Search Result
Results for "
nanomolar
" in MedChemExpress (MCE) Product Catalog:
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- HY-141520
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ART558
Maximum Cited Publications
49 Publications Verification
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DNA/RNA Synthesis
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Cancer
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ART558 is a potent, selective and allosteric DNA polymerase theta (Polθ) inhibitor (IC50=7.9 nM). ART558 elicits BRCA-gene synthetic lethality and DNA damage. ART558 can be used for the research of cancer, such as breast cancer .
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- HY-114361
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- HY-12866
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LOXO-101; ARRY-470
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Trk Receptor
Apoptosis
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Cancer
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Larotrectinib (LOXO-101) is an ATP-competitive oral, selective inhibitor of the tropomyosin-related kinase (TRK) family receptors, with low nanomolar 50% inhibitory concentrations against all three isoforms (TRKA, B, and C).
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- HY-101213
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- HY-12866A
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LOXO-101 sulfate; ARRY-470 sulfate
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Trk Receptor
Apoptosis
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Cancer
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Larotrectinib sulfate (LOXO-101 sulfate; ARRY-470 sulfate) is an ATP-competitive oral, selective inhibitor of the tropomyosin-related kinase (TRK) family receptors, with low nanomolar 50% inhibitory concentrations against all three isoforms (TRKA, B, and C).
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- HY-16978
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- HY-132298
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Adenylate Cyclase
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Others
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TDI-10229 is a potent and orally bioavailable inhibitor of soluble adenylyl cyclase (sAC, ADCY10). TDI-10229 displays nanomolar inhibition of sAC in both biochemical and cellular assays (IC50 of 195 nM) and exhibits mouse pharmacokinetic properties sufficient to warrant its use as an in vivo tool compound .
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- HY-122025
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Androgen Receptor
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Metabolic Disease
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AC-262536 is a selective and non-steroidal androgen receptor modulators (SARMs) with beneficial anabolic effects. AC-262536 exhibits potent agonist activity at the androgen receptor, with an affinity in the low nanomolar range (1-10 nM) .
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- HY-18932
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ERK
Apoptosis
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Cancer
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DEL-22379 is an ERK dimerization Inhibitor. DEL-22379 readily binds to ERK2 with a Kd estimated in the low micromolar range, though binding is detectable even at low nanomolar concentrations. ERK2 dimerization is progressively inhibited with an IC50 of ~0.5 μM.
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- HY-14776
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CX-3543
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DNA/RNA Synthesis
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Cancer
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Quarfloxin (CX-3543), a fluoroquinolone derivative with antineoplastic activity, targets and inhibits RNA pol I activity, with IC50 values in the nanomolar range in neuroblastoma cells. Quarfloxin disrupts the interaction between the nucleolin protein and a G-quadruplex DNA structure in the ribosomal DNA (rDNA) template .
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- HY-N3755
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Estrogen Receptor/ERR
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Cancer
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Dihydroresveratrol, a potent phytoestrogen, is a hormone receptor modulator. Dihydroresveratrol exhibits proliferative effects in androgen-independent prostate and breast cancer cells at picomolar and nanomolar concentrations .
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- HY-114388
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- HY-50001
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Influenza Virus
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Infection
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Nucleozin, a potent inhibitor of influenza A virus infection, induces the formation of nucleoprotein (NP) aggregates and antagonizes its nuclear accumulation, leading to cessation of viral replication. Nucleozin impedes influenza A virus replication in vitro with a nanomolar EC50 .
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- HY-102074
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Measles Virus
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Infection
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ERDRP-0519, an orally bioavailable small-molecule Measles virus (MeV) polymerase inhibitor, prevents measles disease in squirrel monkeys (Saimiri sciureus). ERDRP-0519 inhibits morbilliviruses with nanomolar potency. .
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- HY-101124
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KAR5585
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Tryptophan Hydroxylase
5-HT Receptor
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Cardiovascular Disease
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Rodatristat ethyl (KAR5585) is a first-in-class oral tryptophan hydroxylase 1 (TPH1) Inhibitor with nanomolar in vitro potency. Rodatristat ethyl reduces the level of 5-HT and significantly reduces pulmonary arterial hypertension (PAH) .
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- HY-P10724
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Formyl Peptide Receptor (FPR)
Bacterial
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Infection
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fMIFL is a formyl tetrapeptide derived from Staphylococcus aureus, and also an agonist of mouse formyl peptide receptor 1 (mFPR1). It exhibits nanomolar activity against mFPR1 and micromolar activity against mFPR2. fMIFL is applicable to studies related to bacterial infections .
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- HY-127106
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Potassium Channel
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Neurological Disease
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VU0810464 is a potent and selective non-ureaG protein-gated inwardly-rectifying potassium channels (GIRK, Kir3) activator. VU0810464 displays nanomolar potency for neuronal (EC50=165 nM) and GIRK1/4 (EC50=720 nM) channels with improved brain penetration .
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- HY-18622
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Src
FGFR
PDGFR
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Cancer
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PP58 is a pyrido[2,3-d]pyrimidine-based compound that inhibits PDGFR, FGFR and Src family activities with nanomolar IC50 values.
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- HY-112862
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Arg-AMS
1 Publications Verification
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Aminoacyl-tRNA Synthetase
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Infection
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Arg-AMS (compound 24) is a potent nanomolar inhibitor of arginyl tRNA synthetase, which displays tightly bound inhibitory characteristics for the A-domains in non-ribosomal peptide synthetases (NRPS) enzymes .
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- HY-153213
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TSH Receptor
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Metabolic Disease
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Org 274179-0 is a potent and allosteric antagonist of thyroid-stimulating hormone (TSH) receptor, with an IC50 of nanomolar concentration. Org 274179-0 completely inhibits TSH (and TSI)-mediated TSH receptor activation with little effect on the potency of TSH. Org 274179-0 can be used for the research of Graves' disease (GD) .
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- HY-W022759
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Cholinesterase (ChE)
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Others
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9-Acridinecarboxylic acid is a precursor of a cholinesterase inhibitor, and its derivatives have nanomolar inhibitory potency against AChE and BChE .
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- HY-120530
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mGluR
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Neurological Disease
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JNJ-46281222 is an metabotropic glutamate (mGlu) 2-selective, highly potent PAM (positive allosteric modulator) with nanomolar affinity (Kd = 1.7 nM) and a high modulatory potency (pEC50 = 7.71) .
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- HY-101634
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HCV
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Infection
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ABT-072 is an orally active and potent non-nucleoside HCV NS5B polymerase inhibitor (HCV GT1a EC50=1 nM; HCV GT1b EC50=0.3 nM) .
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- HY-P2274
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Parasite
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Infection
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Argifin is a sub-nanomolar chitinase inhibitor produced by soil microorganisms, with IC50s of 0.025 μM, 6.4 μM , 1.1 μM and 4.5 μM for SmChiA (Serratia marcescens chitinaese A), SmChiB, Aspergillus fumigatus chitinase B1 and human chitotriosidase, respectively .
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- HY-12607
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Parasite
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Infection
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ML251, a potent nanomolar T. brucei and T. cruzi phosphofructokinase (PFK) inhibitor, inhibits T. brucei PFK (IC50=0.37 μM) and T. cruzi PFK (IC50=0.13 μM). ML251 can be used for the research of parasite .
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- HY-138649
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Influenza Virus
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Neurological Disease
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PB2 is a tris(2-carboxyethyl)phosphine (TCEP) analogue increasing retinal ganglion (RGCs) cells survival after axotomy in vitro at nanomolar and picomolar concentrations. PB2 is substantially more permeable than TCEP. PB2, as a reducing agent, is highly neuroprotective for RGCs .
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- HY-108579
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Potassium Channel
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Cardiovascular Disease
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UCL 1684 (dibromide) is a first nanomolar, non-peptidic small conductance calcium-activated potassium (SK) channel blocker. UCL 1684 (dibromide) is effective in preventing the development of atrial fibrillation due to potent atrial-selective inhibition of INa. UCL 1684 (dibromide) causes atrial-selective prolongation of ERP secondary to induction of postrepolarization refractoriness .
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- HY-118438
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Aryl Hydrocarbon Receptor
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Inflammation/Immunology
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10-Cl-BBQ is a high affinity AhR ligand with immunosuppressive activity. 10-Cl-BBQ promotes cytosol to nuclear translocation of AhR and activates the AhR-regulated reporter gene at nanomolar concentrations .
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- HY-19509
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Reverse Transcriptase
HIV
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Infection
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IQP-0528 is a highly potent nonnucleoside reverse transcriptase inhibitor (NNRTI). IQP-0528 shows nanomolar activity against both HIV-1 and HIV-2, with EC50s of 0.2 nM and 100 nM, respectively .
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- HY-153534
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MicroRNA
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Cancer
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microRNA-21-IN-3 (compound 45) can specifically bind to the precursor of oncogenic and pro-inflammatory microRNA-21 with medium nanomolar affinity, reduce cancer cell proliferation and miR-21 levels, and can be used in antitumor research .
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- HY-50055
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ERK
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Cancer
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EtDO-P4 is a nanomolar inhibitor of glycosphingolipid (GSL) synthesis. EtDO-P4 suppresses activation of the EGFR-induced ERK pathway and various receptor tyrosine kinases (RTKs). EtDO-P4 can be used for various types of cancer, including Burkitt’s lymphoma .
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- HY-137392
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1-Naphthalenesulfonyl-Ile-Trp-CHO
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Cathepsin
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Others
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Cathepsin L-IN-4 is an inhibitor of cathepsin L with IC50 at nanomolar concentrations .
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- HY-133735A
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RABV
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Infection
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GRP-60367 hydrochloride is a first-in-class small-molecule rabies virus (RABV) entry inhibitor with nanomolar potency against some RABV strains. GRP-60367 hydrochloride specifically targets the RABV G protein .
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- HY-101634A
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HCV
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Infection
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ABT-072 (potassium trihydrate) is an orally active and potent non-nucleoside HCV NS5B polymerase inhibitor (HCV GT1a EC50=1 nM; HCV GT1b EC50=0.3 nM) .
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- HY-138648
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ERK
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Neurological Disease
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PB1 is a potent intracellular disulfide reducing agent with several advantages including good cell permeability, the ability to form a high intracellular concentration gradient, and stability. PB1 is a borane-protected TCEP (tris(2-carboxyethyl)phosphine) analogue. PB1 increases retinal ganglion cells survival after axotomy in vitro at nanomolar and picomolar concentrations. PB1 can be used for the research of neuroprotective .
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- HY-130613
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Bacterial
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Infection
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MAC-545496 is a nanomolar inhibitor of glycopeptide-resistance-associated protein R (GraR). MAC-545496 displays strong binding affinity to the full-length GraR protein (Kd ≤ 0.1 nM). MAC-545496 is an antivirulence agent that reverses β-lactam resistance in Methicillin-resistant strains (MRSA) .
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- HY-156786
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Reactive Oxygen Species (ROS)
Influenza Virus
SARS-CoV
HSV
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Infection
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TLD-1433 is the fourth-generation ruthenium (II) based photodynamic compound (PDC). TLD-1433 is activated by green light (525 ± 25 nm) and efficiently generates ROS to achieve pathogen inactivation. After photoinactivation, TLD-1433 significantly induces lipid peroxidation of the cell membrane, which can directly damage the integrity of the viral envelope. TLD-1433 has ID50 for enveloped viruses (such as H1N1 influenza virus, coronavirus OC43, HSV-1, Zika virus) is as low as nanomolar level; for non-enveloped viruses (such as adenovirus Ad5, mammalian rotavirus MRV), a concentration of micro-molar level is required for inactivation. TLD-1433 has antigen retention property and can be used for the preparation of inactivated vaccines .
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- HY-133735
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RABV
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Infection
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GRP-60367 is a first-in-class small-molecule rabies virus (RABV) entry inhibitor with nanomolar potency against some RABV strains .
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- HY-141495
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- HY-132170
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Dihydroorotate Dehydrogenase
Parasite
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Infection
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DSM502 is a pyrrole-based Dihydroorotate Dehydrogenase (DHODH) inhibitor. DSM502 exhibits nanomolar potency againsts Plasmodium DHODH and Plasmodium parasites, with no inhibition of mammalian DHODHs .
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- HY-146214
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CDK
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Cancer
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As a cdk4/6 inhibitor. Compounds 10B and 10C showed low nanomolar activity, ideal antiproliferative activity, excellent metabolic properties and acceptable pharmacokinetics on cdk4/6.
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- HY-126275
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ROCK
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Cancer
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HSD1590 is potent ROCK inhibitor, with IC50s of 1.22 and 0.51 nM for ROCK1 and ROCK2, respectively. HSD1590 exhibits single digit nanomolar binding to ROCK (Kds<2 nM). HSD1590 displays low cytotoxicity .
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- HY-132171A
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Dihydroorotate Dehydrogenase
Parasite
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Infection
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DSM705 hydrochloride, an orally active antimalarial compound, is a pyrrole-based Dihydroorotate Dehydrogenase (DHODH) inhibitor. DSM705 hydrochloride exhibits nanomolar potency against Plasmodium DHODH and Plasmodium parasites (IC50=95, 52 nM for P. falciparum and P. vivax DHODH, respectively), with no inhibition of mammalian DHODHs .
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- HY-155840
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HDAC
Apoptosis
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Cancer
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KH16 is a potent and low nanomolar HDAC inhibitor. KH16 is against class I HDACs HDAC1, HDAC2, and HDAC3, with IC50 values ranging from 6 to 34 nM. KH16 induces cell apoptosis and is against tumor cells with various gene expression patterns .
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- HY-156060
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Toll-like Receptor (TLR)
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Inflammation/Immunology
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NCI126224 is a TLR4 signaling inhibitor. NCI126224 suppress LPS (HY-D1056)-induced production of NF-κB, TNF-α, IL-1β, and NO in the nanomolar-low micromolar range. NCI126224 can be used for the research of inflammatory diseases .
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- HY-141520G
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DNA/RNA Synthesis
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Cancer
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ART558 (GMP) is ART558 (HY-141520) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. ART558 is a potent, selective and allosteric DNA polymerase theta (Polθ) inhibitor (IC50=7.9 nM). ART558 elicits BRCA-gene synthetic lethality and DNA damage. ART558 can be used for the research of cancer, such as breast cancer .
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- HY-132171
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Dihydroorotate Dehydrogenase
Parasite
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Infection
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DSM705 is a pyrrole-based Dihydroorotate Dehydrogenase (DHODH) inhibitor. DSM705 exhibits nanomolar potency against Plasmodium DHODH and Plasmodium parasites, with no inhibition of mammalian DHODHs. DSM705 is a potent antimalarial compound .
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- HY-156177
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Toll-like Receptor (TLR)
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Inflammation/Immunology
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TLR7 agonist 16 (compound 16d) is a highly potent TLR7 agonist with an EC50 of 18 nM. TLR7 agonist 16 potently induces the activation of mouse macrophages and hPBMCs at low-nanomolar concentrations .
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- HY-156176
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Toll-like Receptor (TLR)
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Inflammation/Immunology
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TLR7 agonist 15 (compound 16b) is a highly potent TLR7 agonist with an EC50 of 18 nM. TLR7 agonist 15 potently induces the activation of mouse macrophages and hPBMCs at low-nanomolar concentrations .
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- HY-P10331
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SDCBP
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Cancer
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KSL 128114, a peptide inhibitor of syntenin, binds the PDZ1 domain of syntenin with nanomolar affinity. KSL 128114 is resistant toward degradation in human plasma and mouse hepatic microsomes and displays a global PDZ domain selectivity for syntenin .
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- HY-163727
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Parasite
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Infection
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MMV1557817 is an orally active and potent antimalarial compound. MMV1557817 is a selective, nanomolar inhibitor of both Plasmodium falciparum and Plasmodium vivax aminopeptidases M1 and M17, leading to inhibition of end-stage hemoglobin digestion in asexual parasites .
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- HY-118423
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IQP-0410
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HIV
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Inflammation/Immunology
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SJ-3366 (IQP-0410) is a potent inhibitor of HIV nonnucleoside reverse transcriptase . SJ-3366 (IQP-0410) inhibits HIV at sub-nanomolar concentrations primarily through a typical non-nucleoside mechanism .
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- HY-161096
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ROR
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Cancer
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Antitumor agent-127 (compound 1) is a parent macrocyclic peptide. Antitumor agent-127 displays nanomolar cell-based binding to ROR1 and relatively good internalization in 786-O and MDA-MB-231 tumor cell lines .
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- HY-174978
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Isocitrate Dehydrogenase (IDH)
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Others
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SK60 is a dimethylated derivative of GSK321 (HY-18948) with low nanomolar potency and high selectivity for IDH1R132H (IC50 = 14.5 nM). SK60 can be used as a tracer for brain imaging with the fluorescent label [ 18F] .
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- HY-126973
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HCV Protease
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Infection
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BI-1230, a chemical probe, is potent and digit nanomolar inhibitor of HCV NS3 protease and of viral replication. BI-1230 is also highly selective against other serine/cysteine proteases. BI-1230 shows good Pharmacokinetic(PK) activity .
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- HY-W741940
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Others
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Cardiovascular Disease
Cancer
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Evomonoside is a type of cardiac glycoside compound. Evomonoside exhibits significant in vitro anticancer activity, especially having nanomolar inhibitory concentrations against gastric cancer cell lines. Evomonoside has typical cardiac toxicity risks, including arrhythmias and conduction abnormalities. Evomonoside can be used for research on gastric cancer .
