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676541-58-5
  • names:

    (1R,3aS,3bR,5aS,6aS,7aS,9R,11S,11aR,12aS,13aR,13bS,15aR)-3a,11a-dihydroxy-13a-(hydroxymethyl)-9,15a-dimethyl-1-(5-oxo-2,5-dihydrofuran-3-yl)icosahydro-1H-spiro[cyclopenta[7,8]phenanthro[2,3-b]pyrano[3,2-e][1,4]dioxine-11,2'-thiazolidin]-4'-one

  • CAS号:

    676541-58-5

    MDL Number:
  • MF(分子式): C31H43NO9S MW(分子量): 605.743
  • EINECS: Reaxys Number:
  • Pubchem ID: Brand:BIOFOUNT
UNBS-1450
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中文别名 (1R,3aS,3bR,5aS,6aS,7aS,9R,11S,11aR,12aS,13aR,13bS,15aR)-3a,11a-dihydroxy-13a-(hydroxymethyl)-9,15a-dimethyl-1-(5-oxo-2,5-dihydrofuran-3-yl)icosahydro-1H-spiro[cyclopenta[7,8]phenanthro[2,3-b]pyrano[3,2-e][1,4]dioxine-11,2'-thiazolidin]-4'-one
英文别名 UNBS-1450, UNBS 1450, UNBS1450, UBS-1450, UBS1450, UBS 1450
CAS号 676541-58-5
Inchi InChI=1S/C31H43NO9S/c1-16-11-30(32-24(34)14-42-30)31(37)26(39-16)40-22-10-18-3-4-21-20(28(18,15-33)12-23(22)41-31)5-7-27(2)19(6-8-29(21,27)36)17-9-25(35)38-13-17/h9,16,18-23,26,33,36-37H,3-8,10-15H2,1-2H3,(H,32,34)/t16-,18+,19-,20+,21-,22+,23+,26+,27-,28-,29+,30+,31-/m1/s1
InchiKey GRINEMOQBRCRRY-OVGHKGCDSA-N
分子式 Formula C31H43NO9S
分子量 Molecular Weight 605.743
溶解度Solubility
性状 Solid powder
储藏条件 Storage conditions Dry, dark and store at 0-4℃ for short term (days to weeks) or -20℃ for long term (Store correctly 2-3years).
产品说明 UNBS-1450(CAS:676541-58-5):仅限应用于工业或者科学研究过程中非医疗目的,不应用于人类或动物的临床诊断以及治过程疗,该产品非药用,非食用。
IntroductionUNBS-1450, also known as UBS-1450, is a sodium channel antagonist potentially for the treatment of cancer. UNBS-1450 is a hemi-synthetic cardenolide derived from 2″-oxovorusharin extracted from the plant Calotropis procera, which is effective against various cancer cell types with an excellent differential toxicity. At low nanomolar concentrations, UNBS-1450 induces apoptotic cell death. UNBS-1450 inhibits NF-κB transactivation and triggers apoptosis by cleavage of pro-caspases 8, 9 and 3/7, by decreasing expression of anti-apoptotic Mcl-1 and by recruitment of pro-apoptotic Bak and Bax protein eventually resulting in cell death.
Application1
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危险性 Warning
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备注
[1]Schoner W, Scheiner-Bobis G. Endogenous and exogenous cardiac glycosides: their roles in hypertension, salt metabolism, and cell growth. Am J Physiol Cell Physiol. 2007 Aug;293(2):C509-36. Review. PubMed PMID: 17494630.
[2]Cerella C, Muller F, Gaigneaux A, Radogna F, Viry E, Chateauvieux S, Dicato M, Diederich M. Early downregulation of Mcl-1 regulates apoptosis triggered by cardiac glycoside UNBS1450. Cell Death Dis. 2015 Jun 11;
6:e1782. doi: 10.1038/cddis.2015.134. PubMed PMID: 26068790; PubMed Central PMCID: PMC4669823.
[4]Muller F, Cerella C, Radogna F, Dicato M, Diederich M. Effects of Natural Products on Mcl-1 Expression and Function. Curr Med Chem. 2015;22(30):3447-61. Review. PubMed PMID: 26179996.
[5] Juncker T, Cerella C, Teiten MH, Morceau F, Schumacher M, Ghelfi J, Gaascht F, Schnekenburger M, Henry E, Dicato M, Diederich M. UNBS1450, a steroid cardiac glycoside inducing apoptotic cell death in human leukemia cells. Biochem Pharmacol. 2011 Jan 1;81(1):13-23. doi: 10.1016/j.bcp.2010.08.025. PubMed PMID: 20849830.
5: Mijatovic T, Jungwirth U, Heffeter P, Hoda MA, Dornetshuber R, Kiss R, Berger W. The Na+/K+-ATPase is the Achilles heel of multi-drug-resistant cancer cells. Cancer Lett. 2009 Sep 8;282(1):30-4. doi: 10.1016/j.canlet.2009.02.048. PubMed PMID: 19339106.
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