Search Result
Results for "
293T/ACE2-TMPRSS
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-120210
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ROR
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Inflammation/Immunology
Cancer
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XY018 is a potent ROR-γ-selective antagonist. XY018 inhibits ROR-γ constitutive activity in 293T cells with high potency (EC50, 190 nM). XY018 binds to the ROR-γ hydrophobic ligand binding domain (LBD) .
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- HY-138102
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SARS-CoV
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Infection
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SSAA09E3 is a SARS-CoV entry inhibitor that inhibits SARS/HIV pseudotyped virus entry with an EC50 of 9.7 μM in 293T cells and inhibits SARS-CoV infection of Vero cells with an EC50 of 0.15 μM [2].
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- HY-145879
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Keap1-Nrf2
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Cancer
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Nrf2 activator-2 (compound O15), a Osthole derivative, is a potent Nrf2 agonist with an EC50 of 2.9 μM in 293 T cells. Nrf2 activator-2 effectively inhibits the interaction between Keap1 and Nrf2, thus showing the activation effect on Nrf2. Nrf2 activator-2 shows a marked decrease in the level of ubiquitinated Nrf2 in cells .
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- HY-101775A
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Topoisomerase
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Cardiovascular Disease
Cancer
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9-Hydroxyellipticine hydrochloride is a inhibitor of Topo II and RyR. 9-Hydroxyellipticine hydrochloride exhibits antitumor, antioxidant and catecholamine-releasing activities. 9-Hydroxyellipticine hydrochloride exhibits IC50 values of 1.6 μM and 1.2μM in Hela S-3 and 293T cells, respectively [2] .
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- HY-N0041
-
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Gypenoside IV
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NF-κB
COX
NO Synthase
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Inflammation/Immunology
Cancer
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Ginsenoside Rb3 is extracted from steamed Panax ginseng C. A. Meyer. Ginsenoside Rb3 exhibits inhibitory effect on TNFα-induced NF-κB transcriptional activity with an IC50 of 8.2 μM in 293T cell lines. Ginsenoside Rb3 also inhibits the induction of COX-2 and iNOS mRNA.
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- HY-29866
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Microtubule/Tubulin
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Cancer
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Tubulin polymerization-IN-75 (Compound 6) is an inhibitor for tubulin polymerization with an IC50 of 30 μM. Tubulin polymerization-IN-75 inhibits the proliferation of cancer cell Huh7 and 293T with IC50 of 14.3 μM and 13.8 μM .
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- HY-139111
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Cathepsin
SARS-CoV
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Infection
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Oxocarbazate is an inhibitor of human cathepsin L with the IC50 values of 6.9 nM (human Cathepsin L,0 h) 0.4 nM ((human Cathepsin L,4 h) and 5.07 μM (human cathepsin B), respectively. Oxocarbazate blockes both SARS-CoV (IC50 = 273 nM) and Ebola virus (IC50 = 193 nM) entry into 293T cells .
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- HY-163822
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Histone Acetyltransferase
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Others
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WIZ degrader 5 (compound 41) is a WIZ degrader and induces the degradation of WIZ with maximum degradation of 88.6% in 293T cells. WIZ degrader 5 can be used for study of sickle cell disease
.
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- HY-159493
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Polo-like Kinase (PLK)
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Cancer
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BI2536-PEG2-Halo is a bifunctional molecule containing a ligand for Halo tag and a Polo-like kinase 1 (PLK1) inhibitor BI-2536 (HY-50698). BI2536-PEG2-Halo inhibits the proliferation of 293T cells with Halo-p53R273H(FL)-mCherry tag (IC50=23 nM), exhibits selective toxicity against p53 mutant cancer cells .
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- HY-158342
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PROTACs
YAP
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Cancer
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PROTAC TEAD degrader-1 (Compound 27) is a PROTAC degrader for transcriptional enhanced associate domain (TEAD). PROTAC TEAD degrader-1 selectively degrades the Flag TEAD2 in a ubiquitin proteasome-dependent manner, with a DC50 of 54.1 nM in 293T cells, inhibits proliferation of NF2-deficient NCI-H226 with an IC50 of 0.21 μM, and regulates expressions of yes associated protein (YAP) target genes. (Pink: TEAD ligand (HY-158400); Black: linker (HY-W008474); Blue: E3 ligase ligand (HY-W087383))
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- HY-158058
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Toll-like Receptor (TLR)
Pyroptosis
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Inflammation/Immunology
Cancer
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WYJ-2 is a selective agonist for toll-like receptor 2/1 (TLR2/1) with EC50 of 18.57 nM in human TLR2 and TLR1 transient-cotransfected HEK 293T cells. WYJ-2 induces pyroptosis and exhibits anticancer activity against non-small cell lung cancer (NSCLC) .
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- HY-101775
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Topoisomerase
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Cardiovascular Disease
Cancer
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9-hydroxyellipticine is an inhibitor of Topo II and RyR, exhibiting high affinity for DNA with a Pka value of 9.8 at pH 7.4. It has antitumor, antioxidant, and catecholamine-releasing activities, with IC50 values of 1.6 μM and 1.2 μM for Hela S-3 and 293T cells, respectively. It also demonstrates anticancer effects in L1210 leukemia mice .
