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PIK-93

CAS No. : 593960-11-3

MCE 站：PIK-93

产品活性：PIK-93 是一种合成的，有效的 PI4KIIIβ 抑制剂，IC₅₀ 值为 19 nM，同时可抑制 PI3Kγ和 PI3Kα 的活性，IC₅₀ 值分别为 16 nM 和 39 nM。

研究领域：PI3K/Akt/mTOR  |  Anti-infection

作用靶点：PI4K  |  PI3K  |  Virus Protease

In Vitro: PIK-93 inhibits PI3Kγ and PI4KIIIβ, with IC₅₀ values of 16 nM and 19 nM, respectively. PIK-93 also inhibits other members of PI3Ks, including PI3Kα, β, and δ, with IC₅₀ values of 39 nM, 0.59 μM, and 0.12 μM, respectively. PIK-93 shows no obvious inhibitory effect against a panel of other kinases, even at a concentration of 10 μM. In differentiated HL60 (dHL60) cells, PIK-93 (0.5 μM-1 μM) impairs consolidation and stability of the leading edge formed after treatment with uniform f-Met-Leu-Phe (fMLP). PIK-93 alters the localization, but not the amount, of the fMLP-dependent accumulation of total F-actin. In fMLP gradients, PIK-93 reduces the chemotactic index and triples the cells' turning frequency. In COS-7 cells, PIK-93 (250 nM) effectively abrogates the accumulation of CERT-PH domain and FL-Cer in Golgi. PIK-93 of the same concentration also significantly inhibits the conversion of [³H]serine-labeled endogenous ceramide to sphingomyelin. These facts indicate a key role of PI4KIIIβ in ceramide transport between the ER and Golgi, as well as in the regulation of spingomyelin synthesis. In T6.11 cells, PIK-93 (300 nM) reduces carbachol-induced translocation of TRPC6 to the plasma membrane and net Ca²⁺ entry. A recent report shows that PIK-93 has anti-enterovirus effects, as revealed by its inhibition of both poliovirus (PV) and hepatitis C virus (HCV) replication, with EC₅₀ values of 0.14 ?M and 1.9 ?M, respectively.

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