Home Apoptosis Bcl-2 inhibitor ABT-737

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ABT-737 Bcl-2 Inhibitor

Cat.No.S1002

ABT-737 is a BH3 mimetic inhibitor of Bcl-xL, Bcl-2 and Bcl-w with EC50 of 78.7 nM, 30.3 nM and 197.8 nM in cell-free assays, respectively; no inhibition observed against Mcl-1, Bcl-B or Bfl-1. ABT-737 induces mitochondrial pathway apoptosis and mitophagy. Phase 2.
ABT-737 Bcl-2 inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 813.43

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Quality Control

Batch: Purity: 99.99%
99.99

Cell Culture, Treatment & Working Concentration

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
OCI-Ly1  Cell Viability Assay 250 nM  72 h DMSO caused 97% loss of viability in cells transfected with BCL6 siRNA 26657288
KG1a Cell Viability Assay 0-10 μM 24 h DMSO IC50=7.68 μM, decreases cell viability in a dose-dependent manner 26552712
Kasumi-1 Cell Viability Assay 0-10 μM 24 h DMSO IC50=4.87 μM, decreases cell viability in a dose-dependent manner 26552712
KG1a Apoptosis Assay 0-10 μM 24 h DMSO induces cell apoptosis in a dose-dependent manner 26552712
Kasumi-1 Apoptosis Assay 0-10 μM 24 h DMSO induces cell apoptosis in a dose-dependent manner 26552712
MC-3  Growth Inhibition Assay 5/10/20 μM 24 h DMSO inhibits cell growth in a dose-dependent manner 26447615
HN22  Growth Inhibition Assay 2.5/7.5/22.5 μM 24 h DMSO inhibits cell growth in a dose-dependent manner 26447615
MC-3  Apoptosis Assay 5/10/20 μM 24 h DMSO induces caspase-mediated apoptosis 26447615
HN22  Apoptosis Assay 2.5/7.5/22.5 μM 24 h DMSO induces caspase-mediated apoptosis 26447615
MOLT-4 Growth Inhibition Assay 10-5000 nM 72 h DMSO IC50=0.198 μM 26392332
RS4;11 Growth Inhibition Assay 10-5000 nM 72 h DMSO IC50=0.002 μM 26392332
JURKAT Growth Inhibition Assay 10-5000 nM 72 h DMSO IC50=66 μM 26392332
CEM R Growth Inhibition Assay 10-5000 nM 72 h DMSO IC50=5.4 μM 26392332
CEM S Growth Inhibition Assay 10-5000 nM 72 h DMSO IC50=12.1 μM 26392332
MOLT-4 Apoptosis Assay 10-1000 nM 24 h DMSO causes the cleavage of Bcl-2 and the downregulation of Bcl-xL and Mcl-1 26392332
CEM S Apoptosis Assay 10-1000 nM 24 h DMSO causes the cleavage of Bcl-2 and the downregulation of Bcl-xL and Mcl-1 26392332
JURKAT Growth Inhibition Assay 100-1000 nM 48 h DMSO IC50=955±9.3 nM 26172269
LOUCY Growth Inhibition Assay 100-1000 nM 48 h DMSO IC50=32.8±10.9 nM 26172269
WM-115 Cell Viability Assay 100 nM 72 h enhances curcumin-induced anti-survival  26116776
B16 Cell Viability Assay 100 nM 72 h enhances curcumin-induced anti-survival  26116776
HL-60  Growth Inhibition Assay 72 h IC50 = 10.7 nM 26045609
MOLM-13  Growth Inhibition Assay 72 h IC50 = 27.9 nM 26045609
OCI-AML3 Growth Inhibition Assay 72 h IC50 = 1950 nM 26045609
BCWM.1 Apoptosis Assay 0-1.6 μM 24 h induces cell apoptosis 25893290
MWCL-1 Apoptosis Assay 0-1.6 μM 24 h induces cell apoptosis 25893290
MM.1s Apoptosis Assay 0-1.6 μM 24 h induces cell apoptosis 25893290
HCT116 Function Assay 3/10 μM 12 h  DMSO induces a dose-dependent increase in LC3B-II conversion and SQSTM1 degradation 25715028
HCT116 BAX BAK1 DKO Function Assay 3/10 μM 12 h  DMSO induces a dose-dependent increase in LC3B-II conversion and SQSTM1 degradation 25715028
HCT116 Function Assay 10 μM 12 h  DMSO increases GFP-LC3B puncta 25715028
HCT116 BAX BAK1 DKO Function Assay 10 μM 12 h  DMSO increases GFP-LC3B puncta 25715028
HCT116 Autophagy Assay 10 μM 12 h  DMSO induces a complete autophagic response 25715028
