BiS3
BiS3 is a selective hyperbivalent macrocyclic peptide GSK3β inhibitor, with a Kd 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.
For research use only. We do not sell to patients.
- Formula: C93H118N32O19S
- Molecular Weight:2020.20
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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GSK-3β 0.28 nM (Kd) |
GSK-3α 18.4 nM (IC50) |
GSK-3β 4.8 nM (IC50) |
BiS3 binds potently to purified GSK3β with a KD 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].
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
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Molecular Weight 2020.20
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Formula C93H118N32O19S
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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)
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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)
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
BiS3 Related Classifications
HY-P11927 Related Classifications
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