Name | SPHINX31 |
Description | SPHINX31 is a potent inhibitor of serine/arginine-rich protein kinase 1 (SRPK1; IC50: 5.9 nM). |
Cell Research | 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]. |
Animal Research | 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]. |
In vitro | SPHINX31抑制了PC3细胞中丝/精氨酸富集剪接因子1(SRSF1)的磷酸化,该因子是SRPK1的底物(EC50:360nM),并在视网膜色素上皮(RPE)细胞中增加了抗血管生成VEGF-A165b剪接变体的表达[1]。对于MLL突变的AML细胞系,SPHINX31抑制生长,其IC50远低于其他AML细胞系,超过一个数量级。SPHINX31对正常小鼠造血干-祖细胞(HSPCs)的集落形成潜能没有影响。1.5、3和6μMSPHINX31并不影响正常人脐血CD34+细胞的集落形成能力[2]。 |
In vivo | 在体内,SPHINX31(每只眼2μg)抑制了小鼠脉络膜新生血管模型中的血管生长和巨噬细胞浸润[1]。向DBA2J小鼠注射0.8mg/kg SPHINX31(i.p.)后,24小时内血浆中的浓度达到0.225±0.036μM。在接受MOLM-13、THP-1细胞或第一次传导的患者源AMLs的异种移植RAIL小鼠中,SPHINX31(0.8或2.0 mg/kg)显著减少了白血病细胞的生长,并且随剂量增加显著延长了接受MOLM-13、THP-1和源于患者的MLL-X AMLs的小鼠的存活时间[2]。 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | Ethanol : 10 mg/mL H2O : Insoluble DMSO : 5.08 mg/mL (10 mM)
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Keywords | 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 |
Inhibitors Related | SRPIN340 | SBC-115076 | Camostat mesylate | Fasudil hydrochloride | PCSK9-IN-10 | BMT-124110 Formate | FOY 251 | Cetraxate hydrochloride | Benzamidine hydrochloride | HA-1004 | CID755673 | Nafamostat mesylate |
Related Compound Libraries | Inhibitor Library | Bioactive Compound Library | Anti-Cancer Compound Library | Bioactive Compounds Library Max | Cell Cycle Compound Library | Metabolism Compound Library | Kinase Inhibitor Library | Apoptosis Compound Library | NO PAINS Compound Library | Target-Focused Phenotypic Screening Library |