HCT116 BAX BAK1 DKO Autophagy Assay 10 μM 12 h  DMSO induces a complete autophagic response 25715028
U937 Apoptosis Assay 0.125-2 μM 24 h enhances DHA/X-11-induced apoptosis 25714024
U937  Apoptosis Assay 0.5 μM 24 h enhances cleavage of PARP and caspase-3 as well as Noxa level 25714024
HL-60 AAA-Bcl-2 Apoptosis Assay 0-5 μM 48 h IC50=0.87 μm，induces cell apoptosis in a dose-dependent manner 25711460
HL-60 EEE-Bcl-2 Apoptosis Assay 0-5 μM 48 h IC50=5 μm， induces cell apoptosis in a dose-dependent manner 25711460
U87 Function Assay 50 μM 24 h reduces the mRNA expression levels of MMP-2, MMP-14 and Bcl-2 25667663
K562 Cell Viability Assay 1-10 μM 48 h DMSO IC50=26.7 μM 25596561
K562/Mcl -1-IRESBim Growth Inhibition Assay IC50=9.3 μM 25535900
K562/Bcl- 2-IRESBim Growth Inhibition Assay IC50=0.35 μM 25535900
Jurkat Growth Inhibition Assay IC50=0.66 μM 25535900
JurkatΔBak Growth Inhibition Assay IC50>50 μM 25535900
HL60/VCR Growth Inhibition Assay IC50>100 μM 25535900
Kasumi-1 Growth Inhibition Assay IC50=0.01 μM 25535900
Kasumi-1/ABT Growth Inhibition Assay IC50=0.51 μM 25535900
THP-1 Growth Inhibition Assay IC50=1.27 μM 25535900
U937 Growth Inhibition Assay IC50=5.29 μM 25535900
C1498 Growth Inhibition Assay IC50=6.13 μM 25535900
RPMI 8226 Growth Inhibition Assay IC50=0.25 μM 25535900
MM.1S Growth Inhibition Assay IC50=0.40 μM 25535900
NCI-H929 Growth Inhibition Assay IC50=15.21 μM 25535900
U266 Growth Inhibition Assay IC50=0.68 μM 25535900
MCF-7 Cell Viability Assay 5 μM 48 h DMSO enhances the sensitivity to or radiation 25409124
MCF-7 Apoptosis Assay 5 μM 4/24/48 h DMSO increases the cleaved PARP 25409124
MCF-7 Function Assay 5 μM 24 h DMSO enhances thelevel of Mcl-1 expression  25409124
MDA-MB 231  Function Assay 5 μM 24 h DMSO enhances thelevel of Mcl-1 expression  25409124
ZR-75-1  Function Assay 5 μM 24 h DMSO enhances thelevel of Mcl-1 expression  25409124
A549 Cell Viability Assay 0-20 μM 72 h DMSO decreases the cell survival in a dose-dependent manner combined with aspirin 25388762
H1299 Cell Viability Assay 0-20 μM 72 h DMSO decreases the cell survival in a dose-dependent manner combined with aspirin 25388762
HO-8910 Cell Viability Assay 0-20 μM 72 h DMSO decreases the cell survival in a dose-dependent manner combined with aspirin 25388762
HT-29 Cell Viability Assay 0-20 μM 72 h DMSO decreases the cell survival in a dose-dependent manner combined with aspirin 25388762
HCT-116 Cell Viability Assay 0-20 μM 72 h DMSO decreases the cell survival in a dose-dependent manner combined with aspirin 25388762
A549 Apoptosis Assay 20 μM 48 h DMSO induces apoptosis significantly combined with aspirin 25388762
H1299 Apoptosis Assay 20 μM 48 h DMSO induces apoptosis significantly combined with aspirin 25388762
Sc-1 Cell Viability Assay 0.0001-1 μM 96 h decreases the cell viability in a dose-dependent manner 25373508
OcI-LY18 Cell Viability Assay 0.0001-1 μM 96 h decreases the cell viability in a dose-dependent manner 25373508
RL  Cell Viability Assay 0.0001-1 μM 96 h decreases the cell viability in a dose-dependent manner 25373508
RKO Cell Viability Assay 0-10 μM 24 h  DMSO IC50> 25 µM 25304383
Caco-2 Cell Viability Assay 0-10 μM 24 h  DMSO IC50=19.7 µM 25304383
DLD1 Cell Viability Assay 0-10 μM 24 h  DMSO IC50=18.78 µM 25304383
LS411N Cell Viability Assay 0-10 μM 24 h  DMSO IC50=11.47 µM 25304383
SW620 Cell Viability Assay 0-10 μM 24 h  DMSO IC50=12.24 µM 25304383
