1. Cell Cycle/DNA Damage
    Anti-infection
  2. CDK
    HSV
    CMV
    DNA/RNA Synthesis
  3. FIT-039

FIT-039 

Cat. No.: HY-18944 Purity: >98.0%
Handling Instructions

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.

For research use only. We do not sell to patients.

FIT-039 Chemical Structure

FIT-039 Chemical Structure

CAS No. : 1113044-49-7

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5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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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.

IC50 & Target[1]

CDK9/cyclinT1

5.8 μM (IC50)

HSV-1

0.69 μM (IC50)

HSV-2

 

CMV

 

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

315.41

Formula

C₁₇H₁₈FN₃S

CAS No.

1113044-49-7

SMILES

FC1=CC(NC(C2=CC=NC=C2)=S)=C(N3CCCCC3)C=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
References
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Keywords:

FIT-039FIT039FIT 039CDKHSVCMVDNA/RNA SynthesisCyclin dependent kinaseHerpes simplex virusCytomegalovirusCDK9mRNAtranscriptionantiviralDNAvirusesHSV-1HSV-2polymerase-IIorallyInhibitorinhibitorinhibit

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FIT-039
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