Name: I-BET151 (GSK1210151A)
Price: 254.00 USD

- Overview
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    Background
    
    I-BET151 (GSK1210151A) is a selective inhibitor of BET with pIC50 value of 6.1 [1].BET (bromo and extraterminal) is a member of bromodomain family and has been shown to be associated with a variety of diseases (human squamous cell carcinoma and other cancers). BET inhibitor has been implicated as a promising therapy for human cancer treatment [2].I-BET151 is a selective BET inhibitor and has the similar inhibition function as TMZ. When tested with 6 myeloma cell lines, I-BET151 treatment decreased cells percent in S/G2 phase and increased cell apoptosis in a time- and dose- dependent manner [2]. In globlastoma cell line U87MG, administration of I-BET151 arrested cells in the G1 phase and reduced cell proliferation ability [3]. When treated with myeloma implanted mouse model with I-BET151, it reduced tumor volume in a four- or five- fold compared with control group [2]. In immunocompromised mouse model with U87MG cells xenograft, administration of I-BET151 in a concentration of 10 mg/kg i.p. daily significantly reduced tumor volume compared with saline treated group [3].
    
    [1]. Seal, J., et al., Identification of a novel series of BET family bromodomain inhibitors: binding mode and profile of I-BET151 (GSK1210151A). Bioorg Med Chem Lett, 2012. 22(8): p. 2968-72.
    [2]. Chaidos, A., et al., Potent antimyeloma activity of the novel bromodomain inhibitors I-BET151 and I-BET762. Blood, 2014. 123(5): p. 697-705.
    [3]. Chan, C.H., et al., BET bromodomain inhibition suppresses transcriptional responses to cytokine-Jak-STAT signaling in a gene-specific manner in human monocytes. Eur J Immunol, 2015. 45(1): p. 287-97.
- Properties
  - Alternative Name
    
    7-(3,5-dimethyl-1,2-oxazol-4-yl)-8-methoxy-1-[(1R)-1-pyridin-2-ylethyl]-3H-imidazo[4,5-c]quinolin-2-one
    
    CAS Number
    
    1300031-49-5
    
    Molecular Formula
    
    C23H21N5O3
    
    Molecular Weight
    
    415.44
    
    Appearance
    
    A crystalline solid
    
    Purity
    
    98.00%
    
    Solubility
    
    ≥41.5 mg/mL in DMSO; insoluble in H2O; ≥19.5 mg/mL in EtOH
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Xiaojie Ma, Yunkun Lu, et al. "Human expandable pancreatic progenitor-derived β cells ameliorate diabetes." Sci Adv. 2022 Feb 25;8(8):eabk1826. PMID:35196077
    2. Tan X, Tong J, et al. "BET inhibitors potentiate chemotherapy and killing of SPOP-mutant colon cancer cells via induction of DR5." Cancer Res. 2019 Jan 23. pii: canres.3223.2018. PMID:30674532
    3. Piunti A, Hashizume R, et al. "Therapeutic targeting of polycomb and BET bromodomain proteins in diffuse intrinsic pontine gliomas." Nat Med. 2017 Apr;23(4):493-500. PMID:28263307

I-BET151 (GSK1210151A)

I-BET151 (GSK1210151A)

Background

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