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CAS No.: 1906919-67-2

BAY-598 Catalog No. CSN22321

Synonyms: (S)-BAY-598

BAY-598 is an inhibitor of SMYD2. It can inhibit in vitro methylation of p53 at lysine 370 with IC50 value of 27 nM.

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400-920-2911

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

描述BAY-598 is a potent, selective and substrate-competitive SMYD2 inhibitor with IC50 values of 27 nM and <1 µM for inhibition of p53 at lysine 370 in vitro and in whole HEK293T cells with transient transfected withFLAG-tagged SMYD2 and FLAG-tagged p53, respectively, displaying >100-fold selectivity for SMYD2 over a panel of 32 other methyltransferases including SMYD3, SUV420H1, and SUV420H2. BAY-598 dose-dependently decreased endogenous p53 at lysine 370 in KYSE-150 esophageal cancer cells at concentration of 2.5μM and 10μM after 5-day treatment. Also treatment with BAY-598 at concentration of 63-2000nM caused decreased methylation level of AHNAK, a substrate of SMYD2, in MDA-MB231 cells overexpressing SMYD2. BAY-598 at concentration ranging in 5-20μM could enhance apoptotic responses to doxorubicin in KYSE-150, U2OS and A2780 cells. Also this synergistic effect on apoptosis induction could be observed in vivo as combination treatment of BAY-598 at dose of 500 mg/kg, p.o., q.d. for 14 days could enhance the tumor growth inhibition in mice bearing subcutaneous KYSE-150 tumor compared with each agent alone, with a minor body weight loss.
动物研究
剂量
Mice: 50 mg/kg^[1] (i.p.); 10 mg/kg - 100 mg/kg^[2] (p.o.) Rat: 0.8 mg/kg^[2] (p.o.); 0.4 mg/kg^[2] (i.v.)

给药途径
i.p., p.o., i.v.

动物研究
剂量	Mice: 50 mg/kg^[1] (i.p.); 10 mg/kg - 100 mg/kg^[2] (p.o.) Rat: 0.8 mg/kg^[2] (p.o.); 0.4 mg/kg^[2] (i.v.)
给药途径	i.p., p.o., i.v.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.9035 mL
- 9.5177 mL
- 19.0355 mL
- 5 mM
- 0.3807 mL
- 1.9035 mL
- 3.8071 mL
- 10 mM
- 0.1904 mL
- 0.9518 mL
- 1.9035 mL

技术信息

CAS号

1906919-67-2

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C22H20Cl2F2N6O3

运输

蓝冰

分子量

525.34

别名

(S)-BAY-598

溶解度

DMSO	120.0 mg/mL (228.4 mM) warming
Water	Insoluble

动物实验配方

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