NCO-141
NCO-141 is a selective SIRT2 inhibitor with an IC50 of 0.5 μM. NCO-141 induces cell apoptosis via caspase activation and mitochondrial superoxide anion production. NCO-141 induces cell autophagy by increasing LC3-II levels and autophagosome accumulation. NCO-141 is applicable to relevant research on leukemia.
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- CAS No.: 1382354-26-8
- 화학식: C21H19FN2O2
- 분자량:350.39
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
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Biological Activity
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SIRT2 0.5 μM (IC50) |
NCO-141 (0.1-100 μM; 72 h) inhibits the growth of S1T, MT-2, Jurkat, and HL60 leukemic cell lines in a dose-dependent manner, with GI50 values of 34.9 μM, 26.4 μM, 36.7 μM, and 12.1 μM, respectively[1].
NCO-141 (0.1-100 μM; 72 h) induces dose-dependent apoptosis in S1T, MT-2, Jurkat, and HL60 leukemic cell lines, with 100 μM treatment resulting in 85.3%, 39.0%, 85.9%, and 86.7% specific annexin V-positive cells, respectively[1].
NCO-141 (10-50 μM; 6 h) induces mitochondrial superoxide generation in S1T, MT-2, Jurkat, and HL60 leukemic cell lines[1].
NCO-141 (50-100 μM; 72 h) activates caspase-3, -8, and -9 in S1T, MT-2, Jurkat, and HL60 leukemic cell lines, but induces caspase-independent cell death as pan-caspase inhibition does not prevent cell death or caspase-associated markers[1].
NCO-141 (72 h) increases acetylated histone H4 levels and promotes nuclear p53 degradation in S1T, MT-2, Jurkat, and HL60 leukemic cell lines[1].
NCO-141 (25-100 μM; 24-48 h) induces autophagy in S1T, MT-2, Jurkat, and HL60 leukemic cell lines by increasing LC3-II levels, promoting autophagosome accumulation, and inhibiting autophagosome degradation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HTLV-1-infected CD4+ T-cell line S1T, HTLV-1-infected T-cell line MT-2, T-lineage acute lymphoblastic leukemia cell line Jurkat, acute myeloid leukemia cell line HL60
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Concentration:0.1, 1, 10 and 100 μM
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Incubation Time:72 h
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Result:Inhibited the growth of all four leukemic cell lines in a dose-dependent manner.
Achieved GI50 values of 34.9 μM for S1T cells, 26.4 μM for MT-2 cells, 36.7 μM for Jurkat cells, and 12.1 μM for HL60 cells.
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Cell Line:S1T, MT-2, Jurkat, HL60 cell lines
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Concentration:0.1, 1, 5, 10, 25, 50 and 100 μM
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Incubation Time:72 h
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Result:Induced dose-dependent increases in annexin V-positive cells across all four cell lines.
At 100 μM, reached percentages of specific annexin V-positive cells of 85.3% for S1T cells, 39.0% for MT-2 cells, 85.9% for Jurkat cells, and 86.7% for HL60 cells.
Induced early-phase apoptosis (annexin V+/7-amino-actinomycin D- cells) and DNA fragmentation via TUNEL assay.
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Cell Line:S1T, MT-2, Jurkat, HL60 cell lines
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Concentration:25, 50 and 100 μM (48 h incubation); 50 μM (24 h incubation)
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Incubation Time:24 h (autophagic flux analysis); 48 h (Cyto-ID analysis, western blot)
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Result:Increased autophagy levels (detected via increased Cyto-ID fluorescence) in all four cell lines.
Significantly increased LC3-II (autophagic vesicle-associated) levels compared to untreated controls.
Induced LC3 translocation, and analysis of autophagic flux showed NCO-141 both promotes autophagosome formation and inhibits autophagosome degradation.
Chemical Information
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CAS No. 1382354-26-8
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분자량 350.39
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화학식 C21H19FN2O2
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SMILES
O=C(N)C1=CC=CC=C1NC2=CC=CC(OCCC3=CC=CC(F)=C3)=C2
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
NCO-141 Related Classifications
HY-185682 Related Classifications
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