CDDO-Im-RTA-403-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemECDDO-ImCat. No.: HY-15725CAS No.: 443104-02-7Synonyms: RTA-403; TP-235; CDDO-Imidazolide分式: CHNO分量: 541.72作靶点: Keap1-Nrf2; PPAR作通路: NF-B; Cell Cycle/DNA Damage储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 mont

2、h溶解性数据体外实验 DMSO : 50 mg/mL (92.30 mM; Need ultrasonic)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (4.61 mM); Suspended solution; Need ultrasonic2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (4.61 mM); Suspended solution; Need ultrasonic1/3 Master of Small Mo

3、lecules 您边的抑制剂师www.MedChemE3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (4.61 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 CDDO-Im (CDDO-imidazolide)是Nrf2 和 PPAR 的活化剂，对PPAR和PPAR的 Ki 分别为232 nM 和344nM。IC50 & Target PPAR PPAR Nrf2232 nM (Ki) 344 nM (Ki)体外研究 CDDO-Im is highly active in suppress

4、ing cellular proliferation of human leukemia and breast cancer cell lines(IC50 approximately 10-30 nM). In U937 leukemia cells, CDDO-Im also induces monocytic differentiation asmeasured by increased cell surface expression of CD11b and CD36 1. Treatment with CDDO-Im elevatesprotein levels of Nrf2, a

5、 transcription factor previously shown to bind ARE sequences, and increasesexpression of a number of antioxidant and detoxification genes regulated by Nrf2 2. CDDO-Im is one of themost potent synthetic triterpenoids shown to induce growth inhibition and apoptosis in various human cancercells, includ

6、ing multiple myeloma, lung, pancreas and breast cancer. CDDO-Im treatment markedly inducescell cycle arrest at G2/M-phase and apoptosis in the triple-negative breast cancer cell lines, SUM159 andMDA-MB-231. The CD24/EpCAM+ cells in SUM159 tumorspheres are significantly inhibited by CDDO-Imtreatment.

7、 CDDO-Im also significantly decreases sphere forming efficiency and tumorsphere size in bothprimary and secondary sphere cultures 3.体内研究 CDDO-Im is a potent inhibitor of de novo inducible nitric oxide synthase expression in primary mousemacrophages. Moreover, CDDO-Im inhibits growth of B16 murine me

8、lanoma and L1210 murine leukemiacells in vivo. Injection of 10 nM (5.4 g) of CDDO-Im almost completely blocks the ability of IFN- to induceiNOS, and treatment with as little as 1 nmol of CDDO-Im (0.54 g) is partially effective 1.PROTOCOLCell Assay 3 CDDO-Im is dissolved in DMSO. SUM159 and MDA-MB-23

9、1 cells are seeded into each well of 96-well plates(1,000 cell/well) and treated the next day with vehicle control or CDDO-Im (1, 10, 50, 100 and 200 nM) forgiven incubation time. The absorbance is measured with a spectrophotometer to determine cell proliferationrate 3.MCE has not independently conf

10、irmed the accuracy of these methods. They are for reference only.Animal Mice: Mice are injected i.p. with thioglycollate, and the resulting resident peritoneal macrophages areAdministration 1 activated 3 days later with an i.p. injection of IFN-. CDDO and CDDO-Im are injected i.p. 30 min after IFN-.

11、Macrophages are harvested 10 h later, cultured for 12 h, and then assayed for expression of iNOS proteinand production of nitric oxide (NO) 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.2/3 Master of Small Molecules 您边的抑制剂师www.MedChemE户使本产品发表的科研献 En

12、viron Pollut. 2019 Jan 3;247:293-301.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Place AE, et al. The novel synthetic triterpenoid, CDDO-imidazolide, inhibits inflammatory response and tumor growth in vivo. ClinCancer Res. 2003 Jul;9(7):2798-806.2. Liby K, et al. The synthe

13、tic triterpenoids, CDDO and CDDO-imidazolide, are potent inducers of heme oxygenase-1 and Nrf2/AREsignaling. Cancer Res. 2005 Jun 1;65(11):4789-98.3. So JY, et al. A synthetic triterpenoid CDDO-Im inhibits tumorsphere formation by regulating stem cell signaling pathways in triple-negative breast cancer. PLoS One. 2014 Sep 17;9(9):e107616.McePd