HDAC-IN-57

HDAC-IN-57 is an orally active inhibitor of histone deacetylases (HDAC), with IC50s of 2.07 nM, 4.71 nM, 2.4 nM and 107 nM for HDAC1, HDAC2, HDAC6, HDAC8, respectively. HDAC-IN-57 can inhibits LSD1, with IC50 of 1.34 μΜ. HDAC-IN-57 induces apoptosis, and has anti-tumor activity[1].

Signaling Pathways >> Apoptosis >> Apoptosis

Signaling Pathways >> Cell Cycle/DNA Damage >> HDAC

Signaling Pathways >> Epigenetics >> HDAC

HDAC1:2.07 nM (IC50)

HDAC2:4.71 nM (IC50)

HDAC6:2.4 nM (IC50)

HDAC8:107 nM (IC50)

HDAC-IN-57 (Compound 5e) (1.0 μM，2.5 μM，5.0 μΜ； 48 小时) 抑制实体肿瘤细胞系 MGC-803，A549，HCT-116 的迁移和侵袭[1]。 HDAC-IN-57 (1.0 μM，2.5 μM，5.0 μΜ；48小时) 显著抑制实体肿瘤细胞系 MGC-803，A549，HCT-116 的生长，IC50s 值分别为 0.45 μM, 1.48 μM 和 0.57 μM[1]。 HDAC-IN-57 (1.0 μM，2.5 μM，5.0 μΜ；48小时) 以剂量依赖性方式触发 MGC-803 和 HCT-116 细胞凋亡[1]。 HDAC-IN-57 (1.0 μM，2.5 μM，5.0 μΜ；48小时) 抑制 MGC-803 和 HCT-116 细胞系内 LSD1 和 HDACs[1]。 HDAC-IN-57 (1.0 μM，2.5 μM，5.0 μΜ；48小时) 诱导 MGC-803 和 HCT-116 细胞周期 G2/M 期阻滞[1]。 HDAC-IN-57 在体外代谢稳定性高。在人肝脏 (HLM) 和大鼠肝脏微粒体 (RLM) 中孵育1 小时后分别保持母体化合物的 86.1% 和 87.4%，T1/2超过 120 分钟[1]。 Western Blot Analysis[1] Cell Line: MGC-803 cells, HCT-116 cells Concentration: 1.5 μM Incubation Time: 48 hours Result: Inhibited cellular LSD1 and HDACs. Upregulated the expression of apoptotic markers, including cytochrome C, Bax, cleaved caspase-3/7/9, and cleaved PARP, while downregulating the expression of anti-apoptotic protein Bcl-2. Apoptosis Analysis[1] Cell Line: MGC-803 cells, HCT-116 cells Concentration: 1.0 μM, 2.5 μM, 5.0 μM Incubation Time: 48 hours Result: Triggered MGC-803 and HCT116 cells apoptosis in a dose-dependent manner. Induced about 55.4% and 51.5% MGC-803 cell apoptosis at a concentration of 5 μM. Cell Migration Assay [1] Cell Line: MGC-803 cells, HCT-116 cells Concentration: 1.0 μM, 2.0 μM, 4 μM Incubation Time: 48 hours Result: Reduced the number of migrated of MGC-803 and HCT-116 cells. Inhibited the migration and invasion of cancer cells. Cell Cycle Analysis[1] Cell Line: MGC-803 cells, HCT-116 cells Concentration: 1.0 μM, 2.5 μM, 5.0 μM Incubation Time: 48 hours Result: Induced G2/M cycle arrest in MGC-803 and HCT-116 cells.

