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THZ-P1-2

CAS No. 2058075-45-7

THZ-P1-2( —— )

Catalog No. M35120 CAS No. 2058075-45-7

THZ-P1-2 is a selective and potent PI5P4K inhibitor with anti-leukemic activity that acts by disrupting mitochondrial homeostasis and autophagy.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    THZ-P1-2
  • Note
    Research use only, not for human use.
  • Brief Description
    THZ-P1-2 is a selective and potent PI5P4K inhibitor with anti-leukemic activity that acts by disrupting mitochondrial homeostasis and autophagy.
  • 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.
  • In Vitro
    Cell Proliferation Assay 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.
  • In Vivo
    ——
  • Synonyms
    ——
  • Pathway
    PI3K/Akt/mTOR signaling
  • Target
    PI3K
  • Recptor
    PI3K
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    2058075-45-7
  • Formula Weight
    531.61
  • Molecular Formula
    C31H29N7O2
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 100 mg/mL (188.11 mM; Ultrasonic )
  • SMILES
    CN(C)C\C=C\C(=O)Nc1ccc(cc1)C(=O)Nc1cccc(Nc2cc(ncn2)-c2c[nH]c3ccccc23)c1
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Sivakumaren SC, et al. Targeting the PI5P4K Lipid Kinase Family in Cancer Using Covalent Inhibitors. Cell Chem Biol. 2020;27(5):525‐537.e6.?
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