SRPIN340 (Synonyms: SRPK Inhibitor) |
| カタログ番号GC13596 |
SRPIN340 は、SRPK1 に対する Ki が 0.89 μM の ATP 競合性セリン アルギニン リッチ プロテイン キナーゼ (SRPK) 阻害剤です。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 218156-96-8
Sample solution is provided at 25 µL, 10mM.
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SRPIN340 is a highly selective inhibitor of SR protein phosphorylation with a Ki value of 0.89μM for SRPK1 [1].
SRPIN340 has been revealed to inhibit replication of HIV-1 and other viruses that require SR protein-dependent RNA processing for the propagation in HIV-1 transfected or infected Flp-In293 cell lines. In addition, SRPIN340 has been reported to significantly inhibit SRPK1 and SRPK2 kinase activity but not potently inhibit other SRPKs, such as Clk1 and Clk4 with a Ki value of 0.89μM for SRPK1. Besides, SRPIN340 has been exhibited to dose-dependently promote degradation of SRp75 which is necessary for HIV expression. Moreover, SRPIN340 has shown the inhibition of propagation of Sindbis virus with an IC50 of 60μM and the protection against the cytopathic effect of Sindbis virus [1].
References:
[1] Fukuhara T1, Hosoya T, Shimizu S, Sumi K, Oshiro T, Yoshinaka Y, Suzuki M, Yamamoto N, Herzenberg LA, Herzenberg LA, Hagiwara M.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. Epub 2006 Jul 13.
| Cell experiment [1]: | |
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Cell lines |
A375, Omm2.5, Mel270 and 92.1 cells |
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Preparation method |
The solubility of this compound in DMSO is >10.9mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
10 μM; 24 hours |
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Applications |
In A375 cells, SRPIN340 resulted in a 54% reduction in the IGF-1 induced nuclear localisation of SRSF1. In Mel270 cells, SRPIN340 significantly reduced the proportion of nuclear SRSF1 compared with IGF-1 treatment alone. In A375, Omm2.5 and 92.1 cells, SRPIN340 reduced total VEGF protein. |
| Animal experiment [1]: | |
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Animal models |
Mice bearing A375-untransfected tumours |
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Dosage form |
100 μl of 20 μg/ml SRPIN340 (diluted 100× in PBS from 2mg/ml stock in DMSO); injected daily into the peritumoral space |
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Application |
In mice bearing A375-untransfected tumours, SRPIN340 significantly reduced tumour growth compared with DMSO control-injected tumours. SRPIN340 also reduced total VEGF expression and significantly reduced microvascular density (MVD). |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. M V Gammons, R Lucas, R Dean, et al. Targeting SRPK1 to control VEGF-mediated tumour angiogenesis in metastatic melanoma. Br J Cancer. 2014 Jul 29; 111(3): 477-485. | |
| Cas No. | 218156-96-8 | SDF | |
| 同義語 | SRPK Inhibitor | ||
| Chemical Name | N-[2-piperidin-1-yl-5-(trifluoromethyl)phenyl]pyridine-4-carboxamide | ||
| Canonical SMILES | C1CCN(CC1)C2=C(C=C(C=C2)C(F)(F)F)NC(=O)C3=CC=NC=C3 | ||
| Formula | C18H18F3N3O | M.Wt | 349.35 |
| 溶解度 | ≥ 10.9mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 21 reference(s) in Google Scholar.)
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