HDAC-IN-57 (Compound 5e) (静脉注射1 mg/kg，口服10 mg/kg) 显示 T＜sub＞1/2HDAC-IN-57 (25或50 mg/kg灌胃；每天1次，连续21天) 在 NOD-SCID 小鼠 MGC-803 异种移植模型中实现了剂量依赖性肿瘤生长抑制[1]。 Animal Model: MGC-803 xenograft model in NOD-SCID mice[1] Dosage: 25 or 50 mg/ kg Administration: Oral gavage (p.o.); Result: Achieved a dose-dependent tumor growth inhibition (TGI) of 44.8% at 25 mg/kg and 71.5% at 50 mg/kg. Animal Model: Male SD rats (Pharmacokinetic assay)[1] Dosage: 1 mg/kg; 10 mg/kg Administration: Intravenous injection (i.v.); Oral gavage (p.o.) Result: Pharmacokinetic parameters for HDAC-IN-57 (Compound 5e) in SD rats[1] Route Dose (mg/kg) T1/2 (h) Tmax (h) CL (mL•min-1/kg-1) AUC0-t (h•ng/mL) AUC0-Ꝏ (h•ng/mL) Cmax (ng/mL) VZ (L/kg) F (%) i.v. 1 0.37 / 1.61 644.1 645.8 1892.8 0.82 / p.o. 10 2.75 0.25 / 685.2 766.2 716.4 52.2 10.6 分子量 377.39 Formula C21H19N3O4 CAS 号 2716217-79-5 运输条件 Room temperature in continental US; may vary elsewhere. 储存方式 Please store the product under the recommended conditions in the Certificate of Analysis. 纯度 & 产品资料 Data Sheet (535 KB) 产品使用指南 (1538 KB) 参考文献 [1]. Duan Y, et al. Discovery of novel, potent, and orally bioavailable HDACs inhibitors with LSD1 inhibitory activity for the treatment of solid tumors. Eur J Med Chem. 2023 Jun 5;254:115367.  [Content Brief] [1]. Duan Y, et al. Discovery of novel, potent, and orally bioavailable HDACs inhibitors with LSD1 inhibitory activity for the treatment of solid tumors. Eur J Med Chem. 2023 Jun 5;254:115367. 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. 摩尔计算器 稀释计算器 The molarity calculator equation Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol) 质量   浓度   体积   分子量 * kg g mg μg ng pg = M mM μM nM pM × L mL μL × The dilution calculator equation Concentration (start) × Volume (start) = Concentration (final) × Volume (final) This equation is commonly abbreviated as: C1V1 = C2V2 浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final) M mM μM nM pM × L mL μL = M mM μM nM pM × L mL μL C1   V1   C2   V2 Powered by Bioz See more details on Bioz Keywords: HDAC-IN-572716217-79-5HDACApoptosisHistone deacetylasesHDAC1 inhibitoranti-tumorMGC-803HCT-116xenograft modelsInhibitorinhibitorinhibit 您最近查看的产品: Your information is safe with us. * Required Fields.    产品名称：   * 需求量： mg g kg t mL L * 客户姓名：   * Email： * 电话：   * 公司或机构名称：    留言给我们： Bulk Inquiry Inquiry Information 产品名称： HDAC-IN-57 目录号： HY-149946 需求量： Request for HNMR Report Please fill out this form to request the QC report. We will send it to your Email address shortly. Your information is safe with us. * Required Fields.    产品名称：   * Lot #： * 客户姓名：   * Email：    电话：   * 部门： * 公司或机构名称：      留言给我们： Request for HNMR Report We have received your request and will respond to you as soon as possible. sales@MedChemExpress.cn 400-820-3792 联系当地授权经销商 MCE 公司 联系我们 关于我们 全球办事处 许可 职业发展 服务与支持 技术支持 定制合成服务 订购指南 售后服务 物流政策 销售条款和条件 技术资源 学术文献 摩尔计算器 稀释计算器 复溶计算器 比活力计算器 Subscribe to our E-newsletter 姓名 邮箱 * Sorry, but the email address you supplied was invalid. Thanks, your subscription has been confirmed. You will hear from us soon. Submission failed, please try again later. MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。 站点地图 隐私声明 Copyright © 2013-2023 MedChemExpress. All Rights Reserved. 沪ICP备15051369号-4 关注我们 获得 MCE 最新资讯 您的账户在别处登录，如果非您本人行为 请重置密码! 我们的 Cookie 政策 我们使用 Cookies 和类似技术以提高网站的性能和提升您的浏览体验，部分功能也使用 Cookies 帮助我们更好地理解您的需求，为您提供相关的服务。 如果您有任何关于我们如何处理您个人信息的疑问，请阅读我们的《隐私声明》。

[1]. Duan Y, et al. Discovery of novel, potent, and orally bioavailable HDACs inhibitors with LSD1 inhibitory activity for the treatment of solid tumors. Eur J Med Chem. 2023 Jun 5;254:115367.