Autogramin-2

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Chemical Structure| 2375541-45-8 同义名 : -
CAS号 : 2375541-45-8
货号 : A1339705
分子式 : C21H27N3O4S
纯度 : 99%+
分子量 : 417.522
MDL号 : MFCD32174286
存储条件：

Pure form Sealed in dry,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 85 mg/mL(203.58 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Autophagy is a catabolic process aimed at recycling cellular components and damaged organelles in response to diverse conditions of stress, such as nutrient deprivation, viral infection and genotoxic stress. Autophagy mediates the degradation of damaged proteins, organelles and pathogens, and plays a key role in health and disease[1]. Autogramin-2 potently inhibits autophagy induced by either starvation (IC50=0.27 μM) or mTORC1 inhibition (Rapamycin; IC50=0.14 μM).The PH-GRAM construct alone did not transfer cholesterol. The StART domains of GRAMD1B and GRAMD1C also transferred cholesterol, but this could not be inhibited by autogramin-2 or was only inhibited to a minor extent. Autogramin-2 did not compete with binding of 22-NBD-cholesterol to GRAMD1B or GRAMD1C, further confirming its selectivity for GRAMD1A.Autogramins selectively target the recently discovered cholesterol transfer protein GRAM domain-containing protein 1A (GRAMD1A, which had not previously been implicated in autophagy), and directly compete with cholesterol binding to the GRAMD1A StART domain. The positive control 25-hydroxycholesterol was able to compete with binding of 22-NBD-cholesterol to all three GRAMD1 proteins, while no oxysterols hydroxylated in the A- or B-ring were able to compete.GRAMD1A accumulates at sites of autophagosome initiation, affects cholesterol distribution in response to starvation and is required for autophagosome biogenesis. in the presence of 25-hydroxycholesterol or autogramin-2, hydrogen–deuterium exchange was reduced for amino acids 397–405, 426–440, 464–473 and 507–529[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.40mL

0.48mL

0.24mL

11.98mL

2.40mL

1.20mL

23.95mL

4.79mL

2.40mL
参考文献

[1] G Filomeni, D De Zio, F Cecconi. Oxidative stress and autophagy: the clash between damage and metabolic needs. Cell Death Differ. 2015 Mar;22(3):377-88.

[2] Laraia L, et al. The cholesterol transfer protein GRAMD1A regulates autophagosome biogenesis. Nat Chem Biol. 2019 Jul;15(7):710-720.