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Results for "

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" in MCE Product Catalog:

249

Inhibitors & Agonists

2

Screening Libraries

1

Biochemical Assay Reagents

12

Peptides

57

Natural
Products

4

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas
  • HY-A0279
    Pristinamycin

    Pristinamycine

    Bacterial Infection
    Pristinamycin, produced by Streptomyces pristinaespiralis, is an orally active streptogramin-like antibiotic consisting of two chemically unrelated components: Pristinamycin I (PI) and Pristinamycin II (PII). Pristinamycin is highly active against many antibiotic-resistant pathogens, particularly Gram-positive bacteria, including Methicillin-resistant Staphylococcus aureus (MRSA), Vancomycin-resistant S. aureus (VRSA) and Enterococcus faecium (VREF).
  • HY-14267
    Lersivirine

    UK-453061

    HIV Reverse Transcriptase Infection
    Lersivirine (UK-453061) is potent and selective non-nucleoside reverse transcription inhibitor (NNRTI; IC50=119 nM) with excellent efficacy against NNRTI-resistant viruses. Lersivirine exhibits potent antiretroviral activity against wild-type HIV virus and clinically relevant NNRTI-resistant strains.
  • HY-19319
    MI-136

    Epigenetic Reader Domain Androgen Receptor Apoptosis Cancer
    MI-136 is an inhibitor of the menin-MLL protein-protein interaction (PPI), with an IC50 of 31 nM and a Kd of 23.6 nM. MI-136 shows to block AR signaling and has the potential for the study in castration-resistant tumors.
  • HY-103250
    PF-945863

    Antibiotic Infection
    PF-945863 is an orally active macrolide antibiotic that can be used for the research of multidrug resistant respiratory tract bacterial strains.
  • HY-131981
    TP0586532

    Bacterial Infection
    TP0586532 is a non-hydroxamate LpxC inhibitor (IC50=0.101 μM). TP0586532 as a compound with a low cardiovascular risk that is effective against K. pneumoniae, including resistant strains.
  • HY-103645
    GW779439X

    Bacterial Aurora Kinase Apoptosis Cancer Infection
    GW779439X is a pyrazolopyridazine identified in an inhibitor of the S. aureus PASTA kinase Stk1. GW779439X potentiates the activity of β-lactam antibiotics against various MRSA and MSSA isolates, some even crossing the breakpoint from resistant to sensitive. GW779439X is an AURKA inhibitor and induces apoptosis by the caspases 3/7 pathway. MRSA:methicillin-resistant S. aureus; MSSA: methicillin-sensitive S. aureus
  • HY-123390
    DB07107

    Bcr-Abl Akt Cancer
    DB07107 is a potent drug resistant T315I mutant Bcr-Abl tyrosine kinase inhibitor. DB07107 is also a potent Akt1 inhibitor with an IC50 value of 360 nM.
  • HY-100530D
    Rp-cAMPS sodium salt

    PKA Neurological Disease
    Rp-cAMPS sodium salt, a cAMP analog, is a potent, competitive cAMP-induced activation of cAMP-dependent PKA I and II (Kis of 12.5 µM and 4.5 µM, respectively) antagonist. Rp-cAMPS sodium salt is resistant to hydrolysis by phosphodiesterases.
  • HY-100530A
    Rp-cAMPS

    PKA Neurological Disease
    Rp-cAMPS, a cAMP analog, is a potent, competitive cAMP-induced activation of cAMP-dependent PKA I and II (Kis of 12.5 µM and 4.5 µM, respectively) antagonist. Rp-cAMPS is resistant to hydrolysis by phosphodiesterases.
  • HY-100530
    Rp-cAMPS triethylammonium salt

    PKA Neurological Disease
    Rp-cAMPS triethylammonium salt, a cAMP analog, is a potent, competitive cAMP-induced activation of cAMP-dependent PKA I and II (Kis of 12.5 µM and 4.5 µM, respectively) antagonist. Rp-cAMPS triethylammonium salt is resistant to hydrolysis by phosphodiesterases.
  • HY-109014
    Tenofovir exalidex

    CMX-157

    HIV HBV Nucleoside Antimetabolite/Analog Infection
    Tenofovir exalidex (CMX157) is a lipid conjugate of the acyclic nucleotide analog Tenofovir with activity against both wild-type and antiretroviral drug-resistant HIV strains, including multidrug nucleoside/nucleotide analog-resistant viruses. Tenofovir exalidex is active against all major subtypes of HIV-1 and HIV-2 in fresh human PBMCs and against all HIV-1 strains evaluated in monocyte-derived macrophages, with EC50s ranging between 0.2 and 7.2 nM. CMX157 is orally available and has no apparent toxicity. Tenofovir exalidex also shows antiviral activity against HBV.
  • HY-19314A
    Azvudine hydrochloride

    RO-0622 hydrochloride; FNC hydrochloride

    Reverse Transcriptase HIV HBV HCV Infection
    Azvudine (RO-0622) hydrochloride is a potent nucleoside reverse transcriptase inhibitor (NRTI), with antiviral activity on HIV, HBV and HCV. Azvudine hydrochloride exerts highly potent inhibition on HIV-1 (EC50s ranging from 0.03 to 6.92 nM) and HIV-2 (EC50s ranging from 0.018 to 0.025 nM). Azvudine hydrochloride inhibits NRTI-resistant viral strains.
  • HY-19314
    Azvudine

    RO-0622; FNC

    Reverse Transcriptase HIV HBV HCV Infection
    Azvudine (RO-0622) is a potent nucleoside reverse transcriptase inhibitor (NRTI), with antiviral activity on HIV, HBV and HCV. Azvudine exerts highly potent inhibition on HIV-1 (EC50s ranging from 0.03 to 6.92 nM) and HIV-2 (EC50s ranging from 0.018 to 0.025 nM). Azvudine inhibits NRTI-resistant viral strains.
  • HY-117766
    PC945

    Fungal Cytochrome P450 Infection
    PC945, a potent, long-acting antifungal triazole, possesses activity against a broad range of both azole-susceptible and azole-resistant strains of Aspergillus fumigatus. PC945 is also a potent, tightly binding inhibitor of A. fumigatus sterol 14α-demethylase activity, CYP51A and CYP51B, with IC50s of 0.23 μM and 0.22 μM, respectively.
  • HY-111817
    ACT-451840

    Parasite Infection
    ACT-451840 is an orally active, potent and low-toxicity compound, showing activity against sensitive and resistant plasmodium falciparum strains. ACT-451840 targets all asexual blood stages of the parasite, has a rapid onset of action. ACT-451840 behaves in a way similar to artemisinin derivatives, with very rapid onset of action and elimination of parasite. ACT-451840 can be used for the research of malarial.
  • HY-21997
    Dmt-2'fluoro-da(bz) amidite

    DNA/RNA Synthesis Others
    Dmt-2'fluoro-da(bz) amidite, an uniformly modified 2'-deoxy-2'-fluoro phosphorothioate oligonucleotide, is a nuclease-resistant antisense compound with high affinity and specificity for RNA targets. Dmt-2'fluoro-da(bz) amidite is also an intermediate for 5’-DMT-3’-phosphoramidite synthesis.
  • HY-115282A
    JNJ-63576253

    TRC-253

    Androgen Receptor Cancer
    JNJ-63576253 (TRC-253) is a potent and orally active full antagonist of androgen receptor (AR), with IC50s of 37 and 54 nM for F877L mutant AR and wild-type AR in LNCaP cells. JNJ-63576253 can be used for the research of castration-resistant prostate cancer (CRPC).
  • HY-109070
    Ralaniten

