1. Autophagy
  2. Autophagy
  3. THZ-P1-2

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.

For research use only. We do not sell to patients.

THZ-P1-2 Chemical Structure

THZ-P1-2 Chemical Structure

CAS No. : 2058075-45-7

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5 mg USD 450 In-stock
10 mg USD 700 In-stock
50 mg USD 1880 In-stock
100 mg USD 2900 In-stock
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Customer Review

Based on 3 publication(s) in Google Scholar

Top Publications Citing Use of Products

    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.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    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[1].

    In Vitro

    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.

    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.
    Molecular Weight

    531.61

    Formula

    C31H29N7O2

    CAS No.
    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

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    4°C, protect from light

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

    Solvent & Solubility
    In Vitro: 

    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)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.8811 mL 9.4054 mL 18.8108 mL
    5 mM 0.3762 mL 1.8811 mL 3.7622 mL
    View the 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.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    C2

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    In Vivo:

    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.

    • Protocol 1

      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.
    • Protocol 2

      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.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    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).
    Calculation results:
    Working solution concentration: 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)

    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    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.
    Purity & Documentation

    Purity: 99.86%

    References

    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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    THZ-P1-2 Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Cat. No.:
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