SRPIN340SRPIN340
MedChemExpress (MCE)
HY-13949
218156-96-8
SRPK inhibitor
99.97%
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Room temperature in continental US
may vary elsewhere.
SRPIN340 is an ATP-competitive serine-arginine-rich protein kinase (SRPK) inhibitor, with a Ki of 0.89 μM for SRPK1.
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].
Leukemic cells (5 × 104 cells/well) and isolated PBMCs (8 × 104 cells/well) are seeded in 96-well plates. Each well contained 100 μL of complete RPMI medium and 100 μL of SRPIN340 solution at different concentrations. The compound is diluted in RPMI medium with 10% fetal bovine serum and 0.4% DMSO (v/v). After 48 h of culture, MTT (5 mg/mL) is added to the wells (3 h, 37°C). The plates are centrifuged at room temperature for 30 min 500 ×g, followed by the removal of the MTT solution and the addition of 100 μL/well of DMSO to solubilize the formazan. Absorbance is measured at 540 nm in a microplate reader. Each experimental procedure is performed in triplicate[2].
Ki: 0.89 μM (SRPK1)[1] Cellular Effect Cell Line Type Value Description References
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[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]