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Art. -Nr.: HY-P11927

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BiS3

BiS3 is a selective hyperbivalent macrocyclic peptide GSK3β inhibitor, with a K_d of 0.28 nM and an IC₅₀ of 4.8 nM against GSK3β. BiS3 is applicable to studies related to GSK3β signaling and colorectal cancer.

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Formel: C₉₃H₁₁₈N₃₂O₁₉S
Molecular Weight:2020.20

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Kundenspezifische Peptidsynthese

BiS3 Chemical Structure

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
Chemical Information
Reinheit & Dokumentation
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Calculators
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Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]

GSK-3β

0.28 nM (Kd)

GSK-3α

18.4 nM (IC₅₀)

GSK-3β

4.8 nM (IC₅₀)

Alle GSK-3 Isoform-spezifische Produkte anzeigen :

In Vitro

OthersAnti-cancer

Others

BiS3 binds potently to purified GSK3β with a K_D value of 0.28 nM^[1].
BiS3 potently inhibits the kinase activity of GSK3β with an IC₅₀ of 4.8 nM, and exhibits approximately 3.9-fold selectivity over GSK3α^[1].
BiS3 (50 nM-1 μM) exhibits much higher selectivity for GSK3β than for the 7 tested CMGC family kinases. Even at 1 μM, a concentration 200-fold higher than its IC₅₀ against GSK3β, it does not exert significant inhibitory effects on most homologous kinases^[1].
The BiS3 Z5 and Z7 residues are essential for GSK3β inhibitory activity (potency decreases by >100-fold when mutated to phenylalanine), whereas the Z12 residue is not required for potent inhibition^[1].

Anti-cancer

Treatment with unconjugated BiS3 for 72 h has no effect on the viability of HCT116 colorectal cancer cells, which may be attributed to its poor cell permeability^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

Molecular Weight 2020.20
Formel C₉₃H₁₁₈N₃₂O₁₉S
Sequence

Cyclo({CH3-CO}-{d-Tyr}-Arg-Gly-Ser-{Phe(4-(pyrimidin-2-ylamino))}-Arg-{Phe(4-(pyrimidin-2-ylamino))}-Phe-Glu-Ser-Arg-{Phe(4-(pyrimidin-2-ylamino))}-Cys-NH2) (Thioether bond:Tyr1-Cys13)
Sequence Shortening

Cyclo({CH3-CO}-{d-Tyr}-RGS-{Phe(4-(pyrimidin-2-ylamino))}-R-{Phe(4-(pyrimidin-2-ylamino))}-FESR-{Phe(4-(pyrimidin-2-ylamino))}-C-NH2) (Thioether bond:Tyr1-Cys13)
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Haslböck S, et al. Discovery of Supra-Bivalent GSK3β Inhibitory Peptides Containing an ATP-Mimetic Amino Acid. Journal of the American Chemical Society. 2026 Jan 14;148(1):368-378.

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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MOQ

Minimum order quantity

100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
Chemical Information
Reinheit & Dokumentation
Verweise

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BiS3

Alle GSK-3 Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Beschreibung

IC50 & Target

In Vitro

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

BiS3 Related Classifications

HY-P11927 Related Classifications

Bioz

Keywords

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