YUM70

CAS号

423145-35-1

分子式

C21H19ClN2O4

主要靶点

Apoptosis|GPR|HSP

仅限科研使用

Cat No : CM04653

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Synonyms

glucose-regulated|GRP78|endoplasmic|HSP|Heat shock proteins|Apoptosis|cancer|reticulum|protein|pancreatic|inhibit|Inhibitor|YUM 70|YUM70|YUM-70|stress-mediated



产品信息

CAS号 423145-35-1
分子式 C21H19ClN2O4
主要靶点 Apoptosis|GPR|HSP
主要通路 凋亡|内分泌与激素|G 蛋白偶联受体|代谢|细胞骨架
分子量 398.84
纯度 97.25%, 此纯度可做参考,具体纯度与批次有关系,可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
别名 glucose-regulated|GRP78|endoplasmic|HSP|Heat shock proteins|Apoptosis|cancer|reticulum|protein|pancreatic|inhibit|Inhibitor|YUM 70|YUM70|YUM-70|stress-mediated

靶点活性

GRP78:1.5 μM

体内活性

YUM70在胰腺癌异种移植模型中具有体内效能,且对正常组织无毒性。YUM70是一种新型的内质网应激诱导剂,在胰腺癌的临床前研究中,无论是作为单药治疗还是与拓扑异构酶和HDAC抑制剂联合使用,均显示出预期效果。

体外活性

YUM70通过直接结合GRP78并使其失活,抑制了体外胰腺癌细胞的增长,并引起了ER应激介导的细胞凋亡。一个与BODIPY偶联的YUM70类似物显示了该化合物与GRP78在ER中的共定位。

溶解度

DMSO:100 mg/mL (250.73 mM)

参考文献

1.Samanta S, et, al. The hydroxyquinoline analog YUM70 inhibits GRP78 to induce ER stress-mediated apoptosis in pancreatic cancer. Cancer Res. 2021 Feb 2;canres.1540.2020.

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