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TMPRSS2 inhibitors

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Androgen Receptor (1) Autophagy (3) Cathepsin (1) DNA Methyltransferase (1) Endogenous Metabolite (2) HIV (3) Influenza Virus (1) Isotope-Labeled Compounds (1) PAI-1 (1) Parasite (1) PROTACs (1) SARS-CoV (19) Ser/Thr Protease (7)
By Research Areas:	Cancer (3) Cardiovascular Disease (2) Infection (19) Inflammation/Immunology (3) Metabolic Disease (3) Neurological Disease (1)
Click Chemistry:	PROTAC Synthesis (1)

Inhibitors & Agonists

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Isotope-Labeled Compounds

Click Chemistry

Targets Recommended: Serpin

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-W195509

Debrisoquin hydroiodide Debrisoquine hydroiodide; Isocaramidine hydroiodide; Ro 5-3307/1 hydroiodide	SARS-CoV Ser/Thr Protease	Infection
Debrisoquin (hydroiodide) is the hydrochloride form of Debrisoquin (HY-B1624). Debrisoquin is a *TMPRSS2* inhibitors that inhibits SARS-CoV-2 entry into human lung cell line by a TMPRSS2-depedent manner. Debrisoquin can be used for antiviral research .

HY-B1624A

Debrisoquin hemisulfate Debrisoquine hemisulfate; Isocaramidine hemisulfate; Ro 5-3307/1 hemisulfate	Endogenous Metabolite	Infection Cardiovascular Disease
Debrisoquin (Isocaramidine) hemisulfate is a *TMPRSS2* inhibitors that inhibits SARS-CoV-2 entry into human lung cell line by a TMPRSS2-depedent manner, with an IC₅₀ of 22μM. Debrisoquin hemisulfate can be used for antiviral research .

HY-148072

MM3122	SARS-CoV	Infection
MM3122 is a selective type II transmembrane serine protease (TMPRSS2) inhibitor with an IC₅₀ value of 0.34 nM. MM3122 effectively blocks TMPRSS2, thereby inhibiting the entry of SARS-CoV-2 and MERS-CoV into human cells .

HY-108447

BC-11 hydrobromide	Ser/Thr Protease SARS-CoV PAI-1	Infection Cancer
BC-11 hydrobromide is a selective *TMPRSS2* inhibitor (TMPRSS2 is a key host cellular factor for viral entry and SARS-CoV-2 pathogenesis), and a selective urokinase (uPA) inhibitor (IC₅₀=8.2 μM). BC-11 hydrobromide is cytotoxic to triple-negative MDA-MB231 breast cancer cells. BC-11 hydrobromide is used in research on viral infections and cancer .

HY-13512

Camostat mesylate 30+ Cited Publications Camostat mesilate; FOY305; FOY-S980	Ser/Thr Protease SARS-CoV	Infection Inflammation/Immunology
Camostat mesylate (Camostat mesilate) is an orally active, synthetic serine protease inhibitor for chronic pancreatitis. Camostat mesylate, an inhibitor of *TMPRSS2, shows antiviral activity against SARS-CoV-2. Camostat mesylate also inhibits* the activity of prostasin, trypsin, and matriptase .

HY-B1624

Debrisoquin Debrisoquine; Isocaramidine; Ro 5-3307/1	SARS-CoV Ser/Thr Protease	Infection Cardiovascular Disease
Debrisoquin (Isocaramidine) is a *TMPRSS2* inhibitors that inhibits SARS-CoV-2 entry into human lung cell line by a TMPRSS2-depedent manner, with an IC₅₀ of 22μM. Debrisoquin can be used for antiviral research .

HY-130402B

Propamidine	Parasite	Infection
Propamidine is a covalent inhibitor of TMPRSS2 and has some antibacterial activity. .

HY-156441

SARS-CoV-2-IN-65	SARS-CoV	Infection
SARS-CoV-2-IN-65 (compound 2f (81)) is a potent,orally active and reversible SARS-CoV-2 entry inhibitor. SARS-CoV-2-IN-65 inhibits the pseudovirus entry in a ACE2-dependent pathway, via mainly inhibiting RBD:ACE2 interaction and TMPRSS2 activity in Calu-3 cells .

HY-157021

SARS-CoV-2-IN-66	SARS-CoV	Infection Inflammation/Immunology
SARS-CoV-2-IN-66 (1), a vitaminK derivative, is a SARS-CoV-2 inhibitor, with an EC₅₀ of 70.8 μM in VeroE6/TMPRSS2 cells .

HY-157022

SARS-CoV-2-IN-67	SARS-CoV	Infection
SARS-CoV-2-IN-67 (Compound 16), a vitamin K derivatives, has anti-SARS-CoV-2 activity (EC₅₀: 64.8 μM in VeroE6/TMPRSS2 cells). SARS-CoV-2-IN-67 inhibits SARS-CoV-2 RdRp activity .