HCT116 Cell Viability Assay 0-10 μM 24 h  DMSO IC50=20.49 µM 25304383
HaCaT Cell Viability Assay 0.1/1/10 μM 24 h DMSO decreases cell viability in a dose-dependent manner 25210795
A5-RT3 Cell Viability Assay 0.1/1/10 μM 24 h DMSO decreases cell viability in a dose-dependent manner 25210795
HaCaT Function Assay 10 μM 24/48 h DMSO induces MMP and DNA fragmentation 25210795
A5-RT3 Function Assay 10 μM 24/48 h DMSO induces MMP and DNA fragmentation 25210795
A5-RT3 Function Assay 5 μM 6 h DMSO induces the release of mitochondrial proteins and reduces clonogenic survival in a caspase-independent manner 25210795
U266 Function Assay 500/750 nM 24/48 h DMSO downregulates Bim, principally the EL isoform 25208888
RPMI8226 Function Assay 500/750 nM 24/48 h DMSO downregulates Bim, principally the EL isoform 25208888
MM.1S Function Assay 500/750 nM 24/48 h DMSO downregulates Bim, principally the EL isoform 25208888
Clone A Growth Inhibition Assay 0.2–60 μM 72 h DMSO IC50=7.5 μM 25208882
CX-1 Growth Inhibition Assay 0.2–60 μM 72 h DMSO IC50=1.8 μM 25208882
LS174T Growth Inhibition Assay 0.2–60 μM 72 h DMSO IC50=18.3 μM 25208882
HT29 Apoptosis Assay 1/5/10 μM 48 h causes cell death in a dose-dependent manner 25192188
SW480 Apoptosis Assay 1/5/10 μM 48 h causes cell death in a dose-dependent manner 25192188
Colo205 Apoptosis Assay 1/5/10 μM 48 h causes cell death in a dose-dependent manner 25192188
Caco2 Apoptosis Assay 1/5/10 μM 48 h causes cell death in a dose-dependent manner 25192188
PCI-13 Growth Inhibition Assay 72 h DMSO GI50=15 ± 1.8 μM 25139387
PCI-15B Growth Inhibition Assay 72 h DMSO GI50=11 ± 4.5 μM 25139387
UM-SCC22B Growth Inhibition Assay 72 h DMSO GI50=19 ± 2.9 μM 25139387
UM-SCC47 Growth Inhibition Assay 72 h DMSO GI50=19 ± 12.3 μM 25139387
93-VU-147T Growth Inhibition Assay 72 h DMSO GI50=4.3 ± 3.5 μM 25139387
UD-SCC2 Growth Inhibition Assay 72 h DMSO GI50=28 ± 2.9 μM 25139387
UPCI:SCC90 Growth Inhibition Assay 72 h DMSO GI50=6.6 ± 1.5 μM 25139387
RPMI-8226  Cell Viability Assay 125/250/500 nM 48h  DMSO decreases cell viability in a dose-dependent manner 25008202
OPM-2  Cell Viability Assay 125/250/500 nM 48h  DMSO decreases cell viability in a dose-dependent manner 25008202
RPMI-8226  Apoptosis Assay 125/250/500 nM 48h  DMSO induces cell apoptosis in a dose-dependent manner 25008202
OPM-2  Apoptosis Assay 125/250/500 nM 48h  DMSO induces cell apoptosis in a dose-dependent manner 25008202
COG-LL-319 Function Assay 100 nM 1/3/6 h DMSO induces caspase-dependent Mcl-1 cleavage 24951472
RS4;11 Function Assay 100 nM 1/3/6 h DMSO induces caspase-dependent Mcl-1 cleavage 24951472
FL5.12 Function assay Reversal of cytokine withdrawal protection in IL3 dependent Bcl2 overexpressing mouse FL5.12 cells in presence of bovine gelatin, EC50 = 0.008 μM. 17256834
DoHH2 Growth inhibition assay Inhibition of cell growth in human DoHH2 cells overexpressing Bcl2 in presence of 3% FBS, EC50 = 0.0083 μM. 17256834
RS11380 Growth inhibition assay Inhibition of cell growth in human RS11380 cells overexpressing Bcl2 in presence of 3% FBS, EC50 = 0.014 μM. 17256834
FL5.12 Function assay Reversal of cytokine withdrawal protection in IL3 dependent Bcl-xL overexpressing mouse FL5.12 cells in presence of bovine gelatin, EC50 = 0.03 μM. 17256834
FL5.12 Function assay Reversal of cytokine withdrawal protection in IL3 dependent Bcl2 overexpressing mouse FL5.12 cells in presence of 3% FBS, EC50 = 0.05 μM. 17256834
