- OTSSP167
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- $1.00 / 1g
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2020-01-13
- CAS:1431697-89-0
- Min. Order: 1g
- Purity: 99%
- Supply Ability: 1ton
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| | OTSSP 167 hydrochloride Basic information |
| | OTSSP 167 hydrochloride Chemical Properties |
| storage temp. | Store at -20°C | | solubility | insoluble in DMSO; insoluble in H2O; insoluble in EtOH | | form | solid |
| | OTSSP 167 hydrochloride Usage And Synthesis |
| Uses | OTSSP167 is a highly potent MELK (maternal embryonic leucine zipper kinase) inhibitor. | | Definition | ChEBI: 4-[7-acetyl-8-[[4-[(dimethylamino)methyl]cyclohexyl]amino]-1H-1,5-naphthyridin-2-ylidene]-2,6-dichloro-1-cyclohexa-2,5-dienone is a naphthyridine derivative. | | Biological Activity | otssp167 is an inhibitor of maternal embryonic leucine zipper kinase (melk) with ic50 value of 0.41nm [1].melk is a member of the ampk serine/threonine kinase family and is involved in the mammalian embryonic development. it plays roles in cancer cell growth and formation or maintenance of cancer stem cells. otssp167 is a small-molecule inhibitor and can inhibit melk’s activity effectively and selectively. otssp167 inhibits cell proliferation of a variety of cancer cell lines including a549, t47d, du4475 and 22rv1. the ic50 values are 6.7nm, 4.3nm, 2.3nm and 6nm, respectively. in mice bearing mda-mb-231 xenograft, administration of otssp167 inhibits 70% tumor growth at dose of 20 mg/kg. besides that, otssp167 is also found to have effects on psma1 and dbnl which are the novel substrates of melk. it inhibits the phosphorylation of psma1 and dbnl causes the subsequent suppression of mammosphere formation [1]. | | target | MELK | | references | [1] chung s, suzuki h, miyamoto t, et al. development of an orally-administrative melk-targeting inhibitor that suppresses the growth of various types of human cancer. oncotarget, 2012, 3(12): 1629. |
| | OTSSP 167 hydrochloride Preparation Products And Raw materials |
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