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.
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CHIR 99021 trihydrochloride is a hydrochloride salt of CHIR 99021; selective GSK-3 inhibitor.
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SB415286 is a potent GSK3α inhibitor with IC50/Ki of 78 nM/31 nM with equally effective inhibition of GSK-3β.
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