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BAY-598

Katalog-Nr.GC18159

BAY-598 ist ein selektiver niedermolekularer Inhibitor von SMYD2 mit einem IC50 von 27 nM.

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BAY-598 Chemische Struktur

Cas No.: 1906919-67-2

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5mg
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10mg
134,00 $
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25mg
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Sample solution is provided at 25 µL, 10mM.

Product has been cited by 1 publications

Product Documents

Quality Control & SDS

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Protocol

Kinase experiment:

For SMYD2 inhibition, 10 µL of BAY-598 or DMSO is first incubated with recombinant SMYD2 in methylation buffer reaction for 1 h at 30°C, and then 2 µCi of 3H-AdoMet is added to the mix and incubated overnight at 30°C. The reaction mixture is resolved by SDS-PAGE followed by autoradiography, Coomassie stain, or MS analysis[1].

Cell experiment:

Cells are seeded in 96-well plates at 2000 cells per well (optimum density for growth) in a total volume of 100 μL of medium containing 2% fetal bovine serum. Serially diluted BAY-598 in 100 μL of medium is added to the cells 12 h later. After 72 h of incubation, cell viability is assessed by an MTT assay according to the manufacturer's instructions[1].

References:

[1]. Reynoird N, et al. Coordination of stress signals by the lysine methyltransferase SMYD2 promotes pancreaticcancer. Genes Dev. 2016 Apr 1;30(7):772-85.
[2]. Eggert E, et al. Discovery and Characterization of a Highly Potent and Selective Aminopyrazoline-Based in Vivo Probe (BAY-598) for the Protein Lysine Methyltransferase SMYD2. J Med Chem. 2016 May 26;59(10):4578-600.

Background

BAY-598 is a potent, peptide-competitive chemical probe for SET and MYND domain-containing protein 2 (SMYD2), a lysine methyl transferase inhibitor that dimethylates histone H3K36 and methylates histone H3K4. SMYD2 also methylates Lys-370 of p53, leading to decreased DNA-binding activity. SMYD2 is over-expressed in several cancers with poor prognosis. BAY-598 inhibits in vitro methylation of p53K370 with an IC50 value of 27 nM and in cells with an IC50 value < 1 μM. BAY-598 is more than 100-fold selective over other histone methyltransferases and non-epigenetic targets.

References

[1]. Reynoird N, et al. Coordination of stress signals by the lysine methyltransferase SMYD2 promotes pancreaticcancer. Genes Dev. 2016 Apr 1;30(7):772-85.

Chemical Properties

Cas No. 1906919-67-2 SDF
Chemical Name Bay598N-[(4S)-1-[(Cyanoamino)[[3-(difluoromethoxy)phenyl]imino]methyl]-3-(3,4-dichlorophenyl)-4,5-dihydro-1H-pyrazol-4-yl]-N-ethyl-2-hydroxyacetamide
Canonical SMILES CCN(C(CO)=O)[C@H]1CN(/C(NC2=CC(OC(F)F)=CC=C2)=N\C#N)N=C1C3=CC(Cl)=C(C=C3)Cl
Formula C22H20Cl2F2N6O3 M.Wt 523.4
Löslichkeit DMF: 30 mg/ml,DMSO: 30 mg/ml,Ethanol: 30 mg/ml Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 1.9106 mL 9.5529 mL 19.1058 mL
5 mM 0.3821 mL 1.9106 mL 3.8212 mL
10 mM 0.1911 mL 0.9553 mL 1.9106 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Average Rating: 5 ★★★★★ (Based on Reviews and 4 reference(s) in Google Scholar.)

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