Search Result
Results for "
Fusion Inhibitors
" in MedChemExpress (MCE) Product Catalog:
1
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-P99777
-
TTI-621
|
CD47
|
Cancer
|
Ontorpacept (TTI-621) is a soluble fusion protein that consists of the human SIRPα N-terminal (1-118) linked to the Fc region of human IgG1. The N-terminal (1-118)-fragment of ontorpacept is a binding domain for CD47 which is an inhibitor of phagocytosis by macrophages. Ontorpacept is a CD47-blocking checkpoint inhibitor with antitumor activity .
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-
-
- HY-122907
-
|
Influenza Virus
|
Infection
|
JNJ4796 is an oral active fusion inhibitor of influenza virus, neutralizing influenza A group 1 viruses by inhibiting hemagglutinin (HA)-mediated fusion. JNJ4796 mimics the functionality of the broadly neutralizing antibodies (bnAbs) .
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-
-
- HY-19810
-
-
-
- HY-P0052A
-
T20 acetate; DP178 acetate
|
HIV
|
Infection
|
Enfuvirtide (T20; DP178) acetate is an anti-HIV-1 fusion inhibitor peptide.
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-
-
- HY-11097
-
|
RSV
|
Infection
|
TMC353121 is a potent respiratory syncytial virus (RSV) fusion inhibitor with pEC50 of 9.9.
|
-
-
- HY-P10517
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SFT
|
HIV
|
Infection
|
Sifuvirtide (SFT) is a potent HIV fusion inhibitor. Sifuvirtide inhibits HIV-1 mediated cell fusion in a dose-dependent manner and is highly potent against infection by primary and laboratory-adapted HIV-1 isolates of multiple genotypes. Sifuvirtide can be used in the research of anti-HIV drugs .
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-
-
- HY-146108
-
|
RSV
|
Infection
|
RSV-IN-5 (Compound 4) is a potent dual inhibitor of wild-type and mutant respiratory syncytial virus (RSV) fusion proteins. RSV-IN-5 exhibits potent anti-RSV activities against not only wild-type A2 F protein (EC50=2.0 nM), but also D486N-mutant F protein (EC50=8.1 nM) .
|
-
-
- HY-P4110
-
|
iGluR
|
Metabolic Disease
Inflammation/Immunology
|
TAT-NSF222 Fusion Peptide is a fusion polypeptide with two domains, a TAT domain, which enters cells through macropinocytosis, and an NSF domain that inhibits N-ethylmaleimide-sensitive factor (NSF). TAT-NSF222 Fusion Peptide is an exocytosis inhibitor .
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-
-
- HY-122204
-
|
HIV
|
Infection
|
5M038 is an inhibitor of HIV envelope-mediated fusion with potent inhibitory activity against gp41-mediated membrane fusion. 5M038 prevents the formation of the gp41 post-fusion conformation and inhibits envelope-mediated membrane fusion in cell-cell fusion and viral infectivity assays. 5M038 has shown broad fusion inhibition in tests against multiple HIV-1 subtypes, including M and T strains. 5M038 targets a highly conserved hydrophobic pocket and binds to the gp41 trimer, thereby exerting its inhibitory effect .
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-
-
- HY-19874
-
|
RSV
|
Infection
|
RFI-641 is a selective inhibitor of the respiratory syncytial virus (RSV), with an IC50 of 50 nM. RFI-641 inhibit binding and fusion of enveloped virus via interaction with the viral fusion protein .
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-
-
- HY-16727
-
GS-5806
|
RSV
|
Infection
|
Presatovir (GS-5806) is an orally bioavailable RSV fusion inhibitor with a mean EC50 value of 0.43 nM .
|
-
-
- HY-P0052
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T20; DP178
|
HIV
|
Infection
|
Enfuvirtide (T20;DP178) is an anti-HIV-1 fusion inhibitor peptide.
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-
-
- HY-76648
-
|
HIV
|
Infection
|
NBD-556, a CD4 mimetic, is a potent HIV-1 entry inhibitor that blocks the gp120-CD4 interaction. NBD-556 shows potent cell fusion and virus-cell fusion inhibitory activity at low micromolar levels .
|
-
-
- HY-112180
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JNJ-678; JNJ-53718678
|
RSV
|
Infection
|
Rilematovir (JNJ-678) is a novel fusion protein inhibitor. Rilematovir has the potential for respiratory syncytial virus (RSV) research.
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-
-
- HY-12994
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MDT-637
|
RSV
|
Infection
|
MDT-637 (VP 14637) is a novel respiratory syncytial virus (RSV) fusion inhibitor with an IC50 of 1.42 ng/mL.
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-
-
- HY-129111
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EACC
3 Publications Verification
|
Autophagy
|
Infection
Neurological Disease
|
EACC is a reversible autophagy inhibitor, which can block autophagic flux. EACC selectively inhibits the translocation of autophagosome-specific SNARE Stx17 thereby blocking autophagosome-lysosome fusion .
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-
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- HY-B0795
-
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mTOR
Autophagy
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Cancer
|
MHY1485 is a potent cell-permeable mTOR activator that targets the ATP domain of mTOR. MHY1485 inhibits autophagy by suppression of fusion between autophagosomes and lysosomes .
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-
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- HY-114437
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Z-D-Phe-Phe-Gly-OH; FIP; Virus Replication Inhibitory Peptide
|
Influenza Virus
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Infection
|
Fusion Inhibitory Peptide (Z-D-Phe-Phe-Gly-OH, FIP, Virus Replication Inhibitory Peptide) is a potent inhibitor of the virus replication, by inhibiting the membrane fusing activity of a viral glycoprotein .
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-
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- HY-P5497
-
|
HIV
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Others
|
C34 peptide is a biological active peptide. (This C34 peptide, also known as HR2, belongs to the helical region of gp41 of HIV, C-terminal heptad repeat 2 (HR2) defined as C helix or C peptide. It is known that HIV-1 enters cells by membrane fusion, C34 gp41 peptide is a potent inhibitors of HIV-1 fusion.)
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-
-
- HY-134921
-
|
Epigenetic Reader Domain
|
Cancer
|
MI-nc dihydrochloride is a weak inhibitor of the Menin-MLL fusion protein interaction with an IC50 of 193 μM. MI-nc dihydrochloride can be used as a negative control compound of MI-2 .
