2. Cell Cycle/DNA Damage
  3. Deubiquitinase
  4. GSK2643943A

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) .

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

GSK2643943A Chemical Structure

GSK2643943A Chemical Structure

CAS No. : 2449301-27-1

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 121 In-stock
Solution
10 mM * 1 mL in DMSO USD 121 In-stock
Solid
5 mg USD 110 In-stock
10 mg USD 182 In-stock
25 mg USD 385 In-stock
50 mg USD 605 In-stock
100 mg USD 1045 In-stock
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Based on 5 publication(s) in Google Scholar

GSK2643943A Related Antibodies

Top Publications Citing Use of Products

View All Deubiquitinase Isoform Specific Products:

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USP1 USP2 USP7 USP8 USP30 UCHL1

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  • Purity & Documentation

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Description

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) [1][2].

IC50 & Target

IC50: 160 nM (USP20/Ub-Rho)[1]
In Vitro

GSK2643943A blocks the USP20-mediated cleavage of protein-ubiquitin bonds[2].
GSK2643943A (1 μM, 5 μM; overnight) renders SCC9 cells more susceptible to oHSV-1 induced oncolysis[2].
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.

GSK2643943A Related Antibodies

Cell Viability Assay[2]

Cell Line: SCC9 cells
Concentration: 1 μM, 5 μM (GSK+0.01 MOI T1012)
1 μM (GSK+0.01 MOI/ 1 MOI T1012)
Incubation Time: overnight
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.

Western Blot Analysis[2]

Cell Line: SCC9 cells
Concentration: 1 μM
Incubation Time: 3h, 9 h and 20 h
Result: Generally up-regulated the expression of viral proteins at various phases.

RT-PCR[2]

Cell Line: SCC9 cells
Concentration: 1 μM
Incubation Time: 9 h
Result: Significantly increased the accumulation of viral ICP8 and VP16 Mrna in SCC9 cells.
In Vivo

GSK2643943A (5 mg/kg, i.p., daily, for 6 days) potentiates oHSV-1-induced oncolysis in SCC9 tumors[2].
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.

Animal Model: The subcutaneous xenograft model[2].
(SCC9 or SCC7 cells (8×106 cells or 1×106 cells), 5-week-old, female, BALB/c nude mice or C3H/HeN mice, four groups, n = 6-7, per group)[2]
Dosage: 5 mg/kg
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.
Animal Model: The SCC7 mouse model[2].
Dosage: 2.5 mg/kg
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.
Molecular Weight

277.30

Formula

C17H12FN3
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

FC1=CC=CC(/C=C/C2=CC(NC(N)=C3C#N)=C3C=C2)=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
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.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.6062 mL 18.0310 mL 36.0620 mL
5 mM 0.7212 mL 3.6062 mL 7.2124 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, 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.

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

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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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C2

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Volume (final)

V2

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.

  • Protocol 1

    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.
  • Protocol 2

    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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mg/kg

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(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
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).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
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, 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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GSK2643943A 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:

GSK2643943A2449301-27-1DeubiquitinaseDUBsdeubiquitinating enzyme (DUB)USP20USP18USP20/Ub-RhoSCC9 cellsSCC7 cellsSTINGT1012Gvirusoral squamous cell carcinoma (OSCC)anti-tumorcancerInhibitorinhibitorinhibit

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