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Purvalanol B (NG 95) 是选择性可逆的 ATP 竞争性 CDK 抑制剂。它在一系列其他蛋白激酶 (IC50>1000 nM) 中显示出对 CDK 的选择性。它抑制耐氯喹菌株 P. falciparum 的生长。
Purvalanol B (NG 95) 是选择性可逆的 ATP 竞争性 CDK 抑制剂。它在一系列其他蛋白激酶 (IC50>1000 nM) 中显示出对 CDK 的选择性。它抑制耐氯喹菌株 P. falciparum 的生长。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 263 | 现货 | |
5 mg | ¥ 612 | 现货 | |
10 mg | ¥ 818 | 现货 | |
25 mg | ¥ 1,380 | 现货 | |
50 mg | ¥ 1,980 | 现货 | |
100 mg | ¥ 2,870 | 现货 | |
200 mg | ¥ 4,160 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 679 | 现货 |
产品描述 | Purvalanol B (NG 95) is a CDK inhibitor that inhibits Cdk2/cyclin A, Cdk2/cyclin E, Cdk5/p35, and Cdk2/cyclin B (IC50s = 6, 9, 6, and 6 nM, respectively) |
靶点活性 | CDK5-p35:6 nM , CDK2-CyclinE:9 nM , CDK2-CyclinA:6 nM , CDK2-CyclinB:6 nM |
体内活性 | Purvalanol B application decreases the ability of late-stage P.falciparum trophozoites to form multinucleated schizonts and up-regulates proteasome subunits and proteins that contribute to redox homeostasis, which may indicate an increase in oxidative stress as a result of inhibitor application[1]. |
动物实验 | A SYBR Green I parasite growth assay was used to measure the IC50 of Purvalanol B with P. falciparum (strain W2). Purvalanol B or DMSO control were applied to synchronized parasites 36 hours post invasion and parasites were incubated for 12 hours. Giemsa-stained blood smears were used to determine the effect of Purvalanol B on parasite growth, global quantitative proteomic analysis was used to examine differences in protein expression between Purvalanol B-treated and control parasites and results were confirmed by qPCR[1]. |
别名 | NG 95, (2R)-2-[[6-[(3-氯-4-羧基苯基)氨基]-9-(1-甲基乙基)-9H-嘌呤-2-基]氨基]-3-甲基-1-丁醇 |
分子量 | 432.9 |
分子式 | C20H25ClN6O3 |
CAS No. | 212844-54-7 |
Smiles | CC(C)[C@H](CO)Nc1nc(Nc2ccc(C(O)=O)c(Cl)c2)c2ncn(C(C)C)c2n1 |
密度 | 1.43 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 40 mg/mL (92.40 mM) | ||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||
DMSO
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