Powder: -20°C for 3 years | In solvent: -80°C for 2 years
AG14361 is an effective inhibitor of PARP1 (Ki<5 nM).
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
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 |
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 |
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
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 )
You can also refer to dose conversion for different animals. More
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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.
AG14361 328543-09-5 Chromatin/Epigenetic DNA Damage/DNA Repair PARP inhibit Inhibitor poly ADP ribose polymerase AG-14361 AG 14361 inhibitor