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Chemical Structure| 2058075-45-7 Chemical Structure| 2058075-45-7

Structure of THZ-P1-2
CAS No.: 2058075-45-7

Chemical Structure| 2058075-45-7

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THZ-P1-2 is a selective PI5P4K inhibitor with an IC50 value of 190 nM for PI5P4Kα. THZ-P1-2 covalently targets a cysteine residue in the disordered loop of PI5P4Kα/β/γ. THZ-P1-2 induces autophagy disruption and upregulates TFEB signaling. THZ-P1-2 has shown anticancer activity in leukemia cell lines.

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Product Details of THZ-P1-2

CAS No. :2058075-45-7
Formula : C31H29N7O2
M.W : 531.61
SMILES Code : 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
MDL No. :MFCD32858287

Safety of THZ-P1-2

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319
Precautionary Statements:P501-P270-P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313-P301+P312+P330

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
NALM6 cells 1.6, 3.2, 6.4 µM 24 h THZ-P1-2 induced apoptosis in NALM6 cells and caused loss of mitochondrial membrane potential, indicating mitochondrial damage. PMC9643393
Jurkat cells 1.6, 3.2, 6.4 µM 24 h THZ-P1-2 induced apoptosis in Jurkat cells and caused loss of mitochondrial membrane potential, indicating mitochondrial damage. PMC9643393
OCI-AML3 cells 1.6, 3.2, 6.4 µM 24 h THZ-P1-2 induced apoptosis in OCI-AML3 cells and caused loss of mitochondrial membrane potential, indicating mitochondrial damage. PMC9643393
MV4-11 cells 1.6, 3.2, 6.4 µM 24 h THZ-P1-2 induced apoptosis in MV4-11 cells and caused loss of mitochondrial membrane potential, indicating mitochondrial damage. PMC9643393
HeLa cells 250 nM 18 h To evaluate the effect of THZ-P1-2 on autophagy, results showed that THZ-P1-2 caused autophagosome clearance defects and upregulation of TFEB nuclear localization. PMC7286548
U-937 cells 0.3, 0.6, 1.2, 2.5, 5 µM 48 h THZ-P1-2 potentiated venetoclax-induced apoptosis and significantly reduced cell viability PMC10706459
NB4 cells 0.3, 0.6, 1.2, 2.5, 5 µM 48 h THZ-P1-2 potentiated venetoclax-induced apoptosis and significantly reduced cell viability PMC10706459
Kasumi-1 cells 0.3, 0.6, 1.2, 2.5, 5 µM 48 h THZ-P1-2 potentiated venetoclax-induced apoptosis and significantly reduced cell viability PMC10706459
HEK 293T cells 10 μM 1 h The cellular binding activity of THZ-P1-2 was evaluated using CETSA, showing that THZ-P1-2 exhibits good PI5P4K binding activity in HEK 293T cells. PMC7074221

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.88mL

0.38mL

0.19mL

9.41mL

1.88mL

0.94mL

18.81mL

3.76mL

1.88mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

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