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- HY-N0041R
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Gypenoside IV (Standard)
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NF-κB
COX
NO Synthase
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Inflammation/Immunology
Cancer
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Ginsenoside Rb3 (Standard) is the analytical standard of Ginsenoside Rb3. This product is intended for research and analytical applications. Ginsenoside Rb3 is extracted from steamed Panax ginseng C. A. Meyer. Ginsenoside Rb3 exhibits inhibitory effect on TNFα-induced NF-κB transcriptional activity with an IC50 of 8.2 μM in 293T cell lines. Ginsenoside Rb3 also inhibits the induction of COX-2 and iNOS mRNA.
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- HY-164144
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Histone Methyltransferase
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Cancer
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EPZ033294 is an inhibitor of SYMD2 (IC50 is 3.9 nM). SYMD2 itself has catalytic activity and can methylate the lysine residue of BTF3 to BTF3me1, which was experimentally demonstrated by detecting an IC50 of 2.9 nM for inhibition of BTF3ME1 by SYMD2, indicating an active inhibition of SYMD2 by EPZ033294. EPZ033294 (0-50 µM) has an inhibitory effect on SYMD2 and a concentration-dependent inhibitory effect in 293T .
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- HY-149359
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Isocitrate Dehydrogenase (IDH)
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Cancer
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IHMT-IDH1-053 (compound 16) is a highly selectivity and irreversible IDH1-mutant inhibitor with an IC50 of 4.7 nM for IDH1 R132H. IHMT-IDH1-053 displays high selectivity against IDH1 mutants over IDH1 wt and IDH2 wt/mutants. IHMT-IDH1-053 inhibits 2-hydroxyglutarate (2-HG) production in IDH1 R132H mutant transfected 293T cells (IC50=28 nM). IHMT-IDH1-053 binds to the IDH1 R132H protein in the allosteric pocket adjacent to the NAPDH binding pocket through a covalent bond with residue Cys269. IHMT-IDH1-053 inhibits the proliferation of HT1080 cell line and primary AML cells which both bear IDH1 R132 mutants .
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- HY-162464
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PROTACs
SARS-CoV
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Infection
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MPD2 is a Cereblon-binding ligand-based PROTAC that degrades MPro, the main protease of SARS-CoV-2. MPD2 effectively reduced MPro protein levels in 293T cells in a time-dependent manner (DC50=296 nM). MPD2 exhibited potent antiviral activity against multiple SARS-CoV-2 strains and had enhanced potency against Nirmatrelvir (HY-138687) resistant strains. MPD2 provides a new direction for antiviral drug development against SARS-CoV-2 and other emerging coronavirus pathogens (Sturcture Note:(Blue: Cereblon ligand (HY-14658), Black: linker (HY-W275882)；Red: SARS-CoV-2 MPro Inhibitor MP18 (HY-158763)) .
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- HY-158073
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SARS-CoV
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Infection
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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
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- HY-157154
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SARS-CoV
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Infection
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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 .
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- HY-170524
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SARS-CoV
DNA Methyltransferase
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Infection
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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 .
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- HY-118368
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- HY-W585876
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FXR
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Metabolic Disease
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Chenodeoxycholic acid 3-glucuronide is a metabolite of Chenodeoxycholic acid that can activate the key nuclear receptor (FXR), with an EC50 of 8 μM, and in HEK293T cells, the EC50 for activating FXR is 11 μM .
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- HY-108317
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Others
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Cancer
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ABL127 is a selective and covalent inhibitor of protein methylesterase 1 (PME-1) with IC50s of 6.4 nM and 4.2 nM in HEK293T and MDA-MB-231 cells, respectively.
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- HY-153132
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mGluR
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Metabolic Disease
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mGluR3 modulator-1 (compound 3) is a mGluR3 modulator, with an EC50 of 1-10 μM in HEK293T-mGluR-Gqi5 Calcium Mobilization Assay .
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- HY-116895
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Androgen Receptor
MAGL
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Metabolic Disease
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JJH260 is AIG1inhibitor, and inhibit the fluorophosphonate reactivity and fatty acid esters of hydroxy fatty acid (FAHFA) hydrolysis activity of AIG1in HEK293T cells, with IC50 values of 0.50 μM and 0.57 μM, respectively .
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- HY-129808
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LPL Receptor
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Cardiovascular Disease
Cancer
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VPC12249 is a competitive dual LPA1/LPA3 antagonist with Ki values of 137nM and 428 nM, respectively. VPC12249 inhibits calcium mobilization in HEK293T cells with a Ki value of ~130 nM. VPC12249 is promising for research of ovarian cancer and hypertensive diseases .
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- HY-122716
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PPAR
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Others
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PTGR2-IN-1 is a potent PTGR2 inhibitor with an IC50 of ~0.7 μM. PTGR2-IN-1 increases 15-keto-PGE2-dependent PPARγ transcriptional activity in PTGR2-transfected HEK293T cells .
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- HY-15888
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BMI1
Autophagy
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Cancer
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PTC-209 is a specific BMI-1 inhibitor with an IC50 of 0.5 μM in HEK293T cell line. PTC-209 irreversibly impairs colorectal cancer-initiating cells (CICs). PTC-209 shows potent anti-myeloma activity and impairs the tumor microenvironment [2].
