| Bioactivity | CLZ-8 (Compound 8) is an orally active Mcl-1-PUMA interface inhibitor, with a Ki of 0.3 μM. CLZ-8 exhibits dual activity on reduce PUMA-dependent apoptosis while deactivating Mcl-1-mediated anti-apoptosis in cancer cells[1]. | ||||||||||||
| Invitro | CLZ-8 (Compound 8) (0-160 μM, 48 h) significantly inhibits PUMA-dependent apoptosis[1].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[2].CLZ-8 (0-1 μM, 24 h) attenuates the radiation-induced apoptosis[2].CLZ-8 (1 μM, 2 h) protects HUVECs from DNA breaks[2]. Apoptosis Analysis[1][2] Cell Line: | ||||||||||||
| In Vivo | CLZ-8 (0-400 mg/kg; i.g.; once) shows powerful anti-radiation effects in mice[2]. Animal Model: | ||||||||||||
| Name | CLZ-8 | ||||||||||||
| CAS | 678158-55-9 | ||||||||||||
| Formula | C22H23N3O2S | ||||||||||||
| Molar Mass | 393.50 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |