Cat. No.: HY-50698

BI 2536

59 Cited Publications

Customer Review

Based on 59 publication(s) in Google Scholar

BI 2536 is a dual PLK1 and BRD4 inhibitor with IC₅₀s of 0.83 and 25 nM, respectively. BI-2536 suppresses IFNB (encoding IFN-β) gene transcription.

For research use only. We do not sell to patients.

The BI 2536 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.

Purity: 99.92%
CAS No.: 755038-02-9
Formula: C₂₈H₃₉N₇O₃
Molecular Weight:521.65

Storage:

4°C, protect from light

* In solvent : -80°C, 1 year; -20°C, 6 months (protect from light)

BI 2536 Chemical Structure

CAS No.: 755038-02-9

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (59)
Solvent & Solubility
- In Vitro
- In Vivo
Protocol
Purity & Documentation
References
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Classifications
Bioz

Biological Activity

Description

BI 2536 is a dual PLK1 and BRD4 inhibitor with IC₅₀s of 0.83 and 25 nM, respectively^[1]. BI-2536 suppresses IFNB (encoding IFN-β) gene transcription^[4].

IC₅₀ & Target^[1]

PLK1

0.83 nM (IC₅₀)

Plk2/Snk

3.5 nM (IC₅₀)

Plk3/Fnk

9 nM (IC₅₀)

BRD4

25 nM (IC₅₀)

All Polo-like Kinase (PLK) Isoforms :