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- HY-P10672
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- HY-145823
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EGFR
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Cancer
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EGFR-IN-42 (Compound 17b) is a potent inhibitor of EGFR with single-digit nanomolar activity. EGFR-IN-42 connects tamoxifen or endoxifen with the EGFR-inhibitor gefitinib via a covalent linkage. EGFR-IN-42 retains both ER antagonist activity and EGFR inhibition. EGFR-IN-42 has superior anti-cancer activity .
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- HY-145824
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EGFR
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Cancer
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EGFR-IN-43 (Compound 17c) is a potent inhibitor of EGFR with single-digit nanomolar activity. EGFR-IN-43 connects tamoxifen or endoxifen with the EGFR-inhibitor gefitinib via a covalent linkage. EGFR-IN-43 retains both ER antagonist activity and EGFR inhibition. EGFR-IN-43 has superior anti-cancer activity .
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- HY-146229
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VEGFR
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Cancer
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VEGFR-2-IN-25 (compound 5d) is a highly potent VEGFR-2 inhibitor with an IC50 value of 12.1 nM. VEGFR-2-IN-25 can be used for researching anticancer .
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- HY-139625
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Microtubule/Tubulin
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Cancer
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Dolastatinol is a synthetic analog of dolastatin 10 and low nanomolar inhibitor of tubulin polymerization.
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- HY-142253
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HIV
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Infection
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HIV-1 inhibitor-10 is a nanomolar HIV-1 maturation inhibitor.
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- HY-135727
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EGFR
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Cancer
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PF-6422899 is an inhibitor for EGFR, that it selectively binds to EGFR and SOAT1 in nanomolar levels .
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- HY-P2138
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HIV Protease
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Others
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U-85548E is an HIV protease inhibitor with nanomolar affinity for HIV-1 aspartic protease. By studying its structure-activity relationship, a potent nanomolar inhibitor with inhibitory effects on both HIV-1 and HIV-2 proteases was designed, and its binding mode was studied by X-ray crystallography and molecular modeling.
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- HY-172586
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GSK-3
PKA
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Neurological Disease
Cancer
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GSK-3α/β-IN-1 is GSK-3α/β inhibitor with IC50 s of 0.265 μM and 0.255 μM for GSK-3α and GSK-3β, respectively. GSK-3α/β-IN-1 also inhibits PKA with an IC50 of 0.188 μM. GSK-3α/β-IN-1 potently inhibits cell viability of three Glioblastoma (GBM) cell lines (IC50 : 3-6 μM, 72 h) with no toxicity to human astrocytes and good metabolic stability. GSK-3α/β-IN-1 has potential CNS activity in all-human blood-brain barrier (BBB) model of GBM .
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- HY-18287
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Smo
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Cancer
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MRT-83 is a potent antagonist of Smo, with an IC50 in the nanomolar range. MRT-83 also blocks Hedgehog (Hh) signaling.
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- HY-139832
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PI3K
mTOR
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Cancer
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MCX 28, a triple PI3K/mTOR/PIM inhibitor, displays low nanomolar activity.
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- HY-132906
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Parasite
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Infection
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Antimalarial agent 3 shows nanomolar antiplasmodial activity (IC50 = 0.035 μM) and has a very high selectivity index with respect to mammalian cells.
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- HY-143465
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Cholinesterase (ChE)
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Neurological Disease
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BChE-IN-5 is a potent and selective BChE inhibitor of hBChE over hAChE with an IC50 of 2.8 nM for BChE. BChE-IN-5 has the potential for the research of alzheimer’s disease .
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- HY-141841
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SARS-CoV
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Infection
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SARS-CoV-2-IN-7 inhibits viral replication with a nanomolar IC50 value (844 nM) in SARS-CoV-2-infected Vero E6 cells.
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- HY-157551
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JNK
c-Met/HGFR
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Cancer
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JNK-IN-16 is a c-Met and JNK inhibitor with nanomolar potency, with IC50 values of 120 nM and 72 nM, respectively. JNK-IN-16 can be used for cancer research .
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- HY-169199
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MAP4K
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Cancer
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BAY-405 (compund 38) is a MAP4K1 inhibitor that exhibits nanomolar potency in biochemical and cellular assays and achieves in vivo exposure after oral administration .
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- HY-139631
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HIV
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Infection
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HIV-1 inhibitor-9 is found to be potent inhibitor against the wild-type (WT) HIV-1 strain or multiple NNRTI-resistant strains at low nanomolar levels.
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- HY-112080A
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Histone Methyltransferase
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Others
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(R)-BAY-6035 is a novel inhibitor that selectively targets the methylation of MAP3K2 by SMYD3, demonstrating nanomolar potency and specificity against kinases and other protein lysine methyltransferases.
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- HY-146441
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STAT
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Cardiovascular Disease
Inflammation/Immunology
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Prohibitin ligand 1 (Compound 22i), a cardioprotectant prohibitin ligand, induces a phosphorylation of the pro-survival factor STAT3. Prohibitin ligand 1 exhibits in vitro cardioprotectant activities at nanomolar concentrations .
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- HY-118096
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GABA Receptor
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Others
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AHN 070 is an irreversible peripheral benzodiazepine receptor (PBR) ligand. AHN 070 can bind to PBR with nanomolar affinity and is pH-dependent. AHN 070 can be used for studying the structure and function of PBR .
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- HY-145304
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- HY-119951
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Aurora Kinase
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Cancer
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AKI-001 is an prototype pentacyclic inhibitor of aurora kinase with cellular potency of IC50 of less than 100 nM. AKI-001 shows low nanomolar potency against Aurora A and Aurora B enzymes .
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- HY-156402
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Topoisomerase
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Cancer
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AuM1Gly is a topoisomerase I inhibitor. AuM1Gly affects the growth of MDA-MB-231 breast cancer cells, with IC50?values in the low nanomolar range .
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- HY-164005
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- HY-156175
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Toll-like Receptor (TLR)
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Inflammation/Immunology
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TLR7 agonist 14 (compound 17b) is a highly potent TLR7 agonist with an EC50 of 18 nM. TLR7 agonist 14 potently induces the activation of mouse macrophages and hPBMCs at low-nanomolar concentrations .
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- HY-W591307
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PROTAC Linkers
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Cancer
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P131 is a PROTAC molecule comprised of Pomalidomide-based cereblon ligand and IBT6A, linked by a PEG 3 chain. P131 can degrade both wild-type and C481S mutant BTK with nanomolar potencies.
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- HY-173022
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Aminopeptidase
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Others
|
|
BDM_92499 is a nanomolar selective IRAP inhibitor, with an IC50 of 3.4 nM. BDM_92499 also inhibits ERAP1 and ERAP2, with IC50 values of 0.46 μM and 4.2 μM, respectively .
|
-
- HY-119361
-
|
(Rac)-Deoxysappanone B 7,4' dimethyl ether
|
Microtubule/Tubulin
|
Cancer
|
|
(Rac)-Deox B 7,4, a homoisoflavanoid compound, inhibits microtubule polymerization via binding near the colchicine site and promote reversible G2 arrest. (Rac)-Deox B 7,4 possesses nanomolar anti-leukemic activity .
|
-
- HY-115555
-
|
|
Phosphodiesterase (PDE)
|
Cancer
|
|
K-Ras-PDEδ-IN-1 is a novel and potent competitive K-Ras-PDEδ inhibitor. K-Ras-PDEδ-IN-1 binds to the farnesyl binding pocket of PDEδ with a low nanomolar Kd of 8 nM .
|
-
- HY-155149
-
|
|
Methionine Adenosyltransferase (MAT)
|
Cancer
|
|
MAT2A Allosteric inhibitor 2 is a potent and selective MAT2A allosteric inhibitor with an IC50 of 5 nM. MAT2A Allosteric inhibitor 2 shows nanomolar activity (IC50=5 μM) in the the proliferation assay (MTAP -/- cell line) .
|
-
- HY-135845
-
|
CH0793011
|
Topoisomerase
|
Cancer
|
|
TP3011 (CH0793011) is an active metabolite of CH-0793076 and is a potent topoisomerase I inhibitor equipotent as SN38 . TP3011 is against cancer cell lines growth with IC50s at the range sub-nanomolar in vitro .
|
-
- HY-147724
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Compounds 17O (ic50= 14.0 nm, NCI-H460) and 17p (ic50= 2.9 nm, NCI-H460) and furan groups showed effective cytotoxic activity against various human cancer cell lines at the nanomolar level.
|
-
- HY-147728
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Compounds 17O (ic50= 14.0 nm, NCI-H460) and 17p (ic50= 2.9 nm, NCI-H460) and furan groups showed effective cytotoxic activity against various human cancer cell lines at the nanomolar level.
|
-
- HY-120757
-
|
|
Virus Protease
|
Others
|
|
LP-130 is a statin-based inhibitor that is a universal inhibitor with nanomolar inhibitory activity against all tested retroviral proteases. Crystal structure studies of its binding to different retroviral proteases have shown that it can adapt to different active site regions to achieve inhibition.
|
-
- HY-154854
-
|
|
Histone Methyltransferase
|
Cancer
|
|
BBDDL2059 is a selective covalent inhibitor of histone methyltransferase EZH2 with an IC50 of 1.5 nM for EZH2-Y641F. BBDDL2059 inhibits lymphoma cell growth at nanomolar concentrations and can be used for anticancer research .
|
-
- HY-163442A
-
|
|
Pim
|
Cancer
|
|
PIM3-IN-1 hydrochloride (Compound 19a) is an inhibitor of (PIM2/3), with the highest inhibition level being against PIM3, having an IC50 value in the nanomolar range. PIM3-IN-1 hydrochloride can be used in cancer research .
|
-
- HY-116042
-
|
|
Adenosine Receptor
|
Cardiovascular Disease
|
|
FSCPX is a potent and selective irreversible antagonist of A1 adenosine receptor (A1AR), with low nanomolar potency for binding to the A1AR. FSCPX could modify the effect of NBTI, a nucleoside transport inhibitor, by reducing the interstitial adenosine level in the guinea pig atrium .
|
-
- HY-149805
-
|
|
Apoptosis
|
Cancer
|
|
Anticancer agent 110 is an anticancer agent with in vitro anticancer activity and excellent anti-leukemia potency. Anticancer agent 110 is highly cytotoxic to K-562 lineage chronic myelogenous leukemia cells at nanomolar concentrations. Anticancer agent 110 causes DNA damage and leads to apoptosis .
|
-
- HY-12866R
-
|
LOXO-101 (Standard); ARRY-470 (Standard)
|
Reference Standards
Trk Receptor
Apoptosis
|
Cancer
|
|
Larotrectinib (Standard) is the analytical standard of Larotrectinib. This product is intended for research and analytical applications. Larotrectinib (LOXO-101) is an ATP-competitive oral, selective inhibitor of the tropomyosin-related kinase (TRK) family receptors, with low nanomolar 50% inhibitory concentrations against all three isoforms (TRKA, B, and C).
|
-
- HY-162763
-
|
|
Apoptosis
|
Cancer
|
|
FLQY2 is a camptothecin analog that exhibits outstanding antitumor efficacy against various solid tumors. FLQY2 possesses both in vitro and in vivo anti-pancreatic cancer activity, inhibiting cell proliferation, colony formation, inducing apoptosis, and causing cell cycle arrest at nanomolar concentrations .
|
-
- HY-139293
-
|
|
Others
|
Cardiovascular Disease
|
|
PF-07059013 is an orally active and potent noncovalent modulator of sickled hemoglobin (HbS). PF-07059013 specifically binds to Hb with nanomolar affinity and displays strong partitioning into red blood cells (RBCs). PF-07059013 can be used for sickle cell disease (SCD) research .
|
-
- HY-169185
-
|
|
Sigma Receptor
|
Cancer
|
|
Sigma-2 Radioligand 2 (compund 4) exhibits low nanomolar affinity (Ki(σ2)=2.30 nM) and high subtype selectivity (Ki(σ1)/Ki(σ2) > 1500) for the σ2 receptor .
|
-
- HY-101634AR
-
|
|
HCV
Reference Standards
|
Infection
|
|
ABT-072 (potassium trihydrate) (Standard) is the analytical standard of ABT-072 (potassium trihydrate) (HY-101634A). This product is intended for research and analytical applications. ABT-072 (potassium trihydrate) is an orally active and potent non-nucleoside HCV NS5B polymerase inhibitor (HCV GT1a EC50=1 nM; HCV GT1b EC50=0.3 nM) .
|
-
- HY-101634R
-
|
|
HCV
Reference Standards
|
Infection
|
|
ABT-072 (Standard) is the analytical standard of ABT-072 (HY-101634). This product is intended for research and analytical applications. ABT-072 is an orally active and potent non-nucleoside HCV NS5B polymerase inhibitor (HCV GT1a EC50=1 nM; HCV GT1b EC50=0.3 nM) .
|
-
- HY-156442
-
|
|
Lactate Dehydrogenase
|
Infection
|
|
MEDS433 is a potent inhibitor of human dihydroorotate dehydrogenase (hDHODH) with an IC50 of 1.2 nM. MEDS433 exerts a potent antiviral activity against RSV-A and RSV-B in the one-digit nanomolar range. MEDS433 induces the expression of antiviral proteins encoded by interferon stimulated genes (ISGs) able to reduce RSV replication .
|
-
- HY-19928A
-
|
EW-7197 Hydrochloride; TEW-7197 Hydrochloride
|
TGF-β Receptor
|
Cancer
|
|
Vactosertib Hydrochloride (EW-7197 Hydrochloride) is a potent, orally active and ATP-competitive activin receptor-like kinase 5 (ALK5) inhibitor with an IC50 of 12.9 nM. Vactosertib Hydrochloride also inhibits ALK2 and ALK4 (IC50 of 17.3 nM) at nanomolar concentrations. Vactosertib Hydrochloride has potently antimetastatic activity and anticancer effect .
|
-
- HY-124069
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
M-525 is a first-in-class, highly potent, irreversible and covalent menin-MLL protein-protein interaction inhibitor. M-525 binds to menin with an IC50 of 3 nM and achieves low nanomolar potencies in cell growth inhibition and in suppression of MLL regulated gene expression in MLL leukemia cells. Anti-leukemia activity .
|
-
- HY-122650
-
|
|
Autophagy
|
Cancer
|
|
PHY34 is an inhibitor that inhibits ATP6V0A2 and CAS thereby inhibiting autophagy, and has a nanomolar effect. PHY34 inhibits cancer cell growth by inducing apoptosis and inhibits tumor growth in xenograft models. PHY34 can be used for research on high grade serous ovarian cancer .
|
-
- HY-D2348
-
|
|
Fluorescent Dye
|
Infection
Others
|
|
ACE is a low-background, photostable fluorophore with nanomolar binding affinity for the Okra RNA aptamer. ACE enables clear visualization of mRNA in live bacteria and mammalian cells, including tracking the trafficking of mRNA to stress granules and dual-color super-resolution imaging of RNA in live cells. (Ex=488 nm, Em=555 nm) .
|
-
- HY-149292
-
|
|
Casein Kinase
|
Cancer
|
|
SR-4133 is a potent and highly CK1ε selective inhibitor with an IC50 of 58 nM. SR-4133 binds to the ATP-binding site of CK1ε. SR-4133 displays nanomolar growth inhibition of bladder cancer cells, and inhibits the phosphorylation of 4E-BP1 .
|
-
- HY-129334
-
|
|
Telomerase
|
Cancer
|
|
Macrocalin B is a diterpenoid, which can be isolated from Isodon xerophilus. Macrocalin B inhibits the proliferation of cancer cells K562, HL-60, A549, MKN, CA and HCT with IC50 of 2.81-171 μM. Macrocalin B inhibits the telomerase in K562 with an IC50 in nanomolar level .
|
-
- HY-P5914
-
|
WaTx
|
TRP Channel
|
Neurological Disease
|
|
Wasabi Receptor Toxin is a cell-penetrating scorpion toxin. Wasabi Receptor Toxin is the activator for TRPA1 ion channel with EC50 in nanomolar level, and prolongs the channel open time, but reduces Ca 2+ permeability. Wasabi Receptor Toxin causes thermal hypersensitivity and mechanical allodynia in rats, without triggering neurogenic inflammation .
|
-
- HY-170420
-
|
|
JNK
|
Others
|
|
JNK-1-IN-5 (Compound 14) is a potent JNK1 inhibitor with sub-nanomolar efficacy. JNK-1-IN-5 suppresses TGF-β-induced epithelial-mesenchymal transition. JNK-1-IN-5 is promising for research of anti-pulmonary fibrosis agent targeting JNK1 .
|
-
- HY-19928
-
|
EW-7197; TEW-7197
|
TGF-β Receptor
|
Cancer
|
|
Vactosertib (EW-7197) is a potent, orally active and ATP-competitive activin receptor-like kinase 5 (ALK5) inhibitor with an IC50 of 12.9 nM. Vactosertib also inhibits ALK2 and ALK4 (IC50 of 17.3 nM) at nanomolar concentrations. Vactosertib has potently antimetastatic activity and anticancer effect .
|
-
- HY-130492
-
ARCC-4
3 Publications Verification
|
PROTACs
Androgen Receptor
|
Cancer
|
|
ARCC-4 is a low-nanomolar Androgen Receptor (AR) degrader based on PROTAC, with a DC50 of 5?nM. ARCC-4 is an enzalutamide-based von Hippel-Lindau (VHL)-recruiting AR PROTAC and outperforms enzalutamide. ARCC-4 effectively degrades clinically relevant AR mutants associated with antiandrogen therapy .
