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Chemical Structure| 1616391-87-7 Chemical Structure| 1616391-87-7

Structure of GSK591
CAS No.: 1616391-87-7

Chemical Structure| 1616391-87-7

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GSK591 (EPZ015866) is a potent and selective protein methyltransferase 5 (PRMT5) inhibitor with an IC50 of 4 nM.

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Product Details of GSK591

CAS No. :1616391-87-7
Formula : C22H28N4O2
M.W : 380.48
SMILES Code : O=C(C1=CC(NC2CCC2)=NC=C1)NC[C@H](O)CN3CC4=C(C=CC=C4)CC3
InChI Key :TWKYXZSXXXKKJU-FQEVSTJZSA-N
Pubchem ID :117072552

Safety of GSK591

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of GSK591

epigenetics

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
A549 cells 1 μM 4 days To evaluate the effect of GSK591 on A549 cell proliferation, results showed that GSK591 significantly inhibited the proliferation of A549 cells. PMC6349228
H1299 cells 1 μM 4 days To evaluate the effect of GSK591 on H1299 cell proliferation, results showed that GSK591 significantly inhibited the proliferation of H1299 cells. PMC6349228
HCC827 250 nM 4 days To evaluate the effect of GSK591 on SDMR and PD-L1 expression in HCC827 cells, the results showed that GSK591 significantly reduced SDMR expression and increased PD-L1 expression. PMC8801487
NCI-H460 250 nM 4 days To evaluate the effect of GSK591 on SDMR and PD-L1 expression in NCI-H460 cells, the results showed that GSK591 significantly reduced SDMR expression and increased PD-L1 expression. PMC8801487
normal human astrocytes 1 µM 5 days PRMT5 inhibition had minimal effect on normal human astrocytes. PMC7881162
A549 cells 100 nM 5 days Inhibition of PRMT5 significantly enhanced resveratrol-induced cell apoptosis PMC6923546
ASTC-a-1 cells 100 nM 5 days Inhibition of PRMT5 significantly enhanced resveratrol-induced cell apoptosis PMC6923546
HCT116 cells 100 nM 7 days To evaluate the inhibitory effect of GSK591 on the proliferation of HCT116 cells, the results showed that GSK591 significantly inhibited the proliferation of HCT116 cells. PMC7914347
SW480 cells 100 nM 7 days To evaluate the inhibitory effect of GSK591 on the proliferation of SW480 cells, the results showed that GSK591 significantly inhibited the proliferation of SW480 cells. PMC7914347
HSJD-DIPG-007 1 µM 7 days GSK591 significantly reduced the viability of HSJD-DIPG-007 cells, demonstrating inhibition of PRMT5. PMC10764357
GBM stem cells 0.1–1 µM 9–12 days Pharmacological inhibition of PRMT5 significantly suppresses the growth of GBM stem cells, with the proneural subtype showing greater sensitivity. PMC7881162
LLC 1 µM different time points To evaluate the effect of GSK591 on CD274 mRNA and PD-L1 protein expression in LLC cells, the results showed that PD-L1 mRNA and protein expression increased at 1 μM in a time-dependent manner. PMC8801487

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Nude mice HCT116 xenograft model Intraperitoneal injection 2.5 mg/kg Every other day for one month To evaluate the inhibitory effect of GSK591 on the tumor growth of HCT116 xenograft models, the results showed that GSK591 significantly inhibited tumor growth. PMC7914347
Nude mice subcutaneous LLC tumor model intraperitoneal injection 50 mg/kg once daily for 12 days To evaluate the effect of GSK591 on CD274 and PD-L1 expression in subcutaneous LLC tumors in nude mice, the results showed that GSK591 significantly reduced tumor weight and volume and increased PD-L1 expression. PMC8801487
Nude mice HSJD-DIPG-007 brainstem xenograft model Oral gavage 50 mg/kg 3 days on, 4 days off, for 4 weeks GSK591 did not extend survival in the HSJD-DIPG-007 brainstem xenograft model in vivo, but it reduced the infiltration of tumor cells into the mouse forebrain. PMC10764357

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.63mL

0.53mL

0.26mL

13.14mL

2.63mL

1.31mL

26.28mL

5.26mL

2.63mL

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