AMI-1 free acid

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Chemical Structure| 134-47-4 同义名 : AMI-1; free acid; Urea J Acid
CAS号 : 134-47-4
货号 : A221541
分子式 : C21H16N2O9S2
纯度 : 95%
分子量 : 504.49
MDL号 : MFCD00035715
存储条件：

Pure form Sealed in dry, room temperature

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

DMSO: 85 mg/mL(168.49 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
生物活性
描述 The protein arginine N-methyltransferases (PRMTs) are a group of enzymes that monomethylate or dimethylate the arginine side chains. AMI-1 free acid is a potent and cell-permeable PRMT inhibitor with IC50 values of 8.81μM and 3.03μM for PRMT1 and Hmt1p, respectively. It is also a selective HIV-1 reverse transcriptase inhibitor. AMI-1 at a concentration of 2 - 10μM inhibited Npl3 methylation in Hela cells. AMI-1 also inhibited arginine methylation of the endogenously methylated protein, Sam68[5]. AMI-1 inhibited the viability of S180 and U2OS cells with IC50 values of 0.31 ± 0.01mM and 0.75 ± 0.02mM, respectively. In mice inoculated with S180 cells, treatment with 0.5mg AMI-1 for 7 days significantly decreased tumor weight compared to the vehicle-treated controls. AMI-1 treatment also significantly downregulated the expression of PRMT5 and decreased the levels of H4R3me2s and H3R8me2s in mice implanted with S180 cells[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.98mL

0.40mL

0.20mL

9.91mL

1.98mL

0.99mL

19.82mL

3.96mL

1.98mL
参考文献

[1]Donghang Cheng, et al. Small Molecule Regulators of Protein Arginine Methyltransferases. J Biol Chem. 2004 Jun 4;279(23):23892-9.

[2]Zhang, B., et al. Targeting protein arginine methyltransferase 5 inhibits colorectal cancer growth by decreasing arginine methylation of eIF4E and FGFR3. Oncotarget. 2015 Sep 8;6(26):22799-811.

[3]Donghang Cheng, et al. Small Molecule Regulators of Protein Arginine Methyltransferases. J Biol Chem. 2004 Jun 4;279(23):23892-9.

[4]Baolai Zhang, et al. Arginine Methyltransferase inhibitor-1 Inhibits Sarcoma Viability in vitro and in vivo. Oncol Lett. 2018 Aug;16(2):2161-2166.

[5]Cheng D, Yadav N, King RW, Swanson MS, Weinstein EJ, Bedford MT. Small molecule regulators of protein arginine methyltransferases. J Biol Chem. 2004 Jun 4;279(23):23892-9

[6]Zhang B, Chen X, Ge S, Peng C, Zhang S, Chen X, Liu T, Zhang W. Arginine methyltransferase inhibitor-1 inhibits sarcoma viability in vitro and in vivo. Oncol Lett. 2018 Aug;16(2):2161-2166