Dyclonine hydrochloride
Based on 1 publication(s) in Google Scholar
Dyclonine hydrochloride (Dyclocaine hydrochloride) is an orally active, blood-brain barrier-permeable piperidine phenylacetone small molecule commonly used as a local anesthetic. Dyclonine hydrochloride acts as a highly selective allosteric antagonist of TRPV3; it also reversibly inhibits G9a, ALDH2 and ALDH3A1, non-competitively blocks AChE. Dyclonine hydrochloride activates the Nrf2/ARE pathway, relieves the epigenetic silencing of FXN, blocks Aβ42 aggregation, and promotes remyelination and reparative polarization of microglia. Dyclonine hydrochloride alleviates pruritus via TRPV3 inhibition; it is used in studies of neurodegenerative disease models based on its AChE inhibitory, antioxidant and remyelinating effects; it sensitizes drug-resistant tumors through ALDH inhibition, and combined use with protease inhibitors induces more tumor cell apoptosis; it inhibits Candida albicans in vitro. Dyclonine hydrochloride can be used for research on multiple diseases including neurodegenerative diseases, cancer and pruritic dermatitis.
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- Pureté : 99.12%
- CAS No.: 536-43-6
- Formule: C18H28ClNO2
- Masse moléculaire:325.87
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Stockage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Dyclonine hydrochloride
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Activité biologique
Description
IC50 & Target
[3]|
TRPV3 |
ALDH2 |
ALDH3A1 |
AChE |
In Vitro
Dyclonine hydrochloride selectively inhibits purified TRPV3 channels with an IC50 of 3.2 μM; it inhibits purified ALDH2 with an IC50 of 35 μM; it also inhibits purified ALDH3A1 with an IC50 of 76 μM; and it potently and selectively inhibits purified AchE in a non-competitive manner with an IC50 of 0.18 μM[1].
Dyclonine hydrochloride inhibits the proliferation of cultured cardiomyocytes at concentrations of 1-10 μM by suppressing ALDH2; it also inhibits the proliferation of HSC4 oral squamous cell carcinoma cells cultured in vitro, and restores the sensitivity of drug-resistant HSC4 cells to Sulfasalazine (HY-14655) via ALDH inhibition[1].
Dyclonine (0.3-10 μM; 48 h) hydrochloride dose-dependently increases the FXN protein level in lymphoblasts derived from Friedreich's ataxia (FA)[2].
Dyclonine (3-30 μM; 24 h) hydrochloride dose-dependently increases the level of FXN transcripts in lymphoblasts derived from Friedreich's ataxia (FA) patients, reaching a maximum induction of approximately 3.2-fold after treatment with 30 μM for 24 h, and exhibits a stronger inductive effect in cells with longer GAA repeat sequences[2].
Dyclonine hydrochloride (5 μM; 24 h) enhances the binding of Nrf2 to the conserved ARE site in the FXN locus in lymphoblasts from FA patients[2].
Dyclonine (1-10 μM) hydrochloride dose-dependently inhibits the activity of histone methyltransferase G9a in nuclear extracts of healthy lymphoblasts; it also rescues the aconitase activity defect in lymphoblasts derived from Fanconi anemia (FA)[2].
Dyclonine (3-30 μM; with 1 mM 2-APB (HY-W009724)) hydrochloride modulates the inhibitory potency against mouse TRPV3 channels overexpressed in HEK 293T cells, and this regulatory effect relies on amino acid residues located in the channel pore region. Relative to wild-type TRPV3 with an IC50 value of 3.2 μM, L630W, N643A, I644W and L655A mutations reduce its inhibitory capacity, whereas L642A and I659A mutations strengthen its channel-blocking activity[3].
Dyclonine (15 μM) hydrochloride enhances the cytotoxic effect of 40 nM Bortezomib (HY-10227), reduces the survival rate of drug-resistant RPMI8226.BR multiple myeloma cells by approximately 80%, and induces cell apoptosis; it also enhances the cytotoxic activity of MG132 (HY-13259), inhibits the proliferation of BT549 and MDA-MB-231 breast cancer cells, and induces their apoptosis[1].
Dyclonine hydrochloride inhibits the growth of Saccharomyces cerevisiae in vitro, and exerts a synergistic effect with Calyculin A (HY-18983) to enhance this effect by targeting sterol biosynthetic enzymes including Erg2p and ERG24[1].
Dyclonine hydrochloride increases mitochondrial ATP production in cultured primary neurons and enhances their spontaneous excitatory postsynaptic current activity; it also inhibits the formation of Aβ42 oligomers in vitro[1].
Dyclonine hydrochloride potently protects fibroblasts derived from Fanconi anemia (FA) from diamide-induced oxidative stress, with an EC50 of approximately 0.2 μM[2].
