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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
103 Results for "
GTPases
" in MedChemExpress (MCE) Product Catalog:
Products (103)
103 Results for "GTPases" in MCE Product Catalog:
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1 Cited Publications
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Dynole 2−24 is an indole-based dynamin GTPase inhibitor (IC50=0.56 μM for dynamin I). Dynole 2−24 is nontoxic and shows increased potency against dynamin I and II in vitro and in cells (IC₅₀(CME)=1.9 μM). Dynole 2−24 also shows 4.4-fold selectivity for dynamin I. Dynole 2−24 is active in-cell inhibitor of clathrin-mediated endocytosis . CME: Clathrin mediated endocytosis
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1 Cited Publications
Cat. No.: HY-B0515B
CAS No.: 138844-81-2
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Ibandronate Sodium is an orally active, selective inhibitor of farnesyl pyrophosphate synthase (FPP synthase). Ibandronate Sodium can block the mevalonate pathway to inhibit the isoprenylation modification of small GTPases (such as RAS, RHO family proteins), induce tumor cell apoptosis and inhibit bone resorption. Ibandronate Sodium inhibits tumor cell proliferation (such as ER+ breast cancer cells), promotes the expression of the pro-apoptotic gene FAS, and can produce synergistic anti-tumor effects with anti-estrogen compounds. Ibandronate Sodium is used in the study of osteoporosis and bone metastatic tumors (such as breast cancer bone metastasis) .
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1 Cited Publications
SEC induces activation of ANXA7 GTPase via the AMPK/mTORC1/STAT3 signaling pathway. SEC selectively promotes apoptosis in cancer cells, expressing a high level of ITGB4 by inducing ITGB4 nuclear translocation .
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nti-inflammatory agent 49 (compound SC9) is a quite potent and selective inhibitor of Drp1-Fis1 interaction and can reduce FIS1-mediated mitochondrial dysfunction. The IC50 of SC9 inhibiting GTPase in vitro is 270 nM .
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1 Cited Publications
Cat. No.: HY-170327
CAS No.: 664975-73-9
ZCL279 is a small molecule modulator (SMM) that inhibits Cdc42-intersectin (ITSN) interaction. ZCL279 can activate Cdc42 (a cytoplasmic small GTPase in the Ras superfamily) at lower concentrations (<10 μM) and significantly inhibit it at higher concentrations (<10 μM) .
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1 Cited Publications
Bragsin2 is a potent, selective and noncompetitive nucleotide exchange factor BRAG2 inhibitor, with an IC50 of 3 μM. Bragsin2 binds at the interface between the PH domain of BRAG2 and the lipid bilayer, leads BRAG2 unable to activate lipidated Arf GTPase. Bragsin2 affects breast cancer stem cells .
Cat. No.: HY-152086
CAS No.: 1453028-33-5
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DRP1i27 is a potent inhibitor of human Drp1 (dynamin-related protein 1). DRP1i27 binds to the GTPase site of Drp1, with hydrogen bonds to Gln34 and Asp218. DRP1i27 targets Drp1-mediated mitochondrial fission in cell line models and protects against simulated ischemia-reperfusion injury .
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 .
Cat. No.: HY-152086A
Purity: 98.63%
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DRP1i27 dihydrochloride is a potent inhibitor of human Drp1 (dynamin-related protein 1). DRP1i27 dihydrochloride binds to the GTPase site of Drp1, with hydrogen bonds to Gln34 and Asp218. DRP1i27 dihydrochloride targets Drp1-mediated mitochondrial fission in cell line models and protects against simulated ischemia-reperfusion injury .
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-172917
CAS No.: 1309252-99-0
Rho GTPase inhibitor 1 (compound 7) is a potent Rho GTPase inhibitor. Rho GTPase inhibitor 1 exhibits high affinity on Cdc42, Rac1 and RhoA with KDs of 151, 352, and 232 μM, respectively. Rho GTPase inhibitor 1 reduces cell migration on glioma cell line .
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 .
RBC6 is an inhibitor of GTPases RalA. RBC6 inhibits binding of Ral to its effector RALBP1. RBC6 also inhibits Ral-mediated cell spreading of murine embryonic fibroblasts, as well as anchorage-independent growth of human cancer celllines .
Cat. No.: HY-152216
CAS No.: 1345853-49-7
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Dynamin IN-2 (compound 43), a Wiskostatin (HY-12534) analogue, is a potent dynamin inhibitor, with an IC50 of 1.0 μM for dynamin I GTPase. Dynamin IN-2 also blocks clathrin mediated endocytosis (CME), with an IC50 of 9.5 μM .
Cat. No.: HY-163707
CAS No.: 866127-80-2
UR778Br targets the GTPase-activating protein-related domain (GRD domain) of IQGAP1 proteins. UR778Br inhibits the proliferation of human acute myeloid leukemia (AML), arrests the cell cycle at the G2/M phase, and induces apoptosis. UR778Br inhibits colony formation of primary and AML cells, without significant impacts on normal bone marrow cells .
Cat. No.: HY-P2325
CAS No.: 58319-92-9
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Exoenzyme C3, clostridium botulinum, is a mono-ADP-ribosylating enzyme. Exoenzyme C3, clostridium botulinum specifically modifies RhoA, B, and C by transferring ADP-ribose to them, thereby inactivating these GTPases. Exoenzyme C3, clostridium botulinum can induce neuronal axonal and dendritic growth, inhibit macrophage migration, and regulate cytoskeletal dynamics. Exoenzyme C3, clostridium botulinum can be used in the research of spinal cord injury and diabetic painful neuropathy .
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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