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- HY-15888A
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BMI1
Autophagy
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Cancer
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PTC-209 hydrobromide is a specific BMI-1 inhibitor with an IC50 of 0.5 μM in HEK293T cell line. PTC-209 hydrobromide irreversibly impairs colorectal cancer-initiating cells (CICs). PTC-209 hydrobromide shows potent anti-myeloma activity and impairs the tumor microenvironment [2].
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- HY-150089
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CFTR
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Inflammation/Immunology
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SRI-37240 is a potent premature termination codons (PTCs) inhibitor. SRI-37240 suppresses CFTR nonsense mutations. SRI-37240 alters cellular translation termination at PTCs in HEK293T cells. SRI-37240 can also restore CFTR function in primary bronchial epithelial cells when combination with G418 .
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- HY-161740
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AUTOTACs
Estrogen Receptor/ERR
Autophagy
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Cancer
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PHTPP-1304 is a PHTPP-based autophagy targeting chimera (AUTOTAC) that induces p62 self-oligomerization and degradation of estrogen receptor ERβ (DC50:~2 nM, HEK293T). PHTPP-1304 also induces the formation of p62 +ERβ + puncta that are affected by autophagic flux in a dose-dependent manner .
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- HY-151465
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HIF/HIF Prolyl-Hydroxylase
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Cancer
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HIF-1α-IN-4 is a HIF-1α inhibitor with an IC50 value of 24 nM (in HEK293T cell). HIF-1α-IN-4 downregulates VEGF and PDK1 mRNA expressions under hypoxia. HIF-1α-IN-4 can be used in the research of cancer .
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- HY-138997
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PPAR
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Metabolic Disease
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MBX-102 acid is a selective partial PPAR-γ agonist. MBX-102 acid binds highly to plasma proteins, mainly serum albumin. MBX-102 acid can be used to study type 2 diabetes .
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- HY-P1432A
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GHSR
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Cancer
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K-(D-1-Nal)-FwLL-NH2 TFA is a high affinity and potent ghrelin receptor inverse agonist (Ki values are 4.9 and 31 nM in COS7 and HEK293T cells, respectively). K-(D-1-Nal)-FwLL-NH2 blocks ghrelin receptor-mediated Gq- and G13-dependent signaling pathways.
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- HY-P5157
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Potassium Channel
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Neurological Disease
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BmP02 is a selective Kv1.3 channel blocker and a highly-selective Kv4.2 modulator, which can be isolated from Chinese scorpion (Buthus martensi Karsch) venom. BmP02 also delays the inactivation of Kv4.2 in HEK293T cells, with an EC50 value of ~850 nM. BmP02 inhibits the transient outward potassium currents (Ito) in ventricular muscle cells [2].
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- HY-151466
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HIF/HIF Prolyl-Hydroxylase
Monoamine Oxidase
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Cancer
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HIF-1α-IN-5 is a HIF-1α inhibitor with an IC50 value of 24 nM (in HEK293T cell). HIF-1α-IN-5 also inhibits MAO-A activity. HIF-1α-IN-5 downregulates VEGF and PDK1 mRNA expressions under hypoxia. HIF-1α-IN-5 can be used in the research of cancer .
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- HY-168384
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STING
TNF Receptor
Interleukin Related
CD28
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Inflammation/Immunology
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M04 is an agonist of STING. It induces the expression of the IFN reporter gene in HEK293T cells expressing wild-type human STING, but does not induce this expression in HEK293T cells expressing the R71H-G230A-R293Q (HAQ) STING variant or in mouse RAW 264.7 cells, indicating that its activity is dependent on allelic and species variations. M04 induces the production of TNF-α, IL-10, IL-1β, and IL-12p70 in human peripheral blood mononuclear cells (PBMCs). At a concentration of 50 µM, M04 stimulates dendritic cells isolated from PBMCs to express the MHC class II cell surface receptor HLA-DR and co-stimulatory molecules CD40, CD80, and CD86, and also enhances their ability to activate T cells in an ex vivo assay. M04 can be used in research on inflammatory immune diseases .
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- HY-126037
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ROR
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Inflammation/Immunology
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(±)-ML 209 (compound 4n), a diphenylpropanamide, is a retinoic acid-related orphan receptor RORγ antagonist with an IC50 of 1.1 μM. (±)-ML 209 inhibits RORγt transcriptional activity with an IC50 of 300 nM in HEK293t cells. (±)-ML 209 inhibits the transcriptional activity of RORγt, but not RORα in cells. (±)-ML 209 selectively inhibits murine Th17 cell differentiation without affecting the differentiation of naïve CD4 + T cells into other lineages, including Th1 and regulatory T cells .
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- HY-126489
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Parasite
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Infection
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Tetromycin B is a cysteine protease inhibitor with Ki values of 0.62, 1.42, 32.5, and 1.59 μM for rhodesain, falcipain-2, cathepsin L, and cathepsin B, respectively. It inhibits the growth of T. brucei in vitro (IC50=30.87 μM). Tetromycin B is also cytotoxic to HEK293T kidney cells and J774.1 macrophages (IC50s=71.77 and 20.2 μM, respectively).