|
-
- HY-147663
-
|
|
Carbonic Anhydrase
|
Cancer
|
|
Compounds 6b and 14g showed significant inhibitory effect on tumor related subtype HCA IX with low nanomolar potency, while 6k was effective on HCA XII. Compounds 6b, 14g and 6k can be considered as the leading molecules for the development of future cancer therapeutic drugs based on new mechanisms of action.
|
-
- HY-D2348A
-
|
|
Fluorescent Dye
|
Infection
|
|
ACE TFA is a low-background, photostable fluorophore with nanomolar binding affinity for the Okra RNA aptamer. ACE TFA enables clear visualization of mRNA in live bacteria and mammalian cells, including tracking the trafficking of mRNA to stress granules and dual-color super-resolution imaging of RNA in live cells. (Ex=488 nm, Em=555 nm) .
|
-
- HY-163537
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
AChE/BuChE-IN-5 (compound 5a) is a dual target inhibitor. AChE/BuChE-IN-5 has excellent nanomolar inhibitory activity on acetylcholinesterase (AChE) (IC50=46.9 nM) and butyryl cholinesterase (BuChE) (IC50=3.5 nM). AChE/BuChE-IN-5 can be used for Alzheimer's Disease research .
|
-
- HY-157416
-
|
|
ATGL
E1/E2/E3 Enzyme
|
Metabolic Disease
|
|
COP1-ATGL modulator 1 (86) is an orally active modulator for COP1-ATGL axis. COP1-ATGL modulator 1 (86) could increase ATGL protein expression, reduce ATGL ubiquitination and COP1 autoubiquitination, and diminish lipid accumulation in hepatocytes in the nanomolar range .
|
-
- HY-161768
-
|
|
CDK
Apoptosis
|
Cancer
|
|
VCC972839:01 is an inhibitor for cyclin dependent kinase (CDK9), with IC50 of 7 nM. VCC972839:01 inhibits the cell viability of SCLC cells in nanomolar levels. VCC972839:01 induces apoptosis through an intrinsic pathway. VCC972839:01 exhibits antitumor activity in mouse model .
|
-
- HY-10293
-
|
INCB007839; INCB7839
|
MMP
|
Cancer
|
|
Aderbasib (INCB007839) is a potent, orally active and target specific low nanomolar hydroxamate-based inhibitor of ADAM10 and ADAM17. Aderbasib exhibits robust antineoplastic activity and can be used for cancer research, including diffuse large B-cell non-Hodgkin lymphoma, HER2 + breast cancer, gliomas, et al .
|
-
- HY-153333
-
|
|
Adenosine Receptor
|
Cardiovascular Disease
|
|
A1/A3 AR antagonist 3 is an A1R/A3R dual antagonist with high affinity at low-micromolar to low-nanomolar. A1/A3 AR antagonist 3 can be used for the research of chronic heart diseases .
|
-
- HY-103247B
-
|
|
Angiotensin Receptor
|
Cardiovascular Disease
|
|
EMD-66684 potassium salt is a non-peptide angiotensin II receptor antagonist that demonstrates significant antihypertensive effects in spontaneously hypertensive rats. EMD-66684 potassium salt exhibits nanomolar affinity for angiotensin II receptors, comparable to losartan in potency. EMD-66684 potassium salt shows increased activity when modified with acetamides, leading to superior blood pressure reduction.
|
-
- HY-149928
-
|
|
HIV
|
Infection
|
|
NNRT-IN-1 (compound 8r) is a potent non-nucleoside reverse transcriptase (NNRT) inhibitor featuring significantly anti-resistance efficacy. NNRT-IN-1 inhibits the wild-type HIV-1 and five mutant strains with EC50s in the nanomolar range. NNRT-IN-1 displays favorable pharmacokinetic properties .
|
-
- HY-175845
-
|
|
Src
Apoptosis
Reactive Oxygen Species (ROS)
|
Cancer
|
|
Scr-IN-2 is an effective c-Scr inhibitor with an IC50 of 302 nM. Scr-IN-2 exhibits nanomolar-level anti-breast cancer activity. Scr-IN-2 increases the level of ROS in cells, induces mitochondrial damage, G1 phase arrest, and apoptosis. Scr-IN-2 can be used in the research of breast cancer .
|
-
- HY-145733
-
|
|
E1/E2/E3 Enzyme
|
Cardiovascular Disease
|
|
DI-1859 is a potent, selective and covalent inhibitor of DCN1. DI-1859 inhibits neddylation of cullin 3 in cells at low nanomolar concentrations. DI-1859 induces a robust increase of NRF2 protein, a CRL3 substrate, in mouse liver and effectively protects mice from acetaminophen-induced liver damage .
|
-
- HY-100233A
-
|
|
JNK
|
Inflammation/Immunology
Cancer
|
|
IQ-1S is a prospective inhibitor of NF-κB/activating protein 1 (AP-1) activity with an IC50 of 1.8 μM. IQ-1 has binding affinity (Kd values) in the nanomolar range for all three JNKs with Kds of 87 nM, 360 nM, and 390 nM for JNK3, JNK2, and JNK1, respectively.
|
-
- HY-139855
-
|
|
HIF/HIF Prolyl-Hydroxylase
|
Metabolic Disease
|
|
ZG-2033 (Compound 26) is an orally active HIF-2α agonist that demonstrates nanomolar activity in luciferase reporter gene assays (EC50 = 490 nM). ZG-2033 has the effect of alleviating anemia and exhibits synergistic action with AKB-6548 (HY-101277) in anemia, and can be used in the study of renal anemia .
|
-
- HY-156406
-
|
|
PI3K
|
Inflammation/Immunology
|
|
PITCOIN4 is a highly selective Class II Alpha PI3K-C2α inhibitor. PITCOIN4 shows nanomolar inhibition of PI3K-C2α and >100-fold selectivity in a general kinase panel .
|
-
- HY-182705
-
|
|
Estrogen Receptor/ERR
|
Endocrinology
|
|
Org 214444-0 is an orally active, nanomolar-potent and selective FSHR agonist, with EC50 values of 2.0 nM and 1.2 nM in human and rat (measured in CHO cells). Org 214444-0 activates human granulosa cells in vitro, supports rat follicular development and induces ovulation in vivo. Org 214444-0 can be used for the research of infertility .
|
-
- HY-14891
-
|
GSK2248761; FDV
|
HIV
Reverse Transcriptase
|
Infection
|
|
Fosdevirine (GSK2248761) is is a potent, selective, non-nucleoside reverse transcriptase inhibitor (NNRTI) of human immunodeficiency virus type 1 (HIV-1) replication with low nanomolar activity in vitro. Fosdevirine shows good activity against a broad range of HIV-1 strains, including efavirenz (HY-10572)-resistant clinical isolates .
|
-
- HY-12866AR
-
|
LOXO-101 sulfate (Standard); ARRY-470 sulfate (Standard)
|
Trk Receptor
Apoptosis
Reference Standards
|
Cancer
|
|
Larotrectinib sulfate (Standard) is the analytical standard of Larotrectinib sulfate. This product is intended for research and analytical applications. Larotrectinib sulfate (LOXO-101 sulfate; ARRY-470 sulfate) is an ATP-competitive oral, selective inhibitor of the tropomyosin-related kinase (TRK) family receptors, with low nanomolar 50% inhibitory concentrations against all three isoforms (TRKA, B, and C).
|
-
- HY-131904
-
POMHEX
3 Publications Verification
|
Enolase
Apoptosis
|
Metabolic Disease
Cancer
|
|
POMHEX, a racemic mixture and a cell-permeable pivaloyloxymethyl (POM) proagent of HEX, is a potent, ENO2-specific inhibitor of enolase. POMHEX exhibits low-nanomolar potency against ENO1-deleted cells in vitro and is capable of eradicating ENO1-deleted xenografted tumours in vivo. POMHEX is a potent glycolysis inhibitor .
|
-
- HY-171249
-
|
|
TGF-β Receptor
|
Cardiovascular Disease
Endocrinology
|
|
CDD-1431 is a low-nanomolar selective kinase inhibitors of BMPR2, with Kiapp value of 20.6 nM. CDD-1431 suppresses BRE-reporter activity, with an IC50 of 4.87 μM. BMP controls cellular processes across many tissue types, including the kidney, skeletal muscle, heart, and reproductive organs. BMP induces ectopic bone formation .
|
-
- HY-106100
-
|
EMD 49980
|
Dopamine Receptor
Serotonin Transporter
|
Neurological Disease
|
|
Roxindole (EMD 49980), an indot-alkyl-pipenidine, is a potent agonist at dopamine autoreceptors, with an affinity for the D2-like subtype in the low nanomolar range. Roxindole can be used for the research of positive and negative schizophrenic symptoms. Roxindole is a 5-HT1A agonist and 5-HT uptake inhibitor. Antipsychotic and antidepressant activities .
|
-
- HY-181169
-
|
|
Cyclin G-associated Kinase (GAK)
|
Cancer
|
|
GAK-IN-3 is a cyclin G-associated kinase (GAK) inhibitor with an IC50 of 207 nM and a Ki of 66 nM. GAK-IN-3 inhibits kinase activity in the nanomolar range by binding to GAK’s ATP-binding site. GAK-IN-3 acts as a cytotoxic agent that reduces viability of Ewing sarcoma cells. GAK-IN-3 can be used for the research of ewing sarcoma .
|
-
- HY-183747
-
|
|
Parasite
|
Infection
|
|
Antitrypanosomal agent 32 is a antitrypanosomal agent with nanomolar potency against multiple Trypanosoma cruzi strains, including CL-Brener, Y, Dm28c-Luc and Tulahuen. Antitrypanosomal agent 32 sustains inhibition of parasite growth after washing and reduces parasitemia levels in BALB/c mice. Antitrypanosomal agent 32 can be used for the research of trypanosome infection .
|
-
- HY-P99294
-
|
AMG 479; Human Anti-IGF1R Recombinant Antibody
|
IGF-1R
|
Cancer
|
|
Ganitumab (AMG 479) is a recombinant human monoclonal antibody to the human type 1 insulin-like growth factor receptor (IGF1R). Ganitumab recognizes murine IGF1R with sub-nanomolar affinity (KD=0.22 nM) and inhibits the interaction of murine IGF1R with IGF1 and IGF2. Ganitumab can be used in research of cancer .
|
-
- HY-144368
-
|
|
TNF Receptor
|
Inflammation/Immunology
|
|
CO delivery molecule 1 (compound 4) localizes to the endoplasmic reticulum, mitochondria, and lysosomes. Subcellular localization of CO delivery molecule 1 results in CO-induced toxicity effects. Anti-inflammatory effects of CO delivery molecule 1, as measured by TNF-α suppression, occur at the nanomolar level in the absence of CO release, and are enhanced with visible-light-induced CO release .
|
-
- HY-W1117786
-
|
|
ADC Payload
NAMPT
|
Cancer
|
|
Nampt-IN-10 (Compound 4) is an efficient inhibitor of nicotinamide phosphoribosyltransferase (NAMPT). Nampt-IN-10 exhibits nanomolar-level inhibitory activity against cell lines such as MDA-MB453, NCI-N87, and NCI-H526. Nampt-IN-10 can be used as an ADC payload, and the ADC constructed with it as the core demonstrates significant anti-tumor activity .
|
-
- HY-100233
-
|
|
JNK
|
Inflammation/Immunology
Cancer
|
|
IQ-1S free acid is a prospective inhibitor of NF-κB/activating protein 1 (AP-1) activity with an IC50 of 2.3±0.41 μM. IQ-1S free acid has binding affinity (Kd values) in the nanomolar range for all three JNKs with Kds of 100 nM, 240 nM, and 360 nM for JNK3, JNK1, and JNK2, respectively.
|
-
- HY-130622
-
LT052
1 Publications Verification
|
Epigenetic Reader Domain
|
Inflammation/Immunology
|
|
LT052 is a highly selective BET BD1 inhibitor with an IC50 of 87.7 nM. LT052 exhibits nanomolar BRD4 BD1 potency and 138-fold selectivity over BRD4 BD2 (IC50=12.130 μM). LT052 has anti-inflammatory?activity and can be used for acute gout arthritis research .
|
-
- HY-19925
-
|
|
HIV
|
Infection
|
|
AIC-292 is a potent and selective inhibitor of HIV-1 nonnucleoside reverse transcriptase. AIC-292 inhibits wild-type HIV-1 laboratory strains at low nanomolar concentrations. AIC-292 displays potent antiviral in vivo efficacy in a mouse xenograft model. AIC-292 has the potential for the research of HIV-1 infection .
|
-
- HY-P2274R
-
|
|
Reference Standards
Parasite
|
Infection
|
|
Argifin (Standard) is the analytical standard of Argifin. This product is intended for research and analytical applications. Argifin is a sub-nanomolar chitinase inhibitor produced by soil microorganisms, with IC50s of 0.025 μM, 6.4 μM , 1.1 μM and 4.5 μM for SmChiA (Serratia marcescens chitinaese A), SmChiB, Aspergillus fumigatus chitinase B1 and human chitotriosidase, respectively[1].
|
-
- HY-116218
-
|
JPI-289 free base
|
PARP
|
Cardiovascular Disease
Neurological Disease
|
|
Amelparib (JPI-289 free base) is a potent, orally active, and water-soluble inhibitor of PARP-1. Amelparib inhibits PARP-1 activity (IC50=18.5 nM) and cellular PAR formation (IC50=10.7 nM) in the nanomolar range. Amelparib is a potential neuroprotective agent. Amelparib has the potential for the research of acute ischaemic stroke .
|
-
- HY-12284
-
|
|
Prostaglandin Receptor
|
Inflammation/Immunology
|
|
NVP-QAV680 is a potent and selective CRTh2 receptor antagonist with low nanomolar (nM) functional potency to inhibit CRTh2-driven activation of human eosinophils and Th2 lymphocytes. NVP-QAV680 exhibits good oral bioavailability and demonstrates efficacy in CRTh2-dependent mechanisms and allergic disease models in rats .
|
-
- HY-14778
-
|
GSK 221149; GSK 221149A
|
Oxytocin Receptor
|
Neurological Disease
Endocrinology
|
|
Retosiban (GSK221149A) is a potent, selective, and orally active oxytocin receptor antagonist (Ki (hOT) = 0.65 nM, Ki (rOT) = 4.1 nM) with no detectable agonist activity. Retosiban has nanomolar affinity for the oxytocin receptor with >1400-fold selectivity over the closely related vasopressin receptors. Retosiban inhibits spontaneous and induces uterine contractions. Retosiban can be studied in research for preterm labour .
|
-
- HY-119733
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
BU09059 is a potent and selective Kappa-opioid receptor antagonist with a pA2 of 8.62. BU09059 has nanomolar affinity for the κ-receptor, with 15-fold and 616-fold selectivity over μ- and δ-receptors, respectively. BU09059 significantly blocks U50488 (HY-15997B)-induced antinociception .
|
-
- HY-122229
-
|
|
HIV
|
Infection
|
|
GS-9822 is a potent antivira agent with nanomolar activity against wild-type HIV-1 viruses. GS-9822 potently inhibits the LEDGF/p75-integrase interaction with an IC50 of 0.07 μM. GS-9822 has high in vitro metabolic stability and favorable oral pharmacokinetic profiles with low systemic clearance in rats, dogs, and monkeys .
|
-
- HY-173521
-
|
|
SARS-CoV
DNA/RNA Synthesis
Virus Protease
|
Infection
|
|
JNJ-9676 is an orally active Coronavirus M protein inhibitor and selective Sarbecovirus inhibitor. JNJ-9676 binds to the M protein dimer and forces the protein into an alternative conformational state with a compound-induced binding pocket. JNJ-9676 demonstrates in vitro nanomolar antiviral activity against SARS-CoV-2, SARS-CoV and Sarbecovirus strains from bat and pangolin zoonotic origin .
|
-
- HY-19509R
-
|
|
Reverse Transcriptase
HIV
|
Infection
|
|
IQP-0528 (Standard) is the analytical standard of IQP-0528. This product is intended for research and analytical applications. IQP-0528 is a highly potent nonnucleoside reverse transcriptase inhibitor (NNRTI). IQP-0528 shows nanomolar activity against both HIV-1 and HIV-2, with an HIV-1 EC50 of 0.2 nM and an HIV-2 EC50 of 100 nM .
|
-
- HY-155028
-
|
|
FGFR
|
Cancer
|
|
FGFR-IN-11 (compound I-5) is an orally active and covalent FGFR inhibitor with IC50 values of 9.9 nM (FGFR1), 3.1 nM (FGFR2), 16 nM (FGFR3), and 1.8 nM (FGFR4), respectively. FGFR-IN-11 inhibits multiple cancer cell proliferation with nanomolar activity. FGFR-IN-11 inhibits tumor growth significantly in xenograft mice models .
|
-
- HY-103110
-
ST1936
1 Publications Verification
|
5-HT Receptor
Adrenergic Receptor
|
Neurological Disease
|
|
ST1936 is a selective, nanomolar affinity 5-HT6 receptor agonist with Ki values of 13 nM, 168 nM and 245 nM for human 5-HT6, 5-HT7 and 5-HT2B receptors, respectively. ST1936 also shows moderate affinity (Ki of 300 nM) for human and rat α2 adrenergic receptor .
