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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
41 Results for "
GTPase activity
" in MedChemExpress (MCE) Product Catalog:
Products (41)
41 Results for "GTPase activity" in MCE Product Catalog:
23
Category:
Alkaloids Narcissus tazetta Linn. var. chinensis M.Roemer Amaryllidaceae Extract Plants Disease Research Fields Isoquinoline Alkaloids Cancer Agricultural Research
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8
8 Cited Publications
EHop-016 is a potent and selective Rac GTPase Rac1 and Rac3 inhibitor. EHop-016 inhibits Rac1 activity with an IC50 of 1.1 μM in MDA-MB-435 cells. EHop-016 inhibits Vav2 interaction with Rac, Rac-activated PAK1, lamellipodia formation, and cell migration .
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UCM05 (G28UCM) is a fatty acid synthase (FASN) and filamentous temperature-sensitive protein Z (Ftsz) inhibitor. UCM05 inhibits fatty acid synthesis, viral replication, and Gram-positive bacterial growth. UCM05 binds to FtsZ GTP-binding sites, inhibits GTPase activity, and disrupts Z-ring localization. UCM05 can be used for the research of HSV-1/2 infection, HIV-1 infection, and Gram-positive bacterial infections[1][2][3].
1
1 Cited Publications
Dynole 34-2 is a potent dynamin GTPase inhibitor (IC50s=6.9 and 14.2 µM for dynamin1 and dynamin2 GTPase activity, respectively) with antimitotic effect. Dynole 34-2 induces apoptosis, as revealed by cell blebbing, DNA fragmentation, and PARP cleavage. Dynole 34-2 also potently inhibits receptor mediated endocytosis (RME) .
BQU57 is a selective inhibitor of RalA/RalB small GTPases, with a binding potency (Kb) of 7.7 μM for RalB-GDP. BQU57 can block its interaction with effector proteins (such as SEC5 and EXO84), inhibiting tumor cell migration, invasion and non-adherent growth. BQU57 downregulates the NF-κB signaling pathway, reduces the expression of IL-6, IL-8 and MMP-13, and inhibits apoptosis by regulating the Bcl-2/Bax balance. BQU57 also protects the extracellular matrix by inhibiting the Ral/NF-κB pathway and can be used for the study of degenerative diseases. BQU57 exhibits significant antitumor activity in triple-negative breast cancer (TNBC) models, inhibiting orthotopic tumor growth and lung metastasis and enhancing paclitaxel chemotherapy sensitivity .
Cat. No.: HY-P1732
CAS No.: 203716-10-3
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Cat. No.: HY-173350
CAS No.: 2301869-11-2
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Ran-IN-1 is a specific inhibitor of Ran GTPase. Ran-IN-1 selectively induces cytotoxicity and apoptosis in aneuploid ovarian cancer cells and also inhibits DNA repair. Ran-IN-1 exhibits antitumor activity and is useful for research on tumors such as epithelial ovarian cancer .
Cat. No.: HY-161119
CAS No.: 73326-98-4
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Drpitor1a is an orally active DRP1 GTPase inhibitor. Drpitor1a blocks mitochondrial fission, inhibits DRP1 GTPase activity, and reduces ROS levels. Drpitor1a induces mitochondrial fusion and mitochondria-dependent apoptosis by elevating Bak and Smac/Diablo and inhibiting Bcl-2. Drpitor1a inhibits proliferation in pulmonary arterial hypertension hPASMC and induces necrosis and autophagy mediators. Drpitor1a causes regression of non-small cell lung cancer tumors in mouse xenograft models and exhibits higher accumulation and efficacy in females. Drpitor1a can be used in research related to non-small cell lung cancer, myocardial ischemia-reperfusion injury, and pulmonary arterial hypertension .
Synonyms: ZINC08010136
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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) .
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Clathrin-IN-4 (compound 8b), a Wiskostatin?(HY-12534) analogue, is a potent inhibitor of clathrin mediated endocytosis with an IC50 of 2.1 μM. Clathrin-IN-4 is a dynamin I GTPase activity inhibitor with an IC50 of 9.1 μM .
Cat. No.: HY-129189
CAS No.: 2252242-32-1
RAS GTPase inhibitor 1 (example 51) is a RAS GTPase inhibitor with anti-tumor activity, extracted from patent WO2018212774A1. RAS GTPase inhibitor 1 (example 51) exhibits an EC50 less than 1 μM for at least one nucleotide exchange and an IC50 less than 1 μM in H727 cells .
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Bragsin1 is a potent, selective and noncompetitive inhibitor of the ArfGEF BRAG2, inhibits Arf GTPase activation, with an IC50 of 3 μM. Bragsin1 binds to PH domain of BRAG2, and is a noncompetitive interfacial inhibitor. Bragsin1 has no effect on the Sec7 domain of human ArfGEFs. Anti-cancer activity .
Cat. No.: HY-175763
CAS No.: 865271-09-6
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Z55660043 is a Regulator of G protein signaling-14 (RGS14) inhibitor with an IC50 of 2.3 μM. Z55660043 selectively and non-covalently inhibits RGS14 GTPase-accelerating protein (GAP) activity without measurable cytotoxicity. Z55660043 can be used for central nervous system and metabolic disorders research .
Cat. No.: HY-123888
CAS No.: 55625-78-0
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Cat. No.: HY-W235067
CAS No.: 112-18-5
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N,N-Dimethyldodecylamine is a dynamin I inhibitor. N,N-Dimethyldodecylamine has an IC50 value of 14.79 μM for GTPase activity of dynamin I. N,N-Dimethyldodecylamine can be used in the research of diseases associated with endocytic defects, such as Alzheimer's disease and Huntington's disease .
Cat. No.: HY-16563R
CAS No.: 29477-83-6
Synonyms: Lycoricidinol (Standard)
Category:
Alkaloids Narcissus tazetta Linn. var. chinensis M.Roemer Amaryllidaceae Extract Plants Isoquinoline Alkaloids
Target:
Cat. No.: HY-178211
CAS No.: 2446484-96-2
SHY-867 is a pan RAS inhibitor. SHY-867 effectively prevents the binding of K-Ras proteins and other members of the Ras superfamily of small GTPases with EC50 values of 0.5-3 μM. SHY-867 effectively inhibits the phosphorylation of MEK, ERK1/2, and AKT downstream of K-Ras. SHY-867 inhibits the formation of the Ras-GTP activity complex. SHY-867 can be used to the studies of pancreatic cancer and non-small cell lung cancer .
Cat. No.: HY-146330
CAS No.: 2249757-45-5
FtsZ-IN-2 (Compound 19) is an inhibitor of the bacterial cell division protein FtsZ with GTPase inhibitory activity. FtsZ-IN-2 exhibits anti-staphylococcal activity with MIC values of 2 µg/ml for MSSA and MRSA .
Cat. No.: HY-134274
CAS No.: 23197-98-0
Synonyms: 8-Bromoguanosine-5'-triphosphate
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 .
Cat. No.: HY-178194
CAS No.: 2446485-15-8
SHY-855 is a pan RAS inhibitor. SHY-855 effectively prevents the binding of K-Ras proteins and other members of the Ras superfamily of small GTPases with IC50 values of 0.3-5 μM. SHY-855 effectively inhibits the phosphorylation of MEK, ERK1/2, and AKT downstream of K-Ras. SHY-855 inhibits the formation of the Ras-GTP activity complex. SHY-855 can be used to the studies of pancreatic cancer and non-small cell lung cancer .
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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
