Productoverview

• Name
  Cmpd101
• Shortdescription
  Novel,potentandselectiveGRK2/GRK3inhibitor
• BIOLOGicaldescription

  Cmpd101(Compound101)isanovel,potentandselectiveG-proteincoupledreceptorkinase2and3(GRK2/GRK3)inhibitor(IC₅₀valuesare35and32nMatGRK2andGRK3respectively).

  ShowsnoactivityatGRK5atconcentrationsupto125µMandshowslittleactivityatabroadrangeofotherkinases.

  Membranepermeable.

  Cmpd101canbeusedtostudyrolesofGRK2/3inGPCRdesensitizationandotherfunctions.

  Showntopotentiatephosphatidylinositol4,5-bisphosphate(PIP2)depletionandslowagoNIST-induceddesensitizationofprotease-activatedreceptor2(PAR2).

• Alternativenames
  Compound101;Takedacompound101
• Biologicalaction
  Inhibitor
• Purity
  >98%
• Customercomments

  WewouldrecommendCmpd101 fromHelloBio–itperformsexactlyasexpectedinassayslookingatMOPrdesensitisation,phosphorylationandinternalisation.  DrChrisBailey,UniversityofBath,UKandauthoronMolPharmacolpaper,PubMedID26013542

  YourCmpd101–workedgreat!DrStevenGee,PfizerNeuroscience,USA

  YourCmpd101behavedasexpected.Verifiedcustomer,MonashUniversity

• Ourproductsinaction
  6citationsSubmitYourCitationNow

Images

• 
• 
• 
• 

PrevNext

Properties

• Chemicalname
  3-[(4-methyl-5-pyridin-4-yl-1,2,4-triazol-3-yl)methylamino]-N-[[2-(trifluoromethyl)phenyl]methyl]benzamidehydrochloride
• MolecularWeight
  502.92
• Chemicalstructure
  
• MolecularFormula
  C₂₄H₂₁N₆OF₃.HCl
• CASNumber
  865608-11-3
• PubChemidentifier
  11677079
• SMILES
  CN1C(=NN=C1C2=CC=NC=C2)CNC3=CC=CC(=C3)C(=O)NCC4=CC=CC=C4C(F)(F)F
• Source
  Synthetic
• InChi
  InChI=1S/C24H21F3N6O/c1-33-21(31-32-22(33)16-9-11-28-12-10-16)15-29-19-7-4-6-17(13-19)23(34)30-14-18-5-2-3-8-20(18)24(25,26)27/h4-13,29H,14-15H2,1H3,(H,30,34)
• InChiKey
  WFOVEDJTASPCIR-UHFFFAOYSA-N
• Appearance
  Yellowsolid

StoringandUsingYourProduct

• Storageinstructions
  -20°C
• Solubilityoverview
  SolubleinDMSO(100mM)
• Handling
  Hydroscopicsolid,contactwithairmaycausematerialtobecomesticky.Productperformanceshouldnotbeaffectedbutwerecommendstoringthematerialinasealedjar.
• Important
  ThisproductisforRESEARCHUSEONLYandisnotintendedfortherapeuticordiagnosticuse.Notforhumanorveterinaryuse.

ReferencesforCmpd101

• MolecularmechanismofselectivityamongGprotein-coupledreceptorkinase2inhibitors.

  Thaletal(2011)MolPharmacol80:294-303

  PubMedID:21596927

• RoleofGProtein-CoupledReceptorKinases2and3inμ-OpioidReceptorDesensitizationandInternalization.

  Loweetal(2015)MolPharmacol88(2):347-56

  PubMedID:26013542

• Contributionsofproteinkinasesandβ-arrestintoterminationofprotease-activatedreceptor2signaling.

  Jungetal(2016)JGenPhysiol147(3):255-71

  PubMedID:26927499

• Distinctcorticalandstriatalactionsofaβ-arrestin-biaseddopamineD2receptorligandrevealuniqueantipsychotic-likeproperties.

  Ursetal(2016)ProcNatlAcadSciUSA113(50):E8178-E8186

  PubMedID:27911814
品牌介绍
Hello Bio是由一群经验丰富的科学家和化学家们创立的充满活力的生物企业，总部位于英国布里斯托尔，在美国普林斯顿设有分公司，主旨在于提供质优价廉的生命科学研究工具，主要产品线为小分子化合物，如激动剂、拮抗剂、抑制剂等，部分产品价格甚至低至其他供应商的50%。热销产品线：酶抑制剂和激动剂ROCK inhibitor Y-27632, PKA inhibitor KT 5720 , adenylyl cyclase activator Forskolin, and novel GRK2/3 inhibitor Cmpd101等。 离子通道调节剂NMDA antagonist D-AP5, sodium channel blocker tetrodotoxin citrate, TRP antagonist capsazepine, and GABAA antagonist SR 95531 等。信号通路工具各种信号通路抑制剂、激动剂表观遗传学研究工具potent HDAC inhibitor Trichostatin A, DNA methyltransferase inhibitor 5-aza-2'-deoxycytidine,BET bromodomain inhibitor (+)-JQ1 and potent,selective GLP / G9a HMTase inhibitor BIX 01294 等受体配体novel selective GRK2/3 inhibitor,  NMDA antagonist D-AP5, Group I mGlu agonist (S)-3,5-DHPG, and GABAA antagonist SR 95531.等干细胞调节剂ROCK inhibitor Y-27632,  SB 431542 DAPT.