GSK3326595

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Chemical Structure| 1616392-22-3 同义名 : EPZ015938; Pemrametostat
CAS号 : 1616392-22-3
货号 : A416840
分子式 : C24H32N6O3
纯度 : 99%+
分子量 : 452.55
MDL号 : MFCD29991177
存储条件：

Pure form Keep in dark place, inert atmosphere, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 60 mg/mL(132.58 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
生物活性
描述 PRMT5 is a protein arginine methyltransferase that catalyzes H4R3me2 and H3R8me2. It is active on non-histone substrates, such as p53 and programmed cell death 4, and acts as a transcriptional repressor. GSK3326595 is a potent, selective inhibitor of PRMT5 with an IC50 value of 6.2 ± 0.8 nM[1]. It inhibited tumor growth both in vitro and in animal models[2]. Treatment with GSK3326595 (40 mg/kg from day 10) plus anti-PD1 antibodies (200 μg/mouse at days, 8, 11, 14, 17 and 20) augmented the anti-tumor response, reflected in reduced tumor size in both B16 (Fig. 8E; fig. S10C and S10D) and YUMM1.7 melanoma models[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.21mL

0.44mL

0.22mL

11.05mL

2.21mL

1.10mL

22.10mL

4.42mL

2.21mL
参考文献

[1]Vinet M, Suresh S, Maire V, Monchecourt C, Némati F, Lesage L, Pierre F, Ye M, Lescure A, Brisson A, Meseure D, Nicolas A, Rigaill G, Marangoni E, Del Nery E, Roman-Roman S, Dubois T. Protein arginine methyltransferase 5: A novel therapeutic target for triple-negative breast cancers. Cancer Med. 2019 May;8(5):2414-2428

[2]Dose Escalation Study of GSK3326595 in Participants With Solid Tumors and Non-Hodgkin's Lymphoma (NHL)

[3]Kim H, Kim H, Feng Y, Li Y, Tamiya H, Tocci S, Ronai ZA. PRMT5 control of cGAS/STING and NLRC5 pathways defines melanoma response to antitumor immunity. Sci Transl Med. 2020 Jul 8;12(551):eaaz5683.