GUT-70
GUT-70, a tricyclic coumarin, is a Hsp90 inhibitor. GUT-70 activates the caspase 2, 3, 8 and 9, and induces the apoptosis in leukemic cells. GUT-70 inhibits HIV-1 replication in chronically infected cells via suppression of the NF-κB pathway. GUT-70 can be used for the study of leukemic, mantle cell lymphoma (MCL) and HIV-1 infection.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 161633-75-6
- 分子式: C23H26O5
- 分子量:382.45
-
保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
製品説明
|
HSP90 |
HIV-1 |
NF-κB |
Caspase-2 |
Caspase 3 |
Caspase-8 |
Caspase-9 |
Cellular Effect
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Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| MOLT-4 | EC50 |
3.41 μM
Compound: GUT-70
|
Antiviral activity against X4 tropic Human immunodeficiency virus 1 NL4-3 infected human Molt4 cells assessed as intracellular p24 expression after 4 to 7 days by flow cytometry
Antiviral activity against X4 tropic Human immunodeficiency virus 1 NL4-3 infected human Molt4 cells assessed as intracellular p24 expression after 4 to 7 days by flow cytometry
|
[PMID: 23290051] |
| MOLT-4 | IC50 |
>10 μM
Compound: GUT-70
|
Cytotoxicity against Homo sapiens (human) MOLT4 cells by MTT assay
Cytotoxicity against Homo sapiens (human) MOLT4 cells by MTT assay
|
[PMID: 23290051] |
| Raji | IC50 |
268 molar ratio
Compound: 7
|
Inhibition of TPA-induced EBV-early antigen activation in human Raji cells assessed as early antigen activation after 48 hrs relative to control
Inhibition of TPA-induced EBV-early antigen activation in human Raji cells assessed as early antigen activation after 48 hrs relative to control
|
[PMID: 12662094] |
| TZM | IC50 |
>10 μM
Compound: GUT-70
|
Cytotoxicity against Homo sapiens (human) TZM-bl cells by MTT assay
Cytotoxicity against Homo sapiens (human) TZM-bl cells by MTT assay
|
[PMID: 23290051] |
| U1 | EC50 |
3.48 μM
Compound: GUT-70
|
Antiviral activity against Human immunodeficiency virus 1 infected U1 cells assessed as intracellular p24 expression after 24 hr by flow cytometry in presence of PMA
Antiviral activity against Human immunodeficiency virus 1 infected U1 cells assessed as intracellular p24 expression after 24 hr by flow cytometry in presence of PMA
|
[PMID: 23290051] |
| U1 | EC50 |
4.32 μM
Compound: GUT-70
|
Antiviral activity against Human immunodeficiency virus 1 infected U1 cells assessed as intracellular p24 expression after 24 hr by flow cytometry in presence of TNF-alpha
Antiviral activity against Human immunodeficiency virus 1 infected U1 cells assessed as intracellular p24 expression after 24 hr by flow cytometry in presence of TNF-alpha
|
[PMID: 23290051] |
| U1 | IC50 |
8.44 μM
Compound: GUT-70
|
Cytotoxicity against Homo sapiens (human) U1 cells by MTT assay in presence of PMA
Cytotoxicity against Homo sapiens (human) U1 cells by MTT assay in presence of PMA
|
[PMID: 23290051] |
| U1 | IC50 |
8.44 μM
Compound: GUT-70
|
Cytotoxicity against Homo sapiens (human) U1 cells by MTT assay in presence of TNF-alpha
Cytotoxicity against Homo sapiens (human) U1 cells by MTT assay in presence of TNF-alpha
|
[PMID: 23290051] |
化学情報
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CAS 番号 161633-75-6
-
分子量 382.45
-
分子式 C23H26O5
-
SMILES
O=C1C=C(CCC)C2=C3C(C=CC(C)(C)O3)=C(OC)C(C(/C(C)=C/C)=O)=C2O1
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輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[1]. Kimura S, et al. Inhibition of leukemic cell growth by a novel anti-cancer drug (GUT-70) from calophyllum brasiliense that acts by induction of apoptosis. Int J Cancer. 2005 Jan 1;113(1):158-65. [Content Brief]
[2]. Jin L, et al. Antiproliferative and proapoptotic activity of GUT-70 mediated through potent inhibition of Hsp90 in mantle cell lymphoma. Br J Cancer. 2011 Jan 4;104(1):91-100. [Content Brief]
[3]. Matsuda K, et al. Inhibition of HIV-1 entry by the tricyclic coumarin GUT-70 through the modification of membrane fluidity. Biochem Biophys Res Commun. 2015 Feb 13;457(3):288-94. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Keywords
- GUT-70
- 161633-75-6
- GUT70
- GUT 70
- HSP
- NF-κB
- HIV
- Apoptosis
- Caspase
- Heat shock proteins
- Nuclear factor-κB
- Nuclear factor-kappaB
- Human immunodeficiency virus
- Hsp90 inhibitor
- tricyclic coumarin
- caspase 2
- caspase 3
- caspase 8
- caspase 9
- apoptosis
- NF-κB pathway
- HIV-1 replication
- leukemic
- mantle cell lymphoma
- Inhibitor
- inhibitor
- inhibit