Chemical Probes logo
INY-06-061 | INY-06-061 : Degrader (PROTAC) of MAPK7
RATINGS:
Cellular Use: (3 reviews)

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

Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
MAPK7
  • Kd:12 nM
  • DC50:21 nM
Degrader (PROTAC)
500 nM to 1 µM
100 nM up to 1 uM, hook effect at 5 uM

Selectivity

In Cell Selectivity Assessment
Potency Assay Off-Target:
INY-06-061 did not destabilize BRD4 or AURKA in MOLT4 cells. MS-based global proteomics profiling a ...
In Vitro Selectivity Assessment
Potency Assay Off-Target:
Biochemical selectivity across 468 kinases was measured through the scanMAX kinase assay panel (Euro ...

Potency
Cellular
In Vitro

MAPK7

Mode of Action: Degrader (PROTAC)

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1016/j.chembiol.2022.09.004

Negative Control Compounds

CANSAR4199069
Notes: INY-06-089 (INY-06-089) enantiomer is not able to degrade ERK5 up to 5 uM. Kd 9 nM in biochemical assay.

Chemical Information

Molecular Formula C54H67F3N10O6S
SMILEs Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCN2CCN(c3ccc4c(C5CCN(C(=O)c6ccc(OC(F)(F)F)cc6N)CC5)ncnc4c3)CC2)C(C)(C)C)cc1
InChI InChI=1S/C54H67F3N10O6S/c1-33(35-10-12-37(13-11-35)48-34(2)61-32-74-48)62-50(70)45-28-39(68)30-67(45)52(72)49(53(3,4)5)63-46(69)9-7-6-8-20-64-23-25-65(26-24-64)38-14-16-42-44(27-38)59-31-60-47(42)36-18-21-66(22-19-36)51(71)41-17-15-40(29-43(41)58)73-54(55,56)57/h10-17,27,29,31-33,36,39,45,49,68H,6-9,18-26,28,30,58H2,1-5H3,(H,62,70)(H,63,69)/t33-,39+,45-,49+/m0/s1
Molecular weight 1040.49 Da
AlogP 0.0
HBond acceptors 16
HBond donors 5
Atoms 141

Vendors

Note: This is not an exhaustive list and does not indicate endorsement by the portal.

Expert Reviews

by SERP
(on 29 Feb 2024 )
Cellular Use Rating
INY-06-061 demonstrates potent and rapid degradation of ERK5 (MAPK7) in cells at sub-micromolar concentrations, but not at supra-micromolar concentrations due to hook effect. Selectivity for ERK5 was shown...
by SERP+
(on 20 Feb 2025 )
Cellular Use Rating
INY-06-061 is a potent ERK5 degrader that is well profiled, showing high binding affinity to the target and also dependency on ubiquitin-proteasome system. Complete data on Dmax is not yet established,...
by SERP+
(on 6 Feb 2026 )
Cellular Use Rating
This is a potent and selective compound (DC50 = 21 nM, no other proteins significantly downregulated in proteomics after 5h 100 nM treatment). The negative control (inactive VHL isomer) has been shown...
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