Powder: -20°C for 3 years | In solvent: -80°C for 1 year
SPHINX31 是丝氨酸/富含精氨酸的蛋白激酶1的选择性抑制剂,其IC50值为 5.9 nM。它有效抑制丝氨酸/丰富精氨酸的剪接因子1 磷酸化,有用于局部新生血管性眼病的研究潜力。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 319 | 现货 | ||
5 mg | ¥ 739 | 现货 | ||
10 mg | ¥ 996 | 现货 | ||
25 mg | ¥ 1,780 | 现货 | ||
50 mg | ¥ 2,890 | 现货 | ||
100 mg | ¥ 4,370 | 现货 | ||
500 mg | ¥ 9,420 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 833 | 现货 |
产品描述 | SPHINX31 is a potent inhibitor of serine/arginine-rich protein kinase 1 (SRPK1; IC50: 5.9 nM). |
靶点活性 | SRPK1:5.9 nM (cell free) |
体外活性 | SPHINX31 inhibits phosphorylation of serine/arginine-rich splicing factor 1 (SRSF1), an SRPK1 substrate, in PC3 cells (EC50: 360 nM) and increases expression of the anti-angiogenic VEGF-A165b splice variant in retinal pigment epithelial (RPE) cells [1]. SPHINX31 inhibited the growth of MLL-mutant AML cell lines with an IC50? >1 order of magnitude lower than for other AML lines. There was no impact of SPHINX31 on the clonogenic potential of normal mouse hematopoietic stem-progenitor cells (HSPCs). 1.5, 3, and 6?μM SPHINX31 did not affect the colony-forming ability of normal human cord blood CD34+ cells [2]. |
体内活性 | In vivo, SPHINX31 (2 μg per eye) inhibits blood vessel growth and macrophage infiltration in the eyes of a mouse model of choroidal neovascularization [1]. Injection of 0.8?mg/kg SPHINX31 (i.p.) into DBA2J mice resulted in a concentration of 0.225?±?0.036?μM in plasma after 24?h. In xenotransplanted RAIL mice with MOLM-13, THP-1 cells or first passage patient-derived AMLs, SPHINX31 (0.8 or 2.0 mg/kg) led to a significant reduction in leukemic cell growth and a dose-dependent prolongation of survival of mice given MOLM-13, THP-1, and patient-derived MLL-X AMLs [2]. |
细胞实验 | Cells were transduced with gRNA vectors or treated with SPHINX31 and stained at the indicated time points with anti-mouse CD11b PE/Cy5 and anti-human CD11b PE or anti-human CD13 FITC. Data were analyzed by using LSRFortessa and FlowJo. Apoptosis levels were measured in human and/or mouse AML cells transduced with dual gRNA vectors (against SRPK1 and 3' BCL2 enhancer) and/or treated with 1 or 3?μM SPHINX31 at indicated time points, by using Annexin V. Data were analyzed by using LSRFortessa instruments. Cell cycle stages were measured in human and/or mouse AML cells transduced with dual gRNA vectors against SRPK1 and/or treated with 1 or 3?μM SPHINX31 at indicated time points, using Propidium Iodide. Data were analyzed using LSRFortessa instruments [2]. |
动物实验 | For in vivo experiments, 6–10-week-old female Rosa26Cas9/+ mice were treated triweekly for two weeks with either vehicle or 2?mg/kg SPHINX31. Four weeks post-treatment, bone marrow cells from these mice were freshly extracted (as mentioned above) and blocked with anti-mouse CD16/32 and 10% mouse serum. For the identification of LK/LSK, LT-HSC, myeloid and B-cell subpopulations, staining was performed using CD4 PE/Cy5, CD5 PE/Cy5, CD8a PE/Cy5, CD11b PE/Cy5, B220 PE/Cy5, TER-119 PE/Cy5, GR-1 PE/Cy5, SCA-1 Pacific Blue, CD150 PE/Cy7, CD34 FITC and CD117 APC-eFluor780. In each of the multi-colour flow cytometry experiments, we included the fluorescence minus one (FMO) controls. FMO controls provide a measure of spillover in a given channel. This allows for correct gating and selects only the stained cells in the experimental sample. Flow cytometry analysis was performed using a LSRFortessa instrument and resulting data were subsequently analyzed using FlowJo [2]. |
分子量 | 507.51 |
分子式 | C27H24F3N5O2 |
CAS No. | 1818389-84-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 10 mg/mL
H2O: Insoluble
DMSO: 20 mg/mL
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
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