Dyclonine (1.25-10 μM; 24 h) hydrochloride dose-dependently activates the Nrf2/ARE pathway in stable HeLa-ARE-luciferase cells, and luciferase activity is induced to approximately 2.5-fold after treatment with 10 μM for 24 h[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Dyclonine hydrochloride facilitates oligodendrogenesis, remyelination and the conversion of regenerative microglia upon oral delivery in mouse models with drug-triggered brain demyelination lesions[1].
Dyclonine (1-50 μM; intradermal injection; single administration) hydrochloride dose-dependently ameliorates TRPV3-mediated acute pruritus in mice, with the highest tested dose (50 μM) reducing the number of carvacrol (HY-N0711)-induced scratching bouts to 18.0 within 30 min[3].
Dyclonine hydrochloride reduces the number and proliferative activity of cardiomyocytes in neonatal mice after 14 days of treatment; it enhances the tumor volume reduction efficacy of Sulfasalazine in a mouse model of chemoresistant head and neck squamous cell carcinoma; and it improves the substrate oxidation capacity of whole-brain mitochondria in mice[1].
Dyclonine (1-10 mg/kg; intraperitoneal injection, oral administration; daily dosing; for 1 week) hydrochloride dose-dependently increases the levels of frataxin protein and Nrf2 target proteins, as well as aconitase activity, in the cerebellum of FA-YG8 mice[2].
Dyclonine (25 mg/kg; p.o.; daily; 4 weeks) hydrochloride restores the activity of succinate dehydrogenase in the liver, prevents the decline in balance beam performance, and increases the frataxin protein level by up to 2-fold in FA-PandKIKO mice[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Essai clinique
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 536-43-6
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Appearance Solid
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Masse moléculaire 325.87
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Formule C18H28ClNO2
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Color White to off-white
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SMILES
O=C(C1=CC=C(OCCCC)C=C1)CCN2CCCCC2.Cl
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Synonyms
Dyclocaine hydrochloride
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (1)
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Journal Impact Factor
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Most Recent
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Elife
Therapeutic inhibition of keratinocyte TRPV3 sensory channel by local anesthetic dyclonine. [Abstract]2021 Apr 20:10:e68128. PMID: 33876725
Solvant et solubilité
In Vitro:
H2O : 50 mg/mL (153.44 mM; Need ultrasonic)
DMSO : ≥ 25 mg/mL (76.72 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.67 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.67 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Pureté et documentation
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Fiche technique (295 KB)
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SDS (585 KB)
- English - EN (585 KB)
- Français - FR (585 KB)
- Deutsch - DE (585 KB)
- Norwegian - NO (585 KB)
- Español - ES (585 KB)
- Swedish - SV (585 KB)
- Italian - IT (585 KB)
- Korean - KR (585 KB)
- Portuguese - PT (585 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Bailly C, et al. A new horizon for the anesthetic drug dyclonine. Biochemical pharmacology. 2026 Feb;244:117569. [Content Brief]
[2]. Sahdeo S, et al. Dyclonine rescues frataxin deficiency in animal models and buccal cells of patients with Friedreich's ataxia. Human molecular genetics. 2014 Dec 20;23(25):6848-62. [Content Brief]
[3]. Liu Q, et al. Therapeutic inhibition of keratinocyte TRPV3 sensory channel by local anesthetic dyclonine. eLife. 2021 Apr 20;10:e68128. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / H2O | 1 mM | 3.0687 mL | 15.3435 mL | 30.6871 mL | 76.7177 mL |
| 5 mM | 0.6137 mL | 3.0687 mL | 6.1374 mL | 15.3435 mL | |
| 10 mM | 0.3069 mL | 1.5344 mL | 3.0687 mL | 7.6718 mL | |
| 15 mM | 0.2046 mL | 1.0229 mL | 2.0458 mL | 5.1145 mL | |
| 20 mM | 0.1534 mL | 0.7672 mL | 1.5344 mL | 3.8359 mL | |
| 25 mM | 0.1227 mL | 0.6137 mL | 1.2275 mL | 3.0687 mL | |
| 30 mM | 0.1023 mL | 0.5115 mL | 1.0229 mL | 2.5573 mL | |
| 40 mM | 0.0767 mL | 0.3836 mL | 0.7672 mL | 1.9179 mL | |
| 50 mM | 0.0614 mL | 0.3069 mL | 0.6137 mL | 1.5344 mL | |
| 60 mM | 0.0511 mL | 0.2557 mL | 0.5115 mL | 1.2786 mL | |
| H2O | 80 mM | 0.0384 mL | 0.1918 mL | 0.3836 mL | 0.9590 mL |
| 100 mM | 0.0307 mL | 0.1534 mL | 0.3069 mL | 0.7672 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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