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AG14361

Catalog No. T6339 CAS 328543-09-5

Synonyms: AG-14361, AG 14361

AG14361 is an effective inhibitor of PARP1 (Ki<5 nM).

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

AG14361, CAS 328543-09-5

Pack Size	Availability	Price/USD
1 mg	In stock	$ 47.00
2 mg	In stock	$ 65.00
5 mg	In stock	$ 142.00
10 mg	In stock	$ 259.00
25 mg	In stock	$ 503.00
50 mg	In stock	$ 733.00
100 mg	In stock	$ 987.00
1 mL * 10 mM (in DMSO)	In stock	$ 142.00

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Purity: 99.73%

Purity: 98.77%

Purity: 98.68%

Purity: 97.65%

Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	AG14361 is an effective inhibitor of PARP1 (Ki<5 nM).
Targets&IC50	PARP1:<5 nM(Ki)
Kinase Assay	PARP-1 Activity Assays: The activity of full-length recombinant human PARP-1 is measured in a reaction mixture containing 20 nM PARP-1, 500 μM NAD+ plus [32P]NAD+ (0.1–0.3 μCi per reaction mixture), and activated calf thymus DNA (10 μg/mL) at 25oC; the reaction is terminated after 4 minutes by adding ice-cold 10% (wt/vol) trichloroacetic acid. The reaction product [32P]ADP-ribose incorporated into acid-insoluble material is deposited onto Whatman GF/C glass fiber filters with a Bio-Dot microfiltration apparatus and quantified with a PhosphorImager. Inhibition of PARP-1 activity by AG14361 at 0–600 nM is measured, and the Ki for AG14361 is calculated by nonlinear regression analysis.
Cell Research	LoVo and SW620 colorectal cancer cells and A549 non–small-cell lung carcinoma cells are maintained in RPMI-1640 medium containing 10% fetal calf serum. Cell growth inhibition is estimated in exponentially growing LoVo, A549, and SW620 cells in 96-well plates. Cells are exposed to AG14361 (0–20 μM) alone or in the presence of 400 μM temozolomide. After 5 days of culture, these cells are fixed with 10% trichloroacetic acid and stained with sulforhodamine B. The concentration of temozolomide, topotecan, and AG14361 alone or in combination that inhibits growth by 50% (GI50) is calculated from computer-generated curves. Recovery from potentially lethal damage is measured in confluent LoVo cell cultures arrested in G1 phase to mimic the radiation-resistant quiescent cell population in tumors. Such cells are exposed to 8 Gy of γ-irradiation and then harvested and plated for colony formation assay immediately or maintained as growth-arrested confluent cultures for a 4-hour or 24-hour recovery period before harvesting and plating for the colony formation assay. Where indicated, 0.4 μM AG14361 is added 30 minutes before irradiation and is present in the recovery incubation. (Only for Reference)

Synonyms	AG-14361, AG 14361
Molecular Weight	320.39
Formula	C19H20N4O
CAS No.	328543-09-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 2 years

Solubility Information

DMSO: 10 mg/mL (31.2 mM)

H2O: <1 mg/mL

Ethanol: <1 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Calabrese CR, et al. J Natl Cancer Inst, 2004, 96(1), 56-67. 2. Curtin NJ, et al. Clin Cancer Res, 2004, 10(3), 881-9. 3. Smith LM, et al. Clin Cancer Res, 2005, 11(23), 8449-57.

Citations

1. Shi F, Wu L, Cui D, et al.LncFALEC recruits ART5/PARP1 and promotes castration-resistant prostate cancer through enhancing PARP1-meditated self PARylation.Cellular Oncology.2023: 1-16.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Ovarian Cancer Compound Library DNA Damage & Repair Compound Library Target-Focused Phenotypic Screening Library Epigenetics Compound Library Anti-Cardiovascular Disease Compound Library Anti-Cancer Compound Library Anti-Aging Compound Library NO PAINS Compound Library Anti-Cancer Active Compound Library Anti-Breast Cancer Compound Library

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

AG14361 328543-09-5 Chromatin/Epigenetic DNA Damage/DNA Repair PARP inhibit Inhibitor poly ADP ribose polymerase AG-14361 AG 14361 inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.