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GS-9191

Catalog No. T25466 CAS 859209-84-0

Synonyms: GS 9191

GS-9191 is a potent inhibitor of DNA polymerase alpha and ß , a prodrug of the novel nucleoside analogue 9-(2-phosphonomethoxyethyl)guanine (PMEG) , which penetrates the skin and is metabolized in the epithelium to an active nucleoside triphosphate analogue.GS-9191 has antiproliferative activity and reduces the size of papillomas in a dose-related manner.GS-9191 may be useful in the treatment of HPV-induced lesions.

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GS-9191, CAS 859209-84-0

Pack Size	Availability	Price/USD
1 mg	In stock	$ 180.00
5 mg	In stock	$ 450.00
10 mg	In stock	$ 663.00
25 mg	In stock	$ 987.00
50 mg	In stock	$ 1,390.00
100 mg	In stock	$ 1,880.00
500 mg	In stock	$ 3,790.00
1 mL * 10 mM (in DMSO)	In stock	$ 653.00

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Purity: 98.28%

Purity: 98.01%

ee: 98.32%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	GS-9191 is a potent inhibitor of DNA polymerase alpha and ß , a prodrug of the novel nucleoside analogue 9-(2-phosphonomethoxyethyl)guanine (PMEG) , which penetrates the skin and is metabolized in the epithelium to an active nucleoside triphosphate analogue.GS-9191 has antiproliferative activity and reduces the size of papillomas in a dose-related manner.GS-9191 may be useful in the treatment of HPV-induced lesions.
Targets&IC50	HPV-positive cell lines:0.03 nM(EC50), Non-HPV-infected cells:1-15 nM(EC50)
In vitro	GS-9191 was markedly more potent than PMEG or cPrPMEDAP in a series of human papillomavirus (HPV)-positive cell lines, with effective concentrations to inhibit 50% cell growth (EC(50)) as low as 0.03, 207, and 284 nM, respectively. In contrast, GS-9191 was generally less potent in non-HPV-infected cells and primary cells (EC(50)s between 1 and 15 nM). DNA synthesis was inhibited by GS-9191 within 24 h of treatment; cells were observed to be arrested in S phase by 48 h and to subsequently undergo apoptosis (between 3 and 7 days).[2] In an animal model (cottontail rabbit papillomavirus), topical GS-9191 was shown to decrease the size of papillomas in a dose-related manner. At the highest dose (0.1%), cures were evident at the end of 5 weeks, and lesions did not recur in a 30-day follow-up period. These data suggest that GS-9191 may have utility in the treatment of HPV-induced lesions.[2]

Synonyms	GS 9191
Molecular Weight	734.82
Formula	C37H51N8O6P
CAS No.	859209-84-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 7.35 mg/mL (10 mM)

References and Literature

1. Birkus G, et al. Role of cathepsin A and lysosomes in the intracellular activation of novel antipapillomavirus agent GS-919Antimicrob Agents Chemother. 2011;55(5):2166-73. 2. Wolfgang GH, et al. GS-9191 is a novel topical prodrug of the nucleotide analog 9-(2-phosphonylmethoxyethyl)guanine with antiproliferative activity and possible utility in the treatment of human papillomavirus lesions. Antimicrob Agents Chemother. 2009;53(7):2777-2784. 3. De Clercq E. Dancing with chemical formulae of antivirals: a personal account. Biochem Pharmacol. 2013;86(6):711-725. 4. Rai MA, et al. Emerging reverse transcriptase inhibitors for HIV-1 infection. Expert Opin Emerg Drugs. 2018;23(2):149-157.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Drug Repurposing Compound Library Inhibitor Library Anti-Cancer Compound Library Clinical Compound Library DNA Damage & Repair Compound Library Bioactive Compounds Library Max Bioactive Compound Library

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Keywords

GS-9191 859209-84-0 Cell Cycle/Checkpoint DNA Damage/DNA Repair DNA/RNA Synthesis GS 9191 GS9191 inhibitor inhibit

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