    EPI-002

    Androgen Receptor Cancer
    Ralaniten (EPI-002) is a potent and orally active antagonist of the androgen receptor-N-terminal domain (AR-NTD). Ralaniten inhibits AR transcriptional activity, with IC50 of 7.4 μM. Ralaniten can be used for the research of castration-resistant prostate cancer (CRPC).
  • HY-115282
    JNJ-63576253 free base

    TRC-253 free base

    Androgen Receptor Cancer
    JNJ-63576253 (TRC-253) free base is a potent and orally active full antagonist of androgen receptor (AR), with IC50s of 37 and 54 nM for F877L mutant AR and wild-type AR in LNCaP cells. JNJ-63576253 free base can be used for the research of castration-resistant prostate cancer (CRPC).
  • HY-138557
    AKR1C3-IN-4

    Others Cancer
    AKR1C3-IN-4 is a potent and selective aldo-keto reductase 1C3 (AKR1C3) inhibitor with an IC50 of 0.56 μM. AKR1C3-IN-4 has the potential for castrate resistant prostate cancer (CRPC) research.
  • HY-12892
    SKI-178

    SphK Apoptosis Cancer
    SKI-178 is a potent sphingosine kinase-1 (SphK1) and SphK2 inhibitor. SKI-178 is cytotoxic at IC50 concentrations ranging from 1.8 to 0.1 μM in both drug sensitive and multi-drug resistant cancer cell lines (i.e., MTR3, NCI-ADR and HL60/VCR cells). SKI-178 induces apoptosis in a CDK1-dependent manner in human acute myeloid leukemia cell lines.
  • HY-N0790
    Lupeol

    Clerodol; Monogynol B; Fagarasterol

    Androgen Receptor Apoptosis Cancer
    Lupeol (Clerodol; Monogynol B; Fagarasterol) is an active pentacyclic triterpenoid, has anti-oxidant, anti-mutagenic, anti-tumor and anti-inflammatory activity. Lupeol is a potent androgen receptor (AR) inhibitor and can be used for cancer research, especially prostate cancer of androgen-dependent phenotype (ADPC) and castration resistant phenotype (CRPC).
  • HY-N7642
    Oxysanguinarine

    Hydroxysanguinarine; 8-Oxosanguinarine

    Parasite Infection
    Oxysanguinarine (Hydroxysanguinarine;8-Oxosanguinarine) is a protoberberine alkaloid from Meconopsis simplicifolia with antimalarial activity.
  • HY-B1924
    Norvancomycin hydrochloride

    Desmethyl-vancomycin hydrochloride

    Bacterial Infection
    Norvancomycin hydrochloride is applicable for endocarditis, osteomyelitis, pneumonia, sepsis or soft tissue infections caused by Staphylococcus (including Methicillin-resistant strains and multidrug-resistant microbial strains).
  • HY-128384
    Benzyldodecyldimethylammonium chloride dihydrate

    Bacterial Infection
    Benzyldodecyldimethylammonium chloride dihydrate is a quaternary ammonium compound (QAC) and can be used as a biocide to target antibiotic-resistant bacteria, such as methicillin-resistant Staphylococcus aureus (MRSA), multidrug-resistant (MDR) P. aeruginosa et. al. Benzyldodecyldimethylammonium chloride dihydrate, an antimicrobial agent, bacteriostatic or bactericidal properties depending on the concentration.
  • HY-W016420
    Fosfomycin sodium

    MK-0955 sodium

    Bacterial Antibiotic Infection
    Fosfomycin sodium (MK-0955 sodium) is a blood-brain barrier penetrating, broad-spectrum antibiotic by irreversibly inhibiting an early stage in cell wall synthesis. Fosfomycin sodium shows both in vivo and in vitro activity against a wide range of bacteria, including multidrug-resistant (MDR), extensively drug-resistant (XDR), and pan-drug-resistant (PDR) bacteria.
  • HY-119683
    Epoxiconazole

    Fungal Infection
    Epoxiconazole, a fungicide, is a demethylation inhibitor of the Ergosterol biosynthesis pathway. Epoxiconazole exhibits strong inhibitory effects on both carbendazim-resistant and phenamacril-resistant isolates, and can be used for controlling many crop diseases.
  • HY-N0402
    Artemether

    Dihydroqinghaosu methyl ether; Dihydroartemisinin methyl ether; SM224

    Parasite Infection Cancer
    Artemether is an antimalarial for the treatment of resistant strains of falciparum malaria.
  • HY-B0609
    Fosfomycin tromethamine

    MK-0955 tromethamine

    Bacterial Antibiotic Infection
    Fosfomycin tromethamine (MK-0955 tromethamine) is a blood-brain barrier penetrating, broad-spectrum antibiotic by irreversibly inhibiting an early stage in cell wall synthesis. Fosfomycin tromethamine shows both in vivo and in vitro activity against a wide range of bacteria, including multidrug-resistant (MDR), extensively drug-resistant (XDR), and pan-drug-resistant (PDR) bacteria.
  • HY-B1075
    Fosfomycin calcium

    MK-​0955 calcium

    Bacterial Antibiotic Infection
    Fosfomycin calcium (MK-​0955 calcium) is a blood-brain barrier penetrating, broad-spectrum antibiotic by irreversibly inhibiting an early stage in cell wall synthesis. Fosfomycin calcium (MK-​0955 calcium) shows both in vivo and in vitro activity against a wide range of bacteria, including multidrug-resistant (MDR), extensively drug-resistant (XDR), and pan-drug-resistant (PDR) bacteria.
  • HY-106349
    Fosteabine

    Cytarabine ocfosfate; YNK 01

    Nucleoside Antimetabolite/Analog Cancer
    Fosteabine is an oral and prodrug analogue of cytarabine which is resistant to deoxycytidine deaminase.
  • HY-N7115
    Sultamicillin

    Bacterial Antibiotic Infection
    Sultamicillin is an orally active double prodrug of Ampicillin/Sulbactan. Sulbactam is a semisynthetic beta-lactamase inhibitor which, in combination with Ampicillin, extends the antibacterial activity of the latter to include some beta-lactamase-producing strains of bacteria that would otherwise be resistant.
  • HY-B0465
    Oxacillin sodium monohydrate

    Bacterial Antibiotic Infection
    Oxacillin sodium monohydrate is an antibiotic similar to Flucloxacillin used in resistant staphylococci infections study.
  • HY-N8151
    Sanguisorbigenin

    Bacterial Infection
    Sanguisorbigenin is a natural antibacterial agent that inhibits methicillin-resistant S. aureus (MRSA).
  • HY-108917
    Morphothiadin

    GLS4

    HBV Infection
    Morphothiadin is a potent inhibitor on the replication of both wild-type and adefovir-resistant HBV with an IC50 of 12 nM.
  • HY-100358
    AQ-13 dihydrochloride

    Parasite Infection
    AQ-13 dihydrochloride is an aminoquinoline antimalarial drug that is effective against drug-resistant strains of Plasmodium falciparum.
  • HY-126295
    Anti-parasitic agent 3

    Parasite Infection
    Anti-parasitic agent 3 is an anti-parasitic agent which active against drug resistant parasites.
  • HY-108795A
    Albiglutide TFA

    Glucagon Receptor Metabolic Disease
    Albiglutide TFA, a glucagon-like peptide (GLP)-1 mimetic, is a long acting GLP-1 receptor agonist for the treatment of type 2 diabetes mellitus (T2DM). Albiglutide TFA is generated by the genetic fusion of a DPP-4-resistant GLP-1 dimer to human albumin.
  • HY-103095
    Enmetazobactam

