GSK2643943A
Based on 8 publication(s) in Google Scholar
GSK2643943A is a deubiquitinating enzyme (DUB) inhibitor targeting USP20. GSK2643943A has affinity with an IC50 of 160 nM for USP20/Ub-Rho. GSK2643943A has anti-tumor efficacy and can be used for the research of oral squamous cell carcinoma (OSCC) .
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity: 98.79%
- CAS No.: 2449301-27-1
- 화학식: C17H12FN3
- 분자량:277.30
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) GSK2643943A
More- Cancer Res. 2025 Nov 6. [Abstract]
- Autophagy. 2024 Aug;20(8):1780-1797. [Abstract]
- Genes Dis. 2026 Jul 13.
- Int J Biol Macromol. 2026 Jun 23:153185. [Abstract]
- Mol Ther Oncolytics. 2021 Nov 11:23:477-487. [Abstract]
- Anim Cells Syst. 2024 May 11;28(1):237-250. [Abstract]
- Arch Pharm (Weinheim). 2023 Jul;356(7):e2200661. [Abstract]
- bioRxiv. 2023 Jul 28.
Biological Activity
제품 설명
IC50 & Target
IC50: 160 nM (USP20/Ub-Rho)[1]
In Vitro
GSK2643943A blocks the USP20-mediated cleavage of protein-ubiquitin bonds[2].
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GSK2643943A (1 μM, 5 μM; overnight) renders SCC9 cells more susceptible to oHSV-1 induced oncolysis[2].
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GSK2643943A (1μM) leds to a notable increase of virus yields in SCC9 with 0.01 MOI T1012G infection[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SCC9 cells
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Concentration:1 μM, 5 μM (GSK+0.01 MOI T1012)
1 μM (GSK+0.01 MOI/ 1 MOI T1012) -
Incubation Time:overnight
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Result:Displayed a significant drop in viability (R50%) (5 μM GSK+0.01 MOI T1012 infection) and 50% loss of SCC9 viability (1 μM GSK+0.01 MOI T1012 infection) .
Remarkably reduced the viability of SCC9 upon exposure to 1 MOI T1012G infection.
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Cell Line:SCC9 cells
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Concentration:1 μM
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Incubation Time:3h, 9 h and 20 h
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Result:Generally up-regulated the expression of viral proteins at various phases.
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Cell Line:SCC9 cells
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Concentration:1 μM
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Incubation Time:9 h
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Result:Significantly increased the accumulation of viral ICP8 and VP16 Mrna in SCC9 cells.
In Vivo
? GSK2643943A (2.5 mg/kg, i.p., daily, for 9 days) plays a regulatory role in oHSV-1 T1012G replication and oncolysis in SCC7 cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:
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Dosage:5 mg/kg
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Administration:GSK2643943A (alone): intraperitoneal administration, daily, for 6 days.
GSK2643943A (combination): intraperitoneal administration, daily for 6 days + intratumoral injection with 50 mL of 1×106 PFU T1012G in PBS on day 1, day 4, and day 7. -
Result:Caused a visible drop of tumor volumes and significantly reduced the tumor volumes in mice with combined treatment of GSK2643943A and oHSV-1 T1012G.
Increased slightly viral ICP0 and gD mRNA accumulation in SCC9 tumors.
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Animal Model:The SCC7 mouse model[2].
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Dosage:2.5 mg/kg
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Administration:GSK2643943A (alone): intraperitoneal administration, daily, for 9 days.
GSK2643943A (combination): intraperitoneal administration, daily, for 9 days + intratumoral injection, with 50 mL of 1×107 PFU T1012G in PBS on days 1, 4, 7, and 10. -
Result:Caused a visible drop of tumor volumes, significantly reduced in mice with combined treatment of GSK and oHSV-1 T1012G.
Increased slightly viral ICP0 and gD mRNA accumulation in SCC7 tumors.
Chemical Information
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CAS No. 2449301-27-1
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Appearance Solid
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분자량 277.30
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화학식 C17H12FN3
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Color Light yellow to yellow
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SMILES
FC1=CC=CC(/C=C/C2=CC(NC(N)=C3C#N)=C3C=C2)=C1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (8)
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Journal Impact Factor
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Most Recent
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Cancer Res
USP20-Driven Cholesterol Metabolism Links Inflammatory Signaling to Malignancy and Stromal Co-evolution in Pancreatic Cancer. [Abstract]2025 Nov 6. PMID: 41196022 -
Autophagy
USP20 deubiquitinates and stabilizes the reticulophagy receptor RETREG1/FAM134B to drive reticulophagy. [Abstract]2024 Aug;20(8):1780-1797. PMID: 38705724 -
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Int J Biol Macromol
Disruption of the autophagy-ferroptosis axis by ubiquitin-specific peptidase 20-mediated Sequestosome 1 stabilization drives lung adenocarcinoma progression. [Abstract]2026 Jun 23:153185. PMID: 42336010 -
Mol Ther Oncolytics
USP18 and USP20 restrict oHSV-1 replication in resistant human oral squamous carcinoma cell line SCC9 and affect the viability of SCC9 cells. [Abstract]2021 Nov 11:23:477-487. PMID: 34901390 -
Anim Cells Syst
Blocking SLC7A11 attenuates the proliferation of esophageal squamous cell carcinoma cells. [Abstract]2024 May 11;28(1):237-250. PMID: 38741950 -
Arch Pharm (Weinheim)
2023 Jul;356(7):e2200661. PMID: 37196427 -
용액&용해도
In Vitro:
DMSO : ≥ 125 mg/mL (450.78 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (7.50 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.08 mg/mL (7.50 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (279 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.6062 mL | 18.0310 mL | 36.0620 mL | 90.1551 mL |
| 5 mM | 0.7212 mL | 3.6062 mL | 7.2124 mL | 18.0310 mL | |
| 10 mM | 0.3606 mL | 1.8031 mL | 3.6062 mL | 9.0155 mL | |
| 15 mM | 0.2404 mL | 1.2021 mL | 2.4041 mL | 6.0103 mL | |
| 20 mM | 0.1803 mL | 0.9016 mL | 1.8031 mL | 4.5078 mL | |
| 25 mM | 0.1442 mL | 0.7212 mL | 1.4425 mL | 3.6062 mL | |
| 30 mM | 0.1202 mL | 0.6010 mL | 1.2021 mL | 3.0052 mL | |
| 40 mM | 0.0902 mL | 0.4508 mL | 0.9016 mL | 2.2539 mL | |
| 50 mM | 0.0721 mL | 0.3606 mL | 0.7212 mL | 1.8031 mL | |
| 60 mM | 0.0601 mL | 0.3005 mL | 0.6010 mL | 1.5026 mL | |
| 80 mM | 0.0451 mL | 0.2254 mL | 0.4508 mL | 1.1269 mL | |
| 100 mM | 0.0361 mL | 0.1803 mL | 0.3606 mL | 0.9016 mL |
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