生物活性
SRPIN340 is an ATP-competitive serine-arginine-rich protein kinase (SRPK) inhibitor, with a Ki of 0.89 μM for SRPK1.
IC50 & Target
Ki: 0.89 μM (SRPK1)[1]
体外研究
(In Vitro)
SRPIN340 is a serine-arginine-rich protein kinase (SRPK) inhibitor, with a Ki of 0.89 μM for SRPK1. SRPIN340 also inhibits SRPK2, but shows no significant inhibition on other SRPK, such as Clk1 and Clk4. SRPIN340 promotes degradation of SRp75, which is necessary for HIV expression. SRPIN340 suppresses the propagation of Sindbis virus (IC50, 60 μM) as well as severe acute respiratory syndrome virus[1]. SRPIN340 shows inhibitory effect on leukemia cell lines, such as AML HL60, ALL-T Molt4 and Jurkat, with IC50s of 44.7 μM, 92.2 μM and 82.3 μM, respectively[2].
分子量
349.35
性状
Solid
Formula
C18H18F3N3O
CAS 号
218156-96-8
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro:
DMSO : ≥ 42 mg/mL (120.22 mM)
* "≥" means soluble, but saturation unknown.
配制储备液
浓度溶剂体积质量 1 mg 5 mg 10 mg
1 mM 2.8625 mL 14.3123 mL 28.6246 mL
5 mM 0.5725 mL 2.8625 mL 5.7249 mL
10 mM 0.2862 mL 1.4312 mL 2.8625 mL
*
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
参考文献
[1]. Fukuhara T, et al. Utilization of host SR protein kinases and RNA-splicing machinery during viral replication. Proc Natl Acad Sci U S A. 2006 Jul 25;103(30):11329-33. [Content Brief]
[2]. Siqueira RP, et al. Potential Antileukemia Effect and Structural Analyses of SRPK Inhibition by N-(2-(Piperidin-1-yl)-5-(Trifluoromethyl)Phenyl)Isonicotinamide (SRPIN340). PLoS One. 2015 Aug 5;10(8):e0134882. [Content Brief]