All Epigenetic Reader Domain Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A-375	EC₅₀	2 nM Compound: Chemical probe : BI 2536	Antiproliferative activity against human A-375 cells assessed as inhibition in cell growth incubated for 72 hrs by Alamar Blue dye based fluorescence spectrophotometric analysis Antiproliferative activity against human A-375 cells assessed as inhibition in cell growth incubated for 72 hrs by Alamar Blue dye based fluorescence spectrophotometric analysis	[PMID: 17291758]
A-431	EC₅₀	2 nM Compound: Chemical probe : BI 2536	Antiproliferative activity against TP53 mutant human A-431 cells assessed as inhibition in cell growth incubated for 72 hrs by Alamar Blue dye based fluorescence spectrophotometric analysis Antiproliferative activity against TP53 mutant human A-431 cells assessed as inhibition in cell growth incubated for 72 hrs by Alamar Blue dye based fluorescence spectrophotometric analysis	[PMID: 17291758]
A549	EC₅₀	2 nM Compound: Chemical probe : BI 2536	Antiproliferative activity against KRAS mutant human A549 cells assessed as inhibition in cell growth incubated for 72 hrs by Alamar Blue dye based fluorescence spectrophotometric analysis Antiproliferative activity against KRAS mutant human A549 cells assessed as inhibition in cell growth incubated for 72 hrs by Alamar Blue dye based fluorescence spectrophotometric analysis	[PMID: 17291758]
A549	GI₅₀	0.057 μM Compound: BI 2536	Antiproliferative activity against human A549 cells after 72 hrs by CCK8 assay Antiproliferative activity against human A549 cells after 72 hrs by CCK8 assay	[PMID: 29220793]
A549	GI₅₀	57.1 nM Compound: BI 2536	Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 31629162]
A549	IC₅₀	0.05 μM Compound: BI-2536	Antiproliferative activity against human A549 cells assessed as reduction in cell viability by MTT assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability by MTT assay	[PMID: 32631534]
BXPC-3	EC₅₀	2 nM Compound: Chemical probe : BI 2536	Antiproliferative activity against TP53 mutant human BXPC-3 cells assessed as inhibition in cell growth incubated for 72 hrs by Alamar Blue dye based fluorescence spectrophotometric analysis Antiproliferative activity against TP53 mutant human BXPC-3 cells assessed as inhibition in cell growth incubated for 72 hrs by Alamar Blue dye based fluorescence spectrophotometric analysis	[PMID: 17291758]
COLO 205	EC₅₀	2 nM Compound: Chemical probe : BI 2536	Antiproliferative activity against human COLO 205 cells assessed as inhibition in cell growth incubated for 72 hrs by Alamar Blue dye based fluorescence spectrophotometric analysis Antiproliferative activity against human COLO 205 cells assessed as inhibition in cell growth incubated for 72 hrs by Alamar Blue dye based fluorescence spectrophotometric analysis	[PMID: 17291758]
DOHH-2	EC₅₀	2 nM Compound: Chemical probe : BI 2536	Antiproliferative activity against human DOHH-2 cells assessed as inhibition in cell growth incubated for 72 hrs by Alamar Blue dye based fluorescence spectrophotometric analysis Antiproliferative activity against human DOHH-2 cells assessed as inhibition in cell growth incubated for 72 hrs by Alamar Blue dye based fluorescence spectrophotometric analysis	[PMID: 17291758]
DU-145	EC₅₀	2 nM Compound: Chemical probe : BI 2536	Antiproliferative activity against TP53 mutant human DU-145 cells assessed as inhibition in cell growth incubated for 72 hrs by Alamar Blue dye based fluorescence spectrophotometric analysis Antiproliferative activity against TP53 mutant human DU-145 cells assessed as inhibition in cell growth incubated for 72 hrs by Alamar Blue dye based fluorescence spectrophotometric analysis	[PMID: 17291758]
FaDu	EC₅₀	2 nM Compound: Chemical probe : BI 2536	Antiproliferative activity against TP53 mutant human FaDu cells assessed as inhibition in cell growth incubated for 72 hrs by Alamar Blue dye based fluorescence spectrophotometric analysis Antiproliferative activity against TP53 mutant human FaDu cells assessed as inhibition in cell growth incubated for 72 hrs by Alamar Blue dye based fluorescence spectrophotometric analysis	[PMID: 17291758]
Granta-519	EC₅₀	2 nM Compound: Chemical probe : BI 2536	Antiproliferative activity against human Granta-519 cells assessed as inhibition in cell growth incubated for 72 hrs by Alamar Blue dye based fluorescence spectrophotometric analysis Antiproliferative activity against human Granta-519 cells assessed as inhibition in cell growth incubated for 72 hrs by Alamar Blue dye based fluorescence spectrophotometric analysis	[PMID: 17291758]
H4	EC₅₀	2 nM Compound: Chemical probe : BI 2536	Antiproliferative activity against PTEN mutant human H4 cells assessed as inhibition in cell growth incubated for 72 hrs by Alamar Blue based fluorescence spectrophotometric analysis Antiproliferative activity against PTEN mutant human H4 cells assessed as inhibition in cell growth incubated for 72 hrs by Alamar Blue based fluorescence spectrophotometric analysis	[PMID: 17291758]
HCT-116	EC₅₀	2 nM Compound: Chemical probe : BI 2536	Antiproliferative activity against KRAS mutant human HCT-116 cells assessed as inhibition in cell growth incubated for 72 hrs by Alamar Blue dye based fluorescence spectrophotometric analysis Antiproliferative activity against KRAS mutant human HCT-116 cells assessed as inhibition in cell growth incubated for 72 hrs by Alamar Blue dye based fluorescence spectrophotometric analysis	[PMID: 17291758]
HCT-116	IC₅₀	13.6 nM Compound: BI2536	Antiproliferative activity against human HCT-116 cells incubated for 72 to 96 hrs by microplate reader analysis Antiproliferative activity against human HCT-116 cells incubated for 72 to 96 hrs by microplate reader analysis	[PMID: 36889251]
HCT-116	IC₅₀	2.03 μM Compound: BI-2536	Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability by MTT assay Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability by MTT assay	[PMID: 32631534]
HEK293	IC₅₀	0.3 μM Compound: BI-2536	Inhibition of full-length C-terminal NanoLuc-tagged BRD4 BD1 (unknown origin) expressed in human HEK293 cells after 2 hrs by NanoBRET target engagement assay Inhibition of full-length C-terminal NanoLuc-tagged BRD4 BD1 (unknown origin) expressed in human HEK293 cells after 2 hrs by NanoBRET target engagement assay	[PMID: 30789735]
HEK293	IC₅₀	0.89 μM Compound: BI-2536	Inhibition of full-length C-terminal NanoLuc-tagged ALK (unknown origin) expressed in human HEK293 cells after 2 hrs by NanoBRET target engagement assay Inhibition of full-length C-terminal NanoLuc-tagged ALK (unknown origin) expressed in human HEK293 cells after 2 hrs by NanoBRET target engagement assay	[PMID: 30789735]
HEK-293T	IC₅₀	0.6 nM Compound: B12536	Inhibition of cell growth in HEK293T cells incubated for 72 hrs by CellTiter-blue reagent based assay Inhibition of cell growth in HEK293T cells incubated for 72 hrs by CellTiter-blue reagent based assay	[PMID: 34710325]
HEK-293T	IC₅₀	1 nM Compound: BI-2536	Antiproliferative activity against HEK293T cells measured after 72 hrs by CellTiter-Blue assay Antiproliferative activity against HEK293T cells measured after 72 hrs by CellTiter-Blue assay	[PMID: 28792760]
HeLa	GI₅₀	0.034 μM Compound: BI 2536	Antiproliferative activity against human HeLa cells after 72 hrs by CCK8 assay Antiproliferative activity against human HeLa cells after 72 hrs by CCK8 assay	[PMID: 29220793]
HeLa	GI₅₀	34 nM Compound: BI 2536	Antiproliferative activity against human HeLa cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human HeLa cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 31629162]
