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7BIO
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
7BIO图片
CAS NO:916440-85-2
包装与价格:
包装价格(元)
10mg电议
50mg电议

产品介绍
7BIO (7-Bromoindirubin-3-Oxime) 是靛玉红的衍生物。
Cas No.916440-85-2
别名7-Bromoindirubin-3’-oxime
化学名7-bromo-3-[1,3-dihydro-3-(hydroxyimino)-2H-indol-2-ylidene]-1,3-dihydro-2H-indol-2-one
Canonical SMILESO/N=C(C1=CC=CC=C1N2)/C2=C3C(NC4=C(Br)C=CC=C4/3)=O
分子式C16H10BrN3O2
分子量356.2
溶解度Soluble in ethanol;DMSO
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

7-bromoindirubin-3'-oxime (7BIO), a derivative of indirubin, is a caspase independent nonapoptotic cell death inducer [1]. 7-bromoindirubin-3'-oxime is an inhibitor of FLT3, DYRK1A, DYRK2, Aurora B and Aurora C kinases.

FLT3 is a cytokine receptor expressed on the surface of many hematopoietic progenitor cells. Signalling of FLT3 is important for the normal development of haematopoietic stem cells and progenitor cells. DYRK1A and DYRK2 have been involved in catalyzing its autophosphorylation on serine/threonine and tyrosine residues and play a significant role in a signaling pathway regulating cell proliferation. Aurora kinases are serine/threonine kinases which are essential for cell proliferation and cellular division by controlling chromatid segregation.

7-bromoindirubin-3'-oxime (7BIO) showed a marginal inhibitory activity towards CDKs and GSK-3. 7BIO triggered a rapid cell death process distinct from apoptosis. 7BIO induced the appearance of large pycnotic nuclei, without classical features of apoptosis such as chromatin condensation and nuclear fragmentation. 7BIO-induced cell death was not accompanied by cytochrome c release neither by any measurable effector caspase activation. 7BIO triggered the activation of non-apoptotic cell death, possibly through necroptosis or autophagy. 7BIO inhibited FLT3, the dual-specificity tyrosine phosphorylation-regulated kinases, DYRK1A and DYRK2 with the IC50 values of 0.34 μM, 1.9 and 1.3 μM, respectively [2]. 7BIO also inhibited the activity of Aurora B and C kinases with IC50 values of 4.6 and 0.7 μM, respectively [3].

References:
[1] Ribas J, Bettayeb K, Ferandin Y, et al.  7-Bromoindirubin-3′-oxime induces caspase-independent cell death[J]. Oncogene, 2006, 25(47): 6304-6318.
[2] Myrianthopoulos V, Kritsanida M, Gaboriaud-Kolar N, et al.  Novel inverse binding mode of indirubin derivatives yields improved selectivity for DYRK kinases[J]. ACS medicinal chemistry letters, 2012, 4(1): 22-26.
[3] Myrianthopoulos V, Magiatis P, Ferandin Y, et al.  An integrated computational approach to the phenomenon of potent and selective inhibition of aurora kinases B and C by a series of 7-substituted indirubins[J]. Journal of medicinal chemistry, 2007, 50(17): 4027-4037.