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CAS No. : 1627929-55-8
MCE 国际站:PLX51107
产品活性:PLX51107 是一种有效的,选择性的 BET 抑制剂,对 BRD2,BRD3,BRD4 和 BRDT 的 BD1 结构域的亲和力 Kd 值分别为 1.6,2.1,1.7 和 5 nM,BD2 结构域亲和力 Kd 值分别为 5.9,6.2,6.1 和 120 nM;PLX51107 同时与 CBP 和 EP300 的结构域相互作用 (Kd,∼ 100 nM)。
研究领域:Epigenetics
作用靶点:Epigenetic Reader Domain
In Vitro: PLX51107 is a potent and selective BET inhibitor, with Kds of 1.6, 2.1, 1.7, and 5 nM for BD1 and 5.9, 6.2, 6.1, and 120 nM for BD2 of BRD2, BRD3, BRD4, and BRDT, respectively. PLX51107 also interacts with the bromodomains of CBP and EP300 (Kd, in the 100 nM range). PLX51107 (0.156-10 μM) suppresses the CpG-induced proliferation of primary chronic lymphocytic leukemia (CLL) cells. PLX51107 also causes accumulation of p21 and IκBα, reduces c-MYC level, and modulates proapoptotic and antiapoptotic proteins. PLX51107 selectively modulates CLL driver genes.
In Vivo: PLX51107 (2 mg/kg, p.o.) inhibits splenomegaly by 75% in the Ba/F3 (murine IL3-dependent pro-B-cell line) splenomegaly mouse model, with the similar effect of 25 mg/kg OTX015. PLX51107 (20 mg/kg, qd, p.o.) exhibits potent antileukemic effects in disease models of aggressive chronic lymphocytic leukemia (CLL) and Richter transformation (RT) via oral administration once daily.
相关产品:Drug Repurposing Compound Library Plus | Clinical Compound Library Plus | Bioactive Compound Library Plus | Epigenetics Compound Library | Histone Modification Research Compound Library | Anti-Cancer Compound Library | Clinical Compound Library | Drug Repurposing Compound Library | Reprogramming Compound Library | Anti-Blood Cancer Compound Library | Anti-Pulmonary Fibrosis Compound Library | Heterocyclic Compound Library | Highly Selective Inhibitors 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
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货号: HY-111422
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