Home Cell Cycle PLK inhibitor - Epigenetic Reader Domain inhibitor - Myc inhibitor - Autophagy inhibitor - Apoptosis related activator BI 2536 For research use only.

BI 2536

BI-2536 is a potent Plk1 inhibitor with IC50 of 0.83 nM in a cell-free assay. BI-2536 inhibits Bromodomain 4 (BRD4) with Kd of 37 nM and potently suppresses c-Myc expression. BI-2536 induces apoptosis and attenuates autophagy. Phase 2.

BI 2536 Chemical Structure

BI 2536 Chemical Structure

CAS No. 755038-02-9

Purity & Quality Control

BI 2536 Related Products

Signaling Pathway

PLK Signaling Pathways

PLK Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
PSN1 Growth Inhibition Assay IC50=0.00776 μM SANGER
ACN Growth Inhibition Assay IC50=0.00843 μM SANGER
TE-8 Growth Inhibition Assay IC50=0.00941 μM SANGER
LC-2-ad Growth Inhibition Assay IC50=0.01093 μM SANGER
ALL-PO Growth Inhibition Assay IC50=0.013 μM SANGER
EW-16 Growth Inhibition Assay IC50=0.01336 μM SANGER
KM12 Growth Inhibition Assay IC50=0.01348 μM SANGER
GI-1 Growth Inhibition Assay IC50=0.01383 μM SANGER
LS-411N Growth Inhibition Assay IC50=0.01407 μM SANGER
ES8 Growth Inhibition Assay IC50=0.01494 μM SANGER
SNU-C2B Growth Inhibition Assay IC50=0.01526 μM SANGER
CESS Growth Inhibition Assay IC50=0.01602 μM SANGER
697 Growth Inhibition Assay IC50=0.01668 μM SANGER
NCI-H1963 Growth Inhibition Assay IC50=0.01673 μM SANGER
IA-LM Growth Inhibition Assay IC50=0.01688 μM SANGER
SW954 Growth Inhibition Assay IC50=0.01705 μM SANGER
RL95-2 Growth Inhibition Assay IC50=0.01738 μM SANGER
LXF-289 Growth Inhibition Assay IC50=0.0177 μM SANGER
OCUB-M Growth Inhibition Assay IC50=0.01826 μM SANGER
RKO Growth Inhibition Assay IC50=0.01987 μM SANGER
LOUCY Growth Inhibition Assay IC50=0.0205 μM SANGER
NOS-1 Growth Inhibition Assay IC50=0.02093 μM SANGER
A4-Fuk Growth Inhibition Assay IC50=0.02218 μM SANGER
A388 Growth Inhibition Assay IC50=0.02227 μM SANGER
TE-9 Growth Inhibition Assay IC50=0.02261 μM SANGER
KURAMOCHI Growth Inhibition Assay IC50=0.02285 μM SANGER
KALS-1 Growth Inhibition Assay IC50=0.02338 μM SANGER
HOP-62 Growth Inhibition Assay IC50=0.0242 μM SANGER
RPMI-8402 Growth Inhibition Assay IC50=0.02508 μM SANGER
TE-1 Growth Inhibition Assay IC50=0.02512 μM SANGER
CCRF-CEM Growth Inhibition Assay IC50=0.02543 μM SANGER
HUTU-80 Growth Inhibition Assay IC50=0.02624 μM SANGER
NCI-H1648 Growth Inhibition Assay IC50=0.02647 μM SANGER
HCE-4 Growth Inhibition Assay IC50=0.02682 μM SANGER
ETK-1 Growth Inhibition Assay IC50=0.02736 μM SANGER
TE-15 Growth Inhibition Assay IC50=0.02738 μM SANGER
BE-13 Growth Inhibition Assay IC50=0.0274 μM SANGER
KE-37 Growth Inhibition Assay IC50=0.02741 μM SANGER
NCI-H1355 Growth Inhibition Assay IC50=0.02783 μM SANGER
TE-11 Growth Inhibition Assay IC50=0.02809 μM SANGER
BL-70 Growth Inhibition Assay IC50=0.02857 μM SANGER
ES6 Growth Inhibition Assay IC50=0.02881 μM SANGER
GT3TKB Growth Inhibition Assay IC50=0.02953 μM SANGER
LB647-SCLC Growth Inhibition Assay IC50=0.03195 μM SANGER
NB13 Growth Inhibition Assay IC50=0.03316 μM SANGER
ST486 Growth Inhibition Assay IC50=0.03337 μM SANGER
NCI-H82 Growth Inhibition Assay IC50=0.03343 μM SANGER
NTERA-S-cl-D1 Growth Inhibition Assay IC50=0.03399 μM SANGER
ES4 Growth Inhibition Assay IC50=0.03463 μM SANGER
SK-NEP-1 Growth Inhibition Assay IC50=0.03499 μM SANGER
Becker Growth Inhibition Assay IC50=0.03555 μM SANGER
A101D Growth Inhibition Assay IC50=0.03748 μM SANGER
SK-UT-1 Growth Inhibition Assay IC50=0.03774 μM SANGER
SW982 Growth Inhibition Assay IC50=0.0379 μM SANGER
TE-10 Growth Inhibition Assay IC50=0.04046 μM SANGER
OVCAR-4 Growth Inhibition Assay IC50=0.04059 μM SANGER
KP-N-YS Growth Inhibition Assay IC50=0.04085 μM SANGER
BL-41 Growth Inhibition Assay IC50=0.04125 μM SANGER
MZ1-PC Growth Inhibition Assay IC50=0.04127 μM SANGER
PF-382 Growth Inhibition Assay IC50=0.04198 μM SANGER
MOLT-13 Growth Inhibition Assay IC50=0.04238 μM SANGER
HCC1599 Growth Inhibition Assay IC50=0.04258 μM SANGER
IST-MEL1 Growth Inhibition Assay IC50=0.04442 μM SANGER
LU-139 Growth Inhibition Assay IC50=0.04442 μM SANGER
MS-1 Growth Inhibition Assay IC50=0.04701 μM SANGER
MFH-ino Growth Inhibition Assay IC50=0.05003 μM SANGER
IMR-5 Growth Inhibition Assay IC50=0.05021 μM SANGER
TE-5 Growth Inhibition Assay IC50=0.05063 μM SANGER
DJM-1 Growth Inhibition Assay IC50=0.05142 μM SANGER
NB17 Growth Inhibition Assay IC50=0.05207 μM SANGER
KARPAS-45 Growth Inhibition Assay IC50=0.05358 μM SANGER
TGBC1TKB Growth Inhibition Assay IC50=0.05405 μM SANGER
ML-2 Growth Inhibition Assay IC50=0.05414 μM SANGER
no-10 Growth Inhibition Assay IC50=0.05474 μM SANGER
CTV-1 Growth Inhibition Assay IC50=0.05502 μM SANGER
SJSA-1 Growth Inhibition Assay IC50=0.0552 μM SANGER
HC-1 Growth Inhibition Assay IC50=0.05597 μM SANGER
TE-12 Growth Inhibition Assay IC50=0.05613 μM SANGER
