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CAS No. : 1883548-89-7
MCE 国际站：NI-57
产品活性：NI-57 为溴结构域和植物同源锌指结构域 (BRPF) 蛋白家族的抑制剂，对 BRPF1，BRPF2 (BRD1) 和 BRPF3 的 IC50 值分别为 3.1，46 和 140 nM。
研究领域：Epigenetics
In Vitro: NI-57 is an inhibitor of bromodomain and plant homeodomain finger-containing (BRPF), with IC50s of 3.1, 46 and 140 nM for BRPF1, BRPF2 (BRD1) and BRPF3, respectively. NI-57 binds the BRD of BRPF1 with a Kd of 31 ± 2 nM, BRD1 with a Kd of 110 ± 13 nM, and BRPF3 with a Kd of 410 ± 47 nM, whereas binding to BRD9 is weaker (Kd 1000 ± 130 nM) measured by isothermal titration calorimetry. NI-57 shows less active effect on BRD9 (IC50, 520 nM) and BRD4 (BD1) (IC50, 3700 nM), TRIM24 (IC50, 1600 nM). NI-57 also inhibits BRPF BRDs in the nucleus, but shows little effect on the proliferation of many cancer cell lines with GI50s of 10.4 μM (NCI-H1703 cells), 14.7 μM (DMS114), 15.6 μM (HRA-19), and 16.6 μM (RERF-LC-Sq1). Furthermore, Inhibition on BRPF1 of NI-57 (10 μM) reduces the gene expression of CCL-22 by 27.7 ± 9.4%.
In Vivo: NI-57 has favorable oral bioavailability in mice.
相关产品：Bioactive Compound Library Plus | Epigenetics Compound Library | Immunology/Inflammation Compound Library | Histone Modification Research Compound Library | Anti-Cancer Compound Library | Reprogramming Compound Library | Chemical Probe Library | Anti-Blood Cancer Compound Library | BRD4 Inhibitor-18 | ACBI2 | BI01826025 | Curcumin | GSK6853 | MI-1 | GSK 4027 | ZL0590 | BRD4 Inhibitor-26 | Apabetalone | PROTAC BRD2/BRD4 degrader-1 | MS645 | OF-1 | I-CBP112 | BRM/BRG1 ATP Inhibitor-2 | UMB-32 | Ziftomenib | GSK761 | XX-650-23 | KB02-JQ1 | CD235 | I-BET151 | VZ185 | BET-IN-6 | PLK1/BRD4-IN-1 | MI-136 | SF2523 | SNIPER(BRD)-1 | Anacardic Acid
热门产品线：重组蛋白 | 化合物库 | 天然产物 | 荧光染料 | PROTAC | 同位素标记物 | 寡核苷酸 | 抗体 | 点击化学
Trending products：Recombinant Proteins | Bioactive Screening Libraries | Natural Products | Fluorescent Dye | PROTAC | Isotope-Labeled Compounds | Oligonucleotides | Antibodies | Click Chemistry
货号: HY-19537
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