HeLa S3	EC₅₀	2 nM Compound: Chemical probe : BI 2536	Antiproliferative activity against human HeLa S3 cells assessed as inhibition in cell growth incubated for 72 hrs by Alamar Blue dye based fluorescence spectrophotometric analysis Antiproliferative activity against human HeLa S3 cells assessed as inhibition in cell growth incubated for 72 hrs by Alamar Blue dye based fluorescence spectrophotometric analysis	[PMID: 17291758]
HepG2	EC₅₀	2 nM Compound: Chemical probe : BI 2536	Antiproliferative activity against human HepG2 cells assessed as inhibition in cell growth incubated for 72 hrs by Alamar Blue dye based fluorescence spectrophotometric analysis Antiproliferative activity against human HepG2 cells assessed as inhibition in cell growth incubated for 72 hrs by Alamar Blue dye based fluorescence spectrophotometric analysis	[PMID: 17291758]
HL-60	EC₅₀	2 nM Compound: Chemical probe : BI 2536	Antiproliferative activity against human HL-60 cells assessed as inhibition in cell growth incubated for 72 hrs by Alamar Blue dye based fluorescence spectrophotometric analysis Antiproliferative activity against human HL-60 cells assessed as inhibition in cell growth incubated for 72 hrs by Alamar Blue dye based fluorescence spectrophotometric analysis	[PMID: 17291758]
HL-60	IC₅₀	3.42 μM Compound: BI-2536	Antiproliferative activity against human HL60 cells incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human HL60 cells incubated for 72 hrs by CCK-8 assay	[PMID: 31079968]
HL-60	IC₅₀	36.5 nM Compound: 1	Cytotoxicity against BRD4 dependent human HL60 cells assessed as cell viability after 3 days by ATPlite assay Cytotoxicity against BRD4 dependent human HL60 cells assessed as cell viability after 3 days by ATPlite assay	[PMID: 26985285]
HRPE	IC₅₀	>600 nM Compound: BI2536	Antiproliferative activity against human RPE cells expressing C67V mutant PLK1 assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human RPE cells expressing C67V mutant PLK1 assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 34210138]
HRPE	IC₅₀	27.1 nM Compound: BI2536	Antiproliferative activity against human RPE cells expressing wild-type PLK1 assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human RPE cells expressing wild-type PLK1 assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 34210138]
HT-29	EC₅₀	2 nM Compound: Chemical probe : BI 2536	Antiproliferative activity against TP53 mutant human HT-29 cells assessed as inhibition in cell growth incubated for 72 hrs by Alamar Blue dye based fluorescence spectrophotometric analysis Antiproliferative activity against TP53 mutant human HT-29 cells assessed as inhibition in cell growth incubated for 72 hrs by Alamar Blue dye based fluorescence spectrophotometric analysis	[PMID: 17291758]
Huh-7	GI₅₀	0.028 μM Compound: BI 2536	Antiproliferative activity against human HuH7 cells after 72 hrs by CCK8 assay Antiproliferative activity against human HuH7 cells after 72 hrs by CCK8 assay	[PMID: 29220793]
Huh-7	GI₅₀	28.4 nM Compound: BI 2536	Antiproliferative activity against human HuH7 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human HuH7 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 31629162]
HUVEC	EC₅₀	12 nM Compound: Chemical probe : BI 2536	Cytotoxicity against human HUVEC cells assessed as inhibition in cell growth incubated for 72 hrs by Alamar Blue dye based fluorescence spectrophotometric analysis Cytotoxicity against human HUVEC cells assessed as inhibition in cell growth incubated for 72 hrs by Alamar Blue dye based fluorescence spectrophotometric analysis	[PMID: 17291758]
K562	EC₅₀	2 nM Compound: Chemical probe : BI 2536	Antiproliferative activity against human K562 cells assessed as inhibition in cell growth incubated for 72 hrs by Alamar Blue dye based fluorescence spectrophotometric analysis Antiproliferative activity against human K562 cells assessed as inhibition in cell growth incubated for 72 hrs by Alamar Blue dye based fluorescence spectrophotometric analysis	[PMID: 17291758]
K562	GI₅₀	0.068 μM Compound: BI 2536	Antiproliferative activity against human K562 cells after 72 hrs by CCK8 assay Antiproliferative activity against human K562 cells after 72 hrs by CCK8 assay	[PMID: 29220793]
K562	GI₅₀	60.5 nM Compound: BI 2536	Antiproliferative activity against human K562 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human K562 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 31629162]
MCF7	EC₅₀	2 nM Compound: Chemical probe : BI 2536	Antiproliferative activity against TP53 mutant human MCF7 cells assessed as inhibition in cell growth incubated for 72 hrs by Alamar Blue dye based fluorescence spectrophotometric analysis Antiproliferative activity against TP53 mutant human MCF7 cells assessed as inhibition in cell growth incubated for 72 hrs by Alamar Blue dye based fluorescence spectrophotometric analysis	[PMID: 17291758]
MCF7	GI₅₀	0.067 μM Compound: BI 2536	Antiproliferative activity against human MCF7 cells after 72 hrs by CCK8 assay Antiproliferative activity against human MCF7 cells after 72 hrs by CCK8 assay	[PMID: 29220793]
MCF7	GI₅₀	67 nM Compound: BI 2536	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 31629162]
MCF7	IC₅₀	12.5 nM Compound: BI2536	Antiproliferative activity against human MCF7 cells incubated for 72 to 96 hrs by microplate reader analysis Antiproliferative activity against human MCF7 cells incubated for 72 to 96 hrs by microplate reader analysis	[PMID: 36889251]
MDA-MB-231	IC₅₀	1 nM Compound: BI-2536	Antiproliferative activity against human MDA-MB-231 cells measured after 72 hrs by CellTiter-Blue assay Antiproliferative activity against human MDA-MB-231 cells measured after 72 hrs by CellTiter-Blue assay	[PMID: 28792760]
MDA-MB-231	IC₅₀	28.9 nM Compound: BI 2536	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 to 96 hrs by alamar blue assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 to 96 hrs by alamar blue assay	[PMID: 38364599]
MDA-MB-231	IC₅₀	55.6 nM Compound: BI2536	Antiproliferative activity against human MDA-MB-231 cells incubated for 72 to 96 hrs by microplate reader analysis Antiproliferative activity against human MDA-MB-231 cells incubated for 72 to 96 hrs by microplate reader analysis	[PMID: 36889251]
MDA-MB-361	IC₅₀	5.1 nM Compound: BI 2536	Antiproliferative activity against human MDA-MB-361 cells assessed as inhibition of cell growth incubated for 72 to 96 hrs by alamar blue assay Antiproliferative activity against human MDA-MB-361 cells assessed as inhibition of cell growth incubated for 72 to 96 hrs by alamar blue assay	[PMID: 38364599]
MDA-MB-435S	EC₅₀	2 nM Compound: Chemical probe : BI 2536	Antiproliferative activity against TP53 mutant human MDA-MB-435S cells assessed as inhibition in cell growth incubated for 72 hrs by Alamar Blue dye based fluorescence spectrophotometric analysis Antiproliferative activity against TP53 mutant human MDA-MB-435S cells assessed as inhibition in cell growth incubated for 72 hrs by Alamar Blue dye based fluorescence spectrophotometric analysis	[PMID: 17291758]
MDCK	CC₅₀	1.8 μM Compound: 59; BI-2536	Cytotoxicity against MDCK cells Cytotoxicity against MDCK cells	[PMID: 33539089]
MES-SA	EC₅₀	2 nM Compound: Chemical probe : BI 2536	Antiproliferative activity against human MES-SA cells assessed as inhibition in cell growth incubated for 72 hrs by Alamar Blue dye based fluorescence spectrophotometric analysis Antiproliferative activity against human MES-SA cells assessed as inhibition in cell growth incubated for 72 hrs by Alamar Blue dye based fluorescence spectrophotometric analysis	[PMID: 17291758]
MIA PaCa-2	EC₅₀	2 nM Compound: Chemical probe : BI 2536	Antiproliferative activity against TP53/KRAS mutant human MIA PaCa-2 cells assessed as inhibition in cell growth incubated for 72 hrs by Alamar Blue dye based fluorescence spectrophotometric analysis Antiproliferative activity against TP53/KRAS mutant human MIA PaCa-2 cells assessed as inhibition in cell growth incubated for 72 hrs by Alamar Blue dye based fluorescence spectrophotometric analysis	[PMID: 17291758]
