SGC-CBP30

SGC-CBP30

Catalog Number:
L002369247APE
Mfr. No.:
APE-A4491
Price:
$306
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      • Overview
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          Background

          SGC-CBP 30 is a selective inhibitor of CREBBP and EP300 with IC50 value of 21 nM and 38 nM, respectively [1]. EP300 (E1A binding protein p300) is encoded by EP300 gene and plays an important role in regulating cell growth and division, prompting cells mature and assume specialized functions, and preventing tumor cells growth. CREBBP (CREB-binding protein) is encoded by CREBBP gene and involves in the transcriptional coactivation of many different transcription factors [2].

          [1]. Duncan A. Hay, Oleg Fedorov, Sarah Martin, et al. Discovery and Optimization of Small-Molecule Ligands for the CBP/p300 Bromodomains [J]. J. Am. Chem. Soc., 2014, 136 (26), pp 9308–9319.
          [2]. van Belzen M, Bartsch O, Lacombe D, et al. Rubinstein-Taybi syndrome (CREBBP, EP300) [J]. Eur J Hum Genet. 2011 Jan; 19(1):preceeding 118-20.

      • Properties
        • Alternative Name
          SGCCBP30,SGC CBP30; 4-[(2S)-1-[2-[2-(3-chloro-4-methoxyphenyl)ethyl]-5-(3,5-dimethyl-1,2-oxazol-4-yl)benzimidazol-1-yl]propan-2-yl]morpholine
          CAS Number
          1613695-14-9
          Molecular Formula
          C28H33ClN4O3
          Molecular Weight
          509.04
          Purity
          98.09%
          Solubility
          ≥20.05 mg/mL in DMSO; ≥25.7 mg/mL in EtOH with ultrasonic; ≥4.67 mg/mL in H2O with ultrasonic
          Storage
          Store at 4°C

          * For Research Use Only

      • Reference
        • 1. Te Zhang, Xuming Song, et al. "Aberrant super-enhancer landscape reveals core transcriptional regulatory circuitry in lung adenocarcinoma." Oncogenesis. 2020 Oct 17;9(10):92. PMID:33070167
          2. Li N, Yang L, et al. "BET bromodomain inhibitor JQ1 preferentially suppresses EBV-positive nasopharyngeal carcinoma cells partially through repressing c-Myc." Cell Death Dis. 2018 Jul 9;9(7):761. PMID:29988031
          3. Alonso, Victoria Lucia, et al. "Overexpression of bromodomain factor 3 in Trypanosoma cruzi (TcBDF3) affects differentiation of the parasite and protects it against bromodomain inhibitors." FEBS Journal (2016). PMID:27007774

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