Harmine-Telepathine-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEHarmineCat. No.: HY-N0737ACAS No.: 442-51-3Synonyms: Telepathine分式: CHNO分量: 212.25作靶點(diǎn): 5-HT Receptor; RAD51; DYRK作通路: GPCR/G Protein; Neuronal Signaling; Cell Cycle/DNADamage; Protein Tyrosine Kinase/RTK儲(chǔ)存式: Powder -20C 3 years4

2、C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 30 mg/mL (141.34 mM)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (11.78 mM); Clear solution1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (11.78 mM); Clear solutio

3、nBIOLOGICAL ACTIVITY物活性 Harmine種具有抗癌和抗炎活性的天然雙特異性酪氨酸磷酸化調(diào)節(jié)激酶 (DYRK) 抑制劑。IC50 & Target 5-HT2A Receptor DYRK1A RAD51397 nM (Ki)體外研究 Harmine is an inhibitor of 5-HT2A, with an Ki of 397 nM 1. Harmine inhibits tau phosphorylation by DYRK1Aby selected DANDYs, with an IC50 of 190 nM 2.Harmine negatively reg

4、ulates HR by interfering Rad51recruitment, resulting in severe cytotoxicity in hepatoma cells. Furthermore, NHEJ inhibitor Nu7441 markedlysensitizes Hep3B cells to the anti-proliferative effects of Harmine 3.體內(nèi)研究 It is shown that brain water content is significantly increased in the TBI group. Treat

5、ment with Harminesignificantly reduces the tissue water content at 1, 3 and 5 days, compared with the TBI group. Harminetreatment significantly reduces the escape latency at 3 and 5 days, compared with the TBI group. Post-TBIadministration of Harmine significantly improves the motor function recover

6、y of the rats at 1, 3 and 5 daysfollowing TBI, compared with the TBI group without Harmine treatment. The neuronal survival rate in theHarmine-treated group is significantly increased, compared with the TBI group. Administration of Harmineresults in marked elevation in the expression of GLT-1, compa

7、red with the TBI group. The administration ofHarmine significantly reduces the expression of caspase 3, compared with the TBI group 4.PROTOCOLAnimal Rats 4Administration 4 A total of 150 male Sprague-Dawley rats (age, 10-12 weeks; weighing, 280-320 g; are used in the presentstudy. The rats are rando

8、mly divided into three groups: Sham-operated group (sham; n=15); the TBI group(TBI; n=35) and the TBI + Harmine-treated group (Harmine; n=35). Harmine is administered immediatelyfollowing TBI (i.p, 30 mg/kg per day) for up to 5 days. The sham and TBI groups receive equal volumes of0.9% saline soluti

9、on (i.p.). The rats are grouped as follows for examination of behavioral recovery: Sham,n=3; TBI, n=7; and Harmine, n=7. Following TBI, the NSS is evaluated at 1, 3 and 5 days. Each rat isassessed by an observer who is blinded to the animal treatment 4.MCE has not independently confirmed the accurac

10、y of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) Sci Rep. 2015 Aug 3;5:12728. Onco Targets Ther. 2019 Jun 12;12:4585-4593. Prog Neuropsychopharmacol Biol Psychiatry. 2017 Jun 15;79(Pt B):258-267.2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemESee more customer validations on HYPERLINK /

11、www.MedChemEREFERENCES1. Glennon RA, et al. Binding of beta-carbolines and related agents at serotonin (5-HT(2) and 5-HT(1A), dopamine (D(2) andbenzodiazepine receptors. Drug Alcohol Depend. 2000 Aug 1;60(2):121-32.2. Neumann F, et al. DYRK1A inhibition and cognitive rescue in a Down syndrome mouse

12、model are induced by new fluoro-DANDYderivatives. Sci Rep. 2018 Feb 12;8(1):2859.3. Zhang L, et al. Harmine suppresses homologous recombination repair and inhibits proliferation of hepatoma cells. Cancer Biol Ther.2015;16(11):1585-92.4. Zhong Z, et al. Treatment with harmine ameliorates functional impairment and neuronal death following traumatic brain injury. Mol MedRep. 2015 Dec;12(6):7985-91.McePdfHeightCauti