ML228 --- HIF Pathway Activator

ML228 is a hypoxia inducible factor (HIF) pathway activator with an EC50 at ~1.23 µM in HRE gene reporter assay and ~1.4 μM in HIF-1α nuclear translocation assay. It does not inhibit the proteasome, but activates HIF stabilization and nuclear translocation, and induces expression of a HIF specific downstream gene (VEGF). It has no apparent toxicity below 30 μM and appeared to be an iron chelator, independently of PHD. HIFs are transcription factors responsible for the activation of genes which encode proteins that mediate adaptive responses to reduced oxygen availability. HIF pathway is the most significant pathway for cellular response to hypoxia.

Product information

CAS Number: 1357171-62-0

Molecular Weight: 415.49

Formula: C27H21N5

Chemical Name: N-([1,1'-biphenyl]-4-ylmethyl)-6-phenyl-3-(pyridin-2-yl)-1,2,4-triazin-5-amine

Smiles: C(NC1=NC(=NN=C1C1C=CC=CC=1)C1=CC=CC=N1)C1C=CC(=CC=1)C1C=CC=CC=1

InChiKey: QNRODODTMXCRKU-UHFFFAOYSA-N

InChi: InChI=1S/C27H21N5/c1-3-9-21(10-4-1)22-16-14-20(15-17-22)19-29-27-25(23-11-5-2-6-12-23)31-32-26(30-27)24-13-7-8-18-28-24/h1-18H,19H2,(H,29,30,32)

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO up to 100 mM

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

ML228 was used at 10 µM final concentration in various in vitro assays.

References:

1. Theriault JR, et al. Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway. (2012) Bioorg Med Chem Lett. 22(1):76-81.

Products are for research use only. Not for human use.

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