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Cat No.: 1268524-70-4
Biological Description:(+)-JQ1 is a BET bromodomain inhibitor, with IC50 of 77 nM/33 nM for BRD4(1/2).IC50 Value: 77 nM(for BRD4(1)); 33 nM( for BRD4(2))Target: BRD4in vitro: (+)-JQ1 enantiomer binds directly into the Kac binding site of BET bromodomains. (+)-JQ1 (500 nM) binds BRD4 competitively with chromatin resulting in differentiation and growth arrest of NMC cells. (+)-JQ1 (500 nM) attenuates rapid proliferation of NMC 797 and Per403 cell lines as demonstrated by reduced Ki67 staining. (+)-JQ1 (500 nM) potently decreases expression of both BRD4 target genes in NMC 797 cells. (+)-JQ1 inhibits cellular viability with IC50 of 4 nM in NMC 11060 cells. (+)-JQ1 results in robust inhibition of MYC expression in MM cell lines. (+)-JQ1 inhibits proliferating of KMS-34 and LR5 with IC50 of 68 nM and 98 nM, respectively. (+)-JQ1 (500 nM)-treated MM.1S cells results in a pronounced decrease in the proportion of cells in S-phase, with a concomitant increase in cells arrested in G0/G1. (+)-JQ1 (500 nM) results in pronounced cellu...Purity: >98%Molecular formula: C23H25ClN4O2SMolecular Weight: 456.99Storage Instructions: Two years -20°C Powder, 2 weeks4°C in DMSO,6 months-80°C in DMSOReferences: for more information, please visit images/AffixScientific/ Affix Scientific的KRN633是一种有效的选择性VEGFR抑制剂。抑制人脐静脉内皮细胞中VEGFR-2的酪氨酸磷酸化(IC50 = 1.16 nmol / L)。用重组酪氨酸激酶进行的选择性分析表明,KRN633对VEGFR-1,-2和-3具有高度选择性。在无胸腺小鼠和大鼠中,KRN633在几种具有不同组织起源的体内肿瘤异种移植模型(包括肺,结肠和前列腺)中抑制肿瘤生长。KRN633还可以使一些公认的肿瘤以及那些在停止治疗后已长出的肿瘤消退。KRN633具有良好的耐受性,对动物的体重或总体健康没有明显影响。KRN633可用于治疗实体瘤和其他依赖病理性血管生成的疾病。