ML228 - CAS 1357171-62-0
Catalog number:
1357171-62-0
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C27H21N5
Molecular Weight:
415.49
COA:
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Targets:
HIF/HIF Prolyl-Hydroxylase
Description:
HIF pathway activator (EC50 values are 1.23 and 1.4 μM for HRE gene reporter assay and HIF-1α nuclear translocation assay respectively); acts via chelation of iron, independently of PHD. Also exhibits > 80% inhibition of the human A3 receptor, dopamine transporter, μ receptor, hERG and 5-HT2B receptor, and rat sodium channel site 2, at a concentration of 10 μM.
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Purity:
>98%
Synonyms:
ML-228; CID-46742353
MSDS:
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1.Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
Theriault JR1, Felts AS, Bates BS, Perez JR, Palmer M, Gilbert SR, Dawson ES, Engers JL, Lindsley CW, Emmitte KA. Bioorg Med Chem Lett. 2012 Jan 1;22(1):76-81. doi: 10.1016/j.bmcl.2011.11.077. Epub 2011 Nov 28.
Hypoxia and ischemia are linked to several serious public health problems that affect most major organ systems. Specific examples include diseases of the cardiovascular, pulmonary, renal, neurologic, and musculoskeletal systems. The most significant pathway for cellular response to hypoxia is the hypoxia inducible factor (HIF) pathway. HIFs are transcription factors responsible for the activation of genes which encode proteins that mediate adaptive responses to reduced oxygen availability. A high-throughput cell-based HIF-mediated gene reporter screen was carried out using the NIH's Molecular Libraries Small Molecule Repository to identify activators of the HIF pathway. This communication describes the subsequent medicinal chemistry optimization of a triazine scaffold that led to the identification of the new molecular probe ML228. A discussion of HIF activation SAR within this chemotype as well as detailed in vitro characterization of the probe molecule is presented here.
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CAS 1357171-62-0 ML228

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