Indirubin

ALX-270-361

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Inhibitor of CDK and GSK

Inhibitor of cyclin-dependent kinases (CDK1/cyclin B (IC₅₀=10µM), CDK2/cyclin A (IC₅₀=2.2µM), CDK2/cyclin E (IC₅₀=7.5µM), CDK4/cyclin D1 (IC₅₀=12µM), CDK5/p35 (IC₅₀=5.5µM)) and of GSK-3β (IC₅₀=600nM). Inhibits inflammatory reaction in delayed-type hypersensitivity in mice. Ligand of human aryl hydrocarbon receptor. Exhibits anti-cancer activity.

Indirubin is derived from various natural sources, such as Indigofera indica, Isatis tinctoria and I. indigotica by fermentation, oxidation and the presence of light as a by product of indigo formation. Indirubin is also present in human urine and fetal bovine serum. Preclinical studies of indirubin confirmed its anti-tumor activity. Efficacy against chronic myelocytic leukemia was demonstrated in clinical trials in China.

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Product Details

Appearance	Purple powder.
CAS	479-41-4
Couple Target	CDK, GSK
Couple Type	Inhibitor
Formula	C₁₆H₁₀N₂O₂
MW	262.3
Purity	≥97% (HPLC)
Solubility	Soluble in DMSO (10mg/ml) or methanol (0.3mg/ml); sparingly soluble in aqueous buffers (12.5µg/ml).
Source	Synthetic.

Handling & Storage

Use/Stability	As indicated on product label or CoA when stored as recommended. Stable for at least 2 years when stored at +4°C in the dark. Stock solutions should be stored in the dark and used within 1 month.
Handling	Protect from light. Keep cool and dry.
Long Term Storage	+4°C
Shipping	Ambient Temperature

Regulatory Status	RUO – Research Use Only

The nuclear entry of the aryl hydrocarbon receptor (AHR) relies on the first nuclear localization signal and can be negatively regulated through IMPα/β specific inhibitors: R. Haidar, et al.; Sci. Rep. 11, 19668 (2023), Abstract
The role of DNA-binding and ARNT dimerization on the nucleo-cytoplasmic translocation of the aryl hydrocarbon receptor: R. Haider, et al.; Sci. Rep. 11, 18194 (2021), Abstract
Indirubin enhances tumor necrosis factor-induced apoptosis through modulation of nuclear factor-kappa B signaling pathway: G. Sethi, et al.; J. Biol. Chem. 281, 23425 (2006), Abstract
Molecular mechanisms of indirubin and its derivatives: novel anticancer molecules with their origin in traditional Chinese phytomedicine: G. Eisenbrand, et al.; J. Cancer Res. Clin. Oncol. 130, 627 (2004), Abstract
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?: S. Leclerc, et al.; J. Biol. Chem. 276, 251 (2001), Abstract — Full Text
Indirubin and indigo are potent aryl hydrocarbon receptor ligands present in human urine: J. Adachi, et al.; J. Biol. Chem. 276, 31475 (2001), Abstract — Full Text
Indirubin inhibits inflammatory reactions in delayed-type hypersensitivity: T. Kunikata, et al.; Eur. J. Pharmacol. 410, 93 (2000), Abstract
Indirubin, the active constituent of a Chinese antileukaemia medicine, inhibits cyclin-dependent kinases: R. Hoessel, et al.; Nature Cell Biol. 1, 60 (1999), Abstract