1. Epigenetics Autophagy
  2. Histone Methyltransferase Autophagy
  3. SMYD3-IN-2

SMYD3-IN-2 is a SMYD3 inhibitor against gastric cancer via inducing lethal autophagy. SMYD3-IN-2 has inhibitory for SMYD3 and BGC823 cells with IC50 values of 0.81 μM and 0.75 μM, respectively. SMYD3-IN-2 can be used for the research of cancer.

For research use only. We do not sell to patients.

SMYD3-IN-2 Chemical Structure

SMYD3-IN-2 Chemical Structure

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Description

SMYD3-IN-2 is a SMYD3 inhibitor against gastric cancer via inducing lethal autophagy. SMYD3-IN-2 has inhibitory for SMYD3 and BGC823 cells with IC50 values of 0.81 μM and 0.75 μM, respectively. SMYD3-IN-2 can be used for the research of cancer[1].

IC50 & Target

SMYD3

0.81 μM μM (IC50)

In Vitro

SMYD3-IN-2 (compound 7r) (1.0 μM) exhibits potent inhibitory capacity against SMYD3 and BGC823 cells with IC50 values of 0.81 μM and 0.75 μM, respectively[1].
SMYD3-IN-2 (1.0 μM; 24 h) can suppress Akt methylation and activation by SMYD3[1].
SMYD3-IN-2 (0-48 h) suppresses the proliferation of BGC823 stomach adenocarcinoma cells by inducing autophagic cell death[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: BGC823 cells
Concentration: 1.0 μM
Incubation Time: 24 h
Result: Suppressed the methylation levels of H3K4 and could significantly inhibit the lysine methylation of Akt1 by SMYD3.
In Vivo

SMYD3-IN-2 (compound 7r) (i.p.; 15 and 30 mg/kg) suppresses the growth of BGC823 xenograft models in vivo[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Xenograft Balb/c nude mice models[1]
Dosage: 15 and 30 mg/kg
Administration: Intraperitoneally administration
Result: Remarkably suppressed the tumor volume, tumor weight and growth curves of gastric cancer xenografts in a dose-dependent manner.
Resulted in strong immunohistochemistry staining of LC3-II and p62, weak staining of p-Akt (T308) and Ki67.
Molecular Weight

505.36

Formula

C26H21BrN2O4

SMILES

[H][C@]12CN(C([C@]1(O[C@@]3([C@@H]2C4=CC=C(C=C4)Br)C(NC5=CC=CC=C53)=O)O)=O)CC6=CC=CC=C6

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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SMYD3-IN-2 Related Classifications

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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
SMYD3-IN-2
Cat. No.:
HY-152228
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