Ridaifen-B (CAS 886465-70-9)
QUICK LINKS
Ridaifen-B is a novel tamoxifen (TAM) analog which significantly augments apoptosis-inducing effect of TAM in estrogen receptor (ER)-negatives cells. It induces mitochondria-involved apoptosis in Jurkat cells, as evidenced by chromatin-condensed cells as well as downstream activation of caspases (caspase-3, -8 and -9) in a dose- and time-dependent manner. At 4 hours of incubation, IC50 for RID-B is 4 muM (30 muM for TAM). And at prolonged treatment of 48 hours, IC50 for RID-B is 0.1 muM. In a related report on the global anti-tumor activity, RID-B strongly inhibits 39 human cancer cells (JFCR 39), both ER-+ or ER-- at concentrations of equal or less than 1 muM (e.g., at 0.38 muM for SF-539 [central nervous system], at 0.58 muM for HT-29 [colon], at 0.20 muM for DMS114 [lung], at 0.21muM for LOX-IMVI [melanoma], and at 0.23 muM for MKN74 [stomach]. The binding protein of RID-B that exerts the apoptosis events is currently under investigation.
Ridaifen-B (CAS 886465-70-9) References
- Induction of mitochondria-involved apoptosis in estrogen receptor-negative cells by a novel tamoxifen derivative, ridaifen-B. | Nagahara, Y., et al. 2008. Cancer Sci. 99: 608-14. PMID: 18167132
- Ridaifen B, a tamoxifen derivative, directly binds to Grb10 interacting GYF protein 2. | Tsukuda, S., et al. 2013. Bioorg Med Chem. 21: 311-20. PMID: 23199482
- Anaplasma phagocytophilum inhibits apoptosis and promotes cytoskeleton rearrangement for infection of tick cells. | Ayllón, N., et al. 2013. Infect Immun. 81: 2415-25. PMID: 23630955
- Novel tamoxifen derivative Ridaifen-B induces Bcl-2 independent autophagy without estrogen receptor involvement. | Nagahara, Y., et al. 2013. Biochem Biophys Res Commun. 435: 657-63. PMID: 23688426
- Negative regulation of Grb10 Interacting GYF Protein 2 on insulin-like growth factor-1 receptor signaling pathway caused diabetic mice cognitive impairment. | Xie, J., et al. 2014. PLoS One. 9: e108559. PMID: 25268761
- Autophagy in the fight against tuberculosis. | Bento, CF., et al. 2015. DNA Cell Biol. 34: 228-42. PMID: 25607549
- Structure-activity relationships for the antifungal activity of selective estrogen receptor antagonists related to tamoxifen. | Butts, A., et al. 2015. PLoS One. 10: e0125927. PMID: 26016941
- Necroptosis Is an Important Severity Determinant and Potential Therapeutic Target in Experimental Severe Pancreatitis. | Louhimo, J., et al. 2016. Cell Mol Gastroenterol Hepatol. 2: 519-535. PMID: 27642624
- Selective Estrogen Receptor Modulators: Cannabinoid Receptor Inverse Agonists with Differential CB1 and CB2 Selectivity. | Franks, LN., et al. 2016. Front Pharmacol. 7: 503. PMID: 28066250
- Ormeloxifene-induced unfolded protein response contributes to autophagy-associated apoptosis via disruption of Akt/mTOR and activation of JNK. | Bhattacharjee, A., et al. 2018. Sci Rep. 8: 2303. PMID: 29396506
- The tamoxifen derivative ridaifen-B is a high affinity selective CB2 receptor inverse agonist exhibiting anti-inflammatory and anti-osteoclastogenic effects. | Franks, LN., et al. 2018. Toxicol Appl Pharmacol. 353: 31-42. PMID: 29906493
- Anti-proliferative effect of ridaifen-B on hepatoma cells. | Hasegawa, G., et al. 2018. Biomed Rep. 9: 175-180. PMID: 30013780
- Future Aspects for Cannabinoids in Breast Cancer Therapy. | Kisková, T., et al. 2019. Int J Mol Sci. 20: PMID: 30987191
Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
Ridaifen-B, 5 mg | sc-215814 | 5 mg | $193.00 | |||
Ridaifen-B, 25 mg | sc-215814A | 25 mg | $938.00 |