MM1.S	IC₅₀	1 nM Compound: BI-2536	Antiproliferative activity against human MM1S cells measured after 72 hrs by CellTiter-Blue assay Antiproliferative activity against human MM1S cells measured after 72 hrs by CellTiter-Blue assay	[PMID: 28792760]
MM1.S	IC₅₀	1.2 nM Compound: B12536	Inhibition of cell growth in human MM1.S cells incubated for 72 hrs by CellTiter-blue reagent based assay Inhibition of cell growth in human MM1.S cells incubated for 72 hrs by CellTiter-blue reagent based assay	[PMID: 34710325]
MV4-11	GI₅₀	0.0152 μM Compound: BI-2536	Cytotoxicity against human MV4-11 cells after 24 hrs by CellTiter-Blue assay Cytotoxicity against human MV4-11 cells after 24 hrs by CellTiter-Blue assay	[PMID: 26191363]
MV4-11	IC₅₀	0.45 μM Compound: BI-2536	Antiproliferative activity against human MV4-11 cells incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human MV4-11 cells incubated for 72 hrs by CCK-8 assay	[PMID: 31079968]
MV4-11	IC₅₀	13.7 nM Compound: BI 2536	Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 72 to 96 hrs by alamar blue assay Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 72 to 96 hrs by alamar blue assay	[PMID: 38364599]
MV4-11	IC₅₀	16.7 nM Compound: BI2536	Antiproliferative activity against human MV4-11 cells incubated for 72 to 96 hrs by microplate reader analysis Antiproliferative activity against human MV4-11 cells incubated for 72 to 96 hrs by microplate reader analysis	[PMID: 36889251]
NCI-H1975	GI₅₀	0.23 μM Compound: BI 2536	Antiproliferative activity against human NCI-H1975 cells after 72 hrs by CCK8 assay Antiproliferative activity against human NCI-H1975 cells after 72 hrs by CCK8 assay	[PMID: 29220793]
NCI-H1975	GI₅₀	130 nM Compound: BI 2536	Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 31629162]
NCI-H460	EC₅₀	2 nM Compound: Chemical probe : BI 2536	Antiproliferative activity against human NCI-H460 cells assessed as inhibition in cell growth incubated for 72 hrs by Alamar Blue dye based fluorescence spectrophotometric analysis Antiproliferative activity against human NCI-H460 cells assessed as inhibition in cell growth incubated for 72 hrs by Alamar Blue dye based fluorescence spectrophotometric analysis	[PMID: 17291758]
NCI-H520	EC₅₀	2 nM Compound: Chemical probe : BI 2536	Antiproliferative activity against TP53 mutant human NCI-H520 cells assessed as inhibition in cell growth incubated for 72 hrs by Alamar Blue dye based fluorescence spectrophotometric analysis Antiproliferative activity against TP53 mutant human NCI-H520 cells assessed as inhibition in cell growth incubated for 72 hrs by Alamar Blue dye based fluorescence spectrophotometric analysis	[PMID: 17291758]
NCI-N87	EC₅₀	2 nM Compound: Chemical probe : BI 2536	Antiproliferative activity against human NCI-N87 cells assessed as inhibition in cell growth incubated for 72 hrs by Alamar Blue dye based fluorescence spectrophotometric analysis Antiproliferative activity against human NCI-N87 cells assessed as inhibition in cell growth incubated for 72 hrs by Alamar Blue dye based fluorescence spectrophotometric analysis	[PMID: 17291758]
NRK	EC₅₀	12 nM Compound: Chemical probe : BI 2536	Cytotoxicity against rat NRK cells assessed as inhibition in cell growth incubated for 72 hrs by Alamar Blue dye based fluorescence spectrophotometric analysis Cytotoxicity against rat NRK cells assessed as inhibition in cell growth incubated for 72 hrs by Alamar Blue dye based fluorescence spectrophotometric analysis	[PMID: 17291758]
PANC-1	EC₅₀	2 nM Compound: Chemical probe : BI 2536	Antiproliferative activity against TP53/KRAS mutant human PANC-1 cells assessed as inhibition in cell growth incubated for 72 hrs by Alamar Blue dye based fluorescence spectrophotometric analysis Antiproliferative activity against TP53/KRAS mutant human PANC-1 cells assessed as inhibition in cell growth incubated for 72 hrs by Alamar Blue dye based fluorescence spectrophotometric analysis	[PMID: 17291758]
PC-3	EC₅₀	2 nM Compound: Chemical probe : BI 2536	Antiproliferative activity against TP53/PTEN mutant human PC-3 cells assessed as inhibition in cell growth incubated for 72 hrs by Alamar Blue dye based fluorescence spectrophotometric analysis Antiproliferative activity against TP53/PTEN mutant human PC-3 cells assessed as inhibition in cell growth incubated for 72 hrs by Alamar Blue dye based fluorescence spectrophotometric analysis	[PMID: 17291758]
PC-3	IC₅₀	0.46 μM Compound: BI-2536	Antiproliferative activity against human PC3 cells assessed as reduction in cell viability by MTT assay Antiproliferative activity against human PC3 cells assessed as reduction in cell viability by MTT assay	[PMID: 32631534]
Raji	EC₅₀	2 nM Compound: Chemical probe : BI 2536	Antiproliferative activity against TP53 mutant human Raji cells assessed as inhibition in cell growth incubated for 72 hrs by Alamar Blue dye based fluorescence spectrophotometric analysis Antiproliferative activity against TP53 mutant human Raji cells assessed as inhibition in cell growth incubated for 72 hrs by Alamar Blue dye based fluorescence spectrophotometric analysis	[PMID: 17291758]
SAOS-2	EC₅₀	2 nM Compound: Chemical probe : BI 2536	Antiproliferative activity against human SAOS-2 cells assessed as inhibition in cell growth inhibition incubated for 72 hrs by Alamar Blue based fluorescence spectrophotometric analysis Antiproliferative activity against human SAOS-2 cells assessed as inhibition in cell growth inhibition incubated for 72 hrs by Alamar Blue based fluorescence spectrophotometric analysis	[PMID: 17291758]
SK-MEL-28	EC₅₀	2 nM Compound: Chemical probe : BI 2536	Antiproliferative activity against TP53 mutant human SK-MEL-28 cells assessed as inhibition in cell growth incubated for 72 hrs by Alamar Blue dye based fluorescence spectrophotometric analysis Antiproliferative activity against TP53 mutant human SK-MEL-28 cells assessed as inhibition in cell growth incubated for 72 hrs by Alamar Blue dye based fluorescence spectrophotometric analysis	[PMID: 17291758]
SK-OV-3	EC₅₀	2 nM Compound: Chemical probe : BI 2536	Antiproliferative activity against TP53 mutant human SK-OV-3 cells assessed as inhibition in cell growth incubated for 72 hrs by Alamar Blue dye based fluorescence spectrophotometric analysis Antiproliferative activity against TP53 mutant human SK-OV-3 cells assessed as inhibition in cell growth incubated for 72 hrs by Alamar Blue dye based fluorescence spectrophotometric analysis	[PMID: 17291758]
Skut1B	EC₅₀	2 nM Compound: Chemical probe : BI 2536	Antiproliferative activity against TP53/PTEN mutant human Skut1B cells assessed as inhibition in cell growth incubated for 72 hrs by Alamar Blue dye based fluorescence spectrophotometric analysis Antiproliferative activity against TP53/PTEN mutant human Skut1B cells assessed as inhibition in cell growth incubated for 72 hrs by Alamar Blue dye based fluorescence spectrophotometric analysis	[PMID: 17291758]
TERT-RPE1	EC₅₀	12 nM Compound: Chemical probe : BI 2536	Cytotoxicity against human hTERT-RPE1 cells assessed as inhibition in cell growth incubated for 72 hrs by Alamar Blue dye based fluorescence spectrophotometric analysis Cytotoxicity against human hTERT-RPE1 cells assessed as inhibition in cell growth incubated for 72 hrs by Alamar Blue dye based fluorescence spectrophotometric analysis	[PMID: 17291758]
THP-1	EC₅₀	2 nM Compound: Chemical probe : BI 2536	Antiproliferative activity against TP53 mutant human THP-1 cells assessed as inhibition in cell growth incubated for 72 hrs by Alamar Blue dye based fluorescence spectrophotometric analysis Antiproliferative activity against TP53 mutant human THP-1 cells assessed as inhibition in cell growth incubated for 72 hrs by Alamar Blue dye based fluorescence spectrophotometric analysis	[PMID: 17291758]

