Chemical Structure : Y08197
CAS No.:
2450965-35-0
Y08197
Catalog No.: PC-24390Not For Human Use, Lab Use Only.
Y08197 is a selective inhibitor of CBP/EP300 bromodomain, inhibits the CBP bromodomain with IC50 of 100.67 nM, high selectivity for CBP/EP300 over other bromodomain-containing proteins.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
Y08197 is a selective inhibitor of CBP/EP300 bromodomain, inhibits the CBP bromodomain with IC50 of 100.67 nM, high selectivity for CBP/EP300 over other bromodomain-containing proteins.
Y08197 (1, 5 μM) strongly affected downstream signaling transduction, thus markedly inhibiting the expression of androgen receptor (AR)-regulated genes PSA, KLK2, TMPRSS2, and oncogenes C-MYC and ERG in LNCaP, 22Rv1 and VCaP prostate cancer cells.
Y08197 potently inhibited cell growth in several AR-positive prostate cancer cell lines including LNCaP, 22Rv1, VCaP, and C4-2B.
Y08197 (1, 4, 16 μM) dose-dependently induced G0/G1 phase arrest and apoptosis in 22Rv1 prostate cancer cells.
Y08197 (5 μM) significantly decreased ERG-induced invasive capacity of 22Rv1 prostate cancer cells detected in wound-healing assay and cell migration assay.
Physicochemical Properties
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M.Wt
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436.44
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Formula
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C23H21FN4O4
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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3-Acetyl-N-(2-fluoro-5-(hydroxymethyl)-3-(1-methyl-1H-pyrazol-4-yl)phenyl)-7-methoxyindolizine-1-carboxamide
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References
1. Zou LJ, et al. Acta Pharmacol Sin. 2019 Nov;40(11):1436-1447.
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