GSK2643943A

SKU: orb2901823

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) .

Key Properties

• CAS Number: 2449301-27-1
• MW: 277.3
• Purity: >98% (HPLC)
• Formula: C₁₇H₁₂FN₃
• SMILES: Nc1[nH]c2cc(\C=C\c3cccc(F)c3)ccc2c1C#N
• Target: DUB
• Solubility: In Vitro: DMSO : ≥ 125 mg/mL (450.78 mM )

Bioactivity

• In Vivo:
  Animal model: The subcutaneous xenograft model. (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). 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 1×106PFU 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. 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 1×107PFU 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.
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• In Vitro:
  Cell Viability Assay 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. 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 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.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

DUB