| Bioactivity | Bromhexine hydrochloride is a potent and specific TMPRSS2 protease inhibitor with an IC50 of 0.75 μM. Bromhexine hydrochloride can prevent and manage SARS-CoV-2 infection. Bromhexine hydrochloride is an autophagy agonist. Bromhexine hydrochloride is a mucolytic cough suppressant and has the potential for a range of respiratory conditions[1][2][3][4]. |
| Invitro | Bromhexine hydrochloride (BHH; 250μM; 24 hours) also significantly attenuates HGF-induced invasion of LNCaP and C4-2B cells that natively express TMPRSS2[1]. No significant toxicity is observed over a 48-hour period exposing LNCaP, DU145, PC3, or HepG2 cells to Bromhexine hydrochloride concentrations ranging from 0μM to 250μM. Bromhexine hydrochloride exposure does not induce cell death or substantially suppress the growth of DU145 cells[1]. Bromhexine hydrochloride (20 μM; 48 h) inhibits dendritic cells infection with HIV-1[4]. |
| In Vivo | Bromhexine hydrochloride (30mg/kg; ip; three times per week for 5 weeks) significantly reduces the incidence of distant metastasis to lung and liver sites from 55% in vehicle-treated animals to 20% in Wild-type C57BL/6 and TRAMP mice with PIN (prostatic intraepithelial neoplasia). The prostate glands of the mice treated with Bromhexine hydrochloride are generally substantially larger than vehicle-treated TRAMP mice[1]. |
| Name | Bromhexine hydrochloride |
| CAS | 611-75-6 |
| Formula | C14H21Br2ClN2 |
| Molar Mass | 412.59 |
| 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]. Jared M Lucas, et al. The androgen-regulated protease TMPRSS2 activates a proteolytic cascade involving components of the tumor microenvironment and promotes prostate cancer metastasis. Cancer Discov. 2014 Nov;4(11):1310-25. [2]. Li Wen Shen, et al. TMPRSS2: A potential target for treatment of influenza virus and coronavirus infections. Biochimie. 2017 Nov;142:1-10. [3]. Roberto Maggio, et al. Repurposing the mucolytic cough suppressant and TMPRSS2 protease inhibitor bromhexine for the prevention and management of SARS-CoV-2 infection. Pharmacol Res. 2020 Jul;157:104837. [4]. Santosh Chauhan, et al. Pharmaceutical screen identifies novel target processes for activation of autophagy with a broad translational potential. Nat Commun. 2015 Oct 27;6:8620. |
Bromhexine hydrochloride
CAS: 611-75-6 F: C14H21Br2ClN2 W: 412.59
Bromhexine hydrochloride is a potent and specific TMPRSS2 protease inhibitor with an IC50 of 0.75 μM. Bromhexine hydroc
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