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

For research use only. We do not sell to patients.

PARP/EZH2-IN-2 Chemical Structure

PARP/EZH2-IN-2 Chemical Structure

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PARP/EZH2-IN-2 Related Antibodies

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Description

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[1].

IC50 & Target

PARP1

6.89 ± 0.7 nM (IC50)

EZH2

27.34 ± 1. nM (IC50)

In Vitro

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.

PARP/EZH2-IN-2 Related Antibodies
In Vivo

PARP/EZH2-IN-2 (compound 12e) (20-50 mg/kg, IP) exhibits good antitumor activity, more effective than Niraparib (HY-10619) plus GSK126 (HY-13470)[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female BALB/c nude mice (5 weeks after birth, MDA-MB-231 cells subcutaneous injection)[1]
Dosage: 20, 50 mg/kg
Administration: Intraperitoneally for 21 consecutive days
Result: Significantly suppressed tumor growth and downregulated the expression of the PARP1/EZH2 protein in tumor tissues at a dose of 50 mg/kg.
Molecular Weight

573.64

Formula

C33H31N7O3
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
Shipping

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-2 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-2PARPHistone Methyltransferasepoly ADP ribose polymeraseTriple-negative breast cancerMDA-MB-231 cellsBT-549 cellsInhibitorinhibitorinhibit

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