| Field | Specification |
|---|---|
| Target | |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C14H16ClN3O4S2 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
PIK-93 is described as the first potent, synthetic inhibitor of PI4K (PI4KIIIβ), acting with an IC50 of 19 nM. It also inhibits PI3Kγ and PI3Kα, with IC50 values of 16 nM and 39 nM, respectively. It is supplied as a white to off-white solid (C14H16ClN3O4S2, MW 389.88) at 99.74% purity.
Physical & Chemical Properties
| CAS Number | 593960-11-3 |
|---|---|
| Molecular Formula | C14H16ClN3O4S2 |
| Molecular Weight | 389.88 g/mol |
| Purity | 99.74% |
| Appearance | Solid |
| Color | White to off-white |
| SMILES | CC(NC1=NC(C)=C(S1)C2=CC=C(C(S(=O)(NCCO)=O)=C2)Cl)=O |
| Target | PI4KIIIβ, PI4KIIIα, p110γ, p110α, p110δ, p110β, PI3KC2β, PI3KC2α, hsVPS34, DNA-PK, ATM, mTORC1, ATR |
| Signaling Pathway | PI3K/Akt/mTOR; Anti-infection |
| Solubility | In Vitro: DMSO: 100 mg/mL (256.49 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 2 years; -20°C, 1 year. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target[1]
|
PI4KIIIβ 19 nM (IC50) |
PI4KIIIα 1.1 μM (IC50) |
p110γ 16 nM (IC50) |
p110α 39 nM (IC50) |
p110δ 120 nM (IC50) |
p110β 590 nM (IC50) |
PI3KC2β 140 nM (IC50) |
PI3KC2α 16 μM (IC50) |
hsVPS34 320 nM (IC50) |
DNA-PK 64 nM (IC50) |
ATM 490 nM (IC50) |
mTORC1 1.38 μM (IC50) |
ATR 17 μM (IC50) |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 100 mg/mL (256.49 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 2 years) or -20°C (up to 1 year); avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 4.55 mg/mL (11.67 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 4.55 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (45.5 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 2
| Composition | 10% DMSO + 90% (20% SBE-β-CD in saline) |
|---|---|
| Result | ≥ 2.5 mg/mL (6.41 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 900 μL 20% SBE-β-CD in saline. 20% SBE-β-CD in saline: dissolve 2 g SBE-β-CD powder in 10 mL saline until clear (4°C, store up to one week). |
Protocol 3
| Composition | 10% DMSO + 90% Corn Oil |
|---|---|
| Result | ≥ 2.5 mg/mL (6.41 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). Use with caution if continuous dosing will exceed two weeks. For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 900 μL corn oil. |
Data provided by the manufacturer.
In Vitro
PIK-93 inhibits PI3Kγ and PI4KIIIβ with IC50 values of 16 nM and 19 nM, respectively. Other PI3K members, including PI3Kα, β, and δ, are also inhibited (IC50 values of 39 nM, 0.59 μM, and 0.12 μM, respectively). No obvious inhibitory effect is seen against a panel of other kinases, even at 10 μM[1]. In differentiated HL60 cells (dHL60), PIK-93 (0.5 μM-1 μM) impairs the consolidation and stability of the leading edge that develops after uniform f-Met-Leu-Phe (fMLP) treatment. PIK-93 changes where, but not how much, total F-actin accumulates in an fMLP-dependent manner. In fMLP gradients, PIK-93 reduces the chemotactic index and triples the turning frequency of the cells[2]. In COS-7 cells, PIK-93 (250 nM) effectively abrogates CERT-PH domain and FL-Cer accumulation in Golgi. At the same concentration, PIK-93 also significantly inhibits conversion of [3H]serine-labeled endogenous ceramide to sphingomyelin. Together, these data point to PI4KIIIβ as a key player in ceramide transport between the ER and Golgi and in the regulation of sphingomyelin synthesis[3]. In T6.11 cells, PIK-93 (300 nM) lowers carbachol-induced TRPC6 translocation to the plasma membrane, along with net Ca2+ entry[4]. A recent report describes anti-enterovirus effects of PIK-93, shown by inhibited replication of both poliovirus (PV) and hepatitis C virus (HCV), with EC50 values of 0.14 μM and 1.9 μM, respectively[5].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
Kinase Assay[1]
Measure IC50 values with a standard TLC assay for lipid kinase activity. Prepare kinase reactions in a mixture of kinase, PIK-93 (final DMSO concentration of 2%), buffer (25 mM HEPES, pH 7.4, 10 mM MgCl2) and freshly sonicated phosphatidylinositol (100 μg/mL). Initiate reactions by adding ATP containing 10 μCi of γ-32P-ATP to a final concentration of 10 or 100 μM, and allow them to proceed for 20 min at room temperature. For TLC analysis, terminate reactions by adding 105 μL 1N HCl followed by 160 μL CHCl3:MeOH (1:1). Vortex the biphasic mixture, centrifuge briefly, and transfer the organic phase to a new tube with a gel loading pipette tip precoated with CHCl3. Spot this extract on TLC plates and develop in a 65:35 solution of n-propanol:1M acetic acid for 3 hours-4 hours. Dry the TLC plates, expose them to a phosphorimager screen, and quantitate. Measure kinase activity at 10-12 concentrations of PIK-93, using two-fold dilutions from the highest concentration of 100 μM.
Cell Assay[1]
For actin staining, preincubate dHL60 cells in suspension with PIK-93 or vehicle for 40 min, centrifuge at 2000 rpm for 5 min at room temperature in a J6-B centrifuge, resuspend in mHBSS containing the respective agent at the same concentration, let the cells stick to fibronectin-covered coverslips, and stimulate for 3 min with 100 nM f-Met-Leu-Phe (fMLP) at a uniform concentration. Fix cells in 3.7% PFA and stain with 10 units/mL rhodamine-phalloidin for 15 min.
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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Radiotherapy enhances anticancer CD8 T cell responses by cGAMP transfer through LRRC8A/C volume-regulated anion channels. Sci Immunol 2025 Jun 27;10(108):eadn1630. PMID: 40577443
Golgi-localized phosphatidylinositol 4-kinase β mediates Rab11a activation and trafficking to promote ciliogenesis. Sci Adv 2025 Dec 5;11(49):eadw6910. PMID: 41348894
Torin2 Exploits Replication and Checkpoint Vulnerabilities to Cause Death of PI3K-Activated Triple-Negative Breast Cancer Cells. Cell Syst 2020 Jan 22;10(1):66-81.e11. PMID: 31812693
In Vitro and in Vivo Activity of mTOR Kinase and PI3K Inhibitors Against Leishmania donovani and Trypanosoma brucei. Molecules 2020 Apr 23;25(8):1980.
Patent. US20250152599A1.
