Description:Highaffinitygroup1PAKinhibitorChemicalName:8-[(trans-5-Amino-1,3-dioxan-2-yl)methyl]-6-[2-chloro-4-(6-methyl-2-pyridinyl)phenyl]-2-(methylamino)-pyrido[2,3-d]pyrimidin-7(8H)-onePurity:≥98%(HPLC)BIOLOGicalActivityTechnicalDataSolubilityCalculatorsDatasheetsReferencesBiologicalActivityHighaffinitygroup1PAK(pan-PAK1,2and3)inhibitor(Ki=3.7nM;pMEKIC50=69nM).Of235kinasestested,otherthanPAK1,eight(PAK2,PAK3,KHS1,Lck,MST3,MST4,SIK2,andYSK1)wereinhibited>70%.ExhibitslowhERGchannelactivity(<50%inhibitionat10μM).Orallybioavailable.Chemicalprobes.orgisaportalthatoffersindependentguidanceontheselectionand/orapplicationofsmallmoleculesforresearch.TheuseofG5555isreviewedonthechemicalprobeswebsite.TechnicalDataM.Wt492.96FormulaC25H25ClN6O3StorageStoreat-20°CPurity≥98%(HPLC)CASNumber1648863-90-4SmilesCNC1=NC=C2C=C(C3=C(C=C(C4=CC=CC(C)=N4)C=C3)Cl)C(N(C2=N1)C[C@H]5OC[C@@H](CO5)N)=OThetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.AllTocrisproductsareintendedforlaboratoryresearchuseonly.SolubilityDataSolventMaxConc.mg/mLMaxConc.mMSolubility1eq.HCl49.3100DMSO9.8620mMwithgentlewarmingPreparingStockSolutionsThefollowingdataisbasedontheproductmolecularweight492.96.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.Concentration/SolventVolume/Mass1mg5mg10mg1mM2.03mL10.14mL20.29mL5mM0.41mL2.03mL4.06mL10mM0.2mL1.01mL2.03mL50mM0.04mL0.2mL0.41mLMolarityCalculatorMolarityCalculatorCalculatethemass,volume,orconcentrationrequiredforasolution.ReconstitutionCalculatorReconstitutionCalculatorDilutionCalculatorDilutionCalculatorCalculatethedilutionrequiredtoprepareastocksolution.ProductDatasheetsCertificateofAnalysis/ProductDatasheetSafetyDatasheetSelectanotherlanguage:EnglishGermanFrenchSpanishViewSDSReferencesReferencesarepublicationsthatsupporttheproducts'biologicalactivity.Ndubakuetal(2015)DesignofselectivePAK1inhibitorG-5555:improvingpropertiesbyemployinganunorthodoxlow-pKapolarmoiety.ACSMed.Chem.Lett.61241PMID:26713112Keywords:G5555,supplier,G5555,Selective,high,affinity,group,1,PAK,pan-PAK1,PAK2,PAK3,inhibitors,inhibits,orally,bioavailable,p21,activated,kinase,P21-activated,Kinases,P21-activated,Kinases,TocrisBioscience
Tocris Bioscience是一家专卖生命科学研究chemicals, peptides and antibodies的知名品牌，其产品也广为各大药厂、大学、研究机构，超过五万名科学研究者所采用。 目前，產品內容已超過一千六百種以上，並每年持續不斷的增加新的產品。目前，产品内容已超过一千六百种以上，并每年持续不断的增加新的产品。
Tocris bioscience是位于英国布里斯托尔（Bristol）的高品质试剂提供商，共有2000多种产品，主要集中在神经科学和信号传导领域，产品类型包括小分子、多肽、抗体、配体和化合物筛选文库等，主要产品包括GPCR ligands，神经传递素，离子通道调控剂，信号通路抑制剂等，这些产品被广泛选择性地用于阻断或激活生物学通路。Tocris是世界上神经科学研究领域无可争议的领导者，其生产的影响神经系统的化学物质被多次引用，这些物质很多都来自Jeff Watkins（Tocris 的创立人）在Bristol大学原创性的研究工作。
Tocris Bioscience的主要产品包括：
Small Molecules
Peptides
Aptamers
Controlled Substances
Compound Libraries
DREADD Ligands
Fluorescent Imaging
Ligand Sets
Optopharmacology
Reagents
Toxins
按照研究领域细分：
Cancer
Cardiovascular System
Endocrinology
Immunology
Neuroscience
Pain & Inflammation
Respiratory System
