| Identification | Back Directory | [Name]
cyclo-RLsKDK) | [CAS]
1975145-82-4 | [Synonyms]
BK1361
cyclo-RLsKDK)
BK-1361
(BK 1361
BK-1361(cyclo(RLsKDK))
Cyclo(L-arginyl-L-leucyl-D-seryl-L-lysyl-L-α-aspartyl-L-lysyl) | [Molecular Formula]
C31H57N11O9 | [MDL Number]
MFCD33029241 | [MOL File]
1975145-82-4.mol | [Molecular Weight]
727.87 |
| Hazard Information | Back Directory | [Uses]
cyclo(RLsKDK) (BK-1361) is a specific inhibitor of metalloproteinase ADAM8 with an IC50 value of 182 nM. cyclo(RLsKDK) has potential applications in inflammatory diseases and cancer[1]. | [in vivo]
cyclo(RLsKDK) (10 μg/g; i.p.; once weekly for 4 weeks) significantly reduces tumour load in mice which implant Panc1_ctrl or Panc1_A8 cells. cyclo(RLsKDK) improves the survival rate of pancreatic ductal adenocarcinoma (PDAC) mice, reduces soluble ADAM8 (sADAM8) content, pERK1/2 activation, and PDAC metastasis in the liver and lungs of PDAC mice[2].
| [References]
[1] Yim V, et al. Synthesis and biological evaluation of analogues of the potent ADAM8 inhibitor cyclo(RLsKDK) for the treatment of inflammatory diseases and cancer metastasis. Bioorg Med Chem. 2016 Sep 15;24(18):4032-4037. DOI:10.1016/j.bmc.2016.06.042
[2] Schlomann U, et al. ADAM8 as a drug target in pancreatic cancer. Nat Commun. 2015 Jan 28;6:6175. DOI:10.1038/ncomms7175 |
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| Company Name: |
Biorbyt Ltd.
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| Tel: |
+44 (0)1223 859 353 |
| Website: |
http://www.biorbyt.com |
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