2. Cell Cycle/DNA Damage Epigenetics
  3. PARP Histone Methyltransferase
  4. 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.

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PARP/EZH2-IN-1

PARP/EZH2-IN-1 Chemical Structure

CAS No. : 2687273-52-3

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PARP/EZH2-IN-1 Related Antibodies

Top Publications Citing Use of Products

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PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

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EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D ASH1L/KMT2H SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 NSD3/WHSC1L1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

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Description

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[1].

IC50 & Target[1]

PARP-1

6.87 nM (IC50)

EZH2

36.51 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
MCF-10A IC50
> 50 μM
Compound: 5a
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
[PMID: 34455779]
MCF7 IC50
12.11 μM
Compound: 5a
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
[PMID: 34455779]
MDA-MB-231 IC50
2.63 μM
Compound: 5a
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
[PMID: 34455779]
MDA-MB-468 IC50
0.41 μM
Compound: 5a
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
[PMID: 34455779]
In Vitro

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.

PARP/EZH2-IN-1 Related Antibodies

Cell Viability Assay[1]

Cell Line: MDA-MB-231, MDA-MB-468, MCF-7, MCF-10A cells
Concentration: various concentrations
Incubation Time: 72 h
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).

Western Blot Analysis[1]

Cell Line: MDA-MB-231 and MDA-MB-468 cells
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)
Incubation Time: 48 h
Result: Significantly down-regulated BRCA1, BRCA2, EZH2, and CARM1 protein levels.

Western Blot Analysis[1]

Cell Line: MDA-MB-231 and MDA-MB-468 cells
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)
Incubation Time: 48 h
Result: Increased Beclin-1 and LC3B-II expression and decreased p62 levels in a concentration-dependent manner.

Cell Autophagy Assay[1]

Cell Line: MDA-MB-231 cells
Concentration: 5.0 μM
Incubation Time: 12 h
Result: Induced abundant autophagic vacuoles, autophagosomes, and autophagic lysosomes.

Cell Autophagy Assay[1]

Cell Line: MDA-MB-231 and MDA-MB-468 cells
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)
Incubation Time: 48 h
Result: Increased autophagosome formation and autophagic activity in a concentration-dependent manner as shown by MDC-EB staining and LC3B immunofluorescence.
Molecular Weight

768.83

Formula

C43H41FN8O5
CAS No.
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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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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PARP/EZH2-IN-1 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PARP/EZH2-IN-12687273-52-3PARPHistone Methyltransferasepoly ADP ribose polymerasePARP-1EZH2Dual PARP/EZH2 inhibitorTriple-negative breast cancerBRCA wild-typeMDA-MB-231 cellsMDA-MB-468 cellsMCF-10A cellsAutophagyAutophagic cell deathBRCA1BRCA2CARM1Inhibitorinhibitorinhibit

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