PIK-93 is a PI4KIIIβ inhibitor (IC50 at 19 nM). PIK-93 is the first reported PI4-kinase inhibitor, which is able to inhibit PI4KIIIβ at low-nanomolar range. In addition, this compound also inhibits potently PI3Kγ in vitro (IC50 at 16 nM). This compound inhibits p110α, p110β, p110δwith IC50 of 0.039, 0.59, 0.12 µM. PIK-93 also displays the typical hydrogen bonding to the backbone amide of Val882, and additional ones to the backbone carbonyl of Val882 and between its sulphonamide and Asp964.
|Cell lines||Differentiated HL60 (dHL60) cells|
|Preparation method||For actin staining, preincubate dHL60 cells in suspension with PIK-93 or vehicle for 40 min, centrifuge for 5 min at 2000 rpm at room temperature in a J6-B centrifuge, resuspend in mHBSS containing the respective agent at the same concentration, allowed to stick to fibronectin-covered coverslips, and subject to stimulation with a uniform concentration of 100 nM f-Met-Leu-Phe (fMLP) for 3 min. Fixing cellsare in 3.7% PFA and staining with 10 units/mL rhodamine-phalloidin for 15 min|
|Concentrations||0.5 μM–1 μM|
|Incubation time||40 min|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 70 mg/mL|
|Related PI3K Products|
SAR405 is a PIK3C3/Vps34 inhibitor with an IC50 of 1.2 nM. SAR405 also is a proximal inhibitor of the autophagy machinery.
Tenalisib (RP6530) is a potent and selective dual PI3Kδ/γ inhibitor with IC50 values of 24.5 nM and 33.2 nM for PI3Kδ and PI3Kγ, respectively. Its selectivity over α and β isoforms are more than 300-fold and 100-fold, respectively.
PI 828 is a pI 3-kinase inhibitor, more potent than LY 294002.
IPI-3063 is a potent and selective p110δ inhibitor with biochemical IC50 of 2.5 ± 1.2 nM and IC50 values for the other class I PI3K isoforms (p110α, p110β, p110γ) are at least 400-fold higher.
GDC-0084 is a brain penetrant inhibitor of PI3K and mTOR.
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