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SD-36 | Degrader (PROTAC) of STAT3
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (2 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
STAT3
  • Ki:11 nM
  • Kd:44 nM
  • IC50:10 nM
  • DC50:60 nM
  • DC50:28 nM
Degrader (PROTAC)
100 nM up to 5 uM
5 nM up to 5 uM

Selectivity

In Cell Selectivity Assessment
Potency Assay Off-Target:
Multiplexed quantitative proteomics analysis
Selectivity Assessment Description:
>5000 proteins tested and no observed degradation in 3 different cell lines

Potency
Cellular
In Vitro

STAT3

Mode of Action: Degrader (PROTAC)

Structure-Activity-Relationship data available? No

DOI Reference: 10.1021/acs.jmedchem.9b01530

In Vivo Validations

Mouse
Dose: 25 mg/Kg, 50 mg/Kg, 100 mg/Kg
Route of delivery: Intravenous

DOI Reference: 10.1021/acs.jmedchem.9b01530

Negative Control Compounds

SD-36Me

Chemical Information

Molecular Formula C59H62F2N9O12P
SMILEs NC(=O)CC[C@H](NC(=O)[C@@H]1CC[C@@H]2CCN(C(=O)CCCCCC#Cc3cccc4c3CN(C3CCC(=O)NC3=O)C4=O)C[C@H](NC(=O)c3cc4cc(C(F)(F)P(=O)(O)O)ccc4[nH]3)C(=O)N12)C(=O)NC(c1ccccc1)c1ccccc1
InChI InChI=1S/C59H62F2N9O12P/c60-59(61,83(80,81)82)39-21-23-43-38(31-39)32-45(63-43)54(75)65-46-34-68(51(73)20-11-3-1-2-6-13-35-18-12-19-41-42(35)33-69(57(41)78)47-26-28-50(72)66-55(47)76)30-29-40-22-25-48(70(40)58(46)79)56(77)64-44(24-27-49(62)71)53(74)67-52(36-14-7-4-8-15-36)37-16-9-5-10-17-37/h4-5,7-10,12,14-19,21,23,31-32,40,44,46-48,52,63H,1-3,11,20,22,24-30,33-34H2,(H2,62,71)(H,64,77)(H,65,75)(H,67,74)(H,66,72,76)(H2,80,81,82)/t40-,44+,46+,47?,48+/m1/s1
Molecular weight 1157.42 Da
AlogP 4.504500000000006
HBond acceptors 21
HBond donors 9
Atoms 145

References

Publications

Cross References

canSARChEMBLBindingDB

Vendors

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Expert Reviews

by SERP
(on 4 Nov 2020 )
Cellular Use Rating
In Model Organisms
SD-36 is a potent and selective degrader for STAT3 and STAT3 mutants and highly recommended as a chemical probe. STAT3 is a transcription factor implicated in various human diseases such as cancer....
by SERP
(on 11 Nov 2020 )
Cellular Use Rating
In Model Organisms
Recommend dose-response in cell line of interest and note the (p)STAT3 and CRBN status (by western blot for example). Note: At 10 micromolar the recommended control SD-36Me has an effect on STAT3 dimer...
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