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prmt5 inhibitor gsk3326595  (MedChemExpress)


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    MedChemExpress prmt5 inhibitor gsk3326595
    Prmt5 Inhibitor Gsk3326595, supplied by MedChemExpress, used in various techniques. Bioz Stars score: 95/100, based on 40 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
    https://www.bioz.com/result/prmt5 inhibitor gsk3326595/product/MedChemExpress
    Average 95 stars, based on 40 article reviews
    prmt5 inhibitor gsk3326595 - by Bioz Stars, 2026-06
    95/100 stars

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    sam cooperative prmt5 inhibitor  (Selleck Chemicals)
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    Selleck Chemicals sam cooperative prmt5 inhibitor
    Figure 10. TNG462 treatment drives dose-dependent and durable PD activity in the LU99 MTAP-null NSCLC xenograft model. PK/PD analysis of TNG462 following compound treatment for 7-days. (A) <t>PRMT5</t> activity by quantification of a single SDMA-modified protein substrate and free TNG462 plasma concentrations were determined at the indicated time points postlast dose. N = 4 tumors/time point/dose level. Data are presented as mean ± SEM for the PD analyses. (B) SDMA-modified protein levels in tumors collected at the indicated time points postlast dose. TNG908 was dosed at 120 mg/kg BID and TNG462 was dosed at 30 mg/kg BID for 7-days. N = 4 tumors/time point/treatment. Data are presented as mean ± SEM. (C) Cellular thermostability assay where the LN18 MTAP-null cancer cell line was treated with TNG462 at the indicated concentrations and treatment conditions.
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    Figure 10. TNG462 treatment drives dose-dependent and durable PD activity in the LU99 MTAP-null NSCLC xenograft model. PK/PD analysis of TNG462 following compound treatment for 7-days. (A) PRMT5 activity by quantification of a single SDMA-modified protein substrate and free TNG462 plasma concentrations were determined at the indicated time points postlast dose. N = 4 tumors/time point/dose level. Data are presented as mean ± SEM for the PD analyses. (B) SDMA-modified protein levels in tumors collected at the indicated time points postlast dose. TNG908 was dosed at 120 mg/kg BID and TNG462 was dosed at 30 mg/kg BID for 7-days. N = 4 tumors/time point/treatment. Data are presented as mean ± SEM. (C) Cellular thermostability assay where the LN18 MTAP-null cancer cell line was treated with TNG462 at the indicated concentrations and treatment conditions.

    Journal: Journal of medicinal chemistry

    Article Title: Discovery of TNG462: A Highly Potent and Selective MTA-Cooperative PRMT5 Inhibitor to Target Cancers with MTAP Deletion.

    doi: 10.1021/acs.jmedchem.4c03067

    Figure Lengend Snippet: Figure 10. TNG462 treatment drives dose-dependent and durable PD activity in the LU99 MTAP-null NSCLC xenograft model. PK/PD analysis of TNG462 following compound treatment for 7-days. (A) PRMT5 activity by quantification of a single SDMA-modified protein substrate and free TNG462 plasma concentrations were determined at the indicated time points postlast dose. N = 4 tumors/time point/dose level. Data are presented as mean ± SEM for the PD analyses. (B) SDMA-modified protein levels in tumors collected at the indicated time points postlast dose. TNG908 was dosed at 120 mg/kg BID and TNG462 was dosed at 30 mg/kg BID for 7-days. N = 4 tumors/time point/treatment. Data are presented as mean ± SEM. (C) Cellular thermostability assay where the LN18 MTAP-null cancer cell line was treated with TNG462 at the indicated concentrations and treatment conditions.

    Article Snippet: The SAM-cooperative PRMT5 inhibitor, GSK3326595, was sourced from Selleck Chemicals and maintained as a 10 mM DMSO stock.

    Techniques: Activity Assay, Modification, Clinical Proteomics