1. Cell Cycle/DNA Damage Epigenetics
  2. PARP
  3. PARP1-IN-5 dihydrochloride

PARP1-IN-5 dihydrochloride is a low toxicity, orally active, potent and selective PARP-1 inhibitor (IC50 =14.7 nM). PARP1-IN-5 dihydrochloride can be used for the research of cancer.

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

PARP1-IN-5 dihydrochloride Chemical Structure

PARP1-IN-5 dihydrochloride Chemical Structure

CAS No. : 2823308-89-8

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of PARP1-IN-5 dihydrochloride:

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1 Publications Citing Use of MCE PARP1-IN-5 dihydrochloride

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

PARP1-IN-5 dihydrochloride is a low toxicity, orally active, potent and selective PARP-1 inhibitor (IC50 =14.7 nM). PARP1-IN-5 dihydrochloride can be used for the research of cancer[1].

IC50 & Target[1]

PARP-1

14.7 nM (IC50)

PARP-2

0.9 μM (IC50)

In Vitro

PARP1-IN-5 dihydrochloride (0.1~10 μM; A549 cells) can significantly increase the cytotoxicity of CBP on A549 cells in a dose-dependent manner. PARP1-IN-5 dihydrochloride (0.1~10 μM; SK-OV-3 cells) decreases the expressions of MCM2-7. PARP1-IN-5 dihydrochloride (0.1~320 μM; A549 cells) has little cytotoxic effects on A549 cells. PARP1-IN-5 dihydrochloride (SK-OV-3 cells) can significantly decrease the PAR level[1].
PARP1-IN-5 dihydrochloride exerts antitumor effects through PARP-1. PARP1-IN-5 dihydrochloride could increase the γ-H2AX expression[1].

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

In Vivo

PARP1-IN-5 dihydrochloride (1000 mg/kg; p.o.) shows that there is no significant difference in the body weight and blood routine[1].
PARP1-IN-5 dihydrochloride (25 and 50 mg/kg; p.o.; 12 days) significantly enhances the inhibitory effect of carboplatin on A549 cells at 50 mg/kg[1].
PARP1-IN-5 dihydrochloride (50 mg/kg; p.o.) positively correlates with the expression of PARP-1[1].
PARP1-IN-5 dihydrochloride can upregulate the expression of γ-H2AX and decrease the expression of PAR[1].

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

Animal Model: Mice[1]
Dosage: 1000 mg/kg
Administration: P.o.
Result: There was no significant difference in the body weight and blood routine.
Animal Model: Mice[1]
Dosage: 25 and 50 mg/kg
Administration: P.o.; 12 days
Result: Significantly enhanced the inhibitory effect of CBP on A549 cells at 50 mg/kg.
Animal Model: Male Sprague−Dawley (SD) rats[1]
Dosage: 50 mg/kg (Pharmacokinetic Analysis)
Administration: P.o.
Result: Positively correlated with the expression of PARP-1.
Molecular Weight

537.46

Formula

C25H26Cl2N2O5S

CAS No.
Appearance

Solid

Color

Light yellow to green yellow

SMILES

O=C1C=C(OC2=C1C(O)=CC(O)=C2CN3CCN(CC3)CC4=CC=CS4)C5=CC=C(C=C5)O.[H]Cl.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (232.58 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 1 mg/mL (1.86 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8606 mL 9.3030 mL 18.6060 mL
5 mM 0.3721 mL 1.8606 mL 3.7212 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • 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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (3.87 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

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

    Solubility: ≥ 2.08 mg/mL (3.87 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    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.
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 (sealed storage, away from moisture)

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 (sealed storage, away from moisture). 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
H2O / DMSO 1 mM 1.8606 mL 9.3030 mL 18.6060 mL 46.5151 mL
DMSO 5 mM 0.3721 mL 1.8606 mL 3.7212 mL 9.3030 mL
10 mM 0.1861 mL 0.9303 mL 1.8606 mL 4.6515 mL
15 mM 0.1240 mL 0.6202 mL 1.2404 mL 3.1010 mL
20 mM 0.0930 mL 0.4652 mL 0.9303 mL 2.3258 mL
25 mM 0.0744 mL 0.3721 mL 0.7442 mL 1.8606 mL
30 mM 0.0620 mL 0.3101 mL 0.6202 mL 1.5505 mL
40 mM 0.0465 mL 0.2326 mL 0.4652 mL 1.1629 mL
50 mM 0.0372 mL 0.1861 mL 0.3721 mL 0.9303 mL
60 mM 0.0310 mL 0.1551 mL 0.3101 mL 0.7753 mL
80 mM 0.0233 mL 0.1163 mL 0.2326 mL 0.5814 mL
100 mM 0.0186 mL 0.0930 mL 0.1861 mL 0.4652 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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PARP1-IN-5 dihydrochloride 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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PARP1-IN-5 dihydrochloride
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