Search Result
Results for "
HEK-293T
" in MedChemExpress (MCE) Product Catalog:
2
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-101563
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GSK3326595
Maximum Cited Publications
31 Publications Verification
EPZ015938
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Histone Methyltransferase
SARS-CoV
MDM-2/p53
CDK
Apoptosis
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Infection
Cancer
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GSK3326595 is a protein arginine methyltransferase 5 (PRMT5) inhibitor. GSK3326595 decreases SARS-CoV-2 infection, inhibits cancer cell proliferation and induces pro-inflammatory macrophage polarization and increases hepatic triglyceride levels without affecting atherosclerosis. GSK3326595 can be used for research of relapsed/refractory mantle cell lymphoma .
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- HY-B1456A
-
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LILLY-53858
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COX
Melanocortin Receptor
ERK
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Inflammation/Immunology
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Fenoprofen (LILLY-53858) is a nonsteroidal anti-inflammatory agent (NSAID) and inhibits cyclooxygenase (COX). Fenoprofen is a melanocortin receptors (MCRs) positive allosteric modulator (PAM). Fenoprofen also increases ERK1/2 activation in HEK293T cells. Fenoprofen has anti-arthritic activities and can be used for the study of rheumatoid arthritis and osteoarthritis .
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- HY-110204
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Heclin
3 Publications Verification
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E1/E2/E3 Enzyme
Akt
MyD88
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Others
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Heclin is a HECT E3 ubiquitin ligases inhibitor. Heclin inhibits Smurf2, Nedd4, WWP1 (IC50 values are 6.8, 6.3, 6.9 μM) and can be used for the research of gastric cancer .
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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 .
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- HY-108317
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Phosphatase
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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-153166
-
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PROTACs
GSK-3
Tau Protein
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Neurological Disease
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PT-65 is a GSK3α and GSK3β PROTAC degrader with DC50 values of 28.3 nM and 34.2 nM, respectively. PT-65 inhibits excessive tau phosphorylation mediated by GSK3β, Aβ and Okadaic acid (HY-N6785). PT-65 is applicable for the research of Alzheimer's disease .
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- HY-12833
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AMZ30
1 Publications Verification
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Phosphatase
Akt
ERK
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Others
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AMZ30 is selective protein phosphatase methylesterase-1(PME-1) inhibitor with IC50s of 600 nM and 3.5 µM in human cell lysates and in HEK 293T cells, respectively. AMZ30 shows >100-fold selectivity relative to other serine hydrolases. AMZ30 reduces the demethylated form of PP2A in living cells. AMZ30 attenuates muscle cell differentiation. AMZ30 increases the resistance of U87MG and U251MG glioblastoma cells to t-BHP-induced oxidative stress. AMZ30can be used for the study of glioblastoma .
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- HY-150602
-
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Proteasome
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Neurological Disease
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20S Proteasome activator 1 is a potent 20S proteasome activator with EC200 values of 0.3 μM, 0.7 μM and 1.8 μM for trypsin-like site, chymotrypsin-like site and caspase-like site. 20S Proteasome activator 1 translates well in a cellular system, preventing the accumulation of the pathogenic A53T mutant of α-synuclein. 20S Proteasome activator 1 can be used for researching neurodegenerative diseases .
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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-B0288B
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LILLY-53858 Calcium hydrate
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COX
Melanocortin Receptor
ERK
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Inflammation/Immunology
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Fenoprofen (LILLY-53858) Calcium hydrate is a nonsteroidal anti-inflammatory agent (NSAID) and inhibits cyclooxygenase (COX). Fenoprofen Calcium hydrate is a melanocortin receptors (MCRs) positive allosteric modulator (PAM). Fenoprofen Calcium hydrate also increases ERK1/2 activation in HEK293T cells. Fenoprofen Calcium hydrate has anti-arthritic activities and can be used for the study of rheumatoid arthritis and osteoarthritis .
