Merck SGC8158

SGC8158

≥98% (HPLC)

5′-S-[4-[(4′-Chlorobiphenyl-3-ylmethyl)amino]butyl]-5′-thioadenosine

Quality Level

100

assay

≥98% (HPLC)

form

powder

색상

white to beige

solubility

DMSO: 2 mg/mL, clear

저장 온도

2-8°C

SMILES string

ClC(C=C1)=CC=C1C2=CC(CNCCCCSC[C@H]3O[C@@H](N(C=N4)C5=C4C(N)=NC=N5)[C@H](O)[C@@H]3O)=CC=C2

SGC8158 isthe active component produced by cell reductases from the prodrug, SGC3027, a selective and cell-active inhibitor of protein arginine N-methyltransferase (PRMT7). SGC8158 was shown to inhibit PRMT7 with an IC50 value < 2.5 nM for methylation of H2B (23-37) and greater than 40-fold selectivity over other histone methyltransferases and non-epigenetic targets. SGC3027 inhibited the methylation of HSP70 In cellular assays using C2C12 cells with an IC50 value of 1.3 microM. The closely related SGC3027N is significantly less active in the cellular assay, and is a control compound for cellular studies.