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。
生物活性 | Apostatin-1 (Apt-1) is a potentTRADDinhibitor. Apostatin-1 can bind withTRADD-N(KD=2.17 μM), disrupting its binding to both TRADD-C and TRAF2. Apostatin-1 modulates the ubiquitination ofRIPK1andbeclin 1. Apostatin-1 blocksapoptosisand restores cellular homeostasis by activatingautophagyin cells with accumulated mutant tau,α-synuclein, orhuntingtin[1]. |
体外研究 (In Vitro) | Apostatin-1 inhibits Velcade (Bortezomib, HY-134050)-induced apoptosis and RIPK1-dependent apoptosis (RDA) and necroptosis, with an IC50of 0.97 μM[1]. Apostatin-1 (10 μM, 6 h) effectively induces autophagy and the degradation of long-lived proteins[1].
Western Blot Analysis[1] Cell Line: | SH-SY5Y, HeLa, HT-29, and Jurkat cells | Concentration: | 10 μM | Incubation Time: | 6 h | Result: | Effectively induced autophagy by LC3 II induction and p62 reduction. |
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体内研究 (In Vivo) | Apostatin-1 (20 mg/kg, IP, once) inhibits inflammatory responses, and increases survival of systemic inflammation mouse model[1].
Animal Model: | Wild-type mice (n = 10, male, 8 weeks of age, systemic inflammation mouse model)[1] | Dosage: | 20 mg/kg | Administration: | IP, once | Result: | Reduced expression of the TNF-induced inflammatory target gene products, NOS and COXII27, and of inflammatory cytokines in cells stimulated with pathogen-associated molecular patterns, including interferon γ (IFNγ), lipopolysaccharide (LPS), Pam3CSK4 (a synthetic bacterial lipopeptide), and muramyl dipeptide (MDP). Showed increased survival following intravenous delivery of TNF, a mouse model of systemic inflammation. |
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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 | In solvent | -80°C | 6 months | | -20°C | 1 month |
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溶解性数据 | In Vitro: DMSO : 83.33 mg/mL(241.19 mM;ultrasonic and warming and adjust pH to 4 with HCl and heat to 80℃) 配制储备液 1 mM | 2.8944 mL | 14.4718 mL | 28.9436 mL | 5 mM | 0.5789 mL | 2.8944 mL | 5.7887 mL | 10 mM | 0.2894 mL | 1.4472 mL | 2.8944 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 |