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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
Ciliobrevin D targets cytoplasmic dynein, acting as a specific inhibitor of its AAA+ ATPase activity. By inhibiting dynein, it blocks dynein-dependent microtubule gliding and disrupts intracellular transport. This leads to the inhibition of Hedgehog signaling and primary cilia formation. Its mechanism involves the disruption of retrograde transport.
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| ln Vitro |
In NIH-3T3, cells treated with Ciliobrevin D display aberrant γ-tubulin localization and spindles (unfocused, multipolar, or folding). HeLa cells also showed similar spindle addition mediated by ciliary proteins. Spindles generated during the pre-mitotic phase were nevertheless irreversibly damaged by the addition of Ciliobrevin D, and the total amount of microtubules was decreased [1]. In S2 cells, ciliobrevin D reversibly inhibits melanosome aggregation without impairing peroxisomal migration.
In vitro, Ciliobrevin D blocks dynein-dependent microtubule gliding and ATPase activity. It inhibits Hedgehog signaling and primary cilia formation. It reversibly inhibits melanosome aggregation. It serves as a useful probe for dynein function. |
| ln Vivo |
Dync1h1 knockdown or dynamin 1 inactivation in the testis via Ciliobrevin D affects MT architecture by changing EB1's spatial expression, breaking F-actin, and interfering with tagged protein complex replication on the BTB, which results in BTB. Errors are lost. Changes in the spatiotemporal expression of the actin regulatory proteins Arp3 and Eps8 facilitate F-actin disassembly in the seminiferous epithelium following Dync1h1 deletion or dynactin 1's inactivation by Ciliobrevin D [3].
In vivo, Ciliobrevin D is used to study the role of dynein in various cellular processes. As an inhibitor of dynein and Hedgehog signaling, it has potential applications in research on ciliopathies and cancer. Detailed in vivo efficacy data are limited. |
| Enzyme Assay |
In vitro assays for Ciliobrevin D typically measure its inhibition of dynein ATPase activity. Dynein is incubated with ATP in the presence of varying concentrations of the compound. ATP hydrolysis is measured using a colorimetric or luminescent assay. Microtubule gliding assays are used to assess dynein-dependent motility.
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| Cell Assay |
Cellular assays for Ciliobrevin D are performed using cells with primary cilia. Cells are treated with the compound, and cilia formation is assessed by immunofluorescence microscopy. Hedgehog signaling is assessed using reporter gene assays or by measuring the expression of Hedgehog target genes.
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| Animal Protocol |
In vivo animal studies with Ciliobrevin D are limited, as it is primarily a research compound. When used, it is typically administered to animal models to study the role of dynein and primary cilia in development and disease. Detailed dosing regimens and protocols are not widely available.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for Ciliobrevin D are limited. Its molecular weight is 358.18 g/mol. The compound is cell-permeable and reversible. For research use, it is typically dissolved in DMSO for in vitro studies. Its oral bioavailability and metabolic stability have not been extensively characterized.
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| Toxicity/Toxicokinetics |
Comprehensive toxicological data for Ciliobrevin D are limited. In cell-based assays, the compound shows activity at micromolar concentrations. No significant toxicity has been reported at the doses used for dynein inhibition studies. The compound is intended for laboratory research only and should be handled with standard safety precautions.
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| References |
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| Additional Infomation |
Ciliobrevin D is a research compound used as a specific inhibitor of cytoplasmic dynein. It is a valuable tool for studying dynein function, intracellular transport, ciliogenesis, and Hedgehog signaling. The compound is not approved for clinical use and is intended for laboratory research only.
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| Molecular Formula |
C17H8CL3N3O2
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|---|---|
| Molecular Weight |
392.623320579529
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| Exact Mass |
390.968
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| CAS # |
1370554-01-0
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| PubChem CID |
136257953
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
4
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
25
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| Complexity |
669
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| Defined Atom Stereocenter Count |
0
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| SMILES |
ClC1C=CC2C(NC(C(C#N)=C(C3C=CC(=CC=3Cl)Cl)O)=NC=2C=1)=O
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| InChi Key |
HVJSIEVASHGLBF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H8Cl3N3O2/c18-8-1-3-10(13(20)5-8)15(24)12(7-21)16-22-14-6-9(19)2-4-11(14)17(25)23-16/h1-6,24H,(H,22,23,25)
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| Chemical Name |
2-(7-chloro-4-oxo-3H-quinazolin-2-yl)-3-(2,4-dichlorophenyl)-3-hydroxyprop-2-enenitrile
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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 : ~5 mg/mL (~12.73 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 | 2.5470 mL | 12.7350 mL | 25.4699 mL | |
| 5 mM | 0.5094 mL | 2.5470 mL | 5.0940 mL | |
| 10 mM | 0.2547 mL | 1.2735 mL | 2.5470 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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