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GSK3326595

Cat. No. M9420
GSK3326595 Structure
Synonym:

EPZ015938; GSK-3326595

Size Price Availability Quantity
5mg USD 40  USD40 In stock
10mg USD 67  USD67 In stock
50mg USD 227  USD227 In stock
100mg USD 397  USD397 In stock
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Quality Control & Documentation
Biological Activity

GSK3326595 is a potent, selective, reversible inhibitor of protein arginine methyltransferase 5 (PRMT5) with an IC50 of 6.2 nM.

Chemical Information
Molecular Weight 452.55
Formula C24H32N6O3
CAS Number 1616392-22-3
Solubility (25°C) DMSO ≥ 25 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Yuhong Luo, et al. Hepatology. MYC-Protein Arginine Methyltransferase 5 Axis Defines the Tumorigenesis and Immune Response in Hepatocellular Carcinoma

[2] Hyungsoo Kim, et al. Sci Transl Med. PRMT5 control of cGAS/STING and NLRC5 pathways defines melanoma response to antitumor immunity

[3] Shatha AbuHammad, et al. Proc Natl Acad Sci U S A. Regulation of PRMT5-MDM4 axis is critical in the response to CDK4/6 inhibitors in melanoma

[4] Hong Lin, et al. Bioorg Med Chem Lett. Nucleoside protein arginine methyltransferase 5 (PRMT5) inhibitors

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  Catalog
Abmole Inhibitor Catalog




Keywords: GSK3326595, EPZ015938; GSK-3326595 supplier, PRMTs, inhibitors, activators

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