EHT 5372 - ≥95% , CAS No.1425945-63-6

CAS: 1425945-63-6 Cat. No.: E647460 Summenformel: C17H11Cl2N5OS Molekulargewicht: 404.27 PubChem CID: 71529610
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QUALITÄT & REINHEIT ≥95%
Storage
Store at -20°C
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5mg
E647460-5mg
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10mg
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25mg
E647460-25mg
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50mg
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100mg
E647460-100mg
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Warum diese Qualität

≥95% für empfindliche chromatographische und analytische Workflows, die minimale Basislinieninterferenzen erfordern.

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Lagerung & Versand

Store at -20°C Versand Ice chest + Ice pads. Genaue Spezifikationen finden Sie im chargenspezifischen COA.

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Qualitätsdokumente

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Literaturbeleg

In 0 peer-reviewten Publikationen zu Chromatographie, organischer Synthese und Kreuzkupplungsreaktionen zitiert.

Übersicht

EHT 5372 is a highly potent and selective inhibitor of DYRK's family kinases with IC 50 s of 0.22, 0.28, 10.8, 93.2, 22.8, 88.8, 59.0, 7.44, and 221 nM for DYRK1A , DYRK1B , DYRK2 , DYRK3, CLK1, CLK2, CLK4, GSK-3α , and GSK-3β , respectively

In Vitro

EHT 5372 (0.1-10 μM; 24 hours) dose-dependently reduces pS396-Tau levels with an IC 50 of 1.7 μM whereas cell viability remains over 87% in all conditions. EHT 5372 (0.01-1 μM) inhibits the direct phosphorylation of Tau by DYRK1AEHT 5372 reduces Aβ production in a dose-dependent reduction with an IC 50 of 1.06 μM. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: HEK293 cells Concentration: 0.1, 0.5, 1, 5, 10 μM Incubation Time: 24 hours Result: Cell viability remained over 87% in all conditions. Western Blot AnalysisCell Line: HEK293 cells Concentration: 0.01, 0.03, 0.1, 0.3 , 1 μM Incubation Time: Result: Potently and dose-dependently inhibited Tau phosphorylation at pS396.

Form:Solid

IC50& Target:DYRK1A|0.22 nM (IC|50|)|DYRK1B|0.28 nM (IC|50|)|DYRK2|10.8 nM (IC|50|)|DYRK4|93.2 nM (IC|50|)|CLK1|22.8 nM (IC|50|)|CLK2|88.8 nM (IC|50|)|CLK4|59.0 nM (IC|50|)|GSK-3α|7.44 nM (IC|50|)|GSK-3β|221 nM (IC|50|)

Spezifikationen

Spezifikationen & Reinheit
≥95%
Biochemische und physiologische Mechanismen
EHT 5372 is a highly potent and selective inhibitor of DYRK's family kinases with IC 50 s of 0.22, 0.28, 10.8, 93.2, 22.8, 88.8, 59.0, 7.44, and 221 nM for DYRK1A , DYRK1B , DYRK2 , DYRK3, CLK1, CLK2, CLK4, GSK-3α , and GSK-3β , respectively.
Storage
Store at -20°C
Verschickt in
Ice chest + Ice pads
Dieses Produkt erfordert Kühlkettenversand. Grundversand und andere Economy-Optionen sind nicht verfügbar.
Aktionsart
INHIBITOR
Reinheit
≥95%
Namen und Kennungen
Kanonisches Lächeln
COC(=N)C1=NC2=C(S1)C3=C(C=C2)N=CN=C3NC4=C(C=C(C=C4)Cl)Cl
IUPAC Name
methyl 9-(2,4-dichloroanilino)-[1,3]thiazolo[5,4-f]quinazoline-2-carboximidate
InChIKey
QSGKPYRFWJINEH-UHFFFAOYSA-N
INCHI
1S/C17H11Cl2N5OS/c1-25-15(20)17-24-12-5-4-11-13(14(12)26-17)16(22-7-21-11)23-10-3-2-8(18)6-9(10)19/h2-7,20H,1H3,(H,21,22,23)
Isomere SMILES
COC(=N)C1=NC2=C(S1)C3=C(C=C2)N=CN=C3NC4=C(C=C(C=C4)Cl)Cl
PubChem CID
71529610
Molekulargewicht
404.27