|
-
- HY-103110A
-
|
|
5-HT Receptor
Adrenergic Receptor
|
Neurological Disease
|
|
ST1936 oxalate is a selective, nanomolar affinity 5-HT6 receptor agonist with Ki values of 13 nM, 168 nM and 245 nM for human 5-HT6, 5-HT7 and 5-HT2B receptors, respectively. ST1936 oxalate also shows moderate affinity (Ki of 300 nM) for human and rat α2 adrenergic receptor .
|
-
- HY-128128
-
|
|
Transmembrane Glycoprotein
|
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
|
|
ASN04421891 is a GPR17 agonist with nanomolar EC50 and high specificity. ASN04421891 promotes oligodendrocyte precursor cell maturation to mature myelinating oligodendrocytes. ASN04421891 can be used for the research of cerebral ischaemia, cardiac ischaemia, renal ischaemia, cerebral trauma, multiple sclerosis, schizophrenia, depression, alzheimer's disease, alzheimer-like dementia, parkinson's disease, huntington's chorea, amyotrophic lateral sclerosis (ALS), neuroinflammatory disorders .
|
-
- HY-139874
-
|
|
CXCR
|
Inflammation/Immunology
Cancer
|
|
CXCR2 antagonist 3 (compound 11h) is a potent antagonist of CXC chemokine receptor 2 (CXCR2). CXCR2 antagonist 3 demonstrates double-digit nanomolar potencies against CXCR2 and significantly inhibited neutrophil infiltration into the air pouch. CXCR2 antagonist 3 reduces the infiltration of neutrophils and MDSCs and enhance the infiltration of CD3 + T lymphocytes into the Pan02 tumor tissues .
|
-
- HY-108350
-
MI-2-2
1 Publications Verification
|
Epigenetic Reader Domain
|
Cancer
|
|
MI-2-2 is a potent menin-MLL inhibitor. MI-2-2 binds to menin with low nanomolar affinity (Kd=22nM) and very effectively disrupts the bivalent protein-protein interaction between menin and MLL. MI-2-2 has specific and very pronounced activity in MLL leukemia cells, including inhibition of cell proliferation, down-regulation of Hoxa9 expression, and differentiation .
|
-
- HY-158439
-
|
|
JAK
STAT
|
Cancer
|
|
anti-TNBC agent-7 (Compound 13c) possesses anticancer activity, serving as a molecular probe to recognize and regulate the signal transduction of the USP21/JAK2/STAT3 axis, exhibiting nanomolar-level cytotoxicity against MDA-MB-231 and HCC-1806 cancer cells, effectively combating triple-negative breast cancer (TNBC) .
|
-
- HY-12928
-
|
|
Virus Protease
|
Infection
|
|
ML336 is quinazolinone-based inhibitor against venezuelan equine encephalitis virus (VEEV), with IC50s of 32, 20, and 42 nM for VEEV TC-83 CPE , VEEV V3526 CPE, VEEV Wild Type CPE, respectively. ML336 potently inhibits a VEEV-induced cytopathic effect in three strains of the virus (TC-83, V3526, and wild type Trinidad donkey) in the low nanomolar range .
|
-
- HY-108988
-
|
|
Antibiotic
Bacterial
Topoisomerase
DNA/RNA Synthesis
|
Infection
|
|
Albicidin is a peptide antibiotic with phytotoxic activity. Albicidin potently inhibits bacterial and plant DNA gyrase at nanomolar concentrations, blocks DNA replication, and exhibits excellent antibacterial efficacy against multidrug-resistant bacteria. Albicidin possesses bactericidal activity against Gram-positive and Gram-negative microorganisms, and acts as a virulence factor for the systemic plant infection by Xanthomonas albilineans. Albicidin can be used in studies related to bacterial infections and sugarcane leaf blight .
|
-
- HY-137464A
-
OATD-01
1 Publications Verification
|
Glycosidase
|
Inflammation/Immunology
|
|
OATD-01 is a highly potent, first-in-class, orally active and selective chitinase inhibitor with low nanomolar activity toward CHIT1 (hCHIT1,IC50=23 nM). OATD-01 shows excellect PK profile in multiple species and is selectivity against a panel of other off-targets. OATD-01 exhibits significant antifibrotic efficacy in vivo and can be used for pulmonary fibrosis (IPF) research .
|
-
- HY-162568
-
|
|
DNA Stain
|
Cancer
|
|
7-tert-Butylfascaplysin (7-TB) is a derivative of Fascaplysin (HY-112328), that can be isolated from Fascaplysinopsis sp.. 7-tert-Butylfascaplysin induces replication stress, leads to toxic DNA double-strand breaks and apoptosis-like cell death, and thus exhibits cytotoxicity in cancer cells in nanomolar levels. 7-tert-Butylfascaplysin exhibits DNA intercalating activity with EC50 of 3.2 μM .
|
-
- HY-P11224
-
|
|
DNA/RNA Synthesis
|
Cancer
|
RMI-L4 is an efficient cyclic peptide inhibitor that can specifically disrupt the interaction between FANCM and RMI proteins with an IC50 of 54 nM. RMI-L4 engages the FANCM-binding pocket of RMI1/2 with nanomolar affinity (KD = 2.5 nM). RMI-L4 cannot penetrate the cell membrane and can be used to study the FANCM-RMI pathway targeting cancer with alternate lengthening of telomeres (ALT) .
|
-
- HY-P991734
-
|
|
TREM receptor
Syk
Calcium Channel
|
Neurological Disease
Inflammation/Immunology
|
|
VHB937 is a potent and selective TREM2 agonist, a human monoclonal antibody, with sub-nanomolar affinity. VHB937 enhances TREM2 surface expression and downstream signaling, such as Syk phosphorylation and calcium mobilization. VHB937 exhibits robust neuroprotective effects in vivo, significantly reducing pathology and pro-inflammatory markers across a broad range of animal models of neuroinflammation and neurodegeneration. VHB937 can be used for neurodegenerative diseases research .
|
-
- HY-182390
-
|
|
Ferroptosis
Reactive Oxygen Species (ROS)
Keap1-Nrf2
|
Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
|
|
Ferroptosis-IN-24 is a non-classical ferroptosis inhibitor capable of crossing the blood-brain barrier, with nanomolar inhibitory activity against ferroptosis induced by RSL3 (HY-100218A) and Erastin (HY-15763). Ferroptosis-IN-24 alleviates oxidative stress, reduces lipid peroxidation accumulation, and restores redox homeostasis. Ferroptosis-IN-24 is applicable to research related to cerebral ischemia-reperfusion injury and acute liver injury .
|
-
- HY-139590
-
|
BOS-172738; DS-5010
|
RET
PDGFR
|
Cancer
|
|
Zeteletinib (BOS-172738; DS-5010) is an orally active, selective RET kinase inhibitor with nanomolar potency against RET and >300-fold selectivity against VEGFR2. Zeteletinib shows exquisite potency for the wild type RET, RET V804M/L gatekeeper mutants, and the most common oncogenic RET mutation M918T. Zeteletinib has potent antitumor activity .
|
-
- HY-135581
-
|
|
Estrogen Receptor/ERR
|
Endocrinology
|
|
Raloxifene 6-glucuronide is a primary metabolite of Raloxifene. Raloxifene 6-glucuronide is mediated mostly by UGT1A1 and UGT1A8. Raloxifene 6-glucuronide binds to estrogen receptor with an IC50 of 290 μM. Raloxifene is a selective and nonsteroidal estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression .
|
-
- HY-145561
-
|
BLD-0409; PAT-409
|
Phosphodiesterase (PDE)
LPL Receptor
|
Inflammation/Immunology
Cancer
|
|
Cudetaxestat (BLD-0409; PAT-409) is an orally active and noncompetitive autotaxin (ATX) inhibitor. Cudetaxestat inhibits the activity of ATX, reduces the production of LPA, and thereby blocks the signal transduction of the ATX-LPA axis. Cudetaxestat can still maintain nanomolar-level biochemical efficacy even when the concentration of the LPC substrate increases. Cudetaxestat can be used for the study of various diseases related to LPA including fibrosis, tumor metastasis, inflammation and autoimmune diseases, etc .
|
-
- HY-139590A
-
|
BOS-172738 hemiadipate; DS-5010 hemiadipate
|
RET
PDGFR
|
Cancer
|
|
Zeteletinib (BOS-172738; DS-5010) hemiadipate is an orally active, selective RET kinase inhibitor with nanomolar potency against RET and >300-fold selectivity against VEGFR2. Zeteletinib hemiadipate shows exquisite potency for the wild type RET, RET V804M/L gatekeeper mutants, and the most common oncogenic RET mutation M918T. Zeteletinib hemiadipate has potent antitumor activity .
|
-
- HY-135495
-
|
|
Sodium Channel
Histamine Receptor
|
Inflammation/Immunology
|
|
AM-0466 is a sodium channel inhibitor with nanomolar levels of NaV1.7 inhibitory activity. AM-0466 exhibits potent pharmacodynamic activity in a NaV1.7-dependent histamine-induced itch model. AM-0466 also showed significant analgesic effects in capsaicin-induced pain models. After optimizing its pharmacokinetic properties, AM-0466 was advanced into in vivo targeting and efficacy models for testing .
|
-
- HY-172210
-
|
|
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
|
DDO-8958 is an orally active and selective BET BD1 inhibitor with a KD of 5.6 nM for BRD4 BD1. DDO-8958 exhibits low nanomolar inhibitory activity against all BET BD1 bromodomains except for BRDT BD1. DDO-8958 can inhibit the proliferation and migration, induce apoptosis and cell cycle arrest of tumor cells. DDO-8958 has anti-tumor activity .
|
-
- HY-N7049
-
|
|
ADC Payload
Microtubule/Tubulin
|
Cancer
|
|
Tubulysin F is a highly cytotoxic anti-microtubule toxin (anti-microtubule toxins) that is synthesized as an ADC cytotoxin (ADC Cytotoxin). Tubulysin F can be isolated from the myxobacteria Archangium geophyra and Angiococcus disciformis. Tubulysin F displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the low nanomolar range. Tubulysin F inhibits microtubule/Tubulin polymerization and leads to cell cycle arrest and apoptosis .
|
-
- HY-N7052
-
|
|
ADC Payload
Microtubule/Tubulin
|
Cancer
|
|
Tubulysin I is a highly cytotoxic anti-microtubule toxin (anti-microtubule toxins) that is synthesized as an ADC cytotoxin (ADC Cytotoxin). Tubulysin I can be isolated from the myxobacteria Archangium geophyra and Angiococcus disciformis. Tubulysin I displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the low nanomolar range. Tubulysin I inhibits microtubule/tubulin polymerization and leads to cell cycle arrest and apoptosis .
|
-
- HY-N7053
-
|
|
ADC Payload
Microtubule/Tubulin
|
Cancer
|
|
Tubulysin M is a highly cytotoxic anti-microtubule toxin (anti-microtubule toxins) that is synthesized as an ADC cytotoxin (ADC Cytotoxin). Tubulysin M can be isolated from the myxobacteria Archangium geophyra and Angiococcus disciformis. Tubulysin M displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the low nanomolar range. Tubulysin M inhibits microtubule/tubulin polymerization and leads to cell cycle arrest and apoptosis .
|
-
- HY-P5914A
-
|
WaTx TFA
|
TRP Channel
|
Neurological Disease
|
|
Wasabi Receptor Toxin TFA (WaTx TFA) is the TFA salt form of Wasabi Receptor Toxin (HY-P5914). Wasabi Receptor Toxin TFA is a cell-penetrating scorpion toxin. Wasabi Receptor Toxin TFA is the activator for TRPA1 ion channel with EC50 in nanomolar level, and prolongs the channel open time, but reduces Ca 2+ permeability. Wasabi Receptor Toxin TFA causes thermal hypersensitivity and mechanical allodynia in rats, without triggering neurogenic inflammation .
|
-
- HY-10293R
-
|
INCB007839 (Standard); INCB7839 (Standard)
|
Reference Standards
MMP
|
Cancer
|
|
Aderbasib (Standard) is the analytical standard of Aderbasib (HY-10293). This product is intended for research and analytical applications. Aderbasib (INCB007839) is a potent, orally active and target specific low nanomolar hydroxamate-based inhibitor of ADAM10 and ADAM17. Aderbasib exhibits robust antineoplastic activity and can be used for cancer research, including diffuse large B-cell non-Hodgkin lymphoma, HER2+ breast cancer, gliomas, et al .
|
-
- HY-N7050
-
|
|
ADC Payload
Microtubule/Tubulin
|
Cancer
|
|
Tubulysin G is a highly cytotoxic anti-microtubule toxin (anti-microtubule toxins) that is synthesized as an ADC cytotoxin (ADC Cytotoxin). Tubulysin G can be isolated from the myxobacteria Archangium geophyra and Angiococcus disciformis. Tubulysin G displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the low nanomolar range. Tubulysin G inhibits microtubule/tubulin polymerization and leads to cell cycle arrest and apoptosis .
|
-
- HY-N2348
-
|
|
ADC Payload
Microtubule/Tubulin
|
Cancer
|
|
Tubulysin D is a highly cytotoxic anti-microtubule toxin (anti-microtubule toxins) that is synthesized as an ADC cytotoxin (ADC Cytotoxin). Tubulysin D can be isolated from the myxobacteria Archangium geophyra and Angiococcus disciformis. Tubulysin D displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the low nanomolar range. Tubulysin D inhibits microtubule/Tubulin polymerization and leads to cell cycle arrest and apoptosis .
|
-
- HY-139602
-
|
|
Flavivirus
Dengue Virus
Virus Protease
|
Infection
|
|
(+)-JNJ-A07 is a highly potent, orally active pan-serotype dengue virus inhibitor targeting the NS3-NS4B interaction. (+)-JNJ-A07 exerts nanomolar to picomolar activity against a panel of 21 clinical isolates. (+)-JNJ-A07 has a favourable pharmacokinetic profile that results in outstanding efficacy against dengue virus infection in mouse infection models .
|
-
- HY-N2346
-
|
|
ADC Payload
Microtubule/Tubulin
|
Cancer
|
|
Tubulysin E is a highly cytotoxic anti-microtubule toxin (anti-microtubule toxins) that is synthesized as an ADC cytotoxin (ADC Cytotoxin). Tubulysin E can be isolated from the myxobacteria Archangium geophyra and Angiococcus disciformis. Tubulysin E displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the low nanomolar range. Tubulysin E inhibits microtubule/Tubulin polymerization and leads to cell cycle arrest and apoptosis .
|
-
- HY-N2347
-
|
|
ADC Payload
Microtubule/Tubulin
|
Cancer
|
|
Tubulysin C is a highly cytotoxic anti-microtubule toxin (anti-microtubule toxins) that is synthesized as an ADC cytotoxin (ADC Cytotoxin). Tubulysin C can be isolated from the myxobacteria Archangium geophyra and Angiococcus disciformis. Tubulysin C displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the low nanomolar range. Tubulysin C inhibits microtubule/Tubulin polymerization and leads to cell cycle arrest and apoptosis .
|
-
- HY-W703549
-
|
INCB007839-d3; INCB7839-d3
|
Isotope-Labeled Compounds
MMP
|
Cancer
|
|
Aderbasib-d3 (INCB007839-d3) is deuterium labeled Aderbasib. Aderbasib (INCB007839) is a potent, orally active and target specific low nanomolar hydroxamate-based inhibitor of ADAM10 and ADAM17. Aderbasib exhibits robust antineoplastic activity and can be used for cancer research, including diffuse large B-cell non-Hodgkin lymphoma, HER2 +?breast cancer, gliomas, et al .
|
-
- HY-N7051
-
|
|
ADC Payload
Microtubule/Tubulin
|
Cancer
|
|
Tubulysin H is a highly cytotoxic anti-microtubule toxin (anti-microtubule toxins) that is synthesized as an ADC cytotoxin (ADC Cytotoxin). Tubulysin H can be isolated from the myxobacteria Archangium geophyra and Angiococcus disciformis. Tubulysin H displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the low nanomolar range. Tubulysin H inhibits microtubule/tubulin polymerization and leads to cell cycle arrest and apoptosis .
|
-
- HY-135276
-
|
|
MicroRNA
Apoptosis
|
Cancer
|
|
Targaprimir-96 is a potent inhibitor of microRNA-96 (miR-96) processing. Targaprimir-96 selectively modulates miR-96 production in cancer cells and triggers apoptosis. Targaprimir-96 binds primary miR-96 (pri-miR-96) with low nanomolar affinity. Targaprimir-96 directly engages pri-miR-96 in breast cancer cells and is ineffective on healthy breast cells .
|
-
- HY-136927
-
|
|
STING
|
Inflammation/Immunology
Cancer
|
|
MSA-2, a potent and orally available non-nucleotide STING agonist, is bound to STING as a noncovalent dimer with nanomolar affinity. MSA-2 shows EC50s of 8.3 and 24 μM for human STING isoforms WT and HAQ, respectively. MSA-2 stimulates interferon-β secretion in tumors, induces tumor regression with durable antitumor immunity, and synergizes with anti-PD-1 in syngeneic mouse tumor models .
|
-
- HY-135582
-
|
|
Estrogen Receptor/ERR
|
Endocrinology
|
|
Raloxifene 4'-glucuronide is a primary metabolite of Raloxifene. Raloxifene 4'-glucuronide formation is mediated mostly by UGT1A10 and UGT1A8. Raloxifene 4'-glucuronide binds to estrogen receptor with an IC50 of 370 μM. . Raloxifene is a selective estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression .
