL541 causes frank surface hemorrhaging of tumors. XL541 collaborates with Paclitaxel (HY-B0015) to exhibit antitumor activity against breast cancer and lung cancer .
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- HY-13868
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Ras
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Cancer
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SCH-53870 is a Ras activation inhibitor that binds to the Ras-GDP complex, keeping the Ras protein in an inactive GDP-bound state and preventing it from switching to an active GTP-bound state. SCH-53870 affects cell signaling and cell proliferation by preventing the activation of Ras protein. SCH-53870 can be used in cancer research .
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- HY-175529
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Ras
ERK
Apoptosis
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Cancer
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KRASG12D-IN-7 is a selective KRAS G12D inhibitor. KRASG12D-IN-7 displays strong binding activity for KRAS G12D in both its GDP- and GTP- bound states, with Kd value of 1.12 nM and 1.86 nM, respectively. KRASG12D-IN-7 inhibits the proliferation of KRAS G12D harboring AsPC-1 cells with an IC50 value of 10 nM and suppresses MAPK signaling. KRASG12D-IN-7 induces G0/G1 phase arrest and apoptosis in AsPC-1 cells, and strongly inhibits their colony formation. KRASG12D-IN-7 can be used for the study of cancers harboring KRAS G12D mutation, particularly pancreatic ductal adenocarcinoma (PDAC) .
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- HY-137615
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- HY-E70031
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GDP-MP; GDPMP; GMPase
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Endogenous Metabolite
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Others
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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 .
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- HY-137618
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- HY-138616S1
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2'-Deoxyguanosine-5'-triphosphate-d14 dilithium
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Isotope-Labeled Compounds
DNA/RNA Synthesis
Nucleoside Antimetabolite/Analog
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Infection
Cancer
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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.
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- HY-138616S
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2'-Deoxyguanosine-5'-triphosphate-15N5 dilithium
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Isotope-Labeled Compounds
DNA/RNA Synthesis
Nucleoside Antimetabolite/Analog
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Infection
Cancer
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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.
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- HY-138616S2
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2'-Deoxyguanosine-5'-triphosphate-15N5,d14 dilithium
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Isotope-Labeled Compounds
DNA/RNA Synthesis
Nucleoside Antimetabolite/Analog
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Infection
Cancer
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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.
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- HY-135866
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Ras
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Cancer
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KRAS inhibitor-8 is a potent KRAS G12C inhibitor, extracted from patent WO2017087528A1, compound C .
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- HY-145022
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Ras
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Cancer
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KRAS G12C inhibitor 25 is a KRAS G12C inhibitor. KRAS G12C inhibitor 25 inhibits SOSl-assisted GDP/GTP exchanging activity of KRAS-G12C mutant (IC50=0.48 nM). From WO2021216770A1 compound 3 .
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- HY-173047
-
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Ras
ERK
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Cancer
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KRASG12C IN-15 (Compound 21) is the orally active inhibitor for KRAS G12C, and inhibits SOS1-mediated GDP/GTP exchange with an IC50 of 19 nM. KRASG12C IN-15 inhibits the phosphorylation of ERK with IC50 of 0.051 μM. KRASG12C IN-15 inhibits the cell viability of KRAS G12C mutated MIA PaCa-2 with IC50 of 0.023 μM. KRASG12C IN-15 exhibits antitumor effect in MIA PaCa-2 xenograft mouse models .
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- HY-175326
-
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SOS1
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Cancer
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SOS1-IN-21 is an orally active inhibitor of son of Sevenless 1 (SOS1) with an IC50 of 15 nM. SOS1 is a guanine nucleotide exchange factor (GEF) that activates KRAS by facilitating the exchange of GDP for GTP. SOS1-IN-21 exhibits potent antiproliferative activity, with IC50 values of 16 nM in NCI-H358 and 17 nM in Mia Paca-2 cell proliferation assays. SOS1-IN-21 exhibits significant antitumor activity in the Mia Paca-2 xenograft model. SOS1-IN-21 can be used for the study of KRAS mutant tumors, such as pancreatic cancer .
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- HY-137615A
-
-
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- HY-173632A
-
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Ras
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Cancer
|
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AMG410 diTFA is a non-covalent and selective pan-KRAS inhibitor with IC50 values of 1-4 nM for KRAS G12D, KRAS G12V, and KRAS G13D. AMG410 diTFA shows greater than 100-fold selectivity against both HRAS and NRAS. AMG410 diTFA is a dual GTP(on)- and GDP(off)-state inhibitor (Kd(GDP-state) of 1 nM; Kd(GTP-state) of 22 nM). AMG410 diTFA blocks KRAS signaling in a cycling state-independent manner and also blocks proliferation in wildtype KRAS-amplified tumor cells. AMG410 diTFA can be used for the study of colorectal, pancreatic, and lung cancers .
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- HY-W686762
-
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Dopamine Receptor
Adenylate Cyclase
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Neurological Disease
|
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m,p-Dimethyl PPE is a D4 dopamine receptor ligand. m,p-Dimethyl PPE promotes GDP/GTP exchange of the G protein α-subunit, dissociates the receptor-G protein complex, stabilizes the low-affinity receptor state, and inhibits adenylate cyclase activity. m,p-Dimethyl PPE inhibits Forskolin (HY-15371)-induced melatonin synthesis in retinal photoreceptor cells and reduces the efficacy of full agonists when used in combination. m,p-Dimethyl PPE can be used in studies related to attention-deficit hyperactivity disorder .
