For research use only. Not for therapeutic Use.
PRMT5 IN-1 hydrochloride (compound 9), a hemiaminal, is a potent, selective protein arginine methyltransferase 5 (PRMT5) inhibitor with an IC50 of 11 nM for PRMT5/MEP50. PRMT5 IN-1 hydrochloride can be converted to aldehydes and react with C449 to form covalent adducts under physiological conditions[1].
PRMT5 IN-1 (compound 9; 0-500 nM) hydrochlorideinhibits the PRMT5/MEP50 complex [Kinact/KI=1.2×105 M-1 min-1] very rapidly with a Kinact of 0.068 min-1 and a good binding affinity (KI=55 nM)[1].
PRMT5 IN-1 (0-1000 nM; 3 d; Granta-519 cells) hydrochloride inhibits the expression of cellular sDMA with an IC50 value of 0.012 μM[1].
PRMT5 IN-1 (0-1 μM; 10 d; Granta-519 cells) hydrochloride inhibits cell proliferation in a dose-dependent manner with an IC50 value of 0.06 μM[1].
| Catalog Number | I042849 |
| Synonyms | (2R,3S,4R,5R)-2-[(R)-(4-chlorophenyl)-hydroxymethyl]-5-(5-hydroxy-3,6,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1(9),2,7,11-tetraen-10-yl)oxolane-3,4-diol;hydrochloride |
| Molecular Formula | C19H20Cl2N4O5 |
| Purity | ≥95% |
| InChI | InChI=1S/C19H19ClN4O5.ClH/c20-10-3-1-9(2-4-10)13(26)16-14(27)15(28)19(29-16)23-6-5-11-17-21-7-12(25)24(17)8-22-18(11)23;/h1-6,8,12-16,19,25-28H,7H2;1H/t12?,13-,14+,15-,16-,19-;/m1./s1 |
| InChIKey | OREUSXWUJCVJDC-DEPNVVRZSA-N |
| SMILES | C1C(N2C=NC3=C(C2=N1)C=CN3C4C(C(C(O4)C(C5=CC=C(C=C5)Cl)O)O)O)O.Cl |
| Reference | [1]. Lin H, et, al. Discovery of Potent and Selective Covalent Protein Arginine Methyltransferase 5 (PRMT5) Inhibitors. ACS Med Chem Lett. 2019 May 22;10(7):1033-1038. |
