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Celastrol — Datasheet

CAT. NO. DCAPI1155

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ParameterValue
Chemical NameCelastrol
CAS No.34157-83-0
SynonymsCelastrol;(2r,4as,6as,6ar,14as,14br)-10-hydroxy-2,4a,6a,6a,9,14a-hexamethyl-11-oxo-1,3,4,5,6,13,14,14b-octahydropicene-2-carboxylic acid;3-HYDROXY-24-NOR-2-OXO-1(10),3,5,7-FRIEDELATETRAEN-29-OIC ACID;3-HYDROXY-9BETA,13ALPHA-DIMETHYL-2-OXO-24,25,26-TRINOROLEANA-1(10),3,5,7-TETRAEN-29-OIC ACID;TRIPTERIN;Tripterine;CELASTROL(SH);Celastrol (Tripterin);Celastrol (Tripterin );Celasterol;10-Hydroxy-2,4a,6a,9,12b,14a-hexamethyl-11-oxo-1,2,3,4,4a,5,6,6a,11,12b,13,14,14a,14b-tetradecahydro-picene-2-carboxylic acid;C29H38O4;NSC70931;L8GG98663L;Celastrol, Celastrus scandens
FormulaC29H38O4
M.Wt450.6096
SMILESO([H])C([C@]1(C([H])([H])[H])C([H])([H])C([H])([H])[C@]2(C([H])([H])[H])C([H])([H])C([H])([H])[C@]3(C([H])([H])[H])C4=C([H])C([H])=C5C(C([H])([H])[H])=C(C(C([H])=C5[C@]4(C([H])([H])[H])C([H])([H])C([H])([H])[C@@]3(C([H])([H])[H])[C@]2([H])C1([H])[H])=O)O[
Purity>99%
Storage2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Biological Activity

Tripterin (Celastrol) is a proteasome inhibitor which potently and preferentially inhibits the chymotrypsin-like activity of a purified 20S proteasome with IC50 of 2.5 μM.

In Vitro

Tripterin (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 Tripterin (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 Tripterin (Celastrol), the levels of malondialdehyde (MDA) are significantly decreased by 35.2 and 36.7% (P<0.05), respectively. Treatment with 3 and 6 mg/kg Tripterin (Celastrol) markedly restores the GSH level (P<0.05) to almost normal levels[2].

References & source

DC Chemicals original product information

Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.

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