KY821 Growth Inhibition Assay IC50=0.05632 μM SANGER
TALL-1 Growth Inhibition Assay IC50=0.05708 μM SANGER
DEL Growth Inhibition Assay IC50=0.05709 μM SANGER
TE-6 Growth Inhibition Assay IC50=0.05722 μM SANGER
SK-LMS-1 Growth Inhibition Assay IC50=0.05805 μM SANGER
EW-1 Growth Inhibition Assay IC50=0.05837 μM SANGER
8-MG-BA Growth Inhibition Assay IC50=0.05851 μM SANGER
NALM-6 Growth Inhibition Assay IC50=0.05973 μM SANGER
LB771-HNC Growth Inhibition Assay IC50=0.05979 μM SANGER
HT-144 Growth Inhibition Assay IC50=0.0613 μM SANGER
KM-H2 Growth Inhibition Assay IC50=0.06221 μM SANGER
SF268 Growth Inhibition Assay IC50=0.06286 μM SANGER
RS4-11 Growth Inhibition Assay IC50=0.06304 μM SANGER
MHH-PREB-1 Growth Inhibition Assay IC50=0.06319 μM SANGER
ATN-1 Growth Inhibition Assay IC50=0.06345 μM SANGER
BB30-HNC Growth Inhibition Assay IC50=0.06436 μM SANGER
CPC-N Growth Inhibition Assay IC50=0.06524 μM SANGER
NB1 Growth Inhibition Assay IC50=0.06613 μM SANGER
KS-1 Growth Inhibition Assay IC50=0.06748 μM SANGER
RXF393 Growth Inhibition Assay IC50=0.06764 μM SANGER
IST-SL2 Growth Inhibition Assay IC50=0.07004 μM SANGER
GI-ME-N Growth Inhibition Assay IC50=0.07286 μM SANGER
VA-ES-BJ Growth Inhibition Assay IC50=0.07475 μM SANGER
NCI-H1581 Growth Inhibition Assay IC50=0.07478 μM SANGER
U-266 Growth Inhibition Assay IC50=0.07497 μM SANGER
DMS-114 Growth Inhibition Assay IC50=0.07528 μM SANGER
NCI-H187 Growth Inhibition Assay IC50=0.07726 μM SANGER
SW962 Growth Inhibition Assay IC50=0.07839 μM SANGER
MONO-MAC-6 Growth Inhibition Assay IC50=0.07986 μM SANGER
MOLT-16 Growth Inhibition Assay IC50=0.08121 μM SANGER
KNS-42 Growth Inhibition Assay IC50=0.08161 μM SANGER
CMK Growth Inhibition Assay IC50=0.08225 μM SANGER
Ramos-2G6-4C10 Growth Inhibition Assay IC50=0.08225 μM SANGER
Daudi Growth Inhibition Assay IC50=0.08256 μM SANGER
NCI-H510A Growth Inhibition Assay IC50=0.08336 μM SANGER
LB831-BLC Growth Inhibition Assay IC50=0.08561 μM SANGER
HEL Growth Inhibition Assay IC50=0.08668 μM SANGER
LU-134-A Growth Inhibition Assay IC50=0.08708 μM SANGER
NCI-H1694 Growth Inhibition Assay IC50=0.08744 μM SANGER
KGN Growth Inhibition Assay IC50=0.08759 μM SANGER
A253 Growth Inhibition Assay IC50=0.08822 μM SANGER
DG-75 Growth Inhibition Assay IC50=0.08922 μM SANGER
MOLT-4 Growth Inhibition Assay IC50=0.08983 μM SANGER
NCI-SNU-5 Growth Inhibition Assay IC50=0.09258 μM SANGER
ONS-76 Growth Inhibition Assay IC50=0.09276 μM SANGER
NCI-H446 Growth Inhibition Assay IC50=0.09462 μM SANGER
COR-L279 Growth Inhibition Assay IC50=0.09556 μM SANGER
Calu-6 Growth Inhibition Assay IC50=0.09598 μM SANGER
BC-3 Growth Inhibition Assay IC50=0.09662 μM SANGER
NCI-H2126 Growth Inhibition Assay IC50=0.09791 μM SANGER
NCI-H1882 Growth Inhibition Assay IC50=0.09809 μM SANGER
BB65-RCC Growth Inhibition Assay IC50=0.10294 μM SANGER
DU-4475 Growth Inhibition Assay IC50=0.10407 μM SANGER
NCI-H526 Growth Inhibition Assay IC50=0.1044 μM SANGER
NEC8 Growth Inhibition Assay IC50=0.10525 μM SANGER
NCI-H1304 Growth Inhibition Assay IC50=0.10594 μM SANGER
L-540 Growth Inhibition Assay IC50=0.10708 μM SANGER
NCI-SNU-16 Growth Inhibition Assay IC50=0.10742 μM SANGER
HD-MY-Z Growth Inhibition Assay IC50=0.10856 μM SANGER
K-562 Growth Inhibition Assay IC50=0.10858 μM SANGER
JAR Growth Inhibition Assay IC50=0.10925 μM SANGER
MZ2-MEL Growth Inhibition Assay IC50=0.1105 μM SANGER
L-363 Growth Inhibition Assay IC50=0.11079 μM SANGER
BV-173 Growth Inhibition Assay IC50=0.11243 μM SANGER
NCI-H524 Growth Inhibition Assay IC50=0.11274 μM SANGER
EoL-1-cell Growth Inhibition Assay IC50=0.11672 μM SANGER
K052 Growth Inhibition Assay IC50=0.11712 μM SANGER
TK10 Growth Inhibition Assay IC50=0.11728 μM SANGER
KU812 Growth Inhibition Assay IC50=0.12044 μM SANGER
RPMI-8226 Growth Inhibition Assay IC50=0.12052 μM SANGER
MZ7-mel Growth Inhibition Assay IC50=0.12237 μM SANGER
SK-PN-DW Growth Inhibition Assay IC50=0.12287 μM SANGER
SR Growth Inhibition Assay IC50=0.12441 μM SANGER
RPMI-6666 Growth Inhibition Assay IC50=0.12743 μM SANGER
no-11 Growth Inhibition Assay IC50=0.12869 μM SANGER
EW-3 Growth Inhibition Assay IC50=0.12893 μM SANGER
LAMA-84 Growth Inhibition Assay IC50=0.13187 μM SANGER
HT Growth Inhibition Assay IC50=0.13574 μM SANGER
KP-N-RT-BM-1 Growth Inhibition Assay IC50=0.13612 μM SANGER
NCI-H747 Growth Inhibition Assay IC50=0.137 μM SANGER
NCCIT Growth Inhibition Assay IC50=0.13939 μM SANGER
MLMA Growth Inhibition Assay IC50=0.14167 μM SANGER
LP-1 Growth Inhibition Assay IC50=0.1424 μM SANGER
CAL-148 Growth Inhibition Assay IC50=0.14483 μM SANGER
GB-1 Growth Inhibition Assay IC50=0.14526 μM SANGER
COR-L88 Growth Inhibition Assay IC50=0.14802 μM SANGER
NKM-1 Growth Inhibition Assay IC50=0.14906 μM SANGER
NB5 Growth Inhibition Assay IC50=0.15462 μM SANGER
SH-4 Growth Inhibition Assay IC50=0.15466 μM SANGER