DoHH2 Growth inhibition assay Inhibition of cell growth in human DoHH2 cells overexpressing Bcl2 in presence of 10% HS, EC50 = 0.13 μM. 17256834
RS11380 Growth inhibition assay Inhibition of cell growth in human RS11380 cells overexpressing Bcl2 in presence of 10% HS, EC50 = 0.15 μM. 17256834
SUDHL4 Growth inhibition assay Inhibition of cell growth in human SUDHL4 cells overexpressing Bcl2 in presence of 3% FBS, EC50 = 0.22 μM. 17256834
FL5.12 Function assay Reversal of cytokine withdrawal protection in IL3 dependent Bcl-xL overexpressing mouse FL5.12 cells in presence of 3% FBS, EC50 = 0.22 μM. 17256834
SUDHL4 Growth inhibition assay Inhibition of cell growth in human SUDHL4 cells overexpressing Bcl2 in presence of 10% HS, EC50 = 0.85 μM. 17256834
FL5.12 Cytotoxicity assay 24 hrs Cytotoxicity against IL3-dependent mouse FL5.12 cells overexpressing human Bcl2 assessed as cell viability after 24 hrs by MTS assay in absence of serum, EC50 = 0.0077 μM. 18841882
FL5.12 Cytotoxicity assay 24 hrs Cytotoxicity against IL3-dependent mouse FL5.12 cells overexpressing human Bcl-XL assessed as cell viability after 24 hrs by MTS assay in absence of serum, EC50 = 0.03 μM. 18841882
NCI-H146 Cytotoxicity assay 48 hrs Cytotoxicity against human NCI-H146 cells assessed as cell viability after 48 hrs in presence of 10% human serum, EC50 = 0.087 μM. 18841882
CLL Apoptosis assay Induction of apoptosis in human CLL cells, EC50 = 0.0045 μM. 20925433
MEF Cytotoxicity assay 24 hrs Cytotoxicity against mouse mcl-1 deficient MEF cells after 24 hrs by Cell titer glo assay in presence of 1% serum, EC50 = 0.00203 μM. 21366295
MEF Cytotoxicity assay 24 hrs Cytotoxicity against mouse mcl-1 deficient MEF cells after 24 hrs by Cell titer glo assay in presence of 10% serum, EC50 = 0.051 μM. 21366295
MEF Cytotoxicity assay 24 hrs Cytotoxicity against mouse mcl-1 deficient MEF cells after 24 hrs by Cell titer glo assay in presence of 10% fetal bovine serum, EC50 = 0.051 μM. 21366295
RS4:11 Antiproliferative assay Antiproliferative activity against human RS4:11 cells in presence of 10% human serum, EC50 = 0.024 μM. 28926247
MOLT4 Antiproliferative assay Antiproliferative activity against human MOLT4 cells in presence of 10% human serum, EC50 = 0.622 μM. 28926247
Jurkat Cytotoxicity assay 48 hrs Cytotoxicity against human Jurkat cells after 48 hrs by cell titer-blue assay, IC50 = 1.38 μM. 19743858
HCT116 Cytotoxicity assay 48 hrs Cytotoxicity against human HCT116 cells after 48 hrs by cell titer-blue assay, IC50 = 4.06 μM. 19743858
SU-8686 Cytotoxicity assay 48 hrs Cytotoxicity against human SU-8686 cells after 48 hrs by cell titer-blue assay, IC50 = 4.24 μM. 19743858
H460 Cytotoxicity assay 48 hrs Cytotoxicity against human H460 cells after 48 hrs by cell titer-blue assay, IC50 = 8.03 μM. 19743858
Hepa-1c1c7 Cytotoxicity assay 48 hrs Cytotoxicity against mouse Hepa-1c1c7 cells after 48 hrs by cell titer-blue assay, IC50 = 8.68 μM. 19743858
MCF7 Cytotoxicity assay 48 hrs Cytotoxicity against human MCF7 cells after 48 hrs by cell titer-blue assay, IC50 = 21.26 μM. 19743858
DU145 Cytotoxicity assay 48 hrs Cytotoxicity against human DU145 cells after 48 hrs by cell titer-blue assay, IC50 = 27.6 μM. 19743858
HCT116 Cytotoxicity assay 72 hrs Cytotoxicity against human HCT116 cells expressing Bcl-xL, Bcl-2 and Mcl-1 after 72 hrs by MTT assay, IC50 = 47.7 μM. 22172701
BL21 (DE3) Function assay 2 hrs Binding affinity to N-terminus 6X His-tagged human Bcl2 expressed in Escherichia coli BL21 (DE3) cells after 2 hrs by fluorescence polarization assay, IC50 = 0.002 μM. 22448988
