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GTPases

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106

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7

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3

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-113066A
    Guanosine 5'-diphosphate disodium salt
    2 Publications Verification

    GDP disodium salt

    		 Hepcidin Potassium Channel Endogenous Metabolite Neurological Disease Inflammation/Immunology Cancer
    Guanosine 5'-diphosphate (GDP) disodium salt, a purine nucleoside diphosphate, is interconverted to guanosine by the action of exonucleotidase and phosphorylation of nucleoside to guanine. Guanosine 5'-diphosphate disodium salt activates adenosine 5'-triphosphate-sensitive K + channel and is used to study the kinetics and characteristics of GTPases such as those associated with G-protein coupled receptors (GPCR). Guanosine 5'-diphosphate disodium salt is a potential iron mobilizer, which prevents the Hepcidin (HY-P70400)-ferroportin interaction and modulates the interleukin-6 (IL-6)/stat-3 pathway. Elevated levels of guanosine 5’-diphosphate are associated with the pathogenesis of neurological diseases. Guanosine 5'-diphosphate disodium salt is promising for the research of inflammation, such as anemia of inflammation (AI) .
    Guanosine 5'-diphosphate disodium salt
  • HY-16563
    Narciclasine
    20+ Cited Publications

    Lycoricidinol

    		 ROCK Cancer
    Narciclasine is a plant growth modulator. Narciclasine modulates the Rho/Rho kinase/LIM kinase/cofilin signaling pathway, greatly increasing GTPase RhoA activity as well as inducing actin stress fiber formation in a RhoA-dependent manner.
    Narciclasine
  • HY-15723
    NSC 23766
    Maximum Cited Publications
    50 Publications Verification

    		 Ras Cancer
    NSC 23766 is a cell-permeable, reversible and specific inhibitor of Rac GTPase, used for cancer treatment.
    NSC 23766
  • HY-12874
    CASIN
    5+ Cited Publications

    		 Ras Apoptosis Cancer
    CASIN is a selective GTPase Cdc42 inhibitor with an IC50 of 2 uM. CASIN can be used for the research of cancer .
    CASIN
  • HY-12755
    ML141
    30+ Cited Publications

    CID-2950007

    		 Ras Apoptosis Cancer
    ML141 (CID-2950007) is a potent, allosteric, selective and reversible non-competitive inhibitor of Cdc42 GTPase. ML141 inhibits Cdc42 wild type and Cdc42 Q61L mutant with EC50s of 2.1 and 2.6 μM, respectively. ML141 shows low micromolar potency and selectivity against other members of the Rho family of GTPases (Rac1, Rab2, Rab7). ML141 do not show cytotoxicity in multiple cell lines .
    ML141
  • HY-13863
    Hydroxy-Dynasore
    15+ Cited Publications

    Dyngo-4a

    		 Dynamin Neurological Disease
    Hydroxy Dynasore (Dyngo-4a), a structural mimetic analog of Dynasore (HY-15304), is an improved, less cytotoxic and versatile dynamin inhibitor with IC50 values ​​of 0.38 μM and 2.3 μM for brain recombinant dynamin I and recombinant mouse dynamin II, respectively. Hydroxy Dynasore inhibits dynamin-dependent transferrin endocytosis with an IC50 of 5.7 μM.
    Hydroxy-Dynasore
  • HY-12646
    Rhosin hydrochloride
    35+ Cited Publications

    		 Ras Apoptosis Cancer
    Rhosin hydrochloride is a potent, specific RhoA subfamily Rho GTPases inhibitor. Rhosin hydrochloride specifically binds to RhoA to inhibit RhoA-GEF interaction with a Kd of ~ 0.4 uM, and does not interact with Cdc42 or Rac1, nor the GEF, LARG. Rhosin hydrochloride induces cell apoptosis . Rhosin hydrochloride promotes stress resiliency through enhancing D1-MSN plasticity and reducing hyperexcitability .
    Rhosin hydrochloride
  • HY-13452
    CID-1067700
    10+ Cited Publications

    ML282

    		 Ras Inflammation/Immunology
    CID-1067700 (ML282) is a pan GTPase inhibitor, and competitively inhibits Ras-related in brain 7 (Rab7) with a Ki of 13 nM.
    CID-1067700
  • HY-16659
    EHT 1864
    20+ Cited Publications

