GSK2606414 - PERK 抑制劑 - 生命科學(xué)試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEGSK2606414Cat. No.: HY-18072CAS No.: 1337531-36-8分式: CHFNO分量: 451.44作靶點: PERK; Autophagy作通路: Cell Cycle/DNA Damage; Autophagy儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 31 mg/mL (68.67

2、mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.2151 mL 11.0757 mL 22.1513 mL5 mM 0.4430 mL 2.2151 mL 4.4303 mL10 mM 0.2215 mL 1.1076 mL 2.2151 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內(nèi)實驗 GSK2606414 is prepared in a solution with 0.5% hydroxypro

3、pyl methylcellulose and 0.1% Tween 802.BIOLOGICAL ACTIVITY物活性 GSK2606414可滲透細胞且可服的蛋激酶 R 樣內(nèi)質(zhì) (ER) 激酶 (PERK) 抑制劑，IC50值為 0.4 nM。IC50 & Target EIF2AK3 (PERK) EIF2AK1 (HRI) EIF2AK2 (PKR)0.4 nM (IC50) 420 nM (IC50) 696 nM (IC50)1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemE體外研究 GSK2606414 inhibits PERK

4、activation in cells 1.體內(nèi)研究 GSK2606414 (50 and 150 mg/kg, p.o.) inhibits the growth of a human tumor xenograft in mice 1.PROTOCOLAnimal Exponentially growing BxPC3 tumor cells (10106 cells/mouse) from cell culture are implantedAdministration 1 subcutaneously into the right flank of female nude mice.

5、Sixteen days after implantation, mice with -200 mm3tumors are randomized into various treatment groups (n=8 mice/group). Animals are orally treated withvehicle (0.5% hydoxypropylmethylcellulose, 0.1% Tween 80 in water, pH 4.8), compound at 50 or 150 mg/kg,b.i.d. for 21 days. Tumor volume is measured

6、 twice weekly with calipers and calculated. Results arerepresented as percent inhibition on completion of dosing, which is 1001-(average growth of drug-treatedpopulation)/(average growth of vehicle-treated control population). Statistical analysis is performed using atwo-tailed t test.MCE has not in

7、dependently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻 Cell Host Microbe. 2017 Dec 13;22(6):766-776.e4. Dev Cell. 2019 Apr 8;49(1):145-155.e4. Antimicrob Agents Chemother. 2018 Oct 24;62(11). pii: e01442-18. J Virol. 2019 Jun 12. pii: JVI.00887-19. Food Chem Tox

8、icol. 2017 Oct 27;111:19-26.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Axten JM, et al. Discovery of 7-methyl-5-(1-3-(trifluoromethyl)phenylacetyl-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo2,3-dpyrimidin-4-amine (GSK2606414), a potent and selective first-in-class inhibitor of protein kinase R (PKR)-like endoplasmic reticulu2. Zhang M, et al. Inhibiting the Plasmodium eIF2 Kinase PK4 Prevents Artemisinin-Induced Latency. Cell Host Microbe. 2017 Dec13;22(6):766-776.e4.McePdfHeightCaution: Product has not been fully validated for medical ap