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FIT-039

  Cat. No.:  DC21015   Featured
Chemical Structure
1113044-49-7
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More than 5000 active chemicals with high quality for research!
Field of application
FIT-039 is a potent, selective CDK9 inhibitor with IC50 of 5.8 uM for CKD9/cyclin T1, suppresses the replication of HSV-1 (IC50=0.69 uM).
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 1113044-49-7
Chemical Name: FIT-039
Synonyms: FIT 039;FIT-039;FIT-039 (FIT039);4-Pyridinecarbothioamide, N-[5-fluoro-2-(1-piperidinyl)phenyl]-;N-(5-fluoro-2-(piperidin-1-yl)phenyl)pyridine-4-carbothioamide;N-[5-Fluoro-2-(1-piperidinyl)phenyl]-4-pyridinecarbothioamide
SMILES: C1=NC=CC(C(NC2=CC(F)=CC=C2N2CCCCC2)=S)=C1
Formula: C17H18FN3S
M.Wt: 315.40832567215
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: 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.
Target: CDK9/cyclinT1:5.8 μM (IC50) HSV-1:0.69 μM (IC50) HSV-2 CMV
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].
In Vitro: FIT-039 (30 μM; 3 hours; HEK293 cells) treatment decreases phosphorylated CTD in the infected or noninfected cells to a level lower than that shown by Flavopiridol. FIT-039 reduces the expression levels of HSV-1 immediate-early genes (IEGs) and early and late genes[1]. FIT-039 inhibits replication of the HSV-1 genome in a dose-dependent manner (EC50 and EC80 are 0.69 μM and 4.0 μM, respectively)[1]. FIT-039 potently suppresses 8 kinases (GSK3β, PKN1, haspin, p70s6K, DYRK1B, GSK3α, IRR, and DYRK3) other than CDK9 on the 332-kinase panel. These kinases are involved in the replication of various viruses[1]. Western Blot Analysis[1] Cell Line: HEK293 cells Concentration: 30 μM Incubation Time: 3 hours Result: Decreased phosphorylated carboxyterminal domain (CTD) in the infected or noninfected cells to a level lower than that shown by Flavopiridol.
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.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
2018-0101
2018-0101
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