PRMT5-IN-1

PRMT5 IN-1, a hemiaminal, is a potent, selective protein arginine methyltransferase 5 (PRMT5) inhibitor with an IC50 of 11 nM for PRMT5/MEP50. PRMT5 IN-1 can be converted to aldehydes and react with C449 to form covalent adducts under physiological conditions[1].

Product Specifications

CAS Number

[2366149-83-7]

UNSPSC

12352005

Target

Histone Methyltransferase

Type

Reference compound

Related Pathways

Epigenetics

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/prmt5-in-1.html

Solubility

10 mM in DMSO

Smiles

O[C@@H]1[C@@H]([C@@H](C2=CC=C(Cl)C=C2)O)O[C@@H](N3C=CC4=C3N=CN5C4=NCC5O)[C@@H]1O

Molecular Formula

C19H19ClN4O5

Molecular Weight

418.83

References & Citations

[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.