EM-2 Growth Inhibition Assay IC50=0.15467 μM SANGER
TGBC24TKB Growth Inhibition Assay IC50=0.15659 μM SANGER
SCLC-21H Growth Inhibition Assay IC50=0.15702 μM SANGER
COLO-684 Growth Inhibition Assay IC50=0.15721 μM SANGER
KINGS-1 Growth Inhibition Assay IC50=0.1591 μM SANGER
LS-123 Growth Inhibition Assay IC50=0.15917 μM SANGER
MC116 Growth Inhibition Assay IC50=0.16158 μM SANGER
SU-DHL-1 Growth Inhibition Assay IC50=0.16206 μM SANGER
NCI-H64 Growth Inhibition Assay IC50=0.16347 μM SANGER
HCE-T Growth Inhibition Assay IC50=0.16504 μM SANGER
LOXIMVI Growth Inhibition Assay IC50=0.16949 μM SANGER
ARH-77 Growth Inhibition Assay IC50=0.17379 μM SANGER
DOHH-2 Growth Inhibition Assay IC50=0.17672 μM SANGER
COLO-320-HSR Growth Inhibition Assay IC50=0.18154 μM SANGER
NB6 Growth Inhibition Assay IC50=0.18566 μM SANGER
L-428 Growth Inhibition Assay IC50=0.18813 μM SANGER
SNB75 Growth Inhibition Assay IC50=0.18824 μM SANGER
NCI-H2141 Growth Inhibition Assay IC50=0.19011 μM SANGER
KARPAS-299 Growth Inhibition Assay IC50=0.19241 μM SANGER
LC4-1 Growth Inhibition Assay IC50=0.19502 μM SANGER
UACC-257 Growth Inhibition Assay IC50=0.19947 μM SANGER
EVSA-T Growth Inhibition Assay IC50=0.20312 μM SANGER
JiyoyeP-2003 Growth Inhibition Assay IC50=0.20477 μM SANGER
NCI-H720 Growth Inhibition Assay IC50=0.20525 μM SANGER
GAK Growth Inhibition Assay IC50=0.21189 μM SANGER
HH Growth Inhibition Assay IC50=0.21405 μM SANGER
NCI-H1436 Growth Inhibition Assay IC50=0.21464 μM SANGER
GR-ST Growth Inhibition Assay IC50=0.21488 μM SANGER
BC-1 Growth Inhibition Assay IC50=0.22616 μM SANGER
SIG-M5 Growth Inhibition Assay IC50=0.22727 μM SANGER
NCI-H345 Growth Inhibition Assay IC50=0.23805 μM SANGER
OPM-2 Growth Inhibition Assay IC50=0.23882 μM SANGER
LB1047-RCC Growth Inhibition Assay IC50=0.2441 μM SANGER
CTB-1 Growth Inhibition Assay IC50=0.24493 μM SANGER
A3-KAW Growth Inhibition Assay IC50=0.25341 μM SANGER
SF126 Growth Inhibition Assay IC50=0.25383 μM SANGER
KARPAS-422 Growth Inhibition Assay IC50=0.25435 μM SANGER
MEG-01 Growth Inhibition Assay IC50=0.25673 μM SANGER
NCI-H209 Growth Inhibition Assay IC50=0.26374 μM SANGER
SBC-1 Growth Inhibition Assay IC50=0.265 μM SANGER
K5 Growth Inhibition Assay IC50=0.26984 μM SANGER
QIMR-WIL Growth Inhibition Assay IC50=0.27155 μM SANGER
NMC-G1 Growth Inhibition Assay IC50=0.28217 μM SANGER
IST-MES1 Growth Inhibition Assay IC50=0.29238 μM SANGER
SW684 Growth Inhibition Assay IC50=0.30047 μM SANGER
MV-4-11 Growth Inhibition Assay IC50=0.30788 μM SANGER
LAN-6 Growth Inhibition Assay IC50=0.31572 μM SANGER
RH-1 Growth Inhibition Assay IC50=0.31871 μM SANGER
CP66-MEL Growth Inhibition Assay IC50=0.31878 μM SANGER
EC-GI-10 Growth Inhibition Assay IC50=0.32987 μM SANGER
GDM-1 Growth Inhibition Assay IC50=0.33059 μM SANGER
IST-SL1 Growth Inhibition Assay IC50=0.34914 μM SANGER
KMOE-2 Growth Inhibition Assay IC50=0.35175 μM SANGER
OS-RC-2 Growth Inhibition Assay IC50=0.35544 μM SANGER
HDLM-2 Growth Inhibition Assay IC50=0.37814 μM SANGER
DSH1 Growth Inhibition Assay IC50=0.38631 μM SANGER
LS-1034 Growth Inhibition Assay IC50=0.38954 μM SANGER
LB373-MEL-D Growth Inhibition Assay IC50=0.39197 μM SANGER
GOTO Growth Inhibition Assay IC50=0.42118 μM SANGER
MRK-nu-1 Growth Inhibition Assay IC50=0.42205 μM SANGER
SK-MM-2 Growth Inhibition Assay IC50=0.43442 μM SANGER
BOKU Growth Inhibition Assay IC50=0.43792 μM SANGER
NOMO-1 Growth Inhibition Assay IC50=0.4386 μM SANGER
J-RT3-T3-5 Growth Inhibition Assay IC50=0.44878 μM SANGER
COLO-668 Growth Inhibition Assay IC50=0.45668 μM SANGER
SF539 Growth Inhibition Assay IC50=0.48684 μM SANGER
LB2518-MEL Growth Inhibition Assay IC50=0.49703 μM SANGER
TE-441-T Growth Inhibition Assay IC50=0.5012 μM SANGER
MDA-MB-134-VI Growth Inhibition Assay IC50=0.50921 μM SANGER
SCC-3 Growth Inhibition Assay IC50=0.51873 μM SANGER
KLE Growth Inhibition Assay IC50=0.52171 μM SANGER
LB2241-RCC Growth Inhibition Assay IC50=0.52525 μM SANGER
NCI-H1417 Growth Inhibition Assay IC50=0.53435 μM SANGER
NCI-H2081 Growth Inhibition Assay IC50=0.58611 μM SANGER
NCI-H1522 Growth Inhibition Assay IC50=0.59383 μM SANGER
NCI-H889 Growth Inhibition Assay IC50=0.59844 μM SANGER
CGTH-W-1 Growth Inhibition Assay IC50=0.60755 μM SANGER
EB-3 Growth Inhibition Assay IC50=0.61153 μM SANGER
D-336MG Growth Inhibition Assay IC50=0.61791 μM SANGER
LC-1F Growth Inhibition Assay IC50=0.62592 μM SANGER
MHH-NB-11 Growth Inhibition Assay IC50=0.63801 μM SANGER
SK-N-FI Growth Inhibition Assay IC50=0.6391 μM SANGER
NCI-H69 Growth Inhibition Assay IC50=0.64879 μM SANGER
SCH Growth Inhibition Assay IC50=0.66023 μM SANGER
LS-513 Growth Inhibition Assay IC50=0.67259 μM SANGER
CP67-MEL Growth Inhibition Assay IC50=0.67596 μM SANGER
GCIY Growth Inhibition Assay IC50=0.70363 μM SANGER
SHP-77 Growth Inhibition Assay IC50=0.70734 μM SANGER