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- HY-W141374
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DNA/RNA Synthesis
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Neurological Disease
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CB096 binds the 5′CGG/3′GGC internal loop structure of r(G4C2)exp RNA, interrupts its gain-of-function mechanism, and thus results in the regulation of nucleolar focusing, RNA splicing defects, RNA metabolism, nucleocytoplasmic transport dysfunction, and toxic dipeptide repeats (DPRs) generated by RNA translation. CB096 inhibits the RAN translation with an IC50 of 20 μM in HEK293T cells .
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- HY-132866
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P-glycoprotein
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Cancer
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YS-370 (compound 44) is a potent, high selective, and orally active inhibitor of P-glycoprotein (P-gp). YS-370 stimulates the P-gp ATPase activity and has moderate inhibition against CYP3A4. YS-370 effectively reverses multidrug resistance (MDR) to paclitaxel and colchicine in SW620/AD300 and HEK293T-ABCB1 cells. YS-370 in combination with paclitaxel achieves much stronger antitumor activity .
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- HY-155938
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Acyltransferase
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Neurological Disease
Inflammation/Immunology
Cancer
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Cyano-myracrylamide is an inhibitor of zinc finger DHHC domain-containing palmitoyltransferase 20 (zDHHC20) with an IC50 value of 1.35 µM. Cyano-myracrylamide also inhibits the S-Acylation of EGFR and CD36. Cyano-myracrylamide also inhibits S-acylation of Legionella E3 ligase GobX, MyD88, and Ras, which are substrates of zDHHC20, zDHHC9, and zDHHC6, respectively, in HEK293T cells expressing recombinant Legionella GobX, recombinant human MyD88, or endogenous Ras .
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- HY-158432
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Histone Demethylase
PROTACs
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Cancer
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GT-653 is a PROTAC degrader for lysine-specific demethylase 5B (KDM5B). GT-653 degrades 68.35% KDM5B at 10 μM in a ubiquitin proteasome-dependent manner, upregulates H3K4me3 levels, and activates the type-I interferon signaling pathway in prostate cancer cells 22RV1. (Pink: KDM5B ligand (HY-158433); Black: Linker (HY-W004896); Blue: E3 ligase ligand (HY-103596))
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- HY-158433
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- HY-158400
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- HY-158343
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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Thalidomide-NH-PEG2-C2-CH2 is a conjugate of E3 ligase ligand and linker. Thalidomide-NH-PEG2-C2-CH2 is utilized for synthesis of PROTAC TEAD degrader-1 (HY-158342) .
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- HY-162885
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Proteasome
JAK
STAT
Interleukin Related
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Cancer
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YSY01A is a proteasome inhibitor that can suppress cancer cell survival by inducing apoptosis (Apoptosis). Its IC50 values are 51.0 nM for HEK293T, 9.2 nM for A549, 5.2 nM for MCF-7, 8.9 nM for MGC-803, and 35.4 nM for PC-3M cells. Additionally, YSY01A eliminates constitutive STAT3 signaling by downregulating gp130 and JAK2 in human A549 lung cancer cells. YSY01A holds promise for research in the field of cancer therapy .
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- HY-160496
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STAT
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Cancer
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STAT3-IN-25 (compound 2p) is a potent STAT3 inhibitor with a p-trifluoroethoxy benzyl substituent. STAT3-IN-25 shows STAT3 luciferase inhibition activity using HEK293T cells with an IC50 of 22.3 nM and ATP production inhibition activity using BxPC-3 cells with an IC50 of 32.5 nM. STAT3-IN-25 shows potent antiproliferation activities on BxPC-3 and Capan-2 cells. STAT3-IN-25 has the potential for pancreatic cancer research .
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- HY-162492
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Influenza Virus
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Infection
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Influenza A virus-IN-14 (Compound 37) is an inhibitor for influenza virus type A (IAV), which inhibits H1N1 with an EC50 of 23 nM. Influenza A virus-IN-14 exhibits low cytotoxicity with CC50 of more than 100 μM. Influenza A virus-IN-14 inhibits cytopathic effect and improves the survival rates of cell Calu3. Influenza A virus-IN-14 exhibits synergistic activity with the neuraminidase inhibitor Oseltamivir (HY-13317). Influenza A virus-IN-14 exhibits poor pharmacokinetic properties in CD-1 mouse .
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- HY-169166
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HIV Protease
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Infection
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HIV-1 protease-IN-14 (compound 5ae) is a potent HIV-1 protease inhibitor with Ki values of 0.28, 56.9 nM for WT HIV-1 PR, R41T HIV-1 PR, respectively. HIV-1 protease-IN-14 shows low cytotoxicity .
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- HY-156401
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PROTACs
Epigenetic Reader Domain
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Cancer
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BRD9 Degrader-1 (Compound 13-7) is a PROTAC BRD9 degrader . BRD9 Degrader-1 has a micromolar binding affinity for BRD9 and a nanomolar affinity for the BRD9-VCB ternary complex. BRD9 Degrader-1 induces BRD9 proteasome degradation in HEK293T cells, which can be reversed by MLN4924 (HY-70062)。(Blue: VH032-cyclopropane-F (HY-125905); Black: linker (HY-W763939); Pink: HY-168695) .
