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Purity: ≥98%
SRPIN340 is a potent, selective and ATP-competitive SRPK (serine-arginine-rich protein kinase) inhibitor with Ki of 0.89 μM for SRPK1, it exhibited no significant inhibitory activity against more than 140 other kinases. According to research, SRPIN340 requires SR protein-dependent RNA processing in order to prevent HIV-1 and other viruses from replicating in HIV-1 transfected or infected Flp-In293 cell lines. SRPIN340 has also been shown to significantly lower SRPK1 and SRPK2 kinase activity, but not other SRPKs like Clk1 and Clk4. For SRPK1, this reduction is measured at 0.89μM.
| Targets |
SRPK1 (Ki = 0.89 μM)
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| ln Vitro |
SRPIN340 prevents Flp-In293 cells from having SR phosphorylated by SRPK and, in a dose-dependent way, encourages SRp75 degradation, which in turn prevents HIV replication. The chromosomal number and structure of CHO cells show no abnormalities when treated with a dose of SRPIN340 (5 mg/mL).[1] SRPIN340 inhibits HCV subgenomic replicon expression and HCV-JFH1 clone replication in vitro in a dose-dependent manner.[2]
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| ln Vivo |
SRPIN340 inhibits CNV formation in a dose-dependent manner in vivo. SRPIN340 suppresses VEGF, MCP-1, and ICAM-1 protein levels, which in turn prevents macrophage infiltration. [3]
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| Cell Assay |
In 96-well plates, leukemic cells (5 × 104 cells/well) and isolated PBMCs (8 × 104 cells/well) are seeded. Each well held 100 μL of the full RPMI medium and 100 μL of the SRPIN340 solution, which was varied in concentration. 10% fetal bovine serum and 0.4% DMSO (v/v) are added to RPMI medium to dilute the compound. MTT (5 mg/mL) is added to the wells after 48 hours of culture (3 hours, 37°C). After 30 minutes at room temperature and 500 ×g of centrifugation, the MTT solution is removed from the plates and 100 μL/well of DMSO is added to solubilize the formazan. A microplate reader is used to measure absorbance at 540 nm. Every experimental protocol is run through three times[2].
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| Animal Protocol |
mouse model with choroidal neovascularization (CNV)
~20 pmol i.v. |
| References |
| Molecular Formula |
C18H18F3N3O
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| Molecular Weight |
349.35
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| Exact Mass |
349.14
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| Elemental Analysis |
C, 61.88; H, 5.19; F, 16.31; N, 12.03; O, 4.58
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| CAS # |
218156-96-8
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| Related CAS # |
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| Appearance |
Solid powder
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| SMILES |
C1CCN(CC1)C2=C(C=C(C=C2)C(F)(F)F)NC(=O)C3=CC=NC=C3
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| InChi Key |
DWFGGOFPIISJIT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H18F3N3O/c19-18(20,21)14-4-5-16(24-10-2-1-3-11-24)15(12-14)23-17(25)13-6-8-22-9-7-13/h4-9,12H,1-3,10-11H2,(H,23,25)
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| Chemical Name |
N-[2-piperidin-1-yl-5-(trifluoromethyl)phenyl]pyridine-4-carboxamide
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.16 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: 1% DMSO +30% polyethylene glycol+1% Tween 80 : 8 mg/mL (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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