EHEB Growth Inhibition Assay IC50=0.71854 μM SANGER
D-247MG Growth Inhibition Assay IC50=0.73232 μM SANGER
Raji Growth Inhibition Assay IC50=0.74989 μM SANGER
MPP-89 Growth Inhibition Assay IC50=0.75978 μM SANGER
EKVX Growth Inhibition Assay IC50=0.79073 μM SANGER
HCC2218 Growth Inhibition Assay IC50=0.79131 μM SANGER
KNS-81-FD Growth Inhibition Assay IC50=0.81011 μM SANGER
HCC2157 Growth Inhibition Assay IC50=0.84951 μM SANGER
BT-474 Growth Inhibition Assay IC50=0.88854 μM SANGER
NCI-H748 Growth Inhibition Assay IC50=0.912 μM SANGER
EW-24 Growth Inhibition Assay IC50=0.92002 μM SANGER
D-263MG Growth Inhibition Assay IC50=0.94512 μM SANGER
OMC-1 Growth Inhibition Assay IC50=0.96373 μM SANGER
NCI-H2196 Growth Inhibition Assay IC50=0.97777 μM SANGER
HAL-01 Growth Inhibition Assay IC50=0.99872 μM SANGER
NCI-H2107 Growth Inhibition Assay IC50=1.01854 μM SANGER
LB996-RCC Growth Inhibition Assay IC50=1.08051 μM SANGER
NCI-H1395 Growth Inhibition Assay IC50=1.1067 μM SANGER
CHP-126 Growth Inhibition Assay IC50=1.16199 μM SANGER
NB69 Growth Inhibition Assay IC50=1.26148 μM SANGER
CAS-1 Growth Inhibition Assay IC50=1.34231 μM SANGER
JVM-3 Growth Inhibition Assay IC50=1.47855 μM SANGER
DMS-153 Growth Inhibition Assay IC50=1.57674 μM SANGER
SK-MEL-2 Growth Inhibition Assay IC50=1.71789 μM SANGER
NCI-H1155 Growth Inhibition Assay IC50=1.73676 μM SANGER
NCI-H1092 Growth Inhibition Assay IC50=1.76182 μM SANGER
LU-165 Growth Inhibition Assay IC50=1.86476 μM SANGER
HL-60 Growth Inhibition Assay IC50=1.99908 μM SANGER
REH Growth Inhibition Assay IC50=2.00582 μM SANGER
JVM-2 Growth Inhibition Assay IC50=2.06135 μM SANGER
MN-60 Growth Inhibition Assay IC50=2.17308 μM SANGER
SCC-15 Growth Inhibition Assay IC50=2.2027 μM SANGER
SNU-C1 Growth Inhibition Assay IC50=2.21343 μM SANGER
SK-MEL-1 Growth Inhibition Assay IC50=2.32047 μM SANGER
TGW Growth Inhibition Assay IC50=2.35027 μM SANGER
CA46 Growth Inhibition Assay IC50=2.75967 μM SANGER
NCI-H23 Growth Inhibition Assay IC50=2.80791 μM SANGER
MMAC-SF Growth Inhibition Assay IC50=2.86628 μM SANGER
NCI-H2171 Growth Inhibition Assay IC50=3.03448 μM SANGER
A704 Growth Inhibition Assay IC50=3.14194 μM SANGER
DB Growth Inhibition Assay IC50=3.25576 μM SANGER
NCI-H719 Growth Inhibition Assay IC50=3.30384 μM SANGER
MC-CAR Growth Inhibition Assay IC50=3.54817 μM SANGER
SIMA Growth Inhibition Assay IC50=3.58416 μM SANGER
SW872 Growth Inhibition Assay IC50=3.78101 μM SANGER
HCC1187 Growth Inhibition Assay IC50=3.78315 μM SANGER
EW-13 Growth Inhibition Assay IC50=3.83417 μM SANGER
NCI-SNU-1 Growth Inhibition Assay IC50=4.21999 μM SANGER
NCI-H226 Growth Inhibition Assay IC50=4.33606 μM SANGER
RPMI-8866 Growth Inhibition Assay IC50=4.36029 μM SANGER
OCI-AML2 Growth Inhibition Assay IC50=4.5523 μM SANGER
LU-65 Growth Inhibition Assay IC50=4.93033 μM SANGER
SK-N-DZ Growth Inhibition Assay IC50=5.63465 μM SANGER
NB14 Growth Inhibition Assay IC50=5.97135 μM SANGER
COLO-829 Growth Inhibition Assay IC50=6.33359 μM SANGER
MHH-CALL-2 Growth Inhibition Assay IC50=6.51508 μM SANGER
NCI-H1770 Growth Inhibition Assay IC50=6.66904 μM SANGER
ECC4 Growth Inhibition Assay IC50=6.82179 μM SANGER
A498 Growth Inhibition Assay IC50=6.87192 μM SANGER
DMS-79 Growth Inhibition Assay IC50=7.04512 μM SANGER
P30-OHK Growth Inhibition Assay IC50=7.21906 μM SANGER
D-502MG Growth Inhibition Assay IC50=7.9836 μM SANGER
RCC10RGB Growth Inhibition Assay IC50=8.0628 μM SANGER
U-698-M Growth Inhibition Assay IC50=8.29226 μM SANGER
BB49-HNC Growth Inhibition Assay IC50=9.42265 μM SANGER
ES1 Growth Inhibition Assay IC50=9.68956 μM SANGER
MFM-223 Growth Inhibition Assay IC50=10.9927 μM SANGER
C2BBe1 Growth Inhibition Assay IC50=11.3523 μM SANGER
EB2 Growth Inhibition Assay IC50=12.6881 μM SANGER
C8166 Growth Inhibition Assay IC50=13.8303 μM SANGER
ES3 Growth Inhibition Assay IC50=13.9977 μM SANGER
NCI-H1650 Growth Inhibition Assay IC50=16.3765 μM SANGER
Mo-T Growth Inhibition Assay IC50=17.4029 μM SANGER
NB7 Growth Inhibition Assay IC50=17.7467 μM SANGER
ES7 Growth Inhibition Assay IC50=19.5507 μM SANGER
ES5 Growth Inhibition Assay IC50=21.7671 μM SANGER
MSTO-211H Growth Inhibition Assay IC50=21.8858 μM SANGER
U-87-MG Growth Inhibition Assay IC50=25.1966 μM SANGER
THP-1 Growth Inhibition Assay IC50=29.7201 μM SANGER
NB10 Growth Inhibition Assay IC50=30.2694 μM SANGER
NH-12 Growth Inhibition Assay IC50=33.2017 μM SANGER
COLO-824 Growth Inhibition Assay IC50=34.1006 μM SANGER
SKM-1 Growth Inhibition Assay IC50=37.8422 μM SANGER
NCI-H1838 Growth Inhibition Assay IC50=38.3797 μM SANGER
RL Growth Inhibition Assay IC50=39.2477 μM SANGER
COLO-800 Growth Inhibition Assay IC50=40.0773 μM SANGER
KG-1 Growth Inhibition Assay IC50=40.8955 μM SANGER
TUR Growth Inhibition Assay IC50=41.6399 μM SANGER
LNCaP-Clone-FGC Growth Inhibition Assay IC50=41.9017 μM SANGER