    AAI101

    Bacterial Infection
    Enmetazobactam (AAI101) is an extended-spectrum β-lactamase inhibitor, against many resistant Gram-negative pathogens.
  • HY-I0447A
    Sodium 4-aminosalicylate dihydrate

    4-Aminosalicylic acid sodium salt dihydrate

    Bacterial Antibiotic Infection
    Sodium 4-aminosalicylate dihydrate (4-Aminosalicylic acid sodium salt dihydrate) is one of the antimycobacterial drugs currently used for multidrug-resistant tuberculosis.
  • HY-N3373
    Loganetin

    Bacterial Infection
    Loganetin is a non-toxic natural product that may be applied in the antibacterial drug development for treating multidrug-resistant Gram negative infections.
  • HY-P0098
    [D-Ala2]leucine-enkephalin

    Opioid Receptor Cancer
    [D-Ala2]leucine-enkephalin, a delta opioid agonist, is a degradation resistant long-acting Leu-enkephalin.
  • HY-10844
    Pretomanid

    PA-824; (S)-PA 824

    Bacterial Antibiotic Infection Cancer
    Pretomanid (PA-824) is an antibiotic used for the research of multi-drug-resistant tuberculosis affecting the lungs. Pretomanid exhibits a sub-micromolar MIC against M. tuberculosis (MTB). The MIC values of PA-824 against a panel of MTB pan-sensitive and Rifampin mono-resistant clinical isolates range from 0.015 to 0.25 µg/mL.
  • HY-U00255
    BO3482

    Bacterial Infection
    BO3482 has Antimicrobial activity and can inhibit the growth of methicillin-resistant Staphylococci (MRS) with an MIC90 of 6.25 mg/mL.
  • HY-13574A
    Biricodar

    VX-710

    P-glycoprotein Cancer
    Biricodar (VX-710) is a modulator of P-glycoprotein and MRP-1; shows effective chemosensitizing activity in multidrug resistant cells.
  • HY-N8198
    Ardisiacrispin B

    Apoptosis Ferroptosis Cancer
    Ardisiacrispin B displays cytotoxic effects in multi-factorial drug resistant cancer cells via ferroptotic and apoptotic cell death.
  • HY-15194
    Dimethylcurcumin

    ASC-J9; GO-Y025

    Androgen Receptor Cancer
    Dimethylcurcumin (ASC-J9) is an androgen receptor degradation enhancer that effectively suppresses castration resistant prostate cancer cell proliferation and invasion.
  • HY-16672
    AVX 13616

    Bacterial Infection
    AVX 13616 shows the potent in vivo antibacterial activity of Avexa’s lead antibacterial candidate; particularly against drug-resistant Staphylococcus pathogens.
  • HY-U00035
    MGB-BP-3

    Bacterial Infection
    MGB-BP-3 is an antibiotic that has been shown to be active against a broad range of important multi-resistant Gram-positive pathogens.
  • HY-70006
    Galeterone

    TOK-001; VN-124-1

    Cytochrome P450 Cancer
    Galeterone (TOK-001) is a multifunctional antiandrogen and CYP17 inhibitor (IC50=47 nM) in castration resistant prostate cancer (CRPC).
  • HY-15233
    Letermovir

    AIC246

    CMV Infection
    Letermovir (AIC246) is a potent inhibitor of CMV, which targets the viral terminase complex and remains active against virus resistant to DNA polymerase inhibitors.
  • HY-106574
    Ceftobiprole medocaril

    BAL5788

    Bacterial Infection
    Ceftobiprole medocaril is the parenteral prodrug of Ceftobiprole (HY-112579). Ceftobiprole is a broad-spectrum cephalosporin with activity against Methicillin-resistant staphylococcus aureus (MRSA).
  • HY-136384
    Diethofencarb

    Fungal Infection
    Diethofencarb is a fungicide with strong activity against Botrytis cinerea and Benzimidazole-resistant strains of Botryis spp. Diethofencarb has a role as an antifungal agrochemical.
  • HY-14749A
    Pyronaridine tetraphosphate

    Parasite Infection
    Pyronaridine tetraphosphate is a Mannich base anti-malarial with demonstrated efficacy against drug resistant Plasmodium falciparum, P. vivax, P. ovale and P. malariae.
  • HY-13062
    Daunorubicin hydrochloride

    Daunomycin hydrochloride; RP 13057 hydrochloride; Rubidomycin hydrochloride

    Topoisomerase DNA/RNA Synthesis ADC Cytotoxin Bacterial Autophagy Apoptosis Antibiotic Cancer Infection
    Daunorubicin (Daunomycin) hydrochloride is a topoisomerase II inhibitor with potent antineoplastic activities. Daunorubicin hydrochloride inhibits DNA and RNA synthesis in sensitive and resistant Ehrlich ascites tumor cells.
  • HY-N1312
    Sinapaldehyde

    Bacterial Infection
    Sinapaldehyde exhibits moderate antibacterial against Methicillin resistant S. aureus (MRSA) and E. coli with MIC values of 128 and 128 μg/mL.
  • HY-B0402A
    Amantadine hydrochloride

    1-Adamantanamine hydrochloride; 1-Adamantylamine hydrochloride; 1-Aminoadamantane hydrochloride

    Influenza Virus Infection
    Amantadine (1-Adamantanamine) hydrochloride is an antiviral agent with activity against influenza A viruses. Amantadine hydrochloride blocks the proton flow through the M2 ion channel and thus prevents the release of viral RNA into the cytoplasm of the infected cells. Amantadine hydrochloride is an antiparkinsonian agent.
  • HY-103184
    Proxalutamide

    GT0918; Pruxelutamide

    Androgen Receptor SARS-CoV Cancer
    Proxalutamide (GT0918) is an orally active potent androgen receptor (AR) antagonist. Proxalutamide (GT0918) can be used in the study for prostate cancer and COVID-19.
  • HY-17460A
    Garenoxacin Mesylate hydrate

    BMS284756 Mesylate hydrate

    Bacterial Infection
    Garenoxacin Mesylate hydrate (BMS284756 Mesylate hydrate) is a novel oral des-fluoro(6) quinolone with potent antimicrobial activity, against common respiratory pathogens, including resistant strains.
  • HY-A0097
    Teicoplanin

    Antibiotic MDL-507; MDL-507

    Bacterial Antibiotic Infection
    Teicoplanin is a semisynthetic glycopeptide antibiotic used in the prophylaxis and treatment of serious infections caused by Gram-positive bacteria, including Methicillin-resistant Staphylococcus aureus and Enterococcus faecalis.
  • HY-A0241
    Dalfopristin

    RP54476

    Bacterial Antibiotic Infection
    Dalfopristin is a semi-synthetic streptogramin antibiotic. Quinupristin/Dalfopristin (Q/D) is a valuable alternative antibiotic to vancomycin for the treatment of multi-drug resistant Enterococcus faecium infections.
  • HY-122470
    Stampidine

    Reverse Transcriptase HIV Infection
    Stampidine is a nucleoside reverse transcriptase inhibitor (NRTI) with potent and broad-spectrum anti-HIV activity. Stampidine inhibits the laboratory HIV-1 strain HTLVIIIB (B-envelope subtype) and primary clinical isolates with IC50s of 1 nM and 2 nM, respectively. Stampidine also inhibits NRTI-resistant primary clinical isolates and NNRTI-resistant clinical isolates with IC50s of 8.7 nM and 11.2 nM, respectively.
  • HY-135813
    LtaS-IN-1