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- HY-P4076
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HIV
DNA Alkylator/Crosslinker
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Infection
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MPG peptides, Pβ is an amphipathic cell-penetrating peptide. MPG peptides, Pβ consists of three components: the hydrophobic fusion sequence (GALFLGFLGAAGSTMGA) of HIV glycoprotein 41, a spacer domain (WSQP), and the nuclear localization signal (KKKRKV) of the large T antigen of Simian virus 40. MPG peptides, Pβ can form stable non-covalent complexes with nucleic acids (including DNA) through electrostatic interactions and improve their intracellular delivery. MPG peptides, Pβ can be used in studies of HIV-1-related immune responses .
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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-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-155021
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PROTACs
α-synuclein
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Neurological Disease
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PROTAC α-synuclein degrader 5 is a highly selective small-molecule degrader (PROTAC) of α-synuclein aggregates, with a DC50 of 7.51 μM and the highest degradation rate Dmax of 89%. PROTAC α-synuclein degrader 5 contains probe molecule sery308 and E3 ligase ligands. PROTAC α-synuclein degrader 5 can be used for neurological disease research .
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- HY-124833
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- HY-171978
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Adrenergic Receptor
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Cardiovascular Disease
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LM-189 is a β2-adrenergic receptor (β2AR) ligand and G protein-biased modulator with a human β2AR Ki of 0.063 nM.LM-189 promotes β2AR coupling to Gαs and Gαi heterotrimers, stabilizes distinct β2AR conformations including a TM6 outward state, and increases β2AR ICL2 dynamics.LM-189 restricts β2AR ligand-binding pocket conformational heterogeneity, stabilizes polar ligand-receptor interaction networks, and exhibits bias toward Gαi signaling over Gαs signaling.LM-189 enabled cryo-EM structural characterization of the β2AR-Gi complex.LM-189 can be used for the research of congestive heart failure .
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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 has the potential for pancreatic cancer research .
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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-175764
-
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PROTACs
IRAK
NF-κB
p38 MAPK
TNF Receptor
Interleukin Related
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Inflammation/Immunology
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FIP22 is a potent and selective IRAK4 PROTAC degrader (HEK293T cells: DC50 = 3.2 nM; THP-1 cells: DC50 = 10.6 nM). FIP22 induces the ubiquitin-proteasome system by forming an IRAK4-FIP22-CRBN ternary complex (EC50 = 12.63 nM), thereby potently blocking IRAK4-mediated NF-κB and MAPK signaling pathways. FIP22 can be used for the study of atopic dermatitis (Pink: IRAK4 ligand (HY-175765); Blue: CRBN ligand (HY-W087383); Black: Linker (HY-46871)) .
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- HY-118368
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- HY-106275
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Fibrin-derived peptide Bβ15-42
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Flavivirus
Dengue Virus
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Cardiovascular Disease
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FX-06 (Fibrin-derived peptide Bβ15-42) is a fibrin Bbeta chain-derived peptide. FX-06 binds to VE-cadherin and inhibits leukocyte transmigration and initiates VE-cadherin-mediated signaling. FX-06 can be used in the research of ischemia/reperfusion injury, Dengue shock syndrome (DSS) .
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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-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 .
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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-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-W173146
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DNA/RNA Synthesis
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Cancer
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ALKBH5-IN-4 (compound 3) is a RNA m6A demethylase ALKBH5 inhibitor with an IC50 of 0.84 μM. ALKBH5-IN-4 shows inhibitory effect on leukemia cells[1].
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- HY-173444
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HDAC
Transferrin Receptor
Apoptosis
Ferroptosis
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Cancer
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HDAC11-IN-3 (Compound A9) is a selective HDAC11 inhibitor (IC50: 4.1 nM). HDAC11-IN-3 has inhibitory effects on U937 and OCI-AML2 acute myeloid leukemia (AML) cell lines (IC50: 10 μM). HDAC11-IN-3 has significant anti-AML activity, inducing apoptosis, cell cycle arrest, and differentiation. HDAC11-IN-3 upregulates the iron transporters transferrin (TF) and transferrin receptor (TFRC), and activates the p62-Keap1-Nrf2-HMOX1 pathway, which together lead to increased intracellular iron levels and induce ferroptosis in AML cells. HDAC11-IN-3 can be used alone or in combination with Cytarabine (HY-13605) for AML research .
