A novel role of the aryl hydrocarbon receptor (AhR) in centrosome amplification - implications for chemoprevention

Table 1 Activity spectrum of indirubins

Compound	CDK2 inhibition	CDK1 inhibition	GSK-3β inhibition	AhR activation
Indirubin-3'-oxime (IO)	++^a	++^b	+++^b	++^b
1-Methyl-indirubin-3'-oxime (MeIO)	inactive^b	-^b	-^b	++^b
6-Bromo-indirubin-3'-oxime (BIO)	++^a	++^b	+++^b	++^b
1-Methyl-6-bromo-indirubin-3'-oxime (MeBIO)	inactive^b	-^b	-	+++^b
6-Bromo-indirubin-3'-acetoxime (BIA)	+^a	-^b	+++^b	++^b

IC₅₀ (kinases, μM), EC₅₀ (AhR, μM): <0.1 = +++; <1 = ++; 1-10,000 = +; >10,000 = -
^aData from Meijer et al., Chem. Biol. 2003; 10:1255-1266.
^bData from Knockaert et al., Oncogene 2004; 23:4400-4412.

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