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A-196 {[allProObj[0].p_purity_real_show]}

货号:A933282 Ambeed 开学季,买赠积分,赢豪礼

A-196 is a potent and selective inhibitor of SUV420H1 and SUV420H2 with IC50s of 25 and 144 nM respectively.

A-196 化学结构 CAS号:1982372-88-2
A-196 化学结构
CAS号:1982372-88-2
A-196 3D分子结构
CAS号:1982372-88-2
A-196 化学结构 CAS号:1982372-88-2
A-196 3D分子结构 CAS号:1982372-88-2
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A-196 纯度/质量文件 产品仅供科研

货号:A933282 标准纯度: {[allProObj[0].p_purity_real_show]}
批次查询: 批次纯度:

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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

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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

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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

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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

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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。

A-196 生物活性

描述 The homologous protein lysine methyltransferases SUV420H1 and SUV420H2 (collectively named SUV4-20) are important regulators of genomic integrity. A-196 is a selective and potent SUV4-20 inhibitor. It inhibited the methyltransferase activity of SUV420H1 and SUV420H2 with IC50 values of 25 ± 5nM and 144 ± 21nM, respectively. A-196 also showed potent binding affinity for adenosine receptors A1 and A2A with Ki values of 0.021μM and 0.028μM, respectively. A-196 binds to SUV420H1 with a Kd value of 74.8 ± 22.7nM. Treatment of human osteosarcoma cell line U2OS with A-196 for 48 hours led to an increase in H4K20me1 level (EC50 = 735nM) and a decrease in both H4K20me2 (EC50 = 262nM) and H4K20me3 (EC50 = 370nM) levels. Also in U2OS cells, treatment with 6μM A-196 resulted in a robust increase in H4K20me1 level in the S phase and a decrease in H4K20me3 level. A-196 at 1 and 10μM inhibited the ability of primary B cells isolated from the spleens of wild-type mice to switch from IgM to IgG1, IgG3 or IgE[1].
作用机制 A-196 inhibits SUV4-20 in a substrate-competitive manner. It binds within the histone H4 peptide-binding groove of the enzyme and is competitive with the histone peptide substrate, but not with the cofactor S-adenosylmethionine. There is strong cooperativity between the binding of A-196 and S-adenosylmethionine to SUV420H1[1].

A-196 参考文献

[1]Bromberg KD, Mitchell TR, Upadhyay AK, Jakob CG, Jhala MA, Comess KM, Lasko LM, Li C, Tuzon CT, Dai Y, Li F, Eram MS, Nuber A, Soni NB, Manaves V, Algire MA, Sweis RF, Torrent M, Schotta G, Sun C, Michaelides MR, Shoemaker AR, Arrowsmith CH, Brown PJ, Santhakumar V, Martin A, Rice JC, Chiang GG, Vedadi M, Barsyte-Lovejoy D, Pappano WN. The SUV4-20 inhibitor A-196 verifies a role for epigenetics in genomic integrity. Nat Chem Biol. 2017 Mar;13(3):317-324

A-196 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.78mL

0.56mL

0.28mL

13.92mL

2.78mL

1.39mL

27.84mL

5.57mL

2.78mL

A-196 技术信息

CAS号1982372-88-2
分子式C18H16Cl2N4
分子量 359.252
别名
运输蓝冰
存储条件

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 12 mg/mL(33.4 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
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