NCI-H322M Growth Inhibition Assay IC50=42.5984 μM SANGER
LNCaP  Growth Inhibition Assay IC50=91.3 nM 25505174
C4-2 Growth Inhibition Assay IC50=8 nM 25505174
JURKAT Growth Inhibition Assay 24 h IC50=416.66 nM 24519995
MOLT-4 Growth Inhibition Assay 24 h IC50=2853.5 nM 24519995
REH Growth Inhibition Assay 24 h IC50=287.68 nM 24519995
NALM-6 Growth Inhibition Assay 24 h IC50=34330 nM 24519995
RS 4;11 Growth Inhibition Assay 24 h IC50=519.05 nM 24519995
697 Growth Inhibition Assay 24 h IC50=2107.1 nM 24519995
SIL-ALL Growth Inhibition Assay 24 h IC50=199.77 nM 24519995
CEM Growth Inhibition Assay 24 h IC50=52.18 nM 24519995
P12 Growth Inhibition Assay 24 h IC50=39.27 nM 24519995
NALM-16 Growth Inhibition Assay 24 h IC50=96.28 nM 24519995
JURKAT Growth Inhibition Assay 48 h IC50=14.84 nM 24519995
MOLT-4 Growth Inhibition Assay 48 h IC50=26.6 nM 24519995
REH Growth Inhibition Assay 48 h IC50=44.71 nM 24519995
NALM-6 Growth Inhibition Assay 48 h IC50=23.26 nM 24519995
RS 4;11 Growth Inhibition Assay 48 h IC50=164.28 nM 24519995
697 Growth Inhibition Assay 48 h IC50=305.3 nM 24519995
SIL-ALL Growth Inhibition Assay 48 h IC50=74.62 nM 24519995
CEM Growth Inhibition Assay 48 h IC50=24.55 nM 24519995
P12 Growth Inhibition Assay 48 h IC50=18.46 nM 24519995
NALM-16 Growth Inhibition Assay 48 h IC50=63.24 nM 24519995
JURKAT Growth Inhibition Assay 72 h IC50=3.65 nM 24519995
MOLT-4 Growth Inhibition Assay 72 h IC50=7.39 nM 24519995
REH Growth Inhibition Assay 72 h IC50=16.01 nM 24519995
NALM-6 Growth Inhibition Assay 72 h IC50=1.78 nM 24519995
RS 4;11 Growth Inhibition Assay 72 h IC50=4.38 nM 24519995
697 Growth Inhibition Assay 72 h IC50=74.28 nM 24519995
SIL-ALL Growth Inhibition Assay 72 h IC50=7.2 nM 24519995
CEM Growth Inhibition Assay 72 h IC50=5.42 nM 24519995
P12 Growth Inhibition Assay 72 h IC50=6.37 nM 24519995
NALM-16 Growth Inhibition Assay 72 h IC50=77.73 nM 24519995
Y79 Apoptosis Assay 1-50 nM 12/24 h DMSO induced apoptosis which can be enhanced by HT 24366665
WER-Rb-1 Apoptosis Assay 1-50 nM 12/24 h DMSO induced apoptosis which can be enhanced by HT 24366665
G7 Growth Inhibition Assay IC50=3.3 nM 24204733
G166 Growth Inhibition Assay IC50=7.0 nM 24204733
CB660 Growth Inhibition Assay IC50=6.4 nM 24204733
CB1117 Growth Inhibition Assay IC50=15.6 nM 24204733
KB-3-1 Growth Inhibition Assay IC50=1.48 ± 0.53 nM 23962445
KB-8-5-11 Growth Inhibition Assay IC50=5.01 ± 2.01 nM 23962445
KB-C-1 Growth Inhibition Assay IC50=16.76 ± 4.51 nM 23962445
KB-V-1 Growth Inhibition Assay IC50=281.24 ± 31.57 nM 23962445
OVCAR-8 Growth Inhibition Assay IC50=7.19 ± 3.60 nM 23962445
NCI-ADR-RES Growth Inhibition Assay IC50=1273.30 ± 191.20 nM 23962445
MCF7 Growth Inhibition Assay IC50=5.11 ± 1.47 nM 23962445
MCF7-FLV1000 Growth Inhibition Assay IC50=393.18 ± 74.83 nM 23962445
S1 Growth Inhibition Assay IC50=24.30 ± 4.75 nM 23962445
S1-M1-80 Growth Inhibition Assay IC50=261.06 ± 48.25 nM 23962445
CORL-23/P Growth Inhibition Assay IC50=4.38 ± 1.25 nM 23962445
CORL-23/R Growth Inhibition Assay IC50=5.16 ± 1.83 nM 23962445
NIH3T3 Growth Inhibition Assay IC50=40.60 ± 4.97 nM 23962445
NIH3T3-G185 Growth Inhibition Assay IC50=2413.40 ± 423.66 nM 23962445
pcDNA-HEK293 Growth Inhibition Assay IC50=2.75 ± 0.67 nM 23962445
MDR19-HEK293 Growth Inhibition Assay IC50=85.50 ± 13.67 nM 23962445
R482-HEK293 Growth Inhibition Assay IC50=25.97 ± 4.95 nM 23962445
MRP1-HEK293 Growth Inhibition Assay IC50=2.99 ± 1.49 nM 23962445
SF188 Growth Inhibition Assay 10-100 nM 24-96 h DMSO inhibits cell growth in both time- and concentration- depedent manner 23887645
T98G Growth Inhibition Assay 10-100 nM 24-96 h DMSO inhibits cell growth in concentration- depedent manner 23887645
DU145 Growth Inhibition Assay DMSO IC50∼60 nM 23884428
LNCaP  Growth Inhibition Assay DMSO IC50∼75 nM 23884428
PC3 Growth Inhibition Assay DMSO IC50∼175 nM 23884428
RT4 Growth Inhibition Assay IC50=27.21 nM 23792639
5637 Growth Inhibition Assay IC50=45.47 nM 23792639
T24 Growth Inhibition Assay IC50=79.12 nM 23792639
MCF7  Function Assay 100 nM 1 h DMSO reduces the induction of Greb1, Sgk1, Ps2, Serpina3, and Wisp2 23770244
KB-V1  Growth Inhibition Assay IC50=3.92 μM 23593196
Hec50co Growth Inhibition Assay IC50=5 nM 23146687
MDA-MB-468 Apoptosis Assay 1/5/10 nM 24/48/72 h DMSO induces apoptosis in a dose-dependent manner 23144294
MCF10A Apoptosis Assay 1/5/10 nM 24/48/72 h DMSO induces apoptosis in a dose-dependent manner 23144294
Huh-7 Growth Inhibition Assay 1/10/100/1000 nM 48 h decreases the cell viability dose-dependently 22745587
Daoy  Growth Inhibition Assay 1.875-240 nM 72 h DMSO IC50=5 nM 22390279
ONS-76 Growth Inhibition Assay 1.875-240 nM 72 h DMSO IC50=7.5 nM 22390279
SUM 149 Growth Inhibition Assay 0-100 nM 72 h inhibits the cell viability in a dose-dependent mannar 22309939
