UNC0642-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEUNC0642Cat. No.: HY-13980CAS No.: 1481677-78-4分式: CHFNO分量: 546.7作靶點(diǎn): Sigma Receptor; Histone Methyltransferase作通路: GPCR/G Protein; Neuronal Signaling; Epigenetics儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 m

2、onth溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 295 mg/mL (539.60 mM; Need ultrasonic and warming)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 1.8292 mL 9.1458 mL 18.2916 mL5 mM 0.3658 mL 1.8292 mL 3.6583 mL10 mM 0.1829 mL 0.9146 mL 1.8292 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(shí)驗(yàn) 請根據(jù)您的實(shí)驗(yàn)動物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前請先配制?/p>

3、的儲備液，再依次添加助溶劑(為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；以下溶劑前的百分指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (4.57 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (4.57 mM); Clear solution3. 請依序添加每種溶

4、劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (4.57 mM); Clear solution1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 UNC0642有效，選擇性的 G9a/GLP 抑制劑， IC50值于2.5 nM。IC50 & Target IC50: less than 2.5 nM (G9a, GLP) 1體外研究 UNC0642 displays high in vitro and cellular potency, low cell

5、toxicity, and excellent selectivity. UNC0642 iscompetitive with the peptide substrate and non-competitive with the cofactor SAM. The Ki of UNC0642 isdetermined to be 3.71 nM. UNC0642 displays high in vitro potency for GLP (IC50 1.體內(nèi)研究 A single intraperitoneal (IP) injection (5 mg/kg) of UNC0642resul

6、ts in a plasma Cmax (maximumconcentration) of 947 ng/mL and an AUC (area under the curve) of 1265 hr*ng/mL 1.PROTOCOLCell Assay 1 MDA-MB-231, PC3, and U2OS cells are treated with inhibitors (UNC0642) for 48 h. Cell viability assays areperformed by incubating cells with 0.1 mg/mL of resazurin for 3 4

7、 h. Resazurin reduction is monitored with544 nm excitation, measuring fluorescence at 590 nm. In-cell western assay is performed as describedpreviously 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice: Standard PK studies are performed usin

8、g male Swiss albino mice. Plasma and brain concentrationsAdministration 1 are measured at 0.08, 0.25, 0.5, 1, 2, 4, 8, and 24 h following a single IP injection of UNC0642 at 5 mg/kg.The compound concentration at each time point in plasma or brain is the average value from 3 test animals1.MCE has not

9、 independently confirmed the accuracy of these methods. They are for reference only. Proc Natl Acad Sci U S A. 2019 Feb 19;116(8):2961-2966. Cell Death Dis. 2018 Jan 26;9(2):129. Acta Pharmacol Sin. 2019 Aug;40(8):1076-1084. Hum Pathol. 2018 Feb;72:117-126.See more customer validations on HYPERLINK

10、/ www.MedChemEREFERENCES1. Liu F, et al. Discovery of an in vivo chemical probe of the lysine methyltransferases G9a and GLP. J Med Chem. 2013 Nov14;56(21):8931-8942.2. Wang L, et al. Targeting EHMT2 reverses EGFR-TKI resistance in NSCLC by epigenetically regulating the PTEN/AKT signalingpathway. Cell Death Dis. 2018 Jan 26;9(2):1292/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEMcePdfHeightCaution: Product has not been fully