Molecular Weight(MW): 850.04
A-1210477 is a potent and selective MCL-1 inhibitor with Ki and IC50 of 0.454 nM and 26.2 nM, respectively, >100-fold selectivity over other Bcl-2 family members.
Cited by 9 Publications
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U251 glioblastoma (F) or MeWo melanoma (G) cells were treated with selective BH-3 mimetics, GTPP or the combination of both for 24 h (U251) or 48 h (MeWo). Thereafter, cells were stained with annexin V and propidium iodide and analyzed by flow cytometry. Shown are representative flow plots.
Cancer Research, 2017, doi:10.1158/0008-5472. A-1210477 purchased from Selleck.
Cells were treated for 48 h of control (DMSO), 5 μM A-1210477, 3.3 μM ABT-263 or the combination of 5 μM A-1210477 plus 3.3 μM ABT-263, and then subjected to Immunoblot with an antibody recognizing full length and cleaved PARP. The combination treatment increased the cleaved: full-length PARP ratio in all lines. Molecular weight markers are in kDa.
Cell Death Dis, 2018, 9(9):907. A-1210477 purchased from Selleck.
(d) MVA protects against cell death in HeLa induced by the Mcl-1 inhibitor A-1210477. HeLa cells were infected with MVA (MOI=10) for 18 h and afterwards treated with the Mcl-1 inhibitor A-1210477 (10 μM) for 4 h. Apoptosis induction was measured as the percentage of cells positive for active caspase-3 by flow cytometry. Data are representative of three independent experiments (**P=0.007; two-tailed paired t-test).
Cell Death Dis, 2016, 7(8):e2340. . A-1210477 purchased from Selleck.
C. FACs analysis of KCNR after 72-hour treatment with 10 nmol/L ABT199 alone or in combination with 10 μmol/L A-1210477. Data represent the mean percentages of cells in sub-G1 ± SD of three replicate experiments. D. in vitro effects on BIM displacement from BCL-2 and MCL-1 after 24-hour treatment of KCNR with 10 nmol/L of ABT199 or 10μmol/L of A-1210477 and a combination of both compounds. BIM displacement was established by detecting BIM/BCL-2 and BIM/MCL-1 complex levels by anti-BCL-2 and anti-MCL-1 immunoprecipitation, followed by Western blotting for BIM. BCL-2 and MCL-1 levels served as loading control.
Oncotarget, 2016, 7(19):27946-58. A-1210477 purchased from Selleck.
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Choose Selective Bcl-2 Inhibitors
|Description||A-1210477 is a potent and selective MCL-1 inhibitor with Ki and IC50 of 0.454 nM and 26.2 nM, respectively, >100-fold selectivity over other Bcl-2 family members.|
In H929 cells, A-1210477 binds to MCL-1 with high affinity and induces MCL-1 protein elevation. In H929, H2110, and H23 cells, A-1210477 induce the hallmarks of apoptosis, and inhibits MCL-1-dependent cell viability. A-1210477 also synergizes with navitoclax to kill a variety of cancer cell lines.  In SKBR3 cells, A-1210477 inhibits MCL-1–BIM interaction and induces classical features of apoptosis.  In addition, A-1210477 sensitizes non-Hodgkin's lymphoma cell lines to venetoclax (ABT-199). 
Binding affinity assays:TR-FRET-binding affinity assays are performed for BCL-2, BCL-XL, and MCL-1 in 4.52 mM monobasic potassium phosphate, 15.48 mM dibasic potassium phosphate, 1 mM sodium EDTA, 0.05% Pluronic F-68 detergent, 50 mM sodium chloride, and 1 mM DTT (pH 7.5). For MCL-1 assays, GST-tagged MCL-1 (1 nM) is mixed with 100 nM f-Bak, 1 nM Tb-labeled anti-GST antibody, and compound at room temperature (RT) for 60 min. Fluorescence is measured on an Envision plate reader using a 340/35 nm excitation filter and 520/525 (f-Bak) and 495/510 nm (Tb-labeled anti-GST antibody) emission filters.
|In vitro||DMSO||3 mg/mL warmed (3.52 mM)|
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