PI4KIIIbeta-IN-11

Names

[ Name ]:
PI4KIIIbeta-IN-11

Biological Activity

[Description]:

PI4KIIIbeta-IN-11 is an inhibitor of PI4KIIIβ, with a mean pIC50 value of at least 9.1. PI4KIIIβ plays a key role in diseases research of RNA viruses and Plasmodium falciparum[1][2].

[Related Catalog]:

Research Areas >> Infection

Signaling Pathways >> PI3K/Akt/mTOR >> PI4K

[Target]

PI4KIIIβ:9.1 (pIC50)

[In Vitro]

PI4KIIIβ may be a relevant target protein for inhibition of Hedgehog signaling, and regulates trafficking from the Golgi system to the plasma membrane[1]. PI4KIIIbeta-IN-11 (compound 22) (0.5 μM; 0-45 min) shows metabolic stability in human microsomes, with the intrinsic clearance of 33.7 mL/min/g[2].

[In Vivo]

PI4KIIIbeta-IN-11 (compound 22) (1 mg/kg; i.v.; last over 1 h) displays a low spleen concentration in rats[2]. Animal Model: Male Wistar Han Rats[2] Dosage: 1 mg/kg Administration: Intravenous injection, formulated in 2% DMSO in Kleptose (aq, 10% w/v); over 1 hour; euthanised at 12 h Result: Showed a low concentration in spleen of 5.54 ng/g.

[References]

[1]. Kremer L, et al. Discovery of the Hedgehog Pathway Inhibitor Pipinib that Targets PI4KIIIß. Angew Chem Int Ed Engl. 2019 Nov 11;58(46):16617-16628.

[2]. Barton Nicholas Paul, et al. Preparation of pyrazolopyrimidinamines derivatives as PI4kIII-beta inhibitors: World Intellectual Property Organization, WO2019141694. 2019-07-25.

Chemical & Physical Properties

[ Molecular Formula ]:
C₃₃H₃₉N₇O₃

[ Molecular Weight ]:
581.71

Related Compounds

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