    Bacterial Infection
    LtaS-IN-1 (compound 1771) is a potent small-molecule inhibitor of Lipoteichoic acid (LTA) synthesis in multidrug-resistant (MDR) E. faecium and by altering the cell wall morphology. LtaS-IN-1 alone inhibits Enterococcus.spp 28 strains with varying MIC values ranging from 0.5 μg/mL to 64 μg/mL. LtaS-IN-1 combination with antibiotics abolishs multidrug-resistant E. faecium growth almost completely.
  • HY-112579
    Ceftobiprole

    Ro 63-9141; BAL 9141

    Bacterial Infection
    Ceftobiprole (Ro 63-9141) is a broad-spectrum cephalosporin with activity against Methicillin-resistant staphylococcus aureus (MRSA) with the MIC90 value of 2 μg/mL.
  • HY-N2104
    Daurinoline

    Others Cancer
    Daurinoline is an alkaloid that can be isolated from the roots of Menispermum dauricum. Daurinoline may be a potential anti-tumor agent or chemosensitizer for chemo-resistant NSCLC research.
  • HY-118266
    BTdCPU

    Phosphatase Apoptosis Cancer
    BTdCPU is a potent heme-regulated eIF2α kinase (HRI) activator. BTdCPU promotes eIF2α phosphorylation and induced apoptosis in resistant cell.
  • HY-17531
    Pyraclonil

    Others Others
    Pyraclonil is a proporphyrinogen oxidase (PPO) inhibitor. Pyraclonil is a herbicide agent and is highly effective in controlling the susceptible (S) and multiple-herbicide-resistant (MHR) E. indica populations.
  • HY-15228
    RX-3117

    TV-1360; fluorocyclopentenylcytosine

    Nucleoside Antimetabolite/Analog Cancer
    RX-3117(TV-1360; Fluorocyclopentenylcytosine) is novel a cytidine analog; shows anticancer activity in several cancer cell lines, including gemcitabine-resistant variants.
  • HY-114315
    NQO1 substrate

    Others Cancer
    NQO1 substrate acts as an efficient NQO1 substrate and may be a new option for the treatment of NQO1-overexpresssing drug-resistant NSCLC.
  • HY-A0086
    Netilmicin sulfate

    SCH-20569 sulfate

    Bacterial Antibiotic Infection
    Netilmicin (sulfate) (SCH-20569 (sulfate)) is an active aminoglycoside antibiotic against most Gram-negative and some Gram-positive bacteria, including certain strains resistant to gentamicin.
  • HY-N8186
    (3R)-7,4’-Dihydrohomoisoflavanone

    Bacterial Infection
    (3R)-7,4’-Dihydrohomoisoflavanone is a natural product with antibacterial activities against S. aureus and methicillin-resistant Staphylococcus aureus (MRSA).
  • HY-14800
    Radezolid

    RX-1741

    Bacterial Antibiotic Infection
    Radezolid (RX-1741) is a oxazolidinone antibiotic. Radezolid is active against Staphylococcus, Chlamydia, and Legionella species, and remains active against Linezolid-resistant strains.
  • HY-N3386
    Licoricone

    Bacterial Infection
    Licoricone is an flavonoid extracted from licorice, exhibits anti-helicobacter pylori activity against the CLAR and AMOX-resistant strain as well as four CLAR (AMOX)-sensitive strains.
  • HY-N2058
    Neogambogic acid

    Bacterial Apoptosis Cancer Infection
    Neogambogic acid, an active ingredient in garcinia, induces apoptosis and has anticancer effect. Neogambogic acid has significant inhibitory activity toward methicillin-resistant Staphylococcus aureus (MRSA).
  • HY-10844S
    Pretomanid-d4

    Bacterial Antibiotic Infection Cancer
    Pretomanid-d4 (PA-824-d4) is the deuterium labeled Pretomanid. Pretomanid (PA-824) is an antibiotic used for the research of multi-drug-resistant tuberculosis affecting the lungs. Pretomanid exhibits a sub-micromolar MIC against M. tuberculosis (MTB). The MIC values of PA-824 against a panel of MTB pan-sensitive and Rifampin mono-resistant clinical isolates range from 0.015 to 0.25 µg/mL.
  • HY-116387
    WR99210

    Antifolate Bacterial Infection
    WR99210 is a effective inhibitor of dihydrofolate reductase (DHFR) with an IC50 of <0.075 nM. WR99210 is effective against the most pyrimethamine-resistant Plasmodium falciparum strains.
  • HY-128873
    Duocarmycin GA

    ADC Cytotoxin DNA Alkylator/Crosslinker Cancer
    Duocarmycin GA is an antibody drug conjugates (ADCs) toxin. Duocarmycin is a DNA alkylating agent that binds in the minor groove. Duocarmycin GA can be used against multi-drug resistant cell lines.
  • HY-107770
    Duocarmycin MB

    ADC Cytotoxin DNA Alkylator/Crosslinker Cancer
    Duocarmycin MB is an antibody drug conjugates (ADCs) toxin. Duocarmycin is a DNA alkylating agent that binds in the minor groove. Duocarmycin MB can be used against multi-drug resistant cell lines.
  • HY-111503
    Y06137

    Epigenetic Reader Domain Cancer
    Y06137 is a potent and selective BET inhibitor for treatment of castration-resistant prostate cancer (CRPC). Y06137 binds to the BRD4(1) bromodomain with a Kd of 81 nM.
  • HY-135847
    Desmethyl ferroquine

    SSR97213

    Parasite Drug Metabolite Infection
    Desmethyl ferroquine (SSR97213) is the active and major metabolite of Ferroquine. Ferroquine is an antimalarial. Desmethyl ferroquine shows significant activity against Chloroquine-susceptible and resistant P. falciparum strains.
  • HY-18987
    Duocarmycin MA

    ADC Cytotoxin DNA Alkylator/Crosslinker Cancer
    Duocarmycin MA is an antibody drug conjugates (ADCs) toxin. Duocarmycin is a DNA alkylating agent that binds in the minor groove. Duocarmycin MA can be used against multi-drug resistant cell lines.
  • HY-B0255
    Adefovir dipivoxil

    GS 0840

    HBV Reverse Transcriptase Infection Cancer
    Adefovir dipivoxil, an adenosine analogue, is an oral prodrug of the nucleoside reverse transcriptase inhibitor Adefovir. Adefovir dipivoxil inhibits both the wild type and HBV Lamivudine-resistant strains.
  • HY-103048A
    PD-1/PD-L1-IN 3 TFA

    PD-1/PD-L1 Cancer
    PD-1/PD-L1-IN 3 TFA, a macrocyclic peptide, is a potent and selective inhibitor of the PD-1/PD-L1 and CD80/PD-L1 interactions extracted from patent WO2014151634A1, compound No.1. PD-1/PD-L1-IN 3 TFA interferes with PD-L1 binding to PD-1 and CD80 by binding to PD-L1, with IC50s of 5.60 nM and 7.04 nM, respectively. PD-1/PD-L1-IN 3 TFA can be used for the research of various diseases, including cancer and infectious diseases.
  • HY-131708A
    FNDR-20123

