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TMX-4153 | TMX-4153 : Degrader (PROTAC) of PIP4K2C
RATINGS:
Cellular Use: (2 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
PIP4K2C
  • Kd:0.45 nM
  • Kd:42 ± 2 nM
  • DC50:24 nM
  • Dmax:91%
Degrader (PROTAC)
up to 1 uM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
Kinome-wide selectivity profile (KINOMEscan) of TMX-4102 was performed at 1 μM.
In Vitro Selectivity Assessment
Potency Assay Off-Target:
Kinome-wide selectivity profile (KINOMEscan) of TMX-4135 was performed at 1 μM.
In Cell Selectivity Assessment
Potency Assay Off-Target:
Live cell KiNativ profiling of TMX-4102 in H1975 cells.
In Cell Selectivity Assessment
Potency Assay Off-Target:
Profiling on proteome-wide degradation selectivity was performed for both TMX-4153 and TMX-4153-neg ...

Potency
Cellular
In Vitro

PIP4K2C

Mode of Action: Degrader (PROTAC)

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1002/anie.202302364

Negative Control Compounds

canSAR7018955
Notes: TMX-4153-neg was not observed to degrade PIP4K2C or other targets in a proteome-wide degradation selectivity assay.

Chemical Information

Molecular Formula C59H67ClN10O6S
SMILEs Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCC(=O)N2CCC3(CC2)CCN(c2cncc(Nc4ncc(Cl)c(-c5cccc(-c6ccccc6)c5)n4)c2)C3=O)C(C)(C)C)cc1
InChI InChI=1S/C59H67ClN10O6S/c1-37(39-19-21-41(22-20-39)52-38(2)63-36-77-52)64-54(74)48-31-46(71)35-70(48)55(75)53(58(3,4)5)66-49(72)17-10-7-11-18-50(73)68-26-23-59(24-27-68)25-28-69(56(59)76)45-30-44(32-61-33-45)65-57-62-34-47(60)51(67-57)43-16-12-15-42(29-43)40-13-8-6-9-14-40/h6,8-9,12-16,19-22,29-30,32-34,36-37,46,48,53,71H,7,10-11,17-18,23-28,31,35H2,1-5H3,(H,64,74)(H,66,72)(H,62,65,67)/t37-,46+,48-,53+/m0/s1
Molecular weight 1078.47 Da
AlogP 9.700619999999997
HBond acceptors 16
HBond donors 4
Atoms 144

Expert Reviews

by SERP
(on 2 Feb 2025 )
Cellular Use Rating
TMX-4153 is a well-characterized and highly potent chemical probe for studying the biological role and therapeutic potential of PIP4K2C. It exhibits nanomolar binding affinity (KD = below 45 nM) and high...
by SERP
(on 20 Feb 2025 )
Cellular Use Rating
TMX-4153 is a potent and selective degrader of PIP4K2C. Selectivity was assessed by a kinome-screen as well as proteomics.
Note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars. Read more about our evaluation criteria