| Identification | Back Directory | [Name]
1H-Indole-3-carbonitrile, 2-amino-6-[2-(3-fluorophenyl)ethenyl]- | [CAS]
2449301-27-1 | [Synonyms]
1H-Indole-3-carbonitrile, 2-amino-6-[2-(3-fluorophenyl)ethenyl]- | [Molecular Formula]
C17H12FN3 | [MOL File]
2449301-27-1.mol | [Molecular Weight]
277.3 |
| Chemical Properties | Back Directory | [Boiling point ]
540.4±50.0 °C(Predicted) | [density ]
1.33±0.1 g/cm3(Predicted) | [solubility ]
DMSO:90.0(Max Conc. mg/mL);324.56(Max Conc. mM)
Ethanol:8.0(Max Conc. mg/mL);28.85(Max Conc. mM) | [form ]
Solid | [pka]
16.49±0.30(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
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]. | [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]. | 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.
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| 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.
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| [References]
[1] Nishi Kumari, et al. Targeting the Ubiquitin Proteasome System in Cancer. Shahzad, Hafiz Naveed (2018). Neoplasm Targeting the Ubiquitin Proteasome System in Cancer. , 10.5772/intechopen.69560(Chapter 8).
[2] Ruitao Lu, 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. DOI:10.1016/j.omto.2021.11.004 |
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