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- HY-175397
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DFHBI-thalidomide
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PROTACs
NF-κB
Early 2 Factor (E2F)
Bcl-2 Family
VEGFR
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Cancer
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Dth (DFHBI-thalidomide) is an RNA aptamer-based PROTAC degrader. Dth can degrade a variety of endogenous proteins (such as mCherry, p50, p65 and E2F1) by replacing the 3′ module on the RNA scaffold with the RNA aptamer corresponding to the target protein. Dth upregulates IκB-α and Bax, and downregulates Bcl-2 and VEGF. Dth generates green fluorescence upon binding to the Broccoli RNA aptamer, enabling the tracing of RNA scaffolds. Dth can be used in cancer-related research .
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- HY-B0288A
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LILLY-53858 Calcium
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COX
Melanocortin Receptor
ERK
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Inflammation/Immunology
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Fenoprofen (LILLY-53858) Calcium is a nonsteroidal anti-inflammatory agent (NSAID) and inhibits cyclooxygenase (COX). Fenoprofen Calcium is a melanocortin receptors (MCRs) positive allosteric modulator (PAM). Fenoprofen Calcium also increases ERK1/2 activation in HEK293T cells. Fenoprofen Calcium has anti-arthritic activities and can be used for the study of rheumatoid arthritis and osteoarthritis .
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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). PHTPP-1304 induces the degradation of estrogen receptor ERβ through the autophagy pathway, rather than ubiquitination (DC50 ≈ 2 nM, in HEK293T cells; < 100 nM in ACHN renal carcinoma and MCF-7 breast cancer cells). PHTPP-1304 can induce the self-oligomerization of p62. PHTPP-1304 can be used to study various cancers mediated by ERβ .
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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-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-179475
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CaSR
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Endocrinology
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KP-2067 is a form of the CaSR agonist peptide. KP-2067 can result in dose-dependent activation of CaSR in HEK293T overexpressing hCaSR cell line, with an EC50 of 18.4 μM. KP-2067 significantly reduces plasma parathyroid hormone in rat model .
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- HY-148933
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- HY-162269
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NAMPT
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Inflammation/Immunology
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Nampt activator-5 is a NAMPT activator with a KD value of 6.19 μM. Nampt activator-5 activates the rate-limiting enzyme in NAD + biosynthesis and promotes NAD + production. Nampt activator-5 delays the senescence process of senescent hepatocytes, extends the lifespan of *Caenorhabditis elegans*, and alleviates age-related dysfunction and abnormal biomarkers in naturally aged mice. Nampt activator-5 can be used in aging research .
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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-178803
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PROTACs
BCL6
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Cancer
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PROTAC BCL6 Degrader-2 (Compound A19) is an orally active, selective BCL6 PROTAC degrader (DC50s: 34 pM in OCI-LY1 cells and 0.45 nM in HEK293T cells). PROTAC BCL6 Degrader-2 promotes the ubiquitination and degradation of BCL6. PROTAC BCL6 Degrader-2 exhibits anticancer activity against BCL6-dependent diffuse large B-cell lymphoma (Pink: BCL6 ligand (HY-178804); Blue: E3 ligase ligand (HY-W087383); E3 ligase ligand + linker (HY-W998306)) .
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- HY-177071
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HIV
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Infection
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Asuptegravir (Compound 1) is an inhibitor of HIV integrase activity. Asuptegravir inhibits HIV in HEK293T cells (EC50 = 1.08 nM). Asuptegravir can be studied in anti-AIDs/HIV research .
