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TP-064 | TP-064 : Inhibitor of CARM1
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
CARM1
  • Kd:7.1 ± 1.8 nM
  • ΔTm:+ 6 °C
  • IC50:340 nM
  • IC50:42 nM
Inhibitor
up to 1 uM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
TP-064 showed high selectivity for PRMT4 over other PRMTs (> 100 fold). It was inactive against the ...

Potency
Cellular
In Vitro

CARM1

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.18632/oncotarget.24883

Negative Control Compounds

N-((2-(1-(2-methoxyethyl)piperidin-4-yl)pyridin-4-yl)methyl)-N-methyl-3-phenoxybenzamide
Notes: TP-060N inhibitory activity against PRMT4 IC50 2.5 ± 0.6 μM

Chemical Information

Molecular Formula C28H34N4O2
SMILEs CNCCN1CCC(c2cc(CN(C)C(=O)c3cccc(Oc4ccccc4)c3)ccn2)CC1
InChI InChI=1S/C28H34N4O2/c1-29-15-18-32-16-12-23(13-17-32)27-19-22(11-14-30-27)21-31(2)28(33)24-7-6-10-26(20-24)34-25-8-4-3-5-9-25/h3-11,14,19-20,23,29H,12-13,15-18,21H2,1-2H3
Molecular weight 458.27 Da
AlogP 4.544900000000004
HBond acceptors 6
HBond donors 1
Atoms 68

Vendors

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Expert Reviews

by SERP+
(on 22 Mar 2023 )
Cellular Use Rating
( The reviewer did not leave any comments )
by SERP+
(on 17 Jun 2024 )
Cellular Use Rating
Highly potent probe with very good selectivity against other PRMTs and 24 other protein lysine methyltransferases. Structurally very similar negative control compound also tested regarding the selectivity...

Portal Comments

In a 2023 study, Hu et al. evaluated TP-064 in live-cell assays for Phospholipidosis induction, cautioning about adverse effects at concentrations near 1 uM. (DOI:10.1016/j.chembiol.2023.09.003)

(last updated: 7 Nov 2023)

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