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BF738735

CAS No. : 1436383-95-7

MCE 国际站：BF738735

产品活性：BF738735 是一种磷脂酰肌醇 4-激酶 IIIβ (PI4KIIIβ) 抑制剂，IC₅₀ 为 5.7 nM。

研究领域：PI3K/Akt/mTOR  |  Anti-infection

作用靶点：PI4K  |  Reverse Transcriptase

In Vitro: BF738735 (Compound 1) strongly inhibits PI4KIIIβ activity in vitro, with an IC₅₀ of 5.7 nM. BF738735 also impairs PI4KIIIα, but only at an ~300-fold-higher concentration (IC₅₀ of 1.7 μM). In addition, the activity of BF738735 is analyzed on a set of 150 cellular kinases, including 13 lipid kinases at a concentration of 10 μM. For all kinases, the inhibition is less than 10%, indicating that BF738735 specifically inhibits PI4KIIIβ in vitro. BF738735 exhibits a broad spectrum of antiviral activity, as it inhibits all tested species of enteroviruses and rhinoviruses, with 50% effective concentrations ranging between 4 and 71 nM. BF738735 potently inhibits all viruses tested, with EC₅₀s ranging between 4 and 71 nM. The cytotoxicity of BF738735, determined in parallel with the EC₅₀ and using the same culture conditions for 3 to 4 days, is low, with CC₅₀ values ranging from 11 to 65 μM, resulting in high selectivity indices. Low concentrations of BF738735 reduce the amount of luciferase to GuaHCl-treated levels, suggesting that the BF738735 blocks viral RNA replication. The EC₅₀ of BF738735 in this assay is 77 nM, which is comparable to the inhibition observed in the multicycle assay for coxsackievirus serotype B3 (CVB3).

In Vivo: BF738735 is well tolerated by specimens with good plasma levels of the antiviral in circulation and a complete inhibition with 25 mg/kg and some inhibition with 5 mg/kg dose is observed.

相关产品：Bioactive Compound Library Plus  |  Anti-Infection Compound Library  |  Kinase Inhibitor Library  |  PI3K/Akt/mTOR Compound Library  |  Antiviral Compound Library  |  Anti-Aging Compound Library  |  Oxygen Sensing Compound Library  |  Glycolysis Compound Library  |  Cytoskeleton Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  Suramin sodium salt  |  Lamivudine  |  Daidzin  |  Efavirenz  |  Emtricitabine  |  Tenofovir  |  Rilpivirine  |  Tenofovir alafenamide  |  Zalcitabine  |  PI4KIIIbeta-IN-10  |  Stavudine  |  Adefovir dipivoxil  |  Corilagin  |  Nevirapine  |  Abacavir  |  Delavirdine mesylate  |  Didanosine  |  PI-273  |  Etravirine  |  Adefovir  |  Pyridoxal phosphate  |  Gramine  |  KDU691  |  Tenofovir Disoproxil  |  Dapivirine  |  T-00127_HEV1

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