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- HY-174811
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PROTACs
Epigenetic Reader Domain
PD-1/PD-L1
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Inflammation/Immunology
Cancer
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PROTAC BRD4 Degrader-33 is an enzyme activated clickable BRD4 PROTAC degrader with favorable tumor microenvironment-response. PROTAC BRD4 Degrader-33 has superior tumor tissue penetration capabilities and efficiently inhibits PD-L1 protein expression. PROTAC BRD4 Degrader-33 shows potent anti-tumoral immunomodulation activity in 4T1 tumor-bearing mice model . Pink: BRD4 ligand (HY-174812); Blue: CRBN ligase ligand (HY-10984); Black: linker
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- HY-147086
-
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Leukotriene Receptor
G protein-coupled Bile Acid Receptor 1
TNF Receptor
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Metabolic Disease
Inflammation/Immunology
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CAY10789 is a potent CysLT1R (cysteinyl leukotriene receptor 1) antagonist (IC50=2.80 μM) and GPBAR1 (G-protein-coupled bile acid receptor 1) agonist (EC50=3 μM). CAY10789 significantly reduces the adhesion of U937 cells to HAEC, reduces the expression of TNF-α. CAY10789 shows very promising metabolic stability and excellent pharmacokinetics. CAY10789 can be used for the research of colitis, metabolic syndromes, and other GPBAR1/CysLT1R-related diseases .
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- HY-156401
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PROTACs
Epigenetic Reader Domain
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Cancer
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BRD9 c-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-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-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-173431
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Dopamine Receptor
Reactive Oxygen Species (ROS)
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Cancer
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Dopamine D4 receptor ligand 3 (Compound 16) is a dopamine D4 receptor (D4R) antagonist (pKi: 8.86). Dopamine D4 receptor ligand 3 has pIC50 values of 5.78, 5.55, and 6.17 for Go, Gi, and βArr2 sensors in HEK-293T cells, respectively. Dopamine D4 receptor ligand 3 inhibits the viability of three human glioma cell lines, U87 MG, T98G, and U251 MG. Dopamine D4 receptor ligand 3 induces ROS production and mitochondrial dysfunction in glioma cells .
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- HY-160227
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Toll-like Receptor (TLR)
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Inflammation/Immunology
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ORN 06 (Compound R-0006), a U-rich single-stranded RNA (containing 6 repeats of the UUG sequence motif), is a TLR7/8 agonist. ORN 06 stimulates human TLR7/8-mediated or murine TLR7-mediated immunity .
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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-171942A
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C24:1-GM2 ammonium
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Endogenous Metabolite
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Neurological Disease
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C24:1 Ganglioside GM2 (d18:1/24:1) (ammonium) is an endogenous monosialylated ganglioside. C24:1 Ganglioside GM2 (d18:1/24:1) (ammonium) is a self-lipid that can bind to CD1d in HEK293T cells .
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- HY-175136
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GAh acetate
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Adrenergic Receptor
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Infection
Neurological Disease
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Chloroguanabenz (acetate) is an antiprion agent and a derivative of the α2-adrenergic receptor agonist guanabenz. Chloroguanabenz (acetate) can inhibit the formation of prion in yeast and mammalian in vitro assays. Chloroguanabenz (acetate) can reduce the levels of truncated Huntingtin derivative Htt48 in HEK293T cells. Chloroguanabenz (acetate) can be studied in research on Huntington’s disease .
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- HY-176288
-
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Eukaryotic Initiation Factor (eIF)
Bcl-2 Family
Apoptosis
Ras
PERK
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Cancer
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eIF4E/eIF4G PPI-IN-1 is an eIF4E/eIF4G interaction inhibitor with a KD of 20.2 μM for eIF4E protein. eIF4E/eIF4G PPI-IN-1 plays an antitumor role in multiple modes of action including regulating the activity of eIF4E by inhibiting the Ras/MAPK/eIF4E signaling pathway, apoptosis and cell migration. eIF4E/eIF4G PPI-IN-1 suppresses the growth of HepG2 xenografts in nude mice and was relatively nontoxic to mice .
