Basic information Safety Supplier Related

OTSSP 167 hydrochloride

Basic information Safety Supplier Related

OTSSP 167 hydrochloride Basic information

Product Name:
OTSSP 167 hydrochloride
Synonyms:
  • MELK inhibitor
  • OTSSP 167 hydrochloride
  • OTSSP167 (hydrochloride)
  • OTSSP-167 hydrochloride
  • OTSSP 167
  • OTSSP167
  • OTSSP-167
  • CS-1832
CAS:
1431697-89-0
MF:
C25H28Cl2N4O2
MW:
487.42
EINECS:
200-258-5
Product Categories:
  • Inhibitors
  • API
Mol File:
1431697-89-0.mol
More
Less

OTSSP 167 hydrochloride Chemical Properties

storage temp. 
Store at -20°C
solubility 
insoluble in DMSO; insoluble in H2O; insoluble in EtOH
form 
solid
color 
Light yellow to yellow
More
Less

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 hydrochlorideSupplier

Shanghai Boyle Chemical Co., Ltd.
Tel
Email
sales@boylechem.com
Dalian Meilun Biotech Co., Ltd.
Tel
0411-62910999 13889544652
Email
meilunui@163.com
MedChemexpress LLC
Tel
021-58955995
Email
sales@medchemexpress.cn
CEG Chemical Science&Technology Co., Ltd.
Tel
Mobile:13665161512
AdooQ Bioscience CHINA
Tel
025-58849295 18951903616;
Email
info@adooq.cn
More
Less

OTSSP 167 hydrochloride(1431697-89-0)Related Product Information