2. Epigenetics
  3. Histone Methyltransferase
  4. AZ505

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

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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10 mM * 1 mL in DMSO USD 216 In-stock
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5 mg USD 170 In-stock
10 mg USD 250 In-stock
25 mg USD 400 In-stock
50 mg USD 620 In-stock
100 mg USD 837 In-stock
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Customer Review

Based on 23 publication(s) in Google Scholar

Other Forms of AZ505:

AZ505 Related Antibodies

Top Publications Citing Use of Products

    AZ505 purchased from MedChemExpress. Usage Cited in: Mol Carcinog. 2023 Apr 10.  [Abstract]

    AZ505 ditrifluoroacetate (AZ505; 20 μM; 48 h) decreases the expression of c-Myc in PC3 and DU145 cells.

    AZ505 purchased from MedChemExpress. 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 MedChemExpress. 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 SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 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

    SMYD2

     

    Cellular Effect
    Cell Line Type Value Description References
    MDA-MB-231 IC50
    13.1 μM
    Compound: AZ505
    Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo luminescent cell viability assay
    Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo luminescent cell viability assay
    		[PMID: 34656041]
    MDA-MB-231 IC50
    2900 nM
    Compound: 1; AZ505
    Inhibition of N-terminal 2xc-myc-tagged human SMYD2 transfected in human MDA-MB-231 cells assessed as reduction in AHNAK methylation after 72 hrs by ICW assay
    Inhibition of N-terminal 2xc-myc-tagged human SMYD2 transfected in human MDA-MB-231 cells assessed as reduction in AHNAK methylation after 72 hrs by ICW assay
    		[PMID: 27075367]
    U2OS IC50
    < 10000 nM
    Compound: 1; AZ505
    Inhibition of SMYD2 (unknown origin) expressed in human U2OS cells assessed as reduction in p53 methylation by Western blot analysis
    Inhibition of SMYD2 (unknown origin) expressed in human U2OS cells assessed as reduction in p53 methylation by Western blot analysis
    		[PMID: 27075367]
    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].

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

    AZ505 Related Antibodies
    Molecular Weight

    577.54

    Formula

    C29H38Cl2N4O4
    CAS No.
    Appearance

    Solid

    Color

    Off-white to light brown

    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
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 135 mg/mL (233.75 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" 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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

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    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 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

      This protocol yields a clear solution of 6.25 mg/mL.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 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

      This protocol yields a clear solution of 6.25 mg/mL.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.99%

    SDS (393 KB)

    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

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.7315 mL 8.6574 mL 17.3148 mL 43.2870 mL
    5 mM 0.3463 mL 1.7315 mL 3.4630 mL 8.6574 mL
    10 mM 0.1731 mL 0.8657 mL 1.7315 mL 4.3287 mL
    15 mM 0.1154 mL 0.5772 mL 1.1543 mL 2.8858 mL
    20 mM 0.0866 mL 0.4329 mL 0.8657 mL 2.1644 mL
    25 mM 0.0693 mL 0.3463 mL 0.6926 mL 1.7315 mL
    30 mM 0.0577 mL 0.2886 mL 0.5772 mL 1.4429 mL
    40 mM 0.0433 mL 0.2164 mL 0.4329 mL 1.0822 mL
    50 mM 0.0346 mL 0.1731 mL 0.3463 mL 0.8657 mL
    60 mM 0.0289 mL 0.1443 mL 0.2886 mL 0.7215 mL
    80 mM 0.0216 mL 0.1082 mL 0.2164 mL 0.5411 mL
    100 mM 0.0173 mL 0.0866 mL 0.1731 mL 0.4329 mL
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    AZ505 Related Classifications

    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.

    Keywords:

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

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