FIT-039
Modify Date: 2024-01-12 05:31:00
FIT-039 structure
|
Common Name | FIT-039 | ||
|---|---|---|---|---|
| CAS Number | 1113044-49-7 | Molecular Weight | 315.408 | |
| Density | 1.3±0.1 g/cm3 | Boiling Point | 460.4±55.0 °C at 760 mmHg | |
| Molecular Formula | C17H18FN3S | Melting Point | N/A | |
| MSDS | N/A | Flash Point | 232.2±31.5 °C | |
Use of FIT-039FIT-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. |
| Name | N-[5-Fluoro-2-(1-piperidinyl)phenyl]-4-pyridinecarbothioamide |
|---|---|
| Synonym | More Synonyms |
| 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. |
|---|---|
| Related Catalog | |
| Target |
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]. 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]. |
| References |
| Density | 1.3±0.1 g/cm3 |
|---|---|
| Boiling Point | 460.4±55.0 °C at 760 mmHg |
| Molecular Formula | C17H18FN3S |
| Molecular Weight | 315.408 |
| Flash Point | 232.2±31.5 °C |
| Exact Mass | 315.120544 |
| LogP | 3.05 |
| Vapour Pressure | 0.0±1.1 mmHg at 25°C |
| Index of Refraction | 1.662 |
| 4-Pyridinecarbothioamide, N-[5-fluoro-2-(1-piperidinyl)phenyl]- |
| N-[5-Fluoro-2-(1-piperidinyl)phenyl]-4-pyridinecarbothioamide |
| FIT-039 |