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TMPRSS2

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Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-135794
    11-Ketodihydrotestosterone
    1 Publications Verification

    11-KDHT; 5α-Dihydro-11-keto testosterone

    Androgen Receptor Endocrinology
    11-Ketodihydrotestosterone (11-KDHT; 5α-Dihydro-11-keto testosterone) is an endogenous steroid and a metabolite of 11β-Hydroxyandrostenedione. 11-Ketodihydrotestosterone is an active androgen and is also a potent androgen receptor (AR) agonist with a Ki of 20.4 nM and an EC50 of 1.35 nM for human AR. 11-Ketodihydrotestosterone drives gene regulation, protein expression and cell growth in androgen-dependent prostate cancer cells [2].
    11-Ketodihydrotestosterone
  • HY-13512
    Camostat mesylate
    40+ 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 [2] .
    Camostat mesylate
  • 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 [2] .
    Bromhexine hydrochloride
  • HY-15290
    AIM-100
    4 Publications Verification

    Ack1 Cancer
    AIM-100 is a potent and selective Ack1 inhibitor with an IC50 of 21.58 nM. AIM-100 also inhibits Tyr 267 phosphorylation. AIM-100 does not inhibits other kinases including PI3-kinase and AKT subfamily members. AIM-100 has an anticancer effect [2].
    AIM-100
  • HY-134432B
    Boc-Gln-Ala-Arg-AMC acetate
    1 Publications Verification

    Ser/Thr Protease Others
    Boc-Gln-Ala-Arg-AMC acetate is a fluorogenic substrate for trypsin. Boc-Gln-Ala-Arg-AMC acetate can also be used for measuring the proteolytic activity of TMPRSS2 [2].
    Boc-Gln-Ala-Arg-AMC acetate
  • HY-114402

    PROTACs Androgen Receptor 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 of castration-resistant prostate cancer (mCRPC) [2] .
    ARD-69 is composed of a target protein ligand (pink part) AR antagonist 14 (HY-172624), a PROTAC linker (black part) tert-Butyl 4-ethynyl-[1,4'-bipiperidine]-1'-carboxylate (HY-W442074), and a VHL-type E3 ubiquitinase ligand (blue part) VH 101, acid (HY-47070); among them, the VHL ligand and the linker can form a conjugate VH 101-amide-piperidine-Pip-alkyne (HY-172625).
    ARD-69
  • HY-148072

    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 .
    MM3122
  • HY-108447

    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 [2] .
    BC-11 hydrobromide
  • HY-W195509

    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 .
    Debrisoquin hydroiodide
  • HY-B1624A

    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 .
    Debrisoquin hemisulfate
  • HY-13512R

    Camostat mesilate (Standard); FOY305 (Standard); FOY-S980 (Standard)

    Reference Standards 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 [2] .
    Camostat mesylate (Standard)
  • HY-B1624

    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 .
    Debrisoquin
  • HY-RS16739

    Small Interfering RNA (siRNA) Others

    Tmprss2 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Tmprss2 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

    Tmprss2 Mouse Pre-designed siRNA Set A
    Tmprss2 Mouse Pre-designed siRNA Set A
  • HY-RS14769

    Small Interfering RNA (siRNA) Others

    TMPRSS2 Human Pre-designed siRNA Set A contains three designed siRNAs for TMPRSS2 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

    TMPRSS2 Human Pre-designed siRNA Set A
    TMPRSS2 Human Pre-designed siRNA Set A
  • HY-130402B

    Parasite Infection
    Propamidine is a covalent inhibitor of TMPRSS2 and has some antibacterial activity. .
    Propamidine
  • HY-P990524

    Ser/Thr Protease Inflammation/Immunology
    The Anti-TMPRSS2 Antibody is a CHO-expressed humanized antibody that targets TMPRSS2. The Anti-TMPRSS2 Antibody features a huIgG1 heavy chain and a huκ light chain, with an expected molecular weight (MW) of 150 kDa. For the isotype control of the Anti-TMPRSS2 Antibody, please refer to Human IgG1 kappa, Isotype Control (HY-P99001).
    Anti-TMPRSS2 Antibody
  • HY-134432A

    Ser/Thr Protease Others
    Boc-Gln-Ala-Arg-AMC hydrochloride is a fluorogenic substrate for trypsin. Boc-Gln-Ala-Arg-AMC hydrochloride can also be used for measuring the proteolytic activity of TMPRSS2 [2].
    Boc-Gln-Ala-Arg-AMC hydrochloride
  • HY-RS23176

    Small Interfering RNA (siRNA) Others

    Tmprss2 Rat Pre-designed siRNA Set A contains three designed siRNAs for Tmprss2 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.

