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

THZ-P1-2 

Cat. No.: HY-136351 Purity: 99.06%
Handling Instructions

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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Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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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 (10-100000 nM; 72 hours) shows modest anti-proliferative activity in all six AML/ALL cell lines with IC50 values in the low micromolar range[1].

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.

2058075-45-7

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)

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Keywords:

THZ-P1-2AutophagycovalentPI5P4Kleukemiacellscancerleukemogenesiscysteines,TFEBsignalingTHP1Inhibitorinhibitorinhibit

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THZ-P1-2
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