LDC4297 hydrochloride

LDC4297 hydrochloride is a selective inhibitor of CDK7 with an IC50 value of 0.13 nM. LDC4297 hydrochloride inhibits human cytomegalovirus (HCMV) replication with an EC50 value of 24.5 nM. LDC4297 hydrochloride shows broad antiviral activities to Herpesviridae, Adenoviridae, Poxviridae, Retroviridae and Orthomyxoviridae with EC50 values of 0.02-1.21 μM. LDC4297 hydrochloride can be used for the research of infection[1].

Signaling Pathways >> Anti-infection >> HSV

Signaling Pathways >> Anti-infection >> HIV

Research Areas >> Infection

Signaling Pathways >> Cell Cycle/DNA Damage >> CDK

CDK7:0.13 nM (IC50)

166v VP22-GFP:0.02 μM (EC50)

01-6332:0.27 μM (EC50)

HIV-1 (NL4.3 strain):1.04 μM (EC50)

4LIG7:1.13 μM (EC50)

LDC4297 hydrochloride (0-10 μM; 6 d) dose-dependently inhibits HCMV replication with an EC50 value of 24.5 nM[1]. LDC4297 hydrochloride (0-10 μM; 4 d) shows anti-proliferative activity to primary cultures of fibroblasts derived from human (HFF) with a GI50 value of 4.5 μM[1]. LDC4297 hydrochloride (20 μM; 12-96 h) shows anti-HCMV activity through a multifaceted mode of action that involves an interference with virus-induced Rb phosphorylation[1]. LDC4297 hydrochloride (0-10 μM; 7 d) shows broad antiviral activities to HCMV, GPCMV, MCMV, HVV-6A, HSV-1, HSV-2, VZV, EBV, HAdV-2, Vaccinia virus, HIV-1 (nl4-3), HIV-1 (4LIG7) and Influenza A virus with EC50 values of 0.02, 0.05, 0.07, 0.04, 0.02, 0.27, 0.06, 1.21, 0.25, 0.77, 1.04, 1.13 and 0.99 μM, respectively[1]. Western Blot Analysis[1] Cell Line: Primary cultures of fibroblasts derived from human (HFF) with virus infection Concentration: 20 μM Incubation Time: 12, 24, 48 and 96 hours Result: Showed inhibitory effect towards viral protein synthesis at the stage of immediate early (IE) gene expression and the drug-mediated reduction of IE1p72 levels partially recovered over time. Exerted an inhibitory effect on human cytomegalovirus (HCMV) induced an up-regulation of protein expression or protein phosphorylation, and reduced Rb expression in the uninfected control cells at 24 h.

LDC4297 hydrochloride (100 mg/kg; p.o. once) shows promising pharmacokinetic analyses[1]. Animal Model: CD1 mice[1] Dosage: 100 mg/kg Administration: Oral gavage; 100 mg/kg once Result: Showed a half-life (t1/2z) of 1.6 h, and the time to a mean peak plasma concentration of 1297.6 ng/mL is reached 0.5 h after administration with a continued presence in plasma for at least 8 h and a bioavailability of 97.7%.