    Tmprss2 Rat Pre-designed siRNA Set A
    Tmprss2 Rat Pre-designed siRNA Set A
  • HY-161370

    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 .
    VD4162
  • HY-B0372AR

    Reference Standards 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 [2] .
    Bromhexine hydrochloride (Standard)
  • HY-163029

    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 .
    CTSL/B-IN-1
  • HY-158073

    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
    ML2006a4
  • HY-B0372AS

    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 [2] .
    Bromhexine-d3 hydrochloride
  • HY-161902

    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 .
    MI-1904
  • HY-174350

    Casein Kinase SARS-CoV Infection
    CK2-IN-15 (Compound Biv5) is a selective and potent bivalent protein kinase CK2 inhibitor with an IC50 value of 51 pM. CK2-IN-15 significantly reduces the replication of SARS-CoV-2 in HEK-ACE2-TMPRSS2 and Vero cells, and also reduces viral replication in an ex vivo model of human nasal epithelial cells. CK2-IN-15 is promising for research of β-coronavirus infection-related diseases .
    CK2-IN-15
  • HY-B1624C

    Debrisoquine hydrobromide; Isocaramidine hydrobromide; Ro 5-3307/1 hydrobromide

    SARS-CoV Ser/Thr Protease Infection
    Debrisoquine (Ro 5-3307/1) hydrobromide 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. Debrisoquine hydrobromide can be used for antiviral research .
    Debrisoquin hydrobromide
  • HY-179123

    Androgen Receptor Apoptosis Cancer
    ZC9 is a novel androgen receptor (AR) degrader. ZC9 directly binds to AR and inhibits Dihydrotestosterone-induced nuclear translocation of AR. ZC9 promotes AR degradation via the ubiquitin-proteasome system and suppresses AR transcriptional activity. ZC9 significantly decreases the mRNA levels of other AR downstream genes, including PSA, TMPRSS2, and PMEPA1. ZC9 promotes Apoptosis. ZC9 exhibits anticancer activity against prostate cancer .
    ZC9
  • HY-175344

    SARS-CoV Virus Protease Ser/Thr Protease Infection Inflammation/Immunology
    TMP1 is an orally active bispecific inhibitor of M pro (IC50 = 312.5 nM)/TMPRSS2 (IC50 = 1.28 μM, KD = 10.10 μM). TMP1 exhibits broad protection against different SARS-CoV-2 variants in vitro. TMP1 cross-protects against highly pathogenic coronaviruses (SARS-CoV-1, SARS-CoV-2, and MERS-CoV) in vivo and effectively blocks the transmission of SARS-CoV-2. TMP1 can inhibit infection by SARS-CoV-2 escape mutants that are resistant to Nivolumab (HY-P9903). TMP1 can be used in coronavirus research .
    TMP1
  • HY-173148

    SARS-CoV Infection
    TKB272 is an orally active and selective antiviral agent targeting the main protease (Mpro) of SARS-CoV-2. It effectively blocks the infection and replication of various SARS-CoV-2 strains, including Omicron variants such as XBB.1.5 and EG.5.1. The enzymatic inhibitory activity of TKB272 shows an IC50 of 0.7 µM (against SARS-CoV-2WK-521 Mpro), and its antiviral activity at the cellular level reaches an EC50 as low as 2.6 nM (against BQ.1.1 strain in HeLahACE2-TMPRSS2 cells), with a cytotoxicity CC50 of 98 µM, indicating no apparent toxicity. In addition, TKB272 significantly suppresses the replication of SARS-CoV-2XBB.1.5 in B6.Cg-Tg(K18-hACE2)2-Prlmn/J transgenic mouse models. TKB272 holds promise for research in the field of SARS-CoV-2 infection .
    TKB272
  • HY-173459

    SARS-CoV Infection
    N-0920 is a potent TMPRSS2 inhibitor with an IC50 of 0.35 nM. N-0920 effectively inhibits SARS-CoV-2 variants EG.5.1 and JN.1 entry in Calu-3 cells, with picomolar EC50s values of 300 pM and 90 pM, respectively .
    N-0920
  • HY-163067

