Nutlin 3b

"目录号: HY-15335

Apoptosis-

Nutlin-3b是MDM2/p53抑制剂，IC50为13.6 μM。

MDM-2/p53

相关产品

RG7388-Pifithrin-α hydrobromide-Triptolide-Nutlin 3a-AMG 232-RG7112-Puromycin aminonucleoside-NVP-CGM097-Pifithrin-β hydrobromide-SJ-172550-Tenovin 6 Hydrochloride-RITA-SAR405838-Solasodine-PRIMA-1-

生物活性

Description

Nutlin-3b is a MDM2/p53 antagonist or inhibitor with IC50 of 13.6 μM. Nutlin-3b is a less active enantiomer

IC50& Target

IC50: 13.6 μM (MDM2/p53)

In Vitro

Nutlin-3b is a 150-fold less potent (+)-enantiomer of Nutlin-3 as p53 MDM2 antagonist or inhibitor, in comparison with more potent opposite (-)-enantiomer Nutlin-3a. It is useful as a negative control for non-Mdm2 related cellular activities. Nutlin-3b is useful as a negative control s for non-MDM2-related cellular activities. Nutlin-3a induces the expression of MDM2 and p21 (but not p53) only in cells with wild-type p53. Nutlin-3b has no effect regardless of the p53 status of the cells. Only the active enantiomer Nutlin-3a shows a potent antiproliferative activity and clear separation of potency between the cells harboring wild-type p53 and those harboring mutant p53. The potency of Nutlin-3b is much lower in the wild-type p53 cells and nearly identical to the potency of Nutlin-3a against the mutant p53 cells. After 48 hours of exposure to the Nutlin-3a, 45% of the cell population became TUNEL positive, but cells treated with the Nutlin-3b are indistinguishable from the untreated controls.

References

[1].Ye F, Lattif AA, Xie J, Weinberg A, Gao S.Nutlin-3 induces apoptosis, disrupts viral latency and inhibits expression of angiopoietin-2 in Kaposi sarcoma tumor cells.Cell Cycle. 2012 Apr 1;11(7):1393-9. Epub 2012 Apr 1.

[2].Shin JS, Ha JH, He F, Muto Y, Ryu KS, Yoon HS, Kang S, Park SG, Park BC, Choi SU, Chi SW.Structural insights into the dual-targeting mechanism of Nutlin-3.Biochem Biophys Res Commun. 2012 Mar 30;420(1):48-53.

[3].Gasparini C, Tommasini A, Zauli G.The MDM2 inhibitor Nutlin-3 modulates dendritic cell-induced T cell proliferation.Hum Immunol. 2012 Apr;73(4):342-5.

[4].Ma T, Yamada S, Ichwan SJ, Iseki S, Ohtani K, Otsu M, Ikeda MA.Inability of p53-reactivating compounds Nutlin-3 and RITA to overcome p53 resistance in tumor cells deficient in p53Ser46 phosphorylation.Biochem Biophys Res Commun. 2012 Jan 20;417(3):931-7.

[5].Vatsyayan R, Singhal J, Nagaprashantha LD, Awasthi S, Singhal SS.Nutlin-3 enhances sorafenib efficacy in renal cell carcinoma.Mol Carcinog. 2011 Oct 17. doi: 10.1002/mc.20875.