| Size | Price | Stock | Qty |
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| 5mg |
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| Other Sizes |
| Targets |
SRPKIN-1 targets SRPK1 and SRPK2, two members of the serine/arginine-rich protein kinase family that phosphorylate SR proteins involved in pre-mRNA splicing. It is a covalent and irreversible inhibitor with IC50 values of 35.6 nM for SRPK1 and 98 nM for SRPK2.
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| ln Vitro |
At 200 nM concentration, with or without gradient, SRPKIN-1 (10, 50, 100, 200 nM, 16 hours) dramatically lowers steady-state SR protein phosphorylation [1].
SRPKIN-1 is a covalent and irreversible SRPK1/2 inhibitor with IC50 values of 35.6 nM for SRPK1 and 98 nM for SRPK2. It exhibits anti-angiogenic effects. The compound's irreversible binding mechanism provides sustained inhibition of SRPK activity. |
| ln Vivo |
By selectively splicing VEGF, SRPKIN-1 (50 nM, 300 nM, 1 μL; 5 dosages) prevents angiogenesis in the CNV animal model [1].
SRPKIN-1 exhibits anti-angiogenic effects in vivo. By inhibiting SRPK1/2, the compound modulates alternative splicing of VEGF, leading to reduced production of pro-angiogenic VEGF isoforms. Specific animal model data and dosing regimens are not extensively detailed in standard reference sources. |
| Enzyme Assay |
SRPKIN-1's inhibitory activity against SRPK1 and SRPK2 can be assessed using in vitro kinase assays. Recombinant SRPK1 or SRPK2 enzymes are incubated with their substrate (e.g., SR proteins or peptide substrates) and ATP in the presence of varying concentrations of SRPKIN-1. The amount of phosphorylated substrate is measured to determine the IC50.
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: Ba/F3 cells Tested Concentrations: 0-10000 nM Incubation Duration: 72 h Experimental Results: Effectively diminished SR levels phosphorylated in a dose-dependent manner, resulting in an increase in VEGF-A165b RNA and protein, even at doses of 200 nM[1]. The cellular activity of SRPKIN-1 is evaluated in cell-based assays. Cells are treated with increasing concentrations of SRPKIN-1, and SRPK-mediated phosphorylation of SR proteins is assessed by Western blot using phospho-specific antibodies. The effect on alternative splicing of target genes (e.g., VEGF) is examined by RT-PCR. Angiogenesis-related processes such as endothelial cell tube formation are also assessed. |
| Animal Protocol |
Animal/Disease Models: Mice[1]
Doses: 50 nM, 300 nM, 1 μL Route of Administration: Intravitreal injection, 5 times Experimental Results: SRPKIN-1 treated mice were Dramatically inhibited as measured by CNV area in a dose-dependent manner [1]. Specific in vivo animal experimental protocols for SRPKIN-1 are not extensively detailed in standard reference sources. For evaluating its anti-angiogenic activity, SRPKIN-1 would be administered to tumor-bearing mice or models of ocular neovascularization. Tumor growth, angiogenesis markers, and vascular density would be assessed to evaluate efficacy. |
| ADME/Pharmacokinetics |
SRPKIN-1 has a molecular formula of C23H24N6O3S2 and a molecular weight of 496.61. It is soluble in DMSO. Specific pharmacokinetic parameters such as half-life, bioavailability, and plasma protein binding are not extensively detailed in standard reference sources.
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| Toxicity/Toxicokinetics |
The toxicity profile of SRPKIN-1 is not extensively documented. As a covalent kinase inhibitor, potential adverse effects may include off-target reactivity and immunogenicity. Specific LD50 values and organ-specific toxicity data are not readily available.
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| References | |
| Additional Infomation |
SRPKIN-1 (CAS# 2089226-94-6) is a covalent and irreversible inhibitor of SRPK1/2 with IC50 values of 35.6 nM and 98 nM, respectively. It exhibits anti-angiogenic effects. The compound is a research tool for studying SRPK function in splicing, angiogenesis, and cancer.
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| Molecular Formula |
C27H21FN2O3S
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|---|---|
| Molecular Weight |
472.530648946762
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| Exact Mass |
472.125
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| CAS # |
2089226-94-6
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| Related CAS # |
2089226-94-6;
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| PubChem CID |
135324340
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| Appearance |
White to off-white solid powder
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| LogP |
6.3
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
34
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| Complexity |
966
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S(C1=CC=CC(=C1)C1C(CC)=CC2C(C3C4C=CC(C#N)=CC=4NC=3C(C)(C)C=2C=1)=O)(=O)(=O)F
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| InChi Key |
TWKWEBMGDALHPN-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C27H21FN2O3S/c1-4-16-12-21-22(13-20(16)17-6-5-7-18(11-17)34(28,32)33)27(2,3)26-24(25(21)31)19-9-8-15(14-29)10-23(19)30-26/h5-13,30H,4H2,1-3H3
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| Chemical Name |
3-(3-cyano-9-ethyl-6,6-dimethyl-11-oxo-5H-benzo[b]carbazol-8-yl)benzenesulfonyl fluoride
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| Synonyms |
SRPKIN 1; SRPKIN1; SRPKIN-1
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| 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) |
DMSO : ≥ 110 mg/mL (~232.79 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.75 mg/mL (5.82 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% 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 27.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.75 mg/mL (5.82 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 27.5 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1163 mL | 10.5813 mL | 21.1627 mL | |
| 5 mM | 0.4233 mL | 2.1163 mL | 4.2325 mL | |
| 10 mM | 0.2116 mL | 1.0581 mL | 2.1163 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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