| 规格 | 价格 | 库存 | 数量 |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
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| 靶点 |
USP7 (IC50 = 0.75 μM); USP7 (IC50 = 0.43 μM); USP43 (IC50 = 20.3 μM); Ub-MDM2 (IC50 = 0.23 μM)
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| 体外研究 (In Vitro) |
GNE-6640 encourages the natural ubiquitination of MDM2 through Lys48 (K48)-linked polyubiquitin chains, thereby guiding the process of proteasomal degradation13. GNE-6640 focuses on the p53, MDM2, and USP7 signaling pathways in cells. With an IC50 ≤ 10 μM, GNE-6640 reduces the viability of 108 cell lines. Combining GNE-6640 with DNA-damaging drugs like doxorubicin or cisplatin may trigger the p53 response and improve the effectiveness of USP7 inhibitors. GNE-6640 may cause the death of tumor cells. PIM kinase inhibitors and other targeted substances, such as chemotherapeutic agents, increase the cytotoxicity of GNE-6640[1].
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| 参考文献 |
| 分子式 |
C20H18N4O
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|---|---|---|
| 分子量 |
330.39
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| 精确质量 |
330.15
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| 元素分析 |
C, 72.71; H, 5.49; N, 16.96; O, 4.84
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| CAS号 |
2009273-67-8
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| 相关CAS号 |
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| 外观&性状 |
Solid powder
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| SMILES |
CCC1=C(C(=NC=C1C2=CC3=C(C=C2)NN=C3)N)C4=CC=C(C=C4)O
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| InChi Key |
ZHYXJQQBKROZDX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H18N4O/c1-2-16-17(13-5-8-18-14(9-13)10-23-24-18)11-22-20(21)19(16)12-3-6-15(25)7-4-12/h3-11,25H,2H2,1H3,(H2,21,22)(H,23,24)
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| 化学名 |
4-[2-amino-4-ethyl-5-(1H-indazol-5-yl)pyridin-3-yl]phenol
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| 别名 |
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| HS Tariff Code |
2934.99.03.00
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| 存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| 运输条件 |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| 溶解度 (体外) |
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|---|
| 制备储备液 | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.0267 mL | 15.1336 mL | 30.2673 mL | |
| 5 mM | 0.6053 mL | 3.0267 mL | 6.0535 mL | |
| 10 mM | 0.3027 mL | 1.5134 mL | 3.0267 mL |
1、根据实验需要选择合适的溶剂配制储备液 (母液)：对于大多数产品，InvivoChem推荐用DMSO配置母液 (比如：5、10、20mM或者10、20、50 mg/mL浓度），个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息，或者很难将产品溶解在溶液中，请联系我们;
3、建议使用下列计算器进行相关计算（摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等）;
4、母液配好之后，将其分装到常规用量，并储存在-20°C或-80°C，尽量减少反复冻融循环。
计算结果:
工作液浓度： mg/mL；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL)。如该浓度超过该批次药物DMSO溶解度，请首先与我们联系。
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH2O，混匀澄清。
(1) 请确保溶液澄清之后，再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶；
(2) 一定要按顺序加入溶剂 (助溶剂) 。
 Identification and characterization of USP7 inhibitors.Nature.2017 Oct 26;550(7677):534-538. |
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 Selectivity of USP7 inhibitors and synergy with PIM kinase inhibition.
USP7 inhibitors compete with ubiquitin binding to USP7.Nature.2017 Oct 26;550(7677):534-538. |
 USP7 preferentially binds and cleaves ubiquitin moieties with free K48 side chains.Nature.2017 Oct 26;550(7677):534-538. |
GK16S
GK13S
USP7-IN-10 hydrochloride
GSK2643943A
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