BL21 (DE3) Function assay 2 hrs Binding affinity to N-terminus 8X His-tagged human Bcl-xL expressed in Escherichia coli BL21 (DE3) cells after 2 hrs by fluorescence polarization assay, IC50 = 0.006 μM. 22448988
NCI-H146 Growth inhibition assay 4 days Growth inhibition of human NCI-H146 cells after 4 days by WST8 assay, IC50 = 0.097 μM. 22448988
NCI-H1417 Growth inhibition assay 4 days Growth inhibition of human NCI-H1417 cells after 4 days by WST8 assay, IC50 = 0.13 μM. 22448988
CCRF-CEM Cytotoxicity assay 48 hrs Cytotoxicity against human CCRF-CEM cells assessed as cell viability after 48 hrs by celltiter-blue assay, IC50 = 0.74 μM. 22582991
HL60 Cytotoxicity assay 48 hrs Cytotoxicity against human HL60 cells assessed as cell viability after 48 hrs by celltiter-blue assay, IC50 = 0.76 μM. 22582991
K562 Cytotoxicity assay 48 hrs Cytotoxicity against human K562 cells assessed as cell viability after 48 hrs by celltiter-blue assay, IC50 = 34.7 μM. 22582991
NCI-H146 Antiproliferative assay 4 days Antiproliferative activity against human NCI-H146 cells after 4 days by WST8 assay, IC50 = 0.037 μM. 22747598
NCI-H1963 Antiproliferative assay 4 days Antiproliferative activity against human NCI-H1963 cells after 4 days by WST8 assay, IC50 = 0.059 μM. 22747598
NCI-H1417 Antiproliferative assay 4 days Antiproliferative activity against human NCI-H1417 cells after 4 days by WST8 assay, IC50 = 0.412 μM. 22747598
RS4:11 Apoptosis assay 48 hrs Induction of apoptosis in Bcl2 dependent human RS4:11 cells after 48 hrs by Annexin V staining based flow cytometry, IC50 = 0.27 μM. 23314054
K562 Apoptosis assay 48 hrs Induction of apoptosis in Mcl1 dependent human K562 cells after 48 hrs by Annexin V staining based flow cytometry, IC50 = 16.4 μM. 23314054
NCI-H1963 Cytotoxicity assay 4 days Cytotoxicity against human NCI-H1963 cells assessed as growth inhibition after 4 days by WST assay, IC50 = 0.054 μM. 23448298
NCI-H187 Cytotoxicity assay 4 days Cytotoxicity against human NCI-H187 cells assessed as growth inhibition after 4 days by WST assay, IC50 = 0.1377 μM. 23448298
NCI-H1417 Cytotoxicity assay 4 days Cytotoxicity against human NCI-H1417 cells assessed as growth inhibition after 4 days by WST assay, IC50 = 0.1734 μM. 23448298
HL60 Growth inhibition assay 72 hrs Growth inhibition of human HL60 cells after 72 hrs by MTT assay, IC50 = 0.97 μM. 27712939
MCF7 Growth inhibition assay 72 hrs Growth inhibition of human MCF7 cells after 72 hrs by MTT assay, IC50 = 25.33 μM. 27712939
U266 Growth inhibition assay 72 hrs Growth inhibition of human U266 cells after 72 hrs by MTT assay, IC50 = 27.35 μM. 27712939
SKOV3 Growth inhibition assay 72 hrs Growth inhibition of human SKOV3 cells after 72 hrs by MTT assay, IC50 = 46.59 μM. 27712939
RS4:11 Cytotoxicity assay 24 hrs Cytotoxicity against human RS4:11 cells assessed as reduction in cell viability after 24 hrs by MTT assay, IC50 = 0.33 μM. 29453135
Remb1 Cytotoxicity assay 24 hrs Cytotoxicity against human Remb1 cells assessed as reduction in cell viability after 24 hrs by MTT assay, IC50 = 1.4 μM. 29453135
BL21 Function assay 10 uM 3 hrs Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 G196A mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay, Ki = 0.001 μM. 21807512
BL21 Function assay 10 uM 3 hrs Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 A93V mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay, Ki = 0.0014 μM. 21807512