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- HY-162714
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P-glycoprotein
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Cancer
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C3N-Dbn-Trp2 is an inhibitor for ATP-binding cassette transporter ABCB1. C3N-Dbn-Trp2 inhibits the ABCB1-mediated Rhodamine 123 (HY-D0816) efflux in cells HEK293T and HCT-15 with IC50 of 5.9 µM and 2.2 µM. C3N-Dbn-Trp2 inhibits the Doxorubicin (HY-15142A) efflux, enhances the cytotoxicity of Doxorubicin in ABCB1-expressing cells .
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- HY-128426
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Dihydromuconic acid; trans-β-Hydromuconic acid
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Endogenous Metabolite
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Metabolic Disease
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Trans-2-butene-1,4-dicarboxylic acid (Dihydromuconic acid; trans-β-Hydromuconic acid) is an endogenous metabolite [2].
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- HY-19744
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MyD88
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Inflammation/Immunology
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T6167923 is a selective inhibitor of MyD88-dependent signaling pathways. T6167923 directly binds to Toll/IL1 receptor (TIR) domain of MyD88 and disrupts MyD88 homodimeric formation. T6167923 inhibits NF-κB driven Staphylococcus enterotoxin AP (SEAP) activity, and improves anti-inflammatory activity with IC50s of 2.7 μM, 2.9 μM, 2.66 μM and 2.66 μM for IFN-γ, IL-1β, IL-6 and TNF-α, respectively [2].
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- HY-15592
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GSK-1265744; S/GSK1265744
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OAT
HIV
HIV Integrase
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Infection
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Cabotegravir (GSK-1265744) is a orally active and long-acting HIV integrase strand transfer inhibitor and organic anion transporter 1/3 (OAT1/OAT3) inhibitor with IC50 values of 2.5 nM, 0.41 μM and 0.81 μM for HIVADA, OAT3 and OAT1, respectively. Cabotegravir is primarily metabolized by uridine diphosphate glucuronosyltransferase (UGT) 1A1, with low potential to interact with other antiretroviral agents (ARVs). Cabotegravir can be used to research AIDS [2].
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- HY-107404
-
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Orphan Receptor
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Endocrinology
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SID 7969543 is a selective SF-1 (steroidogenic factor 1, NR5A1) inhibitor with an IC50 of 760 nM. SID 7969543 inhibits SF-1-triggered luciferase expression with IC50 of 30 nM. SF-1 is a transcription factor belonging to the nuclear receptor superfamily [2].
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- HY-137458
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ARQ 751
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Akt
Ser/Thr Protease
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Cancer
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Vevorisertib (ARQ 751) is an orally active, potent and selective pan-AKT serine/threonine kinase inhibitor against AKT1 (IC50=0.55 nM), AKT2 (IC50=0.81 nM), and AKT3 (IC50=1.31 nM). Vevorisertib, as a single agent or in combination with other anti-cancer agents, can be used for the research of solid tumors with PIK3CA / AKT / PTEN mutations [2] .
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- HY-147219
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PROTACs
Anaplastic lymphoma kinase (ALK)
EGFR
Apoptosis
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Cancer
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SIAIS164018 is a PROTAC-based ALK and EGFR degrader, with IC50 value of 2.5 nM and 6.6 nM for ALK and ALK G1202R, respectively. SIAIS164018 strongly inhibits cancer cells migration and invasion, causes G1 cell cycle arrest and induces apoptosis. SIAIS164018 exhibits better property than Brigatinib (HY-12857) .
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- HY-147219A
-
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PROTACs
Anaplastic lymphoma kinase (ALK)
EGFR
Apoptosis
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Cancer
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SIAIS164018 hydrochloride is a PROTAC-based ALK and EGFR degrader, with IC50 value of 2.5 nM and 6.6 nM for ALK and ALK G1202R, respectively. SIAIS164018 hydrochloride strongly inhibits cancer cells migration and invasion, causes G1 cell cycle arrest and induces apoptosis. SIAIS164018 hydrochloride exhibits better property than Brigatinib (HY-12857) .
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- HY-15592R
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OAT
HIV
HIV Integrase
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Infection
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Cabotegravir (Standard) is the analytical standard of Cabotegravir. This product is intended for research and analytical applications. Cabotegravir (GSK-1265744) is a orally active and long-acting HIV integrase strand transfer inhibitor and organic anion transporter 1/3 (OAT1/OAT3) inhibitor with IC50 values of 2.5 nM, 0.41 μM and 0.81 μM for HIVADA, OAT3 and OAT1, respectively. Cabotegravir is primarily metabolized by uridine diphosphate glucuronosyltransferase (UGT) 1A1, with low potential to interact with other antiretroviral agents (ARVs). Cabotegravir can be used to research AIDS [2].
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- HY-164445
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STAT
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Cancer
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STAT3-IN-32 (compound 2p) is an orally active, potent STAT3 dual phosphorylation inhibitor with an indole-containing tetra-aromatic heterocycle scaffold. STAT3-IN-32 exhibits STAT3 luciferase inhibition activity using HEK293T cells with an IC50 of 5.3 nM and ATP production inhibition activity using BxPC-3 cells with an IC50 of 4.2 nM. STAT3-IN-32 significantly blocks p-Tyr705 and p-Ser727 and causes the abrogation of the corresponding nuclear transcription and mitochondrial oxidative phosphorylation functions of STAT3 by targeting the STAT3 SH2 domain (KD=21.3 nM). STAT3-IN-32 exhibits significant suppressive effects in a pancreatic cancer xenograft model .
