| Identification | Back Directory | [Name]
FIT-039 | [CAS]
1113044-49-7 | [Synonyms]
FIT-039
FIT-039
(FIT039)
N-[5-Fluoro-2-(1-piperidinyl)phenyl]-4-pyridinecarbothioamide
N-(5-fluoro-2-(piperidin-1-yl)phenyl)pyridine-4-carbothioamide
4-Pyridinecarbothioamide, N-[5-fluoro-2-(1-piperidinyl)phenyl]- | [Molecular Formula]
C17H18FN3S | [MDL Number]
MFCD29770796 | [MOL File]
1113044-49-7.mol | [Molecular Weight]
315.41 |
| Hazard Information | Back Directory | [Description]
FIT-039 is a novel cyclin-dependent kinase 9 (CDK9) inhibitor, suppressing replication of a broad spectrum of DNA viruses through inhibition of mRNA transcription. | [Uses]
FIT-039 is a selective, ATP-competitive and orally active CDK9 inhibitor with an IC50 of 5.8 μM for CKD9/cyclin T1. FIT-039 does not inhibit other CDKs and other kinases. 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. | [in vivo]
Treatment with the FIT-039 ointment twice a day suppresses skin lesions and rescues mice (male BALB/c mice injected with HSV-1) from lethality in a dose-dependent manner. The healing of lesions is observed with 5% to 10% FIT-039 ointment, leading to the complete regression of zosteriform spread on day 10, which is also observed with the 5% ACV ointment[1].
FIT-039 does not affect body weight gain in mice administrated with an overdose of this compound (1000 mg/kg/d) for 14 days, and no changes are observed in biological markers in their blood[1]. | [target]
FIT-039 is a selective, ATP-competitive and orally active CDK9 inhibitor with an IC50 of 5.8 μM for CKD9/cyclin T1. FIT-039 inhibits replication of HSV-1 (IC50 of 0.69 μM), HSV-2, human adenovirus, and human CMV. | [IC 50]
CDK9/cyclinT1: 5.8 μM (IC50); HSV-1: 0.69 μM (IC50); HSV-2; CMV | [References]
[1] Makoto Yamamoto, et al. CDK9 Inhibitor FIT-039 Prevents Replication of Multiple DNA Viruses. J Clin Invest. 2014 Aug;124(8):3479-88. DOI:10.1172/JCI73805 |
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Lynnchem
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| Company Name: |
Novachemistry
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https://www.novachemistry.com/ |
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