    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-103048
    PD-1/PD-L1-IN 3

    PD-1/PD-L1 Cancer
    PD-1/PD-L1-IN 3, a macrocyclic peptide, is a potent and selective inhibitor of the PD-1/PD-L1 and CD80/PD-L1 interactions extracted from patent WO2014151634A1, compound No.1. PD-1/PD-L1-IN 3 interferes with PD-L1 binding to PD-1 and CD80 by binding to PD-L1, with IC50s of 5.60 nM and 7.04 nM, respectively. PD-1/PD-L1-IN 3 can be used for the research of various diseases, including cancer and infectious diseases.
  • HY-P1629
    Temporin A

    Bacterial Fungal Antibiotic Infection
    Temporin A is a short alpha-helical antimicrobial peptide isolated from the skin of the frog Rana temporaria. Temporin A is effective against a broad spectrum of Gram-positive bacteria. Temporin A interacts directly with the cell membrane of the microorganism and it is non-toxic to erythrocytes at concentrations that are antimicrobial. Temporin A also has antifungal activities (against yeast-like Candida albicans).
  • HY-131708
    FNDR-20123 free base

    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-135578
    Artelinic acid

    Parasite Infection
    Artelinic acid, a derivative of Artemisinin, is an antimalarial drug for the treatment of multidrug resistant strains of Plasmodium falciparum. Artelinic acid can be administered by various routes of administration, including intravenous, intramuscular and oral routes.
  • HY-N2103
    Tenacissoside G

    Others Cancer
    Tenacissoside G is a C21 steroid from the stems of Marsdenia tenacissima. Tenacissoside G reverses multidrug resistance in P-glycoprotein (Pgp)-overexpressing multidrug-resistant cancer cells.
  • HY-N0876
    Arenobufagin

    Others Cancer
    Arenobufagin is a natural bufadienolide from toad venom; has potent antineoplastic activity against HCC HepG2 cells as well as corresponding multidrug-resistant HepG2/ADM cells.
  • HY-135336A
    (S)-Verapamil hydrochloride

    (S)-(-)-Verapamil hydrochloride

    Leukotriene Receptor Calcium Channel Apoptosis Cancer
    (S)-Verapamil hydrochloride (S(-)-Verapamil hydrochloride) inhibits leukotriene C4 (LTC4) and calcein transport by MRP1. (S)-Verapamil hydrochloride leads to the death of potentially resistant tumor cells.
  • HY-126320
    EGFR-IN-8

    EGFR c-Met/HGFR Cancer
    EGFR-IN-8 is a dual EGFR and c-Met inhibitor, compound 48. EGFR-IN-8 can be a promising candidate for further development to target EGFR TKI-resistant NSCLC.
  • HY-101287
    MPT0B392

    Microtubule/Tubulin JNK Apoptosis Caspase Cancer
    MPT0B392, an orally active quinoline derivative, induces c-Jun N-terminal kinase (JNK) activation, leading to apoptosis. MPT0B392 inhibits tubulin polymerization and triggers induction of the mitotic arrest, followed by mitochondrial membrane potential loss and caspases cleavage by activation of JNK and ultimately leads to apoptosis. MPT0B392 is demonstrated to be a novel microtubule-depolymerizing agent and enhances the cytotoxicity of sirolimus in sirolimus-resistant acute leukemic cells and the multidrug resistant cell line.
  • HY-B0334
    Sulbactam

    CP45899

    Bacterial Antibiotic Infection
    Sulbactam (CP45899) is a competitive, irreversible beta-lactamase inhibitor. Sulbactam shows antimicrobial activity against multidrug-resistant (MDR) acinetobacter calcoaceticus--Acinetobacter baumannii (Acb) complex.
  • HY-120924
    BRD9185

    Dihydroorotate Dehydrogenase DNA/RNA Synthesis Infection
    BRD9185 is a Dihydroorotate dehydrogenase (DHODH) inhibitor, with an EC50 of 16 nM against multidrug-resistant blood-stage parasites in vitro and is curative after just three doses in a P. berghei mouse model.
  • HY-109050
    Alobresib

    GS-5829

    Epigenetic Reader Domain Cancer
    Alobresib (GS-5829) is a BET bromodomain inhibitor, which represents a highly effective therapeutics agent against recurrent/chemotherapy resistant uterine serous carcinoma (USC) overexpressing c-Myc.
  • HY-15975
    GNF179

    Parasite Infection
    GNF179 is an optimized 8,8-dimethyl IP analog that exhibited the potency(4.8 nM against the multidrug resistant strain W2) in vitro metabolic stability and in vivo oral bioavailability.
  • HY-12459
    Pyrindamycin B

    Bacterial Infection
    Pyrindamycin B is an antibiotic, actives against gram-positive and gram-negative bacterias, and exhibits strong therapeutic effects against both drug-sensitive and resistant cells of P388 leukemia in mice.
  • HY-136595
    3,5-Difluoro-L-tyrosine

    Phosphatase Others
    3,5-Difluoro-L-tyrosine is a functional, tyrosinase-resistant mimetic of tyrosine. 3,5-Difluoro-L-tyrosine can be used to analyze the substrate specificity of protein tyrosine phosphatases (PTPs).
  • HY-13062A
    Daunorubicin

    Daunomycin; RP 13057; Rubidomycin

    Topoisomerase DNA/RNA Synthesis ADC Cytotoxin Autophagy Bacterial Antibiotic Cancer Infection
    Daunorubicin (Daunomycin; RP 13057; Rubidomycin) is a topoisomerase II inhibitor with potent antineoplastic activities. Daunorubicin (Daunomycin; RP 13057; Rubidomycin) inhibites DNA and RNA synthesis in sensitive and resistant Ehrlich ascites tumor cells.
  • HY-B0334A
    Sulbactam sodium

    CP45899 sodium

    Bacterial Antibiotic Infection
    Sulbactam (CP45899) sodium is a competitive, irreversible beta-lactamase inhibitor. Sulbactam sodium shows antimicrobial activity against multidrug-resistant (MDR) acinetobacter calcoaceticus--Acinetobacter baumannii (Acb) complex.
  • HY-N9441
    Ascr#7

    Others Others
    Ascr#7, an ascaroside, is a hormone of nematodes. Ascr#7 is expressed during nematode development. Ascarosides can induce formation of long-lived and highly stress resistant dauer larvae.
  • HY-N9386
    Tellimagrandin II

    Eugeniin

    Bacterial Antibiotic Infection Inflammation/Immunology
    Tellimagrandin II (Eugeniin), the first intermediate in the 4C1-glucose derived series of ellagitannins, also inhibits antibiotic resistance of drug-resistant Staphylococcus aureus.
  • HY-N6932
    Voacamine

    Cannabinoid Receptor P-glycoprotein Cancer Metabolic Disease
    Voacamine, an indole alkaloid, exhibits potent cannabinoid CB1 receptor antagonistic activity. Voacamine also inhibits P-glycoprotein (P-gp) action in multidrug-resistant tumor cells.
  • HY-107271
    Imperialine 3-β-D-glucoside

    Others Cancer
    Imperialine 3-β-D-glucoside is the glycoside of Imperialine. Imperialine 3-β-D-glucoside may exhibit anti-tumor properties against multi-drug resistant tumor cells.
  • HY-12904
    TCA1

    Bacterial Infection
    TCA1 is a small molecule with activity against drug-susceptible and -resistant Mycobacterium tuberculosis (Mtb). TCA1 inhibits enzymes involved in cell wall and molybdenum cofactor biosynthesis, such as DprE1 and MoeW.
  • HY-108689
    Broflanilide

    GABA Receptor Neurological Disease
    Broflanilide is a potential insecticide and metabolized to Desmethyl-Broflanilide, which is a potent antagonist at the insect resistant-to-dieldrin (RDL) GABA Receptor, and inhibits S. litura RDL GABAR, with an IC50 value of 1.3 nM.
  • HY-128938
    EC1167