In Vitro

Exceeding a 100-fold concentration range starting at 10 nM, BI 2536 causes HeLa cells to accumulate with a 4N DNA content, indicative of a cell-cycle block in either G2 phase or mitosis. In addition to HeLa cells, BI 2536 potently inhibits the proliferation of a panel of 32 human cancer cell lines, representing diverse organ derivations (including carcinomas of the breast, colon, lung, pancreas, and prostate, melanomas, and hematopoietic cancers) and varied patterns of tumor suppressor or oncogene mutations (including RB1, TP53, PTEN, andKRAS status). The half-maximal effective concentration (EC₅₀) values in this cell panel ranged 2-25 nM, whereas a concentration of 100 nM of BI 2536 is typically sufficient for inducing a complete mitotic arrest. The proliferation of exponentially growing hTERT-RPE1, human umbilical vein endothelial cells (HUVECs), and normal rat kidney (NRK) cells is blocked at EC₅₀values ranging 12-31 nM, indicating a comparable sensitivity of cycling nontransformed cells to BI 2536^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

BI 2536 (40-50 mg/kg, i.v.) blocks the growth of human cancer xenografts in immunodeficient, nu/nu mice. Consecutive cycles of 40-50 mg/kg BI 2536 given i.v. once or twice per week are found to be highly efficacious in diverse xenograft models, such as the HCT 116 colon cancer with complete tumor suppression with the twice per week schedule (treated versus the control (T/C) value 0.3%) and a T/C value of 16% with once per week treatment; both schedules are well-tolerated, as judged by clinical signs and absence of major body-weight changes^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS No. 755038-02-9
Appearance Solid
Molecular Weight 521.65
Formula C₂₈H₃₉N₇O₃
Color White to light yellow
SMILES

O=C1[C@H](N(C2=C(N1C)C=NC(NC3=CC=C(C(NC4CCN(C)CC4)=O)C=C3OC)=N2)C5CCCC5)CC
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

* In solvent : -80°C, 1 year; -20°C, 6 months (protect from light)

Publications (59)

