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

GSK2643943A 

Cat. No.: HY-111458 Purity: 98.28%
COA Handling Instructions

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

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 121 In-stock
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10 mM * 1 mL in DMSO USD 121 In-stock
Solid
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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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Customer Review

Based on 3 publication(s) in Google Scholar

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  • Biological Activity

  • 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.

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

Appearance

Solid

Formula

C17H12FN3

CAS No.
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)

*"≥" 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
10 mM 0.3606 mL 1.8031 mL 3.6062 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

*All of the co-solvents are available by MedChemExpress (MCE).
Purity & Documentation
References
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GSK2643943A Related Classifications

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  • 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.

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Product Name:
GSK2643943A
Cat. No.:
HY-111458
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