INDIRUBIN-3-MONOXIME

Uses

Indirubin-3′-oxime (IDR3O), a synthetic derivative of indirubin, is a potent inhibitor of cyclin-dependent kinases (CDKs) and glycogen synthase kinase 3β (GSK3β). Indirubin-3′-oxime directly inhibits the activity of all three isoforms of JNK (JNK1, JNK2, and JNK3), with IC50s of 0.8 μM, 1.4 μM, and 1.0 μM, respectively. Indirubin-3′-oxime can enhance height growth via activation of Wnt/β-catenin signaling in chondrocytes[1][2][3].

Definition

ChEBI: Indirubin-3'-monoxime is a member of the class of biindoles that is indirubin in which the keto group at position 3' has undergone condensation with hydroxylamine to form the corresponding oxime. It has a role as an EC 2.7.11.22 (cyclin-dependent kinase) inhibitor, an EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor, an osteogenesis regulator, a neuroprotective agent and an anti-obesity agent. It is a member of oxindoles, a bisindole, a ring assembly, a ketoxime and an alkaloid.

in vivo

IC 50

JNK1: 0.8 μM (IC₅₀); JNK2: 1.4 μM (IC₅₀); JNK3: 1 μM (IC₅₀); GSK-3β; CDK

References

[1] Xie Y, et al. Indirubin-3'-oxime inhibits c-Jun NH2-terminal kinase: anti-apoptotic effect in cerebellar granule neurons. Neurosci Lett. 2004;367(3):355-359. DOI:10.1016/j.neulet.2004.06.044
[2] Hu S, et al. Indirubin-3-Oxime Effectively Prevents 6OHDA-Induced Neurotoxicity in PC12 Cells via Activating MEF2D Through the Inhibition of GSK3β. J Mol Neurosci. 2015;57(4):561-570. DOI:10.1007/s12031-015-0638-y
[3] Choi S, et al. Indirubin-3'-oxime stimulates chondrocyte maturation and longitudinal bone growth via activation of the Wnt/β-catenin pathway. Exp Mol Med. 2019;51(9):1-10. Published 2019 Sep 12. DOI:10.1038/s12276-019-0306-3