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- HY-172541
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CXCR
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Cardiovascular Disease
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LN6023 (hydrochloride) (Compound 27) is a CXCR7 agonist. LN6023 (hydrochloride) induces the recruitment of β-arrestin in HEK293T cells expressing human CXCR7 (EC50 = 3.5 µM). LN6023 (hydrochloride) reduces the surface level of P-selectin in isolated and washed human platelets. LN6023 (hydrochloride) can be used to study platelet-mediated thrombosis .
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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-B1456AR
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LILLY-53858 (Standard)
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Reference Standards
COX
Melanocortin Receptor
ERK
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Inflammation/Immunology
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Fenoprofen (Standard) (LILLY-53858 (Standard)) is the analytical standard of Fenoprofen (HY-B1456A). This product is intended for research and analytical applications. Fenoprofenc is a nonsteroidal anti-inflammatory agent (NSAID) and inhibits cyclooxygenase (COX). Fenoprofen is a melanocortin receptors (MCRs) positive allosteric modulator (PAM). Fenoprofen also increases ERK1/2 activation in HEK293T cells. Fenoprofen has anti-arthritic activities and can be used for the study of rheumatoid arthritis and osteoarthritis.
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- HY-176051
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RgE
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GLUT
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Cancer
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Rapaglutin E (RgE) is a glucose transporter (GLUT) inhibitor. Rapaglutin E exhibits dose-dependent inhibition of [ 3H]-2DG uptake in A549, Jurkat T, PANC10.05, and RBC, with IC50 values 8.9 nM, 3.1 nM, 35.5 nM, 74.2 nM. Rapaglutin E inhibits cell proliferation in A549, PANC10.05, HeLa, Jurkat T, and HEK293T cells .
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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-B0288BR
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LILLY-53858 Calcium hydrate (Standard)
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Reference Standards
COX
Melanocortin Receptor
ERK
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Inflammation/Immunology
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Fenoprofen (LILLY-53858 (Standard)) (Standard) Calcium hydrate is the analytical standard of Fenoprofen Calcium hydrate (HY-B0288B). This product is intended for research and analytical applications. Fenoprofen is a nonsteroidal anti-inflammatory agent (NSAID) and inhibits cyclooxygenase (COX). Fenoprofen is a melanocortin receptors (MCRs) positive allosteric modulator (PAM). Fenoprofen also increases ERK1/2 activation in HEK293T cells. Fenoprofen has anti-arthritic activities and can be used for the study of rheumatoid arthritis and osteoarthritis.
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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-B1456AS
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LILLY-53858-13C6 sodium hydrate
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Isotope-Labeled Compounds
COX
Melanocortin Receptor
ERK
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Inflammation/Immunology
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Fenoprofen- 13C6 (LILLY-53858- 13C6) sodium hydrate is the 13C labeled Fenoprofen (HY-B1456A).Fenoprofen (LILLY-53858) is a nonsteroidal anti-inflammatory agent (NSAID) and inhibits cyclooxygenase (COX). Fenoprofen is a melanocortin receptors (MCRs) positive allosteric modulator (PAM). Fenoprofen also increases ERK1/2 activation in HEK293T cells. Fenoprofen has anti-arthritic activities and can be used for the study of rheumatoid arthritis and osteoarthritis .
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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-178439
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SARS-CoV
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Infection
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SARS-CoV-2 3CLpro-IN-33 (Compound 16) is an orally active SARS-CoV-2 3CL protease inhibitor, with an IC50 value of 1.5 nM. SARS-CoV-2 3CLpro-IN-33 shows excellent anti-SARS-CoV-2 viral activity in the HEK293T-AT cell model with an EC50 of 0.017 μM. SARS-CoV-2 3CLpro-IN-33 can be used for the study of COVID-19 infetction .
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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-172965
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SARS-CoV
Virus Protease
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Infection
Inflammation/Immunology
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SARS-CoV-2 Mpro-IN-43 (Compound 1) is a coronavirus main protease (Mpro) inhibitor (IC50: 72 μM). SARS-CoV-2 Mpro-IN-43 interacts with key residues in the active site of Mpro via non-covalent binding, exerting its anti-coronavirus effect. SARS-CoV-2 Mpro-IN-43 exhibits moderate to low cytotoxicity, with CC50 values of 13.24, 41.02, and 42.26 µM in HaCaT, HEK293T, and HepG2 cells, respectively. SARS-CoV-2 Mpro-IN-43 can be used in anti-SARS-CoV-2 research .
