product name Indirubin
Description: Indirubin is a potent and selective cyclin-dependent kinases and GSK-3β inhibitor with IC50 of about 5 μM and 0.6 μM. Indirubin is the active ingredient of Danggui Longhui Wan, a mixture of plants that is used in traditional Chinese medicine to treat chronic diseases. Indirubin has been used to treat the symptoms of leukemia. Further biological explorations revealed the ability of indirubin to bind cyclin-dependent kinases and 6-bromoindirubin, extracted from mollusks, to bind glycogen synthase kinase-3. Studies have shown that Indirubin can help keep cancer cells from reproducing in rats.
References: J Biol Chem. 2006 Aug 18;281(33):23425-35; J Biol Chem. 2001 Jan 5;276(1):251-60.
262.26
Formula
C16H10N2O2
CAS No.
479-41-4
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 53 mg/mL (202.1 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
NSC 105327
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19424025
| In Vitro |
In vitro activity: Indirubin is the active ingredient of Danggui Longhui Wan, a mixture of plants that is used in traditional Chinese medicine to treat chronic diseases. Indirubin inhibits CDKs activity with IC50 of 2.2 – 10 μM resulting in cell cycle arrest in the G2/M phase. Indirubin also inhibits GSK-3β with an IC50 of 0.6 μM, attenuating CDK5- and GSK-3β-mediated tau phosphorylation, a process over-active in Alzheimer disease states. It also suppresses tumor necrosis factor (TNF)-induced NF-κB activation in a dose- and time-dependent manner. Indirubin also suppresses the NF-κB activation induced by various inflammatory agents and carcinogens. Indirubin blocks the phosphorylation and degradation of IκBα through the inhibition of activation of IκBα kinase and phosphorylation and nuclear translocation of p65 Kinase Assay: Cell Assay: Indirubin exerted its inhibitory effects not only on interferon-γ production by human myelomonocytic HBL-38 cells but also on interferon-γ and interleukin-σ production by murine splenocytes with no influence on the proliferation of either cells. |
|---|---|
| In Vivo | Because of Indirubin’s inhibitory activity on interferon-γ production, the authors further investigated the effects of indirubin on 2,4,6-trinitro-l-chlorobenzene-induced delayed-type hypersensitivity. When injected intraperitoneally, indirubin significantly inhibited the ear swelling of TNCB-elicited mice. Moreover,the amount of interferon-γ in the culture supernatants of elicited mouse lymphocytes was inhibited by indirubin treatment |
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| Formulation & Dosage | |
| References | J Biol Chem. 2006 Aug 18;281(33):23425-35; J Biol Chem. 2001 Jan 5;276(1):251-60. |
