产品说明书

PF-9366

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Chemical Structure| 72882-78-1 同义名 : -
CAS号 : 72882-78-1
货号 : A186389
分子式 : C20H19ClN4
纯度 : 99%+
分子量 : 350.845
MDL号 : MFCD31630724
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 9 mg/mL(25.65 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 Methionine adenosyltransferase 2A (Mat2A) is responsible for the biosynthesis of S-adenosyl-L-methionine (SAM), an enzyme cofactor required for transmethylation reactions and polyamine biosynthesis. PF-9366 is an allosteric inhibitor of Mat2A with an IC50 value of 420±50nM. Pre-incubation of Mat2A with increasing concentrations of Mat2B (0–100nM) reduced the inhibitory effect of PF-9366 in a dose-dependent manner. PF-9366 inhibited SAM production in H520 cells with an IC50 value of 1.2μM. The IC50 of PF-9366 in H520 cells with Mat2B knockdown was 0.86mM. Six-hour exposure of PF-9366 inhibited SAM synthesis in Huh-7 cells with an IC50 value of 225nM[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.85mL

0.57mL

0.29mL

14.25mL

2.85mL

1.43mL

28.50mL

5.70mL

2.85mL
参考文献

[1]Quinlan CL, Kaiser SE, et al. Targeting S-adenosylmethionine biosynthesis with a novel allosteric inhibitor of Mat2A. Nat Chem Biol. 2017 May 29.

[2]Quinlan CL, Kaiser SE, Bolaños B. et al. Targeting S-adenosylmethionine biosynthesis with a novel allosteric inhibitor of Mat2A. Nat Chem Biol. 2017 Jul;13(7):785-792.