2. PI3K/Akt/mTOR NF-κB Metabolic Enzyme/Protease Immunology/Inflammation Apoptosis
  3. PI3K Reactive Oxygen Species Apoptosis
  4. GO-203 TFA

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.

For research use only. We do not sell to patients.

Custom Peptide Synthesis

GO-203 TFA Chemical Structure

GO-203 TFA Chemical Structure

CAS No. : 1222186-26-6

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5 mg USD 240 In-stock
10 mg USD 380 In-stock
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Based on 2 publication(s) in Google Scholar

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GO-203 TFA Related Antibodies

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Description

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[1][2].

IC50 & Target[2]

PI3K

 

In Vitro

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.

GO-203 TFA Related Antibodies

Cell Proliferation Assay[2]

Cell Line: SKCO-1 cells
Concentration: 5 μM
Incubation Time: For three days
Result: Inhibited MUC1 positive colorectal cancer cell proliferation.

Apoptosis Analysis[2]

Cell Line: SKCO-1 cells
Concentration: 5 μM
Incubation Time: For three days
Result: Induced approximately 80% death and resulted in a significant decrease in mitochondrial membrane potential.

Western Blot Analysis[2]

Cell Line: SKCO-1 cells
Concentration: 5 μM
Incubation Time: For three days
Result: Inhibited the activation of S6K1 in SKCO-1 cells.
Inhibited the degradation of PDCD4.
In Vivo

GO-203 (18 mg/kg/day; IP; for 28 days) TFA significantly inhibits growth of the COLO-205 tumors[2].

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

Animal Model: Four- to 6-week-old BALB/c nu/nu male/female mice with Colo-205 or SKCO-1 cells[2]
Dosage: 18 mg/kg
Administration: IP; daily; for 28 days
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.
Molecular Weight

2426.77

Formula

C89H171F3N52O21S2
CAS No.
Appearance

Solid

Color

White to off-white

Sequence

d-{Arg-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Cys-Gln-Cys-Arg-Arg-Lys-Asn} (TFA salt)
Sequence Shortening

d-{Arg-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Cys-Gln-Cys-Arg-Arg-Lys-Asn} (TFA salt)
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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)

Solvent & Solubility
In Vitro: 

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)

H2O : 100 mg/mL (41.21 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.4121 mL 2.0604 mL 4.1207 mL
5 mM 0.0824 mL 0.4121 mL 0.8241 mL
View the 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.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation
References

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 / H2O 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

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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GO-203 TFA Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GO-2031222186-26-6GO203GO 203PI3KReactive Oxygen SpeciesApoptosisPhosphoinositide 3-kinaseMUC1-CCQCRRKNhomodimerizationTIGARS6K1mitochondrial transmembrane potentialcolon cancerSKCO-1Inhibitorinhibitorinhibit

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