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Merck

SML3234

Sigma-Aldrich

GSK778 Hydrochloride

≥98% (HPLC)

别名:

4-{2-(Methoxymethyl)-1-[(R)-1-phenylethyl]-8-[(S)-pyrrolidin-3-ylmethoxy]-1H-imidazo[4,5-c]quinolin-7-yl}-3,5-dimethylisoxazole Hydrochloride, iBET-BD1 Hydrochloride

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About This Item

经验公式(希尔记法):
C30H33N5O3 · xHCl
分子量:
511.61 (free base basis)
MDL號碼:
分類程式碼代碼:
12352200
NACRES:
NA.77

品質等級

化驗

≥98% (HPLC)

形狀

powder

儲存條件

desiccated

顏色

white to beige

溶解度

DMSO: 2 mg/mL, clear

儲存溫度

2-8°C

SMILES 字串

C[C@H](C1=CC=CC=C1)N2C(COC)=NC3=C2C(C=C4OC[C@@H]5CNCC5)=C(N=C3)C=C4C6=C(C)ON=C6C

生化/生理作用

GSK778 (iBET-BD1) is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. GSK778 (iBET-BD1) potently inhibits numerous cancer cells proliferation, inducing cell cycle arrest and apoptosis.

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable


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Structure-Based Design of a Bromodomain and Extraterminal Domain (BET) Inhibitor Selective for the N-Terminal Bromodomains That Retains an Anti-inflammatory and Antiproliferative Phenotype
Soden PE, Taylor S, Watson RJ, Willis R, Woolven JM, Wyspianska BS, Kerr WJ, Prinjha RK
Journal of Medicinal Chemistry, 63, 9020-9044 (2020)
Omer Gilan et al.
Science (New York, N.Y.), 368(6489), 387-394 (2020-03-21)
The two tandem bromodomains of the BET (bromodomain and extraterminal domain) proteins enable chromatin binding to facilitate transcription. Drugs that inhibit both bromodomains equally have shown efficacy in certain malignant and inflammatory conditions. To explore the individual functional contributions of

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