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- HY-163816
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Cytochrome P450
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Cancer
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Antiproliferative agent-53-d3 (Compound C1) is an inhibitor for theta-mediated end joining (TMEJ) in HEK293 cell with an IC50 of 0.14 µM. Antiproliferative agent-53-d3 is the inhibitor for CYP2C19 and CYP2C9 with IC50 of 0.77 and 3.1 µM. Antiproliferative agent-53-d3 inhibits the proliferation of DNA repair-compromised cells, with IC50 of 8.1 µM for BRCA2 -/- DLD-1. Antiproliferative agent-53-d3 exhibits good pharmacokinetic characteristics in CD-1 mice .
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- HY-173411
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Glycosidase
SARS-CoV
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Infection
Inflammation/Immunology
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DNJ-20 is an α-glucosidase inhibitor (IC50: 55.3 μg/mL). DNJ-20 has broad-spectrum anti-SARS-CoV-2 activity. DNJ-20 inhibits the correct processing of viral glycoproteins by interfering with the endoplasmic reticulum-associated glycoprotein folding process (ERQC), thereby blocking the formation and infection of viral particles. DNJ-20 has IC50 values up to 1.49 uM against several SARS-CoV-2 variants, as well as HCoV-229E and HCoV-0C43。DNJ-20 can be used for pan-coronavirus research .
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- HY-149779
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Calcium Channel
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Cardiovascular Disease
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RyR2 stabilizer-1 (compound 12a) is a potent RyR2 stabilizer and SERCA2a activator with EC50s of 2.7 μM for RyR2 and 383 nM for SERCA2. RyR2 stabilizer-1 inhibits Ca 2+ leakage from the SR RyR2 while promoting SERCA2 to pump Ca 2+ back to SR, which make RyR2 stabilizer-1 possible to prevent cardiac arrhythmias .
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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 .
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- HY-180781
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ADAMTS
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Inflammation/Immunology
Cancer
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ADAMTS-5-IN-4 (Compound 4b) is a selective ADAMTS5 inhibitor with an IC₅₀ of 9.4 μM. ADAMTS-5-IN-4 significantly inhibits the degradation of Aggrecan in the implants of the osteoarthritis model. ADAMTS-5-IN-4 effectively inhibits the pseudopod elongation and directional migration of ovarian cancer cells. ADAMTS-5-IN-4 shows significant cytotoxicity to HEK293T cells, human chondrocytes, and porcine chondrocyte implants. ADAMTS-5-IN-4 can be used for the study of osteoarthritis and ovarian cancer .
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- HY-177903
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Drug Derivative
GLUT
DNA/RNA Synthesis
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Cancer
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Triptolide-6-succinate-β-D-glucose (Compound 2) is a glucose-conjugated derivative of Triptolide (HY-32735). Triptolide-6-succinate-β-D-glucose is a tumor-selective prodrug targeting glucose transporters ( GLUT). Triptolide-6-succinate-β-D-glucose can induce the degradation of the RPB subunit of RNA polymerase II. Triptolide-6-succinate-β-D-glucose inhibits the proliferation of HEK293T cells with an IC50 value of 268 nM. Triptolide-6-succinate-β-D-glucose can be used for the research of cancer, such as prostatic cancer .
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- HY-P11592
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Bacterial
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Infection
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KIKIKPWWWPKIKIK-NH2 is a β-turn antimicrobial peptide. KIKIKPWWWPKIKIK-NH2 can inhibit bacterial biofilm formation and bind to lipopolysaccharid. KIKIKPWWWPKIKIK-NH2 shows wound-healing ability in mice bacteria-infected full-thickness wound models. KIKIKPWWWPKIKIK-NH2 can be used for the research of bacterial infection .
