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GSK591

Cat. No. M8649
GSK591 Structure
Synonym:

GSK-591; GSK3203591; EPZ015866

Size Price Availability Quantity
5mg USD 130  USD130 In stock
10mg USD 210  USD210 In stock
25mg USD 430  USD430 In stock
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Quality Control
Biological Activity

GSK591 is a SGC probe for PRMT5. GSK591 is a potent and selective inhibitor of H4 histone methylation by PRMT5/MEP50 complex. GSK591 (5 μM; MCF7, T47D, and MCF10A cells) treatment suppresses breast cancer stem cells (BCSCs) proliferation and self-renewal. GSK591 reduces BCSCs numbers in vitro.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 380.48
Formula C22H28N4O2
CAS Number 1616391-87-7
Purity 99.09%
Solubility DMSO 20 mg/mL
Storage at -20°C
References

[1] Jianhao Huang, et al. PRMT5 Promotes EMT Through Regulating Akt Activity in Human Lung Cancer

[2] Liu Yang, et al. PRMT5 functionally associates with EZH2 to promote colorectal cancer progression through epigenetically repressing CDKN2B expression

[3] Patty Sachamitr, et al. PRMT5 inhibition disrupts splicing and stemness in glioblastoma

[4] Yongrong Yan, et al. PRMT5 regulates colorectal cancer cell growth and EMT via EGFR/Akt/GSK3β signaling cascades

[5] Shikui Zhang, et al. Targeting PRMT5/Akt signalling axis prevents human lung cancer cell growth

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  Catalog
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Keywords: GSK591, GSK-591; GSK3203591; EPZ015866 supplier, PRMTs, inhibitors

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