PARP/EZH2-IN-1
PARP/EZH2-IN-1 is a first-in-class dual PARP-1/EZH2 inhibitor with IC50 values of 6.87 nM and 36.51 nM, respectively. PARP/EZH2-IN-1 induces autophagy in cancer cells and shows potent antiproliferative activity in BRCA wild-type triple-negative breast cancer cells.
For research use only. We do not sell to patients.
- CAS No.: 2687273-52-3
- Formula: C43H41FN8O5
- Molecular Weight:768.83
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Storage:
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
- Purity & Documentation
- References
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Help & FAQs
All Histone Methyltransferase Isoforms
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Biological Activity
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PARP-1 6.87 nM (IC50) |
EZH2 36.51 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| MCF-10A | IC50 |
>50 μM
Compound: 5a
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Antiproliferative activity against human MCF-10A cells assessed as cell viability after 72 hrs by MTT assay
Antiproliferative activity against human MCF-10A cells assessed as cell viability after 72 hrs by MTT assay
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[PMID: 34455779] |
| MCF7 | IC50 |
12.11 μM
Compound: 5a
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Antiproliferative activity against human MCF7 cells assessed as cell viability after 72 hrs by MTT assay
Antiproliferative activity against human MCF7 cells assessed as cell viability after 72 hrs by MTT assay
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[PMID: 34455779] |
| MDA-MB-231 | IC50 |
2.63 μM
Compound: 5a
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Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability after 72 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability after 72 hrs by MTT assay
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[PMID: 34455779] |
| MDA-MB-468 | IC50 |
0.41 μM
Compound: 5a
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Antiproliferative activity against human MDA-MB-468 cells assessed as cell viability after 72 hrs by MTT assay
Antiproliferative activity against human MDA-MB-468 cells assessed as cell viability after 72 hrs by MTT assay
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[PMID: 34455779] |
PARP/EZH2-IN-1 (Compound 5a) (72 h) exhibits potent antiproliferative activity against MDA-MB-231 cells (IC50 = 2.63 μM) and MDA-MB-468 cells (IC50 = 0.41 μM)[1].
PARP/EZH2-IN-1 (72 h) shows weaker activity against MCF-7 cells (IC50 = 12.11 μM) and negligible cytotoxicity against MCF-10A cells (IC50 > 50 μM), and binds EZH2 with a Kd of 14.56 nM[1].
PARP/EZH2-IN-1 (0.5-7.5 μM; 48 h) downregulates BRCA1, BRCA2, EZH2, and CARM1 protein levels in MDA-MB-231 and MDA-MB-468 cells[1].
PARP/EZH2-IN-1 (2.5-7.5 μM; 48 h) induces excessive autophagy rather than apoptosis in MDA-MB-231 and MDA-MB-468 cells, accompanied by concentration-dependent increases of Beclin-1 and LC3B-II and a decrease of p62[1].
PARP/EZH2-IN-1 (7.5 μM; 0-32 h) modulates autophagy-related proteins in a time-dependent manner, leading to autophagic cell death after 8 h in MDA-MB-231 cells[1].
Knockdown of PARP-1 or EZH2 partially rescues the antiproliferative effect of PARP/EZH2-IN-1 in MDA-MB-231 and MDA-MB-468 cells. Additionally, the compound has basically no effect on cell apoptosis and reactive oxygen species (ROS) levels in these cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-231, MDA-MB-468, MCF-7, MCF-10A cells
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Concentration:various concentrations
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Incubation Time:72 h
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Result:Exhibited potent antiproliferative activity against MDA-MB-231 cells (IC50 = 2.63 μM) and MDA-MB-468 cells (IC50 = 0.41 μM), weaker activity against MCF-7 cells (IC50 = 12.11 μM), and negligible cytotoxicity against MCF-10A cells (IC50 > 50 μM).
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Cell Line:MDA-MB-231 and MDA-MB-468 cells
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Concentration:2.5 μM, 5.0 μM, 7.5 μM (MDA-MB-231); 0.5 μM, 1.0 μM, 2.0 μM (MDA-MB-468)
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Incubation Time:48 h
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Result:Significantly down-regulated BRCA1, BRCA2, EZH2, and CARM1 protein levels.
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Cell Line:MDA-MB-231 and MDA-MB-468 cells
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Concentration:2.5 μM, 5.0 μM, 7.5 μM (MDA-MB-231); 0.5 μM, 1.0 μM, 2.0 μM (MDA-MB-468)
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Incubation Time:48 h
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Result:Increased Beclin-1 and LC3B-II expression and decreased p62 levels in a concentration-dependent manner.
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Cell Line:MDA-MB-231 cells
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Concentration:5.0 μM
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Incubation Time:12 h
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Result:Induced abundant autophagic vacuoles, autophagosomes, and autophagic lysosomes.
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Cell Line:MDA-MB-231 and MDA-MB-468 cells
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Concentration:2.5 μM, 5.0 μM, 7.5 μM (MDA-MB-231); 0.5 μM, 1.0 μM, 2.0 μM (MDA-MB-468)
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Incubation Time:48 h
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Result:Increased autophagosome formation and autophagic activity in a concentration-dependent manner as shown by MDC-EB staining and LC3B immunofluorescence.
Chemical Information
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CAS No. 2687273-52-3
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Molecular Weight 768.83
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Formula C43H41FN8O5
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SMILES
O=C(C1=C(C(NC(C)=O)=CC(C2=CC=C(N=C2)N3CCN(CC3)C(C4=CC(CC5=NNC(C6=C5C=CC=C6)=O)=CC=C4F)=O)=C1)C)NCC7=C(C=C(NC7=O)C)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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