FIT-039

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

FIT-039 是一种有效的选择性 CDK9 抑制剂，对 CKD9/cyclin T1 的 IC50 为 5.8 uM，抑制 HSV-1 的复制 (IC50=0.69 uM)

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); shows no marked inhibitory effect on CDK4/cyclinD3, does not inhibit other CDKs, including CDK2/cyclinB1, CDK2/cyclinE1, CDK5/p25, CDK6/cyclinD3, or CDK7/cyclinH/MAT; suppresses viral replication without affecting the host cell cycle, inhibits viral transcription; also inhibits HBV propagation and HIV-1 replication; suppresses HPV viral oncogenes E6 and E7, and shows therapeutic rffect on HPV-induced neoplasia in vivo.HPV Infection Phase 2 Clinical

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.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).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. Western Blot Analysis 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.

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.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.

FIT039

Cell Cycle/DNA Damage

CDK

CDK

Infection

HPV Infection

1113044-49-7

315.41

C17H18FN3S

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (317.05 mM)

C1CCN(CC1)C2=C(C=C(C=C2)F)NC(=S)C3=CC=NC=C3

N-[5-Fluoro-2-(1-piperidinyl)phenyl]-4-pyridinecarbothioamide

(-20℃)

With Ice Pack

≥ 2 years