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-
-
- HY-W048674
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Fmoc-O-acetyl-L-serine
|
Amino Acid Derivatives
|
Infection
|
Fmoc-Ser(Ac)-OH (Fmoc-O-acetyl-L-serine) is a Serine derivative. Fmoc-Ser(Ac)-OH can be used for the preparation of broad-spectrum coronavirus membrane fusion inhibitor .
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-
-
- HY-124871
-
|
Arenavirus
|
Infection
|
LASV inhibitor 3.3 is a Lassa fever virus (LASV) inhibitor. LASV inhibitor 3.3 binds with LASV glycoprotein (GP) and promotes virus membrane fusion and infection. LASV inhibitor 3.3 can be used for LASV infection research .
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-
-
- HY-160880
-
|
Others
|
Infection
|
EBOV-IN-5 (compound 14) is an antiviral agent that inhibits Ebola virus (EBOV) infection. EBOV-IN-5 inhibits the binding of the EBOV glycoprotein EBOV-GPcl to NPC1, an indispensable host receptor required for viral fusion/entry .
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-
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- HY-P10308
-
|
HIV
|
Infection
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[(Cys(Bzl)84,Glu(OBzl)85)]CD4 (81-92) is a selective inhibitor of HIV-1. [(Cys(Bzl)84,Glu(OBzl)85)]CD4 (81-92) inhibits viral infection and cell fusion by blocking the interaction between HIV-1 and CD4 molecules. [(Cys(Bzl)84,Glu(OBzl)85)]CD4 (81-92) can completely inhibit fusion formation at a concentration of 25 μM .
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-
-
- HY-142645
-
|
RSV
|
Infection
|
TP0591816 is a potent dual inhibitor of wild-type and mutant respiratory syncytial virus fusion proteins (wild-type, EC50 = 0.27 nM; D486N-mutant, EC50 = 0.70 nM).
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-
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- HY-146807
-
|
Trk Receptor
|
Cancer
|
Type II TRK inhibitor 1 is a potent TRK inhibitor, which inhibits various TRK fusion protein variants and wild type. Type II TRK inhibitor 1 exhibits antiproliferative activity against Ba/F3 cells harboring CD74-TRKA G667C and ETV6-TRKC G696C fusion proteins with IC50s of 6 nM and 1.7 nM, respectively . Type II TRK inhibitor 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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-
-
- HY-131059
-
|
Influenza Virus
|
Infection
|
CBS1117 is a virus entry inhibitor with an IC50 of 70 nM for influenza A virus, A/Puerto Rico/8/34 (H1N1). CBS1117 interferes with the hemagglutinin (HA)-mediated fusion process .
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-
-
- HY-156794
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DSP-5336
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Others
|
Cancer
|
Enzomenib is an inhibitor of the menin protein encoded by the multiple endocrine neoplasia (MEN) gene. Enzomenib can block the binding of the menin protein to mixed lineage leukemia (MLL) fusion proteins and can be used in the study of hematological malignancies .
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-
-
- HY-119375
-
|
Bacterial
|
Infection
|
Syncytial Virus Inhibitor-1 is a potent, orally bioavailable respiratory syncytial virus (RSV) fusion inhibitor with EC50s of 0.002 μM, 0.004 μM, and 0.002 μM for RSV Long, RSV A2, and RSV B strains, respectively .
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-
-
- HY-123475A
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RV521 hydrochloride
|
RSV
|
Infection
|
Sisunatovir (RV521) hydrochloride, an orally available inhibitor of the RSV fusion (RSV-F) protein, exhibits potent efficacy against a panel of clinical isolates of RSV-A and RSV-B viruses, with IC50s of 1.4 nM and 1.0 nM, respectively .
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-
-
- HY-P10437
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human α1-AT(353-372)
|
HIV
|
Infection
|
VIRIP (human α1-AT(353-372)) is a HIV-1 inhibitor. VIRIP blocks the entry of HIV-1 by interacting with gp41 fusion peptide. VIRIP can be used for virus research .
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-
-
- HY-23193
-
|
Influenza Virus
|
Infection
|
BMS-199945 is a influenza virus fusion inhibitor with the IC50 values of 0.57 μM and approximately 1 μM aganist influenza A/WSN/33 virus-induced hemolysis of chicken RBC and in the trypsin protection assay, respectively .
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-
-
- HY-P1753
-
|
HIV
|
Infection
|
VIR-165 is a modified form of virus inhibitory peptide (VIRIP) that binds the fusion peptide of the gp41 subunit and prevents its insertion into the target membrane. VIRIP inhibits a wide variety of human immunodeficiency virus type 1 (HIV-1) strains .
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-
-
- HY-P35433
-
T-1249
|
HIV
|
Inflammation/Immunology
|
Tifuvirtide (T-1249) is a peptide human immunodeficiency virus type-1 (HIV-1) fusion inhibitor. Tifuvirtide is a synthetically designed hybrid retroviral envelope polypeptide. Tifuvirtide has antiretroviral activity. Tifuvirtide can be used for the research of HIV infection .
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-
-
- HY-108847
-
|
TNF Receptor
Bacterial
|
Inflammation/Immunology
Cancer
|
Etanercept, a dimeric fusion protein that binds TNF, acts as a TNF inhibitor. Etanercept competitively inhibits the binding of both TNF-α and TNF-β to cell surface TNF receptors, rendering TNF biologically inactive. Etanercept shows efficacy against rheumatoid arthritis, juvenile idiopathic arthritis, and plaque psoriasis .
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-
-
- HY-155514
-
|
Influenza Virus
|
Inflammation/Immunology
|
HA-IN-1 (compound 5g) is a Hemagglutinin (HA) ligand with high affinity, targeting to the trypsin cleavage site of HA. HA-IN-1 inhibits HA-mediated membrane fusion and reduces the pulmonary virus titer in vivo. HA-IN-1 is a potential influenza A virus (IAV) inhibitor, and an anti-influenza agent .
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-
-
- HY-108822
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Arcalyst; IL 1 Trap; Interleukin 1 Trap
|
Interleukin Related
|
Inflammation/Immunology
|
Rilonacept (Arcalyst), a dimeric fusion protein, is a interleukin 1 inhibitor. Rilonacept consists of the ligand-binding domains of the extracellular portions of the IL-1R components linked to the Fc portion of human IgG1. Rilonacept can be used for the research of cryopyrin-associated periodic syndromes .