|
-
- HY-121352
-
|
|
Drug Derivative
|
Cancer
|
|
Kibdelone C is a hexacyclic tetrahydroxanthone natural product and anticancer agent with sub-nanomolar GI50 activity against human SR leukemia and SN12C renal carcinoma cell lines. Kibdelone C disrupts the actin cytoskeleton in human cancer cells, leading to cell contraction and actin stress fiber formation, without direct actin binding, actin polymerization effects, topoisomerase I/II inhibition, or DNA binding. Kibdelone C can be used for the research of leukemia, and renal cell carcinoma .
|
-
- HY-W013935
-
|
|
Endogenous Metabolite
Estrogen Receptor/ERR
Reactive Oxygen Species (ROS)
|
Endocrinology
|
|
Bisphenol B is a close structural analog of Bisphenol A (BPA) (HY-18260). Bisphenol B is a potent, orally active endocrine disruptor (ED). Bisphenol B binds to G protein-coupled estrogen receptor (GPER) (IC50 = 3.3 μM) with higher affinity and agonistic activity than BPA. Bisphenol B promotes GPER mediated cell migration. Bisphenol B exerts estrogenic effects via GPER pathway at nanomolar concentration. Bisphenol B is used in the manufacture of polycarbonate resin with ED properties .
|
-
- HY-129937A
-
GNE-987
1 Publications Verification
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
GNE-987 is a VHL-dependent BRD4 PROTAC degrader. GNE-987 exhibits picomolar cell BRD4 degradation activity (DC50=0.03 nM for EOL-1 AML cell line). GNE-987 binds equipotently to the BD1 and BD2 bromodomains of BRD4 with low nanomolar affinities (IC50=4.7 and 4.4 nM, respectively). GNE-987 can be used for the research of cancer .
|
-
- HY-117540
-
|
|
Histone Methyltransferase
|
Cancer
|
|
ZLD10A is a highly potent and selective EZH2 inhibitor with the activity of inhibiting H3K27 methylation. ZLD10A can inhibit wild-type and mutant EZH2 with nanomolar potency and has more than 1000-fold selectivity for the other 10 histone methyltransferases. ZLD10A inhibited cell proliferation of DLBCL cell lines in a concentration- and time-dependent manner, showing a potential antiproliferative effect. ZLD10A can be used in the study of EZH2 mutant lymphomas .
|
-
- HY-181821
-
|
|
Parasite
Na+/K+ ATPase
|
Infection
|
|
MMV1581361 is a PfATP4 inhibitor and an orally active, transmission-blocking agent with nanomolar activity against Plasmodium falciparum blood-stage isolates. MMV1581361 disrupts sodium ion (Na +) homeostasis in Plasmodium falciparum. MMV1581361 inhibits male gamete exflagellation, reduces oocyst intensity, and blocks transmission of Plasmodium falciparum. MMV1581361 demonstrates efficacy in the humanized Plasmodium falciparum NOD scid IL2Rγ null mouse model. MMV1581361 can be used for the research of malaria .
|
-
- HY-180559
-
|
|
nAChR
Interleukin Related
|
Inflammation/Immunology
|
|
nAChR antagonist 2 is a selective nAChR antagonist. nAChR antagonist 2 inhibits nAChR subtype including hα9α10, hα9, and hα7 with IC50 values of 16.0 nM, 26.2 nM, and 336.3 nM, respectively, in Xenopus oocytes. nAChR antagonist 2 suppresses ATP-induced IL-1β release at nanomolar concentrations. nAChR antagonist 2 can be used for nonopioid analgesics and immunomodulators research .
|
-
- HY-149283
-
|
|
JAK
HDAC
Apoptosis
|
Cancer
|
|
JAK/HDAC-IN-2 is a potent 2-amino-4-phenylaminopyrimidine JAK/HDAC dual-target inhibitor. JAK/HDAC-IN-2 potently inhibits HDAC3/6 and JAK1/2 at nanomolar levels. JAK/HDAC-IN-2 has proapoptotic activity and inhibits histone deacetylation and STAT3 phosphorylation. JAK/HDAC-IN-2 presents remarkable antiproliferative activity in both hematological malignancies and solid cancers .
|
-
- HY-106100A
-
|
EMD 38362
|
Dopamine Receptor
Serotonin Transporter
|
Neurological Disease
|
|
Roxindole hydrochloride (EMD 38362), an indot-alkyl-pipenidine, is a potent agonist at dopamine autoreceptors, with an affinity for the D2-like subtype in the low nanomolar range. Roxindole can be used for the research of positive and negative schizophrenic symptoms. Roxindole is a 5-HT1A agonist and 5-HT uptake inhibitor with high affinity for 5-HT1A (IC50=0.9 nM). Antipsychotic and antidepressant activities .
|
-
- HY-174466
-
|
|
5-HT Receptor
Arrestin
|
Neurological Disease
|
|
5-HT2AR ligand 1 (Compound 2 cis) is a 5-HT2AR ligand with nanomolar affinity for 5-HT2AR (Ki: 32 nM). 5-HT2AR ligand 1 is capable of inducing β-arrestin 2 recruitment. 5-HT2AR ligand 1 can be used in the research of neurological diseases .
|
-
- HY-135276A
-
|
|
MicroRNA
Apoptosis
|
Cancer
|
|
Targaprimir-96 TFA is a potent inhibitor of microRNA-96 (miR-96) processing. Targaprimir-96 TFA selectively modulates miR-96 production in cancer cells and triggers apoptosis. Targaprimir-96 TFA binds primary miR-96 (pri-miR-96) with low nanomolar affinity. Targaprimir-96 TFA directly engages pri-miR-96 in breast cancer cells and is ineffective on healthy breast cells .
|
-
- HY-146366
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 26 (compound 3c) is a potent inhibitor of tubulin. Tubulin inhibitor 26 is an indazole derivative compound. Tubulin inhibitor 26 shows noteworthy low nanomolar potency against HepG2, HCT116, SW620, HT29 and A549 cancer cell lines. Tubulin inhibitor 26 arrests tumor cell in G2/M phase and induced cell apoptosis. Tubulin inhibitor 26 suppresses tumor growth in vivo without affecting the mice body weight .
|
-
- HY-113658
-
|
|
Endogenous Metabolite
|
Others
|
|
ts-SA is a carbonic anhydrase (CA) inhibitor with activity against seven human CA homologues. ts-SA can bind to the Zn(II) ion in the enzyme active site in a deprotonated form. The organic skeleton of ts-SA extends in the enzyme cavity and participates in multiple interactions with amino acid residues and water molecules. Due to its structural differences, the inhibitory performance of ts-SA is significantly better than that of another pyridine derivative. ts-SA exhibits low nanomolar inhibitory activity and is a multi-target CA inhibitor .
|
-
- HY-179375
-
|
|
CDK
Aurora Kinase
|
Cancer
|
|
LCI133 is afirst-in-class,nanomolar-potent, selective multikinase inhibitor targeting CDK4/6/9 and AURKA/B (IC50 = 4.7/10.2/4.1 nM and 2.8/10.6 nM). LCI133 induces S/G2 cell-cycle arrest and robust apoptosis in MYCN-amplified neuroblastoma BE(2)-C cells. LCI133 demonstrates significant antitumor efficacy in a BE(2)-C neuroblastoma xenograft model .
|
-
- HY-154978
-
|
|
Drug Derivative
|
Cancer
|
|
Cisplatin-resistant cells-IN-1 (Compound 8) has high cytotoxicity against Cisplatin (HY-17394)-resistant cells. Cisplatin-resistant cells-IN-1 reduces the metabolic activity effectively in the low nanomolar range (IC50: 0.14-1.79 μM in A549/A549-R, K562/K562-R, and MCF-7/MCF-7TamR cells) .
|
-
- HY-153468
-
|
TEQ103; Sera2
|
Sodium Channel
TRP Channel
|
Cancer
|
|
ErSO-TFPy (TEQ103) is an ERα+ tumor cell inhibitor with low nanomolar cytotoxic activity against ERα+ breast cancer cells. ErSO-TFPy activates the sodium channel TRPM4, causes an imbalance of intracellular calcium and sodium ions. ErSO-TFPy dysregulates calcium homeostasis in ERα+ tumor cells, triggers the anticipatory unfolded protein response, and induces rapid immune cell-independent necrotic cell death. ErSO-TFPy can be used for the research of estrogen receptor alpha positive breast cancer .
|
-
- HY-103110R
-
|
|
Reference Standards
5-HT Receptor
Adrenergic Receptor
|
Neurological Disease
|
|
ST1936 (Standard) is the analytical standard of ST1936 (HY-103110). This product is intended for research and analytical applications. ST1936 is a selective, nanomolar affinity 5-HT6 receptor agonist with Ki values of 13 nM, 168 nM and 245 nM for human 5-HT6, 5-HT7 and 5-HT2B receptors, respectively. ST1936 also shows moderate affinity (Ki of 300 nM) for human and rat α2 adrenergic receptor .
|
-
- HY-126247
-
|
|
Ras
|
Cancer
|
|
BI-2852 is a KRAS inhibitor for the switch I/II pocket (SI/II-pocket) by structure-based agent design with nanomolar affinity. BI-2852 is mechanistically distinct from covalent KRASG12C inhibitor (binds to switch II pocket) and binds ten-fold more strongly to active KRASG12D versus KRASwt (740 nM vs 7.5 μM). BI-2852 blocks GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in KRAS mutant cells.
|
-
- HY-122587
-
|
|
DNA/RNA Synthesis
RSV
|
Infection
|
|
AVG-233 is a potent, orally active RNA dependent RNA polymerase (RdRp) inhibitor. AVG-233 prevents initiation of the viral polymerase complex at the promoter. AVG-233 binding site is present in the L1-1749 fragment. AVG-233 has nanomolar activity against both RSV strains and clinical RSV isolates (EC50=0.14-0.31 μM). AVG-233 can be used for research of respiratory syncytial virus (RSV) .
|
-
- HY-112774A
-
|
|
mTOR
Autophagy
Atg8/LC3
p62
Ribosomal S6 Kinase (RSK)
|
Cancer
|
|
ICSN3250 hydrochloride is a halitulin analogue and a mTORC1 inhibitor. ICSN3250 hydrochloride directly binds to mTOR's FRB domain and displaces phosphatidic acid (PA), reversing mTORC1 activation. ICSN3250 hydrochloride shows high cytotoxicity in cancer cells (nanomolar concentration) through a caspase-independent cell death mechanism. ICSN3250 hydrochloride specifically inhibits the mTORC1 pathway, inducing autophagy and G0-G1 cell-cycle arrest in cancer cells. ICSN3250 hydrochloride can be used for the study of cancer .
|
-
- HY-153810
-
|
JNJ-1802
|
Virus Protease
Flavivirus
Dengue Virus
|
Infection
|
|
Mosnodenvir (JNJ-1802) is an orally active pan serotype dengue virus (DENV) inhibitor, with EC50 values ranging from 0.057 to 11 nM for four dengue virus (DENV) serotypes. Mosnodenvir blocks viral replication by inhibiting the formation of complexes between two viral proteins, nonstructural protein 3 (NS3) and NS4B, thereby preventing the formation of new viral RNA. Mosnodenvir exhibits picomolar to nanomolar antiviral activity in vitro and has antiviral efficacy in mice and non-human primates .
|
-
- HY-108672
-
|
|
P2Y Receptor
|
Inflammation/Immunology
|
|
NF157 is a highly selective nanomolar P2Y11 antagonist with a pKi of 7.35. The IC50s are 463 nM, 1811 µM, 170 µM for P2Y11 (Ki=44.3 nM), P2Y1 (Ki=187 µM), P2Y2 (Ki=28.9 µM), respectively . NF157, significantly reduces expression of metalloproteinase (MMP)-3, MMP-13, can be used in the treatment of osteoarthritis (OA) .
|
-
- HY-112774
-
|
|
mTOR
Autophagy
Atg8/LC3
p62
Ribosomal S6 Kinase (RSK)
|
Cancer
|
|
ICSN3250 is a halitulin analogue and specific mTORC1 inhibitor. ICSN3250 directly binds to mTOR's FRB domain and displaces phosphatidic acid (PA), reversing mTORC1 activation. ICSN3250 shows high cytotoxicity in cancer cells (nanomolar concentration) through a caspase-independent cell death mechanism. ICSN3250 specifically inhibits the mTORC1 pathway, inducing autophagy and G0-G1 cell-cycle arrest in cancer cells. ICSN3250 can be used for the study of cancer .
|
-
- HY-107428
-
|
|
MMP
|
Cardiovascular Disease
|
|
PD-166793 is a potent, selective, orally active and wide-broad spectrum inhibitor of MMP, exhibiting nanomolar potency against MMP-2, MMP-3 and MMP-13 (IC50=4, 7, and 8 nM, respectively) and micromolar potency vs MMP-1, -7 and -9 (IC50=6.0, 7.2, and 7.9 μM, respectively). PD-166793 can attenuate left ventricular remodeling and dysfunction in a rat model of progressive heart failure .
|
-
- HY-119799
-
|
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
UK-500001 is an orally active inhibitor for phosphodiesterase 4 (PDE4), which inhibits PDE4D3 (IC50 is 0.28 nM), PDE4B2 (IC50 is 22.8 nM), PDE4A4 (IC50 is 26.1 nM) and PDE4C2 (IC50 is 271 nM). UK-500001 exhibits anti-inflammatory efficacy and inhibits TNF-α and IFN-γ release in human and rodent macrophagic cell lines in nanomolar levels. UK-500001 ameliorates chronic obstructive pulmonary disease (COPD) and asthma .
|
-
- HY-149269
-
|
|
COX
Carbonic Anhydrase
LOX-1
|
Inflammation/Immunology
|
|
COX-2-IN-30 is a benzenesulfonamide derivative, as well as an orally active and dual inhibitor of COX (IC50=49 nM for COX-2, 10.4 μM for COX-1) and 5-LOX (IC50=2.4 μM). COX-2-IN-30 also inhibits transmembrane hCA IX and hCA XII isoform with nanomolar calss Ki values. COX-2-IN-30 exhibits analgesic, anti-inflammatory, and ulcerogenic activities, and does not show acute gastric effect .
|
-
- HY-12513
-
|
LY3023414
|
PI3K
DNA-PK
mTOR
Autophagy
|
Cancer
|
|
Samotolisib (LY3023414) potently and selectively inhibits class I PI3K isoforms, DNA-PK, and mTORC1/2 with IC50s of 6.07 nM, 77.6 nM, 38 nM, 23.8 nM, 4.24 nM and 165 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ, DNA-PK and mTOR, respectively. Samotolisib potently inhibits mTORC1/2 at low nanomolar concentrations .
|
-
- HY-173564
-
|
|
Epigenetic Reader Domain
Necroptosis
|
Inflammation/Immunology
|
|
DW34 is an orally active pan-BRD4-D1 biased inhibitor with additional BRD4-D2 inhibitive activity. DW34 displays comparable inhibitive efficacy to I-BET151 (HY-13235) (EC50 = 0.16 μM) with low nanomolar EC50 values of 0.14 μM. DW34 significantly reduces liver inflammation induced by LPS (HY-D1056) and APAP (HY-66005) via reducing chemokine expression and cellular necrosis .
|
-
- HY-170894
-
|
|
SARS-CoV
|
Infection
|
|
SARS-CoV-2 Mpro-IN-37 (compound 8r) is a SARS-CoV-2 main protease (M pro) inhibitor, with an IC50 of 0.0199 μM. SARS-CoV-2 Mpro-IN-37 inhibits SARS-CoV-1 M pro and MERS-CoV M pro with IC50s of 0.00945 and 0.111 μM, respectively. SARS-CoV-2 Mpro-IN-37 displays high antiviral activity in the nanomolar range without showing cellular toxicity .
|
-
- HY-135582S1
-
|
|
Isotope-Labeled Compounds
Estrogen Receptor/ERR
|
Endocrinology
|
|
Raloxifene 4'-glucuronide-d4 (lithium) is deuterium labeled Raloxifene 4'-glucuronide. Raloxifene 4'-glucuronide is a primary metabolite of Raloxifene. Raloxifene 4'-glucuronide formation is mediated mostly by UGT1A10 and UGT1A8. Raloxifene 4'-glucuronide binds to estrogen receptor with an IC50 of 370 μM. . Raloxifene is a selective estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression .
|
-
- HY-15350
-
|
LY 300046 hydrochloride
|
Reverse Transcriptase
|
Others
|
|
Trovirdine hydrochloride, a phenethylthiazolylthiourea (PETT) derivative, is an HIV reverse transcriptase (RT) non-nucleoside inhibitor (NNI). A novel computer model of the RT/NNI binding pocket revealed spatial gaps around Trovirdine hydrochloride's pyridyl ring. Docking studies suggested that replacing this planar ring with a nonplanar piperidinyl or piperazinyl ring could better occupy the binding pocket, enhancing anti-HIV activity. Synthesized heterocyclic compounds based on this modification demonstrated greater potency than Trovirdine hydrochloride, effectively inhibiting HIV replication at nanomolar concentrations without cytotoxicity in infected peripheral blood mononuclear cells .
|
-
- HY-135581S1
-
|
|
Isotope-Labeled Compounds
Estrogen Receptor/ERR
|
Endocrinology
|
|
Raloxifene 6-glucuronide-d4 (lithium) is deuterium labeled Raloxifene 6-glucuronide. Raloxifene 6-glucuronide is a primary metabolite of Raloxifene. Raloxifene 6-glucuronide is mediated mostly by UGT1A1 and UGT1A8. Raloxifene 6-glucuronide binds to estrogen receptor with an IC50 of 290 μM. Raloxifene is a selective and nonsteroidal estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression .
