INO-1001 is a novel poly(ADP-ribose) polymerase (PARP) inhibitor improves cardiac and pulmonary function after crystalloid cardioplegia and extracorporal circulation. The present study tested INO-1001 for its in vivo effect on the chemoresponse of two p53 deficient tumors, human breast cancer MDA-MB-231 and murine mammary carcinoma MCa-K. Doxorubicin was used as the DNA damaging agent and tumor growth delay assay was used as the endpoint. Results showed that INO-1001 was highly effective in enhancing the anti-tumor effects of Doxorubicin for both MDA-MB-231 (EF=1.88) and MCa-K (EF=1.64).
Bioact Mater. 2022 Feb 9.
pH and lipase-responsive nanocarrier-mediated dual drug delivery system to treat periodontitis in diabetic rats
INO-1001 purchased from AbMole
Cell Commun Signal. 2020 Feb 17;18(1):27.
mTOR May Interact With PARP-1 to Regulate Visible Light-Induced Parthanatos in Photoreceptors
INO-1001 purchased from AbMole
|Source||Exp Gerontol (2007). Figure 2. INO-1001|
|Cell Lines||male Lewis rats|
|Incubation Time||2 h|
|Results||Single dose treatment with the potent PARP-inhibitor INO-1001 notably decreased PAR formation both in the myocardium and the aortic wall.|
|Cell lines||cultured podocytes|
|Preparation method||Apoptosis detection. Apoptotic nuclei of cultured podocytes were detected on paraformaldehyde-fixed cells using DAPI (4′,6-diamidino-2-phenylindole) staining (1 μg/ml) for 10 min. Cells were analyzed under a fluorescence microscope and assessed for chromatin condensation and segregation. Caspase-3 activity was measured in podocyte extracts using EnzCheck Caspase-3 Assay kit (Molecular Probes) following the manufacturer’s protocol. Nuclear extracts were prepared using Transfactor DB Nuclear extraction kit (Clontech BD Bioscience) following the manufacturer’s protocol. Western blotting was performed using NFκB p50 (Santa Cruz Biotechnology) antibody. NFκB p50 nuclear binding assay was performed using TransFactor Colorimetric kit (Clontech BD) according to the manufacturer’s protocol.|
|Incubation time||45 min|
|Animal models||diabetic nephropathy of Leprdb/db mice model|
|Dosages||60 mg/kg initiated at 5 weeks of age to around 8 weeks of age|
|Administration||oral in drinking water|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
|Solubility||DMSO 22 mg/mL
Water ≥ 4 mg/mL
 Morrow DA, et al. J Thromb Thrombolysis. A randomized, placebo-controlled trial to evaluate the tolerability, safety, pharmacokinetics, and pharmacodynamics of a potent inhibitor of poly(ADP-ribose) polymerase (INO-1001) in patients with ST-elevation myocardial infarction undergoing primary percutaneous coronary intervention: results of the TIMI 37 trial.
 Robert S B Clark, et al. J Neurotrauma. Local administration of the poly(ADP-ribose) polymerase inhibitor INO-1001 prevents NAD+ depletion and improves water maze performance after traumatic brain injury in mice
|Related PARP Products|
Amelparib is a potent, water soluble PARP-1 inhibitor with oral activity.
Veliparib (dihydrochloride) is a potent inhibitor of PARP1 and PARP2 with Kis of 5.2 nM and 2.9 nM in cell-free assays, respectively.
Talazoparib tosylate (BMN 673ts) is a novel, potent and orally available PARP1/2 inhibitor with an IC50 of 0.57 nM for PARP1.
RK-287107 is a potent and specific tankyrase inhibitor with IC50s of 14.3 and 10.6 nM for tankyrase-1 and tankyrase-2, respectively. RK-287107 blocks colorectal cancer cell growth.
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.
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