PARP/EZH2-IN-2
PARP/EZH2-IN-2 (compound 12e) is a dual target PARP1 and EZH2 inhibitor, with IC50 values of 6.89 and 27.34 nM, respectively. PARP/EZH2-IN-2 shows anticancer activity, with no toxicity to normal cells. PARP/EZH2-IN-2 achieves synthetic lethality indirectly by inhibiting EZH2 to increase the sensitivity to PARP1, and induces cell death by regulating excessive autophagy.
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- CAS No.: 3026744-15-7
- 화학식: C33H31N7O3
- 분자량:573.64
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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
- 순도&문서
- References
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Help & FAQs
All Histone Methyltransferase Isoforms
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Biological Activity
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PARP1 6.89 ± 0.7 nM (IC50) |
EZH2 27.34 ± 1. nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BT-549 | IC50 |
0.91 μM
Compound: 12e
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Cytotoxicity against human BT-549 cells incubated for 72 hrs by MTT assay
Cytotoxicity against human BT-549 cells incubated for 72 hrs by MTT assay
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[PMID: 38134746] |
| MCF-10A | IC50 |
>40 μM
Compound: 12e
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Cytotoxicity against human MCF-10A cells incubated for 72 hrs by MTT assay
Cytotoxicity against human MCF-10A cells incubated for 72 hrs by MTT assay
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[PMID: 38134746] |
| MDA-MB-231 | IC50 |
2.84 μM
Compound: 12e
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Cytotoxicity against human MDA-MB-231 cells incubated for 72 hrs by MTT assay
Cytotoxicity against human MDA-MB-231 cells incubated for 72 hrs by MTT assay
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[PMID: 38134746] |
PARP/EZH2-IN-2 (compound 12e) shows an optimal cytotoxicity against MDA-MB-231 cells (IC50=2.84 μM) and BT-549 cells (IC50=0.91 μM), with no toxicity on normal breast cell lines[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female BALB/c nude mice (5 weeks after birth, MDA-MB-231 cells subcutaneous injection)[1]
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Dosage:20, 50 mg/kg
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Administration:Intraperitoneally for 21 consecutive days
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Result:Significantly suppressed tumor growth and downregulated the expression of the PARP1/EZH2 protein in tumor tissues at a dose of 50 mg/kg.
Chemical Information
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CAS No. 3026744-15-7
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분자량 573.64
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화학식 C33H31N7O3
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SMILES
CC1=CC(C)=C(C(N1)=O)CNC(C2=CC(C3=CC=C(C4=NC5=C(C(N)=O)C=CC=C5N4)C=C3)=CC6=C2C=NN6C(C)C)=O
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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)
PARP/EZH2-IN-2 Related Classifications
HY-161083 Related Classifications
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