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- HY-101563R
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EPZ015938 (Standard)
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Histone Methyltransferase
Reference Standards
SARS-CoV
MDM-2/p53
CDK
Apoptosis
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Infection
Cancer
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GSK3326595 (Standard) is the analytical standard of GSK3326595 (HY-101563). This product is intended for research and analytical applications. GSK3326595 is a protein arginine methyltransferase 5 (PRMT5) inhibitor. GSK3326595 decreases SARS-CoV-2 infection, inhibits cancer cell proliferation and induces pro-inflammatory macrophage polarization and increases hepatic triglyceride levels without affecting atherosclerosis. GSK3326595 can be used for research of relapsed/refractory mantle cell lymphoma .
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- HY-183148
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NAMPT
ATP Synthase
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Neurological Disease
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NAMPT activator-10 (Compound B11) is an orally active NAMPT activator with a target Kd value of 0.64 μM. NAMPT activator-10 activates the rate-limiting enzyme in NAD + biosynthesis and promotes intracellular NAD + synthesis. NAMPT activator-10 reduces lactate accumulation, enhances glycogen storage in the liver and muscle, increases tissue ATP production, improves exercise endurance and muscle strength, and exerts a protective effect against fatigue-induced muscle damage in mouse fatigue models. NAMPT activator-10 can be used in studies related to muscle fatigue .
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- HY-183728
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YAP
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Cancer
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LC-TEAD01 is a potent covalent transcription enhancer-associated domain (TEAD) inhibitor with an IC50 of 116 nM and a Ki of 0.132 μM. LC-TEAD01 disrupts the TEAD-YAP interaction and inhibits TEAD-dependent transcriptional activity. LC-TEAD01 suppresses the proliferation of NF2-deficient cancer cells. LC-TEAD01 inhibits tumor growth in NF2-deficient xenograft models. LC-TEAD01 can be used in studies related to NF2-deficient malignant pleural mesothelioma .
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- HY-182308
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Interleukin Related
TNF Receptor
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Inflammation/Immunology
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LC-PDA-01 is a selective peroxiredoxin 1 (PRDX1) activator with an EC50 of 111.8 nM and a human KD of 123.2 nM. LC-PDA-01 inhibits the expression of pro-inflammatory cytokines IL-1β, IL-6 and TNF-α. LC-PDA-01 can be used in antioxidant/anti-inflammatory research .
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- HY-182289
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Glycosidase
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Metabolic Disease
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LY-23 is an orally active α-glucosidase inhibitor (Ki = 0.05 μM), with IC50 values of 0.18 μM, 0.14 μM and 0.51 μM against maltase, sucrase and isomaltase, respectively. LY-23 reduces the level of postprandial blood glucose elevation. LY-23 is applicable to research related to postprandial hyperglycemia .
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- HY-183754
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EGFR
PI3K
Akt
Apoptosis
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Cancer
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EGFR-IN-213 is a selective inhibitor of EGFR L858R/T790M/C797S with a human IC50 of 0.48 nM. EGFR-IN-213 acts as an antiproliferative agent, inducing apoptosis and cell cycle arrest, and inhibiting colony formation, cell migration, and tube formation. EGFR-IN-213 can be used for the research of non-small cell lung cancer, chronic myeloid leukemia, gastric cancer, prostate cancer .
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- HY-183630
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DNA/RNA Synthesis
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Cancer
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AZD4956 is a potent and selective DNA polymerase theta (POLQ) inhibitor. AZD4956 exhibits an IC50 value of less than 3 μmol/L against POLQ and 3.4 μmol/L against MMEJ. AZD4956 suppresses the MMEJ pathway and enhances the activity of DNA-damaging agents in HRR-deficient cellular contexts. AZD4956 shows antitumor activity in BRCA1/2-mutated triple-negative breast cancer and prostate cancer models. AZD4956 can be used for the study of homologous recombination-deficient tumors .
