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BI2536 | BI2536 : ATP competitive inhibitor of PLK1, PLK2, PLK3
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (3 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
PLK1
  • IC50:0.83 nM
PLK2
  • IC50:3.5 nM
PLK3
  • IC50:9 nM
ATP competitive
10-100 nM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
>1,000-fold selective for PLK proteins over 63 additional protein kinases

Potency
Cellular
In Vitro

PLK1

Mode of Action: ATP competitive

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1016/j.cub.2006.12.037

PLK2

Mode of Action: ATP competitive

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1016/j.cub.2006.12.037

PLK3

Mode of Action: ATP competitive

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1016/j.cub.2006.12.037

Chemical Information

Molecular Formula C28H39N7O3
SMILEs CC[C@@H]1C(=O)N(C)c2cnc(Nc3ccc(C(=O)NC4CCN(C)CC4)cc3OC)nc2N1C1CCCC1
InChI InChI=1S/C28H39N7O3/c1-5-22-27(37)34(3)23-17-29-28(32-25(23)35(22)20-8-6-7-9-20)31-21-11-10-18(16-24(21)38-4)26(36)30-19-12-14-33(2)15-13-19/h10-11,16-17,19-20,22H,5-9,12-15H2,1-4H3,(H,30,36)(H,29,31,32)/t22-/m1/s1
Molecular weight 521.31 Da
AlogP 3.5568
HBond acceptors 10
HBond donors 2
Atoms 77

Vendors

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Expert Reviews

by SERP
(on 21 May 2016 )
Cellular Use Rating
In Model Organisms
BI 2536 given i.v. once or twice per week is highly efficacious in diverse xenograft models with acceptable tolerability by inhibiting cell proliferation through a mitotic arrest, and subsequently induction...
by SERP
(on 13 Jun 2016 )
Cellular Use Rating
In Model Organisms
BI-2356 has been subject to kinome profiling (doi:10.1038/nbt.1990). Although it is active against >20 kinases at 1 uM, it is potent and selective for PLK1, PLK2, and to a lesser extent PLK3 at very...
by SERP
(on 13 Dec 2016 )
Cellular Use Rating
In Model Organisms
BI2536 is a potent inhibitor of the PLK kinase family (PLK1/2/3 IC50 0.83/3.5/9.0 nM). Its selectivity was excellent in a protein kinase panel of modest size (63 other kinases). PLK4 was not a member...
BI2536 is a reasonably selective PLK inhibitor (PLK1/2/3) but BI2536 also targets BET bromodomains (10.1021/acsmedchemlett.5b00084). Despite being a PLK1 inhibitor that induces all the hallmarks of...

Portal Comments

BI2536 is a reasonably selective PLK inhibitor (PLK1/2/3) but BI2536 has subsequently been shown to target BET bromodomains (DOI: 10.1021/acsmedchemlett.5b00084). Despite being a PLK1 inhibitor that induces...

(last updated: 12 Mar 2020)

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