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SGK3-PROTAC1 | SGK3-PROTAC1 : Degrader (PROTAC) of SGK3
RATINGS:
Cellular Use: (2 reviews)

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

Targets Biochemical/Biophysical Potency Cellular Potency
SGK3
  • IC50:300 nM
  • Dmax:65%
Degrader (PROTAC)
300 nM to ensure selective degradation
300 nM, up to 3 uM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
Dundee Kinase panel (140 targets) at 1 µM: Closest off-targets are [% activity remaining] SGK1 (34), ...
In Cell Selectivity Assessment
Potency Assay Off-Target:
Proteomic analysis of HEK293 cells: clean

Potency
Cellular
In Vitro

SGK3

Mode of Action: Degrader (PROTAC)

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acschembio.9b00505

Negative Control Compounds

cisSGK3-PROTAC
Notes: Biochemical assay: IC50 = 600 nM, SGK1 (IC50 = 1.4 µM), S6K1 (IC50 = 1.7 µM); no degradation of SGK3 even at 3 µM. Dundee Kinase panel (140 targets) at 1 µM: Closest off-target is [% activity remaining] RPS6KB1 (20)
SMILES: Cc1ccc(c(c1)S(Nc1ccc(cc1)c1nc(c2cn[nH]c2n1)OC[C@H]1CN(CCCCCCOCCOCCOCC(N[C@H](C(N2C[C@H](C[C@H]2C(NCc2ccc(cc2)c2c(C)ncs2)=O)O)=O)C(C)(C)C)=O)CCO1)(=O)=O)F

Chemical Information

Molecular Formula C57H73FN10O11S2
SMILEs Cc1ccc(F)c(S(=O)(=O)Nc2ccc(-c3nc(OC[C@H]4CN(CCCCCCOCCOCCOCC(=O)N[C@H](C(=O)N5C[C@H](O)C[C@H]5C(=O)NCc5ccc(-c6scnc6C)cc5)C(C)(C)C)CCO4)c4cn[nH]c4n3)cc2)c1
InChI InChI=1S/C57H73FN10O11S2/c1-37-10-19-46(58)48(28-37)81(73,74)66-42-17-15-41(16-18-42)52-63-53-45(31-61-65-53)55(64-52)79-34-44-33-67(21-23-78-44)20-8-6-7-9-22-75-24-25-76-26-27-77-35-49(70)62-51(57(3,4)5)56(72)68-32-43(69)29-47(68)54(71)59-30-39-11-13-40(14-12-39)50-38(2)60-36-80-50/h10-19,28,31,36,43-44,47,51,66,69H,6-9,20-27,29-30,32-35H2,1-5H3,(H,59,71)(H,62,70)(H,61,63,64,65)/t43-,44-,47+,51-/m1/s1
Molecular weight 1156.49 Da
AlogP 0.0
HBond acceptors 21
HBond donors 5
Atoms 154

Expert Reviews

by SERP
(on 9 Apr 2024 )
Cellular Use Rating
Excellent probe to study the biology of SGK3 at the concentration where degradation is driven . High selectivity against other member of the same family. There is modest degradation of S6K1 at concentrations...
by SERP+
(on 31 Oct 2024 )
Cellular Use Rating
A specific Dmax value would be nice to have.
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