    Others Cancer
    EC1167 is the linker for EC1169. EC1169 is prostate-specific membrane antigen targeting-tubulysin conjugate. EC1169 has the potential to treat recurrent metastatic, castration-resistant prostate cancer (MCRPC).
  • HY-111746
    CWHM-1008

    Parasite Infection
    CWHM-1008 is a potent and orally active antimalarial agent, with EC50 values of 46 and 21 nM against drug-sensitive Plasmodium falciparum 3D7 and drug-resistant Dd2 strains, respectively.
  • HY-125170
    Galiellalactone

    STAT Cancer
    Galiellalactone is a is a small non-toxic and non-mutagenic fungal metabolite, a selective inhibitor of STAT3 signaling, with an IC50 of 250-500 nM. Galiellalactone can be used to research castration-resistant prostate cancer.
  • HY-10392
    Sutezolid

    PNU-100480; U-100480; PF-02341272

    Bacterial Antibiotic Infection
    Sutezolid (PNU-100480), an orally active oxazolidinone antimicrobial agent, acts by inhibiting bacterial protein synthesis. Sutezolid has potent activity against mycobacteria, and is used for the research of drug-resistant tuberculosis.
  • HY-14814
    Delafloxacin

    RX-3341; WQ-3034; ABT492

    Bacterial Antibiotic Infection
    Delafloxacin (RX-3341; WQ-3034; ABT492) is a broad-spectrum fluoroquinolone antibiotic. Delafloxacin has a broad spectrum of activity that includes drug-resistant Staphylococcus aureus, Streptococcus pneumoniae, and Klebsiella pneumonia.
  • HY-N0944
    (-)-Heraclenol

    Others Cancer
    (-)-Heraclenol is a derivative of furocoumarin isolated from Ducrosia anethifolia. (-)-Heraclenol shows antiproliferative and cytotoxic activities on cancer cell lines.
  • HY-121295
    Roseoflavin

    Bacterial Infection
    Roseoflavin, a natural pigment originally isolated from Streptomyces davawensis, is an antimetabolite analog of Riboflavin and flavin mononucleotide that has antimicrobial properties.
  • HY-18702
    Targocil

    Bacterial Infection
    Targocil functions as a bacteriostatic inhibitor of wall teichoic acid (WTA) biosynthesis which can inhibit the growth of methicillin-susceptible S. aureus (MSSA) and methicillin-resistant S. aureus (MRSA) with MIC90s of 2 μg/ mL for both MRSA and MSSA.
  • HY-16662
    Oncrasin-1

    Ras Apoptosis Cancer
    Oncrasin-1 is a potent and effective anticancer inhibitor that kills various human lung cancer cells with K-Ras mutations at low or submicromolar concentrations; also led to abnormal aggregation of PKCι in nucleus of sensitive cells but not in resistant cells.
  • HY-P1872
    OV-1, sheep

    Bacterial Infection
    OV-1, sheep is an alpha-helical antimicrobial ovispirin peptide derived from SMAP29 peptide (sheep), which inhibits several antibiotic-resistant bacterial strains including mucoid and nonmucoid Pseudomonas aeruginosa.
  • HY-14737
    Ceftaroline fosamil

    TAK-599; PPI0903

    Bacterial Antibiotic Infection
    Ceftaroline fosamil (TAK-599), a cephalosporin derivative, is an N-phosphono prodrug of anti-methicillin-resistant Staphylococcus aureus (MRSA) T-91825. Ceftaroline fosamil can be used for the research of MRSA infection.
  • HY-19915A
    Contezolid acefosamil

    MRX-4

    Bacterial Antibiotic Infection Inflammation/Immunology
    Contezolid acefosamil (MRX-4) is the orally active prodrug of the active antimicrobial metabolite Contezolid (MRX-I), an oxazolidinone which shows potent in vitro activity against various multidrug-resistant Gram-positive bacteria, including MRSA.
  • HY-15980
    GNF179 (Metabolite)

    Parasite Infection
    GNF179 metabolite is the metabolite of GNF179, which is an optimized 8,8-dimethyl IP analog that exhibited the potency(4.8 nM against the multidrug resistant strain W2) in vitro metabolic stability and in vivo oral bioavailability.
  • HY-N6908
    Continentalic acid

    Bacterial Cancer Infection Inflammation/Immunology
    Continentalic acid from Aralia continentalis has minimum inhibitory concentrations (MICs) of approximately 8-16 µg/mL against S. aureus, including the Methicillin susceptible Staphylococcus aureus (MSSA) and Methicillin-resistant Staphylococcus aureus (MRSA) standard strains.
  • HY-124628
    IPI-9119

    Fatty Acid Synthase (FASN) Cancer
    IPI-9119 is an orally active, selective and irreversible FASN inhibitor with an IC50 of 0.3 nM in vitro biochemical assay. IPI-9119 inhibits tumor growth of castration-resistant prostate cancer (CRPC) xenografts mouse models.
  • HY-14738
    Ceftaroline fosamil inner salt

    TAK-599 free acid; PPI0903 free acid

    Bacterial Antibiotic Infection
    Ceftaroline fosamil (TAK-599) inner salt, a cephalosporin derivative, is an N-phosphono prodrug of anti-methicillin-resistant Staphylococcus aureus (MRSA) T-91825. Ceftaroline fosamil inner salt can be used for the research of MRSA infection.
  • HY-B0030
    D-Cycloserine

    iGluR Bacterial Antibiotic Infection Neurological Disease
    D-Cycloserine is an antibiotic which targets sequential bacterial cell wall peptidoglycan biosynthesis enzymes. D-Cycloserine is a partial NMDA agonist that can improve cognitive functions. D-Cycloserine can be used for multidrug-resistant tuberculosis research.
  • HY-N7010
    (-)-Corynoxidine

    AChE Bacterial Infection
    (-)-Corynoxidine is an acetylcholinesterase inhibitor with an IC50 value of 89.0 μM, isolated from the aerial parts of Corydalis speciosa. (-)-Corynoxidine exhibits antibacterial activities against Staphylococcus aureus and methicillin-resistant S. aureus strains in different degrees.
  • HY-112543
    S119-8

    Influenza Virus Infection
    S119-8 is a broad spectrum inhibitor of influenza A and B viruses, showing activity against multiple influenza B viruses and an oseltamivir-resistant influenza A virus, but does not inhibit a non-influenza virus, vesicular stomatitis nirus (VSV).
  • HY-B0770
    Artemotil

    β-Arteether; (+)-Arteether; Arteether

    Parasite Infection Cancer
    Artemotil (β-Arteether) has antimalarial activity for the treatment of chloroquine-resistant Plasmodium falciparum malaria with an IC50 of 1.61 nM. Artemotil also has central nervous system (CNS) neurotoxicity and anorectic toxicity in rats, dogs and monkeys.
  • HY-10088
    Zibotentan

    ZD4054

    Endothelin Receptor Apoptosis Cancer Endocrinology
    Zibotentan (ZD4054) is a potent, selective and orally active endothelin A (ETA) receptor antagonist with a Ki of 13 nM. Zibotentan has no inhibitory effect on ETB. Zibotentan has anticancer effects and can be used for castration-resistant prostate cancer (CRPC) research.
  • HY-110201
    Estrogen receptor modulator 1

    Estrogen Receptor/ERR Cancer
    Estrogen receptor modulator 1 (compound 18) is an orally active and selective estrogen receptor modulator (SERM), with a pIC50 of 0.46. Estrogen receptor modulator 1 induces regression of Tamoxifen-resistant, hormone independent xenograft tumors.
  • HY-130603
    DCZ0415

