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Cat. No.: HY-157137

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PARP1-IN-17

PARP1-IN-17 is a PARP-1 inhibitor (IC₅₀ = 19.24 nM for PARP-1 and = 32.58 nM for PARP-2) and induce apoptosis. PARP1-IN-17 shows excellent anti-proliferative activity.

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

Formula: C₂₄H₂₇FN₄O
Molecular Weight:406.50

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (276 KB)

PARP1-IN-17 Chemical Structure

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Bioz

Biological Activity

Description

PARP1-IN-17 is a PARP-1 inhibitor (IC₅₀ = 19.24 nM for PARP-1 and = 32.58 nM for PARP-2) and induce apoptosis. PARP1-IN-17 shows excellent anti-proliferative activity^[1].

IC₅₀ & Target

PARP-1

Caspase 3

All PARP Isoforms :

All Caspase Isoforms :

In Vitro

PARP1-IN-17 (Compound 11b) (72 h) exhibits anti-proliferative effects in A549 cells, OVCAR-3 cells, HCT-116 cells and MCF-7 cells ^[1].
PARP1-IN-17 (1-4 μM, 48 h) can reduce the biosynthesis of PAR induce apoptosis in A549 cells^[1].

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

Cell Proliferation Assay^[1]

Cell Line:

A549 cells, OVCAR-3 cells, HCT-116 cells, MCF-7 cells
Concentration:
Incubation Time:

72 h
Result:

Had excellent anti-proliferative activity against A549 cell, OVCAR-3 cells, HCT-116 cells and MCF-7 cells (IC₅₀=1.95 ± 0.33 µM, 4.02 ± 0.24 µM, 7.45 ± 1.98 µM and 9.21 ± 2.54 µM).

Apoptosis Analysis^[1]

Cell Line:

A549 cells
Concentration:

1 μM, 2 μM, 4 μM
Incubation Time:

48 h
Result:

Induced apoptosis in cancer cells and increased the apoptosis rates of A549 cells in a dose-dependent manner.

Western Blot Analysis^[1]

Cell Line:

A549 cells, OVCAR-3 cells, HCT-116 cells, MCF-7 cells
Concentration:

1 μM, 2 μM, 4 μM
Incubation Time:
Result:

Reduced the biosynthesis of PAR, and had the best effect at 4.0 µM.
Decreased the expression of Caspase 3.

Chemical Information

Molecular Weight 406.50
Formula C₂₄H₂₇FN₄O
SMILES

OC1C2=CC=CC=C2C3(CCCCC3)N(CC4=CN(C5=CC=CC=C5F)N=N4)CC1
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Yu L, et al. Discovery of novel 2, 3, 4, 5-tetrahydrospiro [benzo [c] azepine-1, 1’-cyclohexan]-5-ol derivatives as PARP-1 inhibitors [J]. BMC chemistry, 2023, 17(1): 147. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Purity & Documentation
References

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PARP1-IN-17

All PARP Isoforms

All Caspase Isoforms