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产品名称 | Transferase ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Tipifarnib |
+++
FTase, IC50: 0.6 nM |
99%+ | |||||||||||||||||
Tolcapone |
+
COMT, Ki: 30 nM |
99%+ | |||||||||||||||||
Lonafarnib |
+++
H-ras, IC50: 1.9 nM K-ras-4B, IC50: 2.8 nM |
99%+ | |||||||||||||||||
(E)-Daporinad |
++++
NMPRTase, Ki: 0.4 nM |
99%+ | |||||||||||||||||
FTI-277 HCl |
++++
FTase, IC50: 500 pM |
98% | |||||||||||||||||
A 922500 |
++
mouse DGAT-1, IC50: 24 nM human DGAT-1, IC50: 7 nM |
98% | |||||||||||||||||
Lomeguatrib |
++
O6-alkylguanine-DNA-alkyltransferas, IC50: 5 nM |
99%+ | |||||||||||||||||
PF-04620110 |
+
DGAT1, IC50: 19 nM |
98% | |||||||||||||||||
LB42708 |
+++
FTase (N-ras), IC50: 1.2 nM FTase (K-Ras), IC50: 0.8 nM |
98% | |||||||||||||||||
GGTI298 Trifluoroacetate | ✔ | 98%+ | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
靶点 |
|
描述 | The mammalian protein arginine methyltransferases are a group of nine enzymes that perform NG-mono methylation-, asymmetric-, or symmetric dimethylation of arginine residues on a range of nuclear and cytoplasmic protein substrates. Protein arginine methyltransferase-5 (PRMT5) is one member of this group which catalyzes the transfer of up to two methyl groups to arginine residues, forming ω-NG-monomethyl arginine and symmetrical ω-NG-dimethyl arginine on protein substrates[3]. EPZ015666 (GSK3235025) is an orally available inhibitor of PRMT5 enzymatic activity with IC50 of 22 nM[4]. SCID mice bearing subcutaneous mantle cell lymphoma cell lines Z-138 and Maver-1 xenografts were orally given EPZ015666 on four doses: 25, 50, 100 and 200 mg/kg twice daily. Dosing at 200 mg/kg induced tumor stasis in Z-138 cells, with >93% tumor-growth inhibition (TGI) after 21 d, whereas Maver-1 cells showed >70% TGI[4]. EPZ0156660 (0 to 10 uM) dose-dependently inhibited the proliferation of multiple myeloma cell lines[5]. EPZ015666 at 5 uM also inhibited growth in patient multiple myeloma (pMM) cells cultured on a BMSCs monolayer, and also induced apoptosis of pMM cells within bone marrow mononuclear cell cultures[5]. 10 uM -EPZ treatment significantly suppressed the proliferation of several human glioblastoma cell lines: GI261, T98G, U-87 MG and A172, with loss of active S phase cells and accumulation of G2/M populations, but did not induce apoptosis[6]. |
作用机制 | EPZ015666 binds in the peptide-binding site of PRMT5, including in the pocket occupied by the substrate arginine side chain. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.61mL 0.52mL 0.26mL |
13.04mL 2.61mL 1.30mL |
26.08mL 5.22mL 2.61mL |
CAS号 | 1616391-65-1 |
分子式 | C20H25N5O3 |
分子量 | 383.444 |
别名 | GSK3235025 |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Keep in dark place,Inert atmosphere,2-8°C |
溶解度 |
DMSO: 105 mg/mL(273.83 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 |
动物实验配方 |
2% DMSO+30% PEG 300+water 5 mg/mL |