|2-(2,6-二氧代哌啶-3-基)-5-羟基-1H-苯并[de]异喹啉-1,3(2H)-二酮|CsnPharm

CAS No.: 2407829-65-4

CRBN modulator-1 Catalog No. CSN27721

Synonyms: WUN-29654

WUN29654 is a CRBN modulator with CRBN modulatory activity with IC50 value of 2.6μM, Ki value of 0.7μM and cell proliferation IC50 value of ~21.53μM.

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400-920-2911

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生物活性

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技术信息

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..
参考文献

[1] Wen-Jing Fan,et al. Molecular Mechanism of CRBN in the Activity of Lenalidomid eagainst Myeloma—Review. Zhongguo Shi Yan Xue Ye Xue Za Zhi. 2018 Aug;26(4):1240-1243.
[2] A Lopez-Girona,et al. Cereblon is a direct protein target for immunomodulatory and antiproliferative activities of lenalidomide and pomalidomide. Leukemia. 2012 Nov;26(11):2326-35.
[3] Tomoko Asatsuma-Okumura,et al. p63 is a cereblon substrate involved in thalidomide teratogenicity.Nat Chem Biol. 2019 Nov;15(11):1077-1084.
[4] Yuki Hirose,et al. Hypnotic effect of thalidomide is independent of teratogenic ubiquitin/proteasome pathway. Proc Natl Acad Sci U S A. 2020 Sep 15;117(37):23106-23112.

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
- 3.0837 mL
- 15.4184 mL
- 30.8368 mL
- 5 mM
- 0.6167 mL
- 3.0837 mL
- 6.1674 mL
- 10 mM
- 0.3084 mL
- 1.5418 mL
- 3.0837 mL

技术信息

CAS号	2407829-65-4	储存条件	粉末 Inert atmosphere,Room Temperature 液体 -20°C:3-6 月 -80°C:12月
分子式	C17H12N2O5	运输	蓝冰
分子量	324.29	别名	WUN-29654

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CRBN modulator-1 Catalog No. CSN27721

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