| Name | FIT-039 |
| Description | FIT-039 is a selective and ATP-competitive, orally active inhibitor of CDK9( IC50 : 5.8 μM;CDK9/cyclin T1). FIT-039 inhibits replication of HSV-1 (IC50 of 0.69 μM), HSV-2, human adenovirus, and human CMV. FIT-039 is a promising antiviral agent for inhibiting drug-resistant HSVs and other DNA viruses. |
| Cell Research | Examined FIT-039 for its effect on HPV gene expression in HPV+ cervical cancer cells.?Primary keratinocytes monolayer and organotypic raft culture models were used to evaluate HPV viral replication and cervical intraepithelial neoplasia (CIN) phenotypes.?Preclinical pharmacokinetics and toxicity tests for FIT-039 were also conducted.?Finally, the anti-HPV effect of FIT-039 was further examined in vivo, using HPV+ cervical cancer xenografts[1] |
| In vitro | FIT-039 inhibits HPV replication and expression of E6 and E7 viral oncogenes, restoring tumor suppressors p53 and pRb in HPV+?cervical cancer cells. The therapeutic effect of FIT-039 was demonstrated in CIN model of an organotypic raft culture, where FIT-039 suppressed HPV18-induced dysplasia/hyperproliferation with reduction in viral load. FIT-039 also repressed growth of HPV16+, but not HPV-?cervical cancer xenografts without any significant adverse effects. Safety and pharmacokinetics of FIT-039 were confirmed for systemic and topical routes[1]. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 30 mg/mL (95.11 mM), Sonication is recommended.
10% DMSO+90% Corn Oil : 2 mg/mL (6.34 mM), Sonication is recommended.
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| Keywords | viruses | transcription | RNASynthesis | RNA Synthesis | polymerase-II | orally | mRNA | Inhibitor | inhibit | HSV-2 | HSV-1 | HSV | Herpes simplex virus | FIT-039 | FIT039 | FIT 039 | DNASynthesis | DNA/RNA Synthesis | DNA Synthesis | DNA | Cytomegalovirus | Cyclin dependent kinase | CMV | CDK9/cyclin T1 | CDK9 | CDK | antiviral |
| Inhibitors Related | 5-Fluorouracil | Phenytoin sodium | 2-Chloropyrazine | Kojic acid | Guanidine hydrochloride | Hexane-1,6-diol | 1,4-Naphthoquinone | Adenine | Oxyresveratrol | Carbazole | Thymidine | Usnic Acid |
| Related Compound Libraries | Anti-Pancreatic Cancer Compound Library | Bioactive Compound Library | ReFRAME Related Library | Kinase Inhibitor Library | Anti-Breast Cancer Compound Library | Inhibitor Library | NO PAINS Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Cell Cycle Compound Library | Anti-Cancer Compound Library | Anti-Infection Compound Library |
United States