BL21 Function assay 10 uM 3 hrs Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 Y195F mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay, Ki = 0.0015 μM. 21807512
BL21 Function assay 10 uM 3 hrs Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Wild type Bcl-2-like protein 1 expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay, Ki = 0.0034 μM. 21807512
BL21 Function assay 10 uM 3 hrs Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 E129H mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay, Ki = 0.0045 μM. 21807512
BL21 Function assay 10 uM 3 hrs Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 E96G mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay, Ki = 0.0058 μM. 21807512
BL21 Function assay 10 uM 3 hrs Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 A142Gdelta136T mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay, Ki = 0.01 μM. 21807512
BL21 Function assay 10 uM 3 hrs Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 A142G mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay, Ki = 0.021 μM. 21807512
BL21 Function assay 10 uM 3 hrs Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 L130V mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay, Ki = 0.058 μM. 21807512
BL21 Function assay 10 uM 3 hrs Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 delta136T mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay, Ki = 0.06 μM. 21807512
BL21 Function assay 10 uM 3 hrs Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 L130A mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay, Ki = 0.073 μM. 21807512
BL21 Function assay 10 uM 3 hrs Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 R100E mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay, Ki = 0.16 μM. 21807512
BL21 Function assay 10 uM 3 hrs Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 V141A mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay, Ki = 0.19 μM. 21807512
BL21 Function assay 10 uM 3 hrs Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 A142T mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay, Ki = 0.27 μM. 21807512
BL21 Function assay 10 uM 3 hrs Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 L130G mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay, Ki = 0.29 μM. 21807512
BL21 Function assay 10 uM 3 hrs Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 F97V mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay, Ki = 0.3 μM. 21807512
BL21 Function assay 10 uM 3 hrs Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 Y101H mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay, Ki = 0.38 μM. 21807512
BL21 (DE3) Function assay 2 hrs Binding affinity to N-terminus 6X His-tagged human Bcl2 expressed in Escherichia coli BL21 (DE3) cells after 2 hrs by fluorescence polarization assay, Ki = 0.0006 μM. 22448988
BL21 (DE3) Function assay 2 hrs Binding affinity to N-terminus 8X His-tagged human Bcl-xL expressed in Escherichia coli BL21 (DE3) cells after 2 hrs by fluorescence polarization assay, Ki = 0.001 μM. 22448988
Toledo Apoptosis assay Induction of apoptosis in human Toledo cells, LD50 = 0.06 μM. 24900652
KB Cytotoxicity assay 0.5 uM Cytotoxicity in human siRNA-mediated-MCL1-kncok down KB cells overexpressing BCL2 at 0.5 uM 18040043
Eu-Myc Apoptosis assay 1 uM Induction of apoptosis in mouse Eu-Myc cells overexpressing BCL2 assessed as inhibition of colony formation at 1 uM 18040043