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Mol Cancer

The phospholipid transporter PITPNC1 links KRAS to MYC to prevent autophagy in lung and pancreatic cancer. [Abstract]

2023 May 20;22(1):86. PMID: 37210549
Sci Bull

The mechanisms of MTOCs maturation in human and mouse oocytes. [Abstract]

2025 Aug 11:S2095-9273(25)00813-8. PMID: 40903356
Cancer Res

An In Vivo CRISPR Screen Identifies Stepwise Genetic Dependencies of Metastatic Progression. [Abstract]

2022 Feb 15;82(4):681-694. PMID: 34916221
Cancer Res

Hsp72 and Nek6 Cooperate to Cluster Amplified Centrosomes in Cancer Cells. [Abstract]

2017 Sep 15;77(18):4785-4796. PMID: 28720575
Nat Commun

CRISPR knockout screening identifies combinatorial drug targets in pancreatic cancer and models cellular drug response. [Abstract]

2018 Oct 15;9(1):4275. PMID: 30323222
Nat Commun

Coupling of Polo kinase activation to nuclear localization by a bifunctional NLS is required during mitotic entry. [Abstract]

2017 Nov 22;8(1):1701. PMID: 29167465

BI 2536 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2017 Nov 22;8(1):1701. [Abstract]

Cells are transfected and treated with BI 2536 as indicated and were fractionated into cytoplasmic (C) and nuclear (N) fractions analyzed by Western blots. The position of Cdc25 and its phosphorylated forms are indicated by arrows. MEK and Histone H3 are respectively cytoplasmic and nuclear proteins probed as controls.
Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
Leukemia

Unraveling the impact of crizotinib to promote megakaryopoiesis for alleviating thrombocytopenia in myelodysplastic neoplasms. [Abstract]

2025 Aug 14. PMID: 40813622
Biomark Res

Gasdermin E benefits CD8+T cell mediated anti-immunity through mitochondrial damage to activate cGAS-STING-interferonβ axis in colorectal cancer. [Abstract]

2024 Jun 9;12(1):59. PMID: 38853246
Cell Death Dis

Distinct outcomes of CRL-Nedd8 pathway inhibition reveal cancer cell plasticity. [Abstract]

2016 Dec 1;7(12):e2505. PMID: 27906189
Proc Natl Acad Sci U S A

MGMT-activated DUB3 stabilizes MCL1 and drives chemoresistance in ovarian cancer. [Abstract]

2019 Feb 19;116(8):2961-2966. PMID: 30718431
Cell Commun Signal

Reversible arginine methylation of PI3KC2α controls mitotic spindle dynamics. [Abstract]

2025 Oct 2;23(1):409. PMID: 41039590
EMBO J

PLK1 inhibition delays mitotic entry revealing changes to the phosphoproteome of mammalian cells early in division. [Abstract]

2025 Apr;44(7):1891-1920. PMID: 40033019
EMBO J

CEP192 localises mitotic Aurora-A activity by priming its interaction with TPX2. [Abstract]

2024 Nov;43(22):5381-5420. PMID: 39327527
Apoptosis

Copper modulates cell fate through the PLK1-FOXO3a-β-catenin signaling pathway by differentially regulating cuproptosis and EMT. [Abstract]

2026 Jan 10;31(1):12. PMID: 41518407
NPJ Precis Oncol

Consensus artificial intelligence-driven prognostic signature for predicting the prognosis of hepatocellular carcinoma: a multi-center and large-scale study. [Abstract]

2025 Jul 1;9(1):207. PMID: 40595395
Biomed Pharmacother

Overcoming PLK1 inhibitor resistance by targeting mevalonate pathway to impair AXL-TWIST axis in colorectal cancer. [Abstract]

2021 Dec:144:112347. PMID: 34700228
Cell Rep

Extracellular matrix stiffness drives post-mitotic nuclear pore complex assembly to promote neuroblastoma pathogenesis. [Abstract]

2026 Jan 22;45(2):116858. PMID: 41575851
Cell Rep

Activation of polo-like kinase 1 correlates with selective motor neuron vulnerability in familial ALS. [Abstract]

2025 Aug 25;44(9):116113. PMID: 40857153
Cell Rep

Polo-like kinase 2 promotes microglial activation via regulation of the HSP90α/IKKβ pathway. [Abstract]

2024 Oct 8;43(10):114827. PMID: 39383034
J Cell Biol

Adapting plasma membrane for mitotic cell rounding through Aurora A phosphorylation of numb. [Abstract]

2025 Dec 1;224(12):e202412005. PMID: 41212116
J Cell Biol

DNA damage promotes microtubule dynamics through a DNA-PK-AKT axis for enhanced repair. [Abstract]

2021 Feb 1;220(2):e201911025. PMID: 33404607
Elife

Rapid changes in tissue mechanics regulate cell behaviour in the developing embryonic brain. [Abstract]

2019 Jan 15:8:e39356. PMID: 30642430
Cell Biosci

Multi-omics analysis of the HMGB2+ tumor epithelial cells in lactylation subgroups in colorectal cancer. [Abstract]

2025 Nov 19;15(1):158. PMID: 41261427
EMBO Rep

The GCN2/eIF2αK stress kinase regulates PP1 to ensure mitotic fidelity. [Abstract]

2023 Aug 3;24(8):e56100. PMID: 37291955
EMBO Rep

CK1-mediated phosphorylation of FAM110A promotes its interaction with mitotic spindle and controls chromosomal alignment. [Abstract]

2021 Jul 5;22(7):e51847. PMID: 34080749
Cancer Cell Int

Construction of a lipid metabolism-based prognostic gene signature in cervical squamous cell carcinoma and validation of LIPG's oncogenic role. [Abstract]

