Gallocyanine
Gallocyanine (NCI8642) is a DKK/LRP interaction inhibitor and Wnt/β-catenin signaling pathway activator. Gallocyanine binds to the YWTD repeat domains of LRP5/6, competitively blocks the interaction between DKK and LRP5/6, with an IC50 of approximately 3 μM for inhibiting DKK1 binding to LRP5, an IC50 of 6.38 μM for inhibiting DKK1 binding to LRP6, and a Ki of 14 μM for inhibiting the DKK2C/LRP6-E3E4 interaction. Gallocyanine reverses the inhibitory effect of DKK1 on WNT3A signaling, with an EC50 of approximately 5 μM. Gallocyanine can be used in studies related to Alzheimer's disease, bone formation and glucose metabolism.
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- CAS No.: 524-26-5
- Formule: C15H12N2O5
- Masse moléculaire:300.27
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
[1]|
LPR6 14 μM (Ki) |
In Vitro
Gallocyanine (NCI8642) (1-10 μM) potently reverses DKK1-mediated inhibition of WNT3A-stimulated reporter gene activity in NIH 3T3 cells with an EC50 of ~5 μM[1].
Gallocyanine (0.1-100 μM) inhibits DKK1-AP binding to wild-type LRP5-expressing HEK293 cells with an IC50 of about 3 μM, without affecting binding to Kremen1-expressing cells[1].
Gallocyanine inhibits the binding of DKK2C to recombinant LRP6-E3E4 with an inhibition constant of 14 μM[1].
Gallocyanine (100 μM; 2 h) inhibits DKK1 binding to LRP6 in HEK-293LRP6 cells with an IC50 of 6.38 μM, reducing DKK1 binding to 47.8% at 100 μM[2].
Gallocyanine (10-100 μM; 24 h) is not cytotoxic to SH-SY5Y cells at concentrations up to 100 μM after 24 hours of incubation[2].
Gallocyanine (10 μM; 1 h) inhibits PGJ2-induced Tau phosphorylation at serine 396 in mouse primary cortical neurons, reducing phosphorylation levels to 55% at 10 μM[2].
Gallocyanine (0.1-10 μM; 1 h) dose-dependently inhibits DKK1-induced Tau phosphorylation at serine 396 in SH-SY5Y cells[2].
Gallocyanine (0.1-10 μM; 1 h) dose-dependently activates Wnt/β-catenin signaling in SH-SY5Y cells by increasing pGSK3β and β-catenin levels[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:SH-SY5Y
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Concentration:0.1-10 μM
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Incubation Time:1 h
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Result:Dose-dependently decreased DKK1-induced Tau phosphorylation at serine 396 relative to cells treated with DKK1 alone.\nDose-dependently increased levels of pGSK3β and β-catenin relative to cells treated with DKK1 alone.
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Cell Line:SH-SY5Y
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Concentration:10-100 μM
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Incubation Time:24 h
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Result:Exhibited no detectable toxic effects on SH-SY5Y cells at concentrations up to 100 μM.
In Vivo
Gallocyanine (IIIC3; 3.5 or 7.0 mg/kg/day; intraperitoneal injection) exerts no obvious overall effect on whole-body bone mineral density (BMD) in mice, but the BMD of the 3.5 mg/kg/day group increases by approximately 3% at the end of the experiment[1].
Gallocyanine (IIIC3; i.p.) reduces blood glucose levels during routine toxicity monitoring in mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CD-1 (6 weeks old)[1]
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Dosage:3.5 mg/kg/d; 7.0 mg/kg/d
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Administration:s.c.; three times daily; 5 days; i.p.; daily
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Result:Did not meaningfully alter whole-body BMD; 3.5 mg/kg/day increased BMD by approximately 3% at endpoint.
Chemical Information
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CAS No. 524-26-5
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Masse moléculaire 300.27
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Formule C15H12N2O5
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SMILES
O=C(C1=CC(C(O)=C2OC3=C(N=C21)C=CC(N(C)C)=C3)=O)O
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Synonyms
NCI8642
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
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Alzheimer’s Disease Modeling
Alzheimer’s Disease (AD) is a neurodegenerative disorder characterized by a progressive decline in cognitive functions and loss of specific types of neurons and synapses. Alzheimer's symptoms can be simulated in mice by injecting drugs (such as Aβ) or genetically modified.
Pureté et documentation
Références
[1]. Li X, et al. Chemical and genetic evidence for the involvement of Wnt antagonist Dickkopf2 in regulation of glucose metabolism. Proceedings of the National Academy of Sciences of the United States of America. 2012 Jul 10;109(28):11402-7. [Content Brief]
[2]. Thysiadis S, et al. Design and Synthesis of Gallocyanine Inhibitors of DKK1/LRP6 Interactions for Treatment of Alzheimer's Disease. Bioorganic Chemistry. 2018 [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Gallocyanine Related Classifications
HY-124841 Related Classifications
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