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Furamidine dihydrochloride (DB75 dihydrochloride) is a cell-permeable, selective small molecule inhibitor of protein arginine methyltransferase 1 (PRMT1) that also binds preferentially to strings of AT base pair sequences within the minor groove of DNA; it targets the PRMT1 enzyme active site primarily through a competitive mechanism with the protein substrate and is noncompetitive toward the cofactor, ultimately leading to the blockade of cell proliferation in various leukemia cell lines irrespective of their genetic lesions.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $34 | In Stock | |
5 mg | $77 | In Stock | |
10 mg | $135 | In Stock | |
25 mg | $293 | In Stock | |
50 mg | $519 | In Stock | |
100 mg | $893 | In Stock | |
200 mg | $1,180 | In Stock |
Description | Furamidine dihydrochloride (DB75 dihydrochloride) is a cell-permeable, selective small molecule inhibitor of protein arginine methyltransferase 1 (PRMT1) that also binds preferentially to strings of AT base pair sequences within the minor groove of DNA; it targets the PRMT1 enzyme active site primarily through a competitive mechanism with the protein substrate and is noncompetitive toward the cofactor, ultimately leading to the blockade of cell proliferation in various leukemia cell lines irrespective of their genetic lesions. |
Targets&IC50 | Protein arginine methyltransferase 1 (PRMT1):9.4 μM (IC50), PRMT4:>400 µM (IC50), PRMT6:283 µM (IC50), PRMT5:166 µM (IC50) |
In vitro | Furamidine dihydrochloride (20 μM, 72 hours) treatment of leukemia cell lines inhibited cell growth in most leukemia cell lines except HEL cells harboring the JAK2V617F mutation.[6] |
In vivo | Furamidine dihydrochloride (1 mg/kg, intraperitoneal injection, 3 times a week, repeated every 4 weeks for 34 weeks) was used to treat female NZB/NZW mice and was found to suppress proteinuria and prolong the survival of lupus-prone NZB/NZW mice when combined with irinotecan. [5] |
Synonyms | NSC305831 dihydrochloride, NSC 305831 dihydrochloride, DB75 dihydrochloride |
Molecular Weight | 377.27 |
Formula | C18H18Cl2N4O |
Cas No. | 55368-40-6 |
Smiles | N=C(C1=CC=C(C2=CC=C(C3=CC=C(C(N)=N)C=C3)O2)C=C1)N.Cl.Cl |
Relative Density. | no data available |
Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||
Solubility Information | DMSO: 10 mg/mL (26.51 mM), Sonication is recommended. | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
DMSO
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