Apostatin-1 (Apt-1) 是一种有效的 TRADD 抑制剂。Apostatin-1 可与 TRADD-N 结合 (KD=2.17 μM)，破坏其与 TRADD-C 和 TRAF2 的结合。Apostatin-1 调节 RIPK1 和 beclin 1 的泛素化。Apostatin-1 通过激活突变 tau、α-synuclein 或 huntingtin 积累的细胞中的自噬 (autophagy)，阻断凋亡 (apoptosis)，并恢复细胞内稳态。
货号:ajcx38724
CAS:2559703-06-7
分子式:C19H27N3OS
分子量：345.5
溶解度:DMSO : 83.33 mg/mL (241.19 mM; ultrasonic and warming and adjust pH to 4 with HCl and heat to 80°C)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

Apostatin-1 (Apt-1) is a potent TRADD inhibitor. Apostatin-1 can bind with TRADD-N (KD=2.17 μM), disrupting its binding to both TRADD-C and TRAF2. Apostatin-1 modulates the ubiquitination of RIPK1 and beclin 1. Apostatin-1 blocks apoptosis and restores cellular homeostasis by activating autophagy in cells with accumulated mutant tau, α-synuclein, or huntingtin[1].

Apostatin-1 inhibits Velcade (Bortezomib, 0)-induced apoptosis and RIPK1-dependent apoptosis (RDA) and necroptosis, with an IC50 of 0.97 μM[1].Apostatin-1 (10 μM, 6 h) effectively induces autophagy and the degradation of long-lived proteins[1].

Apostatin-1 (20 mg/kg, IP, once) inhibits inflammatory responses, and increases survival of systemic inflammation mouse model[1].

[1]. Xu D, et al. Modulating TRADD to restore cellular homeostasis and inhibit apoptosis. Nature. 2020 Nov;587(7832):133-138.