HeLa Function assay 1 uM 12 hrs Induction of Bcl-xL-mediated apoptosis in doxycyclin-stimulated human HeLa cells overexpressing Noxa at 1 uM after 12 hrs by Hoechst staining 22386982
HeLa Function assay 10 uM 16 hrs Inhibition of Rluc-Bax/eYFP-Bcl-xL interaction expressed in human HeLa cells at 10 uM after 16 hrs by BRET assay 22425031
MDA-MB-231 Function assay 0.03 to 1 uM 1 hr Antagonist activity at recombinant Bcl-XL assessed as restoration of BIM BH3-induced Smac protein release in mitochondria isolated from MDA-MB-231 cells at 0.03 to 1 uM after 1 hr by Western blot analysis 22747598
MDA-MB-231 Function assay 0.03 to 1 uM 1 hr Antagonist activity at recombinant Bcl-XL assessed as restoration of BIM BH3-induced cytochrome c release in mitochondria isolated from MDA-MB-231 cells at 0.03 to 1 uM after 1 hr by Western blot analysis 22747598
BP3 Apoptosis assay 10 uM 24 hrs Induction of apoptosis in human BP3 cells at 10 uM incubated for 24 hrs by Annexin V and propidium iodide staining based FACS method 23047228
IM9 Apoptosis assay 10 uM 24 hrs Induction of apoptosis in human IM9 cells at 10 uM incubated for 24 hrs by Annexin V and propidium iodide staining based FACS method 23047228
RS4:11 Apoptosis assay 10 uM 24 hrs Induction of apoptosis in human RS4:11 cells at 10 uM incubated for 24 hrs by Annexin V and propidium iodide staining based FACS method 23047228
HCT116 Apoptosis assay 48 hrs Induction of apoptosis in human HCT116 p53+/+ cells after 48 hrs by Annexin V-FITC staining-based flow cytometric method 26982372
DMS53 Apoptosis assay 5 to 10 uM 12 hrs Induction of apoptosis in human DMS53 cells harboring p53 mutant assessed as cytochrome c release at 5 to 10 uM after 12 hrs by immunoblotting method 26982372
DMS53 Function assay 5 to 10 uM 12 hrs Inhibition of BCl-2/Bim interaction in human DMS53 cells harboring p53 mutant at 5 to 10 uM after 12 hrs by immunoprecipitation method 26982372
DMS53 Apoptosis assay 5 to 10 uM 12 hrs Induction of apoptosis in human DMS53 cells harboring p53 mutant assessed as PARP cleavage at 5 to 10 uM after 12 hrs by immunoblotting method 26982372
DMS53 Apoptosis assay 5 to 10 uM 12 hrs Induction of apoptosis in human DMS53 cells harboring p53 mutant assessed as caspase-3 cleavage at 5 to 10 uM after 12 hrs by immunoblotting method 26982372
DMS53 Function assay 5 to 10 uM 12 hrs Inhibition of BCl-2/Bax interaction in human DMS53 cells harboring p53 mutant at 5 to 10 uM after 12 hrs by immunoprecipitation method 26982372
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
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY 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
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
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
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells 29435139
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY 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
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) 29435139
Rh30 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 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
U-2 OS qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 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
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
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 163 mg/mL (200.38 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight
Dilution Calculator Molecular Weight Calculator

