Scoulerine

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Scoulerine 是 ? 位点淀粉样蛋白前体蛋白裂解酶 1 (BACE1) 的抑制剂。 Scoulerine 是一种有效的抗有丝分裂化合物，可抑制癌细胞增殖、阻止细胞周期并诱导癌细胞凋亡。

Scoulerine is an inhibitor of ?-site amyloid precursor protein cleaving enzyme 1(BACE1). Scoulerine a potent antimitotic compound that inhibits proliferation, arrests cell cycle, and induces apoptosis in cancer cells.(In Vitro):Scoulerine shows significant cytotoxic effects against both two cancer cell lines (Caco-2 and Hep-G2 cancer cells), with IC50 values 6.44 ± 0.87 and 4.57 ± 0.42, respectively. Scoulerine shows antiplasmodial activity with IC50 values of 5.4 μM and 3.1 μM against the antifolate sensitive and the multidrug resistant P. falciparum strains: TM4/8.2 and K1CB1, respectively.

Scoulerine ((-)-Scoulerine) inhibits mini-panel of human leukemic cells, MOLT-4 (WT), Jurkat (TP53 mutated), Raji (TP53 mutated), HL-60 (TP53 null), U-937 (TP53 mutated), and HEL 92.1.7 (wild-type), with IC50s ranging from 2.7?μM to 6.5?μM.Scoulerine (2.5-20?μM; 24 hours) decreases proliferation of Jurkat and MOLT-4 cells.Scoulerine (2.5-20?μM; 24 hours) induces MOLT-4 and Jurkat cells apoptosis.Scoulerine induces G2 or M cell cycle arrest.Scoulerine (2.5-5?μM; 24?hours) shows an upregulation of p53 protein in p53 wild-type MOLT-4 cells.Scoulerine (2.5-5?μM; 24-48 hours) activates caspase-3/7, -8 and -9 in a dose-dependent manner.Scoulerine (5-10 μM; 24 hours) disrupts microtubule structure of A549 lung carcinoma cells .Cell Proliferation Assay Cell Line:Jurkat and MOLT-4 cellsConcentration:2.5, 5, 10, 15 and 20?μM Incubation Time:24?hours Result:Significantly reduced the viability and proliferation of Jurkat and MOLT-4 cells in a dose dependent manner.Apoptosis Analysis Cell Line:MOLT-4 and Jurkat cells Concentration:2.5, 5, 10, 15 and 20?μM Incubation Time:24 hours Result:Induced MOLT-4 and Jurkat cells apoptosis.Cell Cycle Analysis Cell Line:Jurkat and MOLT-4 leukemic cells Concentration:2.5-20 μM Incubation Time:16 hours Result:Induced cell cycle arrest at the G2/M transition.Western Blot Analysis Cell Line:MOLT-4 cells Concentration:2.5, 5?μM Incubation Time:24?hours Result:Showed an upregulation of p53 protein in p53 wild-type MOLT-4 cells.

——

(-)-Scoulerine | Discretamine

Apoptosis

Apoptosis

Apoptosis

——

——

6451-73-6

327.38

C19H21NO4

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (305.46 mM)

COc1cc2CCN3Cc4c(C[C@H]3c2cc1O)ccc(OC)c4O

——

(-20℃)

With Ice Pack

≥ 2 years