    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 .
    SARS-CoV-2-IN-71
  • HY-170820

    Molecular Glues Bcl-2 Family CDK EGFR HSP Androgen Receptor c-Myc Cancer
    XYD049 is a CRBN-based molecular glue degrader targeting GSPT1, with a DC50 of 19 nM. XYD049 mediates the formation of a ternary complex between CRBN and GSPT1, thereby triggering CRBN- and proteasome-dependent degradation of GSPT1. By degrading GSPT1, XYD049 downregulates castration-resistant prostate cancer (CRPC)-related oncogenes, including BCL2, CDK2, E2F3, EGFR, HSP90B1, TMPRSS2, AR, AR-V7, PSA and c-Myc. XYD049 inhibits cancer cell growth and suppresses tumor growth in mice. XYD049 can be used for research on castration-resistant prostate cancer. XYD049 consists of a linker (black part) NH2-C5-NH-Boc (HY-W004710), a CRBN-based E3 ligase ligand (blue part) Thalidomide 4-fluoride (HY-41547), and a target protein ligand (red part) GSPT1 ligand-1 (HY-170821), among which the E3 ligase ligand plus linker forms the conjugate E3 Ligase Ligand-linker Conjugate 158 (HY-170822) .
    XYD049
  • HY-157021

    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 .
    SARS-CoV-2-IN-66
  • HY-156441

    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 .
    SARS-CoV-2-IN-65
  • HY-173421

    SARS-CoV Infection
    (H)S(OMe)-DFR-kbt (compound 9) is a potent and selective TMPRSS2 inhibitor with a Ki of 0.13 nM. (H)S(OMe)-DFR-kbt can be used in the study of SARS-CoV-2 .
    (H)S(OMe)-DFR-kbt
  • HY-157022

    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 .
    SARS-CoV-2-IN-67
  • HY-105747A

    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.
    Guanoxyfen nitrate
  • HY-117744

    Pim Endocrinology Cancer
    NMS-P645 is a PIM1 inhibitor. NMS-P645 exhibits anti-proliferative activity when combined with GDC-0941 (HY-50094) in TMPRSS2/ERG positive and negative PCa cells. NMS-P645 can reverse PIM1-induced pro-survival signals in prostate cells. NMS-P645 can be studied in research on prostate cancer .
    NMS-P645
  • HY-157154

    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 .
    MAT-POS-e194df51-1
  • HY-135794R

    11-KDHT (Standard); 5α-Dihydro-11-keto testosterone (Standard)

    Reference Standards Androgen Receptor Endocrinology
    11-Ketodihydrotestosterone (Standard) is the analytical standard of 11-Ketodihydrotestosterone. This product is intended for research and analytical applications. 11-Ketodihydrotestosterone (11-KDHT; 5α-Dihydro-11-keto testosterone) is an endogenous steroid and a metabolite of 11β-Hydroxyandrostenedione. 11-Ketodihydrotestosterone is an active androgen and is also a potent androgen receptor (AR) agonist with a Ki of 20.4 nM and an EC50 of 1.35 nM for human AR. 11-Ketodihydrotestosterone drives gene regulation, protein expression and cell growth in androgen-dependent prostate cancer cells [2].
    11-Ketodihydrotestosterone (Standard)
  • HY-162719

    DNA/RNA Synthesis 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 .
    RH12
  • HY-162604

    SARS-CoV Infection
    SARS-CoV-2-IN-90 (compound 3i) is a SARS-CoV-2 inhibitor. SARS-CoV-2-IN-90 can be used in coronavirus infection related research .
    SARS-CoV-2-IN-90
  • HY-179708

    Ser/Thr Protease Factor Xa SARS-CoV Influenza Virus Infection
    Cbz-QFR-kbt is a ketone-based benzothiazole ketone inhibitor of TMPRSS2, with an IC50 value of 0.42 nM. Cbz-QFR-kbt also has inhibitory activity against Matriptase, Hepsin, HGFA, and Factor Xa, with IC50 values of 1, 1.3, 85, and 85 nM respectively. Cbz-QFR-kbt shows significant inhibitory effects against SARS-CoV-2 and H1N1 (IC50 = 60 nM). Cbz-QFR-kbt can be used in antiviral research .
    Cbz-QFR-kbt

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