1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEHLCL-61 hydrochlorideCat. No.: HY-100025ACAS No.: 1158279-20-9分式: CHClNO分量: 380.91作靶點(diǎn): Histone Methyltransferase作通路: Epigenetics儲(chǔ)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(shí)驗(yàn) DMSO : 50 mg/mL (131

2、.26 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 2.6253 mL 13.1265 mL 26.2529 mL5 mM 0.5251 mL 2.6253 mL 5.2506 mL10 mM 0.2625 mL 1.3126 mL 2.6253 mL請(qǐng)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(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。體內(nèi)實(shí)驗(yàn) 請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍福渲魄罢?qǐng)先配制澄清的儲(chǔ)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；

3、澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)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(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (6.56 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (6.56 mM); Clear solution3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/

4、mL (6.56 mM); Clear solution1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 HLCL-61 hydrochloride流的分蛋精氨酸甲基轉(zhuǎn)移酶 5 (PRMT5) 抑制劑。IC50 & Target Protein arginine methyltransferase 5 1體外研究 HLCL-61 hydrochloride (1-100 M; 24-72 hours) reduces cells growth at dose-dependent manner with

5、 IC50sof 14.12, 16.74, 6.3, 8.72 M for MV4-11 cells, THP-1 cells, FLT3-WT blast, and FLT3-ITD blast, respectively1.HLCL-61 hydrochloride shows effective inhibition of symmetric arginine dimethylation (me2) of histones H3and H4 in AML samples, starting at 12h post-treatment and persisting after 48h 1

6、.Cell Viability Assay 1Cell Line: MV4-11 cells, THP-1 cells, FLT3-WT blast (primary blasts from patients), FLT3-ITD blast(primary blasts from patients)Concentration: 1, 5, 10, 25, 50, 100 MIncubation Time: 24, 48, 72 hoursResult: Dose-dependent reduction in cell viability with IC50s of 14.12, 16.74,

7、 6.3, 8.72 M forMV4-11 cells, THP-1 cells, FLT3-WT blast, and FLT3-ITD blast, respectively.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) Proc Natl Acad Sci U S A. 2019 Feb 19;116(8):2961-2966.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Tarighat SS, et al. The dual epigenetic role of PRMT5 in acute myeloid leukemia: gene activation and repression via histone argininemethylation. Leukemia. 2016 Apr;30(4):789-99.McePdfHeightCaution: Product has not been fully validated for medical applications.For resea