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M344 (D 237) HDAC inhibitor

Cat.No.S2779

M344 is a potent HDAC inhibitor with IC50 of 100 nM and able to induce cell differentiation.
M344 (D 237) HDAC inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 307.39

Quality Control

Batch: S277901 DMSO]62 mg/mL]false]Ethanol]4 mg/mL]false]Water]Insoluble]false Purity: 99.36%
99.36

Chemical Information, Storage & Stability

Molecular Weight 307.39 Formula

C16H25N3O3

Storage (From the date of receipt)
CAS No. 251456-60-7 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CN(C)C1=CC=C(C=C1)C(=O)NCCCCCCC(=O)NO

Solubility

In vitro
Batch:

DMSO : 62 mg/mL (201.69 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 4 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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In vivo Formulation Calculator (Clear solution)

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Mechanism of Action

Features
An inducer of terminal cell differentiation and a potent HDAC inhibitor.
Targets/IC50/Ki
HDAC [1]
100 nM
In vitro

M344 produces a more significant effect on cell proliferation than on cell differentiation in MEL DS19 cells. This compound is toxic at concentrations above 10 μM, while a maximum of only 20% of the surviving cell population are induced to differentiate. [1] In vitro, this chemical shows the significant anti-proliferative activities against the endometrial cancer cell line Ishikawa and the ovarian cancer cell line SK-OV-3 with EC50 of 2.3 μM and 5.1 μM, respectively. While the normal human endometrial epithelial cells shows little sensitivity to this compound. In addition, it also leads to decreased proportion of cells in the S-phase and increased proportion in the G0/G1 phases of the cell cycle, induces apoptosis and decreases the transmembrane potential of mitochondria. [2] This chemical potently inhibits proliferation of embryonal nervous system tumor cells including medulloblastoma cells (D341 Med, Daoy) and neuroblastoma cells (CH-LA 90,SHSY-5Y ) with GI50 of 0.65 μM, 0.63 μM, 0.63 μM and 0.67 μM, respectively. [3]

Kinase Assay
Enzyme Inhibition
Radioactively labeled chicken core histones are used as the enzyme substrate. The enzyme liberated tritiated acetic acid from the substrate which is quantitated by scintillation counting. IC50 values are results of triple determinations. 50 μL of maize enzyme (at 30 °C) is incubated (30 minutes) with 10 μL of total [3H]acetate-prelabeled chicken reticulocyte histones (1 mg/mL). Reaction is stopped by addition of 36 μL of 1 M HCl/0.4 M acetate and 800 μL of ethyl acetate. After centrifugation (10000g, 5 minutes) an aliquot of 600 μL of the upper phase is counted for radioactivity in 3 mL of liquid scintillation cocktail. This compound is tested in a starting concentration of 40 μM, and active substances are diluted further.
References

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