Chemical Probes logo
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
Download

Probe Summary

More...

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

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

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)

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