Bioactivity | Dyclonine (Dyclocaine) hydrochloride is an orally effective ALDH covalent inhibitor (crosses blood-brain barrier), with an IC50 of 35 µM for ALDH2 and 76 µM for ALDH3A1. Dyclonine hydrochloride has sensitizing activities for targeted cancer cells 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]. |
Invitro | 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: |
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: |
Name | Dyclonine hydrochloride |
CAS | 536-43-6 |
Formula | C18H28ClNO2 |
Molar Mass | 325.87 |
Appearance | Solid |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
Reference | [1]. Okazaki S, et al. Synthetic lethality of the ALDH3A1 inhibitor dyclonine and xCT inhibitors in glutathione deficiency-resistant cancer cells. Oncotarget. 2018 Sep 18;9(73):33832-33843. [2]. FLORESTANO HJ, et al. Antimicrobial properties of dyclonine hydrochloride, a new topical anesthetic. J Am Pharm Assoc Am Pharm Assoc. 1956 May;45(5):320-5. [3]. Khanna M, et al. Discovery of a novel class of covalent inhibitor for aldehyde dehydrogenases. J Biol Chem. 2011 Dec 16;286(50):43486-94. |