| S8479 |
LLY-284 |
LLY-284 is the diastereomer of LLY-283, which is a potent and selective SAM-competitive chemical probe for PRMT5. LLY-284 is much less active than LLY-283 and can be used as a negative control for LLY-283. |
Selective |
|
| S8664 |
Pemrametostat (GSK3326595) |
Pemrametostat (GSK3326595, EPZ015938) is an orally active, potent and selective inhibitor of protein arginine methyltransferase 5 (PRMT5) and potently inhibits tumor growth in vitro and in vivo in animal models. |
Selective |
|
| S8624 |
Onametostat (JNJ-64619178) |
Onametostat (JNJ-64619178) is a PRMT5 inhibitor with high selectivity and potency (subnanomolar range, PRMT5-MEP-50 IC50=0.14 nM) under different in vitro and cellular conditions, paired with favorable pharmacokinetics and safety properties.
|
Selective |
PRMT5, IC50: 0.14 nM |
| S8111 |
GSK591 |
GSK591 (EPZ015866, GSK3203591) is a potent selective inhibitor of the arginine methyltransferase PRMT5 with IC50 of 4 nM. |
Selective |
PRMT5, IC50: 4 nM |
| S7748 |
EPZ015666 (GSK3235025) |
EPZ015666 (GSK3235025) is a potent, selective and orally bioavailable PRMT5 inhibitor with Ki of 5 nM, >20,000-fold selectivity over other PMTs.
|
Selective |
PRMT5, Ki: 5 nM |
| S8883 |
LLY-283 |
LLY-283 is a novel and selective inhibitor of protein arginine methyltransferase 5 (PRMT5). 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. |
Selective |
PRMT5, IC50: 22 nM; PRMT5, IC50: 25 nM |
| S8209 |
HLCL-61 HCL |
HLCL-61 hydrochloride is a potent and selective PRMT5 inhibitor for the treatment of acute myeloid leukemia. |
Selective |
PRMT5, IC50: 16.74 μM |
