General
Preferred name
THZ-P1-2
Synonyms
P&D ID
PD135292
CAS
2058075-45-7
Tags
available
probe
covalent binder
Probe info
Probe type
experimental probe
Probe selectivity
family-selective
Probe sources
Gray Laboratory Probes
High-quality chemical probes
Probe targets
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION THZ-P1-2 is a first-in-class and selective PI5P4K inhibitor, with an IC50 of 190 nM for PI5P4K¦Á. THZ-P1-2 covalently targets cysteines on a disordered loop in PI5P4K¦Á/¦Â/¦Ã. THZ-P1-2 causes autophagy disruption and upregulates TFEB signaling. THZ-P1-2 displays anticancer activity in leukemia cell lines[1].
PRICE 285
DESCRIPTION THZ-P1-2 is a selective and potent PI5P4K inhibitor with anti-leukemic activity that acts by disrupting mitochondrial homeostasis and autophagy.THZ-P1-2 induces cell death and mitochondrial damage, and can be used in the study of leukemias. (TargetMol Bioactive Compound Library)
Compound Sets
6
CovalentInDB
CI004560
CZ-OPENSCREEN Bioactive Library
Gray Laboratory Probes
High-quality chemical probes
PD135292
MedChem Express Bioactive Compound Library
HY-136351
TargetMol Bioactive Compound Library
T39459
External IDs
9
Properties
(calculated by RDKit )
Molecular Weight
531.24
Hydrogen Bond Acceptors
6
Hydrogen Bond Donors
4
Rotatable Bonds
9
Ring Count
5
Aromatic Ring Count
5
cLogP
5.68
TPSA
115.04
Fraction CSP3
0.1
Chiral centers
0.0
Largest ring
6.0
QED
0.18
Structural alerts
0
No structural alerts detected
Custom attributes
(extracted from source data)
Target
PI5P4K
PIP4K2A
PIP4K2B
PIP4K2C
Autophagy
Negative control
THZ-P1-2-R
Pathway
PI3K/Akt/mTOR signaling
Source data