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ML327

Catalog No. T4252 CAS 1883510-31-3

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

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ML327, CAS 1883510-31-3

Pack Size	Availability	Price/USD
1 mg	In stock	$ 45.00
5 mg	In stock	$ 113.00
10 mg	In stock	$ 178.00
25 mg	In stock	$ 372.00
50 mg	In stock	$ 597.00
100 mg	In stock	$ 852.00
1 mL * 10 mM (in DMSO)	In stock	$ 119.00

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Purity: 99.48%

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Description	ML327 is a MYC blocker. ML327 can also de-repress E-cadherin transcription and reverse Epithelial-to-Mesenchymal Transition (EMT).
In vitro	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. 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.
In vivo	Treatment with ML327 leads to a significant reduction in MYCN expression, evidenced by a two-fold decrease, thus verifying its inhibitory effect on xenograft MYCN expression (p=0.0035). Furthermore, ML327 markedly diminishes tumor volume, achieving a three-fold reduction over a two-week period (p=0.02), and similarly, tumor explant weights in ML327-treated mice are approximately three-fold lighter compared to those in control mice (p=0.01). Additionally, ML327 administration results in a 12% greater loss of body weight in treated mice compared to those receiving the vehicle.
Cell Research	ML327 is solubilized in DMSO for in vitro experiments.Cells are seeded onto 96-well plates at equivalent density (3,000 to 10,000 depending upon cell line), permitted to attach overnight, and treated with either ML327 (10 μM) or vehicle. Daily absorbance measurements (450 nm) using the cell counting kit are obtained. For estimation of IC50 values, cells are plated at equal density, permitted to attach, and baseline absorbance is obtained using cell counting kit. Cells are then treated with varying doses of ML327 (0.1 to 30 μM) and cell viability is measured 72 h after treatment.
Animal Research	ML327 is solubilized in 70% polyethylene glycol for in vivo experiments.Male athymic nude mice (4 to 6 weeks old) are maintained as described. BE(2)-C cells xenografts are established as previously described. 1×106 cells/100 μL of HBSS is injected subcutaneously into flanks using a 26-gauge needle (n=10 per group). Mice are monitored daily for xenograft formation and assessed by measuring the two greatest perpendicular tumor diameter with venier calipers. Xenograft volumes are estimated using the following formula [(length×width2)/2]. Once tumors reach 75 to 100 mm3, mice are randomized to receive either 50 mg/kg of ML327 or control vehicle (70% polyethylene glycol) via intraperitoneal injection twice daily for 14d. Weight and tumor volume are recorded daily. After completion of two weeks of treatment, mice are euthanized and tumors are excised, weighed, and RNA is isolated.

Molecular Weight	366.37
Formula	C19H18N4O4
CAS No.	1883510-31-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 13.75 mg/mL (37.53 mM)

References and Literature

1. Rellinger EJ, et al. Isoxazole compound ML327 blocks MYC expression and tumor formation in neuroblastoma. Oncotarget. 2017 Jul 20;8(53):91040-91051. 2. An H, et al. Small molecule/ML327 mediated transcriptional de-repression of E-cadherin and inhibition of epithelial-to-mesenchymal transition.Oncotarget. 2015 Sep 8;6(26):22934-48.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Bioactive Compound Library Bioactive Compounds Library Max Wnt/Hedgehog/Notch Compound Library Anti-Cancer Metabolism Compound Library Glycolysis Compound Library Apoptosis Compound Library NO PAINS Compound Library Anti-Cancer Compound Library Reprogramming Compound Library

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10074-G5 CBP/p300-IN-2 m-Se3 c-Myc inhibitor 12 MYC-RIBOTAC KSI-3716 Lusianthridin Aaptamine

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Keywords

ML327 1883510-31-3 Autophagy Cell Cycle/Checkpoint c-Myc Myc Inhibitor ML-327 inhibit ML 327 inhibitor

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