2. Epigenetics
  3. Histone Methyltransferase
  4. AZ505

AZ505 

Cat. No.: HY-15226 Purity: 99.94%
COA Handling Instructions

AZ505 is a potent and selective SMYD2 inhibitor with an IC50 of 0.12 μM.

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

AZ505 Chemical Structure

AZ505 Chemical Structure

CAS No. : 1035227-43-0

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 290 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 290 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 200 In-stock
Estimated Time of Arrival: December 31
10 mg USD 320 In-stock
Estimated Time of Arrival: December 31
25 mg USD 775 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1100 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1800 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 17 publication(s) in Google Scholar

Other Forms of AZ505:

Top Publications Citing Use of Products

    AZ505 purchased from MCE. Usage Cited in: Cell Death Dis. 2018 Feb 27;9(3):326.  [Abstract]

    Inhibition of SMYD2 with AZ505 (40 μM, 2 h) decreases the methylation and phosphorylation of STAT3 and p65, but dpes not affect their expression in MDA-MB231 cells.

    AZ505 purchased from MCE. Usage Cited in: J Clin Invest. 2017 Jun 30;127(7):2751-2764.  [Abstract]

    PKD-associated signaling pathways can be affected by SMYD2 in Pkd1 mutant renal epithelial cells and cystic tissues. Western blot analysis of the phosphorylation of ERK, S6, AKT, and Rb as well as the total protein levels of these proteins in Pkd1-null MEK cells with or without AZ505 treatment for 2 hours.

    View All Histone Methyltransferase Isoform Specific Products:

    View All Isoforms
    EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT8

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    AZ505 is a potent and selective SMYD2 inhibitor with an IC50 of 0.12 μM.

    IC50 & Target

    IC50: 0.12 μM (SMYD2)[1]
    In Vitro

    AZ505 is highly selective and shows an activity at submicromolar concentrations 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)[1]. AZ505 is a potent and selective SMYD2 inhibitor with an IC50 of 0.12 μM. The human SMYD (SET and MYND domain-containing protein) family of protein lysine methyltransferases contains five members (SMYD1-5). Moreover, AZ505 fails to inhibit the enzymatic activities of a panel of protein lysine methyltransferases. AZ505 is nominated for ITC binding study with Kd of 0.5 μM. In contrast, the calculated Kd for the p53 substrate peptide is 3.7 μM. AZ505 binding to SMYD2 is driven primarily by entropy, which often suggests that binding is mediated by hydrophobic interactions with few specific hydrogen bonds[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Molecular Weight

    577.54

    Appearance

    Solid

    Formula

    C29H38Cl2N4O4
    CAS No.
    SMILES

    O=C(N(C1CCCCC1)CCNCCC2=C(OCC(N3)=O)C3=C(O)C=C2)CCNCCC4=CC=C(Cl)C(Cl)=C4
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 250 mg/mL (432.87 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.7315 mL 8.6574 mL 17.3148 mL
    5 mM 0.3463 mL 1.7315 mL 3.4630 mL
    10 mM 0.1731 mL 0.8657 mL 1.7315 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: 6.25 mg/mL (10.82 mM); Clear solution; Need ultrasonic

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: 6.25 mg/mL (10.82 mM); Clear solution; Need ultrasonic

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: 6.25 mg/mL (10.82 mM); Clear solution; Need ultrasonic

    *All of the co-solvents are available by MCE.
    Purity & Documentation

    Purity: 99.99%

    COA (244 KB) HNMR (212 KB) LCMS (377 KB)

    Handling Instructions (2659 KB)
    References
    Kinase Assay
    [2]

    SMYD2 is expressed in insect cells and purified. AlphaScreen technology is used to screen our chemical library for small molecule inhibitors of SMYD2. Methylation (12 μL) reactions are carried out in TDT buffer (50 mM Tris-HCl [pH 9.0], 2 mM DTT, and 0.01% Tween 20) at room temperature using 1.25 nM SMYD2 protein, 200 nM SAM, and 100 nM biotinylated p53 peptide substrate (Biotin-aminohexanoyl-GSRAHSSHLKSKKGQSTSRH) in low volume 384-well plates. Following a 75 min incubation period, reactions are quenched by the addition of 5 μL of detection solution (20 mM HEPES [pH 7.4], 1.7 mg/mL BSA, 340 mM NaCl, 680 μM SAH, 0.04 mg/mL Streptavidin-coated AlphaScreen donor, and Protein A-coated acceptor beads), and 1 nM of a custom p53K370me1 polyclonal antibody. Reaction plates are incubated overnight in the dark at room temperature, and read using an Envision 2101 Multi-label Reader. Compounds showing >50% inhibition of SMYD2 are nominated for concentration dose-response determination, and are also subjected to an artifact assay. Seven compound concentrations are selected beginning at 30 μM with six half-log dilution steps. The artifact assay conditions are identical to those in the SMYD2 enzymatic activity assay, except for the absence of SMYD2 protein and the presence of 1 nM methylated p53 peptide. IC50 values are calculated from dose-response data using in-house software[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    References
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    Help & FAQs
    • Do most proteins show cross-species activity?

      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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    Keywords:

    AZ5051035227-43-0AZ 505AZ-505Histone MethyltransferaseInhibitorinhibitorinhibit

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