| Description | ISA-2011B is an inhibitor of PIP5K1α and can be used in anticancer studies. |
| In vitro | ISA-2011B显著降低22Rv1细胞核和胞浆中的AR-V7和CDK1水平。ISA-2011B对PIP5K1α以及across 460 kinases中的MAP/microtubule affinity-regulating kinase 1和4（MARK1和MARK4）展现出较高的亲和力。ISA-2011B处理使PC-3细胞中PIP5K1α表达量降低78.6%[1]。ISA-2011B处理还能清除核内的AR表达，而不消耗胞浆中的AR[2]。使用10, 20, 50 μM ISA-2011B处理PC-3细胞后，其增殖率明显下降至对照组的58.77%、48.65%及21.62%。 |
| In vivo | AR-V7的过表达增加了PIP5K1α的表达，促进了异种移植小鼠中前列腺癌（PCa）的快速生长，而通过其抑制剂ISA-2011B抑制PIP5K1α可以抑制过表达AR-V7的异种移植肿瘤的生长和侵袭性。ISA-2011B显著抑制了异种移植小鼠中肿瘤细胞的生长，并通过靶向与PIP5K1α相关的PI3K/AKT及其下游的生存、增殖和侵袭途径来介导此作用[1]。ISA-2011B通过破坏依赖于PIP5K1α的AR-V7的蛋白稳定性，从而抑制了异种移植小鼠中AR-V7高表达肿瘤的侵袭性生长[2]。 |
| molecular weight | 423.85 |
| Molecular formula | C22H18ClN3O4 |
| CAS | 1395347-24-6 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 100 mg/mL (235.93 mM), Sonication is recommended. |
| References | 1. Sarwar M, et al. Targeted suppression of AR-V7 using PIP5K1α inhibitor overcomes MDV3100 resistance in prostate cancer cells. Oncotarget. 2016 Sep 27;7(39):63065-63081. 2. Semenas J, et al. The role of PI3K/AKT-related PIP5K1α and the discovery of its selective inhibitor for treatment of advanced prostate cancer. Proc Natl Acad Sci U S A. 2014 Sep 2;111(35):E3689-98. |