SU6656 | SU6656 : ATP Competitive inhibitor of SRC, YES1, LYN, FYN
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (1 reviews)
Control Compounds

Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
SRC
  • IC50:280 nM
  • % in:49-100%
YES1
  • IC50:20 nM
  • % in:49-100 %
LYN
  • IC50:130 nM
  • % in:49-100%
FYN
  • IC50:170 nM
  • % in:49-100%
ATP Competitive
up to 2 uM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
SU6656 does not inhibit the PDGF receptor and exhibited greater-than-6.5-fold selectivity for Src re ...

Potency
Cellular
In Vitro

SRC

Mode of Action: ATP Competitive

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1128/mcb.20.23.9018-9027.2000

YES1

Mode of Action: ATP Competitive

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1128/mcb.20.23.9018-9027.2000

LYN

Mode of Action: ATP Competitive

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1128/mcb.20.23.9018-9027.2000

FYN

Mode of Action: ATP Competitive

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1128/mcb.20.23.9018-9027.2000

In Vivo Validations

Mouse
Dose: 2-4 mg/Kg
Route of delivery: Intraperitoneal

DOI Reference: 10.1128/mcb.20.23.9018-9027.2000

Orthogonal Probes def

eCF506

Chemical Information

Molecular Formula C19H21N3O3S
SMILEs CN(C)S(=O)(=O)c1ccc2c(c1)/C(=C/c1cc3c([nH]1)CCCC3)C(=O)N2
InChI InChI=1S/C19H21N3O3S/c1-22(2)26(24,25)14-7-8-18-15(11-14)16(19(23)21-18)10-13-9-12-5-3-4-6-17(12)20-13/h7-11,20H,3-6H2,1-2H3,(H,21,23)/b16-10-
Molecular weight 371.13 Da
AlogP 2.6365000000000007
HBond acceptors 6
HBond donors 2
Atoms 47

References

Cross References

Vendors

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Expert Reviews


(on 3 Jan 2022 )
Cellular Use Rating
This is a probe first described in 2000. It is useful only as an historical probe, one that was used in hundreds of papers before it became clear that kinase inhibitors could be quite selective and before...
(on 5 Jan 2022 )
Cellular Use Rating
In Model Organisms
Whilst SU-6656 has been shown to inhibit four of the nine Src family kinases with an IC50 less than 1 uM and does not inhibit PDGFRβ at 10 uM, it also hits a number of additional kinases such as Abl, Met,...
(on 19 Jan 2022 )
Cellular Use Rating
SU6656 inhibits kinases of the Src family, with some selectivity over PDGFR. However, SU6656 also inhibits BRSK2 and MST2 with similar potency to its inhibition of Src and Lck. Furthermore, SU6656 inhibits...
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