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-
-
- HY-14904A
-
|
Influenza Virus
SARS-CoV
|
Infection
|
Umifenovir hydrochloride is a potent, orally active broad-spectrum antiviral with activity against a number of enveloped and non-enveloped viruses. Umifenovir hydrochloride is used as an anti-influenza virus agent. Umifenovir hydrochloride could effectively inhibit the fusion of virus with host cells . Umifenovir hydrochloride is an efficient inhibitor of SARS-CoV-2 in vitro. Anti-inflammatory activity .
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-
-
- HY-112698
-
|
p62
Atg8/LC3
Autophagy
Apoptosis
|
Cancer
|
CA-5f is a potent late-stage macroautophagy/autophagy inhibitor via inhibiting autophagosome-lysosome fusion. CA-5f increases LC3B-II (a marker to monitor autophagy) and SQSTM1 protein, and also increases ROS production. Anti-tumor activity .
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-
-
- HY-106428
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ITF1697
|
P-selectin
|
Cardiovascular Disease
Inflammation/Immunology
|
Icrocaptide (ITF1697) is a stable Lys-Pro-containing peptide that inhibits the intracellular Ca 2+-dependent fusion of Weibel-Palade bodies with the plasma membrane. Icrocaptide exerts its activity at the early stages of endothelial activation and inhibits P-selectin and von Willebrand factor secretion. Icrocaptide can be used for the study of a variety of microvascular disorders .
|
-
-
- HY-109142
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AK0529; RO-0529
|
RSV
|
Infection
|
Ziresovir (AK0529;RO-0529) is a potent, selective, and orally bioavailable respiratory syncytial virus (RSV) fusion (F) protein (RSV F) protein inhibitor. Ziresovir shows anti-RSV activity (EC50=3 nM) and highlights pharmacokinetics in animal species .
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-
-
- HY-131042
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NNMTi
3 Publications Verification
|
Others
|
Metabolic Disease
|
NNMTi is a potent nicotinamide N-methyltransferase (NNMT) inhibitor (IC50=1.2 μM) and selectively binds to the NNMT substrate-binding site residues . NNMTi promotes myoblast differentiation in vitro and enhances fusion and regenerative capacity of muscle stem cells (muSCs) in aged mice .
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-
-
- HY-19587
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NSC335153
|
DNA/RNA Synthesis
|
Cancer
|
Ditercalinium chloride is an anticancer agent. Ditercalinium chloride inhibits human DNA polymerase gamma activity. Ditercalinium chloride can deplete mitochondrial DNA in both mouse and human cells. Ditercalinium chloride is a potential ligand against the COMMD10-AP3S1 fusion protein .
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-
-
- HY-159625
-
Ro 91-4714
|
PIKfyve
|
Cancer
|
WX8 (Ro 91-4714) is an ATP-competitive PIKFYVE inhibitor, with Kd values of 0.9 nM and 340 nM for PIKFYVE and PIP4K2C, respectively. WX8 (Ro 91-4714) inhibits lysosomal fission without effecting homotypic lysosomal fusion. WX8 (Ro 91-4714) is used in the research of autophagy-dependent cancer .
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-
-
- HY-168616
-
|
RSV
IGF-1R
|
Infection
|
CL-A3-7 is a virus-cell fusion inhibitor targeting the RSV F protein. It exerts its effect by blocking the interaction between the virus and the host IGF1R, effectively inhibiting infections of both wild-type RSV and the K394R variant. It is applicable to anti-RSV drug development and resistance-related research .
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-
-
- HY-144321
-
|
Trk Receptor
|
Cancer
|
Trk-IN-9 (Compound 12) is a potent inhibitor of TRK. Trk-IN-9 inhibits the proliferation of Km-12 cell lines. Trk-IN-9 induces the apoptosis of Km-12 cells in a concentration-dependent manner. Trk-IN-9 inhibits the phosphorylation of TRK to block downstream pathways. Trk-IN-9 has the potential for the research of NTRK-fusion cancers .
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-
-
- HY-148202
-
|
HIV
|
Infection
|
Influenza antiviral conjugate-1 (INT-2) is a HIV inhibitor, shows potent cell fusion inhibition . Influenza antiviral conjugate-1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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-
-
- HY-13491
-
|
Trk Receptor
|
Cancer
|
GNF-5837 is a potent, selective, and orally bioavailable pan-tropomyosin receptor kinase (TRK) inhibitor which display antiproliferative effects in cellular Ba/F3 assays ( IC50 values of 7 nM, 9 nM and 11 nM for cells containing the fusion proteins Tel-TrkC, Tel-TrkB and Tel-TrkA, respectively) .
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-
-
- HY-141429
-
|
Histone Methyltransferase
Apoptosis
|
Cancer
|
AS-99 is a first-in-class, potent and selective ASH1L histone methyltransferase inhibitor (IC50= 0.79 µM, Kd= 0.89 µM) with anti-leukemic activity. AS-99 blocks cell proliferation, induces apoptosis and differentiation, downregulates MLL fusion target genes, and reduces the leukemia burden in vivo .
|
-
-
- HY-141429C
-
|
Histone Methyltransferase
Apoptosis
|
Cancer
|
AS-99 is a first-in-class, potent, and selective ASH1L histone methyltransferase inhibitor (IC50= 0.79 µM, Kd= 0.89 µM) with anti-leukemic activity. AS-99 blocks cell proliferation, induces apoptosis and differentiation, downregulates MLL fusion target genes, and reduces the leukemia burden in vivo .
|
-
- HY-P99720
-
ACE-536; luspatercept–aamt
|
TGF-beta/Smad
|
Metabolic Disease
Cancer
|
Luspatercept (ACE-536) is a recombinant modified ActRIIB fusion protein that binds with transforming growth factor β superfamily ligands. Luspatercept increases the erythrocyte numbers and promotes maturation of erythroid precursors. Luspatercept binds with GDF11 and inhibits Smad2/3 signaling. Luspatercept can be used for the research of anemia .
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-
- HY-112301
-
BLU-667
|
RET
|
Cancer
|
Pralsetinib (BLU-667) is a highly potent, selective RET inhibitor. Pralsetinib (BLU-667) inhibits WT RET, RET mutants V804L, V804M, M918T and CCDC6-RET fusion with IC50s of 0.4, 0.3, 0.4, 0.4, and 0.4 nM, respectively .