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- HY-186073
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HDAC
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Neurological Disease
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HDAC1 activator-1 is a specific HDAC1 activator with orally activity, exerting no significant effects on other HDAC family members. HDAC1 activator-1 exhibits neuroprotective activity, ameliorates cognitive and motor function deficits by reducing neuronal loss and gliosis. HDAC1 activator-1 specifically activates HDAC1 in SH-SY5Y cells and exerts regulatory effects on aberrant cell cycle and DNA damage. HDAC1 activator-1 can be used for the research of TDP-43 proteinopat1-related neurodegenerative diseases including Amyotrophic Lateral Sclerosis (ALS) and cerebral ischemia-related neurological injury .
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| Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P4076
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HIV
DNA Alkylator/Crosslinker
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Infection
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MPG peptides, Pβ is an amphipathic cell-penetrating peptide. MPG peptides, Pβ consists of three components: the hydrophobic fusion sequence (GALFLGFLGAAGSTMGA) of HIV glycoprotein 41, a spacer domain (WSQP), and the nuclear localization signal (KKKRKV) of the large T antigen of Simian virus 40. MPG peptides, Pβ can form stable non-covalent complexes with nucleic acids (including DNA) through electrostatic interactions and improve their intracellular delivery. MPG peptides, Pβ can be used in studies of HIV-1-related immune responses .
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- HY-106275
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Fibrin-derived peptide Bβ15-42
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Flavivirus
Dengue Virus
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Cardiovascular Disease
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FX-06 (Fibrin-derived peptide Bβ15-42) is a fibrin Bbeta chain-derived peptide. FX-06 binds to VE-cadherin and inhibits leukocyte transmigration and initiates VE-cadherin-mediated signaling. FX-06 can be used in the research of ischemia/reperfusion injury, Dengue shock syndrome (DSS) .
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- HY-179475
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CaSR
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Endocrinology
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KP-2067 is a form of the CaSR agonist peptide. KP-2067 can result in dose-dependent activation of CaSR in HEK293T overexpressing hCaSR cell line, with an EC50 of 18.4 μM. KP-2067 significantly reduces plasma parathyroid hormone in rat model .
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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 .
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- HY-P11592
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Bacterial
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Infection
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KIKIKPWWWPKIKIK-NH2 is a β-turn antimicrobial peptide. KIKIKPWWWPKIKIK-NH2 can inhibit bacterial biofilm formation and bind to lipopolysaccharid. KIKIKPWWWPKIKIK-NH2 shows wound-healing ability in mice bacteria-infected full-thickness wound models. KIKIKPWWWPKIKIK-NH2 can be used for the research of bacterial infection .
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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. The 1 mL is defined as the base specification. All larger sizes correspond to incremental volumes of this base.
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| Cat. No. |
Product Name |
Chemical Structure |
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- HY-B1456AS
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Fenoprofen- 13C6 (LILLY-53858- 13C6) sodium hydrate is the 13C labeled Fenoprofen (HY-B1456A).Fenoprofen (LILLY-53858) is a nonsteroidal anti-inflammatory agent (NSAID) and inhibits cyclooxygenase (COX). Fenoprofen is a melanocortin receptors (MCRs) positive allosteric modulator (PAM). Fenoprofen also increases ERK1/2 activation in HEK293T cells. Fenoprofen has anti-arthritic activities and can be used for the study of rheumatoid arthritis and osteoarthritis .
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- HY-163816
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Antiproliferative agent-53-d3 (Compound C1) is an inhibitor for theta-mediated end joining (TMEJ) in HEK293 cell with an IC50 of 0.14 µM. Antiproliferative agent-53-d3 is the inhibitor for CYP2C19 and CYP2C9 with IC50 of 0.77 and 3.1 µM. Antiproliferative agent-53-d3 inhibits the proliferation of DNA repair-compromised cells, with IC50 of 8.1 µM for BRCA2 -/- DLD-1. Antiproliferative agent-53-d3 exhibits good pharmacokinetic characteristics in CD-1 mice .
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| Cat. No. |
Product Name |
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Classification |
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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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