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- HY-110315
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Apoptosis
MDM-2/p53
Epigenetic Reader Domain
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Cardiovascular Disease
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Ischemin sodium is a CBP bromodomain inhibitor that inhibits p53 interaction with CBP and transcriptional activity in cells. Ischemin sodium salt inhibits p53-induced p21 activation with an IC50 value of 5 µM. Ischemin sodium salt also prevents apoptosis in ischemic cardiomyocytes. Ischemin sodium salt can be used in the study of cardiovascular diseases (such as myocardial ischemia) .
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- HY-161342
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Cathepsin
SARS-CoV
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Infection
Inflammation/Immunology
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CTSL/CAPN1-IN-2 (Compound 14b) is an orally active inhibitor of both CTSL and CAPN1, with IC50 values of 6.88 nM and 347.6 nM, respectively. CTSL/CAPN1-IN-2 possesses anti-inflammatory properties and favorable pharmacokinetic characteristics. CTSL/CAPN1-IN-2 exhibits broad-spectrum antiviral activity against coronaviruses by blocking viral entry .
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- HY-168593
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β-catenin
PROTACs
Histone Demethylase
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Cancer
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Wnt/β-catenin-IN-5 (Compound 4) is an inhibitor of the Wnt/β-catenin signaling pathway. Wnt/β-catenin-IN-5 eliminates colorectal cancer stem cells and inhibits tumor growth by suppressing the Wnt signaling pathway. PROTACs Wnt/β-catenin-IN-5, which is also a PROTAC based on IOX1, effectively induces the degradation of KDM3A and KDM3B (Target protein ligand (Pink): HY-12304; linker (Black): HY-22335; Conjugate of E3 ligase ligand and linker: HY-112599; E3 ligase (Blue): HY-41547) .
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- HY-170688
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Bacterial
Reactive Oxygen Species
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Infection
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Antibacterial agent 119 (Compound 21 g) is an antibacterial candidate against Methicillin (HY-121544)-resistant Staphylococcus aureus (MICs less than 1 μg/mL against tested strains). Antibacterial agent 119 induces ROS production. Antibacterial agent 119 also acts on the bacterial cell membrane to cause membrane breakage. Antibacterial agent 119 exhibits potent antibacterial activity with low cytotoxicity, rapid bactericidal ability, and good in vivo antibacterial activity .
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- HY-170492
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Epoxide Hydrolase
Interleukin Related
TNF Receptor
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Inflammation/Immunology
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sEH inhibitor-19 (Compound (R)-14i) is an orally active inhibitor for soluble epoxide hydrolase (sEH) with an IC50 of 1.2 nM. sEH inhibitor-19 inhibits the expression of TNF-α and IL-6, exhibits anti-inflammatory activity in mouse acute pancreatitis or Carrageenan (HY-125474)-induced edema models .
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- HY-17605A
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GS-9883 sodium
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HIV Integrase
HIV
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Infection
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Bictegravir sodium is a potent inhibitor of HIV-1 integrase, with an IC50 of 7.5 nM. Bictegravir sodium exhibits potent and selective anti-HIV activity and low cytotoxicity .
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- HY-157136
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CRM1
COX
c-Myc
Survivin
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Cancer
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LFS-1107 is a reversible CRM1 inhibitor (Kd: 12.5 pM). LFS-1107 can selectively eliminate extranodal natural killer/T cell lymphoma (ENKTL) cells and can be used for cancer research .
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- HY-17605AR
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HIV Integrase
HIV
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Infection
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Bictegravir (sodium) (Standard) is the analytical standard of Bictegravir (sodium). This product is intended for research and analytical applications. Bictegravir sodium is a potent inhibitor of HIV-1 integrase, with an IC50 of 7.5 nM. Bictegravir sodium exhibits potent and selective anti-HIV activity and low cytotoxicity .
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- HY-114366
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CXCR
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Others
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BC-1485 is a small molecule inhibitor of Fibrosis-inducing E3 ligase 1 (FIEL1). BC-1485 protects PIAS4 from ubiquitin-mediated degradation. BC-1485 decreases α-SMA, BAL and CXCL1. BC-1485 ameliorates fibrotic lung injury in murine models [2].
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- HY-137458A
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ARQ 751 trihydrochloride
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Akt
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Cancer
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Vevorisertib (ARQ 751) trihydrochloride is a selective, allosteric, pan-AKT and AKT1-E17K mutant inhibitors. Vevorisertib trihydrochloride potently inhibit phosphorylation of AKT. Vevorisertib trihydrochloride has Kd values of 1.2 nM and 8.6 nM for AKT1 and AKT1-E17K, respectively. Vevorisertib trihydrochloride has IC50 values of 0.55, 0.81, and 1.3 nM for AKT1, AKT2, and AKT3, respectively. Vevorisertib trihydrochloride can be used for the research of cancer .
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- HY-163818
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Histone Methyltransferase
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Others
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WIZ degrader 2 (Compound 142) is a degrader for widely interspaced zinc finger motifs with an AC50 of 0.011 μM. WIZ degrader 2 induces the expression of fetal hemoglobin (HbF) with an EC50 of 0.038 μM. WIZ degrader 2 can be used in research about inherited blood disorders .
