A PRMT4 inhibitor (IC50 = 6 nM); decreases asymmetric methylation of PABP1 (IC50 = 0.038 µM) and increases levels of demethylated SmB (EC50 = 0.018 µM) in RPMI-8226 multiple myeloma cells; inhibits proliferation in a panel of 36 hematopoietic cancer cell lines (IC50s =

EZM2302 – 1 mg

Brand:
Cayman
CAS:
1628830-21-6
Storage:
-20
UN-No:
Non-Hazardous - /

EZM2302 is an inhibitor of protein arginine methyltransferase 4 (PRMT4; IC50 = 6 nM).{53436} It decreases asymmetric methylation of the PRMT4 substrate PABP1 (IC50 = 0.038 µM) and increases levels of demethylated SmB (EC50 = 0.018 µM) in RPMI-8226 multiple myeloma cells. EZM2302 inhibits proliferation in a panel of 36 hematopoietic cancer cell lines, with IC50 values of less than 100 μM for nine of the 15 multiple myeloma cell lines included in the panel. It reduces tumor growth and decreases asymmetric PABP1 methylation in tumor tissue in an RPMI-8226 mouse xenograft model when administered at doses of 75, 150, and 300 mg/kg twice per day. Intrathecal injection of EZM2302 (10 µg) reduces acute mechanical allodynia and thermal hyperalgesia in a mouse model of neuropathic pain induced by chronic constriction injury (CCI).{53437}  

 

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SKU: 29954 - 1 mg Category:

Description

A PRMT4 inhibitor (IC50 = 6 nM); decreases asymmetric methylation of PABP1 (IC50 = 0.038 µM) and increases levels of demethylated SmB (EC50 = 0.018 µM) in RPMI-8226 multiple myeloma cells; inhibits proliferation in a panel of 36 hematopoietic cancer cell lines (IC50s = <100 µM for 9 out of 15 multiple myeloma cell lines); reduces tumor growth and decreases asymmetric PABP1 methylation in tumor tissue in an RPMI-8226 mouse xenograft model at 75, 150, and 300 mg/kg twice per day; reduces acute mechanical allodynia and thermal hyperalgesia in a mouse model of CCI-induced neuropathic pain at 10 µg

Formal name: 2-[2-[2-chloro-5-[(2R)-2-hydroxy-3-(methylamino)propoxy]phenyl]-6-(3,5-dimethyl-4-isoxazolyl)-5-methyl-4-pyrimidinyl]-2,7-diazaspiro[3.5]nonane-7-carboxylic acid, methyl ester

Synonyms:  GSK3359088

Molecular weight: 585.1

CAS: 1628830-21-6

Purity: ≥98%

Formulation: A solid

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