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-
- HY-14904
-
|
SARS-CoV
Influenza Virus
|
Infection
|
Umifenovir is a potent, orally active broad-spectrum antiviral agent with activity against a number of enveloped and non-enveloped viruses. Umifenovir is used as an anti-influenza virus agent. Umifenovir could effectively inhibit the fusion of virus with host cells . Umifenovir is an efficient inhibitor of SARS-CoV-2 in vitro . Umifenovir shows anti-inflammatory activity .
|
-
- HY-100558
-
Bafilomycin A1
Maximum Cited Publications
470 Publications Verification
BafA1
|
Proton Pump
Autophagy
Antibiotic
Bacterial
Apoptosis
|
Infection
Cancer
|
Bafilomycin A1 (BafA1) is a specific and reversible inhibitor of vacuolar H +-ATPase (V-ATPase) with IC50 values of 4-400 nmol/mg. Bafilomycin A1, a macrolide antibiotic, is also used as an autophagy inhibitor at the late stage. Bafilomycin A1 blocks autophagosome-lysosome fusion and inhibits acidification and protein degradation in lysosomes of cultured cells. Bafilomycin A1 induces apoptosis .
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-
- HY-153386
-
|
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
CPD-1224 is an orally effective ALK inhibitor, a derivative of an ALK inhibitor that connects to the cereblon ligand. CPD-1224 targets the EML4-ALK oncogenic fusion protein and degrades both ALK and the mutant forms L1196M/G1202R. CPD-1224 can slow down tumor growth .
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-
- HY-153331
-
|
WDR5
|
Cancer
|
DDO-2213 is an orally active and potent WDR5-MLL1 inhibitor, with an IC50 of 29 nM and a Kd value of 72.9 nM for the WDR5 protein. DDO-2213 selectively inhibits MLL (mixed lineage leukemia) histone methyltransferase activity and the proliferation of MLL translocation-harboring cells. DDO-2213 can be used for MLL fusion leukemia research .
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-
- HY-141429A
-
|
Histone Methyltransferase
Apoptosis
|
Cancer
|
AS-99 TFA is a first-in-class, potent and selective ASH1L histone methyltransferase inhibitor (IC50= 0.79 µM, Kd= 0.89 µM) with anti-leukemic activity. AS-99 TFA blocks cell proliferation, induces apoptosis and differentiation, downregulates MLL fusion target genes, and reduces the leukemia burden in vivo .
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-
- HY-150072
-
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PKA
|
Cancer
|
DS89002333 is an orally active and potent PRKACA inhibitor, with an IC50 of 0.3 nM. DS89002333 shows good anti-tumor activity in an FL-HCC patient-derived xenograft model (expressing the DNAJB1-PRKACA fusion gene). DS89002333 can be used in study of fibrolamellar hepatocellular carcinoma (FL-HCC) .
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-
- HY-P99268
-
SAR 256212; MM 121; Anti-Human ERBB3/ErbB 3 Recombinant Antibody
|
EGFR
Apoptosis
|
Cancer
|
Seribantumab (MM 121) is a fully human IgG2 monoclonal antibody that targets HER3. Seribantumab blocks the activation of epidermal growth factor receptor (ErbB) family members and its downstream signal. Seribantumab inhibits neuregulin 1 (NRG1) fusion-dependent tumorigenesis in vitro and in vivo in breast, lung and ovarian patient-derived cancer models .
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-
- HY-152292
-
NVL-520; NUV-520
|
ROS Kinase
|
Cancer
|
Zidesamtinib (NVL-520) is a potent, selective, orally active and brain-penetrant inhibitor of diverse ROS1 fusions and resistance mutations, with IC50s of 0.7 and 7.9 nM for wild-type ROS1 and ROS1 G2032R, respectively, and spares TRK inhibition. Zidesamtinib can be used for the research of cancer .
|
-
- HY-149368
-
|
SARS-CoV
|
Infection
|
SARS-CoV-2-IN-51 (S-10) is a potent lead compound of Omicron fusion inhibitor. SARS-CoV-2-IN-51 inhibits Omicron and other variants with EC50s of 0.82-5.45 μM. SARS-CoV-2-IN-51 inhibits SARS-CoV-2 virus entry, by the direct interaction with S in the prefusion state .
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-
- HY-14904AS
-
|
Isotope-Labeled Compounds
Influenza Virus
SARS-CoV
|
Infection
|
Umifenovir-d6 (hydrochloride) is the deuterium labeled Umifenovir hydrochloride. Umifenovir hydrochloride is a potent, orally active broad-spectrum antiviral with activity against a number of enveloped and non-enveloped viruses. Umifenovir hydrochloride is used as an anti-influenza virus agent. Umifenovir hydrochloride could effectively inhibit the fusion of virus with host cells[1][2]. Umifenovir hydrochloride is an efficient inhibitor of SARS-CoV-2 in vitro. Anti-inflammatory activity[3].
|
-
- HY-150636
-
|
Autophagy
Apoptosis
|
Cancer
|
Autophagy-IN-1 is a potent autophagy/mitophagy inhibitor, acts by selectively increasing the autophagic flux while blocking the autophagosome-lysosome fusion in cancer cells. Autophagy-IN-1 can induce apoptosis and cell cycle arrest. Autophagy-IN-1 significantly inhibits tumor growth in an HCT116 xenograft mouse model and with low toxicity. Autophagy-IN-1 can be used for researching colorectal cancer .
|
-
- HY-116182
-
|
Influenza Virus
|
Infection
|
RO5487624, an analogue of RO5464466 (HY-120690), is an orally active hemagglutinin (HA) inhibitor of influenza H1N1 viruses that abolishes influenza virus fusion by blocking HA conformational changes in low pH environments. RO5487624 displays a protective effect on mice that are lethally challenged with influenza H1N1 virus .
