AZ505

SKU: orb1296204

Description

AZ505 is a potent and selective small molecule inhibitor of SMYD2, exhibiting an IC50 of 0.12 µM. It serves as a valuable chemical probe for investigating SMYD2's role in cancer biology and epigenetics, enabling target validation in both cellular and animal models of disease.

Research Area

Epigenetics & Chromatin

Key Properties

• CAS Number: 1035227-43-0
• MW: 577.54
• Purity: 98.48% (May vary between batches)
• Formula: C₂₉H₃₈Cl₂N₄O₄
• SMILES: Oc1ccc(CCNCCN(C2CCCCC2)C(=O)CCNCCc2ccc(Cl)c(Cl)c2)c2OCC(=O)Nc12
• Target: Histone Methyltransferase
• Solubility: DMSO:145 mg/mL (251.06 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (8.66 mM)

Bioactivity

• Target IC50:
  SMYD2:0.12 μM
• In Vitro:
  The IC50 of AZ505 for SMYD2 is 0.12 μM, which is >600-fold greater than the IC50s of AZ505 for other histone methyltransferases, such as SMYD3 (IC50>83.3 μM), DOT1L (IC50>83.3 μM) and EZH2 (IC50>83.3 μM) . AZ505 fails to inhibit the enzymatic activities of a panel of protein lysine methyltransferases. AZ505 is nominated for an ITC binding study with Kd of 0.5 μM. In contrast, the calculated Kd for the p53 substrate peptide is 3.7 μM .
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

AZ 505, AZ505, AZ-505, Histone Methyltransferase, HistoneMethyltransferase, Inhibitor, inhibit, SMYD2

Compound Identifiers

PubChem CID

24961094