PIK-93

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

PIK-93 是一种有效的合成 PI4K 抑制剂，IC50 为 19 nM (PI4KIIIβ)。

PIK-93 is a potent, synthetic PI4K inhibitor with IC50 of 19 nM (PI4KIIIβ), also inhibits PI3Kγ and PI3Kα with IC50 of 16 nM and 39 nM, respectively; also inhibits other PI3Ks, including PI3Kα, β, and δ, with IC50 values of 39 nM, 0.59 uM, and 0.12 uM, shows no inhibitory effect against a panel of other kinases; significantly inhibits the conversion of [3H]serine-labeled endogenous ceramide to sphingomyelin, reduces carbachol-induced translocation of TRPC6 to the plasma membrane and net Ca2+ entry in T6.11 cells at 300 nM; also demonstrates anti-enterovirus effects by inhibition of both poliovirus and HCV replication with EC50 of 0.14 uM and 1.9 uM, respectively.

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 μM and 1.9 μM, respectively.

——

PIK 93 | PIK93

PI3K/Akt/mTOR signaling

PI4K

ATM|C2β|DNA-PK|hsVps34|mTORC1|p110α|p110β|p110γ|p110δ|PI3KIIIβ

Cancer

——

593960-11-3

389.8775

C14H16ClN3O4S2

>98% (HPLC)

10 mM in DMSO

CC(NC1=NC(C)=C(C2=CC=C(Cl)C(S(=O)(NCCO)=O)=C2)S1)=O

Acetamide, N-[5-[4-chloro-3-[[(2-hydroxyethyl)amino]sulfonyl]phenyl]-4-methyl-2-thiazolyl]-

(-20℃)

With Ice Pack

≥ 2 years