|
-
- HY-18971
-
TG4-155
1 Publications Verification
|
Prostaglandin Receptor
|
Neurological Disease
Inflammation/Immunology
Endocrinology
Cancer
|
|
TG4-155 is a potent, brain-permeant and selective EP2 receptor antagonist with a Ki of 9.9 nM . TG4-155 shows low nanomolar antagonist activity against only EP2 and DP1 . TG4-155 has an EP2 Schild KB of 2.4 nM and displays 550-4750-fold selectivity for EP2 over EP1, EP3, EP4 and IP, but only 14-fold selectivity against the DP1 receptor .
|
-
- HY-182317
-
|
|
Drug Isomer
Dengue Virus
|
Infection
|
|
(+)-Mosnodenvir is an isomer of Mosnodenvir (HY-153810). Mosnodenvir (JNJ-1802) is an orally active pan serotype dengue virus (DENV) inhibitor, with EC50 values ranging from 0.057 to 11 nM for four dengue virus (DENV) serotypes. Mosnodenvir blocks viral replication by inhibiting the formation of complexes between two viral proteins, nonstructural protein 3 (NS3) and NS4B, thereby preventing the formation of new viral RNA. Mosnodenvir exhibits picomolar to nanomolar antiviral activity in vitro and has antiviral efficacy in mice and non-human primates .
|
-
- HY-180912
-
|
|
CDK
Apoptosis
|
Cancer
|
|
HS-36 is a highly selective and orally active dual inhibitor of CDK4 and CDK9 with IC50 values of 18.9 and 4.2 nM respectively. HS-36 exhibits nanomolar-level potent activity against various cancer cells, inducing G0/G1 phase arrest and promoting cell apoptosis. HS-36 efficiently inhibits tumor growth in a mouse model of MV-4-11 tumors. HS-36 can be used for the study of acute myeloid leukemia .
|
-
- HY-P2265
-
|
|
SOS1
Ras
|
Cancer
|
|
SAH-SOS1A is a peptide-based SOS1/KRAS protein interaction inhibitor. SAH-SOS1A binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity (EC50=106-175 nM), directly and independently blocks nucleotide association, impairs KRAS-driven cancer cell viability, and exerts its effects by on-mechanism blockade of the ERK-MAPK phosphosignaling cascade downstream of KRAS .
|
-
- HY-136910
-
|
USP7-IN-7
|
Deubiquitinase
MDM-2/p53
|
Cancer
|
|
USP7-797 (USP7-IN-7) is an orally available, selective USP7 inhibitor (IC50=0.5 nmol/L) with antitumor activity. USP7-797 reduces the level of MDM2, thereby increasing the stability and activity of p53, leading to cell cycle arrest and apoptosis. USP7-797 has low nanomolar cytotoxicity against p53 mutant cancer cell lines, p53 wild-type hematological tumors, and neuroblastoma cell lines .
|
-
- HY-106100AR
-
|
EMD 38362 (Standard)
|
Reference Standards
Dopamine Receptor
Serotonin Transporter
|
Neurological Disease
|
|
Roxindole (hydrochloride) (Standard) is the analytical standard of Roxindole (hydrochloride). This product is intended for research and analytical applications. Roxindole hydrochloride (EMD 38362), an indot-alkyl-pipenidine, is a potent agonist at dopamine autoreceptors, with an affinity for the D2-like subtype in the low nanomolar range. Roxindole can be used for the research of positive and negative schizophrenic symptoms. Roxindole is a 5-HT1A agonist and 5-HT uptake inhibitor with high affinity for 5-HT1A (IC50=0.9 nM). Antipsychotic and antidepressant activities .
|
-
- HY-P10548
-
|
|
Bacterial
|
Infection
|
|
Cyclic L27-11 is a cyclic peptide-like antibiotic with strong antibacterial activity against specific bacteria such as Pseudomonas sp. Cyclic L27-11 shows nanomolar antibacterial activity against Pseudomonas sp., especially Pseudomonas aeruginosa. Cyclic L27-11 interferes with the function of bacterial outer membrane protein LptD, preventing the normal transport of lipopolysaccharide (LPS), leading to the accumulation of membrane-like substances in bacterial cells, which in turn affects the survival of bacteria. Cyclic L27-11 can be used in the development of antibacterial agents .
|
-
- HY-179599
-
|
|
DYRK
EGFR
|
Neurological Disease
Cancer
|
|
Dyrk1A-IN-15 is a selective, brain-penetrant and ATP-competitive Dyrk1A inhibitor with a IC50 of 19 nM. Dyrk1A-IN-15 displays high selectivity across a broad kinase panel (specific for DYRK kinases) with nanomolar potency. Dyrk1A-IN-15 impairs neurosphere self-renewal, cell invasion, and EGFR stability in vitro. Dyrk1A-IN-15 inhibits tumor growth and prolongs survival in vivo. Dyrk1A-IN-15 has potential for glioblastoma (GBM) research .
|
-
- HY-135582S
-
|
|
Estrogen Receptor/ERR
Isotope-Labeled Compounds
|
Endocrinology
|
|
Raloxifene 4'-glucuronide-d4 is deuterated labeled Raloxifene 4'-glucuronide (HY-135582). Raloxifene 4'-glucuronide is a primary metabolite of Raloxifene. Raloxifene 4'-glucuronide formation is mediated mostly by UGT1A10 and UGT1A8. Raloxifene 4'-glucuronide binds to estrogen receptor with an IC50 of 370 μM. . Raloxifene is a selective estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression .
|
-
- HY-W013935R
-
|
|
Reference Standards
Endogenous Metabolite
Estrogen Receptor/ERR
Reactive Oxygen Species (ROS)
|
Endocrinology
|
|
Bisphenol B (Standard) is the analytical standard of Bisphenol B. This product is intended for research and analytical applications. Bisphenol B is a close structural analog of Bisphenol A (BPA) (HY-18260). Bisphenol B is a potent, orally active endocrine disruptor (ED). Bisphenol B binds to G protein-coupled estrogen receptor (GPER) (IC50 = 3.3 μM) with higher affinity and agonistic activity than BPA. Bisphenol B promotes GPER mediated cell migration. Bisphenol B exerts estrogenic effects via GPER pathway at nanomolar concentration. Bisphenol B is used in the manufacture of polycarbonate resin with ED properties .
|
-
- HY-179600
-
|
|
DYRK
EGFR
|
Neurological Disease
Cancer
|
|
Dyrk1A-IN-16 is a selective, brain-penetrant and ATP-competitive Dyrk1A inhibitor with a IC50 of 53 nM. Dyrk1A-IN-16 displays high selectivity across a broad kinase panel (specific for DYRK kinases) with nanomolar potency. Dyrk1A-IN-16 impairs neurosphere self-renewal, cell invasion, and EGFR stability in vitro. Dyrk1A-IN-16 inhibits tumor growth and prolongs survival in vivo. Dyrk1A-IN-16 has potential for glioblastoma (GBM) research .
|
-
- HY-180836
-
|
|
Molecular Glues
IKZF Family
Apoptosis
|
Cancer
|
|
DIX-01 is a molecular gel degrader that can simultaneously induce the degradation of IKZF1/3 and GSPT1 mediated by CRBN. Its DC50 values are: IKZF1 (19.80 nM), IKZF3 (45.31 nM), and GSPT1 (120.1 nM). DIX-01 exhibits nanomolar-level potent anti-proliferative activity in various cancer cell lines. DIX-01 induces apoptosis in MV4-11 cells and significantly inhibits the growth of leukemia cells in zebrafish. DIX-01 can be used for the study of malignant hematological tumors .
|
-
- HY-149878
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
BD-9136 is a potent and highly selective BRD4 PROTAC depressant. BD-9136 has low-nanomolar degradation potencies against BRD4 , and its degradation selectivity for BRD4 is 1000 times that of BRD2 and BRD3 proteins. BD-9136 has antitumor activity .(Pink: Desmethyl-QCA276 (HY-44103); Black: 3-(2-(4-Methylpiperazin-1-yl)ethyl)azetidin-3-ol; Blue: Thalidomide-4-OH (HY-103596))
|
-
- HY-100233R
-
|
|
JNK
Reference Standards
|
Inflammation/Immunology
Cancer
|
|
IQ-1S (free acid) (Standard) is the analytical standard of IQ-1S (free acid) (HY-100233). This product is intended for research and analytical applications. IQ-1S free acid is a prospective inhibitor of NF-κB/activating protein 1 (AP-1) activity with an IC50 of 2.3±0.41 μM. IQ-1S free acid has binding affinity (Kd values) in the nanomolar range for all three JNKs with Kds of 100 nM, 240 nM, and 360 nM for JNK3, JNK1, and JNK2, respectively.
|
-
- HY-100552
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
VUF10166 is a potent and high-affinity 5-HT3 receptor antagonist, with Ki values of 0.04 nM (5-HT3A) and 22 nM (5-HT3AB). VUF10166 inhibits 5-HT-induced responses at 5-HT3A and 5-HT3AB receptors at nanomolar concentrations. At 5-HT3 receptor, VUF10166 at higher concentrations also acts as a partial agonist, with an EC50 of 5.2 μM .
|
-
- HY-108350R
-
|
|
Reference Standards
Epigenetic Reader Domain
|
Cancer
|
|
MI-2-2 (Standard) is the analytical standard of MI-2-2 (HY-108350). This product is intended for research and analytical applications. MI-2-2 is a potent menin-MLL inhibitor. MI-2-2 binds to menin with low nanomolar affinity (Kd=22nM) and very effectively disrupts the bivalent protein-protein interaction between menin and MLL. MI-2-2 has specific and very pronounced activity in MLL leukemia cells, including inhibition of cell proliferation, down-regulation of Hoxa9 expression, and differentiation .
|
-
- HY-164977
-
|
|
PROTACs
Phosphatase
|
Cancer
|
|
JCS-1 is a potent DcpS PROTAC degrader. JCS-1 non-covalently binds DcpS with a RG3039-based warhead and recruits the E3
ligase VHL. JCS-1 promotes ubiquitination and degradation of DcpS at nanomolar concentrations (DC50 in MOLM-14 cells: 87 nM). JCS-1 can be used for the research of AML and other DcpS-dependent genetic disorders (Pink: DcpS ligand (HY-102020); Blue: E3 ligase VHL ligand (HY-151227); Black: linker (HY-141230)) .
|
-
- HY-16787
-
|
|
Sodium Channel
|
Cardiovascular Disease
|
|
ICA-121431 is a nanomolar potent and broad-spectrum voltage-gated sodium channel (Nav) blocker, shows equipotent selectivity for human Nav1.1 and Nav1.3 subtypes with IC50 values of 13 nM and 23 nM, respectively. ICA-121431 shows less potent inhibition of Nav1.2 (IC50=240 nM) and 1,000 fold selectivity against Nav1.4, Nav1.6, and the TTX-resistant human Nav1.5 and Nav1.8 channels (IC50s >10 μM).
|
-
- HY-153519
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
WWL0245 is a potent and seletive BRD4 PROTAC. WWL0245 selectively degrades BRD4 with sub-nanomolar DC50 (<1 nM) than BRD2/3 and PLK1 ( DC50>1 μM). WWL0245 shows excellent selective cytotoxicity in the BETi sensitive cancer cell lines, including AR-positive prostate cancer cell lines. WWL0245 is a promising drug candidate for AR-positive prostate cancer research and a valuable tool compound to study the biological function of BRD4 .
|
-
- HY-122557
-
|
|
|
Neurological Disease
|
|
AZD3676 is an orally active and blood-brain barrier-permeable ligand for 5-HT1A and 5-HT1B receptors, with nanomolar binding affinity for human and monkey receptors (human 5-HT1A: 0.16 nM, monkey 5-HT1A: 0.13 nM, human 5-HT1B: 2.3 nM, monkey 5-HT1B: 2.4 nM). AZD3676 is applicable to research related to cognitive impairment in Alzheimer's disease .
|
-
- HY-155007
-
|
|
Bacterial
|
Infection
|
|
DNA gyrase B-IN-2 (Compound E) is a 2-aminobenzothiazole-based DNA gyrase B inhibitor with promising activity against ESKAPE bacterial pathogens. DNA gyrase B-IN-2 showed low nanomolar inhibition of DNA gyrase (IC50 < 10 nM) and broad-spectrum antibacterial activity against pathogens belonging to the ESKAPE group, with the minimum inhibitory concentration < 0.03 μg/mL for most Gram-positive strains and 4–16 μg/mL against Gram-negative E. coli, Acinetobacter baumannii, Pseudomonas aeruginosa, and Klebsiella pneumoniae.DNA gyrase B-IN-2 can be used for the research of infection .
|
-
- HY-156401
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
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) .
|
-
- HY-131708A
-
|
|
HDAC
Parasite
|
Infection
|
|
FNDR-20123 is a safe, first-in-class, and orally active anti-malarial HDAC inhibitor with IC50s of 31 nM and 3 nM for Plasmodium and human HDAC, respectively. FNDR-20123 exerts anti-malarial activity against Plasmodium falciparum asexual stage (IC50=41 nM) and sexual blood stage (IC50=190 nM for male gametocytes). FNDR-20123 inhibits HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8 (IC50=25/29/2/11/282 nM, respectively.) and inhibits Class III HDAC isoforms at nanomolar concentrations .
|
-
- HY-12443
-
|
|
Casein Kinase
|
Neurological Disease
|
|
PF-5006739 is a potent and selective inhibitor of CK1δ/ε with IC50s of 3.9 nM and 17.0 nM, respectively. PF-5006739 is a potential therapeutic agent for a range of psychiatric disorders with low nanomolar in vitro potency for CK1δ/ε and high kinome selectivity. PF-5006739 attenuats opioid agent-seeking behavior in a rodent operant reinstatement model in animals in a dose-dependent manner . PF-5006739 improves glucose tolerance in both diet-induced obesity (DIO) and genetic (ob/ob) mice models of obesity .
|
-
- HY-115314
-
|
LG 30435
|
Histamine Receptor
|
Inflammation/Immunology
|
|
Mequitamium iodide (LG 30435) is an antihistamine drug with antiallergic and bronchodilatory activity. Mequitamium iodide can effectively antagonize airway contraction and inflammatory responses induced by histamine and antigens. Mequitamium iodide has nanomolar affinity for the H1 and smooth muscle receptors of histamine and mequitin. Mequitamium iodide, when administered in aerosol form, significantly inhibits histamine- and antigen-induced increases in airway pressure in allergic mice. Mequitamium iodide reduces antigen-induced eosinophil accumulation in the airways. Mequitamium iodide also exhibits inhibitory effects on PAF-induced platelet aggregation and bronchoconstriction, and can be used in the study of allergic diseases such as rhinitis and asthma .
|
-
- HY-W030338
-
|
|
Endogenous Metabolite
|
Inflammation/Immunology
|
|
aPKC-IN-2 is a small molecule inhibitor that inhibits aPKC activity. aPKC-IN-2 can effectively block vascular endothelial permeability in cell culture and in vivo experiments. aPKC-IN-2 shows biological activity in interfering with NFκB-driven gene transcription and is associated with inflammatory responses. aPKC-IN-2 has a significant inhibitory effect on vascular endothelial permeability induced by VEGF and TNF, and its EC50 value is in the low nanomolar range. The structural characteristics of aPKC-IN-2 reveal key elements of its inhibitory activity, providing the possibility for further development of small molecule aPKC inhibitors .
|
-
- HY-123882
-
|
|
Endogenous Metabolite
|
Others
|
|
IRAK4-IN-29 is an IRAK4 inhibitor with good selectivity and low nanomolar activity. IRAK4-IN-29 can effectively block the TLR-mediated signal transduction pathway. IRAK4-IN-29 showed significant inhibitory effects in LPS- and R848-induced cytokine experiments. IRAK4-IN-29 can inhibit LPS-induced TNFα in an in vivo model, showing a similar phenotype to IRAK4 gene-deficient mice. IRAK4-IN-29 has good medicinal chemical properties, such as microsomal stability and solubility, showing potential clinical application value .
|
-
- HY-112626
-
|
|
CDK
|
Cancer
|
|
CDK12-IN-2 is a potent, selective and nanomolar CDK12 inhibitor (IC50=52 nM) with good physicochemical properties. CDK12-IN-2 is also a strong CDK13 inhibitor due to CDK13 is the closest homologue of CDK12. CDK12-IN-2 shows excellent kinase selectivity for CDK12 over CDK2, 9, 8, and 7. CDK12-IN-2 inhibits the phosphorylation of Ser2 in the C-terminal domain of RNA polymerase II. CDK12-IN-2 can be used an excellent chemical probe for functional studies of CDK12 .
|
-
- HY-125327
-
|
|
SGLT
|
Metabolic Disease
|
|
YM-543 is a selective SGLT2 inhibitor that effectively reduces hyperglycemia in type 2 diabetic mice through increased urinary glucose excretion. YM-543 demonstrates potent inhibition of both mouse and human SGLT2 activities at nanomolar concentrations. YM-543, when administered orally, significantly improves glucose tolerance in diabetic models and sustains its effects for over 12 hours. YM-543, in combination with other antidiabetic agents like rosiglitazone or metformin, enhances the therapeutic effects on diabetic symptoms. YM-543 does not affect blood glucose levels in normal mice, indicating its specificity for diabetic conditions.
