1、ML327Cat. No.: HY-103038CAS No.: 1883510-31-3分式: CHNO分量: 366.37作靶点: c-Myc作通路: Apoptosis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 : 32 mg/mL (87.34 mM; Need ultrasonic and warming)ConcentrationSolvent Mass 1 mg 5 mg 10 mg1 mM 2.7295 mL 13.6474 mL 27.2948 mL5
2、 mM 0.5459 mL 2.7295 mL 5.4590 mL制备储备液10 mM 0.2729 mL 1.3647 mL 2.7295 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BIOLOGICAL ACTIVITY物活性 ML327 是 MYC 的阻断剂，也可以去阻遏 E-钙粘蛋转录和逆转上-间质转化 ( EMT)。IC p0.0001)1. ML327 reduces SW620inv cell invasion through Matrigel by 60% and reduces H520 cell invasion by 30% in these in vit
3、ro assays. ML327 partially restores E-cadherin expression at the plasma membrane in NMuMG cells induced to undergo Epithelial-to-Mesenchymal Transition (EMT) 体外研究Product Data Sheet InhibitorsAgonistsScreening Librarieswww.MedChemE1by TGF-1 treatment2.体内研究 ML327 treatment significantly reduces tumor
4、volume by three-fold over the two-week treatment period (p=0.02). Tumor explant weights are approximately three-fold smaller in the ML327-treated mice (p=0.01). Mice treated with ML327 lost 12% more body weight than vehicle treated mice. ML327 treatment results in a two-fold decrease in MYCN express
5、ion, confirming that ML327 inhibits xenograft MYCN expression (p=0.0035)1.PROTOCOLCell Assay 1 Cells are seeded onto 96-well plates at equivalent density (3,000 to 10,000 depending upon cell line), permitted to attach overnight, and treated with either ML327 (10 M) or vehicle. Daily absorbance measu
6、rements (450 nm) using the cell counting kit are obtained. For estimation of IC50 values, cells are plated at equal density, permitted to attach, and baseline absorbance is obtained using cell counting kit. Cells are then treated with varying doses of ML327 (0.1 to 30 M) and cell viability is measur
7、ed 72 h after treatment1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Administration 1Male athymic nude mice (4 to 6 weeks old) are maintained as described. BE(2)-C cells xenografts are established as previously described. Briefly, 1106 cells/
8、100 L of HBSS are injected subcutaneously into flanks using a 26-gauge needle (n=10 per group). Mice are monitored daily for xenograft formation and assessed by measuring the two greatest perpendicular tumor diameter with venier calipers. Xenograft volumes are estimated using the following formula (
9、lengthwidth2)/2. Once tumors reach 75 to 100 mm3, mice are randomized to receive either 50 mg/kg of ML327 or control vehicle (70% polyethylene glycol) via intraperitoneal injection twice daily for 14d. Weight and tumor volume are recorded daily. After completion of two weeks of treatment, mice are e
10、uthanized and tumors are excised, weighed, and RNA is isolated1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Rellinger EJ, et al. Isoxazole compound ML327 blocks MYC expression and tumor formation in neuroblastoma. Oncotarget. 2017 Jul 2
11、0;8(53):91040-91051.2. An H, et al. Small molecule/ML327 mediated transcriptional de-repression of E-cadherin and inhibition of epithelial-to-mesenchymal transition.Oncotarget. 2015 Sep 8;6(26):22934-48.McePdfHeightCaution: Product has not been fully validated for medical applications. For research
12、use only.Tel: 400-820-3792; 021-58955995 Fax: 021-53700325 E-mail: techMedChemEMaster of Small Molecules 您边的抑制剂师www.MedChemE2NeflamapimodCat. No.: HY-10328CAS No.: 209410-46-8分式: CHClFNOS分量: 436.26作靶点: p38 MAPK作通路: MAPK/ERK Pathway储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 mont
13、h溶解性数据体外实验 DMSO : 13.08 mg/mL (29.98 mM; Need ultrasonic)ConcentrationSolvent Mass 1 mg 5 mg 10 mg1 mM 2.2922 mL 11.4611 mL 22.9221 mL5 mM 0.4584 mL 2.2922 mL 4.5844 mL制备储备液10 mM 0.2292 mL 1.1461 mL 2.2922 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BIOLOGICAL ACTIVITY物活性 Neflamapimod (VX-745) 是有效的，有选择性的 p38 抑制剂，
14、具有抗炎活性 。体外研究 Neflamapimod (VX-745) exhibits PBMC IL-1 and TNF IC50 values of 45 and 51 nM, respectively. Neflamapimod is also effective in whole blood, blocking IL-1 and TNF release with IC50 values of 150 and 180 nM, respectively. Neflamapimod shows a promising selectivity profile, with 20-fold selectivity for p38 over p38 (Ki=220 nM)1. Neflamapimod (VX-745) solutions in DMSO/DMEM inhibits the IL-6 production with IC50 of 159 nM2. Neflamapimod (VX-745; 5.0 nM) displays potent