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- HY-149696
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NF-κB
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Cancer
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IR-Crizotinib is a NF-κB-inducing kinase (NIK) inhibitor that crosses the blood-brain barrier and fluorescently localizes intracranial glioblastoma (GBM) in mice (IC50=3.381 μM). IR-Crizotinib is conjugated from the near-infrared dye IR-786 and the NF-κB-inducing kinase (NIK) inhibitor Crizotinib. IR-Crizotinib can effectively inhibit the growth and invasion of glioma in vitro and in vivo and can be used in cancer research .
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- HY-N0565A
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MMP
Bacterial
Antibiotic
Parasite
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Infection
Cancer
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Doxycycline hydrochloride, an antibiotic, is an orally active and broad-spectrum metalloproteinase (MMP) inhibitor . Doxycycline hydrochloride shows antibacterial activity and anti-cancer cell proliferation activity [2] .
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- HY-N0565B
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Doxycycline hydrochloride hemiethanolate hemihydrate; WC2031
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Antibiotic
MMP
Bacterial
Parasite
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Infection
Cancer
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Doxycycline hyclate, an antibiotic, is an orally active and broad-spectrum metalloproteinase (MMP) inhibitor . Doxycycline hyclate shows antibacterial activity and anti-cancer cell proliferation activity [2] .
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- HY-N0565
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Doxycycline
Maximum Cited Publications
98 Publications Verification
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MMP
Bacterial
Antibiotic
Parasite
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Infection
Cancer
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Doxycycline, an antibiotic, is an orally active and broad-spectrum metalloproteinase (MMP) inhibitor . Doxycycline shows antibacterial activity and anti-cancer cell proliferation activity [2] .
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- HY-144318
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Epigenetic Reader Domain
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Cancer
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CREB-IN-1 TFA is a potent, orally active CREB inhibitor (IC50=0.18 µM). CREB-IN-1 TFA inhibits breast cancer cell growth .
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- HY-144316
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Cholinesterase (ChE)
GSK-3
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Neurological Disease
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ZLWH-23 is a selective AChE inhibitor (IC50=0.27 μM) with GSK-3β inhibitory property (IC50=6.78 μM). ZLWH-23 possesses selectivity for AChE over BChE (IC50=20.82 μM) and for GSK-3β over multi-kinases. ZLWH-23 has the potential for the research of Alzheimer's disease .
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- HY-N0565C
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MMP
Bacterial
Antibiotic
Parasite
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Infection
Cancer
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Doxycycline calcium, an antibiotic, is an orally active and broad-spectrum metalloproteinase (MMP) inhibitor . Doxycycline calcium shows antibacterial activity and anti-cancer cell proliferation activity [2] .
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- HY-N0565BR
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Antibiotic
MMP
Bacterial
Parasite
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Infection
Cancer
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Doxycycline hyclate (Standard) is the analytical standard of Doxycycline hyclate. This product is intended for research and analytical applications. Doxycycline hyclate, an antibiotic, is an orally active and broad-spectrum metalloproteinase (MMP) inhibitor . Doxycycline hyclate shows antibacterial activity and anti-cancer cell proliferation activity [2] .
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- HY-N0565AR
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MMP
Bacterial
Antibiotic
Parasite
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Infection
Cancer
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Doxycycline (hydrochloride) (Standard) is the analytical standard of Doxycycline (hydrochloride). This product is intended for research and analytical applications. Doxycycline hydrochloride, an antibiotic, is an orally active and broad-spectrum metalloproteinase (MMP) inhibitor . Doxycycline hydrochloride shows antibacterial activity and anti-cancer cell proliferation activity [2] [4] .
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- HY-N0565R
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MMP
Bacterial
Antibiotic
Parasite
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Infection
Cancer
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Doxycycline (Standard) is the analytical standard of Doxycycline. This product is intended for research and analytical applications. Doxycycline, an antibiotic, is an orally active and broad-spectrum metalloproteinase (MMP) inhibitor . Doxycycline shows antibacterial activity and anti-cancer cell proliferation activity [2] [4] .
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- HY-150221
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PARP
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Cancer
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DB008 is potent and selective PARP16 inhibitor with an IC50 value of 0.27 μM, containing an acrylamide electrophilic reagent. DB008 is membrane-permeable and marks PARP16 selectively . DB008 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-W009066
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EHDPP; Octicizer
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PPAR
Progesterone Receptor
Estrogen Receptor/ERR
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Endocrinology
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2-Ethylhexyl diphenyl phosphate is an organophosphate flame retardants (OPFRs) and a PPARG agonist (EC20: 2.04 µM). 2-Ethylhexyl diphenyl phosphate also inhibits ERRγ transcriptional activity (IC50: 1.3 µM). 2-Ethylhexyl diphenyl phosphate upregulates 3β-HSD1, human chorionic gonadotropin (hCG) and progesterone secretion. 2-Ethylhexyl diphenyl phosphate can be used in studies of female reproduction and fetal development [2].
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- HY-112764
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Liposome
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Metabolic Disease
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DMG-PEG 2000 is used?for the preparation of liposome for siRNA delivery with improved transfection efficiency in vitro. DMG-PEG 2000 is also used for the?lipid nanoparticle for an oral plasmid DNA delivery approach in vivo through a facile surface modification to improve the mucus permeability and delivery efficiency of the nanoparticles .
