产品说明书
CRBN modulator-1
 |
同义名 : | - |
| CAS号 : | 2407829-65-4 | |
| 货号 : | A1371036 | |
| 分子式 : | C17H12N2O5 | |
| 纯度 : | 98%+ | |
| 分子量 : | 324.288 | |
| MDL号 : | MFCD33029299 | |
| 存储条件： |
粉末 Inert atmosphere,Room Temperature 液体 -20°C:3-6个月-80°C:12个月 |
|
| 溶解度 : |
DMSO: 9 mg/mL(27.75 mM)，配合低频超声，并调节pH至2，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 | Thalidomide and its immunomodulatory analogues have numerous effects on the body's immune system, including potential anti-cancer and anti-inflammatory activities. Thalidomide is currently used experimentally to treat various cancers, dermatological, neurological and inflammatory diseases Steve K Teo,et al. Thalidomide as a novel therapeutic agent: new uses for an old product. Drug Discov Today. 2005 Jan 15;10(2):107-14. . Cereblon（CRBN) is a brain-associated protein with ionic protease activity, which interacts with DNA damage-binding protein-1 (DDB1), Cullin 4 (Cul4A or Cul4B), and regulator of Cullins 1 (RoC1) to form the functional E3 ubiquitin ligase complex(CRBN-CRL4) that performs proteolysis via the ubiquitin-proteasome pathway[1].The ubiquitously expressed E3 ligase protein cereblon (CRBN) has been identified as the primary teratogenic target of thalidomide[2]. CRBN functions as a substrate receptor of the E3 ubiquitin ligase CRL4, whose substrate specificity is modulated by thalidomide and its analogs[3].Thalidomide increased non-REM sleep time in Crbn YW/AA knock-in homozygotes and heterozygotes to a similar degree as seen in wild-type littermates. Thalidomide similarly depressed excitatory synaptic transmission in the cortical slices obtained from wild-type and Crbn YW/AA homozygous knock-in mice without affecting GABAergic inhibition. Thalidomide induced Fos expression in vasopressin-containing neurons of the supraoptic nucleus and reduced Fos expression in the tuberomammillary nuclei[4]. WUN29654 is a Thalidomide analog and CRBN modulator,has an IC50 of 3.5 μM and a Ki of 0.98 μM. Nathanael Gray, et al. New crbn modulators. WO2020006262A1.. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
|
1 mM 5 mM 10 mM |
3.08mL 0.62mL 0.31mL |
15.42mL 3.08mL 1.54mL |
30.84mL 6.17mL 3.08mL |
| 参考文献 |
|---|