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HIV-1 integrase inhibitor 8

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Chemical Structure| 1568-80-5 同义名 : -
CAS号 : 1568-80-5
货号 : A218060
分子式 : C21H24O2
纯度 : 98%
分子量 : 308.414
MDL号 : MFCD01412945
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 120 mg/mL(389.09 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：
生物活性
描述 HIV encodes three enzymes: reverse transcriptase (RT), protease (PR), and integrase (IN). IN is a promising target because integration is an essential step in retroviral replication cycle. HIV-1 integrase inhibitor 8 is a HIV-1 integrase inhibitor. HIV-1 integrase inhibitor 8 inhibited 3′-processing (TC) and strand-transfer (ST) activities in the presence of Mn2+ as the cationic cofactor by gel assay with IC50 values of 275 µM and 200 µM, respectively. Furthermore, HIV-1 integrase inhibitor 8 inhibited MCV (molluscum contagiosum virus) topoisomerase and DNA religation with IC50 values of 500 µM and 200 µM, respectively. Moreover, HIV-1 integrase inhibitor 8 induced cell cytotoxicity and yielded a LD50 (dose at which the signal was reduced 50% due to cell death) of 20 μM in HeLa cells[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.24mL

0.65mL

0.32mL

16.21mL

3.24mL

1.62mL

32.42mL

6.48mL

3.24mL
参考文献

[1]Molteni, et al. A New Class of HIV-1 Integrase Inhibitors: The 3,3,3', 3'-tetramethyl-1,1'-spirobi(indan)-5,5',6,6'-tetrol Family.J Med Chem

[2]Molteni V, Rhodes D, Rubins K, Hansen M, Bushman FD, Siegel JS. A new class of HIV-1 integrase inhibitors: the 3,3,3', 3'-tetramethyl-1,1'-spirobi(indan)-5,5',6,6'-tetrol family. J Med Chem. 2000 May 18;43(10):2031-9.