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-
- HY-14904AR
-
|
Influenza Virus
SARS-CoV
|
Infection
|
Umifenovir (hydrochloride) (Standard) is the analytical standard of Umifenovir (hydrochloride). This product is intended for research and analytical applications. Umifenovir hydrochloride is a potent, orally active broad-spectrum antiviral with activity against a number of enveloped and non-enveloped viruses. Umifenovir hydrochloride is used as an anti-influenza virus agent. Umifenovir hydrochloride could effectively inhibit the fusion of virus with host cells . Umifenovir hydrochloride is an efficient inhibitor of SARS-CoV-2 in vitro. Anti-inflammatory activity .
|
-
- HY-152100
-
|
Autophagy
|
Cancer
|
CUR5g is a potent autophagy inhibitor. CUR5g selectively inhibits autophagosome degradation in cancer cells by blocking autophagosome-lysosome fusion. CUR5g blocks the recruitment of STX17 to autophagosomes via a UVRAG-dependent mechanism, resulting in the inability of autophagosomes to fuse with lysosomes. CUR5g improves the anticancer effect of Cisplatin (HY-17394) against A549 cells both in vitro and in vivo .
|
-
- HY-163004
-
|
Trk Receptor
|
Cancer
|
Type II TRK inhibitor 2 (compound 40l) is a selective type II TRK inhibitor with plasma stability and moderate hepatic microsomal stability. Type II TRK inhibitor 2 significantly inhibits Km-12, Ba/F3-TRKA G595R and Ba/F3-TRKA G667C cell proliferation (IC50: 4.1 nM, 41.5 nM, 1.4 nM). Type II TRK inhibitor 2 can be used to study NTRK fusion cancers .
|
-
- HY-N0485
-
|
Autophagy
Mitophagy
|
Cardiovascular Disease
|
Liensinine Diperchlorate is a major isoquinoline alkaloid, extracted from the seed embryo of Nelumbo nucifera Gaertn. Liensinine Diperchlorate inhibits late-stage autophagy/mitophagy through blocking autophagosome-lysosome fusion. Liensinine Diperchlorate has a wide range of biological activities, including anti-arrhythmias, anti-hypertension, anti-pulmonary fibrosis, relaxation on vascular smooth muscle, etc .
|
-
- HY-N10177
-
|
HSV
|
Infection
|
Peniterphenyl A is a natural product obtained from a deep-sea-derived Penicillium sp. Peniterphenyl A inhibits HSV-1/2 virus entry into cells and may block HSV-1/2 infection through direct interaction with virus envelope glycoprotein D to interfere with virus adsorption and membrane fusion. Peniterphenyl A is a promising lead compound against HSV-1/2 .
|
-
- HY-112301R
-
|
RET
|
Cancer
|
Pralsetinib (Standard) is the analytical standard of Pralsetinib. This product is intended for research and analytical applications. Pralsetinib (BLU-667) is a highly potent, selective RET inhibitor. Pralsetinib (BLU-667) inhibits WT RET, RET mutants V804L, V804M, M918T and CCDC6-RET fusion with IC50s of 0.4, 0.3, 0.4, 0.4, and 0.4 nM, respectively .
|
-
- HY-14904R
-
|
SARS-CoV
Influenza Virus
|
Infection
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Umifenovir (Standard) is the analytical standard of Umifenovir. This product is intended for research and analytical applications. Umifenovir is a potent, orally active broad-spectrum antiviral agent with activity against a number of enveloped and non-enveloped viruses. Umifenovir is used as an anti-influenza virus agent. Umifenovir could effectively inhibit the fusion of virus with host cells . Umifenovir is an efficient inhibitor of SARS-CoV-2 in vitro . Umifenovir shows anti-inflammatory activity .
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-
- HY-161819
-
|
Trk Receptor
|
Cancer
|
TRK-IN-29 (Compound B31) is a second-generation TRK inhibitor (IC50: 9 nM, 0.6 nM, 18 nM, 5 nM, 6 nM for TRKA G595R, TRKA F589L, TRKA G667C, TRKA and TRKC respectively). TRK-IN-29 inhibits the phosphorylation of TRKA. TRK-IN-29 has good antiproliferative activities against NTRK fusion positive cells. TRK-IN-29 has exellent plasma stability and moderate pharmacokinetic properties .
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-
- HY-159147
-
|
PROTACs
ROS Kinase
Apoptosis
|
Cancer
|
SIAIS039 is an orally active c-ros oncogene 1 (ROS1)-specific PROTAC with DC50s of 154.46 nM, 126.47 nM, 143.69 nM for HCC78 cells, Ba/F3 expressing the CD74-ROS1 fusion and Ba/F3 expressing the SDC4-ROS1 fusion, respectively. SIAIS039 suppresses cell proliferation, induces cell cycle arrest and apoptosis, and inhibits clonogenicity against ROS1-positive cells. SIAIS039 demonstrates anti-tumour effects against ROS1-driven tumor growth vivo. SIAIS039 is composed of the ALK inhibitor Brigatinib (HY-12857), a linker EM-12 (HY-138793), and a VHL ligand E3 ubiquitin ligase 1-Butyne (Red: Brigatinib; Blue: VHL ligand; Black: linker) .
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-
- HY-12220
-
MM-102
4 Publications Verification
HMTase Inhibitor IX
|
Histone Methyltransferase
Apoptosis
NF-κB
TNF Receptor
Interleukin Related
|
Inflammation/Immunology
Cancer
|
MM-102 (HMTase Inhibitor IX) is a cell-permeable and tightly binding inhibitor of MLL1-WDR5 interaction (IC50=2.4 nM). MM-102 can specifically inhibit the growth and induce apoptosis of leukemia cells containing MLL1 fusion protein, and reduce renal fibrosis and inflammation in mice with ischemia-reperfusion injury. In addition, MM-102 also acts as an H3K4 histone methyltransferase inhibitor to improve the development of porcine somatic cell nuclear transfer (SCNT) embryos .
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-
- HY-124582
-
NEO214
1 Publications Verification
|
Autophagy
mTOR
|
Cancer
|
NEO214 is an autophagy inhibitor and a covalent conjugate of the PDE4 inhibitor Rolipram (HY-16900) and perillyl alcohol (HY-N7000). It has anti-cancer activity and blood-brain barrier (BBB) permeability. Over sex. NEO214 prevents autophagy-lysosome fusion, thereby blocking autophagic flux and triggering glioma cell death. The process involves mTOR activation, andTFEB(Transcription Factor EB) aggregation. NEO214 inhibitionMacroautophagy/autophagy in glioblastoma cells has the potential to overcome chemotherapy resistance in glioblastoma .
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-
- HY-135960
-
|
FGFR
Apoptosis
|
Cancer
|
BO-264 is a highly potent and orally active transforming acidic coiled-coil 3 (TACC3) inhibitor with an IC50 of 188 nM and a Kd of 1.5 nM. BO-264 specifically blocks the function of FGFR3-TACC3 fusion protein. BO-264 induces spindle assembly checkpoint (SAC)-dependent mitotic arrest, DNA damage and apoptosis. BO-264 has broad-spectrum antitumor activity .
