Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
1 mg
5 mg
10 mg
1 mM
2.9210 mL
14.6049 mL
29.2099 mL
5 mM
0.5842 mL
2.9210 mL
5.8420 mL
10 mM
0.2921 mL
1.4605 mL
2.9210 mL
50 mM
0.0584 mL
0.2921 mL
0.5842 mL
Description
LLY-283 is a novel and selective inhibitor of . LLY-283 inhibits PRMT5 enzymatic activity in vitro and in cells with IC50 of 22 nM and 25 nM, respectively. LLY-283 shows antitumor activity.
LLY-283 inhibits PRMT5 enzymatic activity in vitro and in cells with IC50 of 22 ± 3 and 25 ± 1 nM, respectively. LLY-283 directly binds to and occupies the SAM pocket. LLY-283 is a low nanomolar enzymatic inhibitor of the PRMT5:MEP50 complex in biochemical assays and is selective for PRMT5 over other methyltransferases including related family members.
In vivo
LLY-283 shows antitumor activity in mouse xenografts when dosed orally and can serves as an excellent probe molecule for understanding the biological function of PRMT5 in normal and cancer cells. LLY-283 can be used as an in vivo tool compound to evaluate the pharmacology of PRMT5 inhibition.
