BRD-810作为一种新型MCL1抑制剂,通过抑制MCL1的功能,阻断了其与促凋亡蛋白的结合,从而恢复了肿瘤细胞的凋亡途径。 2024年8月,Nature cancer上发表了题为“BRD-810 Is A Highly Selective MCL1 Inhibitor with Optimized in Vivo Clearance...
S63845 is a selective myeloid leukemia 1(MCL1) inhibitor that binds to human MCL1 with a Kd of 0.19 nM. 靶点活性 MCL1:0.19 nM (Kd) 体外活性 方法:S63845(0.001-10μM)处理HCT-116细胞,Western blot分析细胞中MCL1和BCL-XL蛋白水平。
In this study, we show that the MCL1 inhibitor S64315 reduces melanoma tumor growth in an immune cell-dependent manner in mice. Specifically, S64315 enhances antitumor immunity by reducing MDSC frequency and by promoting the activity of CD8+T cells. Additionally, human MDSCs are 10 times more...
Mcl1-IN-1 is a myeloid cell factor 1 inhibitor (IC50=2.4 μM). 规格价格库存数量 2 mg ¥ 1,890 5日内发货 5 mg ¥ 2,890 5日内发货 25 mg ¥ 9,620 6-8周 50 mg ¥ 12,500 6-8周 100 mg ¥ 17,500 6-8周 1 mL x 10 mM (in DMSO) ¥ 2,790 5日内发货 ...
MlM1, a hydrocarbon-stapled MCL1 inhibitor, exhibited apoptosis-inducing efficacy in leukemia cells. Bl97C1, Bl112D1 and TW-37, that are developed with improved and selective affinity in binding to MCL1, induced apoptosis in a BAX/BAK- and caspase-9-dependent manner. Combination of ABT-263 ...
Interestingly, primary cells from a patient in progression under venetoclax treatment were not sensitive ex vivo to neither venetoclax nor to MCL1 inhibitor, whereas the combination of both efficiently induced cell death. This finding suggests that the combination could overcome venetoclax resistance. The...
In contrast, S227928 + venetoclax was active in 9/14 primary AML cases, comparable to non-conjugated MCL1 inhibitor + venetoclax (activity in 9/14) and greater than either unconjugated anti-CD74 + venetoclax (activity in 3/14) or an isotype-conjugated MCL1 inhibitor control (activity in 0/...
2b). An IC50 study showed that MCL1-positive MMCLs, except for U266 cells, were sensitive to the MCL1 inhibitor (Fig. 1g). Early PCs were sensitive to BCL-XL inhibition, while tumor PCs were resistant. SKMM2 and XG21 cells were sensitive to venetoclax, and all eight MMCLs were ...
Mcl1-IN-3 is an inhibitor of Mcl1 extracted from patent WO2015153959A2, compound example 57; has an IC50 and Ki of 0.67 and 0.13 μM, respectively. IC50 & Target IC50: 0.67 μM (Mcl1)[1] Ki: 0.13 μM (Mcl1) [1] 分子量 487.93 Formula C27H22ClN3O4 CAS 号 1814891-79-6 ...
Kotschy, A., Szlavik, Z., Murray, J.et al.The MCL1 inhibitor S63845 is tolerable and effective in diverse cancer models.Nature538, 477–482 (2016). https://doi.org/10.1038/nature19830 Download citation Received19 July 2016 Accepted07 September 2016 ...