BI 2536

Name: BI 2536
Brand: MedChemExpress
SKU: HY-50698
Rating: 5.0 (59 reviews)

Cat. No.: HY-50698 Purity: 99.92%: Data Sheet
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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.

CAS No. : 755038-02-9

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10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 59 publication(s) in Google Scholar

Other Forms of BI 2536:

BI 2536 (GMP) Get quote

59 Publications Citing Use of MCE BI 2536

: 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.

: 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.

: 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.

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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)

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]
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]
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]
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	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]
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]
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]
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]
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]
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]
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.

Molecular Weight

521.65

Formula

C₂₈H₃₉N₇O₃

CAS No.

755038-02-9

Appearance

Solid

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)

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the Complete Stock Solution Preparation Table

* 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
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.

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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.95%

Select Batch:

Data Sheet (282 KB) SDS (394 KB)

COA (251 KB) HNMR (213 KB) LCMS (465 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]

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

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

BI 2536 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BI 2536755038-02-9BI2536BI-2536Polo-like Kinase (PLK)Epigenetic Reader DomainApoptosisInhibitorinhibitorinhibit

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BI 2536

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