GSK2643943A |
Catalog No.GC34354
One-Click Copy Product Info
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GSK2643943A는 USP20을 표적으로 하는 유비퀴틴화효소(DUB) 억제제이다. GSK2643943A는 USP20/Ub-Rho에 대해 160nM의 IC50과 친화력이 있습니다. GSK2643943A는 항종양 효능이 있어 구강 편평 세포 암종(OSCC) 연구에 사용할 수 있습니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2449301-27-1
Sample solution is provided at 25 µL, 10mM.
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GSK2643943A is a deubiquitinase (DUB) inhibitor targeting USP20. GSK2643943A blocks the cleavage of protein-ubiquitin bonds by inhibiting USP20/Ub-Rho (IC50=160nM)[1-2]. GSK2643943A can be used in research related to cancers such as oral squamous cell carcinoma (OSCC) and T-cell acute lymphoblastic leukemia (T-ALL)[3-4].
In vitro, A549 and NCI-H460 cells were treated with GSK2643943A (160nM) for 24-72 hours. GSK2643943A reduced cytoplasmic PTEN protein levels and increased PTEN ubiquitination. When co-treated with pcDNA3.1-OTUD5, GSK2643943A reversed the inhibitory effects of OTUD5 overexpression on cell proliferation, migration, and invasion[5]. HEK293FT cells were incubated with GSK2643943A (1-5μM) for 12 hours. GSK2643943A led to elevated levels of ubiquitination of the endoplasmic reticulum autophagy receptor RETREG1[6].
In vivo, GSK2643943A (15mg/kg) was administered via intraperitoneal injection once daily for a total of 10 times (5 consecutive days, followed by a 2-day interval, then another 5 consecutive days) to NSG mice inoculated with T-ALL cells. GSK2643943A significantly prolonged the survival of the mice[7]. GSK2643943A (5mg/kg or 2.5mg/kg) was administered via intraperitoneal injection once daily for 6 or 9 consecutive days to mice bearing SCC9 or SCC7 tumors. The combination treatment of GSK2643943A and the oncolytic virus T1012G significantly inhibited tumor growth in mice[8].
References:
[1] Qin B, Zhou L, Wang F, et al. Ubiquitin-specific protease 20 in human disease: Emerging role and therapeutic implications. Biochem Pharmacol. 2022 Dec;206:115352.
[2] Jiang X, Zhao B, Wang T, et al. USP20-Driven Cholesterol Metabolism Links Inflammatory Signaling to Malignancy and Stromal Coevolution in Pancreatic Cancer. Cancer Res. 2026 Feb 2;86(3):712-729.
[3] Li WT, Jin X, Song SJ, et al. Blocking SLC7A11 attenuates the proliferation of esophageal squamous cell carcinoma cells. Anim Cells Syst (Seoul). 2024 May 11;28(1):237-250.
[4] Böhm K, Schulze-Niemand E, Kähne T, et al. Synthesis and structure-activity relationships of USP48 deubiquitinylase inhibitors. Arch Pharm (Weinheim). 2023 Jul;356(7):e2200661.
[5] Li X, Lu B, Zhang L, et al. Mechanism of OTUD5 in non-small cell lung cancer cell proliferation, invasion, and migration. Bosn J Basic Med Sci. 2022 Oct 23;22(6):901-911.
[6] Zhang M, Wang Z, Zhao Q, et al. USP20 deubiquitinates and stabilizes the reticulophagy receptor RETREG1/FAM134B to drive reticulophagy. Autophagy. 2024 Aug;20(8):1780-1797.
[7] Xu L, Zhang Z, Yu J, et al. USP20 as a super-enhancer-regulated gene drives T-ALL progression via HIF1A deubiquitination. Acta Pharm Sin B. 2025 Sep;15(9):4751-4771.
[8] Lu R, Wu G, Chen M, et al. USP18 and USP20 restrict oHSV-1 replication in resistant human oral squamous carcinoma cell line SCC9 and affect the viability of SCC9 cells. Mol Ther Oncolytics. 2021 Nov 11;23:477-487.
| Cell experiment [1]: | |
Cell lines | Human Embryonic Kidney 293 cells stably expressing the SV40 large T antigen (HEK293FT) |
Preparation Method | HEK293FT culture methods within the document indicate cells were maintained in DMEM supplemented with 10% fetal bovine serum at 37°C under 5% CO₂. The cells were treated with GSK2643943A (1-5μM) for 12h. |
Reaction Conditions | 1-5μM; 12h. |
Applications | Treatment with GSK2643943A elevated levels of RETREG1 ubiquitination compared to the control. |
| Animal experiment [2]: | |
Animal models | NSG mice (NOD scid gamma mice) |
Preparation Method | NSG mice were injected via the tail vein with J.gamma1 T-ALL cells expressing firefly luciferase. The experimental group then received intraperitoneal injections of GSK2643943A (15mg/kg). |
Dosage form | 15mg/kg; i.p.; once daily for 10 times (After continuous injection for 5 days, continue injection for another 5 days after a 2-day interval). |
Applications | Treatment with GSK2643943A significantly prolonged survival and significantly reduced the bioluminescence signal (indicating inhibition of tumor growth) in the T-ALL mouse model. |
References: | |
| Cas No. | 2449301-27-1 | SDF | |
| Canonical SMILES | FC1=CC=CC(/C=C/C2=CC(NC(N)=C3C#N)=C3C=C2)=C1 | ||
| Formula | C17H12FN3 | M.Wt | 277.3 |
| Solubility | DMSO : ≥ 125 mg/mL (450.78 mM);Water : < 0.1 mg/mL (insoluble) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.6062 mL | 18.031 mL | 36.062 mL |
| 5 mM | 721.2 μL | 3.6062 mL | 7.2124 mL |
| 10 mM | 360.6 μL | 1.8031 mL | 3.6062 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 31 reference(s) in Google Scholar.)