MKC8866 - IRE1α RNase 抑制剂 - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEMKC8866Cat. No.: HY-104040CAS No.: 1338934-59-0分式: CHNO分量: 361.35作靶点: IRE1作通路: Cell Cycle/DNA Damage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 DMSO : 16.67 mg/mL (46.13 mM; Need ultrasonic)Ma

2、ss Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.7674 mL 13.8370 mL 27.6740 mL5 mM 0.5535 mL 2.7674 mL 5.5348 mL10 mM 0.2767 mL 1.3837 mL 2.7674 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。体内实验 请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的

3、百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 1.67 mg/mL (4.62 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 1.67 mg/mL (4.62 mM); Clear solutionBIOLOGICAL ACTIVITY1/3 Master of Small Molecules 您边的抑制剂师www.MedChemE物活性 MKC886

4、6种杨醛类似物，有效的选择性 IRE1 RNase 抑制剂，在体外的 IC50 为 0.29 M。 MKC8866强烈抑制 DTT 诱导的 XBP1s 表达，EC50 为 0.52 M。MKC8866 抑制应激 RPMI 8226 细胞，IC50 为 0.14M。 MKC8866 抑制乳腺癌细胞中的 IRE1 RNase 导致促肿瘤发因减少，同时也能抑制前列腺癌 (PCa) 肿瘤的长。IC50 & Target IC50: 0.29M (IRE1 RNase) 1体外研究MKC8866 (20M; 6 days) decreases proliferation of all breast ca

5、ncer cell lines 2.MKC8866 (20 M; 48 hours) reduces the number of cells entering S phase 2.MKC8866 (0.2-10 M; 3 days) suppresses the viability of all four cell lines in a dose-dependent mannerunder normal conditions, with the most robust effect in LNCaP cells 1.MKC8866 (20 M; 72hours) is sufficient t

6、o completely block paclitaxel-induced expression of XBP1s 1.Cell Proliferation Assay 2Cell Line: MCF7, SKBR3, MDA-MB-231 and MCF10A cellsConcentration: 20MIncubation Time: For 6 daysResult: Decreased proliferation of all breast cancer cell lines.Cell Cycle Analysis 2Cell Line: MDA-MB-231, MCF7 and S

7、KBR3 cellsConcentration: 20MIncubation Time: 48 hoursResult: Reduced the number of cells entering S phase.Cell Cycle Analysis 1Cell Line: LNCaP, VCaP, 22Rv1 and C4-2B cellsConcentration: 0.2, 0.5, 1, 5, 10 MIncubation Time: 3 daysResult: Suppressed the viability of all four cell lines in a dose-depe

8、ndent manner.Cell Cycle Analysis 2Cell Line: MDA-MB-231 cellsConcentration: 20 M2/3 Master of Small Molecules 您边的抑制剂师www.MedChemEIncubation Time: 72 hoursResult: Completely blocked paclitaxel-induced expression of XBP1s.体内研究 MKC8866 (oral ; 300 mg/kg; for 28 days) reduces tumor regrowth post-paclita

9、xel withdrawal 1.Animal Model: Female athymic nude mice with MDA-MB-231 tumor 1Dosage: 300 mg/kgAdministration: Oral; for 28 daysResult: Reduced tumor regrowth post-paclitaxel withdrawal.户使本产品发表的科研献 Science. 2019 Jul 19;365(6450). pii: eaau6499. Sci Rep. 2019 Mar 1;9(1):3210.See more customer valida

10、tions on HYPERLINK / www.MedChemEREFERENCES1. Sheng X, et al. IRE1-XBP1s pathway promotes prostate cancer by activating c-MYC signaling. Nat Commun. 2019 Jan 24;10(1):323.2. Logue SE, et al. Inhibition of IRE1 RNase activity modulates the tumor cell secretome and enhances response to chemotherapy. NatCommun. 2018 Aug 15;9(1):3267.McePdfHeightCaution: Product has not been fully va