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CAS No.: 1818389-84-2

SPHINX31 Catalog No. CSN23673

SPHINX31 is a potent and selective inhibitor of serine/arginine-rich protein kinase 1 (SRPK1), with an IC50 of 5.9 nM. SPHINX31 inhibits phosphorylation of serine/arginine-rich splicing factor 1 (SRSF1). SPHINX31 is a potential topical therapeutic for neovascular eye disease[1].

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技术信息

生物活性

描述SRPK1 (serine/arginine-protein kinase 1) regulates splicing of pro-angiogenic VEGFA₁₆₅a through phosphorylation of SRSF1, enabling SRSF1 nuclear translocation and binding to the proximal splice site in VEGF-A pre-mRNA. SPHINX31 is a highly selective SRPK1 inhibitor with IC50 value of 6nM. Treatment with SPHINX31 dose-dependently inhibited TNFα-induced phosphorylation of SRSF1 (serine/arginine splicing factor 1) mediated by SRPK1 with EC50 value of about 360nM in PC3 prostate cancer cells and switched splicing from VEGF-A₁₆₅a to VEGF-A₁₆₅b in RPE cells. SPHINX31 exhibited ocular penetrance and showed anti-angiogenic efficacy as it potently inhibited blood vessel growth in models of wet age-related macular degeneration in vivo when used as eye drops (20 μg/ml) post 14 days. Inhibition of SRPK1 by SPHINX31 halted AML expansion in vitro and in vivo, leading to cell cycle arrest, leukemic cell differentiation, and prolonged survival of immunocompromised mice transplanted with MLL-rearranged AML cells, and affected BRD4 recruitment to chromatin.
作用机制SPHINX31 occupies a binding pocket created by the unique helical insert of SRPK1 and triggers a backbone flip in the hinge region, resulting potent and selective inhibition of SRPK1 kinase activity.^[1]
动物研究
剂量
DBA2J Mice: 0.8 mg/kg - 2 mg/kg^[2] (i.p.)

给药途径
i.p.
参考文献

动物研究
剂量	DBA2J Mice: 0.8 mg/kg - 2 mg/kg^[2] (i.p.)
给药途径	i.p.

[1] Batson J, Toop HD, 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] Tzelepis K, De Braekeleer E, et al. SRPK1 maintains acute myeloid leukemia through effects on isoform usage of epigenetic regulators including BRD4. Nat Commun. 2018 Dec 19;9(1):5378.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.9704 mL
- 9.8521 mL
- 19.7042 mL
- 5 mM
- 0.3941 mL
- 1.9704 mL
- 3.9408 mL
- 10 mM
- 0.1970 mL
- 0.9852 mL
- 1.9704 mL

技术信息

CAS号

1818389-84-2

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C27H24F3N5O2

运输

蓝冰

分子量

507.51

别名

溶解度

DMSO	25.0 mg/mL (49.3 mM)
Water	Insoluble
Ethanol	12.0 mg/mL (23.6 mM)

动物实验配方

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