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| Targets |
SRI-29329 is a potent and specific inhibitor of CDC-like kinase (CLK). It has IC50 values of 78 nM, 16 nM, and 86 nM for CLK1, CLK2, and CLK4, respectively. CLKs are involved in the regulation of alternative splicing and gene expression. By inhibiting CLKs, SRI-29329 modulates splicing and gene expression. It shows no significant activity against CLK3, CDK1, CDK4, and CDK6.
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| ln Vitro |
SRI-29329 (compound 8) exhibits no substantial CDK1,4,6 activity but a moderate (about 5-fold) preference for CLK2 over CLK1 and CLK4 [1].
In vitro, SRI-29329 is a specific CLK inhibitor with IC50 values of 78 nM, 16 nM, and 86 nM for CLK1, CLK2, and CLK4, respectively. It shows no significant activity against CLK3, CDK1, CDK4, and CDK6 (IC50 > 1,000 nM). Its in vitro activity is characterized by potent and selective inhibition of CLK1, CLK2, and CLK4. SRI-29329 is a specific CLK inhibitor. |
| ln Vivo |
In vivo, SRI-29329 has potential therapeutic applications in diseases where CLKs play a role. However, detailed in vivo efficacy data for specific disease models are limited. SRI-29329 is primarily used as a research tool for studying CLK biology and splicing regulation.
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| Enzyme Assay |
In vitro enzyme assays for SRI-29329 typically involve measuring the inhibition of CLK1, CLK2, and CLK4 kinase activities. The compound has IC50 values of 78 nM, 16 nM, and 86 nM for CLK1, CLK2, and CLK4, respectively. Its selectivity over CLK3, CDK1, CDK4, and CDK6 is also assessed. These assays confirm its mechanism of action as a CLK inhibitor.
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| Cell Assay |
In vitro cellular assays for SRI-29329 typically involve treating cells with the compound and measuring CLK activity or downstream effects on splicing and gene expression. The compound inhibits CLK1, CLK2, and CLK4. These cell-based studies demonstrate its functional inhibition of CLKs and its effects on cellular processes.
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| ADME/Pharmacokinetics |
SRI-29329 has a molecular formula of C20H26ClN7 and a molecular weight of 399.92. Its CAS number is 2086809-58-5. The compound is a specific CLK inhibitor with IC50 values of 78 nM, 16 nM, and 86 nM for CLK1, CLK2, and CLK4, respectively. It shows no significant activity against CLK3, CDK1, CDK4, and CDK6. SRI-29329 is a potent and specific CLK inhibitor.
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| Toxicity/Toxicokinetics |
SRI-29329 is a CLK inhibitor with a well-characterized mechanism of action. As with any kinase inhibitor, potential toxicity may include off-target effects on other kinases and disruption of normal cellular signaling. The compound's safety profile should be evaluated in preclinical toxicology studies. SRI-29329 is for research use only and is not approved for human therapeutic use. It represents a valuable tool for studying CLK biology and splicing regulation.
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| References | |
| Additional Infomation |
SRI-29329 (CAS# 2086809-58-5) is a potent and specific inhibitor of CDC-like kinase (CLK). It has IC50 values of 78 nM, 16 nM, and 86 nM for CLK1, CLK2, and CLK4, respectively. SRI-29329 shows no significant activity against CLK3, CDK1, CDK4, and CDK6. The compound is for research use only and not for human therapeutic use.
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| Molecular Formula |
C20H26CLN7
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| Molecular Weight |
399.920341968536
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| Exact Mass |
399.193
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| CAS # |
2086809-58-5
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| PubChem CID |
134397451
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| Appearance |
White to off-white solid powder
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| LogP |
4
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
28
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| Complexity |
507
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| Defined Atom Stereocenter Count |
2
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| SMILES |
ClC1=CC=CC(=C1)NC1C2=C(N(C=N2)C(C)C)N=C(N=1)N[C@H]1CCCC[C@@H]1N
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| InChi Key |
JPJBCKSRGYPABG-HOTGVXAUSA-N
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| InChi Code |
InChI=1S/C20H26ClN7/c1-12(2)28-11-23-17-18(24-14-7-5-6-13(21)10-14)26-20(27-19(17)28)25-16-9-4-3-8-15(16)22/h5-7,10-12,15-16H,3-4,8-9,22H2,1-2H3,(H2,24,25,26,27)/t15-,16-/m0/s1
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| Chemical Name |
2-N-[(1S,2S)-2-aminocyclohexyl]-6-N-(3-chlorophenyl)-9-propan-2-ylpurine-2,6-diamine
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| Synonyms |
SRI29329; SRI 29329; SRI-29329
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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 |
| 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 : ~50 mg/mL (~125.03 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.25 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 25.0 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: 2.5 mg/mL (6.25 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5005 mL | 12.5025 mL | 25.0050 mL | |
| 5 mM | 0.5001 mL | 2.5005 mL | 5.0010 mL | |
| 10 mM | 0.2501 mL | 1.2503 mL | 2.5005 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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