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产品名称 | Histone Methyltransferase ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
BRD4770 | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
UNC1999 |
+++
EZH1, IC50: 45 nM EZH2, IC50: 2 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, Ki: 2.5 nM EZH2, IC50: 11 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, Ki: 0.33 nM SETD7, IC50: 2 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 |
+++
EZH1, IC50: 240 nM EZH2, IC50: 4 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 | AZ505 is highly selective and shows an activity at submicromolar concentrations in vitro. The IC50 value of AZ505 against SMYD2 is 0.12 μM, representing a >600-fold difference compared to its IC50 values against other histone methyltransferases, such as SMYD3 (IC50>83.3 μM), DOT1L (IC50>83.3 μM), and EZH2 (IC50>83.3 μM) [1]. AZ505 functions as a potent and selective inhibitor of SMYD2, with an IC50 of 0.12 μM. The human SMYD (SET and MYND domain-containing protein) family comprises five members (SMYD1-5). Additionally, AZ505 does not inhibit the enzymatic activities of a range of protein lysine methyltransferases. AZ505 has been proposed for an isothermal titration calorimetry (ITC) binding study, with a Kd value of 0.5 μM. Conversely, the calculated Kd for the p53 substrate peptide is 3.7 μM. The interaction between AZ505 and SMYD2 is primarily governed by entropy, implying that binding is predominantly facilitated by hydrophobic interactions with minimal specific hydrogen bonding [2]. |
体外研究 | AZ505 is highly selective and shows an activity at submicromolar concentrations in vitro. The IC50 value of AZ505 against SMYD2 is 0.12 μM, representing a >600-fold difference compared to its IC50 values against other histone methyltransferases, such as SMYD3 (IC50>83.3 μM), DOT1L (IC50>83.3 μM), and EZH2 (IC50>83.3 μM) [1]. AZ505 functions as a potent and selective inhibitor of SMYD2, with an IC50 of 0.12 μM. The human SMYD (SET and MYND domain-containing protein) family comprises five members (SMYD1-5). Additionally, AZ505 does not inhibit the enzymatic activities of a range of protein lysine methyltransferases. AZ505 has been proposed for an isothermal titration calorimetry (ITC) binding study, with a Kd value of 0.5 μM. Conversely, the calculated Kd for the p53 substrate peptide is 3.7 μM. The interaction between AZ505 and SMYD2 is primarily governed by entropy, implying that binding is predominantly facilitated by hydrophobic interactions with minimal specific hydrogen bonding [2]. |
作用机制 | AZ505 is a substrate competitive inhibitor which can bound in the peptide binding groove of SMYD2.[1] |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.73mL 0.35mL 0.17mL |
8.66mL 1.73mL 0.87mL |
17.31mL 3.46mL 1.73mL |
CAS号 | 1035227-43-0 |
分子式 | C29H38Cl2N4O4 |
分子量 | 577.542 |
别名 | |
运输 | 蓝冰 |
存储条件 |
粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 250 mg/mL(432.87 mM),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 |