GSK3326595 free base · Synonyms: Pemrametostat | EPZ015938

Pemrametostat is an orally active, potent and selective inhibitor of protein arginine methyltransferase 5.

For research use only. Not for human or veterinary use.

Target Bcl-2 Family

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

GSK3326595 structure

CAS No.: 1616392-22-3

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
250 mg	USD 585.00	BP-02339-250mg	In stock	Get quote
500 mg	USD 700.00	BP-02339-500mg	In stock	Get quote
1 g	USD 1,049.00	BP-02339-1g	In stock	Get quote
5 g	USD 3,300.00	BP-02339-5g	In stock	Get quote
10 g	Inquire	BP-02339-10g	In stock	Inquire

Need another size or custom synthesis? Request a quote.

Description

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.

Biological activity

GSK3326595 is a potent, reversible and selective protein arginine methyltransferase 5 (PRMT5) inhibitor with broad antiproliferative activity for studies related to lymphoma and leukemia.

Identifiers

SMILES: CC(=O)N1CCC(CC1)NC1=NC=NC(=C1)C(=O)NC[C@@H](O)CN1CCC2=C(C1)C=CC=C2
InChIKey: JLCCNYVTIWRPIZ-OAQYLSRUSA-N

Specifications

MW (average): 452.5493
Formula: C₂₄H₃₂N₆O₃
CAS No.: 1616392-22-3
Physical state: Solid
Color: White to light yellow
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

In vitro: DMSO : 62.5 mg/mL

Documents

References

[1]. Che Y, et al. Exploiting PRMT5 as a target for combination therapy in mantle cell lymphoma characterized by frequent ATM and TP53 mutations [J]. Blood cancer journal, 2023, 13(1): 27.

[2]. Fedoriw A, et al. Anti-tumor activity of the type I PRMT inhibitor, GSK3368715, synergizes with PRMT5 inhibition through MTAP loss [J]. Cancer cell, 2019, 36(1): 100-114. e25.

[3]. Zhang Y, et al. PRMT5 inhibition induces pro‐inflammatory macrophage polarization and increased hepatic triglyceride levels without affecting atherosclerosis in mice [J]. Journal of Cellular and Molecular Medicine, 2023, 27(8): 1056-1068.

[4]. Li Z, et al. GSK3326595 is a promising drug to prevent SARS-CoV-2 Omicron and other variants infection by inhibiting ACE2-R671 di-methylation [J]. Journal of Medical Virology, 2023, 95(1): e28158.

[5]. Luo Y, et al. Myelocytomatosis-protein arginine N-methyltransferase 5 Axis defines the tumorigenesis and immune response in hepatocellular carcinoma [J]. Hepatology, 2021, 74(4): 1932-1951.

Same target

Search Bcl-2 Family

Same research area

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