GS-9191

SKU: orb1702225

Description

GS-9191 is a prodrug of the nucleoside analog PMEG, which acts as a potent inhibitor of DNA polymerases alpha and beta. Its active triphosphate form exhibits antiproliferative effects, demonstrating dose-dependent reduction of papilloma size in vivo, supporting its research application for HPV-related lesion studies.

Research Area

Cell Biology, Infectious Disease & Virology, Molecular Biology

Key Properties

• CAS Number: 859209-84-0
• MW: 734.82
• Purity: 98.28% (May vary between batches)
• Formula: C₃₇H₅₁N₈O₆P
• SMILES: C(COCP(N[C@@H](CC1=CC=CC=C1)C(OCC(C)C)=O)(N[C@@H](CC2=CC=CC=C2)C(OCC(C)C)=O)=O)N3C=4C(=C(NC5CC5)N=C(N)N4)N=C3
• Target: DNA/RNA Synthesis
• Solubility: DMSO:7.35 mg/mL (10 mM)

Bioactivity

• Target IC50:
  HPV-positive cells: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). 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.
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Storage & Handling

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

Alternative Names

DNASynthesis, DNA Synthesis, DNA polymerase beta, DNA polymerase α, GS9191, GS-9191, GS 9191, RNA Synthesis, RNASynthesis

Compound Identifiers

PubChem CID

44181731