    NF-κB Apoptosis Cancer
    DCZ0415, a potent TRIP13 inhibitor, impairs nonhomologous end joining repair and inhibits NF-κB activity. DCZ0415 induces anti-myeloma activity in vitro, in vivo, and in primary cells derived from drug-resistant myeloma patients.
  • HY-128780
    SPR206

    Bacterial Cancer Infection
    SPR206, a polymyxin analogue, and shows antibiotic activity against multidrug resistant Gram-negative pathogen. The MIC values of SPR206 against Pseudomonas aeruginosa Pa14 and Acinetobacter baumannii NCTC13301 are both 0.125 mg/L.
  • HY-10528
    Tasquinimod

    ABR-215050

    HDAC Cancer
    Tasquinimod is an oral antiangiogenic agent, which has the potential for castration-resistant prostate cancer treatment. Tasquinimod binds to the regulatory Zn 2+ binding domain of HDAC4 with Kd of 10-30 nM. Tasquinimod also is a S100A9 inhibitor.
  • HY-14814A
    Delafloxacin meglumine

    ABT492 meglumine; RX-3341 meglumine; WQ-3034 meglumine

    Bacterial Antibiotic Infection
    Delafloxacin meglumine (ABT492 meglumine; RX-3341 meglumine; WQ-3034 meglumine) is a broad-spectrum fluoroquinolone antibiotic. Delafloxacin has a broad spectrum of activity that includes drug-resistant Staphylococcus aureus, Streptococcus pneumoniae, and Klebsiella pneumonia.
  • HY-N7047
    8-Epidiosbulbin E acetate

    Bacterial Infection
    8-Epidiosbulbin E acetate, a furanoid, is abundant in Dioscorea bulbifera L.. 8-Epidiosbulbin E acetate exhibits broad-spectrum plasmid-curing activity against multidrug-resistant (MDR) bacteria. 8-Epidiosbulbin E acetate induces liver injury in mice.
  • HY-130794
    ALK/ROS1-IN-1

    ALK ROS Cancer
    ALK/ROS1-IN-1 (compound 2e) is a potent and selective anti crizotinib-resistant ALK/ROS1 dual inhibitor, with IC50s of 0.174 μM and 0.530 μM for ALK and ROS1 enzyme, respectively.
  • HY-124325
    PIP-199

    DNA Alkylator/Crosslinker Cancer
    PIP-199 is a selective inhibitor of RMI (RecQ-mediated genome instability protein) core complex/MM2 interaction, with an IC50 of 36 μM. PIP-199 can be used for the research of sensitizing resistant tumors to DNA crosslinking chemotherapeutics.
  • HY-19915
    Contezolid

    MRX-I

    Bacterial Antibiotic Monoamine Oxidase Infection Inflammation/Immunology
    Contezolid (MRX-I), a new and oraly active oxazolidinone, is an antibiotic in study for complicated skin and soft tissue infections (cSSTI) caused by resistant Gram-positive bacteria. Contezolid (MRX-I) markedly reduces potential for myelosuppression and monoamine oxidase inhibition (MAOI).
  • HY-117407
    ALLO-2

    Smo Cancer
    ALLO-2 is a potent drug-resistant Smoothened (Smo) mutant antagonist that inhibits Smo agonist Hh-Ag1.5-induced luciferase expression in TM3-Gli-Luc cells with IC50 of 6 nM.
  • HY-N5109
    Cheilanthifoline

    Parasite Infection
    Cheilanthifoline, an alkaloid, is isolated from Corydalis calliantha. Cheilanthifoline exhibits antiplasmodial activities against Plasmodium falciparum, with IC50s of 0.90 μg/mL and 1.22 μg/mL for wild type (TM4) and multidrug resistant (K1) strains, respectively.
  • HY-10394
    Linezolid

    PNU-100766

    Bacterial Antibiotic Infection
    Linezolid (PNU-100766) is the first member of the class of oxazolidinone synthetic antibiotic. Linezolid acts by inhibiting the initiation of bacterial protein synthesis. Linezolid is used for the treatment of serious infections caused by Gram-positive bacteria that are resistant to several other antibiotics.
  • HY-14818A
    Laninamivir octanoate

    CS-8958

    Influenza Virus Infection
    Laninamivir octanoate (CS-8958), a prodrug of Laninamivir, is a long-acting neuraminidase (NA) inhibitor with anti-influenza virus activity. Laninamivir octanoate shows anti-influenza activity against Oseltamivir-resistant viruses, and also against the pandemic influenza viruses.
  • HY-19447A
    Besifovir Dipivoxil maleate

    LB80380 maleate

    HBV Infection
    Besifovir Dipivoxil maleate (LB80380 maleate) is an oral prodrug of LB80317. Besifovir Dipivoxil maleate (LB80380 maleate) is effective in hepatitis B virus (HBV) DNA suppression for both treatment-naive and lamivudine-resistant chronic hepatitis B (CHB) patients in preliminary studies[2]
  • HY-114147
    Tuberculosis inhibitor 3

    Bacterial Infection Inflammation/Immunology
    Tuberculosis inhibitor 3 (compound 2i) displays potent anti-TB activity (MIC < 0.016 µg/mL) against drug-sensitive/resistant MTB strains. Tuberculosis inhibitor 3 (compound 2i) shows acceptable PK profiles with oral bioavailability.
  • HY-15794
    Nemorubicin

    Methoxymorpholinyl doxorubicin; FCE 23762; PNU 152243

    Others Cancer
    Nemorubicin (Methoxymorpholinyl doxorubicin) is a Doxorubicin derivative with potent antitumor activity. Nemorubicin is highly cytotoxic to a variety of tumor cell lines presenting a multidrug-resistant phenotype. Nemorubicin requirs an intact nucleotide excision repair (NER) system to exert its activity.
  • HY-B0840
    Chlorfenapyr

    Others Others
    Chlorfenapyr is a pyrrole pro-insecticide that is metabolized in vivo into CL 303268 by mixed function oxidases. Chlorfenapyr is active against a variety of insects including those susceptible and resistant to pyrethroid and organophosphate insecticides. Formulations containing Chlorfenapyr have been used to control termites and in agriculture to control various insects.
  • HY-108024A
    Ganaplacide hydrochloride

    KAF156 hydrochloride; GNF156 hydrochloride

    Parasite Infection
    Ganaplacide (KAF156) hydrochloride is a first-in-class, orally active imidazolopiperazine antimalarial agent. Ganaplacide hydrochloride is active against a broad range of Plasmodium species, including drug-resistant parasites. Ganaplacide hydrochloride is parasiticidal against both asexual and sexual blood stages as well as the liver stages of the parasite.
  • HY-120504
    N-Acetyltyramine

    Bacterial Cancer Infection
    N-Acetyltyramine is a quorum-sensing inhibitor (QSI) compound produced by V. alginolyticus M3-10. N-Acetyltyramine is capable of inhibiting the QS of C. violaceum ATCC 12472. N-acetyltyramine reverses resistance in Doxorubicin-resistant leukemia P388 cells.
  • HY-N2264
    Wulignan A1

    Influenza Virus Infection
    Wulignan A1 is isolated from the stems of Schisandra henryi. Wulignan A1 exhibits anti-influenza virus H1N1 and H1N1-TR (a Tamiflu drug resistant virus strain) activities.
  • HY-13053
    Ro-0335

