Reagenzien und Instrumente für die Immunologie Zellbiologie und Molekularbiologie

BI 2536 [755038-02-9]

Drucken

Katalog-Nummer HY-50698-5mg

Size : 5mg

Marke : MedChemExpress

Weitere Informationen anfordern

Beschreibung

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.

Lösungsmittel & Löslichkeit

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.

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

Reinheit & Dokumentation

Purity: 99.95%

Data Sheet (282 KB) SDS (394 KB)

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

Handling Instructions (2659 KB)

Verweise

[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]

Sie könnten auch an folgenden Produkten interessiert sein:

Katalog-Nummer

Beschreibung

Cond.

Preis zzgl. MwSt.

BI 2536 [755038-02-9]

Katalog-Nummer HY-50698-5mg

Marke : MedChemExpress

BI 2536 Related Antibodies

Sie könnten auch an folgenden Produkten interessiert sein: