| Field | Specification |
|---|---|
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C31H29N7O2 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
THZ-P1-2 is a first-in-class, selective PI5P4K inhibitor with an IC50 of 190 nM for PI5P4Kα. It covalently targets cysteines on a disordered loop within PI5P4Kα/β/γ, disrupting autophagy and upregulating TFEB signaling. It also displays anticancer activity in leukemia cell lines[1]. It is supplied as a light yellow to yellow solid (C31H29N7O2, MW 531.61) at 99.86% purity.
Physical & Chemical Properties
| CAS Number | 2058075-45-7 |
|---|---|
| Molecular Formula | C31H29N7O2 |
| Molecular Weight | 531.61 g/mol |
| Purity | 99.86% |
| Appearance | Solid |
| Color | Light yellow to yellow |
| SMILES | O=C(C(C=C1)=CC=C1NC(/C=C/CN(C)C)=O)NC2=CC=CC(NC3=CC(C4=CNC5=CC=CC=C45)=NC=N3)=C2 |
| Signaling Pathway | Autophagy |
| Solubility | In Vitro: DMSO: 100 mg/mL (188.11 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | 4°C, protect from light. In solvent: -80°C, 6 months; -20°C, 1 month (protect from light). |
| Shipping | Room temperature in continental US; may vary elsewhere. |
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 (188.11 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); protect from light; 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 + 90% (20% SBE-β-CD in saline) |
|---|---|
| Result | 25 mg/mL (47.03 mM); suspension; requires sonication |
| How to prepare | Gives a suspension at 25 mg/mL. The suspension is suitable for oral and intraperitoneal dosing. For 1 mL of working solution: add 100 μL DMSO stock (250.0 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 2
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 2.5 mg/mL (4.70 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 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 3
| Composition | 10% DMSO + 90% Corn Oil |
|---|---|
| Result | ≥ 2.5 mg/mL (4.70 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
THZ-P1-2 (0.2-11.4 μM) inhibits formation of PI-4,5-P2 by PI5P4Kα and PI5P4Kγ by approximately 75%, and by PI5P4Kβ by 50%, at a concentration of 0.7 μM[1]. In all six AML/ALL cell lines, THZ-P1-2 (10 nM-100 μM; 72 h) displays only modest anti-proliferative activity, with IC50 values in the low micromolar range[1].
Cell Proliferation Assay[1]
| Cell Line | THP1, SEMK2, OCI/AML-2, HL60, SKM1, NOMO1 cells |
|---|---|
| Concentration | 10-100000 nM |
| Incubation Time | 72 hours |
| Result | Showed anti-proliferative activity in all six AML/ALL cell lines with IC50 values ranging from 0.87 to 3.95 μM. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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PIP4K2B is mechanoresponsive and controls heterochromatin-driven nuclear softening through UHRF1. Nat Commun 2023 Mar 14;14(1):1432. PMID: 36918565
Pharmacological Inhibition of PIP4K2 Potentiates Venetoclax-Induced Apoptosis in Acute Myeloid Leukemia. Int J Mol Sci 2023 Nov 29;24(23):16899. PMID: 38069220