Dokumentation

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Erweiterte Daten

Taxonomic Classification

Taxonomy Tree

KingdomOrganic compounds
SuperclassOrganoheterocyclic compounds
KlasseDiazanaphthalenes
SubclassBenzodiazines
Intermediate Tree Nodes Quinazolines
Direct ParentQuinazolinamines
Alternative Parents Benzothiazoles  Dichlorobenzenes  Aniline and substituted anilines  Aminopyrimidines and derivatives  Imidolactams  Aryl chlorides  Thiazoles  Heteroaromatic compounds  Carboximidic acids and derivatives  Azacyclic compounds  Organooxygen compounds  Organochlorides  Hydrocarbon derivatives  Amines  
Molecular FrameworkAromatic heteropolycyclic compounds
Substituents Quinazolinamine - 1,3-benzothiazole - 1,3-dichlorobenzene - Aniline or substituted anilines - Aminopyrimidine - Chlorobenzene - Halobenzene - Aryl chloride - Aryl halide - Monocyclic benzene moiety - Pyrimidine - Imidolactam - Benzenoid - Heteroaromatic compound - Thiazole - Azole - Azacycle - Carboximidic acid derivative - Organochloride - Organohalogen compound - Hydrocarbon derivative - Organic oxygen compound - Organonitrogen compound - Organooxygen compound - Amine - Organic nitrogen compound - Aromatic heteropolycyclic compound
BeschreibungThis compound belongs to the class of organic compounds known as quinazolinamines. These are heterocyclic aromatic compounds containing a quianazoline moiety substituted by one or more amine groups.
External Descriptors Not available
3D-Struktur
Interaktives chemisches Strukturmodell





Zugehörige Ziele (menschlich)
DYRK1B Tchem Dual specificity tyrosine-phosphorylation-regulated kinase 1B (4 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
DYRK2 Tchem Dual specificity tyrosine-phosphorylation-regulated kinase 2 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
DYRK1A Tchem Dual specificity tyrosine-phosphorylation-regulated kinase 1A (4 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
CLK1 Tchem Dual specificity protein kinase CLK1 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
GSK3A Tclin Glycogen synthase kinase-3 alpha (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
GSK3B Tclin Glycogen synthase kinase-3 beta (11785 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
GSK3A Tclin Glycogen synthase kinase-3 alpha (3764 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CDK2 Tchem Cyclin-dependent kinase 2 (9050 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CDK1 Tchem Cyclin-dependent kinase 1 (3927 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
DYRK1A Tchem Dual-specificity tyrosine-phosphorylation regulated kinase 1A (6484 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CDK3 Tchem Cyclin-dependent kinase 3 (565 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CLK1 Tchem Dual specificty protein kinase CLK1 (2189 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CLK2 Tchem Dual specificity protein kinase CLK2 (3942 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CLK3 Tchem Dual specificity protein kinase CLK3 (2711 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CLK4 Tchem Dual specificity protein kinase CLK4 (4053 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
DYRK2 Tchem Dual-specificity tyrosine-phosphorylation regulated kinase 2 (2095 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
DYRK3 Tchem Dual-specificity tyrosine-phosphorylation regulated kinase 3 (1018 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
DYRK1B Tchem Dual specificity tyrosine-phosphorylation-regulated kinase 1B (2654 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Zugehörige Ziele (nicht menschlich)
Cdk4 Cyclin-dependent kinase 4 (3 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Wirkungsmechanismen
Zertifikate (CoA, COO, BSE/TSE und Analyse-Diagramm)
C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:
Chemische und physikalische Eigenschaften
LöslichkeitDMSO : 6.67 mg/mL (16.50 mM; ultrasonic and warming and heat to 60°C)
Lösungsrechner
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