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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Matrix Metalloproteinase (MMP)-BK-1361
BK-1361

Chemical Structure : BK-1361

CAS No.: 1975145-82-4

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

货号: PC-60981Not For Human Use, Lab Use Only.

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.

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纯度 & COA & 质检文件 纯度: 99.08% (HPLC) Select Batch:

生物&药学活性

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.
BK-1361 displays no significant activity against ADAM 9, 10, 12, 17 , as well as MMP-2, -9, and -14 at 10 uM.
BK-1361 inhibits 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.
BK-1361 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.

物理化学性质&存储条件

分子量 727.865
分子式 C31H57N11O9
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

cyclo-RLsKDK; s=D-serine

参考文献

1. Schlomann U, et al. Nat Commun. 2015 Jan 28;6:6175.

2. Chen J, et al. Sci Rep. 2016 Jul 26;6:30451.

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

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