| Size | Price | Stock | Qty |
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| 2mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
Dynapyrazole-A targets microtubule dynein, a motor protein that moves along microtubules and is involved in intracellular transport, cell division, and ciliary/flagellar motility. The compound specifically inhibits the ATPase activity of microtubule-stimulated dynein but does not block the microtubule-independent basal activity. It inhibits dynein 1 and dynein 2-dependent microtubule gliding with IC50 values of 2.3 and 2.6 μM, respectively. Dynapyrazole-A also inhibits Hedgehog signaling with an IC50 of 1.9 μM.
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| ln Vitro |
In MA-104 cells infected with the RVA-NMTL virus, dynapyrazole A (1–3 μg/mL, 14 h) can lower virus titers in a dose-dependent manner; its EC 50 value is 0.73 μg/mL[1].
In vitro studies demonstrate that Dynapyrazole-A specifically inhibits the ATPase activity of microtubule-stimulated dynein but does not block the microtubule-independent basal activity. The compound inhibits dynein 1 and dynein 2-dependent microtubule gliding with IC50 values of 2.3 and 2.6 μM, respectively. Dynapyrazole-A also inhibits Hedgehog signaling with an IC50 of 1.9 μM. The compound's specificity for dynein over other motor proteins makes it a valuable tool for studying dynein function. |
| ln Vivo |
No detailed in vivo activity data has been published for Dynapyrazole-A. The compound has been primarily characterized in vitro as a research tool for studying dynein function and Hedgehog signaling. Its ability to inhibit dynein ATPase activity and microtubule gliding suggests that it could have potential for in vivo applications in studying dynein-related processes. Further studies would be needed to evaluate its efficacy in animal models.
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| Enzyme Assay |
The dynein ATPase inhibitory activity of Dynapyrazole-A can be assessed using in vitro ATPase assays. In a typical assay, purified dynein is incubated with ATP and varying concentrations of Dynapyrazole-A. The release of inorganic phosphate is measured using a colorimetric assay, and the IC50 is calculated. Microtubule gliding assays can be performed to assess the compound's ability to inhibit dynein-dependent microtubule movement. The IC50 for dynein 1 and dynein 2-dependent microtubule gliding are 2.3 and 2.6 μM, respectively.
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| Cell Assay |
The cellular activity of Dynapyrazole-A is assessed using cell-based assays that measure dynein function. Cells are treated with varying concentrations of Dynapyrazole-A. Intracellular transport, cell division, and ciliary/flagellar motility are assessed using microscopy. Hedgehog signaling activity is assessed using reporter assays or by measuring the expression of Hedgehog target genes. The compound's ability to inhibit Hedgehog signaling with an IC50 of 1.9 μM has been demonstrated.
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| Animal Protocol |
No detailed in vivo animal model data has been published for Dynapyrazole-A. The compound has been primarily characterized in vitro as a research tool for studying dynein function and Hedgehog signaling. Future studies may involve the use of animal models to study dynein-related processes or Hedgehog-dependent cancers.
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| ADME/Pharmacokinetics |
No detailed pharmacokinetic data has been published for Dynapyrazole-A. The compound has a molecular weight of 486.7 and a molecular formula of C20H12ClIN4O. It has a purity of ≥98%. The compound is typically stored at -20°C. It appears as a white to off-white solid powder. Further studies would be needed to characterize its absorption, distribution, metabolism, and excretion properties.
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| Toxicity/Toxicokinetics |
No detailed toxicity data has been published for Dynapyrazole-A. As a dynein inhibitor, the compound may have on-target effects on dynein-dependent processes in normal cells, including intracellular transport, cell division, and ciliary function. Comprehensive toxicology studies would be required to evaluate its safety profile for potential therapeutic development. The compound is intended for research use only.
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| References | |
| Additional Infomation |
Dynapyrazole-A (CAS# 2226517-75-3) is a specific inhibitor of microtubule dynein that inhibits the ATPase activity of microtubule-stimulated dynein with IC50 values of 2.3 and 2.6 μM for dynein 1 and dynein 2-dependent microtubule gliding. The compound also inhibits Hedgehog signaling with an IC50 of 1.9 μM. It has the molecular formula C20H12ClIN4O and a molecular weight of 486.7. Dynapyrazole-A is a research tool for studying dynein function and Hedgehog signaling.
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| Molecular Formula |
C20H12CLIN4O
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|---|---|
| Molecular Weight |
486.69
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| Exact Mass |
485.974
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| CAS # |
2226517-75-3
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| PubChem CID |
136213044
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| Appearance |
White to off-white solid powder
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| Density |
1.9±0.1 g/cm3
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| Boiling Point |
551.3±50.0 °C at 760 mmHg
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| Flash Point |
287.2±30.1 °C
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| Vapour Pressure |
0.0±1.5 mmHg at 25°C
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| Index of Refraction |
1.821
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| LogP |
5.45
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
27
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| Complexity |
668
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1CC1(C2=CC=C(C=C2)Cl)C3=NN4C5=C(C=C(C=C5)I)C(=O)NC4=C3C#N
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| InChi Key |
VABPBCMFKJDOHP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H12ClIN4O/c21-12-3-1-11(2-4-12)20(7-8-20)17-15(10-23)18-24-19(27)14-9-13(22)5-6-16(14)26(18)25-17/h1-6,9H,7-8H2,(H,24,27)
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| Chemical Name |
2-[1-(4-chlorophenyl)cyclopropyl]-7-iodo-5-oxo-4H-pyrazolo[1,5-a]quinazoline-3-carbonitrile
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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 : 25 mg/mL (51.37 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.14 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 (5.14 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 25.0 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 | 2.0547 mL | 10.2735 mL | 20.5470 mL | |
| 5 mM | 0.4109 mL | 2.0547 mL | 4.1094 mL | |
| 10 mM | 0.2055 mL | 1.0273 mL | 2.0547 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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