    		 Ras Neurological Disease Cancer
    EHT 1864 is an inhibitor of Rac family small GTPases. EHT 1864 directly binds and impairs the ability of this small GTPase to engage critical downstream effectors required for growth transformation. The Kd values are 40, 50, 60, and 230 nM for Rac1, Rac1b, Rac2 and Rac3, respectively. EHT 1864 also potently inhibits other Rac-dependent transformation processes, Tiam1- and Ras-mediated growth transformation. EHT 1864 prevents Aβ 40 and Aβ 42 production in vivo. EHT 1864 dependently suppresses the release of migrasomes from podocytes induced by LPS, PAN, or HG .
    EHT 1864
  • HY-107545
    Dynole 34-2
    1 Publications Verification

    		 Dynamin Apoptosis Cancer
    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) .
    Dynole 34-2
  • HY-12810
    EHop-016
    5+ Cited Publications

    		 Ras Cancer
    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 .
    EHop-016
  • HY-12646A
    Rhosin
    35+ Cited Publications

    		 Ras Apoptosis Cancer
    Rhosin is a potent, specific RhoA subfamily Rho GTPases inhibitor, which specifically binds to RhoA to inhibit RhoA-GEF interaction with a Kd of ~ 0.4 uM, and does not interact with Cdc42 or Rac1, nor the GEF, LARG. Rhosin induces cell apoptosis . Rhosin promotes stress resiliency through enhancing D1-MSN plasticity and reducing hyperexcitability .
    Rhosin
  • HY-131649
    Compound C108
    1 Publications Verification

    		 DNA/RNA Synthesis Cancer
    Compound C108 is a G3BP2 inhibitor. Compound C108 also targeted stress granule-associated proteins and Gtpase-activating protein (SH3 domain) binding protein 2. Compound C108 potently inhibits esophageal squamous cell carcinoma (ESCC) cell metastasis .
    Compound C108
  • HY-104064
    1A-116
    5+ Cited Publications

    		 Ras Apoptosis Cancer
    1A-116, a potent Rac1 inhibitor, is specific for W56 residues, can prevent EGF-induced Rac1 activation and block Rac1-P-Rex1 interaction. 1A-116 can induce apoptosis and inhibit cell proliferation, migration and cycle progression in a concentration-dependent manner. 1A-116 also demonstrates a high antimetastatic activity in vivo .
    1A-116
  • HY-100047
    Nα,Nα-Bis(carboxymethyl)-L-lysine

    		Taste Receptor Others
    Nα,Nα-Bis(carboxymethyl)-L-lysine is a competitive inhibitor of bitter taste receptor 4, with an IC50 of 59 nM. Nα,Nα-Bis(carboxymethyl)-L-lysine can be used in bitter receptors related study .
    Nα,Nα-Bis(carboxymethyl)-L-lysine
  • HY-12762
    QS11
    2 Publications Verification

    		 β-catenin Wnt Arf Family GTPase Cancer
    QS11 is an inhibitor of ARFGAP1 (ADP-ribosylation factor GTPase-activating protein 1), with an EC50 of 1.5 μM. QS11 activates Wnt/β-catenin signaling through an effect on protein trafficking. QS11 inhibits migration of ARFGAP overexpressing breast cancer cells .
    QS11
  • HY-152086
    DRP1i27

    		Dynamin Cardiovascular Disease
    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 .
    DRP1i27
  • HY-B0515
    Ibandronate Sodium Monohydrate
    1 Publications Verification

    BM-210955; RPR-102289A

    		 Apoptosis Metabolic Disease Cancer
    Ibandronate Sodium Monohydrate (BM-210955; RPR-102289A) is an orally active, selective inhibitor of farnesyl pyrophosphate synthase (FPP synthase). Ibandronate Sodium Monohydrate 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 Monohydrate 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 Monohydrate is used in the study of osteoporosis and bone metastatic tumors (such as breast cancer bone metastasis) .
    Ibandronate Sodium Monohydrate
  • HY-113849
    MLS-573151
    3 Publications Verification

    MLS000573151

    		 Ras Inflammation/Immunology
    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 .
    MLS-573151
  • HY-P1732
    Transportan

