Formulation: A solid
Formal Name: N-[5-fluoro-2-(1-piperidinyl)phenyl]-4-pyridinecarbothioamide
Purity: ≥98%
Formula Markup: C17H18FN3S
Formula Weight: 315,4
Shelf life (days): 1460
CAS Number: 1113044-49-7
Notes: FIT-039 is an inhibitor of cyclin-dependent kinase 9 (Cdk9; IC50 = 5.8 µM for Cdk9/cyclin T1).{65181} It is selective for Cdk9/cyclin T1 over Cdk4/cyclin D3 at 30 µM and Cdk2/cyclin A2, Cdk2/cyclin E1, Cdk5/p25, Cdk6/cyclin D3, and Cdk7/cyclin/MAT1 at 10 µM but also inhibits GSK3α, GSK3β, PKN1, haspin, p70S6K, DYRK1B, DYRK3, and IRR at 10 µM. FIT-039 inhibits DNA replication of herpes simplex virus 1 (HSV-1) in HeLa cells (IC50 = 0.69 µM). Topical application of FIT-039 (1.25-10% w/w) reduces skin lesions and improves survival in HSV-1-infected mice. FIT-039 (300 mg/kg) also reduces tumor growth in a human papillomavirus (HPV) type 16-positive Ca Ski cervical cancer mouse xenograft model.{65182}
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