MDA-MB-231 Growth Inhibition Assay 0-100 nM 72 h inhibits the cell viability in a dose-dependent mannar 22309939
HR5 Growth Inhibition Assay 0-100 nM 72 h inhibits the cell viability in a dose-dependent mannar 22309939
BT-474-M1 Growth Inhibition Assay 0-100 nM 72 h inhibits the cell viability in a dose-dependent mannar 22309939
AU565 Growth Inhibition Assay 0-100 nM 72 h inhibits the cell viability in a dose-dependent mannar 22309939
T47D Growth Inhibition Assay 0-100 nM 72 h inhibits the cell viability in a dose-dependent mannar 22309939
MCF7 Growth Inhibition Assay 0-100 nM 72 h inhibits the cell viability in a dose-dependent mannar 22309939
HCT116p53(+/+) Growth Inhibition Assay 10-1000 nM 24/48 h inhibits cell proliferation completely at 25 nM 22262171
HCT116p53(-/-) Growth Inhibition Assay 10-1000 nM 24/48 h inhibits cell proliferation completely at 25 nM 22262171
HeLa  Growth Inhibition Assay 10-100 nM 48 h DMSO IC50=52.9 nM 22080235
HeLa  Growth Inhibition Assay 10-100 nM 72 h DMSO IC50=50.5 nM 22080235
GBC Growth Inhibition Assay 72 h IC50=14.78 nM 21965739
GB-CL-1 Growth Inhibition Assay 72 h IC50=5.22 nM 21965739
Mz-ChA-2 Growth Inhibition Assay 72 h IC50=3.31 nM 21965739
TGBC1-TKB Growth Inhibition Assay 144 h IC50=6.72 nM 21965739
Wittier Growth Inhibition Assay 72 h IC50=3.26 nM 21965739
H-1 Growth Inhibition Assay 72 h IC50=9.54 nM 21965739
HuH-28 Growth Inhibition Assay 72 h IC50=11.19 nM 21965739
NEC Growth Inhibition Assay 72 h IC50=9.98 nM 21965739
REB Growth Inhibition Assay 72 h IC50=13.51 nM 21965739
CC-LP-1 Growth Inhibition Assay 72 h IC50=5.84 nM 21965739
CC-SW-1 Growth Inhibition Assay 72 h IC50=9.55 nM 21965739
EGI-1 Growth Inhibition Assay 72 h IC50=10.72 nM 21965739
Sk-ChA-1 Growth Inhibition Assay 72 h IC50=17.2 nM 21965739
TFK-1 Growth Inhibition Assay 72 h IC50=13.45 nM 21965739
786-O Growth Inhibition Assay 5-80 nM 96 h HCl suppresses the proliferation in a dose-dependent manner with IC50 values of 2 to 20 nM 21642374
A498 Growth Inhibition Assay 5-80 nM 96 h HCl suppresses the proliferation in a dose-dependent manner with IC50 values of 2 to 20 nM 21642374
ACHN Growth Inhibition Assay 5-80 nM 96 h HCl suppresses the proliferation in a dose-dependent manner with IC50 values of 2 to 20 nM 21642374
Caki-1 Growth Inhibition Assay 5-80 nM 96 h HCl suppresses the proliferation in a dose-dependent manner with IC50 values of 2 to 20 nM 21642374
SN12C Growth Inhibition Assay 5-80 nM 96 h HCl suppresses the proliferation in a dose-dependent manner with IC50 values of 2 to 20 nM 21642374
HMC-1.1 Growth Inhibition Assay 1-1000 nM 72 h inhibits the cell proliferation in a dose-dependent manne 21242189
HMC-1.2 Growth Inhibition Assay 1-1000 nM 72 h inhibits the cell proliferation in a dose-dependent manne 21242189
C2 Growth Inhibition Assay 1-1000 nM 72 h inhibits the cell proliferation in a dose-dependent manne 21242189
CHP-212 Growth Inhibition Assay 1-125 nM 24-120 h inhibits the cell proliferation in both time- and dose-dependent manne 21169242
IMR-32 Growth Inhibition Assay 1-125 nM 24-120 h inhibits the cell proliferation in both time- and dose-dependent manne 21169242
Kelly Growth Inhibition Assay 1-125 nM 24-120 h inhibits the cell proliferation in both time- and dose-dependent manne 21169242
SH-EP Growth Inhibition Assay 1-125 nM 24-120 h inhibits the cell proliferation in both time- and dose-dependent manne 21169242
SH-SY5Y Growth Inhibition Assay 1-125 nM 24-120 h inhibits the cell proliferation in both time- and dose-dependent manne 21169242
SK-N-AS Growth Inhibition Assay 1-125 nM 24-120 h inhibits the cell proliferation in both time- and dose-dependent manne 21169242
SK-N-BE Growth Inhibition Assay 1-125 nM 24-120 h inhibits the cell proliferation in both time- and dose-dependent manne 21169242
KG1 Growth Inhibition Assay 1/10/100 nM 72 h DMSO inhibits the cell proliferation in both time- and dose-dependent manne 19458358
U937 Growth Inhibition Assay 1/10/100 nM 72 h DMSO inhibits the cell proliferation in both time- and dose-dependent manne 19458358
CAL62 Growth Inhibition Assay 0.1-100 nM 72 h DMSO EC50=1.4 nM 19223553
OCUT-1 Growth Inhibition Assay 0.1-100 nM 72 h DMSO EC50=2.3 nM 19223553
8505C Growth Inhibition Assay 0.1-100 nM 72 h DMSO EC50=3.2 nM 19223553
ACT-1 Growth Inhibition Assay 0.1-100 nM 72 h DMSO EC50=5.4 nM 19223553
SW1736 Growth Inhibition Assay 0.1-100 nM 72 h DMSO EC50=5.6 nM 19223553
HEK293 Function assay 1 hr Binding affinity to PLK1 (unknown origin) expressed in HEK293 cells after 1 hr by proprietary competition assay, Ki = 0.00022 μM. 26191363
HEK293T Antiproliferative assay 72 hrs Antiproliferative activity against HEK293T cells measured after 72 hrs by CellTiter-Blue assay, IC50 = 0.001 μM. 28792760
