STM2457
作者：齐岳
发布时间：2023-09-06
08:59:46
点击数：
产品名称：STM2457
产品描述：
| 产品描述 | STM2457 is a first-in-class, highly potent, selective and orally active inhibitor of METTL3 . It can be used for the research of acute myeloid leukaemia (AML). |
| 体外活性 | STM2457 (Compound 72) inhibits MOLM13 cells proliferation with an IC50?of 8.699 μM[1]. STM2457, a highly potent and selective first-in-class catalytic inhibitor of METTL3, and a crystal structure of STM2457 in complex with METTL3-METTL14. Treatment of tumours with STM2457 leads to reduced AML growth and an increase in differentiation and apoptosis. These cellular effects are accompanied by selective reduction of m6A levels on known leukaemogenic mRNAs and a decrease in their expression consistent with a translational defect. We demonstrate that pharmacological inhibition of METTL3 in vivo leads to impaired engraftment and prolonged survival in various mouse models of AML, specifically targeting key stem cell subpopulations of AML[2]. |
| 化合物与蛋白结合的复合物 |
METTL3-METTL14 heterodimer bound to the SAM competitive small molecule inhibitor STM2457 |
| 分子量 | 444.53 |
| 分子式 | C25H28N6O2 |
| CAS No. | 2499663-01-1 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 100 mM,Need ultrasonic
( < 1 mg/mL refers to the product slightly soluble or insoluble )
联系我们：
邮箱：2519696869@qq.com
QQ: 2519696869
电话：18066853083
微信：18066853083
公司介绍：
西安齐岳生物科技有限公司是集化学科研和定制与一体的高科技化学公司。业务范围包括化学试剂和产品的研发、生产、销售等。涉及产品为通用试剂的分销、非通用试剂的定制与研发，涵盖生物科技、化学品、中间体和化工材料等领域。
主营产品：COF、MOF单体系列：三蝶烯衍生物、金刚烷衍生物、四苯甲烷衍生物、peg、上转换、石墨烯、光电材料、点击化学、凝集素、载玻片、蛋白质交联剂、脂质体、蛋白、多肽、氨基酸、糖化学等。
