化合物SPHINX31 T5194

Product Introduction
Bioactivity


英文名: SPHINX31

描述: 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。

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].

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].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: Ethanol : 10 mg/mL
H2O : Insoluble
DMSO : 5.08 mg/mL (10 mM)


关键字: SPHINX-31 | Serine-arginine protein kinases | retinal permeability | eye disease | neovascular | SPHINX 31 | Inhibitor | Norway Brown rats | SRPK | SPHINX31 | inhibit | Vascular endothelial growth factor receptor | HuCCA-1 | VEGFR | diabetics | angiogenic

相关产品: Fasudil | CRT0066101 | Chymotrypsin | HTH-01-091 | Piceatannol | 1-NM-PP1 | SRPKIN-1 | WNK-IN-11 | SBC-110736 | FOY 251

相关库: Anti-Aging Compound Library | Cell Cycle Compound Library | Anti-Cancer Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Kinase Inhibitor Library | Apoptosis Compound Library | Metabolism Compound Library | NO PAINS Compound Library | Bioactive Compound Library

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