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FIT-039

CAS No. : 1113044-49-7

MCE 站：FIT-039

产品活性：FIT-039 是一种选择性，ATP 竞争性且具有口服活性的 CDK9 抑制剂，对 CKD9/cyclin T1 的 IC₅₀ 为 5.8 μM。FIT-039 不抑制其他 CDK 和其他激酶。FIT-039 抑制 HSV-1 (IC₅₀ 为 0.69 μM)，HSV-2，人腺病毒和人 CMV 的复制。FIT-039 是一种有前途的抗病毒剂，可用于抑制耐药性 HSV 和其他 DNA 病毒。

研究领域：Cell Cycle/DNA Damage  |  Anti-infection

作用靶点：CDK  |  HSV  |  CMV  |  DNA/RNA Synthesis

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.
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.

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.
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.

相关产品：Remdesivir  |  Gemcitabine  |  Palbociclib  |  2-Deoxy-D-glucose  |  Brefeldin A  |  Bleomycin sulfate  |  Abemaciclib methanesulfonate  |  Cytarabine  |  Carboplatin  |  THZ531  |  α-Amanitin  |  Ribociclib  |  Streptozocin  |  Favipiravir  |  Dinaciclib  |  THZ1  |  Anisomycin  |  Flavopiridol  |  Imiquimod  |  Ro-3306  |  Seliciclib  |  Daunorubicin Hydrochloride  |  AZD4573  |  NVP-2  |  Capecitabine  |  Fludarabine

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