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-
- HY-P99463
-
AVB-S6-500
|
TAM Receptor
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Cancer
|
Batiraxcept (AVB-S6-500) is a highly potent and specific AXL inhibitor, a recombinant fusion protein dimer containing the extracellular domain of human AXLM and human immunoglobulin G1 heavy chain (Fc). Batiraxcept binds to GAS6 and inhibits the interaction of GAS6 with AXL, thereby substantially reducing AXL signaled invasion and migration of highly metastatic cells in vitro and inhibiting metastatic disease in nonclinical models of aggressive human cancers. Batiraxcept is available for studies in advanced or metastatic clear cell renal cell carcinoma (ccRCC) and platinum sensitive recurrent ovarian cancer .
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-
- HY-150561
-
|
Trk Receptor
|
Cancer
|
Trk-IN-20 is a kind of 3-vinylindazole derivatives. Trk-IN-20 suppresses Trk kinases functions by phosphorylation inhibition of TrkA/B/C with IC50 values of 1.6 nM, 2.9 nM and 2.0 nM, respectively .
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-
- HY-P990088
-
|
VEGFR
PD-1/PD-L1
|
Cardiovascular Disease
|
Sotiburafusp alfa is a bispecific fusion protein, which is a humanized VEGFR-1 extracellular domain fragment (129-228, 1-100 in the current sequence) fused via the peptide linker 101GGSGGSGGSGGSGGS 115 to the N-terminus of the heavy chain (116-564) of a humanized IgG1-kappa anti-human PD-L1 heavy chain variant L352>A, L353>A. Sotiburafusp alfa is also an angiogenesis inhibitor .
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-
- HY-168551
-
|
PROTACs
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
PROTAC ALK degrader-3 (4B) is an orally active ALK degrader based on PROTACs, which can effectively induce persistent degradation of ALK fusion protein in Karpas 299 cells and strong inhibition of downstream pathways,IC50 is 119.33 nM. PROTAC ALK degrader-3 exhibits antitumor activity. (Structure Note: PINK, ALK Inhibitor (HY-15656); Blue, E3 (HY-W023573); Black, linker (HY-168552)) .
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-
- HY-P5395
-
|
HIV
|
Others
|
TAT-GluR23A Fusion Peptide is a biological active peptide. (This is the GluR23A sequence, a control inactive peptide used as a mutant counterpart to glutamate receptor endocytosis inhibitor (GluR23Y), connected to an 11 amino acid cell permeable HIV Trans-Activator of Transcription (TAT) protein transduction domain (PTD). GluR23A is derived from GluR23Y amino acids 869 to 877, with Ala substituted for Tyr, and thus lacking essential phosphorylation sites.Control peptide of HY-P2259)
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-
- HY-P3492
-
|
SARS-CoV
|
Infection
|
SARS-CoV-2-IN-34 (S-20-1) is a blood brain barrier penetrable pan-coronavirus (CoV) fusion inhibitor with broad-spectrum inhibitory activity. SARS-CoV-2-IN-34 effectively inhibits infection by pseudotyped and authentic SARS-CoV-2, and pseudotyped variants of concern (VOCs). SARS-CoV-2-IN-34 shows high affinity to RBD in S1 and HR1 domain in S2 of SARS-CoV-2 S protein. SARS-CoV-2-IN-34 can be used for the research of infection .
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-
- HY-P2200
-
BMY-29304
|
HIV
Antibiotic
|
Infection
Inflammation/Immunology
|
Siamycin I (BMY-29304), a 21-residue tricyclic peptide, is a secondary metabolite in actinomycetes. Siamycin I is a HIV fusion inhibitor with ED50s of 0.05 to 5.7 μM for acute HIV type 1 (HIV-1) and HIV-2 infections. Siamycin I inhibits the gelatinase and gelatinase biosynthesis-activating pheromone (GBAP) signaling via the FsrC-FsrA two-component regulatory system in a noncompetitive manner. Siamycin I suppresses the expression of both fsrBDC and gelE-sprE transcripts. Siamycin I, a lasso peptide, interacts with lipid II and inhibits cell wall biosynthesis. Siamycin I, an antibiotic, has the potential for enterococcal infections research .
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-
- HY-137465
-
|
PROTACs
Trk Receptor
|
Cancer
|
CG428 is a potent and selective tropomyosin receptor kinase (TRK) PROTAC degrader that has anti-tumor activity. CG428 reduces levels of the tropomyosin 3 (TPM3)-TRKA fusion protein in KM12 colorectal carcinoma cells (DC50 = 0.36 nM) and inhibits downstream PLCγ1phosphorylation (IC50 = 0.33 nM). CG428 has a higher binding affinity for TRKA than TRKB and TRKC (Kd = 1 nM, 28 nM and 4.2 nM, respectively). In addition, CG428 effectively inhibits KM12 cell growth (IC50 = 2.9 nM) .(Pink: TRK inhibitor (HY-118271); Black: linker (HY-W067489); Blue: CRBN Ligand (HY-41547))
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-
- HY-161804
-
|
PROTACs
Dengue virus
|
Infection
|
GNF-2-deg is a PROTAC degrader for dengue virus envelope protein (DENV E protein) with DC50 of 0.83 μM. GNF-2-deg prevents viral entry by inhibiting E-mediated membrane fusion, prevents virion production by protein degradation, and thereby exhibits antiviral activity against DENV 2 with EC90 of 3.5 μM. GNF-2-deg exhibits antiviral activity against ZIKV, JEV, WNV and YFV with EC90 of 1.96-7.79 μM. (Pink: ligand for target protein (HY-161805); Black: linker (HY-42149); Blue: ligand for E3 ligase (HY-23095))
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-
Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P4113
-
|
Peptides
|
Neurological Disease
|
TAT-NSF700 Fusion Peptide is a potent N-ethyl-maleimide-sensitive factor (NSF) inhibitor. TAT-NSF700 Fusion Peptide can readily permeate the cell membrane and interact with the intracellular organelle directly .
