XY1 is a negative control of SGC 707 which works as a potent and selective allosteric inhibitor of PRMT3, while XY1 shows almost no activity.
规格 | 价格 | 会员价 | 库存 | 数量 | |||
---|---|---|---|---|---|---|---|
{[ item.pr_size ]} |
{[ getRatePrice(item.pr_rmb, 1,1) ]} {[ getRatePrice(item.pr_rmb_sale, 1,1) ]} |
{[ getRatePrice(item.pr_rmb, 1,1) ]} {[ getRatePrice(item.pr_rmb,item.pr_rate,1) ]} |
{[ getRatePrice(item.pr_rmb, 1,1) ]} | {[ getRatePrice(item.pr_rmb_sale, 1,1) ]} {[ getRatePrice(item.pr_rmb,item.pr_rate,item.mem_rate) ]} {[ getRatePrice(item.pr_rmb,1,item.mem_rate) ]} | 现货 | 咨询 | - + |
快速发货 顺丰冷链运输,1-2 天到达
品质保证
技术支持
免费溶解
产品名称 | Histone Methyltransferase ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
BRD4770 | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
UNC1999 |
+++
EZH2, IC50: 2 nM EZH1, IC50: 45 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
EPZ005687 |
++
EZH2, Ki: 24 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
EPZ015666 |
+++
PRMT5, Ki: 5 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
3-Deazaneplanocin A HCl |
++++
S-adenosylhomocysteine hydrolase, Ki: 50 pM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
EPZ6438 |
+++
EZH2, IC50: 11 nM EZH2, Ki: 2.5 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
GSK126 |
++
EZH2, IC50: 9.9 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
MI-3 |
+
Menin-MLL, IC50: 648 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
MM-102 |
++
MLL1, IC50: 0.4 μM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
EI1 |
++
Ezh2 (wild-type), IC50: 15 nM EZH2 (Y641F), IC50: 13 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
SGC0946 |
++++
DOT1L, IC50: 0.3 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
PFI-2 HCl |
++++
SETD7, IC50: 2 nM SETD7, Ki: 0.33 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Pinometostat |
++++
DOT1L, Ki: 80 pM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
EPZ004777 |
+++
DOT1L, IC50: 0.4 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Entacapone |
++
COMT, IC50: 151 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
UNC0379 |
+
SETD8, IC50: 7.9 μM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Menin-MLL inhibitor MI-2 |
+
Menin-MLL, IC50: 446 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
GSK343 |
+++
EZH2, IC50: 4 nM EZH1, IC50: 240 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
BIX-01294 3HCl |
+
G9a, IC50: 2.7 μM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
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。 |
描述 | Protein arginine N-methyltransferase 3 (PRMT3) is a cytoplasmic enzyme that utilizes S-adenosyl-L-methionine (AdoMet) to methylate specific proteins, most of which contain GAR (glycine-arginine rich) motifs. PRMT3 has been shown to play a role in the proper maturation of the 80S ribosome by binding to and catalyzing the methylation of rpS2, a component of the 40S ribosomal subunit[2]. The expression of lipogenic proteins was increased by PRMT3 overexpression, but decreased by PRMT3 silencing and use of the PRMT3 knockout (KO) mouse embryonic fibroblast cell line. PRMT3 also increased the transcriptional activity of LXRα by directly binding with LXRα in a methylation-independent manner[3]. In cells, PRMT3 overexpression triggered metabolic reprogramming and enhanced glycolysis and mitochondrial respiration simultaneously in a glyceraldehyde-3-phosphate dehydrogenase (GAPDH)-dependent manner. PRMT3-overexpressing cancer cells were addicted to GAPDH-mediated metabolism and sensitive to the inhibition of GAPDH and mitochondrial respiration. The combination of inhibitors of GAPDH and oxidative phosphorylation induced a synergistic inhibition on cellular growth in vitro and in vivo[4]. XY1 is a very close analogue of SGC707 (a potent, selective, and non-competitive inhibitor of PRMT3 with IC50 of 31 nM), but XY1 is completely inactive against PRMT3 at concentrations as high as 100 μM. XY1 contains a naphthyl group replacing the isoquinoline group, lacks the key hydrogen bond with T466. The naphthyl ring of XY1 could act as a weak hydrogen-bond acceptor, but this should come with a substantial enthalpic penalty. The more than 1000-fold potency loss of XY1 compared with SGC707 supports this analysis. SGC707 and XY1 are a pair of excellent tools for the biomedical community to further elucidate biological functions and disease associations of PRMT3[5]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
3.36mL 0.67mL 0.34mL |
16.82mL 3.36mL 1.68mL |
33.63mL 6.73mL 3.36mL |
CAS号 | 1624117-53-8 |
分子式 | C17H19N3O2 |
分子量 | 297.352 |
别名 | |
运输 | 蓝冰 |
存储条件 |
粉末 Sealed in dry,Store in freezer, under -20°C 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 65 mg/mL(218.6 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 |