3-Aminobenzamide-PARP-IN-1-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemE3-AminobenzamideCat. No.: HY-12022CAS No.: 3544-24-9Synonyms: PARP-IN-1分式: CHNO分量: 136.15作靶点: PARP作通路: Cell Cycle/DNA Damage; Epigenetics储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 H2O : 11.11

2、 mg/mL (81.60 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 7.3448 mL 36.7242 mL 73.4484 mL5 mM 1.4690 mL 7.3448 mL 14.6897 mL10 mM 0.7345 mL 3.6724 mL 7.3448 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 3-Aminobenzamide种有效的 PAR

3、P 抑制剂，在 CHO 细胞中，对 PARP 的 IC50 值约为 50 nM。IC50 & Target PARP50 nM (IC50)1/3 Master of Small Molecules 您边的抑制剂师www.MedChemE体外研究 3-Aminobenzamide (1 M) causes more than 95% inhibition of PARP activity without significant cellulartoxicity. INO-1001 significantly sensitizes CHO cells by blocking most of th

4、e DNA repair occurring betweenradiation fractions 1. 3-Aminobenzamide significantly improves endothelial function by enhancing theacetylcholine-induced, endothelium-dependent, nitric oxide mediated vasorelaxation after exposure with 400M H2O2 2.体内研究 In a db/db (Leprdb/db) mouse model, 3-Aminobenzami

5、de ameliorates diabetes-induced albumin excretionand mesangial expansion, and also decreases diabetes-induced podocyte depletion 3. 3-Aminobenzamide(1.6 mg/kg via intracerebral injection) prevents NAD+ depletion and improves water maze performance aftercontrolled cortical impact (CCI) in mice 4.PROT

6、OCOLKinase Assay 1 PARP activity is measured with a PARP Activity Assay Kit. This method measures relative PARP activity bydetermining the level of incorporation of 3H-NAD into trichloroacetic acid (TCA) precipitable material in thepresence of sheared genomic DNA, which activates PARP. The reaction

7、mixture is added directly to washedcultures in 12-well culture plates and the reaction is allowed to proceed for 60 minutes at 37C before thecells are removed mechanically, transferred to a microcentrifuge tube, and precipitated with ice-cold 5%TCA.MCE has not independently confirmed the accuracy of

8、 these methods. They are for reference only.Animal Male db/db (Leprdb/db) mice, together with nondiabetic control db/m mice on C57BLKs/J background, areAdministration 3 used. INO-1001 and PJ-34 treatment are initiated at 5 weeks of age. In sterile water that is sweetened withNutraSweet, 4.8 g/L 3-Am

9、inobenzamide and 2.4 g/L PJ-34 is dissolved. Control animals receive sweetenedwater only. The average inhibitor consumption is 60 mg/kg 3-Aminobenzamide and 30 mg/kg PJ-34.MCE has not independently confirmed the accuracy of these methods. They are for reference only.户使本产品发表的科研献 J Mol Med (Berl). 201

10、9 Jun 14. Biochim Biophys Acta. 2016 Dec;1863(12):3027-3039. Acta Pharmacol Sin. 2019 May;40(5):589-598. Mol Cell Endocrinol. 2018 Oct 15;474:137-150. J Cell Biochem. 2019 Apr;120(4):4813-4826.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Brock WA, et al. Radiosensitization o

11、f human and rodent cell lines by INO-1001, a novel inhibitor of poly(ADP-ribose) polymerase.Cancer Lett. 2004 Mar 18;205(2):155-60.2. Radovits T, et al. Poly(ADP-ribose) polymerase inhibition improves endothelial dysfunction induced by reactive oxidant hydrogenperoxide in vitro. Eur J Pharmacol. 200

12、7 Jun 14;564(1-3):158-66.2/3 Master of Small Molecules 您边的抑制剂师www.MedChemE3. Szabo C, et al. Poly(ADP-ribose) polymerase inhibitors ameliorate nephropathy of type 2 diabetic Leprdb/db mice. Diabetes. 2006Nov;55(11):3004-12.4. Clark RS, et al. Local administration of the poly(ADP-ribose) polymerase inhibitor INO-1001 prevents NAD+ depletion and improveswater maze performance after traumatic brain injury in mice. J Neurotrauma. 2007 Aug;24(8):1399-405.McePdfHeightCa