Celastrol产品描述:Celastrol is a proteasome inhibitor, potently and preferentially inhibits the chymotrypsin-like activity of a purified 20S proteasome (IC50=2.5 μM). IC50 & Target: IC50: 2.5 μM (20S proteasome)[1] In Vitro: Celastrol significantly inhibits the proteasomal chymotrypsin activity in PC-3 cells in a concentration-dependent manner; at 2.5 μM it reaches ~55% inhibition, comparable to its potency to a purified 20S proteasome (IC50=2.5 μM). Furthermore, increased levels of IκB-α, Bax, and p27 are observed, three well known target proteins of the proteasome in PC-3 cells treated with Celastrol[1]. In Vivo: Treatment of PC-3 tumor-bearing nude mice with Celastrol (1-3 mg/kg/d, i.p., 1-31 days) results in significant inhibition (65-93%) of the tumor growth[1]. Following treatment with 3 and 6 mg/kg Celastrol, the levels of malondialdehyde (MDA) are significantly decreased by 35.2 and 36.
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Purity:98%
MWt:239.2692
Formula:C15H13NO2
SMILES:OC1=CC=C(CC(C#N)C2=CC=C(O)C=C2)C=C1
Pathway:Others;
Mechanisms:Estrogen Receptor/ERR;
Research Area:Neurological Disease
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