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

PARP-1-IN-2 (compound 11g) is a potent and BBB-penetrated PARP1 inhibitor, with an IC50 of 149 nM. PARP1-IN-2 shows significantly potent anti-proliferative activity against Human lung adenocarcinoma epithelial cell line A549. PARP1-IN-2 can induce A549 cells apoptosis.

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

PARP-1-IN-2 Chemical Structure

PARP-1-IN-2 Chemical Structure

CAS No. : 684234-55-7

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10 mg USD 480 In-stock
25 mg USD 950 In-stock
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Based on 1 publication(s) in Google Scholar

PARP-1-IN-2 Related Antibodies

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Description

PARP-1-IN-2 (compound 11g) is a potent and BBB-penetrated PARP1 inhibitor, with an IC50 of 149 nM. PARP1-IN-2 shows significantly potent anti-proliferative activity against Human lung adenocarcinoma epithelial cell line A549. PARP1-IN-2 can induce A549 cells apoptosis[1].

IC50 & Target

PARP-1

149 ± 11.0 nM (IC50)

Caspase-3

 

Caspase-9

 

In Vitro

PARP-1-IN-2 (compound 11g) (0-10 μM, 24-48 h) shows significantly potent anti-proliferative activity against A549 cells[1].
PARP-1-IN-2 (0-10 μM, 24 h) decreases the expression of pro-caspase-3 and phosphorylated AKT, increases the expression of caspase-3, caspase-9 protein and the cleaved PARP-1[1].

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

PARP-1-IN-2 Related Antibodies

Cell Proliferation Assay

Cell Line: A549, HFF cells[1]
Concentration: 0, 0.1, 1, 10 μM
Incubation Time: 24, 48 h
Result: Showed significantly potent anti-proliferative activity against A549 cells, and didn’t display any significant cytotoxicity on HFF cells.

Western Blot Analysis

Cell Line: A549 cells[1]
Concentration: 0, 0.1, 1, 10 μM
Incubation Time: 24 h
Result: Reduced expression of pro-caspase-3 and phosphorylated AKT, significantly increased the expression of caspase-3 and caspase-9 protein, and enhanced expression of the cleaved PARP-1.
Molecular Weight

424.28

Formula

C22H15Cl2N3O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NC1=CC=CC(Cl)=C1)CN(N=C(C2=CC=C(Cl)C=C2)C3=C4C=CC=C3)C4=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 83.33 mg/mL (196.40 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 2.3569 mL 11.7847 mL 23.5693 mL
5 mM 0.4714 mL 2.3569 mL 4.7139 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.08 mg/mL (4.90 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.08 mg/mL (4.90 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
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 (protect from light). 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 2.3569 mL 11.7847 mL 23.5693 mL 58.9234 mL
5 mM 0.4714 mL 2.3569 mL 4.7139 mL 11.7847 mL
10 mM 0.2357 mL 1.1785 mL 2.3569 mL 5.8923 mL
15 mM 0.1571 mL 0.7856 mL 1.5713 mL 3.9282 mL
20 mM 0.1178 mL 0.5892 mL 1.1785 mL 2.9462 mL
25 mM 0.0943 mL 0.4714 mL 0.9428 mL 2.3569 mL
30 mM 0.0786 mL 0.3928 mL 0.7856 mL 1.9641 mL
40 mM 0.0589 mL 0.2946 mL 0.5892 mL 1.4731 mL
50 mM 0.0471 mL 0.2357 mL 0.4714 mL 1.1785 mL
60 mM 0.0393 mL 0.1964 mL 0.3928 mL 0.9821 mL
80 mM 0.0295 mL 0.1473 mL 0.2946 mL 0.7365 mL
100 mM 0.0236 mL 0.1178 mL 0.2357 mL 0.5892 mL
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PARP-1-IN-2 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.

Keywords:

PARP-1-IN-2684234-55-7PARPCaspaseApoptosispoly ADP ribose polymerase HFF cellsA549 cellsphthalazinoneLung adenocarcinomaBBB-penetratedInhibitorinhibitorinhibit

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