Dyclonine (Dyclocaine) hydrochloride 是一种口服有效的ALDH共价抑制剂 (可穿过血脑屏障)，其对ALDH2和ALDH3A1的IC50分别为 35 和 76 μM. Dyclonine hydrochloride 具有靶向癌细胞的增敏活性和抗菌活性。Dyclonine hydrochloride 还是一种局部麻醉剂，能阻断各种神经冲动或刺激的传导，抑制触觉和痛觉。
| 生物活性 | Dyclonine (Dyclocaine) hydrochloride is an orally effectiveALDHcovalent inhibitor (crosses blood-brain barrier), with anIC50of 35 μM forALDH2and 76 μM forALDH3A1. Dyclonine hydrochloride has sensitizing activities for targetedcancercells and antibacterial. Dyclonine hydrochloride is also a local anesthetic that blocks the transmission of various nerve impulses or stimuli and inhibits the sensation of touch and pain[1][2][3]. |
| IC50& Target[3] | ALDH2 35 μM (IC50) | ALDH3 76 μM (IC50) |
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体外研究
(In Vitro) | Dyclonine hydrochloride (50 μM; 24 h) sensitizes cancer cells to deficiency of cysteine and GSH[1].
Dyclonine hydrochloride (0-2048 μg/mL; 24 or 48 h) shows significant bactericidal and fungicidal activity[2].
Cell Viability Assay[1] | Cell Line: | HSC-4 cells | | Concentration: | 50 μM | | Incubation Time: | 24 h | | Result: | Inhibited ALDH activity and induced 4-HNE accumulation in GSH-depleted cancer cells. |
Cell Viability Assay[2] | Cell Line: | S. aureus,B. subtilis,E. coli,T. mentagrophyte | | Concentration: | 0-2048 μg/mL | | Incubation Time: | 24 h (for bacterial), 48 h (for fungi) | | Result: | Showed good antibacterial and antifungal activity, with minimum microbicidal concentration of 0.006%, 0.025%, 0.012% and 0.025% forS. aureus,B. subtilis,E. coli,T. mentagrophyte, separately. |
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体内研究
(In Vivo) | Dyclonine hydrochloride (5 mg/kg; i.p.; single daily for 24 days) sensitizes the involucrin+differentiated tumor cells to sulfasalazine treatment in vivo[1].
Dyclonine hydrochloride (5 mg/kg; i.p.; single daily for 21 days) suppress the growth of tumors formed by ALDH3A1-expressing gastric cancer stemlike cells when combines with sulfasalazine[1].
| Animal Model: | Athymic nude mice (HSC-2 cells implanted model)[1]. | | Dosage: | 5 mg/kg | | Administration: | Intraperitoneal injection; single daily for 24 days (combine with sulfasalazine). | | Result: | Attenuated the formation of tumors by HSC-2 cells implanted in nude mice when combined with sulfasalazine. |
| Animal Model: | C57BL6 mice (K19-Wnt1/C2mE-KP cells implanted model)[1]. | | Dosage: | 5 mg/kg | | Administration: | Intraperitoneal injection; single daily for 21 days (combine with sulfasalazine). | | Result: | Enhanced the antitumor effect of sulfasalazine on HNSCC tumors consisting of CD44vhigh stemlike tumor cells and involucrin+differentiated tumor cells. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 溶解性数据 | In Vitro: H2O : 50 mg/mL(153.44 mM;Need ultrasonic) DMSO : ≥ 25 mg/mL(76.72 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 3.0687 mL | 15.3435 mL | 30.6871 mL | | 5 mM | 0.6137 mL | 3.0687 mL | 6.1374 mL | | 10 mM | 0.3069 mL | 1.5344 mL | 3.0687 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (7.67 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (7.67 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (7.67 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (7.67 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (7.67 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (7.67 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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