Adipogen/CX4945 . hydrochloride/AGCR13629M001/1 mg

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ProductDetails
Synonyms	Silmitasertib.HCl;8-Carboxy-N-(3-chlorophenyl)benzo[c][2,6]naphthyridin-5-aminiumchloride
ProductType	Chemical
Properties
Formula	C₁₉H₁₂ClN₃O₂.HCl
MW	349.8.36.5
CAS	1009820-21-6(freeacid)
PurityChemicals	≥98%
Appearance	Yellowsolid.
Solubility	SolubleinDMSO.Insolubleinwater.
InChiKey	OBOIGMDUOMSAHW-UHFFFAOYSA-N
ShippingandHandling
Shipping	AMBIENT
ShortTermStorage	+4°C
LongTermStorage	-20°C
HandlingAdvice	Keepcoolanddry.
Use/Stability	Stableforatleast2yearsafterreceiptwhenstoredat-20°C.
Documents
MSDS	DownloadPDF
ProductSpecificationSheet
Datasheet	DownloadPDF

Orallyactive,potentandselectiveATP-competitiveinhibitoroftheproteinkinaseCK2(IC₅₀=1nM).
Anticancercompound.InhibitsproliferationinapanelofcancercelllinesthatoverexpressCK2.Inhibitedmigration,blockssurvivalandinducesapoptosisincancerstemcells,glioblastomasandleukemiacells.
Showntodecreasetheglucosemetabolismincancercells.
PotentinhibitorofCdc2-likekinases(Clks)invitro,consequentlyinterferingwithalternativesplicing.
PotentATP-competitiveinhibitorofDYRK1A(IC₅₀=6.8nM),DYRK1B(IC₅₀=6.4nM)andDYRK3(IC₅₀=18nM),involvedinneurodegeneration-associateddiseases.
CK2αdeletionselectivelyincreasedM3muscarinicreceptors(M3Rs)-mediatedinsulinsecretionfrompancreaticislets.
PromotedcAMP-inducedthermogenesisinwhiteadipocytes.
CK2inhibitionamelioratesdiet-inducedobesityandinsulinresistanceinmiceinvivobypromotingUCP1-dependentthermogenesis.

ProductReferences

CX-4945,anorallybioavailableselectiveinhibitorofproteinkinaseCK2,inhibitsprosurvivalandangiogenicsignalingandexhibitsantitumorefficacy:A.Siddiqui-Jain,etal.;CancerRes.70,10288(2010)
StructuralbasisofCX-4945bindingtohumanproteinkinaseCK2:A.D.Ferguson,etal.;FEBSLett.585,104(2011)
DiscoveryandSARof5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylicacid(CX-4945),thefirstclinicalstageinhibitorofproteinkinaseCK2forthetreatmentofcancer:F.Pierre,etal.;J.Med.Chem.54,635(2011)
Pre-clinicalcharacterizationofCX-4945,apotentandselectivesmallmoleculeinhibitorofCK2forthetreatmentofcancer:F.Pierre,etal.;Mol.CellBiochem.356,37(2011)
CX-4945,aselectiveinhibitorofcaseinkinase-2(CK2),exhibitsanti-tumoractivityinhematologicmalignanciesincludingenhancedactivityinchroniclymphocyticleukemiawhencombinedwithfludarabineandinhibitorsoftheB-cellreceptorpathway:R.C.Prins,etal.;Leukemia27,2094(2013)
CK2inhibitorCX4945inducessequentialinactivationofproteinsinthesignalingpathwaysrelatedwithcellmigrationandsuppressesmetastasisofA549humanlungcancercells:M.J.Ku,etal.;Bioorg.Med.Chem.Lett.23,5609(2013)
IdentificationofanovelfunctionofCX-4945asasplicingregulator:H.Kim,etal.;PLosOne9,e94978(2014)
Activityoftheclinical-stageCK2-specificinhibitorCX-4945againstchroniclymphocyticleukemia:L.R.Martins,etal.;Leukemia28,179(2014)
PhosphoproteomicsidentifiesCK2asanegativeregulatorofbeigeadipocytethermogenesisandenergyexpenditure:K.Shinoda,etal.;CellMetab.22,997(2015)
CK2actsasapotentnegativeregulatorofreceptor-mediatedinsulinreleaseinvitroandinvivo:M.Rossi,etal.;PNAS112,E6818(2015)
Thecaseinkinase2inhibitor,CX-4945,asananti-cancerdrugintreatmentofhumanhematologicalmalignancies:H.J.Chon,etal.;Front.Pharmacol.6,70(2015)
AchemicalwithprovenclinicalsafetyrescuesDown-syndrome-relatedphenotypesinthroughDYRK1Ainhibition:H.Kim,etal.;Dis.ModelMech.9,839(2016)
TargetingproteinkinaseCK2suppressesbladdercancercellsurvivalviatheglucosemetabolicpathway:X.Zhang,etal.;Oncotarget7,87361(2016)

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Adipogen/CX4945 . hydrochloride/AGCR13629M001/1 mg