BAY-598
目录号 : GC18159
An inhibitor of SMYD2
Cas No.:1906919-67-2
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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. | |
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.
| Cas No. | 1906919-67-2 | SDF | |
| 化学名 | 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 | ||
| 分子式 | C22H20Cl2F2N6O3 | 分子量 | 523.4 |
| 溶解度 | DMF: 30 mg/ml,DMSO: 30 mg/ml,Ethanol: 30 mg/ml | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。