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-
- HY-P0052A
-
T20 acetate; DP178 acetate
|
HIV
|
Infection
|
Enfuvirtide (T20; DP178) acetate is an anti-HIV-1 fusion inhibitor peptide.
|
-
- HY-P0052
-
T20; DP178
|
HIV
|
Infection
|
Enfuvirtide (T20;DP178) is an anti-HIV-1 fusion inhibitor peptide.
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-
- HY-114437
-
Z-D-Phe-Phe-Gly-OH; FIP; Virus Replication Inhibitory Peptide
|
Influenza Virus
|
Infection
|
Fusion Inhibitory Peptide (Z-D-Phe-Phe-Gly-OH, FIP, Virus Replication Inhibitory Peptide) is a potent inhibitor of the virus replication, by inhibiting the membrane fusing activity of a viral glycoprotein .
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-
- HY-P10517
-
SFT
|
HIV
|
Infection
|
Sifuvirtide (SFT) is a potent HIV fusion inhibitor. Sifuvirtide inhibits HIV-1 mediated cell fusion in a dose-dependent manner and is highly potent against infection by primary and laboratory-adapted HIV-1 isolates of multiple genotypes. Sifuvirtide can be used in the research of anti-HIV drugs .
|
-
- HY-P4110
-
|
iGluR
|
Metabolic Disease
Inflammation/Immunology
|
TAT-NSF222 Fusion Peptide is a fusion polypeptide with two domains, a TAT domain, which enters cells through macropinocytosis, and an NSF domain that inhibits N-ethylmaleimide-sensitive factor (NSF). TAT-NSF222 Fusion Peptide is an exocytosis inhibitor .
|
-
- HY-P5497
-
|
HIV
|
Others
|
C34 peptide is a biological active peptide. (This C34 peptide, also known as HR2, belongs to the helical region of gp41 of HIV, C-terminal heptad repeat 2 (HR2) defined as C helix or C peptide. It is known that HIV-1 enters cells by membrane fusion, C34 gp41 peptide is a potent inhibitors of HIV-1 fusion.)
|
-
- HY-W048674
-
Fmoc-O-acetyl-L-serine
|
Amino Acid Derivatives
|
Infection
|
Fmoc-Ser(Ac)-OH (Fmoc-O-acetyl-L-serine) is a Serine derivative. Fmoc-Ser(Ac)-OH can be used for the preparation of broad-spectrum coronavirus membrane fusion inhibitor .
|
-
- HY-P10308
-
|
HIV
|
Infection
|
[(Cys(Bzl)84,Glu(OBzl)85)]CD4 (81-92) is a selective inhibitor of HIV-1. [(Cys(Bzl)84,Glu(OBzl)85)]CD4 (81-92) inhibits viral infection and cell fusion by blocking the interaction between HIV-1 and CD4 molecules. [(Cys(Bzl)84,Glu(OBzl)85)]CD4 (81-92) can completely inhibit fusion formation at a concentration of 25 μM .
|
-
- HY-P10437
-
human α1-AT(353-372)
|
HIV
|
Infection
|
VIRIP (human α1-AT(353-372)) is a HIV-1 inhibitor. VIRIP blocks the entry of HIV-1 by interacting with gp41 fusion peptide. VIRIP can be used for virus research .
|
-
- HY-P1753
-
|
HIV
|
Infection
|
VIR-165 is a modified form of virus inhibitory peptide (VIRIP) that binds the fusion peptide of the gp41 subunit and prevents its insertion into the target membrane. VIRIP inhibits a wide variety of human immunodeficiency virus type 1 (HIV-1) strains .
|
-
- HY-P35433
-
T-1249
|
HIV
|
Inflammation/Immunology
|
Tifuvirtide (T-1249) is a peptide human immunodeficiency virus type-1 (HIV-1) fusion inhibitor. Tifuvirtide is a synthetically designed hybrid retroviral envelope polypeptide. Tifuvirtide has antiretroviral activity. Tifuvirtide can be used for the research of HIV infection .
|
-
- HY-106428
-
ITF1697
|
P-selectin
|
Cardiovascular Disease
Inflammation/Immunology
|
Icrocaptide (ITF1697) is a stable Lys-Pro-containing peptide that inhibits the intracellular Ca 2+-dependent fusion of Weibel-Palade bodies with the plasma membrane. Icrocaptide exerts its activity at the early stages of endothelial activation and inhibits P-selectin and von Willebrand factor secretion. Icrocaptide can be used for the study of a variety of microvascular disorders .
|
-
- HY-P5395
-
|
HIV
|
Others
|
TAT-GluR23A Fusion Peptide is a biological active peptide. (This is the GluR23A sequence, a control inactive peptide used as a mutant counterpart to glutamate receptor endocytosis inhibitor (GluR23Y), connected to an 11 amino acid cell permeable HIV Trans-Activator of Transcription (TAT) protein transduction domain (PTD). GluR23A is derived from GluR23Y amino acids 869 to 877, with Ala substituted for Tyr, and thus lacking essential phosphorylation sites.Control peptide of HY-P2259)
|
-
- HY-P3492
-
|
SARS-CoV
|
Infection
|
SARS-CoV-2-IN-34 (S-20-1) is a blood brain barrier penetrable pan-coronavirus (CoV) fusion inhibitor with broad-spectrum inhibitory activity. SARS-CoV-2-IN-34 effectively inhibits infection by pseudotyped and authentic SARS-CoV-2, and pseudotyped variants of concern (VOCs). SARS-CoV-2-IN-34 shows high affinity to RBD in S1 and HR1 domain in S2 of SARS-CoV-2 S protein. SARS-CoV-2-IN-34 can be used for the research of infection .
|
-
- HY-P2200
-
BMY-29304
|
HIV
Antibiotic
|
Infection
Inflammation/Immunology
|
Siamycin I (BMY-29304), a 21-residue tricyclic peptide, is a secondary metabolite in actinomycetes. Siamycin I is a HIV fusion inhibitor with ED50s of 0.05 to 5.7 μM for acute HIV type 1 (HIV-1) and HIV-2 infections. Siamycin I inhibits the gelatinase and gelatinase biosynthesis-activating pheromone (GBAP) signaling via the FsrC-FsrA two-component regulatory system in a noncompetitive manner. Siamycin I suppresses the expression of both fsrBDC and gelE-sprE transcripts. Siamycin I, a lasso peptide, interacts with lipid II and inhibits cell wall biosynthesis. Siamycin I, an antibiotic, has the potential for enterococcal infections research .
