C-7280948

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Chemical Structure| 587850-67-7 同义名 : -
CAS号 : 587850-67-7
货号 : A336868
分子式 : C14H16N2O2S
纯度 : 99%+
分子量 : 276.35
MDL号 : MFCD03716650
存储条件：

Pure form Keep in dark place, inert atmosphere, room temperature

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

DMSO: 40 mg/mL(144.74 mM)，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
生物活性
描述 The protein arginine methyltransferase 1 (PRMT1) is implicated in the activation of sexual hormone receptors and therefore could be a potential therapeutic target for hormone-dependent cancers. C-7280948 is a potent PRMT1 inhibitor with an IC50 value of 12.75 ± 2.88μM for human PRMT1 with residues 1–21 of human histone H4 as methylation substrates.[2] The IC50 value of C-7280948 for human PRMT1 with non-histone protein Npl3 as methylation substrates is 26.7 ± 3.5μM.[3]
作用机制 C-7280948 is a potent and selective inhibitor of PRMT1.[2]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.62mL

0.72mL

0.36mL

18.09mL

3.62mL

1.81mL

36.19mL

7.24mL

3.62mL
参考文献

[1]Bissinger EM, Heinke R, et al. Acyl derivatives of p-aminosulfonamides and dapsone as new inhibitors of the arginine methyltransferase hPRMT1. Bioorg Med Chem. 2011 Jun 15;19(12):3717-31.

[2]Heinke R, Spannhoff A, Meier R, Trojer P, Bauer I, Jung M, Sippl W. Virtual screening and biological characterization of novel histone arginine methyltransferase PRMT1 inhibitors. ChemMedChem. 2009 Jan;4(1):69-77

[3]Bissinger EM, Heinke R, Spannhoff A, Eberlin A, Metzger E, Cura V, Hassenboehler P, Cavarelli J, Schüle R, Bedford MT, Sippl W, Jung M. Acyl derivatives of p-aminosulfonamides and dapsone as new inhibitors of the arginine methyltransferase hPRMT1. Bioorg Med Chem. 2011 Jun 15;19(12):3717-31