Pinometostat epz5676

Manufactured by Selleck Chemicals

Sourced in United States

Pinometostat EPZ5676 is a selective inhibitor of the histone methyltransferase DOT1L. It functions by binding to and inhibiting the enzymatic activity of DOT1L, which is involved in the methylation of histone H3 at lysine 79.

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EPZ5676 (14 citations) Pinometostat (5 citations)

2 protocols using pinometostat epz5676

Investigating ERα, Dot1L, and Menin Interactions

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The antibodies used for co-immunoprecipitation and/or western blot analyses were the following: anti-ERα C-terminal (F-10 sc-8002, Santa Cruz Biotechnology, Dallas, Texas), anti-ERα (ab3575) and anti-KMT4/Dot1L (ab72454) from Abcam (Cambridge, UK), anti-Dot1L (A300-953A), antimenin (A300–105 A) and anti-WSTF (BAZ1B; A300-446A) from Bethyl Laboratories (Montgomery, Alabama), anti-β-actin (A1978) from Sigma-Aldrich (Milan, Italy), Rabbit IgG Isotype Control (31,235) from Thermo Fisher (Milan, Italy). Compounds used for cell treatments were 4-hydroxytamoxifen (TAM; H7904, Sigma-Aldrich), fulvestrant (ICI; I4409, Sigma-Aldrich), 17β-estradiol (E887-5G, Sigma-Aldrich). Pharmacological inhibition was performed with EPZ004777 (S7353; only for RNA-seq experiments) and Pinometostat EPZ5676 (S7062; for all the other experiments included in the manuscript) for Dot1L and with MI-136 (S7815) and MI-503 (S7817) for menin, all purchased from Selleckchem (Houston, TX, USA). All inhibitors were dissolved in DMSO (Sigma-Aldrich), which was therefore used as a vehicle.

Salvati A., Melone V., Sellitto A., Rizzo F., Tarallo R., Nyman T.A., Giurato G., Nassa G, & Weisz A. (2022). Combinatorial targeting of a chromatin complex comprising Dot1L, menin and the tyrosine kinase BAZ1B reveals a new therapeutic vulnerability of endocrine therapy-resistant breast cancer. Breast Cancer Research : BCR, 24, 52.

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Immunoblotting for DNA Repair Proteins

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Olaparib (AZD2281), rucaparib, and pinometostat (EPZ5676) were obtained from Selleckchem. The following antibodies and reagents were obtained from the indicated suppliers: anti-BRCA2 (Bethyl Laboratories, cat. No. A311-267A, 1:5000), anti-BRCA2 ab-1 (Millipore, cat. No. OP95, 1:1000), anti-BRCA2 ab-2 (Millipore, cat. No. CA1033), anti-β-actin (Sigma, cat. No. A1978), anti-GAPDH (Millipore, cat. No. MAB374, 1:20000), anti-DOT1L (Cell Signaling, cat. No.77087), anti-RAD51 (Millipore, cat. No. ABE257 1:500), and anti-BRCA1 (Calbiochem, cat. No. OP92, 1:500), anti-phospho-γH2AX (Ser139) (Millipore, cat. No. 05-636, 1:400), anti-Vinculin (Cell signaling, cat. No. 13901, 1:1000), anti-H3K79Me (Abcam, cat. No. Ab177185 1:1000) and anti-BrdU (BD Biosciences, cat. No. 347583).

Park P.H., Yamamoto T.M., Li H., Alcivar A.L., Xia B., Wang Y., Bernhardy A.J., Turner K.M., Kossenkov A.V., Watson Z.L., Behbakht K., Casadei S., Swisher E.M., Mischel P.S., Johnson N, & Bitler B.G. (2019). Amplification of the mutation-carrying BRCA2 allele promotes RAD51 loading and PARP inhibitor resistance in the absence of reversion mutations.. Molecular cancer therapeutics, 19(2), 602-613.

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