ML327 is a blocker of MYC which can also de-repress E-cadherin transcription and reverse Epithelial-to-Mesenchymal Transition (EMT).

Product information

CAS Number: 1883510-31-3

Molecular Weight: 366.37

Formula: C19H18N4O4

Chemical Name: 2-oxo-N-{3-[(5-phenyl-1,2-oxazol-3-yl)formamido]propyl}-1,2-dihydropyridine-3-carboxamide

Smiles: O=C(NCCCNC(=O)C1=CC=CNC1=O)C1C=C(ON=1)C1C=CC=CC=1

InChiKey: NNNDNXLMQAPQQQ-UHFFFAOYSA-N

InChi: InChI=1S/C19H18N4O4/c24-17-14(8-4-9-20-17)18(25)21-10-5-11-22-19(26)15-12-16(27-23-15)13-6-2-1-3-7-13/h1-4,6-9,12H,5,10-11H2,(H,20,24)(H,21,25)(H,22,26)

Technical Data

Appearance: Solid Power

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

Solubility: DMSO : 32 mg/mL (87.34 mM; Need ultrasonic and warming).

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:

Treatment with ML327 induces an elongated morphology in neuroblastoma cells. BE(2)-C cells treated with ML327 demonstrates G1 cell cycle arrest with a concordant decrease in S phase population, and a significant increase in the sub G0 population. ML327 induces the expression of CDH1 in all seven of the neuroblastoma cell lines with a 50 to 1,400-fold induction of CDH1 mRNA expression. ML327 blocks the expression of MYC family of oncogenic transcription factors in all tested neuroblastoma cell lines. Immunoblotting time course demonstrates early repression of N-MYC expression within 2 h of treatment with ML327 (10 µM). p53 levels are also suppressed by treatment with ML327. ML327-pretreated cells demonstrates reduced proliferative potential in both tetrazolium-based (p<0.0001) and adherent 2D colony formation (41 vs. 400; p<0.0001). ML327 reduces SW620inv cell invasion through Matrigel by ~60% and reduces H520 cell invasion by ~30% in these in vitro assays. ML327 partially restores E-cadherin expression at the plasma membrane in NMuMG cells induced to undergo Epithelial-to-Mesenchymal Transition (EMT) by TGF-β1 treatment.

In Vivo:

ML327 treatment significantly reduces tumor volume by three-fold over the two-week treatment period (p=0.02). Tumor explant weights are approximately three-fold smaller in the ML327-treated mice (p=0.01). Mice treated with ML327 lost 12% more body weight than vehicle treated mice. ML327 treatment results in a two-fold decrease in MYCN expression, confirming that ML327 inhibits xenograft MYCN expression (p=0.0035).

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