1. Cell Cycle/DNA Damage Epigenetics Apoptosis
  2. PARP Apoptosis Caspase
  3. PARP-1-IN-3

PARP-1-IN-3, a benzamide derivative, is a potent PARP-1 inhibitor with IC50 values of 0.25 nM and 2.34 nM for PARP-1 and PARP-2, respectively. PARP-1-IN-3 induces apoptosis and arrest cell cycle at G2/M phase. PARP-1-IN-3 can be used in research of cancer.

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

PARP-1-IN-3 Chemical Structure

PARP-1-IN-3 Chemical Structure

CAS No. : 2976342-33-1

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10 mg USD 480 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

PARP-1-IN-3, a benzamide derivative, is a potent PARP-1 inhibitor with IC50 values of 0.25 nM and 2.34 nM for PARP-1 and PARP-2, respectively. PARP-1-IN-3 induces apoptosis and arrest cell cycle at G2/M phase. PARP-1-IN-3 can be used in research of cancer[1].

IC50 & Target[1]

PARP-1

0.25 nM (IC50)

PARP-2

2.34 nM (IC50)

In Vitro

PARP-1-IN-3 (compound 13f; 48 h) has potent anticancer activity with IC50 values of 0.30, 2.83, 33.69, and 486.87 μM for HCT116, DLD-1, SW480, and NCM460 cells, respectively[1].
PARP-1-IN-3 (0.3-3 μM; 24-48 h) inhibits colony formation and migration of HCT116 cells[1].
PARP-1-IN-3 (0.3-3 μM; 48 h) induces accumulation of DNA double-strand breaks in HCT116 cells[1].
PARP-1-IN-3 (0.3-7.5 μM; 48-72 h) arrests cell cycle at G2/M phase, reduces mitochondrial membrane potential and ultimately induce apoptosis in HCT116 cells[1].

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

Apoptosis Analysis[1]

Cell Line: HCT116 cells
Concentration: 0.3, 1.5, 7.5 μM
Incubation Time: 48 and 72 h
Result: Increased the percentage of total apoptotic cells from 1.05% (control group) to 79.49% (7.5 μM).

Cell Cycle Analysis[1]

Cell Line: HCT116 cells
Concentration: 0.3, 1.5, 7.5 μM
Incubation Time: 48 and 72 h
Result: Blocked the cell cycle progression at G2/M phase.

Western Blot Analysis[1]

Cell Line: HCT116 cells
Concentration: 0.3, 1, 3 μM
Incubation Time: 48 h
Result: Increased expression levels of γH2AX in a concentration-dependent manner.

Western Blot Analysis[1]

Cell Line: HCT116 cells
Concentration: 0.3, 1, 3 μM
Incubation Time: 48 h
Result: Increased the expression levels of Bax, cleaved Caspase-3 and cleaved-PARP, and decreased the expression level of Bcl-2.
Molecular Weight

425.28

Formula

C21H17BrN2O3

CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

NC(C1=CC=CC=C1OCC2=CC=CC(NC(C3=CC=C(C=C3)Br)=O)=C2)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (293.92 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3514 mL 11.7570 mL 23.5139 mL
5 mM 0.4703 mL 2.3514 mL 4.7028 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3514 mL 11.7570 mL 23.5139 mL 58.7848 mL
5 mM 0.4703 mL 2.3514 mL 4.7028 mL 11.7570 mL
10 mM 0.2351 mL 1.1757 mL 2.3514 mL 5.8785 mL
15 mM 0.1568 mL 0.7838 mL 1.5676 mL 3.9190 mL
20 mM 0.1176 mL 0.5878 mL 1.1757 mL 2.9392 mL
25 mM 0.0941 mL 0.4703 mL 0.9406 mL 2.3514 mL
30 mM 0.0784 mL 0.3919 mL 0.7838 mL 1.9595 mL
40 mM 0.0588 mL 0.2939 mL 0.5878 mL 1.4696 mL
50 mM 0.0470 mL 0.2351 mL 0.4703 mL 1.1757 mL
60 mM 0.0392 mL 0.1959 mL 0.3919 mL 0.9797 mL
80 mM 0.0294 mL 0.1470 mL 0.2939 mL 0.7348 mL
100 mM 0.0235 mL 0.1176 mL 0.2351 mL 0.5878 mL
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PARP-1-IN-3 Related Classifications

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.

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PARP-1-IN-3
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