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Indirubin 479-41-4

Product Description

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Molecular Weight: 262.26 Indirubin is a potent 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 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.


Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)


Species Baboon Dog Monkey Rabbit Guinea pig Rat Hamster Mouse
Weight (kg) 12 10 3 1.8 0.4 0.15 0.08 0.02
Body Surface Area (m2) 0.6 0.5 0.24 0.15 0.05 0.025 0.02 0.007
Km factor 20 20 12 12 8 6 5 3

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.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) × mouse Km(3) = 11.2 mg/kg
rat Km(6)





Chemical Information




Molecular Weight (MW) 262.26
Formula

C16H10N2O2

CAS No. 479-41-4

Storage 3 years -20℃Powder
6 months-80℃in solvent (DMSO, water, etc.)
Synonyms



Solubility (25°C) * In vitro DMSO 53 mg/mL (202.08 mM)
Water <1 mg/mL (
Ethanol <1 mg/mL (
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.




Chemical Name 2H-Indol-2-one, 3-(1,3-dihydro-3-oxo-2H-indol-2-ylidene)-1,3-dihydro-







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