货号	规格	价格	上海	北京	珠海	重庆	武汉	购买数量
T93558-1ml促销	10mM in DMSO	￥720.00 ￥648.00 T93558-1ml ￥648.00 现货	9 9	-	-	-	-

货号

规格

价格

上海

北京

珠海

重庆

武汉

购买数量

T93558-1ml促销

10mM in DMSO

￥720.00 ￥648.00

产品描述：

丝氨酸/苏氨酸激酶抑制剂;Serine/threonin kinase Inhibitors;;InformationSPHINX31 SPHINX31 is a SRPK1 inhibiror with an IC50 of 5.9 nM with highly selectivity for SRPK1 over SRPK2 (50-fold) and CLK1 (100-fold).TargetsSRPK1 (Cell-free assay) 5.9 nMIn vitroKinase assays showed that SPHINX31 is a type 1 kinase inhibitor (ATP competitive). SPHINX31 treatment results in inhibition of SRSF1 phosphorylation at 300 nM in PC3 prostate cancer cells. Metabolic stability in mouse liver microsomes shows that SPHINX31 had medium clearance with a T1/2 of 95.79 min. Inhibition of SRPK1 using SPHINX31 leads to cell cycle arrest and leukemic cell differentiation.In vivoSPHINX31 could penetrate into the eye. SPHINX31 exerts a dose dependent inhibition of choroidal neovascularisation in mouse model. SPHINX31 inhibits blood vessel growth and macrophage infiltration. SPHINX31 treatment prolongs survival of immunocompromised mice transplanted with MLL-rearranged AML cells.Cell Research(from reference)Cell lines：THP1 cells Concentrations：3\u2009µM Incubation Time：24 h

靶点：

IC50: 5.9 nM (SRPK1);VEGF-A165a

体内研究：

SPHINX31 (200 μg/mL；每日两次外用滴眼液) 保护视网膜内皮通透性屏障免受糖尿病相关完整性丧失的影响。

参考文献：

1. Batson J, et al. Development of Potent, Selective SRPK1 Inhibitors as Potential Topical Therapeutics for Neovascular Eye Disease. ACS Chem Biol. 2017 Mar 17;12(3):825-832.
2. Supradit K, et al. Inhibition of serine/arginine-rich protein kinase-1 (SRPK1) prevents cholangiocarcinoma cells induced angiogenesis. Toxicol In Vitro. 2022 Aug;82:105385.
3. C. Allen, et al. The SRPK1 inhibitor SPHINX31 prevents increased retinal permeability in a rodent model of diabetes. Acta Ophthalmologica. Volume 95, Issue S259.

保存条件：

-80℃（运输条件：冰袋低温运输）

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.97 ml	9.852 ml	19.704 ml
5 mM	0.394 ml	1.97 ml	3.941 ml
10 mM	0.197 ml	0.985 ml	1.97 ml
50 mM	0.039 ml	0.197 ml	0.394 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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