HY-105747A

Guanoxyfen nitrate N-(3-Phenoxypropyl)guanidine nitrate; (3-Phenoxypropyl)guanidine nitrate	Endogenous Metabolite	Infection Neurological Disease
Guanoxyfen (N-(3-Phenoxypropyl)guanidine) nitrate is a compound that exhibits potent inhibitory activity against the serine protease enzyme TMPRSS2, which plays a crucial role in the infectivity of coronaviruses. Guanoxyfen nitrate is also an effective inhibitor of vasoconstrictor responses to sympathetic nerve stimulation.

HY-B0372A

Bromhexine hydrochloride 3 Publications Verification	SARS-CoV Autophagy HIV	Metabolic Disease
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 .

HY-158073

ML2006a4	SARS-CoV	Infection
ML2006a4 is an orally active inhibitor for SARS-CoV-2 main protease (M ^pro) with IC₅₀ in picomolare value. ML2006a4 is cell permeable and antiviral active, that inhibits replication in SARS-CoV-2 in cells Huh7.5.1-ACE2-TMPRSS2 (Huh7.5.1++) in picomolare level

HY-13512R

Camostat (mesylate) (Standard)	Ser/Thr Protease SARS-CoV	Infection Inflammation/Immunology
Camostat (mesylate) (Standard) is the analytical standard of Camostat (mesylate). This product is intended for research and analytical applications. Camostat mesylate (Camostat mesilate) is an orally active, synthetic serine protease inhibitor for chronic pancreatitis. Camostat mesylate, an inhibitor of *TMPRSS2, shows antiviral activity against SARS-CoV-2. Camostat mesylate also inhibits* the activity of prostasin, trypsin, and matriptase .

HY-161902

MI-1904	Ser/Thr Protease Influenza Virus SARS-CoV	Infection
MI-1904 is the inhibitor for *matriptase/TMPRSS2, that exhibits antiviral activity against influenza virus* H1N1 and H9N2. MI-1904 blocks the cleavage of glycoproteins on the viral surface, prevents the virus from binding to host cell receptors, and thus inhibits the entry and replication of the virus .

HY-163067

SARS-CoV-2-IN-71	SARS-CoV	Infection
SARS-CoV-2-IN-71 (compound 8h) is a potent inhibitor of SARS-CoV-2. SARS-CoV-2-IN-71 inhibits coronavirus replication at multiple stages. SARS-CoV-2-IN-71 displays anti-coronaviral effect by simultaneously acting on 3CL ^pro and *TMPRSS2* .

HY-B0372AS

Bromhexine-d3 hydrochloride	Isotope-Labeled Compounds SARS-CoV Autophagy HIV	Metabolic Disease
Bromhexine-d₃ (hydrochloride) is deuterium labeled Bromhexine (hydrochloride). 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].

HY-161370

VD4162	Ser/Thr Protease	Cancer
VD4162 (Compound 8b) is a macrocyclic inhibitor of serine proteases. VD4162 can significantly improve potency for all four target enzymes TMPRSS2 (IC₅₀ = 3.7 nM), HGFA(IC₅₀ = 3.3 nM), matriptase (IC₅₀ = 2.9 nM), and hepsin (IC₅₀ = 0.54 nM). VD4162 can be used for the research of cancer .

HY-157154

MAT-POS-e194df51-1	SARS-CoV	Infection
MAT-POS-e194df51-1 is an orally active, non-covalent and non-peptide SARS-CoV-2 main protease (M ^pro) inhibitor with an IC₅₀ value of 37nM. MAT-POS-e194df51-1 is cytotoxic with EC₅₀ values of 64 nM and 126 nM in A549-ACE2-TMPRSS2 cells and HeLa -ACE2 cells, respectively .

HY-B0372AR

Bromhexine (hydrochloride) (Standard)	SARS-CoV Autophagy HIV	Metabolic Disease
Bromhexine (hydrochloride) (Standard) is the analytical standard of Bromhexine (hydrochloride). This product is intended for research and analytical applications. 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 .

HY-163029

CTSL/B-IN-1	Cathepsin SARS-CoV	Infection
CTSLCTSB-IN-1 (compound 212-148) is a bispecific inhibitor of host viral spike cleaver proteins CTSL/CTSB and *TMPRSS2* with IC₅₀s of 2.13/64.07 nM and 1.38 μM, respectively. CTSLCTSB-IN-1 blocks two relevant SARS-CoV-2 viral entry pathways by inhibiting the viral spike cleavage and can be applied to anti-SARS-CoV-2 research .