2025 Oct 14;25(1):349. PMID: 41088247
Biochem Pharmacol

STING activation in macrophages by vanillic acid exhibits antineoplastic potential. [Abstract]

2023 Jul:213:115618. PMID: 37211172
Pharmaceutics

Navitoclax Enhances the Therapeutic Effects of PLK1 Targeting on Lung Cancer Cells in 2D and 3D Culture Systems. [Abstract]

2022 Jun 6;14(6):1209. PMID: 35745782
Mol Cancer Ther

Essential Role of Polo-like Kinase 1 (Plk1) Oncogene in Tumor Growth and Metastasis of Tamoxifen-Resistant Breast Cancer. [Abstract]

2018 Apr;17(4):825-837. PMID: 29437878

BI 2536 purchased from MedChemExpress. Usage Cited in: Mol Cancer Ther. 2018 Apr;17(4):825-837. [Abstract]

Effect of Plk1 inhibitor on cell proliferation of TAMR-MCF-7 cells. Effects of BI2536 on Plk1 signaling in TAMR-MCF-7 cells. TAMR-MCF-7 cells are incubated with BI2536 (1, 5 and 10 nM) for 24 h and total cell lysates are subjected to immunoblottings for Plk1, Cdc25c and Cyclin B1.
Cells

Mitotic Acetylation of Microtubules Promotes Centrosomal PLK1 Recruitment and Is Required to Maintain Bipolar Spindle Homeostasis. [Abstract]

2021 Jul 22;10(8):1859. PMID: 34440628
Int Immunopharmacol

BI-2536 attenuates IPF progression by inhibiting the PLK2/JNK/SP1 Signaling pathway in AT2 cells. [Abstract]

2026 Jan 1;168(Pt 1):115812. PMID: 41237696
Int Immunopharmacol

Comprehensive quantifications of tumour microenvironment to predict the responsiveness to immunotherapy and prognosis for paediatric neuroblastomas. [Abstract]

2024 May 30:133:112145. PMID: 38691920
iScience

The matricellular protein Fibulin-5 regulates β-cell proliferation in an autocrine/paracrine manner. [Abstract]

2025 Jan 21;28(2):111856. PMID: 39995864
iScience

Pathogenic LRRK2 regulates centrosome cohesion via Rab10/RILPL1-mediated CDK5RAP2 displacement. [Abstract]

2022 May 30;25(6):104476. PMID: 35721463
Sci Rep

Identification of Polo-like kinase 1 interaction inhibitors using a novel cell-based assay. [Abstract]

2016 Nov 22;5:37581. PMID: 27874094
PLoS Genet

Genetic enhancers of partial PLK1 inhibition reveal hypersensitivity to kinetochore perturbations. [Abstract]

2023 Aug 28;19(8):e1010903. PMID: 37639469
J Photochem Photobiol B

Shedding light on the binding mechanism of kinase inhibitors BI-2536, Volasetib and Ro-3280 with their pharmacological target PLK1. [Abstract]

2022 Jul:232:112477. PMID: 35644070
J Photochem Photobiol B

Binding of the anticancer drug BI-2536 to human serum albumin. A spectroscopic and theoretical study. [Abstract]

2017 Jul:172:77-87. PMID: 28531794
J Cell Sci

14-3-3ε inhibits premature centriole disengagement by inhibiting the activity of Plk1 and separase. [Abstract]

2025 Jun 27:jcs.263808. PMID: 40576425
Development

PPP4C facilitates homologous recombination DNA repair by dephosphorylating PLK1 during early embryo development. [Abstract]

2022 May 15;149(10):dev200351. PMID: 35546066
PLoS Negl Trop Dis

Structure-Bioactivity Relationship for Benzimidazole Thiophene Inhibitors of Polo-Like Kinase 1 (PLK1), a Potential Drug Target in Schistosoma mansoni. [Abstract]

2016 Jan 11;10(1):e0004356. PMID: 26751972
Naunyn Schmiedebergs Arch Pharmacol

Overexpression of KIF2C amplifies tamoxifen resistance and lung metastasis of breast cancer through PLK1/C-Myc pathway. [Abstract]

2025 Mar 18. PMID: 40100379
Vet Microbiol

PRV-encoded UL13 protein kinase acts as an antagonist of innate immunity by targeting IRF3-signaling pathways. [Abstract]

2020 Nov;250:108860. PMID: 33045632
Eur J Neurosci

Characterization and Regulation of Alpha-Synuclein Phosphorylation in Enteric Neurons. [Abstract]

2025 Jul;62(2):e70198. PMID: 40673719
Cancer Chemother Pharmacol

A polo-like kinase 1 inhibitor enhances erastin sensitivity in head and neck squamous cell carcinoma cells in vitro. [Abstract]

2024 Aug;94(2):183-195. PMID: 38536443
Oncol Lett

PLK1 inhibition leads to mitotic arrest and triggers apoptosis in cholangiocarcinoma cells. [Abstract]

2024 May 14;28(1):316. PMID: 38807667
Oncol Lett

Expression of FOXM1 and PLK1 predicts prognosis of patients with hepatocellular carcinoma. [Abstract]

2022 May;23(5):146. PMID: 35350587
Res Sq

2026 Mar 24.
bioRxiv

2026 Feb 25.
AUTHOREA

2025 May 27.
bioRxiv

2024 Jul 25.
bioRxiv

Regulated Induced Proximity Targeting Chimeras (RIPTACs): a Novel Heterobifunctional Small Molecule Therapeutic Strategy for Killing Cancer Cells Selectively. [Abstract]

2023 Jan 2:2023.01.01.522436. PMID: 36711980
Research Square Preprint

2021 Jan.
University of Cambridge

2018 Aug.
Patent

US20180235964A1.
University of California

2016.
Seoul National University

2015 Feb.

BI 2536 purchased from MedChemExpress. Usage Cited in: Seoul National University. 2015 Feb.

