Reversine

Short Summary : A3 adenosine receptor antagonist,ARK-1/-2/-3 inhibitor

Category : Chromatin/Epigenetics|Aurora Kinase

Purity : 0.9909

CAS Number : 656820-32-5

Formula : C21H27N7O

Molecular Weight : 393.49

SMILE : C1CCC(CC1)NC2=NC(=NC3=C2NC=N3)NC4=CC=C(C=C4)N5CCOCC5

Solubility : >19.7mg/mL in DMSO

Storage : Store at -20°C

Description : IC50: 150, 500 and 400 nM for Aurora Kinase A, B and C respectivelyReversine is a novel Aurora kinases inhibitor. Aurora kinases are serine/threonine kinases playing a key role in mitotic regulation. Aurora A kinase resides at spindle poles during mitosis and is implicated in the control of centrosome maturation, duplication, and separation. Aurora B is part of a chromosome passenger complex and is implicated directly in the control of microtubule kinetochore attachment. Aurora kinases have emerged as valuable targets in cancer therapy.In vitro: Reversine could be used to induce dedifferentiation of murine myoblasts. Previous reports also showed that reversine had a role in regeneration. Moreover, a recent report indicated reversine had anti-tumor capabilities for a myeloma cell line, as demonstrated by that reversine could suppress the expression of cell cycle related proteins Aurora kinase A and Aurora kinase B [1]. In vivo: The effects of reversine on tumor weight and volume were assessed using a murine model of cervical cancer with U14 cells, separately or combined with aspirin. The inhibition rate of cells in the combination group significantly increased; moreover, such combination could synergistically inhibit the proliferation of five cervical cancer cell lines. In the mouse model, tumor weight and volume of cervical cancer bearing mice were more reduced [1]. Clinical trial: N/AReference:[1] Qin HX,Yang J,Cui HK,Li SP,Zhang W,Ding XL,Xia YH. Synergistic antitumor activity of reversine combined with aspirin in cervical carcinoma in vitro and in vivo. Cytotechnology.2013 Aug;65(4):643-53.

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