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Apostatin-1
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Apostatin-1图片
CAS NO:2559703-06-7
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品名称
Apt-1
产品介绍
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RIPK1beclin 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.
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.
分子量

345.50

性状

Solid

Formula

C19H27N3OS

CAS 号

2559703-06-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
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
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.8944 mL14.4718 mL28.9436 mL
5 mM0.5789 mL2.8944 mL5.7887 mL
10 mM0.2894 mL1.4472 mL2.8944 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。