MDA-MB-231 Antiproliferative assay 72 hrs Antiproliferative activity against human MDA-MB-231 cells measured after 72 hrs by CellTiter-Blue assay, IC50 = 0.001 μM. 28792760
MM1S Antiproliferative assay 72 hrs Antiproliferative activity against human MM1S cells measured after 72 hrs by CellTiter-Blue assay, IC50 = 0.001 μM. 28792760
TY82 Antiproliferative assay 72 hrs Antiproliferative activity against human TY82 cells after 72 hrs by CCK8 assay, IC50 = 0.001 μM. 28586718
NMC-797 Cytotoxicity assay 3 days Cytotoxicity against BRD4 dependent human NMC-797 cells assessed as cell viability after 3 days by ATPlite assay, IC50 = 0.0107 μM. 26985285
MV4-11 Cytotoxicity assay 24 hrs Cytotoxicity against human MV4-11 cells after 24 hrs by CellTiter-Blue assay, GI50 = 0.0152 μM. 26191363
BL21(DE3) Function assay 60 mins Inhibition of recombinant human N-terminal His6-tagged BRD4 expressed in Escherichia coli BL21(DE3) cells using biotinylated histone H4 peptide as substrate after 60 mins by AlphaScreen assay, IC50 = 0.025 μM. 28195723
BL21(DE3) Function assay Inhibition of human N-terminal His6-tagged BRD4-BD1 (44 to 168 residues) expressed in Escherichia coli BL21 (DE3) cells using protein thermal shift dye as fluorescence probe by differential scanning fluorimetry, IC50 = 0.025 μM. 28586718
HuH7 Antiproliferative assay 72 hrs Antiproliferative activity against human HuH7 cells after 72 hrs by CCK8 assay, GI50 = 0.028 μM. 29220793
HeLa Antiproliferative assay 72 hrs Antiproliferative activity against human HeLa cells after 72 hrs by CCK8 assay, GI50 = 0.034 μM. 29220793
HL60 Cytotoxicity assay 3 days Cytotoxicity against BRD4 dependent human HL60 cells assessed as cell viability after 3 days by ATPlite assay, IC50 = 0.0365 μM. 26985285
A549 Antiproliferative assay 72 hrs Antiproliferative activity against human A549 cells after 72 hrs by CCK8 assay, GI50 = 0.057 μM. 29220793
MCF7 Antiproliferative assay 72 hrs Antiproliferative activity against human MCF7 cells after 72 hrs by CCK8 assay, GI50 = 0.067 μM. 29220793
K562 Antiproliferative assay 72 hrs Antiproliferative activity against human K562 cells after 72 hrs by CCK8 assay, GI50 = 0.068 μM. 29220793
MDA-MB-23 Function assay 6 hrs Inhibition of PLK1 in human MDA-MB-23 cells assessed as decrease in TCTP phosphorylation after 6 hrs by Western blot method, IC50 = 0.1 μM. 28792760
HEK293T Function assay 6 hrs Inhibition of PLK1 in HEK293T cells assessed as decrease in TCTP phosphorylation after 6 hrs by Western blot method, IC50 = 0.1 μM. 28792760
NCI-H1975 Antiproliferative assay 72 hrs Antiproliferative activity against human NCI-H1975 cells after 72 hrs by CCK8 assay, GI50 = 0.23 μM. 29220793
BL21(DE3) Function assay 4 hrs Inhibition of JQ1-FITC binding to His6-tagged BRD4-BD1 (unknown origin) expressed in Escherichia coli BL21 (DE3)-codon plus-RIL cells incubated in dark for 4 hrs by fluorescence anisotropy assay, IC50 = 0.25 μM. 28586718
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells 29435139
U-2 OS qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells 29435139
Fibroblast cells qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells 29435139
MG 63(6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells 29435139
Fibroblast cells qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for control Hh wild type fibroblast cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells 29435139
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells 29435139
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells 29435139
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells 29435139
DU145 Apoptosis assay 100 nM 24 hrs Induction of apoptosis in human DU145 cells assessed as increase in PARP cleavage at 100 nM after 24 hrs by immunoblotting method 25685941
HeLa Function assay 100 nM Inhibition of PLK1 Thr210 phosphorylation in human HeLa cells at 100 nM by immunoblotting method 25685941
DU145 Function assay 100 nM Inhibition of PLK1 protein accumulation in human DU145 cells at 100 nM by immunoblotting method 25685941
HeLa Function assay 100 nM Inhibition of PLK1 protein accumulation in human HeLa cells at 100 nM by immunoblotting method 25685941
HeLa Function assay 100 nM 18 hrs Induction of monopolar mitotic spindles in human HeLa cells at 100 nM incubated for 18 hrs by indirect immunofluorescence microscopy 25685941
HeLa Apoptosis assay 100 nM 24 hrs Induction of apoptosis in human HeLa cells assessed as increase in PARP cleavage at 100 nM after 24 hrs by immunoblotting method 25685941
PC3 Function assay 100 nM 18 hrs Induction of monopolar mitotic spindles in human PC3 cells at 100 nM incubated for 18 hrs by indirect immunofluorescence microscopy 25685941
DU145 Function assay 100 nM Inhibition of PLK1 Thr210 phosphorylation in human DU145 cells at 100 nM by immunoblotting method 25685941
Click to View More Cell Line Experimental Data