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- HY-150687
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ERK
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Metabolic Disease
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ZINC12409120 is a high selective ERK inhibitor. ZINC12409120 acts on disrupting FGF23:α-Klotho interaction to inhibit ERK activity with an IC50 of 5.0 μM .
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- HY-112764A
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Liposome
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Metabolic Disease
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DMG-PEG Excipient is used?for the preparation of liposome for siRNA delivery with improved transfection efficiency in vitro. DMG-PEG Excipient is also used for the?lipid nanoparticle for an oral plasmid DNA delivery approach in vivo through a facile surface modification to improve the mucus permeability and delivery efficiency of the nanoparticles .
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| Cat. No. |
Product Name |
Type |
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- HY-149696
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Dyes
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IR-Crizotinib is a NF-κB-inducing kinase (NIK) inhibitor that crosses the blood-brain barrier and fluorescently localizes intracranial glioblastoma (GBM) in mice (IC50=3.381 μM). IR-Crizotinib is conjugated from the near-infrared dye IR-786 and the NF-κB-inducing kinase (NIK) inhibitor Crizotinib. IR-Crizotinib can effectively inhibit the growth and invasion of glioma in vitro and in vivo and can be used in cancer research .
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| Cat. No. |
Product Name |
Type |
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- HY-112764
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Drug Delivery
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DMG-PEG 2000 is used?for the preparation of liposome for siRNA delivery with improved transfection efficiency in vitro. DMG-PEG 2000 is also used for the?lipid nanoparticle for an oral plasmid DNA delivery approach in vivo through a facile surface modification to improve the mucus permeability and delivery efficiency of the nanoparticles .
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Product Name |
Target |
Research Area |
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- HY-P1432A
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GHSR
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Cancer
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K-(D-1-Nal)-FwLL-NH2 TFA is a high affinity and potent ghrelin receptor inverse agonist (Ki values are 4.9 and 31 nM in COS7 and HEK293T cells, respectively). K-(D-1-Nal)-FwLL-NH2 blocks ghrelin receptor-mediated Gq- and G13-dependent signaling pathways.
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- HY-P5157
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Potassium Channel
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Neurological Disease
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BmP02 is a selective Kv1.3 channel blocker and a highly-selective Kv4.2 modulator, which can be isolated from Chinese scorpion (Buthus martensi Karsch) venom. BmP02 also delays the inactivation of Kv4.2 in HEK293T cells, with an EC50 value of ~850 nM. BmP02 inhibits the transient outward potassium currents (Ito) in ventricular muscle cells [2].
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- HY-K2014
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MCE PEI Transfection Reagent is designed based on 25 kDa PEI. It has high-efficiency, low-toxicity, strong-stability, and is suitable for many cell types, such as HEK-293、HEK-293T、CHO-K1、COS-1、COS-7、NIH/3T3、Sf9、HepG2 and HeLa et, even some hard-to-transfect cells. It can also be applied to large-scale recombinant protein expression and virus production.
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| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
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Classification |
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- HY-150221
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Alkynes
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DB008 is potent and selective PARP16 inhibitor with an IC50 value of 0.27 μM, containing an acrylamide electrophilic reagent. DB008 is membrane-permeable and marks PARP16 selectively . DB008 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-159493
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Azide
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BI2536-PEG2-Halo is a bifunctional molecule containing a ligand for Halo tag and a Polo-like kinase 1 (PLK1) inhibitor BI-2536 (HY-50698). BI2536-PEG2-Halo inhibits the proliferation of 293T cells with Halo-p53R273H(FL)-mCherry tag (IC50=23 nM), exhibits selective toxicity against p53 mutant cancer cells .
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| Cat. No. |
Product Name |
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Classification |
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- HY-112764
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Pegylated Lipids
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DMG-PEG 2000 is used?for the preparation of liposome for siRNA delivery with improved transfection efficiency in vitro. DMG-PEG 2000 is also used for the?lipid nanoparticle for an oral plasmid DNA delivery approach in vivo through a facile surface modification to improve the mucus permeability and delivery efficiency of the nanoparticles .
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- HY-160050
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Aptamers
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CD63-1 aptamer sodium is a high-affinity and specific DNA aptamer targeting the CD63 protein (Kd: 38.71 nM). CD63-1 aptamer sodium efficiently binds to CD63-positive cells, including breast cancer MDA-MB-231 cells and CD63-overexpressing HEK293T cells, with moderate binding affinity (Kd~100 nM) as assessed by flow cytometry .
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- HY-160051
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Aptamers
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CD63-2 aptamer sodium is a high-affinity and specific DNA aptamer targeting the CD63 protein (Kd: 78.43 nM). CD63-1 aptamer sodium efficiently binds to CD63-positive cells, including breast cancer MDA-MB-231 cells and CD63-overexpressing HEK293T cells, with moderate binding affinity (Kd~100 nM) as assessed by flow cytometry .
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- HY-112764A
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Emulsifiers
Liposomal Film-forming Agents
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DMG-PEG Excipient is used?for the preparation of liposome for siRNA delivery with improved transfection efficiency in vitro. DMG-PEG Excipient is also used for the?lipid nanoparticle for an oral plasmid DNA delivery approach in vivo through a facile surface modification to improve the mucus permeability and delivery efficiency of the nanoparticles .
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