| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
Zapalog targets protein-protein interactions by dimerizing any two proteins tagged with FKBP and DHFR domains. The compound brings these two proteins together, enabling the study of protein-protein interactions and signaling pathways. Upon exposure to light, Zapalog undergoes photolysis, causing the two proteins to dissociate.
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|---|---|
| ln Vitro |
Zapalog demonstrates potent in vitro activity as a photocleavable heterodimerizer. It effectively dimerizes FKBP- and DHFR-tagged proteins, enabling precise, reversible control of protein-protein interactions within cells using light. The compound's activity can be repeatedly initiated and instantaneously terminated by controlling light exposure.
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| ln Vivo |
In vivo, Zapalog is used as a research tool for optogenetic control of protein-protein interactions. The compound's photocleavable nature enables precise spatiotemporal control of protein function in living systems. It is widely used in cell signaling research to study dynamic protein interactions and signaling pathway regulation.
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| Enzyme Assay |
In vitro binding assays for Zapalog typically employ purified FKBP and DHFR proteins or their tagged variants. Binding affinity is assessed using surface plasmon resonance (SPR), isothermal titration calorimetry (ITC), or fluorescence polarization. Photocleavage efficiency is evaluated by exposing the compound-protein complex to UV light and monitoring dissociation by gel electrophoresis or analytical ultracentrifugation.
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| Cell Assay |
In vitro cellular assays for Zapalog involve transfecting cells with FKBP- and DHFR-tagged proteins of interest. Cells are treated with Zapalog (typically 0.1-10 microM range) to induce dimerization. Light exposure at appropriate wavelengths (typically UV or near-UV) induces photolysis and termination of the interaction. Readouts include assessment of protein localization by fluorescence microscopy, signaling pathway activation, and functional outputs.
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| Animal Protocol |
In vivo animal studies for Zapalog are typically performed in model organisms such as zebrafish, Drosophila, or mice, where FKBP- and DHFR-tagged proteins are expressed. The compound is administered via injection or other appropriate routes, and light exposure is used to control protein-protein interactions in specific tissues or developmental stages. Behavioral, physiological, or developmental endpoints are monitored.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Zapalog are characteristic of small molecule heterodimerizers. With a molecular weight of 1108.24, the compound is relatively large. Following administration, distribution, metabolism, and elimination would be determined via LC-MS/MS analysis. The compound is typically soluble in DMSO and stored at -20degC.
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| Toxicity/Toxicokinetics |
Zapalog is a research-grade chemical tool and not intended for human use. As with all research chemicals, standard safety precautions should be observed during handling including appropriate PPE and work in a fume hood. The compound is not approved for clinical use. Comprehensive toxicology data is not publicly available.
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| References | |
| Additional Infomation |
Zapalog (CAS# 1708091-24-0) is a photocleavable small-molecule heterodimerizer used in optogenetics and cell signaling research. It enables precise, reversible control of protein-protein interactions using light. The compound dimerizes FKBP- and DHFR-tagged proteins until light exposure causes photolysis. It is for research use only and not for human therapeutic applications.
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| Molecular Formula |
C58H73N7O15
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|---|---|
| Molecular Weight |
1108.24
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| Exact Mass |
1107.516
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| CAS # |
1708091-24-0
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| PubChem CID |
118048999
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| Appearance |
White to yellow solid powder
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| LogP |
8.1
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
19
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| Rotatable Bond Count |
29
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| Heavy Atom Count |
80
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| Complexity |
1920
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| Defined Atom Stereocenter Count |
2
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| SMILES |
O(C1C(=CC(CC2=CN=C(N)N=C2N)=CC=1OC)OC)CCOC(C1C=C(OC)C(OCCCC(=O)NC2C=CC=C([C@@H](CCC3C=CC(OC)=C(OC)C=3)OC([C@@H]3CCCCN3C(=O)C(=O)C(C)(C)CC)=O)C=2)=CC=1N(=O)=O)C
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| InChi Key |
ONSMHWXTRWDIMR-SXIGHEGWSA-N
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| InChi Code |
InChI=1S/C58H73N7O15/c1-10-58(3,4)53(67)55(68)64-23-12-11-17-42(64)56(69)80-44(21-19-36-20-22-45(72-5)46(28-36)73-6)38-15-13-16-40(31-38)62-51(66)18-14-24-78-48-33-43(65(70)71)41(32-47(48)74-7)35(2)77-25-26-79-52-49(75-8)29-37(30-50(52)76-9)27-39-34-61-57(60)63-54(39)59/h13,15-16,20,22,28-35,42,44H,10-12,14,17-19,21,23-27H2,1-9H3,(H,62,66)(H4,59,60,61,63)/t35?,42-,44+/m0/s1
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| Chemical Name |
[(1R)-1-[3-[4-[4-[1-[2-[4-[(2,4-diaminopyrimidin-5-yl)methyl]-2,6-dimethoxyphenoxy]ethoxy]ethyl]-2-methoxy-5-nitrophenoxy]butanoylamino]phenyl]-3-(3,4-dimethoxyphenyl)propyl] (2S)-1-(3,3-dimethyl-2-oxopentanoyl)piperidine-2-carboxylate
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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 : ~100 mg/mL (~90.23 mM)
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.9023 mL | 4.5117 mL | 9.0233 mL | |
| 5 mM | 0.1805 mL | 0.9023 mL | 1.8047 mL | |
| 10 mM | 0.0902 mL | 0.4512 mL | 0.9023 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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