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- HY-134505
-
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Ras
Phospholipase
ERK
Akt
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Cancer
|
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Avicin G is a sphingomyelinase inhibitor and plasma membrane disruptor. Avicin G inhibits the enzymatic activities of neutral sphingomyelinases (SMPD2/3) and acid sphingomyelinase (SMPD1), elevates intracellular sphingomyelin levels, and alters the distribution of sphingomyelin. Avicin G interferes with the lateral segregation of GTP- and GDP-bound H-Ras, inhibits the signal output of oncogenic K-Ras and H-Ras, reduces the phosphorylation of ERK and Akt, increases lysosomal pH, and inhibits the endocytic recycling of epidermal growth factor receptor. Avicin G can be used in research related to pancreatic ductal adenocarcinoma and non-small cell lung cancer .
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- HY-13963S
-
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Isotope-Labeled Compounds
Endogenous Metabolite
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Infection
Cancer
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ZCL278- 13C is a 13C-labeled version of ZCL278 (HY-13963). ZCL278 is a selective Cdc42 inhibitor with Kds of 6.4 μM in fluorescence titration and 11.4 μM in surface plasmon resonance (SPR) measurement. ZCL278 can disrupt the interaction between Cdc42 and ITSN, and also inhibit the binding of GTP and GDP. ZCL278 has inhibitory effects on various enveloped viruses, but is ineffective against non-enveloped viruses. ZCL278 can be used in the research of arsenic neurotoxicity and HER2-positive gastric cancer (GC) [1][2][3][4].
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- HY-181964
-
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Cancer
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KRAS G12C-IN-77 is an orally active and selective KRAS G12C covalent dual-state inhibitor that binds with high affinity to both GDP-bound (inactive state) and GTP-bound (active state) KRAS G12C (IC50 = 133 nM). KRAS G12C-IN-77 rapidly inhibits ERK1/2 phosphorylation, induces the formation of covalent adducts with endogenous KRAS G12C, suppresses the expression of MAPK pathway genes, and inhibits the proliferation of KRAS G12C-mutant cells. KRAS G12C-IN-77 is applicable to research related to KRAS G12C-mutant solid tumors, including pancreatic ductal adenocarcinoma and non-small cell lung cancer .
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| Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P5979
-
|
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LRRK2
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Neurological Disease
|
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LRRKtide is a polypeptide substrate. LRRKtide is a specific phosphorylation substrate of LRRK2, a kinase associated with Parkinson's disease, and its phosphorylation site is a threonine residue. LRRKtide can be used for characterization of the catalytic properties of LRRK2, as well as studies on kinase activity and inhibition. LRRKtide is applicable to research related to Parkinson's disease .
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- HY-P5072
-
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Bombesin Receptor
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Metabolic Disease
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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 .
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| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
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- HY-176785S
-
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MCB-294 is a dual-state pan-KRAS inhibitor that selectively inhibits KRAS over NRAS and HRAS. MCB-294 capable of binding both the active (GTP-bound) and inactive (GDP-bound) forms of KRAS with Kds of approximately 1 pM and 10 nM, respectively. MCB-294 broadly impairs the growth of hTERT-HPNE cells expressing G12D, G12C, G12V, G12S, G13D, and wild-type KRAS, with IC50s of approximately 700 nM. MCB-294 induces irreversible apoptosis in KRAS-mutated tumors. MCB-294 effectively suppress KRAS G12C inhibitor-resistant cancer cells and remodel the tumor immune microenvironment. MCB-294 can be used for the study of pancreatic cancer, colorectal cancer and lung cancer .
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- HY-138616S3
-
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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.
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- HY-138616S4
-
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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.
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- HY-138616S1
-
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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.
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- HY-138616S
-
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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.
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- HY-138616S2
-
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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.
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- HY-13963S
-
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ZCL278- 13C is a 13C-labeled version of ZCL278 (HY-13963). ZCL278 is a selective Cdc42 inhibitor with Kds of 6.4 μM in fluorescence titration and 11.4 μM in surface plasmon resonance (SPR) measurement. ZCL278 can disrupt the interaction between Cdc42 and ITSN, and also inhibit the binding of GTP and GDP. ZCL278 has inhibitory effects on various enveloped viruses, but is ineffective against non-enveloped viruses. ZCL278 can be used in the research of arsenic neurotoxicity and HER2-positive gastric cancer (GC) [1][2][3][4].
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| Cat. No. |
Product Name |
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Classification |
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- HY-176785S
-
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Alkynes
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MCB-294 is a dual-state pan-KRAS inhibitor that selectively inhibits KRAS over NRAS and HRAS. MCB-294 capable of binding both the active (GTP-bound) and inactive (GDP-bound) forms of KRAS with Kds of approximately 1 pM and 10 nM, respectively. MCB-294 broadly impairs the growth of hTERT-HPNE cells expressing G12D, G12C, G12V, G12S, G13D, and wild-type KRAS, with IC50s of approximately 700 nM. MCB-294 induces irreversible apoptosis in KRAS-mutated tumors. MCB-294 effectively suppress KRAS G12C inhibitor-resistant cancer cells and remodel the tumor immune microenvironment. MCB-294 can be used for the study of pancreatic cancer, colorectal cancer and lung cancer .
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