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商品描述
AlternativeName3-(4)-Dimethylaminobenzylidineanabaseine
LyophilizedPowderLyophilizedPowder
Thisproductisfreezedried.Allwatermoleculeshavebeenremoved.
BioassayTestedBioassayTested
Everylotistried&testedinarelevantBIOLOGicalassay.
OurBioassay
SourceSynthetic
MW:364.3
Purity:>98%
Effectiveconcentration0.1-10µM.
Chemicalname4-[(5,6-Dihydro[2,3"-bipyridin]-3(4H)-ylidene)methyl]-N,N-dimethylbenzenaminedihydrochloride.
MolecularformulaC19H21N3*2HCl.
CASNo.:154149-38-9,32013-69-7.
ActivityDMAB-anabaseinedihydrochlorideisapartialagoNISTofα7nicotinicacetylcholinereceptors(nAChR)andantagonistofα4/β2nAChR1.Itblockstheacetylcholineinducedα7currentwithIC50 ~5µM2.DMAB-anabaseinedihydrochloridecanalsodisplaceisotopic(-)-cytisineandα-bungarotoxinbindingtoratbrainmembraneswithhighaffinity3.
- Kem,W.R. etal. (1997) J.Pharmacol.Exp.Therap. 283, 979.
- Weltzin,M.M. etal. (2010) J.Pharmacol. 334, 917.
- deFiebre,C.M. etal. (1995) Mol.Pharmacol. 47, 164.
ShippingandstorageShippedatroomtemperature.Productassuppliedcanbestoredintactatroomtemperatureforseveralweeks.Forlongerperiods,itshouldbestoredat-20°C.
SolubilityAnyaqueousbuffer.Centrifugeallproductpreparationsbeforeuse(10000xg5min).
StorageofsolutionsUptooneweekat4°Corsixmonthsat-20°C.
AlomoneLabsDMAB-anabaseinedihydrochlorideinhibitsα7nicotinicacetylcholinereceptorsheterologouslyexpressedin Xenopus oocytes.A.Currenttracesofα7nicotinicacetylcholinereceptoractivityat-60mVholdingpotential.Currentswereelicitedbyapplicationof100µMacetylcholineevery50seconds.Inhibitionoftheseinducedcurrentswasachieveduponperfusionof1or10µM DMAB-anabaseinedihydrochloride (#D-110)(indicatedbyhorizontalbars).B.Superimposedcurrentresponsestotheapplicationofeither100µMacetylcholine(Ach)or100µMDMAB-anabaseinedihydrochloride(Ana),demonstratingthepartialagonisteffectonα7channels.
References-Scientificbackground
- 1.Kombo,D.C. etal. (2011) Eur.J.Med.Chem. 46,5625.
- 2.Papke,R.L. etal. (1994) GiacobiniE,BeckerR(eds)Alzheimerdisease: therapeuticstrategies,206.
- 3.deFiebre,C.M. etal. (1995) Mol.Pharmacol. 47, 164.
- 4.Kem,W.R. etal. (1997) J.Pharmacol.Exp.Therap. 283, 979.
- 5.Stevens,K.E. etal. (1998) Psychopharmacology 136, 320.
- 6.Weltzin,M.M. etal. (2010) J.Pharmacol. 334, 917.
nAChRsaremembersoftheCys-loopligand-gatedionchannelsuperfamily,locatedbothintheperipheralandcentralnervoussystems(PNSandCNS,respectively).Thesereceptors,existingasbothhomopentamericandheteropentamerictransmembraneionchannels,arevalidatedtherapeutictargetsforvariousCNSpathologies1.
DMAB-anabaseine(DMAB),ananabaseineanalog,isaselectivelypartialagonistatα7receptorswhicharepredominantlyfoundintheCNS2,3.Incontrast,DMABisanantagonistatα3β4,α4β2andothernicotinicreceptors4,5andblockstheα4β2currentwithIC50 ~5µM6.
TargetnAChR
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Lastupdate:23/10/2019
DMAB-anabaseinedihydrochloride(#D-110) isahighlypure,synthetic,andbiologicallyactivecompound.
Forresearchpurposesonly,notforhumanuse
Discovery Antibodies的Cyclin dependant kinase 2 (CDK2) is a serine/threonine protein kinase which controls both G1/S and G2/M transitions. CDKs along with cyclins and CDK inhibitors regulate cell cycle progression. Specific cyclins activate different CDKs; in early G1, CDK2 pairs with cyclin E to promote entry into the S phase before switching to partner with cyclin A to drive the cell through S phase. Once activated CDKs phosphorylate downstream proteins to initiate signalling cascades. CDK2 phosphorylates and inactivates the RB1 (pRb) tumour suppressor family of proteins.CDK的活动受到严格控制。CDK2活性可以被包括P21在内的一系列抑制剂抑制。细胞周期失调和增殖控制的丧失与细胞转化和癌症密切相关。CDK2在DNA损伤反应（DDR）中的细胞周期停滞中也似乎起着积极作用，它的抑制作用会阻碍DDR，并使细胞对电离辐射敏感，从而诱导细胞死亡。该抗体与AlexaFluor®488偶联。AlexaFluor®488是一种流行的鲜绿色荧光染料，具有高pH稳定性。
