1982372-88-2|A-196|CsnPharm

CAS No.: 1982372-88-2

A-196 Catalog No. CSN19081

Synonyms: A-196

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

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靶点选择性

生物活性

实验方案

技术信息

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 K_i values of 0.021μM and 0.028μM, respectively. A-196 binds to SUV420H1 with a K_d 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].
临床研究
NCT号适应症或疾病临床期招募状态预计完成时间地点
NCT02876757 - - Completed - -
NCT02876757 - - Completed - -
参考文献

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT02876757	-	-	Completed	-	-
NCT02876757	-	-	Completed	-	-

[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

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.7836 mL
- 13.9179 mL
- 27.8358 mL
- 5 mM
- 0.5567 mL
- 2.7836 mL
- 5.5672 mL
- 10 mM
- 0.2784 mL
- 1.3918 mL
- 2.7836 mL

技术信息

CAS号

1982372-88-2

储存条件

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

液体: -20°C:3-6 月 -80°C:12月

分子式

C18H16Cl2N4

运输

蓝冰

分子量

359.25

别名

A-196

溶解度

DMSO	insoluble
Water	insoluble

动物实验配方

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A-196 Catalog No. CSN19081

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