Art. -Nr.: HY-15226

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AZ505

22 Cited Publications

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Based on 22 publication(s) in Google Scholar

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

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Reinheit: 99.98%
CAS. Nr.: 1035227-43-0
Formel: C₂₉H₃₈Cl₂N₄O₄
Molecular Weight:577.54

Speicherung:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

AZ505 Chemical Structure

CAS. Nr.: 1035227-43-0

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Publications (22)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Bioz

Biologische Aktivität

Beschreibung

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

IC₅₀ & Target

SMYD2

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
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]
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]
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 K_d of 0.5 μM. In contrast, the calculated K_d 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.

Chemical Information

CAS. Nr. 1035227-43-0
Appearance Solid
Molecular Weight 577.54
Formel C₂₉H₃₈Cl₂N₄O₄
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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (22)

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Journal Impact Factor

Cell

Positive selection of somatically mutated clones identifies adaptive pathways in metabolic liver disease. [Abstract]

2023 Apr 27;186(9):1968-1984.e20. PMID: 37040760
J Clin Invest

Lysine methyltransferase SMYD2 promotes cyst growth in autosomal dominant polycystic kidney disease. [Abstract]

2017 Jun 30;127(7):2751-2764. PMID: 28604386

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.
Theranostics

Inhibition of SMYD2 suppresses tumor progression by down-regulating microRNA-125b and attenuates multi-drug resistance in renal cell carcinoma. [Abstract]

2019 Oct 22;9(26):8377-8391. PMID: 31754403
Sci Adv

SMYD2 inhibition-mediated hypomethylation of Ku70 contributes to impaired nonhomologous end joining repair and antitumor immunity. [Abstract]

2023 Jun 16;9(24):eade6624. PMID: 37315132
Sci Adv

Cross-talk between CDK4/6 and SMYD2 regulates gene transcription, tubulin methylation, and ciliogenesis. [Abstract]

2020 Oct 30;6(44):eabb3154. PMID: 33127671
Cell Death Dis

SMYD2 targets RIPK1 and restricts TNF-induced apoptosis and necroptosis to support colon tumor growth. [Abstract]

2022 Jan 12;13(1):52. PMID: 35022391
Cell Death Dis

SMYD2 promotes tumorigenesis and metastasis of lung adenocarcinoma through RPS7. [Abstract]

2021 May 2;12(5):439. PMID: 33935284
Cell Death Dis

Lysine methyltransferase SMYD2 promotes triple negative breast cancer progression. [Abstract]

2018 Feb 27;9(3):326. PMID: 29487338

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.
Oncogene

BRD4 inhibition sensitizes cervical cancer to radiotherapy by attenuating DNA repair. [Abstract]

2021 Apr;40(15):2711-2724. PMID: 33712705
Cell Death Discov

SMYD2 aggravates gastrointestinal stromal tumor via upregulation of EZH2 and downregulation of TET1. [Abstract]

2022 Jun 6;8(1):274. PMID: 35668081
Biochem Pharmacol

Lysine methylation-mediated SMYD2 degradation by casticin sensitizes non-small-cell lung cancer cells to osimertinib therapy. [Abstract]

2026 Jan;243(Pt 2):117562. PMID: 41314435
Cells

SMYD2 Inhibition Downregulates TMPRSS2 and Decreases SARS-CoV-2 Infection in Human Intestinal and Airway Epithelial Cells. [Abstract]

2022 Apr 8;11(8):1262. PMID: 35455942
FASEB J

Critical roles of SMYD2 lysine methyltransferase in mediating renal fibroblast activation and kidney fibrosis. [Abstract]

2021 Jul;35(7):e21715. PMID: 34143514
Biomedicines

SMYD2 Promotes Calcium Oxalate-Induced Glycolysis in Renal Tubular Epithelial Cells via PTEN Methylation. [Abstract]

2024 Oct 8;12(10):2279. PMID: 39457592
Development

The Gridlock transcriptional repressor impedes vertebrate heart regeneration by restricting expression of lysine methyltransferase. [Abstract]

2020 Sep 28;147(18):dev190678. PMID: 32988975
Exp Cell Res

SMYD2 suppresses p53 activity to promote glucose metabolism in cervical cancer. [Abstract]

2021 Jul 15;404(2):112649. PMID: 34015314
Am J Physiol Renal Physiol

Cross talk between lysine methyltransferase Smyd2 and TGF-β-Smad3 signaling promotes renal fibrosis in autosomal dominant polycystic kidney disease. [Abstract]

2022 Aug 1;323(2):F227-F242. PMID: 35759739
Mol Carcinog

PRMT1 inhibition promotes ferroptosis sensitivity via ACSL1 upregulation in acute myeloid leukemia. [Abstract]

2023 Aug;62(8):1119-1135. PMID: 37144835
Mol Carcinog

Targeting SMYD2 inhibits prostate cancer cell growth by regulating c-Myc signaling. [Abstract]

2023 Jul;62(7):940-950. PMID: 37036190

AZ505 purchased from MedChemExpress. Usage Cited in: Mol Carcinog. 2023 Jul;62(7):940-950. [Abstract]

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

A Novel Inhibitor of Methyltransferase SMYD2, AZ505 Protects Against Peritoneal Fibrosis in Mice. [Abstract]

2025 Jul;52(7):e70035. PMID: 40414794
J Bone Metab

Effects of the Lysine Methyltransferase Inhibitor AZ505 on Bone Metabolism. [Abstract]

2021 Nov;28(4):297-305. PMID: 34905676
Research Square Preprint

2021 Oct.

Lösungsmittel & Löslichkeit

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. 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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of 6.25 mg/mL. If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Protokoll

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].

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)
SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Portuguese - PT (394 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Komatsu S, et al. Overexpression of SMYD2 contributes to malignant outcome in gastric cancer. Br J Cancer. 2015 Jan 20;112(2):357-64. [Content Brief]

[2]. Ferguson AD, et al. Structural basis of substrate methylation and inhibition of SMYD2. Structure. 2011 Sep 7;19(9):1262-73. [Content Brief]

[3]. Li LX, et al. Lysine methyltransferase SMYD2 promotes cyst growth in autosomal dominant polycystic kidney disease. J Clin Invest. 2017 Jun 30;127(7):2751-2764. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

AZ505

22 Cited Publications

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AZ505

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Reprogramming Compound Library

Anti-Blood Cancer Compound Library

Highly Selective Inhibitors Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

Epigenetics Compound Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

Methylation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) AZ505

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (22)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

AZ505

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Reprogramming Compound Library

Anti-Blood Cancer Compound Library

Highly Selective Inhibitors Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

Epigenetics Compound Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

Methylation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) AZ505

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (22)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

AZ505 Related Classifications

Art. -Nr.: HY-15226