|
Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P99777
-
TTI-621
|
CD47
|
Cancer
|
Ontorpacept (TTI-621) is a soluble fusion protein that consists of the human SIRPα N-terminal (1-118) linked to the Fc region of human IgG1. The N-terminal (1-118)-fragment of ontorpacept is a binding domain for CD47 which is an inhibitor of phagocytosis by macrophages. Ontorpacept is a CD47-blocking checkpoint inhibitor with antitumor activity .
|
-
- HY-P99568
-
RC18
|
Inhibitory Antibodies
|
Inflammation/Immunology
|
Telitacicept (RC18) is a fully human TACI-Fc fusion protein. Telitacicept is a dual B lymphocyte stimulator (BLyS)/APRIL (a proliferation-inducing ligand) inhibitor that effectively blocks proliferation of B lymphocytes. Telitacicept can be used in research of B-cell autoimmune disease .
|
-
- HY-108847
-
|
TNF Receptor
Bacterial
|
Inflammation/Immunology
Cancer
|
Etanercept, a dimeric fusion protein that binds TNF, acts as a TNF inhibitor. Etanercept competitively inhibits the binding of both TNF-α and TNF-β to cell surface TNF receptors, rendering TNF biologically inactive. Etanercept shows efficacy against rheumatoid arthritis, juvenile idiopathic arthritis, and plaque psoriasis .
|
-
- HY-108822
-
Arcalyst; IL 1 Trap; Interleukin 1 Trap
|
Interleukin Related
|
Inflammation/Immunology
|
Rilonacept (Arcalyst), a dimeric fusion protein, is a interleukin 1 inhibitor. Rilonacept consists of the ligand-binding domains of the extracellular portions of the IL-1R components linked to the Fc portion of human IgG1. Rilonacept can be used for the research of cryopyrin-associated periodic syndromes .
|
-
- HY-P99446
-
TACI-Ig; TACI-Fc 5
|
Inhibitory Antibodies
|
Inflammation/Immunology
|
Atacicept (TACI-Ig) is a is a recombinant fusion protein containing the extracellular, ligand-binding portion of the TACI receptor and the Fc portion of human IgG. Atacicept inhibits B cell stimulation by binding to B lymphocyte stimulator and a proliferation-inducing ligand. Atacicept can be used in research of B-cell autoimmune disease .
|
-
- HY-P99720
-
ACE-536; luspatercept–aamt
|
TGF-beta/Smad
|
Metabolic Disease
Cancer
|
Luspatercept (ACE-536) is a recombinant modified ActRIIB fusion protein that binds with transforming growth factor β superfamily ligands. Luspatercept increases the erythrocyte numbers and promotes maturation of erythroid precursors. Luspatercept binds with GDF11 and inhibits Smad2/3 signaling. Luspatercept can be used for the research of anemia .
|
-
- HY-P99268
-
SAR 256212; MM 121; Anti-Human ERBB3/ErbB 3 Recombinant Antibody
|
EGFR
Apoptosis
|
Cancer
|
Seribantumab (MM 121) is a fully human IgG2 monoclonal antibody that targets HER3. Seribantumab blocks the activation of epidermal growth factor receptor (ErbB) family members and its downstream signal. Seribantumab inhibits neuregulin 1 (NRG1) fusion-dependent tumorigenesis in vitro and in vivo in breast, lung and ovarian patient-derived cancer models .
|
-
- HY-P99463
-
AVB-S6-500
|
TAM Receptor
|
Cancer
|
Batiraxcept (AVB-S6-500) is a highly potent and specific AXL inhibitor, a recombinant fusion protein dimer containing the extracellular domain of human AXLM and human immunoglobulin G1 heavy chain (Fc). Batiraxcept binds to GAS6 and inhibits the interaction of GAS6 with AXL, thereby substantially reducing AXL signaled invasion and migration of highly metastatic cells in vitro and inhibiting metastatic disease in nonclinical models of aggressive human cancers. Batiraxcept is available for studies in advanced or metastatic clear cell renal cell carcinoma (ccRCC) and platinum sensitive recurrent ovarian cancer .
|
-
- HY-P990088
-
|
VEGFR
PD-1/PD-L1
|
Cardiovascular Disease
|
Sotiburafusp alfa is a bispecific fusion protein, which is a humanized VEGFR-1 extracellular domain fragment (129-228, 1-100 in the current sequence) fused via the peptide linker 101GGSGGSGGSGGSGGS 115 to the N-terminus of the heavy chain (116-564) of a humanized IgG1-kappa anti-human PD-L1 heavy chain variant L352>A, L353>A. Sotiburafusp alfa is also an angiogenesis inhibitor .
|
Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
Cat. No. |
Product Name |
Chemical Structure |
-
- HY-14904AS
-
|
Umifenovir-d6 (hydrochloride) is the deuterium labeled Umifenovir hydrochloride. Umifenovir hydrochloride is a potent, orally active broad-spectrum antiviral with activity against a number of enveloped and non-enveloped viruses. Umifenovir hydrochloride is used as an anti-influenza virus agent. Umifenovir hydrochloride could effectively inhibit the fusion of virus with host cells[1][2]. Umifenovir hydrochloride is an efficient inhibitor of SARS-CoV-2 in vitro. Anti-inflammatory activity[3].
|
-
Cat. No. |
Product Name |
|
Classification |
-
- HY-148202
-
|
|
Alkynes
|
Influenza antiviral conjugate-1 (INT-2) is a HIV inhibitor, shows potent cell fusion inhibition . Influenza antiviral conjugate-1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-159147
-
|
|
Azide
|
SIAIS039 is an orally active c-ros oncogene 1 (ROS1)-specific PROTAC with DC50s of 154.46 nM, 126.47 nM, 143.69 nM for HCC78 cells, Ba/F3 expressing the CD74-ROS1 fusion and Ba/F3 expressing the SDC4-ROS1 fusion, respectively. SIAIS039 suppresses cell proliferation, induces cell cycle arrest and apoptosis, and inhibits clonogenicity against ROS1-positive cells. SIAIS039 demonstrates anti-tumour effects against ROS1-driven tumor growth vivo. SIAIS039 is composed of the ALK inhibitor Brigatinib (HY-12857), a linker EM-12 (HY-138793), and a VHL ligand E3 ubiquitin ligase 1-Butyne (Red: Brigatinib; Blue: VHL ligand; Black: linker) .
|
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