MCE 的所有產品僅用作科學研究或藥證申報，我們不為任何個人用途提供產品和服務。

(+)-JQ-1

CAS No. : 1268524-70-4

MCE 國際站：(+)-JQ-1

產品活性：(+)-JQ-1 (JQ1) 是一種有效特異性的可逆 BET bromodomain 抑制劑，抑制 BRD4(1/2) 的 IC₅₀ 分別為 77 nM 和 33 nM。(+)-JQ-1 激活自噬 (autophagy)。

研究領域：Epigenetics  |  Autophagy  |  PROTAC

作用靶點：Epigenetic Reader Domain  |  Autophagy  |  Ligands for Target Protein for PROTAC

In Vitro: (+)-JQ-1 represents a potent, highly specific and Kac competitive inhibitor for the BET family of bromodomains. (+)-JQ-1 (100 nM, 48 h) prompts squamous differentiation exhibited by cell spindling, flattening and increased expression of keratin. (+)-JQ-1 (250 nM) induces rapid expression of keratin in treated NMC 797 cells compared to (-)-JQ1 (250 nM) and vehicle controls, as determined by quantitative immunohistochemistry.(+)-JQ-1 (250 nM) elicits a time-dependent induction of strong (3+) keratin staining of treated NMC 797 cells, compared to (-)-JQ1 (250 nM). De-repression of autophagy genes is observed almost immediately after (+)-JQ-1 addition. (+)-JQ-1 is a potent thienodiazepine inhibitor (K_d=90 nM) of the BET family coactivator protein BRD4, which is implicated in the pathogenesis of cancer via transcriptional control of the MYC oncogene. Dose-ranging studies of (+)-JQ-1 demonstrates potent inhibition of H4Kac4 binding with a IC₅₀ value of 10 nM for murine BRDT(1) and 11 nM for human BRDT(1).

In Vivo: Matched cohorts of mice with established tumors are randomized to treatment with (+)-JQ1 (50 mg/kg) or vehicle, administered by daily intraperitoneal injection. Prior to randomization, and after four days of therapy, mice are evaluated by FDG-PET imaging. A marked reduction in FDG uptake is observed with (+)-JQ1 treatment. Tumor-volume measurements confirm a reduction in tumor growth with JQ1 treatment. Pharmacokinetic studies of (+)-JQ1 are performed in CD1 mice following intravenous and oral administration. Mean plasma concentration-time profiles of (+)-JQ1 after intravenous dosing (5 mg/kg). The pharmacokinetic parameters for intravenous (+)-JQ1 demonstrate excellent drug exposure (AUC=2090 hr*ng/mL) and an approximately one hour half-life (T1/2). Mean plasma concentration-time profiles of (+)-JQ1 after oral dosing (10 mg/kg). The pharmacokinetic parameters for oral (+)-JQ1 demonstrate excellent oral bioavailability (F=49%), peak plasma concentration (C_max=1180 ng/mL) and drug exposure (AUC=2090 hr*ng/mL).

相關產品：Bioactive Compound Library Plus  |  Epigenetics Compound Library  |  Histone Modification Research Compound Library  |  Anti-Cancer Compound Library  |  CNS-Penetrant Compound Library  |  Autophagy Compound Library  |  Reprogramming Compound Library  |  Chemical Probe Library  |  Anti-Blood Cancer Compound Library  |  Target Protein Ligand Library  |  Heterocyclic Compound Library  |  Highly Selective Inhibitors Library  |  Highly Selective Activators Library  |  Cell Death 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  |  Abemaciclib metabolite M18 hydrochloride  |  PROTAC Bcl-xL ligand-1  |  Ziftomenib  |  GSK761  |  XX-650-23  |  KB02-JQ1  |  CD235  |  I-BET151  |  VZ185  |  BET-IN-6  |  PLK1/BRD4-IN-1  |  MI-136  |  AP1867-2-(carboxymethoxy)

熱門產品線：重組蛋白  |  化合物庫  |  天然產物  |  熒光染料  |  PROTAC  |  同位素標記物  |  寡核苷酸  |  抗體  |  點擊化學

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Fluorescent Dye  |  PROTAC  |  Isotope-Labeled Compounds  |  Oligonucleotides  |  Antibodies  |  Click Chemistry