|
-
- HY-126247B
-
|
|
Drug Derivative
Ras
|
Cancer
|
|
(R)-BI-2852 is the isomer of BI-2852 (HY-126247), and can be used as an experimental control. BI-2852 is a KRAS inhibitor for the switch I/II pocket (SI/II-pocket) by structure-based agent design with nanomolar affinity. BI-2852 is mechanistically distinct from covalent KRASG12C inhibitor (binds to switch II pocket) and binds ten-fold more strongly to active KRASG12D versus KRASwt (740 nM vs 7.5 μM). BI-2852 blocks GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in KRAS mutant cells.
|
-
- HY-173059
-
|
|
CDK
|
Cancer
|
|
CDK12/13-IN-3 (Compound 12b) is the orally active inhibitor for CDK that inhibits CDK12 and CDK13 with IC50 of 107.4 nM and 79.4 nM. CDK12/13-IN-3 inhibits the phosphorylation of Ser2 on the CTD of RNA polymerase II, induces DNA damage, and downregulates the gene expression of DNA damage response (DDR). CDK12/13-IN-3 exhibits antiproliferative activity against multiple cancer cells with IC50 of nanomolar levels. CDK12/13-IN-3 exhibits antitumor effect in mouse models, exhibits good pharmacokinetic properties with an oral bioavailability of 53.6% .
|
-
- HY-176948
-
|
|
mTOR
|
Cancer
|
|
M-1111 is a Rapa-Link inhibitor. M-1111 is covalently linked by Rapamycin (HY-10219) and an inhibitor of the active site mTOR. M-1111 has strong inhibitory activity on the mTORC1 signaling pathway (pS6 and p4E-BP1). M-1111 has nanomolar-level inhibitory activity against various cancer cells. M-1111 completely inhibits p4E-BP1 without inhibiting pAkt S473. M-1111 can be used for research on liver cancer, kidney cancer, and colorectal cancer .
|
-
- HY-W002942
-
|
1,2,3,4-Tetrahydroquinolin-8-ol; 8-hydroxy-1,2,3,4-tetrahydroquinoline
|
Ferroptosis
Reactive Oxygen Species (ROS)
|
Inflammation/Immunology
|
|
Ferroptosis-IN-21 is a ferroptosis inhibitor that protects against renal I/R injury by suppressing ferroptosis and directly scavenging peroxyl radicals. Ferroptosis-IN-21 displays broad-spectrum anti-ferroptotic efficacy across multiple inducers in renal tubular epithelial cells, with nanomolar potency and robust suppression of lipid Reactive Oxygen Species (ROS). Ferroptosis-IN-21 significantly ameliorates renal I/R injury in mice, reducing histological damage, functional impairment, and inflammatory cytokine expression, while decreasing lipid peroxidation biomarkers such as 4-hydroxynonenal. Ferroptosis-IN-12 can be used for research in the field of ferroptosis-targeted drug development .
|
-
- HY-131708
-
|
|
HDAC
Parasite
|
Infection
|
|
FNDR-20123 free base is a safe, first-in-class, and orally active anti-malarial HDAC inhibitor with IC50s of 31 nM and 3 nM for Plasmodium and human HDAC, respectively. FNDR-20123 free base exerts anti-malarial activity against Plasmodium falciparum asexual stage (IC50=41 nM) and sexual blood stage (IC50=190 nM for male gametocytes). FNDR-20123 free base inhibits HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8 (IC50=25, 29, 2, 11, and 282 nM, respectively) and inhibits Class III HDAC isoforms at nanomolar concentrations .
|
-
- HY-19932
-
|
|
HCV Protease
HCV
|
Infection
|
|
MK-2748 is a hepatitis C virus (HCV) NS3/4a protease inhibitor. MK-2748 exhibits broad-spectrum and potent antiviral activity, with nanomolar-level activity against all genotypes (gt1a-gt6) (IC₅₀ < 0.115 nM), showing only slightly weaker activity against gt3a (1.212 nM), and maintaining high inhibitory activity against drug-resistant mutant strains such as gt1b R155K (IC₅₀ = 0.032 nM) and D168Y (IC₅₀ = 0.057 nM). MK-2748 can be used in the research of HCV infection .
|
-
- HY-168936
-
|
|
PROTACs
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
|
DP-15 is the degrader for GSPT1 and BRD4 with DC50s of 5.25 nM and 0.48 nM. DP-15 exhibits anti-proliferative activity of AML cells and NHL cells with an IC50 of nanomolar levels, arrests the cell cycle at G1 phase, and induces apoptosis in MOLM13. DP-15 exhibits anti-leukemia activity in MOLM-13 xenograft mouse models . (Pink: ligand for target protein JQ-1 carboxylic acid (HY-78695); Black: linker (HY-W262798); Blue: ligand for E3 ligase Cereblon Thalidomide-5-OH (HY-23095))
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-
- HY-107428R
-
|
|
Reference Standards
MMP
|
Cardiovascular Disease
|
|
PD-166793 (Standard) is the analytical standard of PD-166793 (HY-107428). This product is intended for research and analytical applications. PD-166793 is a potent, selective, orally active and wide-broad spectrum inhibitor of MMP, exhibiting nanomolar potency against MMP-2, MMP-3 and MMP-13 (IC50=4, 7, and 8 nM, respectively) and micromolar potency vs MMP-1, -7 and -9 (IC50=6.0, 7.2, and 7.9 μM, respectively). PD-166793 can attenuate left ventricular remodeling and dysfunction in a rat model of progressive heart failure .
|
-
- HY-160696
-
|
|
CD73
|
Cancer
|
|
ORIC-533 is an orally active, highly selective, AMP-competitive CD73 inhibitor that potently blocks adenosine production with sub-nanomolar affinity (Ka=0.03 nM). In multiple myeloma, ORIC-533 restores and enhances the cytotoxicity of the immune system against tumor cells through multiple immunological mechanisms, including reversing the immunosuppressive microenvironment, inducing immunogenic cell death, and activating dendritic cells, T cells and NK cells, with no direct toxicity to normal cells. The combination of ORIC-533 with Daratumumab (HY-P9915) synergistically enhances anti-tumor efficacy, significantly increases intratumoral CD8 + T cell infiltration and inhibits tumor growth in vivo .
|
-
- HY-P2265A
-
|
|
SOS1
Ras
|
Cancer
|
|
SAH-SOS1A TFA is a peptide-based SOS1/KRAS protein interaction inhibitor. SAH-SOS1A TFA binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity (EC50=106-175 nM). SAH-SOS1A TFA directly and independently blocks nucleotide association. SAH-SOS1A TFA impairs KRAS-driven cancer cell viability and exerts its effects by on-mechanism blockade of the ERK-MAPK phosphosignaling cascade downstream of KRAS .
|
-
- HY-181266
-
|
|
Parasite
Aminopeptidase
|
Infection
|
|
Antimalarial agent 55 is an orally potent inhibitor of PfA-M1 and PfA-M17 aminopeptidases from Plasmodium falciparum, with Ki values of 27 nM and 81 nM, respectively. Antimalarial agent 55 exhibits potent nanomolar activity against homologous enzymes from Plasmodium vivax and Plasmodium berghei, with Ki values of 2 nM, 4 nM, 190 nM and 18 nM for Pv-M1, Pb-M1, Pv-M17 and Pb-M17, respectively. Antimalarial agent 55 possesses significant antiplasmodial activity, as well as cross-species inhibitory capacity and broad-spectrum activity that is unaffected by existing drug resistance mechanisms. Antimalarial agent 55 can be used in malaria research .
|
-
- HY-178166
-
|
|
Toll-like Receptor (TLR)
p38 MAPK
TNF Receptor
ERK
JNK
NF-κB
Interleukin Related
|
Inflammation/Immunology
|
|
ETI41 is an orally active, selective TLR inhibitor that targets the nucleoside-binding Site I on TLR7 (IC50 = 0.63 μM) and TLR9 (IC50 = 0.16 μM), sparing surface TLRs (including TLR1/TLR2, TLR2/TLR6, TLR4 and TLR5). ETI41 potently inhibits endosomal TLR-mediated pro-inflammatory signaling with nanomolar activity in cellular, biophysical and in vivo assays. ETI41 suppresses the expression of inflammation-associated genes and effectively ameliorates symptoms in mouse models of psoriasis, and systemic lupus erythematosus (SLE). ETI41 can be used for autoimmune and inflammatory diseases research .
|
-
- HY-178169
-
|
|
Toll-like Receptor (TLR)
p38 MAPK
TNF Receptor
ERK
JNK
NF-κB
Interleukin Related
|
Inflammation/Immunology
|
|
ETI60 is an orally active, selective TLR inhibitor that targets the nucleoside-binding Site I on TLR7 (IC50 = 0.68 μM) and TLR9 (IC50 = 0.12 μM), sparing surface TLRs (including TLR1/TLR2, TLR2/TLR6, TLR4 and TLR5). ETI60 potently inhibits endosomal TLR-mediated pro-inflammatory signaling with nanomolar activity in cellular, biophysical and in vivo assays. ETI60 modulates the expression of genes associated with inflammation. ETI60 effectively ameliorates symptoms in mouse models of psoriasis, and systemic lupus erythematosus (SLE). ETI60 can be used for autoimmune and inflammatory diseases research .
|
-
- HY-104042
-
|
AG-881
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
|
|
Vorasidenib (AG-881) is an orally available, brain penetrant second-generation dual mutant isocitrate dehydrogenases 1 and 2 (mIDH1/2) inhibitor. Vorasidenib (AG-881) exhibits nanomolar inhibition of (D)-2-hydroxyglutarate (D-2-HG), and the IC50 ranges of 0.04~22 nM against IDH1 R132C, IDH1 R132G, IDH1 R132H and IDH1 R132S and 7~14 nM against IDH2 R140Q and 130 nM against IDH2 R172K. Vorasidenib can be used for the study of grade 2 astrocytoma or oligodendroglioma with a susceptible IDH1/2 mutation .
|
-
- HY-12583
-
|
|
Histone Methyltransferase
Epigenetic Reader Domain
|
Cancer
|
|
A-366, a chemical probe, is a potent, highly selective, peptide-competitive histone methyltransferase G9a inhibitor with IC50s of 3.3 and 38 nM for G9a and GLP (EHMT1), respectively. A-366 shows >1000-fold selectivity over 21 other methyltransferases. A-366 is also a potent, nanomolar inhibitor of the Spindlin1-H3K4me3-interaction (IC50=182.6 nM). A-366 displays high affinity at human histamine H3 receptor (Ki=17 nM) and shows subtype selectivity among subsets of the histaminergic and dopaminergic receptor families .
|
-
- HY-122575
-
|
|
P2X Receptor
Influenza Virus
Topoisomerase
MicroRNA
Apoptosis
|
Infection
Neurological Disease
Inflammation/Immunology
|
|
Aurintricarboxylic acid is a nanomolar-potency, allosteric antagonist with selectivity towards αβ-methylene-ATP-sensitive P2X1Rs and P2X3Rs, with IC50s of 8.6 nM and 72.9 nM for rP2X1R and rP2X3R, respectively . Aurintricarboxylic acid is a potent anti-influenza agent by directly inhibiting the neuraminidase . Aurintricarboxylic acid is an inhibitor of topoisomerase II and apoptosis . Aurintricarboxylic acid is a selective inhibitor of the TWEAK-Fn14 signaling pathway . Aurintricarboxylic acid also acts as a cystathionine-lyase (CSE) inhibitor with an IC50 of 0.6 μM . Aurintricarboxylic acid is a modifier of miRNAs that regulate miRNA function, with an IC50 of 0.47 µM .
|
-
- HY-179404
-
|
|
Ras
|
Cancer
|
|
KRASG12C IN-18 is an orally active covalent KRAS G12C inhibitor that achieves complete covalent engagement of KRAS G12C in both GDP- and GMPPNP-bound states and displays strong antiproliferative activity against KRAS G12C and resistance-associated variants, including KRAS G12C/R68S, with low-nanomolar IC50 values.
KRASG12C IN-18 exhibits marked in vivo efficacy in KRAS G12C-driven solid tumor and KRAS G12C/R68S xenograft models and can be used for colorectal cancer research .
|
-
- HY-156240
-
|
|
E1/E2/E3 Enzyme
Keap1-Nrf2
|
Metabolic Disease
|
|
DI-1548 is a potent, selective, and irreversible covalent inhibitor of DCN1 (IC50 = 4.6 nM). DI-1548 potently and selectively inhibits cullin 3 neddylation at nanomolar concentrations, and exhibits no obvious effect on the neddylation of other cullin members (including cullin 1, 2, 4A, 4B, and 5). DI-1548 exhibits no cytotoxicity. DI-1548 covalently binds to DCN1, disrupting the DCN1-UBC12 interaction, causing the collapse of the neddylation complex, inactivating CRL3, leading to NRF2 accumulation and upregulation of its target genes, and ultimately protecting mice from liver damage. DI-1548 can be used in liver injury research .
|
-
- HY-134813
-
|
|
Ras
|
Cancer
|
|
MRTX1133 is a noncovalent, potent, and selective alkyne-based KRAS G12D inhibitor. MRTX1133 optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated KD against KRAS G12D of 0.2 pM. MRTX1133 prevents SOS1-catalyzed nucleotide exchange and/or formation of the KRAS G12D/GTP/RAF1 complex, thereby inhibiting mutant KRAS-dependent signal transduction. MRTX1133 selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tumor cells. MRTX1133 has single digit nanomolar activity in cellular assays and marked in vivo efficacy in tumor models harboring KRAS G12D mutations .
|
-
- HY-183366
-
|
|
HDAC
Caspase
Akt
|
Inflammation/Immunology
Cancer
|
|
HDAC1-IN-14 is an indole-based benzamide selective HDAC1 inhibitor with an IC50 of 77 nM. HDAC1-IN-14 acts as an antiproliferative agent, with GI50 values ranging from nanomolar to low micromolar levels in various cancer cells. HDAC1-IN-14 induces G0-G1 cell cycle arrest in colon cancer cells. HDAC1-IN-14 upregulates the expression of Caspase-3, Cyto-C and Bax, and downregulates the expression of AKT-1. HDAC1-IN-14 can be used in research related to leukemia, non-small cell lung cancer, colon cancer, central nervous system cancer, melanoma, ovarian cancer, renal cancer, prostate cancer and breast cancer .
|
-
- HY-13590
-
|
|
VEGFR
|
Cancer
|
|
CEP-7055 (compound 21) is a novel vascular endothelial growth factor R2 (VEGF-R2) tyrosine kinase inhibitor with potent inhibitory activity. Studies have found that the inhibitor activity can be significantly improved by optimizing the R9 substituent. Compound 21 has potent low nanomolar inhibition of human VEGF-R tyrosine kinase and shows good selectivity against multiple tyrosine and serine/threonine kinases. N,N-dimethylglycine ester 40 was prepared to improve its water solubility and oral bioavailability. In animal pharmacokinetic studies, a significant increase in the plasma level of 21 was observed after oral administration of 40. Compound 21 showed significant in vivo antitumor activity in multiple tumor models and has entered phase I clinical trials as a water-soluble N,N-dimethylglycine ester proagent of 40 (CEP-7055).
|
-
- HY-104042R
-
|
AG-881 (Standard)
|
Reference Standards
Isocitrate Dehydrogenase (IDH)
|
Cancer
|
|
Vorasidenib (Standard) is the analytical standard of Vorasidenib (HY-104042). This product is intended for research and analytical applications. Vorasidenib (AG-881) is an orally available, brain penetrant second-generation dual mutant isocitrate dehydrogenases 1 and 2 (mIDH1/2) inhibitor. Vorasidenib (AG-881) exhibits nanomolar inhibition of (D)-2-hydroxyglutarate (D-2-HG), and the IC50 ranges of 0.04~22 nM against IDH1 R132C, IDH1 R132G, IDH1 R132H and IDH1 R132S and 7~14 nM against IDH2 R140Q and 130 nM against IDH2 R172K. Vorasidenib can be used for the study of grade 2 astrocytoma or oligodendroglioma with a susceptible IDH1/2 mutation .
|
-
- HY-15334
-
|
|
VEGFR
|
Cancer
|
|
CEP-5214, derived from a new indenopyrrolocarbazole template, is a potent inhibitor of vascular endothelial growth factor R2 (VEGF-R2) tyrosine kinase. Structurally, it features optimal substitutions at positions 9 (ethoxymethyl) and 12 (hydroxypropyl) on the indeno[2,1-a]pyrrolo[3,4-c]carbazole-5-one scaffold, leading to high potency against VEGF-R2 (IC50 8 nM). Compound 21 (CEP-5214) exhibits low-nanomolar inhibition of human VEGF-R tyrosine kinases (IC50 4 nM for VEGF-R2/KDR), with good selectivity over other kinases. The compound demonstrated significant cellular and in vivo antitumor activity across various models and advanced into phase I clinical trials as a water-soluble prodrug (CEP-7055) to enhance oral bioavailability .