HY-162719

RH12	SARS-CoV	Infection
RH12 is a dual inhibitor for SARS-CoV-2 related RNA-dependent RNA polymerase (RdRp, IC₅₀ is 4.42 nM) and human transmembrane serine protease 2 (TMPRSS2, IC₅₀ is 4.2 nM). RH12 exhibits antiviral efficacy. RH12 inhibits viral replication and absorption, and exhibits a 90.5% virucidal effects on Vero-E6 cells. RH12 inhibits cell viability of Calu-3 with an IC₅₀ of 17.5 nM .

HY-170524

TDI-015051	SARS-CoV DNA Methyltransferase	Infection
TDI-015051 is an orally active inhibitor for SARS-CoV-2 nonstructural protein 14 (NSP14) with an IC₅₀ ≤0.15 nM. TDI-015051 inhibits SARS-CoV-2 NSP14 in Huh-7.5 cell (EC₅₀=11.4 nM) and in ACE2-TMPRSS2 expressing A549 cell (EC₅₀=64.7 nM). TDI-015051 also inhibits other coronaviruses like α-hCoV-NL63, α-hCoV-229E and β-hCoV-MERS with IC₅₀s of 1.7, 2.6 and 3.6 nM, respectively. TDI-015051 binds to the SAH-stabilized cap binding pocket, inhibits viral RNA methylation and viral replication, and exhibits anti-infectious activity in mouse models .

HY-114402

ARD-69	Androgen Receptor PROTACs	Cancer
ARD-69 is a PROTAC degrader based on the E3 ubiquitin ligase VHL and targeting the androgen receptor, which can induce androgen receptor (AR) protein degradation in AR-positive prostate cancer cells. ARD-69 inhibits AR-regulated gene expression, binds to the AR ligand binding domain at one end and binds to VHL at the other end, prompting AR to be recruited to the E3 ubiquitin ligase complex, triggering proteasome degradation, thereby inhibiting AR signaling pathways and downstream gene expression (such as PSA, *TMPRSS2*). ARD-69 can be used to study the treatment of castration-resistant prostate cancer (mCRPC) .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-B1624A

Debrisoquin hemisulfate Debrisoquine hemisulfate; Isocaramidine hemisulfate; Ro 5-3307/1 hemisulfate	Infection Structural Classification Alkaloids Classification of Application Fields Source classification Endogenous metabolite Isoquinoline Alkaloids Disease Research Fields	Endogenous Metabolite
Debrisoquin (Isocaramidine) hemisulfate is a *TMPRSS2* inhibitors that inhibits SARS-CoV-2 entry into human lung cell line by a TMPRSS2-depedent manner, with an IC₅₀ of 22μM. Debrisoquin hemisulfate can be used for antiviral research .

HY-13512

Camostat mesylate 30+ Cited Publications Camostat mesilate; FOY305; FOY-S980	Human Gut Microbiota Metabolites Microorganisms Source classification Endogenous metabolite	Ser/Thr Protease SARS-CoV
Camostat mesylate (Camostat mesilate) is an orally active, synthetic serine protease inhibitor for chronic pancreatitis. Camostat mesylate, an inhibitor of *TMPRSS2, shows antiviral activity against SARS-CoV-2. Camostat mesylate also inhibits* the activity of prostasin, trypsin, and matriptase .

HY-13512R

Camostat (mesylate) (Standard)	Human Gut Microbiota Metabolites Microorganisms Source classification Endogenous metabolite	Ser/Thr Protease SARS-CoV
Camostat (mesylate) (Standard) is the analytical standard of Camostat (mesylate). This product is intended for research and analytical applications. Camostat mesylate (Camostat mesilate) is an orally active, synthetic serine protease inhibitor for chronic pancreatitis. Camostat mesylate, an inhibitor of *TMPRSS2, shows antiviral activity against SARS-CoV-2. Camostat mesylate also inhibits* the activity of prostasin, trypsin, and matriptase .

Cat. No.	Product Name	Chemical Structure

HY-B0372AS

Bromhexine-d3 hydrochloride
Bromhexine-d₃ (hydrochloride) is deuterium labeled Bromhexine (hydrochloride). 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].

Bromhexine-d3 hydrochloride

Bromhexine-d₃ (hydrochloride) is deuterium labeled Bromhexine (hydrochloride). 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].

Cat. No.	Product Name		Classification

HY-114402

ARD-69		PROTAC Synthesis
ARD-69 is a PROTAC degrader based on the E3 ubiquitin ligase VHL and targeting the androgen receptor, which can induce androgen receptor (AR) protein degradation in AR-positive prostate cancer cells. ARD-69 inhibits AR-regulated gene expression, binds to the AR ligand binding domain at one end and binds to VHL at the other end, prompting AR to be recruited to the E3 ubiquitin ligase complex, triggering proteasome degradation, thereby inhibiting AR signaling pathways and downstream gene expression (such as PSA, *TMPRSS2*). ARD-69 can be used to study the treatment of castration-resistant prostate cancer (mCRPC) .

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