[CAS NO. 134-47-4] AMI-1freeacid

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PRODUCTS SPECIFICATIONS [134-47-4]

Catalog

HY-18962A

Brand

MCE

CAS

134-47-4

DESCRIPTION [134-47-4]

Overview

MDL	MFCD00035715
Molecular Weight	504.49
Molecular Formula	C21H16N2O9S2
SMILES	O=C(NC1=CC2=CC(S(=O)(O)=O)=CC(O)=C2C=C1)NC3=CC4=CC(S(=O)(O)=O)=CC(O)=C4C=C3

For research use only. We do not sell to patients.

Summary

AMI-1 free acid is a potent, cell-permeable and reversible inhibitor of protein arginine N-methyltransferases (PRMTs) , with IC ₅₀ s of 8.8 μM and 3.0 μM for human PRMT1 and yeast-Hmt1p, respectively. AMI-1 free acid exerts PRMTs inhibitory effects by blocking peptide-substrate binding ^[1] .

IC50 & Target

IC50: 8.8 μM (PRMT1), 3.0 μM (yeast-Hmt1p) ^[1]

In Vitro

AMI-1 free acid can inhibit the in vitro methylation reactions performed by all five recombinantly active PRMTs (PRMT1, -3, -4, and -6 and Hmt1p) ^[2] .
AMI-1 free acid not only inhibits type I PRMTs (PRMT1, 3, 4 and 6) but also type II PRMT5 ^[2] .
AMI-1 free acid specifically inhibits arginine, but not lysine, methyltransferase activity in vitro and does not compete for the AdoMet binding site ^[3] .
AMI-1 free acid inhibits methylation of GFP-Npl3 and cellular proteins ^[3] .
AMI-1 free acid (0.6-2.4 mM; 48-96 hours) inhibits the cell viability of sarcoma in S180 and U2OS cells in a time-dependent and dose-dependent manner in vitro ^[4] .
AMI-1 free acid (1.2-2.4 mM; 48-72 hours) reduces S180 cell viability through the induction of cell apoptosis ^[4] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay ^[4]

Cell Line:	S180 cells, U2OS cells
Concentration:	0.6 mM, 1.2 mM, 2.4 mM
Incubation Time:	48 hours, 72 hours, 96 hours
Result:	Inhibited the cell viability.

Apoptosis Analysis ^[4]

Cell Line:	S180 cells
Concentration:	1.2 mM, 2.4 mM
Incubation Time:	48 hours, 72 hours
Result:	Increased the percentages of cells undergoing apoptosis.

In Vivo

AMI-1 free acid (0.5 mg; intratumorally; daily; for 7 days) inhibits S180 viability in vivo ^[4] .
AMI-1 free acid (0.5 mg; intratumorally; daily; for 7 days) downregulates PRMT5 but does not regulate the expression of PRMT7 in a tumor xenograft model ^[4] .
AMI-1 free acid (0.5 mg; intratumorally; daily; for 7 days) decreases the levels of H4R3me2s and H3R8me2s in a tumor xenograft model ^[4] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	6-7 weeks old male Kunming mice (18-22 g), with S180 cells xenograft ^[4]
Dosage:	0.5 mg
Administration:	Intratumorally, daily, for 7 days
Result:	Decreased tumor weight.

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 83.33 mg/mL ( 165.18 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.9822 mL	9.9110 mL	19.8220 mL
5 mM	0.3964 mL	1.9822 mL	3.9644 mL
10 mM	0.1982 mL	0.9911 mL	1.9822 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.08 mg/mL (4.12 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.08 mg/mL (4.12 mM); Clear solution

* All of the co-solvents are available by MCE.

References

Synonyms

2-Naphthalenesulfonic acid, 7,7′-(carbonyldiimino)bis[4-hydroxy-

2-Naphthalenesulfonic acid, 7,7′-ureylenebis[4-hydroxy-

1-Naphthol-3-sulfonic acid, 6,6′-ureylenebis-

7,7′-(Carbonyldiimino)bis[4-hydroxy-2-naphthalenesulfonic acid]

I Acid Urea

J acid urea

N,N′-Bis[1-oxy-3-sulfonaphthyl(6)]urea

N,N′-Bis[1-hydroxy-3-sulfonaphthyl(6)]urea

N,N′-Bis(7-sulfo-5-hydroxy-2-naphthyl)urea

N,N′-Bis(5-hydroxy-7-sulfo-2-naphthyl)urea

6,6′-Ureylenebis(1-naphthol-3-sulfonic acid)

Urea J Acid

7,7′-Ureylenebis(4-hydroxy-2-naphthalenesulfonic acid)

Scarlet Acid

5,5′-Dihydroxy-2,2′-dinaphthylcarbamide-7,7′-disulfonic acid

Carbonyl J

NSC 1699

NSC 45174