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THZ-P1-2 | THZ-P1-2 : Covalent Inhibitor of PIP4K2A, PIP4K2B, PIP4K2C
RATINGS:
Cellular Use: (4 reviews)

In Model Organisms: (0 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
PIP4K2A
  • IC50:190 nM
  • Activity:0.2 µM
  • Activity:500 nM
  • IC50:870 - 3950 nM
  • ΔTm:9 K
PIP4K2B
  • Activity:0.2 µM
  • ΔTm:~12 K
  • Activity:500 nM
PIP4K2C
  • Activity:0.2 µM
  • Activity:500 nM
1 -5 µM for 6 h or ideally several time points
up to 10 uM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
Kinome-wide selectivity of THZ-P1-2 was assessed in the commercially available DiscoverX KINOMEscan ...
Selectivity Assessment Description:
IC50 of 40 nM on PIKfyve in a fixed time point ADP-Glo assay. The additional potential off-targets i ...
In Cell Selectivity Assessment
Selectivity Assessment Description:
To further assess if THZ-P1-2 biochemical inhibition was maintained in cells, dtb-THZ-P1-2 binding o ...

Potency
Cellular
In Vitro

PIP4K2A

Mode of Action: Covalent Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1016/j.chembiol.2020.02.003

PIP4K2B

Mode of Action: Covalent Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1016/j.chembiol.2020.02.003

PIP4K2C

Mode of Action: Covalent Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1016/j.chembiol.2020.02.003

Negative Control Compounds

THZ-P1-2-R
SMILES: CN(C)CCCC(NC1=CC=C(C=C1)C(NC2=CC=CC(NC3=CC(C4=CNC5=CC=CC=C45)=NC=N3)=C2)=O)=O

Chemical Information

Molecular Formula C31H29N7O2
SMILEs CN(C)C/C=C/C(=O)Nc1ccc(C(=O)Nc2cccc(Nc3cc(-c4c[nH]c5ccccc45)ncn3)c2)cc1
InChI InChI=1S/C31H29N7O2/c1-38(2)16-6-11-30(39)36-22-14-12-21(13-15-22)31(40)37-24-8-5-7-23(17-24)35-29-18-28(33-20-34-29)26-19-32-27-10-4-3-9-25(26)27/h3-15,17-20,32H,16H2,1-2H3,(H,36,39)(H,37,40)(H,33,34,35)/b11-6+
Molecular weight 531.24 Da
AlogP 5.677100000000004
HBond acceptors 9
HBond donors 4
Atoms 69

Expert Reviews

by SERP+
(on 9 Jul 2026)
Cellular Use Rating
THZ-P1-2 is a valuable covalent cellular probe for PI5P4Kα/β/γ, supported by sub-micromolar cellular potency. PI5P4Kα–THZ-P1-2 co-crystal structure identified the binding pose at the ATP-site. The cysteine-containing...
by SERP
(on 7 Aug 2026)
Cellular Use Rating
THZ-P1-2 is a pan PI5P4kinase inhibitor which is reported to have a covalent mode of inhibition. The compound is well characterised with biochemical IC50 values and evidence of cellular target engagement...
by SERP
(on 14 Aug 2026)
Cellular Use Rating
The fast molecular reaction within 2 hours of THZ-P1-2 with all the PI5P4K lipid kinase family (PIP4K2A/PIP4K2B/PIP4K2C) is biophysically supporting the claim of a covalent reaction at cysteines in a disordered...
by SERP
(on 16 Aug 2026)
Cellular Use Rating
THZ-P1-2 is a covalent inhibitor of PI5P4K2A (biochemical IC50 = 190 nM), PI5P4K2B, and PI5P4K2C. While IC50 values have not been determined for PI5P4K2B and PI5P4K2C, the radiometric TLC assay shows lower...
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