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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mg/kg
g
μL

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% DMSO
%
% Tween 80
% ddH2O
% DMSO
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Calculation results:

Working concentration: mg/ml;

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. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight 813.43 Formula

C42H45ClN6O5S2

 Storage (From the date of receipt)
CAS No. 852808-04-9 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CN(C)CCC(CSC1=CC=CC=C1)NC2=C(C=C(C=C2)S(=O)(=O)NC(=O)C3=CC=C(C=C3)N4CCN(CC4)CC5=CC=CC=C5C6=CC=C(C=C6)Cl)[N+](=O)[O-]

Mechanism of Action

Features
First-generation inhibitor of anti-apoptotic Bcl-2 proteins.
Targets/IC50/Ki
Bcl-2
(Cell-free assay)
30.3 nM(EC50)
Bcl-xL
(Cell-free assay)
78.7 nM(EC50)
Bcl-w
(Cell-free assay)
197.8 nM(EC50)
Bcl-B
(Cell-free assay)
1.82 μM(EC50)
In vitro
ABT-737 shows low activity to Bcl-B and no effects to Mcl-1 and BFL-1. This compound is sensitive to HL60, KG1 and NB4 cells with IC50 of 50 nM, 80 nM and 80 nM, respectively. It induces apoptosis in HL60 cells, which due to decreased Bcl-2/Bax heterodimerization and has no effect on cell cycle distribution. It also induces cytochrome c release from purified mitochondria and promotes conformational changes in Bax that are associated with apoptosis. Resistant cells (Hela and MCF-7) can be sensitized to this chemical by approaches that down-regulate, destabilize, or inactivate Mcl-1. It also causes Bax/BAK-dependent cytochrome c release only when Mcl-1 has been neutralized. This compound displaces Bim from Bcl2's BH3-binding pocket, allowing Bim to activate Bax, induce mitochondrial permeabilization, and rapidly commit the primary chronic lymphocytic leukemia (CLL) cells to death. Knockdown of Mcl-1 with siRNA sensitizes two resistant SCLC cell lines H196 and DMS114 to it by enhancing the induction of apoptosis. Likewise, up-regulation of Noxa sensitizes H196 cells to this chemical. It inhibits proliferation and induces apoptosis in many SCLC cell lines including NCI-H889, NCI-H1963, NCI-H1417, NCI-H146 and etc. Bcl-2 and Noxa may contribute mechanistically to the cellular response to it in NCI-H146 cells. A recent study shows that it significantly induces apoptosis in HTLV-1 infected T-cell lines as well as in fresh ATLL cells.
Kinase Assay
Fluorescence polarization assays
Binding affinity of GST-Bcl-2 family proteins to the FITC-conjugated BH3 domain of Bim (FITC-Ahx-DMRPEIWIAQELRRIGDEFNAYYAR) is determined. Briefly, 100 nM of GST-Bcl-2 family fusion proteins are incubated with serial dilutions of ABT-737 in PBS for 2 min. Then, 20 nM of FITC-Bim BH3 peptide (FITC-Ahx-DMRPEIWIAQELRRIGDEFNAYYAR) is added. Fluorescence polarization is measured using an Analyst TM AD Assay Detection System after 10 min using the 96-well black plate. Then IC50 are determined.
In vivo
In aggressive leukemia model, ABT-737 suppresses the leukemia burden by 53% at the 30 mg/kg, with significantly extended survival of mice. This compound does not induce significantly abnormalities in blood cell counts or serum chemistries. It prolongs the survival of recipient mice transplanted with Bcl-2-transduced tumors. This chemical shows great antitumor activity in an ATLL mouse model at a dose of 100 mg/kg.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/17283153/
  • [5] https://pubmed.ncbi.nlm.nih.gov/22138435/
  • [6] https://pubmed.ncbi.nlm.nih.gov/18451169/
  • [7] https://pubmed.ncbi.nlm.nih.gov/18604177/
  • [8] https://pubmed.ncbi.nlm.nih.gov/18591385/
  • [9] https://pubmed.ncbi.nlm.nih.gov/19246337/

Applications

Methods Biomarkers Images PMID
Western blot PARP / c-PARP / cleaved caspase 3 Hif-1a γ-H2AX / p-ATM
S1002-WB1
21393866
Immunofluorescence cytochrome C Bax Bim AIF p65
S1002-IF1
26447615
Growth inhibition assay Cell viability
S1002-viability1
22311987
ELISA IL-6 / IL-8
S1002-ELISA1
21084274

Tech Support

Handling Instructions

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Frequently Asked Questions

Question 1:
What is the recommended method for reconstituting it for in vivo animal study?

Answer:
For oral administration, we suggest the vehicle: 30% Propylene glycol, 5% Tween 80, 65% D5W, at up to 30mg/ml; For injection, it can be dissolved in 2% DMSO/50% PEG 300/5% Tween 80/ddH2O at 2.5 mg/ml.

Signaling Pathway Map