    		Biochemical Assay Reagents Cancer
    Transportan is an amphipathic cell-penetrating peptide containing 12 functional amino acids from the amino terminus of the neuropeptide galanin and mastoparan in the carboxyl terminus, connected via a lysine. Transportan interacts with galanin receptors and G-proteins, modulates GTPase activity, enters cells via direct translocation and endocytic pathways, accumulates in cytoplasmic, nuclear, and membranous structures, and delivers cargo including peptides, PNAs, proteins, siRNA, and liposomes [12].
    Transportan
  • HY-154959
    AZD4747

    		Ras Cancer
    AZD4747 is a selective, blood-brain barrier-permeable mutant GTPase KRAS G12C inhibitor. AZD4747 has the potential to study cancer .
    AZD4747
  • HY-124306
    ML-099
    5 Publications Verification

    CID-888706

    		 Ras Cancer
    ML-099 (CID-888706) is a pan Ras-related GTPases activator that can activate Rac1, cell division cycle 42, Ras, Rab7, and Rab-2A .
    ML-099
  • HY-B0580B
    (R)-Ketorolac
    1 Publications Verification

    (+)-Ketorolac

    		 Ras Cancer
    (R)-Ketorolac is an orally active Cdc42 and Rac1 inhibitor. (R)-Ketorolac inhibits GTPase. (R)-Ketorolac alters ovarian cancer cell behaviors critical for invasion and metastasis. (R)-Ketorolac ameliorates cancer-associated cachexia .
    (R)-Ketorolac
  • HY-173350
    Ran-IN-1

    		Arf Family GTPase Apoptosis Cancer
    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 .
    Ran-IN-1
  • HY-152086A
    DRP1i27 dihydrochloride

    		Dynamin Cardiovascular Disease
    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 .
    DRP1i27 dihydrochloride
  • HY-110354
    UCM05
    2 Publications Verification

    G28UCM

    		 Fatty Acid Synthase (FASN) Bacterial Infection
    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].
    UCM05
  • HY-115376
    Z62954982

    ZINC08010136

    		 Ras Inflammation/Immunology
    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) .
    Z62954982
  • HY-117149
    MLS000532223

    		Ras Cancer
    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 .
    MLS000532223
  • HY-152218
    Clathrin-IN-4

    		Dynamin Neurological Disease
    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 .
    Clathrin-IN-4
  • HY-145080
    Dynole 2−24
    1 Publications Verification

    		 Dynamin Neurological Disease
    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
    Dynole 2−24
  • HY-B0515B
    Ibandronate Sodium
    1 Publications Verification

    		 Apoptosis Metabolic Disease Cancer
    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) .
    Ibandronate Sodium
  • HY-125987
    RBC6

    		Ras Cancer
    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 .
    RBC6
  • HY-125355
    SEC
    1 Publications Verification

    		 Apoptosis Annexin A Cancer
    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 .
    SEC
  • HY-172917
    Rho GTPase inhibitor 1

    		Ras Cancer
    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 .
    Rho GTPase inhibitor 1
  • HY-129189
    RAS GTPase inhibitor 1

    		Ras Cancer
    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 .
    RAS GTPase inhibitor 1
  • HY-118208
    ML-097
    2 Publications Verification

    CID-2160985

    		 Ras Cancer
    ML-097 (CID-2160985) is a pan Ras-related GTPases activator that can activate Rac1, cell division cycle 42, Ras, and Rab7 .
    ML-097
  • HY-155656
    Anti-inflammatory agent 49

    		Dynamin Inflammation/Immunology
    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 .
    Anti-inflammatory agent 49
  • HY-152216
    Dynamin IN-2

    		Dynamin Neurological Disease
    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 .
    Dynamin IN-2
  • HY-W013158
    Trimethyloctadecylammonium bromide

    		Dynamin Infection
    Trimethyloctadecylammonium bromide is an inhibitor of dynamin, with an IC50 value of 1.9 μM for dynamin I. Trimethyloctadecylammonium bromide exhibits antibacterial activity against Staphylococcus aureus .
    Trimethyloctadecylammonium bromide
  • HY-163707
    UR778Br

    		Apoptosis Cancer
    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 .
    UR778Br
  • HY-P2325
    Exoenzyme C3, clostridium botulinum

