Indirubin is a cyclin-dependent kinase inhibitor which functions by competing with ATP for binding to the catalytic subunit. Indirubin is used in traditional Chinese medicine for anti-inflammatory, anti-tumor, and neuroprotective effects. Indirubin inhibits glycogen synthase kinase-3 (IC50 = 2.5 μM) and cyclin-dependent kinases 1 and 5 (IC50 = 10 μM for both isoforms). Indirubin also inhibits CDK1/5 with IC50 of 10 μM and 5.5 μM. Indirubin exhibits antiproliferative activity leading to G2/M arrest in many cell lines and G1/S arrest in Jurkat cells. Indirubin induces cell cycle arrest and inhibits cell proliferation.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 50 mg/mL|
Indirubins inhibit glycogen synthase kinase-3 beta and CDK5/p25, two protein kinases involved in abnormal tau phosphorylation in Alzheimer's disease. A property common to most cyclin-dependent kinase inhibitors?
Leclerc S, et al. J Biol Chem. 2001 Jan 5;276(1):251-60. PMID: 11013232.
Indirubin, the active constituent of a Chinese antileukaemia medicine, inhibits cyclin-dependent kinases.
Hoessel R, et al. Nat Cell Biol. 1999 May;1(1):60-7. PMID: 10559866.
|Related GSK-3 Products|
IM-12 is a potent and selective GSK-3β inhibitor with IC50 of 53 nM, which also enhances canonical Wnt signalling.
SB415286 is a potent GSK3α inhibitor with IC50/Ki of 78 nM/31 nM with equally effective inhibition of GSK-3β.
TDZD-8 is a non-ATP competitive GSK-3β inhibitor with IC50 of 2 μM; minimal inhibitory effect observed on CDK1, casein kinase II, PKA and PKC.
LY2090314 is a potent GSK-3 inhibitor for GSK-3α/β with IC50 of 1.5 nM/0.9 nM; may improve the efficacy of platinum-based chemotherapy regimens. Phase 1/2.
AZD1080 is a selective, orally active, brain permeable GSK3 inhibitor, inhibits human GSK3α and GSK3β with Ki of 6.9 nM and 31 nM, respectively.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.