|
-
- HY-170978
-
|
|
PROTACs
CDK
|
Cancer
|
|
PROTAC CDK9 degrader-11 (Compound C3) is an orally active PROTAC degrader for CDK9 with DC50 of 1.09 nM. PROTAC CDK9 degrader-11 exhibits cytotoxicity in multi small cell lung cancer cell with IC50 of nanomolar levels. PROTAC CDK9 degrader-11 arrests cell cycle at G0/G1 phase, inhibits the cell invasion in DMS114 and DMS53 cell. PROTAC CDK9 degrader-11 exhibits antitumor efficacy in NCI-H446 xenograft mouse models .(Pink: ligand for target protein CDK9 ligand 3 (HY-170979); Black: linker; Blue: ligand for E3 ligase Cereblon E3 ligase Ligand 56 (HY-W247437))
|
-
- HY-180556
-
|
|
mTOR
PI3K
|
Inflammation/Immunology
|
PI3K/mTOR-IN-20 is a selective dual PI3K/mTOR inhibitor. PI3K/mTOR-IN-20 demonstrates nanomolar antiproliferative effects with IC50s of 0.380 and 0.090 μM for MRC-5 and Mlg2908 cells. PI3K/mTOR-IN-20 reduces Ashcroft scores, hydroxyproline content, collagen deposition, and downregulates fibrosis-related proteins, while restoring lung architecture in a Bleomycin-induced pulmonary fibrosis model. PI3K/mTOR-IN-20 shows a favorable safety profile with steady weight recovery and no distinct liver or kidney toxicity. PI3K/mTOR-IN-20 can be used for fetal lung fibroblasts research .
|
-
- HY-182354
-
|
|
VEGFR
FGFR
FLT3
PDGFR
RET
Akt
ERK
c-Kit
|
Cancer
|
|
VEGFR2-IN-84 is an orally active, multi-targeted tyrosine kinase inhibitor based on a naphthalene ring scaffold. VEGFR2-IN-84 inhibits VEGFR2 with sub-nanomolar affinity and broadly targets kinases including Kit, FGFR, PDGFR, and Ret. By competitively binding to the ATP-binding pocket, VEGFR2-IN-84 blocks the phosphorylation of VEGFR2 and its downstream AKT/ERK signaling pathway, thereby significantly inhibiting endothelial cell proliferation, migration, and tumor angiogenesis. VEGFR2-IN-84 exhibits broad-spectrum antiproliferative activity against various solid tumors such as liver cancer, lung cancer, and renal cancer, shows weak toxicity to normal cells, and has superior potency to Lenvatinib (HY-10981). VEGFR2-IN-84 possesses favorable pharmacokinetic properties and high safety (LD50>2000 mg/kg), and can be used in related studies of various malignant tumors .
|
-
- HY-167690
-
|
|
Endogenous Metabolite
|
Infection
|
|
MK-6186 is a novel non-nucleoside reverse transcriptase inhibitor with sub-nanomolar activity against wild-type viruses and the two most common NNRTI-resistant RT mutants (K103N and Y181C). MK-6186 exhibits excellent antiviral activity against K103N and Y181C mutant viruses. When MK-6186 targets 12 common NNRTI-associated mutant viruses, only two relatively rare mutants (Y188L and V106I/Y188L) show high resistance, with FC values exceeding 100, while the FC values of the remaining viruses are all below 10. In addition, when MK-6186 faces 96 clinical virus isolates carrying NNRTI-resistant mutations, most (70%) viruses show more than 10-fold resistance to efavirenz (EFV), while only 29% of mutant viruses show more than 10-fold resistance to MK-6186 .
|
-
- HY-130133
-
|
|
PI3K
mTOR
Akt
Apoptosis
Paraptosis
p38 MAPK
Mitochondrial Metabolism
P-glycoprotein
CDK
MMP
HIF/HIF Prolyl-Hydroxylase
VEGFR
|
Cancer
|
|
DHW-221 is a potent orally active dual PI3K/mTOR inhibitor, exhibiting low nanomolar potency against all four Class I PI3K isoforms and mTOR (PI3Kα, IC50 = 0.50 nM; PI3Kβ, IC50 = 1.9 nM; PI3Kγ, IC50 = 1.8 nM; PI3Kδ, IC50 = 0.74 nM; mTOR, IC50 = 3.9 nM). DHW-221 exerts antitumor effects by blocking the PI3K/Akt/mTOR pathway and inducing mitochondrial apoptosis and paraptosis (via Endoplasmic Reticulum (ER) stress and MAPK signaling) and arrests cell cycle, thereby inhibiting cell migration, invasion and angiogenesis. DHW-221 inhibits tumor growth in both the A549/Taxol (HY-B0015) and the HCC827 xenograft mouse models. DHW-221 can be used for non-small cell lung cancer (NSCLC), colon and breast cancer research .
|
-
- HY-180525
-
|
|
Influenza Virus
|
Infection
|
|
PB2-IN-2 is an orally active PB2 inhibitor with RNA-dependent RNA Polymerase (RNP) IC50 = 0.2 nM, LRA (Ligand Receptor Assay) EC50 = 0.8 nM, Cytopathic Effect (CPE) EC50 = 0.1 nM. PB2-IN-2 exhibits broad-spectrum, nanomolar antiviral potency against a panel of influenza A strains (including H1N1pdm09, Lyon/1337/2007/H1N1, Tex12-Like/H3N2, PR/8/34/H1N1, WSN/1933/H1N1, rPR8(H1N1)/H7N9 with EC50 = 1.5, 3.6, 3.7, 13.8, 2.9 and 9.8 nM and all the CC50 values > 2 μM. PB2-IN-2 possesses an excellent pharmacokinetic profile and metabolic stability. PB2-IN-2 can be used for anti-influenza research .
|
-
-
- HY-D2348A
-
|
|
蛍光色素
|
|
ACE TFA is a low-background, photostable fluorophore with nanomolar binding affinity for the Okra RNA aptamer. ACE TFA enables clear visualization of mRNA in live bacteria and mammalian cells, including tracking the trafficking of mRNA to stress granules and dual-color super-resolution imaging of RNA in live cells. (Ex=488 nm, Em=555 nm) .
|
-
- HY-D2348
-
|
|
蛍光色素
|
|
ACE is a low-background, photostable fluorophore with nanomolar binding affinity for the Okra RNA aptamer. ACE enables clear visualization of mRNA in live bacteria and mammalian cells, including tracking the trafficking of mRNA to stress granules and dual-color super-resolution imaging of RNA in live cells. (Ex=488 nm, Em=555 nm) .
|
-
- HY-141520G
-
|
|
蛍光色素
|
|
ART558 (GMP) is ART558 (HY-141520) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. ART558 is a potent, selective and allosteric DNA polymerase theta (Polθ) inhibitor (IC50=7.9 nM). ART558 elicits BRCA-gene synthetic lethality and DNA damage. ART558 can be used for the research of cancer, such as breast cancer .
|
-
- HY-141520G
-
|
|
生化学アッセイ試薬
|
|
ART558 (GMP) is ART558 (HY-141520) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. ART558 is a potent, selective and allosteric DNA polymerase theta (Polθ) inhibitor (IC50=7.9 nM). ART558 elicits BRCA-gene synthetic lethality and DNA damage. ART558 can be used for the research of cancer, such as breast cancer .
|
-
- HY-P10724
-
|
|
Formyl Peptide Receptor (FPR)
Bacterial
|
Infection
|
|
fMIFL is a formyl tetrapeptide derived from Staphylococcus aureus, and also an agonist of mouse formyl peptide receptor 1 (mFPR1). It exhibits nanomolar activity against mFPR1 and micromolar activity against mFPR2. fMIFL is applicable to studies related to bacterial infections .
|
-
- HY-P2274
-
|
|
Parasite
|
Infection
|
|
Argifin is a sub-nanomolar chitinase inhibitor produced by soil microorganisms, with IC50s of 0.025 μM, 6.4 μM , 1.1 μM and 4.5 μM for SmChiA (Serratia marcescens chitinaese A), SmChiB, Aspergillus fumigatus chitinase B1 and human chitotriosidase, respectively .
|
-
- HY-P2265A
-
|
|
SOS1
Ras
|
Cancer
|
|
SAH-SOS1A TFA is a peptide-based SOS1/KRAS protein interaction inhibitor. SAH-SOS1A TFA binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity (EC50=106-175 nM). SAH-SOS1A TFA directly and independently blocks nucleotide association. SAH-SOS1A TFA impairs KRAS-driven cancer cell viability and exerts its effects by on-mechanism blockade of the ERK-MAPK phosphosignaling cascade downstream of KRAS .
|
-
- HY-137392
-
|
1-Naphthalenesulfonyl-Ile-Trp-CHO
|
Cathepsin
|
Others
|
|
Cathepsin L-IN-4 is an inhibitor of cathepsin L with IC50 at nanomolar concentrations .
|
-
- HY-P11224
-
|
|
DNA/RNA Synthesis
|
Cancer
|
RMI-L4 is an efficient cyclic peptide inhibitor that can specifically disrupt the interaction between FANCM and RMI proteins with an IC50 of 54 nM. RMI-L4 engages the FANCM-binding pocket of RMI1/2 with nanomolar affinity (KD = 2.5 nM). RMI-L4 cannot penetrate the cell membrane and can be used to study the FANCM-RMI pathway targeting cancer with alternate lengthening of telomeres (ALT) .
|
-
- HY-P2265
-
|
|
SOS1
Ras
|
Cancer
|
|
SAH-SOS1A is a peptide-based SOS1/KRAS protein interaction inhibitor. SAH-SOS1A binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity (EC50=106-175 nM), directly and independently blocks nucleotide association, impairs KRAS-driven cancer cell viability, and exerts its effects by on-mechanism blockade of the ERK-MAPK phosphosignaling cascade downstream of KRAS .
|
-
- HY-P10331
-
|
|
SDCBP
|
Cancer
|
|
KSL 128114, a peptide inhibitor of syntenin, binds the PDZ1 domain of syntenin with nanomolar affinity. KSL 128114 is resistant toward degradation in human plasma and mouse hepatic microsomes and displays a global PDZ domain selectivity for syntenin .
|
-
- HY-161096
-
|
|
ROR
|
Cancer
|
|
Antitumor agent-127 (compound 1) is a parent macrocyclic peptide. Antitumor agent-127 displays nanomolar cell-based binding to ROR1 and relatively good internalization in 786-O and MDA-MB-231 tumor cell lines .
|
-
- HY-P10672
-
-
- HY-P2138
-
|
|
HIV Protease
|
Others
|
|
U-85548E is an HIV protease inhibitor with nanomolar affinity for HIV-1 aspartic protease. By studying its structure-activity relationship, a potent nanomolar inhibitor with inhibitory effects on both HIV-1 and HIV-2 proteases was designed, and its binding mode was studied by X-ray crystallography and molecular modeling.
|
-
- HY-120757
-
|
|
Virus Protease
|
Others
|
|
LP-130 is a statin-based inhibitor that is a universal inhibitor with nanomolar inhibitory activity against all tested retroviral proteases. Crystal structure studies of its binding to different retroviral proteases have shown that it can adapt to different active site regions to achieve inhibition.
|
-
- HY-P5914
-
|
WaTx
|
TRP Channel
|
Neurological Disease
|
|
Wasabi Receptor Toxin is a cell-penetrating scorpion toxin. Wasabi Receptor Toxin is the activator for TRPA1 ion channel with EC50 in nanomolar level, and prolongs the channel open time, but reduces Ca 2+ permeability. Wasabi Receptor Toxin causes thermal hypersensitivity and mechanical allodynia in rats, without triggering neurogenic inflammation .
|
-
- HY-P2274R
-
|
|
Reference Standards
Parasite
|
Infection
|
|
Argifin (Standard) is the analytical standard of Argifin. This product is intended for research and analytical applications. Argifin is a sub-nanomolar chitinase inhibitor produced by soil microorganisms, with IC50s of 0.025 μM, 6.4 μM , 1.1 μM and 4.5 μM for SmChiA (Serratia marcescens chitinaese A), SmChiB, Aspergillus fumigatus chitinase B1 and human chitotriosidase, respectively[1].
|
-
- HY-P5914A
-
|
WaTx TFA
|
TRP Channel
|
Neurological Disease
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Wasabi Receptor Toxin TFA (WaTx TFA) is the TFA salt form of Wasabi Receptor Toxin (HY-P5914). Wasabi Receptor Toxin TFA is a cell-penetrating scorpion toxin. Wasabi Receptor Toxin TFA is the activator for TRPA1 ion channel with EC50 in nanomolar level, and prolongs the channel open time, but reduces Ca 2+ permeability. Wasabi Receptor Toxin TFA causes thermal hypersensitivity and mechanical allodynia in rats, without triggering neurogenic inflammation .
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- HY-P10548
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Bacterial
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Infection
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Cyclic L27-11 is a cyclic peptide-like antibiotic with strong antibacterial activity against specific bacteria such as Pseudomonas sp. Cyclic L27-11 shows nanomolar antibacterial activity against Pseudomonas sp., especially Pseudomonas aeruginosa. Cyclic L27-11 interferes with the function of bacterial outer membrane protein LptD, preventing the normal transport of lipopolysaccharide (LPS), leading to the accumulation of membrane-like substances in bacterial cells, which in turn affects the survival of bacteria. Cyclic L27-11 can be used in the development of antibacterial agents .
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- HY-P99294
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AMG 479; Human Anti-IGF1R Recombinant Antibody
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IGF-1R
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Cancer
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Ganitumab (AMG 479) is a recombinant human monoclonal antibody to the human type 1 insulin-like growth factor receptor (IGF1R). Ganitumab recognizes murine IGF1R with sub-nanomolar affinity (KD=0.22 nM) and inhibits the interaction of murine IGF1R with IGF1 and IGF2. Ganitumab can be used in research of cancer .
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(5)
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- HY-P991734
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TREM receptor
Syk
Calcium Channel
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Neurological Disease
Inflammation/Immunology
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VHB937 is a potent and selective TREM2 agonist, a human monoclonal antibody, with sub-nanomolar affinity. VHB937 enhances TREM2 surface expression and downstream signaling, such as Syk phosphorylation and calcium mobilization. VHB937 exhibits robust neuroprotective effects in vivo, significantly reducing pathology and pro-inflammatory markers across a broad range of animal models of neuroinflammation and neurodegeneration. VHB937 can be used for neurodegenerative diseases research .
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(5)
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- HY-W703549
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Aderbasib-d3 (INCB007839-d3) is deuterium labeled Aderbasib. Aderbasib (INCB007839) is a potent, orally active and target specific low nanomolar hydroxamate-based inhibitor of ADAM10 and ADAM17. Aderbasib exhibits robust antineoplastic activity and can be used for cancer research, including diffuse large B-cell non-Hodgkin lymphoma, HER2 +?breast cancer, gliomas, et al .
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- HY-135582S1
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Raloxifene 4'-glucuronide-d4 (lithium) is deuterium labeled Raloxifene 4'-glucuronide. Raloxifene 4'-glucuronide is a primary metabolite of Raloxifene. Raloxifene 4'-glucuronide formation is mediated mostly by UGT1A10 and UGT1A8. Raloxifene 4'-glucuronide binds to estrogen receptor with an IC50 of 370 μM. . Raloxifene is a selective estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression .
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- HY-135581S1
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Raloxifene 6-glucuronide-d4 (lithium) is deuterium labeled Raloxifene 6-glucuronide. Raloxifene 6-glucuronide is a primary metabolite of Raloxifene. Raloxifene 6-glucuronide is mediated mostly by UGT1A1 and UGT1A8. Raloxifene 6-glucuronide binds to estrogen receptor with an IC50 of 290 μM. Raloxifene is a selective and nonsteroidal estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression .
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- HY-135582S
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Raloxifene 4'-glucuronide-d4 is deuterated labeled Raloxifene 4'-glucuronide (HY-135582). Raloxifene 4'-glucuronide is a primary metabolite of Raloxifene. Raloxifene 4'-glucuronide formation is mediated mostly by UGT1A10 and UGT1A8. Raloxifene 4'-glucuronide binds to estrogen receptor with an IC50 of 370 μM. . Raloxifene is a selective estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression .
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- HY-134813
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Alkynes
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MRTX1133 is a noncovalent, potent, and selective alkyne-based KRAS G12D inhibitor. MRTX1133 optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated KD against KRAS G12D of 0.2 pM. MRTX1133 prevents SOS1-catalyzed nucleotide exchange and/or formation of the KRAS G12D/GTP/RAF1 complex, thereby inhibiting mutant KRAS-dependent signal transduction. MRTX1133 selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tumor cells. MRTX1133 has single digit nanomolar activity in cellular assays and marked in vivo efficacy in tumor models harboring KRAS G12D mutations .
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- HY-167690
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Alkynes
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MK-6186 is a novel non-nucleoside reverse transcriptase inhibitor with sub-nanomolar activity against wild-type viruses and the two most common NNRTI-resistant RT mutants (K103N and Y181C). MK-6186 exhibits excellent antiviral activity against K103N and Y181C mutant viruses. When MK-6186 targets 12 common NNRTI-associated mutant viruses, only two relatively rare mutants (Y188L and V106I/Y188L) show high resistance, with FC values exceeding 100, while the FC values of the remaining viruses are all below 10. In addition, when MK-6186 faces 96 clinical virus isolates carrying NNRTI-resistant mutations, most (70%) viruses show more than 10-fold resistance to efavirenz (EFV), while only 29% of mutant viruses show more than 10-fold resistance to MK-6186 .
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- HY-179404
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Alkynes
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KRASG12C IN-18 is an orally active covalent KRAS G12C inhibitor that achieves complete covalent engagement of KRAS G12C in both GDP- and GMPPNP-bound states and displays strong antiproliferative activity against KRAS G12C and resistance-associated variants, including KRAS G12C/R68S, with low-nanomolar IC50 values.
KRASG12C IN-18 exhibits marked in vivo efficacy in KRAS G12C-driven solid tumor and KRAS G12C/R68S xenograft models and can be used for colorectal cancer research .
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