    		Biochemical Assay Reagents ROCK Neurological Disease Metabolic Disease
    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 .
    Exoenzyme C3, clostridium botulinum
  • HY-110174
    NAB2

    		α-synuclein Neurological Disease
    NAB2 is a neuroprotectant that targets the small GTPase Rab1a. NAB2 selectively binds to the GDP-bound form of Rab1a and protects multiple cell types from α-synuclein toxicity by increasing Rab1a expression. Rab1a regulates ER-to-Golgi trafficking and mediates endosomal trafficking events of the E3 ubiquitin ligase Rsp5/Nedd4. NAB2 stimulates ubiquitination of related proteins in a Nedd4-dependent manner and rescues α-synuclein-associated trafficking defects associated with early-onset Parkinson's disease .
    NAB2
  • HY-W549903
    p67phox-IN-1

    		NADPH Oxidase Ras Cancer
    p67phox-IN-1 (Formula IIIa Compound) is an inhibitor targeting the interaction between Rac GTPase and p67 phox protein .
    p67phox-IN-1
  • HY-113066AR
    Guanosine 5'-diphosphate disodium salt (Standard)

    GDP disodium salt (Standard)

    		 Hepcidin Endogenous Metabolite Potassium Channel Reference Standards Neurological Disease Inflammation/Immunology Cancer
    Guanosine 5'-diphosphate (disodium salt) (Standard) is the analytical standard of Guanosine 5'-diphosphate (disodium salt). This product is intended for research and analytical applications. Guanosine 5'-diphosphate (GDP) disodium salt, a purine nucleoside diphosphate, is interconverted to guanosine by the action of exonucleotidase and phosphorylation of nucleoside to guanine. Guanosine 5'-diphosphate disodium salt activates adenosine 5'-triphosphate-sensitive K+ channel and is used to study the kinetics and characteristics of GTPases such as those associated with G-protein coupled receptors (GPCR). Guanosine 5'-diphosphate disodium salt is a potential iron mobilizer, which prevents the Hepcidin (HY-P70400)-ferroportin interaction and modulates the interleukin-6 (IL-6)/stat-3 pathway. Elevated levels of guanosine 5’-diphosphate are associated with the pathogenesis of neurological diseases. Guanosine 5'-diphosphate disodium salt is promising for the research of inflammation, such as anemia of inflammation (AI) .
    Guanosine 5'-diphosphate disodium salt (Standard)
  • HY-158359
    5′-XDP sodium

    Xanthosine 5′-diphosphate sodium

    		 Endogenous Metabolite Others
    5’-XDP sodium (Xanthosine 5' -diphosphate sodium) is an ADP analog involved in the synthesis of ribosomes .
    5′-XDP sodium
  • HY-149464
    ARN22089

    		Ras Cancer
    ARN22089 is a oral active novel class of trisubstituted pyrimidine, blocks the interaction of CDC42 GTPases with specific downstream effectors. ARN22089 blocks tumor growth in BRAF mutant mouse melanoma model .
    ARN22089
  • HY-111549
    Bragsin1

    		Arf Family GTPase Cancer
    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 .
    Bragsin1
  • HY-175763
    Z55660043

    		RGS Protein Neurological Disease Metabolic Disease
    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 .
    Z55660043
  • HY-123888
    Viomellein

    		E1/E2/E3 Enzyme Bacterial Cancer
    Viomellein is a SUMOylation inhibitor with antibacterial and anticancer activities. Viomellein inhibits biofilm formation of strains produced from the fungus Aspergillus ochraceus from the Mediterranean sponge Agelas oroides. Viomellein exhibits cytotoxicity against A2780 human ovarian cancer cells with an IC50 value of 5.0 μM. Viomellein also inhibits SUMOylation of RanGAP1 (GTPase activating protein) with an IC50 of 10.2 μM .
    Viomellein
  • HY-152217
    Clathrin-IN-2

    		Dynamin Neurological Disease Metabolic Disease Cancer
    Clathrin-IN-2 is potent inhibitor of clathrin mediated endocytosis (CME) with an IC50 value of 2.3 μM. Clathrin-IN-2 also has inhibitiory for dyn I GTPase with an IC50 value of 7.7 μM .
    Clathrin-IN-2

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