THZ-P1-2
Based on 2 publication(s) in Google Scholar
THZ-P1-2 is a first-in-class and selective PI5P4K inhibitor, with an IC50 of 190 nM for PI5P4Kα. THZ-P1-2 covalently targets cysteines on a disordered loop in PI5P4Kα/β/γ. THZ-P1-2 causes autophagy disruption and upregulates TFEB signaling. THZ-P1-2 displays anticancer activity in leukemia cell lines.
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- Pureté: 99.86%
- CAS No.: 2058075-45-7
- Formule: C31H29N7O2
- Masse moléculaire:531.61
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Stockage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Anti-Cancer Compound Library
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Publications Citing Use of MedChemExpress (MCE) THZ-P1-2
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Customer Validation & Images
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WB
Activité biologique
THZ-P1-2 (0.2-11.4 μM) exhibits approximately 75% inhibition of PI-4,5-P2 formation by PI5P4Kα and PI5P4Kγ and 50% inhibition by PI5P4Kβ at a concentration of 0.7 μM[1].
THZ-P1-2 (10 nM-100 μM; 72 h) shows modest anti-proliferative activity in all six AML/ALL cell lines with IC50 values in the low micromolar range[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:THP1, SEMK2, OCI/AML-2, HL60, SKM1, NOMO1 cells
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Concentration:10-100000 nM
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Incubation Time:72 hours
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Result:Showed anti-proliferative activity in all six AML/ALL cell lines with IC50 values ranging from 0.87 to 3.95 μM.
Chemical Information
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CAS No. 2058075-45-7
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Appearance Solid
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Masse moléculaire 531.61
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Formule C31H29N7O2
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Color Light yellow to yellow
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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
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (2)
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Journal Impact Factor
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Most Recent
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Nat Commun
PIP4K2B is mechanoresponsive and controls heterochromatin-driven nuclear softening through UHRF1. [Abstract]2023 Mar 14;14(1):1432. PMID: 36918565
THZ-P1-2 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 Mar 14;14(1):1432. [Abstract]
THZ-P1-2 (5, 10 µM; 24 h) leads to impairment of UHRF1 levels in hTERT-RPE1 cells.
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Int J Mol Sci
Pharmacological Inhibition of PIP4K2 Potentiates Venetoclax-Induced Apoptosis in Acute Myeloid Leukemia. [Abstract]2023 Nov 29;24(23):16899. PMID: 38069220
Solvant et solubilité
DMSO : 100 mg/mL (188.11 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 25 mg/mL (47.03 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 25 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (250.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.70 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (271 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8811 mL | 9.4054 mL | 18.8108 mL | 47.0270 mL |
| 5 mM | 0.3762 mL | 1.8811 mL | 3.7622 mL | 9.4054 mL | |
| 10 mM | 0.1881 mL | 0.9405 mL | 1.8811 mL | 4.7027 mL | |
| 15 mM | 0.1254 mL | 0.6270 mL | 1.2541 mL | 3.1351 mL | |
| 20 mM | 0.0941 mL | 0.4703 mL | 0.9405 mL | 2.3513 mL | |
| 25 mM | 0.0752 mL | 0.3762 mL | 0.7524 mL | 1.8811 mL | |
| 30 mM | 0.0627 mL | 0.3135 mL | 0.6270 mL | 1.5676 mL | |
| 40 mM | 0.0470 mL | 0.2351 mL | 0.4703 mL | 1.1757 mL | |
| 50 mM | 0.0376 mL | 0.1881 mL | 0.3762 mL | 0.9405 mL | |
| 60 mM | 0.0314 mL | 0.1568 mL | 0.3135 mL | 0.7838 mL | |
| 80 mM | 0.0235 mL | 0.1176 mL | 0.2351 mL | 0.5878 mL | |
| 100 mM | 0.0188 mL | 0.0941 mL | 0.1881 mL | 0.4703 mL |
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