GO-203 TFA
Based on 2 publication(s) in Google Scholar
GO-203 TFA is a potent MUC1-C oncoprotein inhibitor. GO-203 TFA 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 TFA downregulates TIGAR (TP53-induced glycolysis and apoptosis regulator) protein synthesis by inhibiting the PI3K-AKT-S6K1 pathway. GO-203 TFA induces the production of ROS and loss of mitochondrial transmembrane potential. GO-203 TFA inhibits the growth of colon cancer cells in vitro and as xenografts in nude mice.
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- Purity: 98.39%
- CAS No.: 1222186-26-6
- 화학식: C89H171F3N52O21S2
- 분자량:2426.77
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보관:
Sealed storage, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) GO-203 TFA
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Biological Activity
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PI3K |
GO-203 (5 μM; for three days) TFA inhibits MUC1 positive colorectal cancer cell proliferation by decreasing intracellular GSH levels and enhanced ROS production. GO-203 TFA has no effect on cell growth on MUC1-negative SW480 and LOVO cells[2].
GO-203 (5 μM; for three days) TFA induces approximately 80% death of SKCO-1 cells. GO-203 TFA results in a significant decrease in mitochondrial membrane potential[2].
GO-203 (5 μM; for three days) TFA inhibits AKT-mTORC-S6K1 translation pathway in colorectal cancer cells[2].
GO-203 (5 μM; for three days) TFA significantly decreases GSH levels in SKCO-1 cells[2].
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.
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.
d-{Arg-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Cys-Gln-Cys-Arg-Arg-Lys-Asn} (TFA salt)
d-{RRRRRRRRRCQCRRKN} (TFA salt)
Chemical Information
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CAS No. 1222186-26-6
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Appearance Solid
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분자량 2426.77
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화학식 C89H171F3N52O21S2
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Color White to off-white
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Sealed storage, away from moisture
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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
용액&용해도
DMSO : 100 mg/mL (41.21 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
순도&문서
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Data Sheet (284 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
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]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 0.4121 mL | 2.0604 mL | 4.1207 mL | 10.3018 mL |
| 5 mM | 0.0824 mL | 0.4121 mL | 0.8241 mL | 2.0604 mL | |
| 10 mM | 0.0412 mL | 0.2060 mL | 0.4121 mL | 1.0302 mL | |
| 15 mM | 0.0275 mL | 0.1374 mL | 0.2747 mL | 0.6868 mL | |
| 20 mM | 0.0206 mL | 0.1030 mL | 0.2060 mL | 0.5151 mL | |
| 25 mM | 0.0165 mL | 0.0824 mL | 0.1648 mL | 0.4121 mL | |
| 30 mM | 0.0137 mL | 0.0687 mL | 0.1374 mL | 0.3434 mL | |
| 40 mM | 0.0103 mL | 0.0515 mL | 0.1030 mL | 0.2575 mL |
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