Biological Activity

Description BI-2536 is a potent Plk1 inhibitor with IC50 of 0.83 nM in a cell-free assay. BI-2536 inhibits Bromodomain 4 (BRD4) with Kd of 37 nM and potently suppresses c-Myc expression. BI-2536 induces apoptosis and attenuates autophagy. Phase 2.
Features The first potent and selective Plk1 inhibitor that induces all hallmarks of Plk1 inhibition.
Targets
c-Myc [3] PLK1 [1]
(Cell-free assay)		 PLK2 [1]
(Cell-free assay)		 PLK3 [1]
(Cell-free assay)		 BRD4 [3]
(Cell-free assay)
0.83 nM 3.5 nM 9.0 nM 37 nM(Kd)
In vitro
In vitro

BI 2536 blocks the activities of Plk2 and Plk3 to a slightly lesser extent with IC50 of 3.5 nM and 9.0 nM, respectively. In HeLa cells, BI 2536 treatment ranging from 10-100 nM leads to the blocking of the recruitment of γ-tubulin and phosphorylation of Apc6 at mitotic centrosomes, inhibition of cohesin release from chromosome arms, induction of monopolar spindles, as well as a range of other mitotic processes that are known to depend on Plk1. BI 2536 treatment leads to the HeLa cells arrested in G2/M, subsequently a sub-G1 DNA peak indicative of DNA breakdown and apoptosis, and accumulated cleaved PARP p85 fragments in a concentration-dependent manner. BI 2536 inhibits the growth of a panel of 32 human cancer cell lines with EC50 of 2-25 nM, while blocking the proliferation of exponentially growing hTERT-RPE1, human umbilical vein endothelial cells (HUVECs), and normal rat kidney (NRK) cells with EC50 of 12-31 nM. [1] Plk1 inhibition by BI 2536 reduces the growth and viability of anaplastic thyroid carcinoma (ATC) cells such as CAL62, OCUT-1, SW1736, 8505C, and ACT-1 with EC50 values of 1.4-5.6 nM. [2]
Kinase Assay Plk1 in vitro kinase assay
Recombinant human Plk1 (residues 1-603) is expressed as N-terminal, GST-tagged fusion protein with a baculoviral expression system and purified by affinity chromatography with Glutathione-agarose. Enzyme activity assays for Plk1 are performed in the presence of serially diluted BI 2536 with 20 ng of recombinant kinase and 10 μg casein from bovine milk as the substrate. Kinase reactions are performed in a final volume of 60 μL for 45 minutes at 30 °C (15 mM MgCl2, 25 mM MOPS [pH 7.0], 1 mM DTT, 1% DMSO, 7.5 mM ATP, 0.3 μCi γ-33P-ATP). Reactions are terminated by the addition of 125 μL of ice-cold 5% TCA. After transfer of the precipitates to Multi-Screen mixed ester cellulose filter plates, plates are washed with 1% TCA and quantified radiometrically. Dose-response curve is used for calculating IC50 value.
Cell Research Cell lines HeLa, A43, SKOV-3, HT-29, K562, A549, Saos-2, MCF7, HCT116, COLO 205, Hep G2, Raji and PC-3 cells, etc.
Concentrations Dissolved in DMSO, final concentrations ~1 μM
Incubation Time 24 and 72 hours
Method

Cells are exposed to various concentrations of BI 2536 for 24, and 72 hours. Cell growth is assessed by the measurement of Alamar Blue dye conversion in a fluorescence spectrophotometer. For determining the DNA content of the cultures, cell suspensions are fixed in 80% ethanol, treated for 5 minutes with 0.25% Triton X-100 in PBS, and incubated with 0.1% RNase and 10 μg/mL propidium iodide (PI) in PBS for 20 minutes at RT. Cell-cycle profiles are determined by flow cytometric analysis.
Experimental Result Images Methods Biomarkers Images PMID
Western blot Aurora B / pAurora B / pAurora C / pH3 / Cyclin B1 / Securin / pBcl-XL / MPM2 pPlk1 / Plk1 / pMyt1 pMEK / MEK / pERK / ERK / pRSK1 / RSK1 p-HH3 / PARP / Myc / p-Myc pro-caspase-8 / cleaved caspase-8 / cleaved caspase-3 / cleaved caspase-9 25169932
Immunofluorescence Pericentrin / α-tubulin p-H2AX / propidium iodide 21772266
Growth inhibition assay Cell viability 21772266
In Vivo
In vivo

BI 2536 given i.v. once or twice per week is highly efficacious in diverse xenograft models with acceptable tolerability by inhibiting cell proliferation through a mitotic arrest, and subsequently induction of tumor-cell death. Administration of BI 2536 at 50 mg/kg once or twice per week significantly inhibits growth of HCT 116 xenografts with T/C of 15% and 0.3%, respectively. BI 2536 treatment twice-weekly also leads to excellent tumor-growth in BxPC-3 and A549 models with T/C of 5% and 14%, respectively. [1]
Animal Research Animal Models Female BomTac:NMRI-Foxn1nu mice injected subcutaneously with HCT 116, NCI-H460, or A549 cells
Dosages ~50 mg/kg
Administration Injection i.v. once or twice per week
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02215044 Terminated
Pancreatic Neoplasms
Boehringer Ingelheim
 June 2007 Phase 1
NCT02211833 Completed
Carcinoma Non-Small-Cell Lung
Boehringer Ingelheim
 October 2006 Phase 1
NCT00701766 Completed
Leukemia Myeloid Acute
Boehringer Ingelheim
 October 2006 Phase 2
NCT00706498 Completed
Prostatic Neoplasms
Boehringer Ingelheim
 September 2006 Phase 2
NCT00376623 Completed
Carcinoma Non-Small-Cell Lung
Boehringer Ingelheim
 July 25 2006 Phase 2
NCT02211872 Completed
Neoplasms
Boehringer Ingelheim
 August 2004 Phase 1

Chemical Information & Solubility

Molecular Weight 521.66 Formula

C28H39N7O3
CAS No. 755038-02-9 SDF Download BI 2536 SDF
Smiles CCC1C(=O)N(C2=CN=C(N=C2N1C3CCCC3)NC4=C(C=C(C=C4)C(=O)NC5CCN(CC5)C)OC)C
Storage (From the date of receipt)

In vitro
Batch:

Ethanol : 104 mg/mL

DMSO : 96 mg/mL ( (184.02 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble


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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Frequently Asked Questions

Question 1:
We need to use BI 2536 in preclinical studies using mice, how to formulate the inhibitor for this in vivo study?

Answer:
For in vivo study, DMSO should not be more than 5% because the toxicity. You can formulated BI2536 in hydrochloric acid (0.1 N), and diluted with 0.9% NaCl for animal study according to the reference :( Supplemental Data) http://linkinghub.elsevier.com/retrieve/pii/S0960-9822(06)02671-6

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