Tak 243

Manufactured by Active Motif

TAK-243 is a small-molecule inhibitor that targets the E1 enzyme of the Ubiquitin-Proteasome System (UPS). It functions by inhibiting the activation of Ubiquitin, which is a crucial step in the ubiquitination process, leading to the degradation of target proteins.

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5 protocols using tak 243

Inhibitor Stock Solution Preparation

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Stock solutions were prepared for the following inhibitors: MG132 (Boston Biochem, I-130, 10 mm, DMSO); bortezomib (LC Laboratories, B-1408, 100 mm, DMSO); TAK243 (Active Biochem, A1384, 10 mm, DMSO); ML4924 (Boston Biochem, I-502, 20 mm, DMSO). The SAE inhibitor ML-792 (20 mm, DMSO) was kindly provided by Takeda Co.

Sha Z., Blyszcz T., González-Prieto R., Vertegaal A.C, & Goldberg A.L. (2019). Inhibiting ubiquitination causes an accumulation of SUMOylated newly synthesized nuclear proteins at PML bodies. The Journal of Biological Chemistry, 294(42), 15218-15234.

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Preparation of Inhibitor Stock Solutions

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Stock solutions were prepared for the following inhibitors: bortezomib (LC Laboratories; catalog no.: B-1408; 100 mM in dimethyl sulfoxide [DMSO]), NMS-873 (Sigma; catalog no.: SML1128; 10 mM in DMSO), pifithrin μ (Selleckchem; catalog no.: S2930; 20 mM in DMSO), TAK-243 (Active Biochem; catalog no.: A1384; 10 mM in DMSO), nelfinavir (Cayman Chemical; catalog no.: 15144; 20 mM in methanol), and Ub-aldehyde (Boston Biochem; catalog no.: U201; 1600 μM in 50 mM HCl).

Collins G.A., Sha Z., Kuo C.L., Erbil B, & Goldberg A.L. (2022). Mammalian Ddi2 is a shuttling factor containing a retroviral protease domain that influences binding of ubiquitylated proteins and proteasomal degradation. The Journal of Biological Chemistry, 298(5), 101875.

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Dose-dependent UNC8153 Inhibition Assay

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1 × 10⁴ U2OS cells per 100 μL per well were seeded in a Nunc MicroWell 96-Well Flat Clear Bottom Black Microplate (Thermo Fisher 165305). A dose−response series of 5× concentrated UNC8153 was prepared in a medium containing 50 μM MG132 (Abcam ab141003), 5 μM MLN4924 (Cayman Chemical 15217), or 5 μM TAK243 (Active Biochem A-1384). 25 μL of the 5× compound-containing mixture was added to each well, reaching a final concentration of 1× UNC8153 and 10 μM MG132, 1 μM MLN4924, or 1 μM TAK243. The plate was incubated for 6 h at 37 °C before being fixed for ICW (see the ICW protocol above).

Hanley R.P., Nie D.Y., Tabor J.R., Li F., Sobh A., Xu C., Barker N.K., Dilworth D., Hajian T., Gibson E., Szewczyk M.M., Brown P.J., Barsyte-Lovejoy D., Herring L.E., Wang G.G., Licht J.D., Vedadi M., Arrowsmith C.H, & James L.I. (2023). Discovery of a Potent and Selective Targeted NSD2 Degrader for the Reduction of H3K36me2. Journal of the American Chemical Society, 145(14), 8176-8188.

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Whole-cell Extraction and Immunoblotting

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To prepare whole-cell extracts, the cells were lysed with SDS sample buffer (50 mM Tris-HCl [pH 6.8], 10% glycerol, and 1% SDS) containing a protease inhibitor cocktail (PIC) (Nacalai Tesque). For immunoblotting using TAK-243 (catalog number MLN7243; Active Biochem), cells were lysed with radioimmunoprecipitation assay (RIPA) buffer (25 mM Tris-HCl [pH 7.6], 150 mM NaCl, 1% NP-40, 1% sodium deoxycholate, and 0.1% SDS) containing protease inhibitors.

Waku T., Nakamura N., Koji M., Watanabe H., Katoh H., Tatsumi C., Tamura N., Hatanaka A., Hirose S., Katayama H., Tani M., Kubo Y., Hamazaki J., Hamakubo T., Watanabe A., Murata S, & Kobayashi A. (2020). NRF3-POMP-20S Proteasome Assembly Axis Promotes Cancer Development via Ubiquitin-Independent Proteolysis of p53 and Retinoblastoma Protein. Molecular and Cellular Biology, 40(10), e00597-19.

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Comprehensive Epigenetic Probe Acquisition

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Epigenetic probes described in Table S1 were obtained from the Structural Genomics Consortium (Toronto, Canada). TAK-243 was purchased from Active Biochem (catalog# A-1384), pevonedistat (MLN4924/TAK-924) (catalog #15217), TAK-981 (catalog# 32741), bortezomib (catalog# 10008822), mitoxantrone (catalog# 14842), panobinostat (catalog# 13280), lenalidomide (catalog# 14643), imatinib (catalog# 13139), vincristine (catalog# 11764), cyclophosphamide (catalog# 13849), and cisplatin (catalog# 13119) from Cayman chemicals, zosuquidar (catalog# 5456) and Ko143 (catalog# 3241) from Tocris, GSK-5959 (catalog# HY-18665), inobrodib (catalog# HY-111784), and ivosidenib (catalog# HY-18767) from
MedChemExpress. cisplatin was dissolved in molecular-grade water and all other drugs were dissolved in DMSO.

Barghout S.H., Mann M.K., Aman A., Yu Y., Alteen M.G., Schimmer A.D., Schapira M., Arrowsmith C.H, & Barsyte-Lovejoy D. (2022). Combinatorial Anticancer Drug Screen Identifies Off-Target Effects of Epigenetic Chemical Probes. ACS chemical biology, 17(10).

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