Diarylpropio
nitrile(DPN)是一種非甾體雌激素受體(ER_beta_)選擇性配體。
Celastrol產品描述: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 (IC
50=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 malo
ndialdehyde
(MDA) are significantly decreased by 35.2 and 36.
公司介紹:MedChemExpress(MCE)專注于各種抑制劑、激動劑、API及化合物庫,總部位于美國新澤西,分別在瑞典和上海設有歐洲區子公司和區總代理,營銷網點遍及20多個地區。MCE經過多年努力已成為生物活性小分子領域的供應商,
產品涵蓋癌癥、神經科學、抗感染、表觀遺傳學等20個熱門研究領域,PI3K、MAPK等近千個細分靶點,超過4000個活性小分子化合物現貨,以及GPCR、API、離子通道等超過20種不同類型的化合物庫,同時提供從毫克到千克的專業定制合成服務。
MCE 對每批產品都進行嚴格的LCMS和NMR檢驗,其產品已被近萬名客戶廣泛使用并發表大量文章、;
MCE 定期增加各領域熱門抑制劑、激動劑,不斷擴增已有化合物庫,以滿足新的科研需求;
數千種產品在上海有充足備貨,24-48小時內送達客戶;
大量產品提供試用裝; 已為多個知名企業、院校構建各種定制型化合物庫。
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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