PIK-93

SKU: orb1305263

Description

PIK-93 is a potent and selective synthetic inhibitor of phosphatidylinositol 4-kinase (PI4K) with an IC50 of 19 nM, and it also inhibits PI3Kα with an IC50 of 39 nM. This small molecule is a valuable chemical probe for studying phosphoinositide signaling in cancer research and has been utilized in both cellular and in vivo models to investigate lipid kinase function.

Research Area

Infectious Disease & Virology, Metabolism Research, Molecular Biology, Signal Transduction

Key Properties

• CAS Number: 593960-11-3
• MW: 389.88
• Purity: 99.83% (May vary between batches)
• Formula: C₁₄H₁₆ClN₃O₄S₂
• SMILES: CC(=O)Nc1nc(C)c(s1)-c1ccc(Cl)c(c1)S(=O)(=O)NCCO
• Target: Virus Protease,ATM/ATR,PI3K,Carbonic Anhydrase,mTOR,DNA-PK,PI4K,HSV
• Solubility: DMSO:39 mg/mL (100.03 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (10.26 mM)

Bioactivity

• Target IC50:
  hsVPS34:320 nM|ATM:490 nM|p110β:590 nM|PI3KC2β:140 nM|PI4K:19 nM|PI3KC2α:16 μM|ATR:17 μM|p110γ:16 nM|PI4KIIIα:1.1 μM|PI3Kα:39 nM|DNA-PK:64 nM|p110δ:120 nM|mTORC1:1.38 μM
• In Vivo:
  At concentrations ranging from 0.5 μM to 1 μM, PIK-93 impairs the stability of aggregates formed in differentiated HL60 cells treated with f-Met-Leu-Phe. In COS-7 cells, 250 nM of PIK-93 effectively eliminates the accumulation of the CERT-PH domain and FL-Cer in the Golgi apparatus. Additionally, in T6.11 cells, 300 nM of PIK-93 reduces Carbachol-induced translocation of TRPC6 to the plasma membrane and subsequent Ca2+ entry. The same concentration of PIK-93 also significantly inhibits the conversion of [3H]-labeled serine to endogenous sphingomyelin, indicating the critical role of PI4KIIIβ in the endoplasmic reticulum and Golgi apparatus for ceramide transfer and sphingomyelin synthesis regulation. Research demonstrates that PIK-93 possesses antiviral capabilities, inhibiting replication of the poliovirus and hepatitis C virus with EC50 values of 0.14 μM and 1.9 μM, respectively. PIK-93 effectively inhibits PI3Kγ and PI4KIIIβ, with IC50 values of 16 nM and 19 nM, respectively, and other PI3K members, including PI3Kα, β, and δ, with IC50 values of 39 nM, 0.59 μM, and 0.12 μM, while showing negligible inhibition effects on other kinases at concentrations up to 10 μM.
• Cell Research:
  For actin staining, dHL60 cells are preincubated in suspension with PIK-93 or vehicle for 40 min, centrifuged for 5 min at 2000 rpm at room temperature in a J6-B centrifuge, resuspended in mHBSS containing the respective agent at the same concentration, allowed to stick to fibronectin-covered coverslips, and subjected to stimulation with a uniform concentration of 100 nM f-Met-Leu-Phe (fMLP) for 3 min. Cellsare fixed in 3.7% PFA and stained with 10 units/mL rhodamine-phalloidin for 15 min.(Only for Reference)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

DNAPK, DNA-PK, Carbonic Anhydrase, CarbonicAnhydrase, C2β, ATM, ATR, hsVps34, Inhibitor, mTORC1, inhibit, p110α, p110β, p110γ, p110δ, Phosphatidylinositol 4 kinases, Phosphoinositide 3-kinase, PIK93, PIK-93, PIK 93, PI4 kinases, PI4K, PI3K, PI3KIIIβ, Virus Protease, VirusProtease

Compound Identifiers

PubChem CID

6852167