BK-1361 ( BK 1361 | BK1361 | cyclo-RLsKDK )

产品货号. M21713 CAS No. 1975145-82-4

COA

Datasheet

HNMR

HPLC

MSDS

Handing Instructions

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产品名称

BK-1361
注意事项

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
产品简述

BK-1361(BK1361, cyclo-RLsKDK) 是一种带有 RLsKDK (s=D-丝氨酸) 的环肽，可作为 ADAM8 的有效选择性抑制剂，IC50 为 120 nM。
产品描述

BK-1361(BK1361, cyclo-RLsKDK) is a cyclic peptide with RLsKDK (s=D-serine) that functions as a potent, selective inhibitor of ADAM8 with IC50 of 120 nM; displays no significant activity against ADAM 9, 10, 12, 17 , as well as MMP-2, -9, and -14 at 10 uM; inhibit shedding of CD23 with IC50 of 182 nM in cell-based shedding assays, reduces migration/invasion of pancreatic cancer cells and less ERK1/2 and MMP activation, causes change in cell morphology; decreases tumour burden and metastasis of implanted pancreatic tumour cells and provides improved metrics of clinical symptoms and survival in Kras(G12D)-driven mouse model of PDAC.
体外实验

Cell Invasion Assay Cell Line:Panc1_A8 cells.Concentration:10, 100 and 1,000?nM.Incubation Time:6?h.Result:Reduced cell invasion with dose-dependent manner.
体内实验

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同义词

BK 1361 | BK1361 | cyclo-RLsKDK
通路

Others
靶点

Other Targets
受体

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研究领域

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适应症

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1. Yim V, et al. Bioorg Med Chem. 2016 Sep 15;24(18):4032-4037.

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