Home PI3K/Akt/mTOR PI4K inhibitor PIK-93

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PIK-93 PI4K inhibitor

Cat.No.S1489

PIK-93 is the first potent, synthetic PI4K (PI4KIIIβ) inhibitor with IC50 of 19 nM; this compound is shown to inhibit PI3Kα with IC50 of 39 nM.
PIK-93 PI4K inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 389.88

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Quality Control

Batch: S148901 DMSO]78 mg/mL]false]Ethanol]1 mg/mL]false]Water]Insoluble]false Purity: 99.81%
99.81

Chemical Information, Storage & Stability

Molecular Weight 389.88 Formula

C14H16ClN3O4S2

 Storage (From the date of receipt)
CAS No. 593960-11-3 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CC1=C(SC(=N1)NC(=O)C)C2=CC(=C(C=C2)Cl)S(=O)(=O)NCCO

Solubility

In vitro
Batch:

DMSO : 78 mg/mL (200.06 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 1 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Mechanism of Action

Features
A novel and potent inhibitor of both PI3Kγ and PI4KIIIβ.
Targets/IC50/Ki
p110γ [1]
16 nM
PI4KIIIβ [1]
19 nM
p110α [1]
39 nM
DNA-PK [1]
64 nM
p110δ [1]
120 nM
C2β [1]
140 nM
hsVps34 [1]
320 nM
ATM [1]
490 nM
p110β [1]
590 nM
PI4KIIIα [1]
1.1 μM
mTORC1 [1]
1.38 μM
In vitro
PIK-93 inhibits PI3Kγ and PI4KIIIβ, with IC50 values of 16 nM and 19 nM, respectively. This compound 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. It shows no obvious inhibitory effect against a panel of other kinases, even at a concentration of 10 μM. [1] In differentiated HL60 (dHL60) cells, this compound (0.5 μM–1 μM) impairs consolidation and stability of the leading edge formed after treatment with uniform f-Met-Leu-Phe (fMLP). It alters the localization, but not the amount, of the fMLP-dependent accumulation of total F-actin. In fMLP gradients, this chemical reduces the chemotactic index and triples the cells' turning frequency. [2] In COS-7 cells, this compound (250 nM) effectively abrogates the accumulation of CERT-PH domain and FL-Cer in Golgi. It 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. [3] In T6.11 cells, this compound (300 nM) reduces carbachol-induced translocation of TRPC6 to the plasma membrane and net Ca2+ entry. [4] A recent report shows that this chemical 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. [5]
Kinase Assay
Assay of PI3Ks
IC50 values are measured using a standard TLC assay for lipid kinase activity. Kinase reactions are performed by preparing a reaction mixture containing kinase, PIK-93 (2% DMSO final concentration), buffer (25 mM HEPES, pH 7.4, 10 mM MgCl2), and freshly sonicated phosphatidylinositol (100 µg/ml). Reactions are initiated by the addition of ATP containing 10 µCi of γ-32P-ATP to a final concentration 10 or 100 µM, and allowed to proceed for 20 min at room temperature. For TLC analysis, reactions are then terminated by the addition of 105 µL 1N HCl followed by 160 µL CHCl3:MeOH (1:1). The biphasic mixture is vortexed, briefly centrifuged, and the organic phase transferred to a new tube using a gel loading pipette tip precoated with CHCl3. This extract is spotted on TLC plates and developed for 3 hours–4 hours in a 65:35 solution of n-propanol:1M acetic acid. The TLC plates are then dried, exposed to a phosphorimager screen, and quantitated. Kinase activity is typically measured at 10–12 concentrations of this compound representing two-fold dilutions from the highest concentration of 100 μM.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/22493444/
  • [5] https://pubmed.ncbi.nlm.nih.gov/21177810/

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