GO-203 hydrochloride
Based on 2 publication(s) in Google Scholar
GO-203 hydrochloride is a potent MUC1-C oncoprotein inhibitor. GO-203 hydrochloride is an all D-amino acid peptide that consists of a poly-R transduction domain linked to a CQCRRKN motif that binds to the MUC1-C cytoplasmic tail and blocks MUC1-C homodimerization. GO-203 hydrochloride downregulates TIGAR (TP53-induced glycolysis and apoptosis regulator) protein synthesis by inhibiting the PI3K-AKT-S6K1 pathway. GO-203 hydrochloride induces the production of ROS and loss of mitochondrial transmembrane potential. GO-203 hydrochloride inhibits the growth of colon cancer cells in vitro and as xenografts in nude mice.
For research use only. We do not sell to patients.
- Formula: C87H170N52O19S2·xHCl
- Molecular Weight:2312.75 (free base)
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications Citing Use of MedChemExpress (MCE) GO-203 hydrochloride
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Biological Activity
Description
IC50 & Target
[2]|
PI3K |
In Vitro
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SKCO-1 cells
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Concentration:5 μM
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Incubation Time:For three days
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Result:Inhibited MUC1 positive colorectal cancer cell proliferation.
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Cell Line:SKCO-1 cells
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Concentration:5 μM
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Incubation Time:For three days
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Result:Induced approximately 80% death and resulted in a significant decrease in mitochondrial membrane potential.
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Cell Line:SKCO-1 cells
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Concentration:5 μM
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Incubation Time:For three days
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Result:Inhibited the activation of S6K1 in SKCO-1 cells.
Inhibited the degradation of PDCD4.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Four- to 6-week-old BALB/c nu/nu male/female mice with Colo-205 or SKCO-1 cells[2]
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Dosage:18 mg/kg
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Administration:IP; daily; for 28 days
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Result:Significantly inhibited growth of the COLO-205 tumors.
These tumors regressed completely by the end of treatment (day 28) and there was no evidence for regrowth by day 180.
Chemical Information
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Molecular Weight 2312.75 (free base)
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Formula C87H170N52O19S2·xHCl
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SMILES
O=C(N[C@H](CCCNC(N)=N)C(N[C@H](CCCNC(N)=N)C(N[C@H](CCCNC(N)=N)C(N[C@H](CCCNC(N)=N)C(N[C@H](CCCNC(N)=N)C(N[C@H](CCCNC(N)=N)C(N[C@H](CCCNC(N)=N)C(N[C@H](CCCNC(N)=N)C(N[C@H](CS)C(N[C@H](CCC(N)=O)C(N[C@H](CS)C(N[C@H](CCCNC(N)=N)C(N[C@H](CCCNC(N)=N)C(N[C@H](CCCCN)C(N[C@H](CC(N)=O)C(O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)[C@@H](CCCNC(N)=N)N.[x].Cl
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Sequence
d-{Arg-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Cys-Gln-Cys-Arg-Arg-Lys-Asn}
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Sequence Shortening
d-{RRRRRRRRRCQCRRKN}
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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.
Publications (2)
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Journal Impact Factor
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Most Recent
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Respir Res
MUC1 attenuates neutrophilic airway inflammation in asthma by reducing NLRP3 inflammasome-mediated pyroptosis through the inhibition of the TLR4/MyD88/NF-κB pathway. [Abstract]2023 Oct 25;24(1):255. PMID: 37880668 -
J Inflamm Res
Mesenchymal Stem Cells Ameliorate DSS-Induced Experimental Colitis by Modulating the Gut Microbiota and MUC-1 Pathway. [Abstract]2023 May 11:16:2023-2039. PMID: 37197438
Purity & Documentation
References
[1]. Masanori Hasegawa, et al. Intracellular Targeting of the Oncogenic MUC1-C Protein with a Novel GO-203 Nanoparticle Formulation. Clin Cancer Res. 2015 May 15;21(10):2338-47. [Content Brief]
[2]. Rehan Ahmad, et al. Targeting MUC1-C inhibits the AKT-S6K1-elF4A pathway regulating TIGAR translation in colorectal cancer. Mol Cancer. 2017 Feb 2;16(1):33. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)