CLZ-8

目录号: PL02548 纯度: ≥99%
CLZ-8 (Compound 8) 是具有口服活性的 Mcl-1-PUMA 的抑制剂,Ki 值为 0.3 μM。CLZ-8 在下调 PUMA 依赖的凋亡(apoptosis)的同时还能抑制 Mcl-1 介导的癌细胞抗凋亡作用。
CAS No. :678158-55-9
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中文名称
CLZ-8
英文名称
CLZ-8
英文别名
Mcl1-IN-8;STK795397;5-([1,1'-Biphenyl]-4-ylmethylene)-2-(4-(2-hydroxyethyl)piperazin-1-yl)thiazol-4(5H)-one;(5Z)-5-(biphenyl-4-ylmethylidene)-2-[4-(2-hydroxyethyl)piperazin-1-yl]-1,3-thiazol-4(5H)-one;CLZ-8
Cas No.
678158-55-9
分子式
C22H23N3O2S
分子量
393.50
包装储存
Powder -20°C 3 years;4°C 2 years
详情描述
CLZ-8 (Compound 8) 是具有口服活性的 Mcl-1-PUMA 的抑制剂,Ki 值为 0.3 μM。CLZ-8 在下调 PUMA 依赖的凋亡(apoptosis)的同时还能抑制 Mcl-1 介导的癌细胞抗凋亡作用。
产品详情
CLZ-8 (Compound 8) 是具有口服活性的 Mcl-1-PUMA 的抑制剂,Ki 值为 0.3 μM。CLZ-8 在下调 PUMA 依赖的凋亡(apoptosis)的同时还能抑制 Mcl-1 介导的癌细胞抗凋亡作用。
生物活性
CLZ-8 (Compound 8) is an orally active Mcl-1-PUMA interface inhibitor, with a K i of 0.3 μM. CLZ-8 exhibits dual activity on reduce PUMA-dependent apoptosis while deactivating Mcl-1-mediated anti-apoptosis in cancer cells.
性状
Solid
IC50 & Target[1][2]
Mcl-1 0.3 μM (Ki) PUMA
体外研究(In Vitro)
CLZ-8 (Compound 8) (0-160 μM, 48 h) significantly inhibits PUMA-dependent apoptosis.
CLZ-8 (0-1 μM, 2 h) significantly enhance the irradiated cell viability in a dose-dependent manner, provides significant protection for HUVECs, and inhibits overexpressed PUMA.
CLZ-8 (0-1 μM, 24 h) attenuates the radiation-induced apoptosis.
CLZ-8 (1 μM, 2 h) protects HUVECs from DNA breaks. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
CLZ-8 (0-400 mg/kg; i.g.; once) shows powerful anti-radiation effects in mice. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: 6-8 week-old male BALB/c mice
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Liu J, et al. Targeting the apoptotic Mcl-1-PUMA interface with a dual-acting compound. Oncotarget. 2017 Apr 20;8(33):54236-54242.
[2]. Feng T, et al. CLZ-8, a potent small-molecular compound, protects radiation-induced damages both in vitro and in vivo. Environ Toxicol Pharmacol. 2018 Jul;61:44-51.
溶解度数据
In Vitro: DMSO : 50 mg/mL (127.06 mM; Need ultrasonic)配制储备液
搜索质检报告(COA)
[1]. Liu J, et al. Targeting the apoptotic Mcl-1-PUMA interface with a dual-acting compound. Oncotarget. 2017 Apr 20;8(33):54236-54242.
[2]. Feng T, et al. CLZ-8, a potent small-molecular compound, protects radiation-induced damages both in vitro and in vivo. Environ Toxicol Pharmacol. 2018 Jul;61:44-51.

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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