Plk1 inhibition-mediated down-regulation of cdc25c and up-regulation of cyclin B1 in TAMR-MCF-7. BI 2536 (1, 5 and 10 nM) is treated for either 24 h or 48 h.
J Biomol Screen

Differential determinants of cancer cell insensitivity to antimitotic drugs discriminated by a one-step cell imaging assay. [Abstract]

2013 Oct;18(9):1062-71. PMID: 23788527

Solvent & Solubility

In Vitro:

DMSO : 65 mg/mL (124.60 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

0.1 M HCl : 25 mg/mL (47.92 mM; ultrasonic and adjust pH to 4 with HCl)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.9170 mL

9.5850 mL

19.1699 mL

5 mM

0.3834 mL

1.9170 mL

3.8340 mL

10 mM

0.1917 mL

0.9585 mL

1.9170 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (protect from light). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 3.25 mg/mL (6.23 mM); Clear solution

This protocol yields a clear solution of ≥ 3.25 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (32.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 3.25 mg/mL (6.23 mM); Clear solution

This protocol yields a clear solution of ≥ 3.25 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (32.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (3.99 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 50% PEG300 50% Saline

Solubility: 25 mg/mL (47.92 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocol

Cell Assay^[3]

Cell proliferation assays are performed by incubation in the presence of various concentrations of BI 2536 (10 nM-1 μM) for 72 hr, and cell growth is assessed by the measurement of Alamar Blue dye conversion in a fluorescence spectrophotometer. Effective concentrations at which cellular growth is inhibited by 50% (EC₅₀) are extrapolated from the dose-response curve fit^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[3]

Mice^[3]
Female BomTac:NMRI-Foxn1nu mice are grafted subcutaneously with HCT 116 colon-carcinoma, NCI-H460, or A549 lung-carcinoma cells by subcutaneous injection, respectively, of 2×10⁶, 1×10⁶, and 1×10⁷ cells into the flank of each mouse. When tumors reached a volume of approximately 50 mm³, animals are pair-matched into treatment and control groups of ten mice each. In regression experiments, treatment is not initiated until the mean tumor volume reached 500 mm³. BI 2536 is injected intravenously into the tail vein at the indicated dose and schedule. The administration volume is 10 mL per kg body weight. Tumor volumes are determined three times a week with a caliper. The results are converted to tumor volume (mm³) by the following formula: length×width²×π/6. The weight of the mice is determined as an indicator of tolerability on the same days. For statistical analysis, the treatment group is compared with the vehicle control group in a one-sided (decreasing) exact Wilcoxon test.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 KB)
SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Lénárt P, et al. The Small-Molecule Inhibitor BI 2536 Reveals Novel Insights into Mitotic Roles of Polo-like Kinase 1. Curr Biol. 2007 Feb 20;17(4):304-15. [Content Brief]

[2]. Chen L, et al. BRD4 Structure-Activity Relationships of Dual PLK1 Kinase/BRD4 Bromodomain Inhibitor BI-2536. ACS Med Chem Lett. 2015 May 18;6(7):764-9. [Content Brief]

[3]. Steegmaier M, et al. BI 2536, a Potent and Selective Inhibitor of Polo-like Kinase 1, Inhibits Tumor Growth In Vivo. Current Biology (2007), 17(4), 316-322. [Content Brief]

[4]. Malik N, et al. Suppression of IFN β gene transcription by inhibitors of bromodomain and extra-terminal (BET) family members. Biochem J. 2015 Jun 15;468(3):363-72. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
0.1 M HCl / DMSO	1 mM	1.9170 mL	9.5850 mL	19.1699 mL	47.9249 mL
	5 mM	0.3834 mL	1.9170 mL	3.8340 mL	9.5850 mL
	10 mM	0.1917 mL	0.9585 mL	1.9170 mL	4.7925 mL
	15 mM	0.1278 mL	0.6390 mL	1.2780 mL	3.1950 mL
	20 mM	0.0958 mL	0.4792 mL	0.9585 mL	2.3962 mL
	25 mM	0.0767 mL	0.3834 mL	0.7668 mL	1.9170 mL
	30 mM	0.0639 mL	0.3195 mL	0.6390 mL	1.5975 mL
	40 mM	0.0479 mL	0.2396 mL	0.4792 mL	1.1981 mL
DMSO	50 mM	0.0383 mL	0.1917 mL	0.3834 mL	0.9585 mL
	60 mM	0.0319 mL	0.1597 mL	0.3195 mL	0.7987 mL
	80 mM	0.0240 mL	0.1198 mL	0.2396 mL	0.5991 mL
	100 mM	0.0192 mL	0.0958 mL	0.1917 mL	0.4792 mL

Keywords

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent:

Product Name:
CAS No.:
Species:
Purity:
Quantity:

BI 2536

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

Kinase Inhibitor Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Reprogramming Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Targeted Diversity Library

Anti-Prostate Cancer Compound Library

Heterocyclic Compound Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

Anti-Aging Compound Library Mini

Epigenetics Compound Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) BI 2536

All Polo-like Kinase (PLK) Isoforms

All Epigenetic Reader Domain Isoforms

Biological Activity

Chemical Information

Publications (59)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

BI 2536

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

Kinase Inhibitor Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Reprogramming Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Targeted Diversity Library

Anti-Prostate Cancer Compound Library

Heterocyclic Compound Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

Anti-Aging Compound Library Mini

Epigenetics Compound Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) BI 2536

All Polo-like Kinase (PLK) Isoforms

All Epigenetic Reader Domain Isoforms

Biological Activity

Chemical Information

Publications (59)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

BI 2536 Related Classifications

Cat. No.: HY-50698