    Reverse Transcriptase Cancer
    RO-0335 is a novel and potent diphenylether nonnucleoside reverse transcriptase inhibitor(NNRTI). RO-0335 inhibits Wt HIV-1 with an IC50 of 1.1 nM and retained activity (IC50< 100 nM) against 92% of a large number of NNRTI-resistant clinical isolates.
  • HY-50846
    SCH772984

    ERK Cancer
    SCH772984 is a highly selective and ATP-competitive ERK inhibitor, with IC50s of 4 and 1 nM for ERK1 and ERK2, respectively. SCH772984 has antitumor activity in MAPK inhibitor-naïve and MAPK inhibitor-resistant cells containing BRAF or RAS mutations.
  • HY-109035
    Inarigivir soproxil

    SB9200

    HCV Infection
    Inarigivir soproxil is an agonist of innate immunity and shows potent antiviral activity against resistant hepatitis C virus (HCV) variants, with EC50s of 2.2 and 1.0 μM for HCV 1a/1b in cells of genotype 1 HCV replicon systems.
  • HY-126143
    CHMFL-ABL-039

    Bcr-Abl Cancer
    CHMFL-ABL-039 is a type II native ABL kinase and drug-resistant V299L mutant BCR-ABL inhibitor with the IC50s of 7.9 nM and 27.9 nM, respectively. CHMFL-ABL-039 is used in the research of chronic myeloid leukemia.
  • HY-14881
    Bedaquiline

    TMC207; R207910

    Bacterial Antibiotic Infection
    Bedaquiline (TMC207) is a diarylquinoline drug and inhibits Mycobacterium tuberculosis (Mtb) F1FO-ATP synthase through targeting of both the c- and the ε-subunit. Bedaquiline has uncoupler activity. Bedaquiline is used for the multi-drug resistant tuberculosis.
  • HY-12930
    SPR719

    VXc-486

    Topoisomerase Bacterial Infection
    SPR719 (VXc-486) is a gyrase B inhibitor, with bactericidal activity. SPR719 potently inhibits multiple drug-sensitive isolates and drug-resistant isolates of Mycobacterium tuberculosis, with MICs of 0.03 to 0.30 μg/ml and 0.08 to 5.48 μg/ml, respectively.
  • HY-135336AS
    (S)-Verapamil D7 hydrochloride

    (S)-(-)-Verapamil D7 hydrochloride

    Leukotriene Receptor Calcium Channel Apoptosis Cancer
    (S)-Verapamil D7 hydrochloride ((S)-(-)-Verapamil D7 hydrochloride) is a deuterium labeled (S)-Verapamil hydrochloride. (S)-Verapamil hydrochloride (S(-)-Verapamil hydrochloride) inhibits leukotriene C4 (LTC4) and calcein transport by MRP1. (S)-Verapamil hydrochloride leads to the death of potentially resistant tumor cells.
  • HY-125810
    4'-Ethynyl-2'-deoxyadenosine

    HIV Reverse Transcriptase Infection Inflammation/Immunology
    4'-Ethynyl-2'-deoxyadenosine (4'-E-dA), a nucleoside reverse transcriptase (RT) inhibitor, is an antiretroviral agent which is potent against drug-resistant HIV variants, with an EC50 of 98 nM in MT-4 cells for anti-HIV-1 activity.
  • HY-124663
    CBK289001

    Protease-Activated Receptor (PAR) Cancer
    CBK289001 is a tartrate-resistant acid phosphatase (TRAP/ACP5) inhibitor. CBK289001 inhibits TRAP 5b MV, TRAP 5b OX and TRAP 5a OX with IC50s of 125 µM, 4.21 µM and 14.2 µM, respectively.
  • HY-16745
    Lascufloxacin

    KRP-AM1977X

    Bacterial Infection
    Lascufloxacin (KRP-AM1977X) is a potent and orally active fluoroquinolone antibacterial agent. Lascufloxacin potently inhibits infections caused by various pathogens, including quinolone-resistant strains. Lascufloxacin has the potential for various infectious diseases treatment, including lower respiratory tract infections.
  • HY-N4302
    Monensin

    Bacterial Apoptosis Antibiotic Cancer Infection
    Monensin is a naturally occurring bioactive ionophore produced by Streptomyces spp. Monensin can bind protons and monovalent cations. Monensin exhibits a broad spectrum activity against opportunistic pathogens of humans in both drug sensitive and resistant strains. Monensin also induces apoptosis in multiple cancer cell lines.
  • HY-131976
    BVDV-IN-1

    DNA/RNA Synthesis Infection
    BVDV-IN-1 is a non-nucleoside inhibitor (NNI) of bovine viral diarrhea virus (BVDV), with an EC50 of 1.8 μM. BVDV-IN-1 directly binds to a hydrophobic pocket of the BVDV RdRp. BVDV-IN-1 has antiviral activity against BVDV resistant to NNI thiosemicarbazone (TSC).
  • HY-B0117D
    Tigecycline hydrate

    GAR-936 hydrate

    Bacterial Autophagy Antibiotic Infection
    Tigecycline hydrate (GAR-936 hydrate) is a broad spectrum glycylcycline antibiotic. Tigecycline hydrate is bacteriostatic, that inhibits protein synthesis by binding to the 30S ribosomal subunit of bacteria and thereby blocking entry of Aminoacyl-tRNA into the A site of the ribosome during prokaryotic translation. Tigecycline hydrate is active against resistant strains of Gram-positive and Gram-negative bacteria.
  • HY-B0334AS
    Sulbactam-d5 sodium

    Bacterial Antibiotic Infection
    Sulbactam-d5 sodium (CP45899-d5) sodium is the deuterium labeled Sulbactam sodium. Sulbactam (CP45899) sodium is a competitive, irreversible beta-lactamase inhibitor. Sulbactam sodium shows antimicrobial activity against multidrug-resistant (MDR) acinetobacter calcoaceticus--Acinetobacter baumannii (Acb) complex.
  • HY-124573
    OBI-3424

    TH-3424

    DNA Alkylator/Crosslinker Cancer
    OBI-3424 (TH-3424) is a prodrug that is selectively converted by AKR1C3 (aldo-keto reductase 1C3) to a potent DNA-alkylating agent. OBI-3424 can be used for hepatocellular carcinoma, castrate-resistant prostate cancer, and acute lymphoblastic leukemia (ALL) research.
  • HY-130613
    MAC-545496

    Bacterial Infection
    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).
  • HY-B0593
    Ceftazidime

    GR20263

    Bacterial Antibiotic Infection
    Ceftazidime (GR20263) is a third generation cephalosporin administered intravenously or intramuscularly. Ceftazidime has a broad spectrum of in vitro activity against Gram-positive and Gram-negative aerobic bacteria. Ceftazidime is particularly active against Enterobacteriaceae (including beta-lactamase-positive strains) and is resistant to hydrolysis by most beta-lactamases.
  • HY-139279
    TPX-0131

    ALK Cancer
    TPX-0131 is a potent, selective, CNS-penetrant and orally active inhibitor of wild-type ALK (IC50 of 1.4 nM) and ALK-resistant mutation, e.g. G1202R (IC50 of 0.3 nM), L1196M (IC50 of 0.3 nM). TPX-0131 has strong antitumor activities.
  • HY-B1751D
    Quinidine sulfate dihydrate

    Cytochrome P450 Cancer
    Quinidine sulfate dihydrate is a potent and selective inhibitor of cytochrome P450db and inhibits amphetamine metabolism in vivo. Quinidine sulfate dihydrate enhances the cytotoxicity of vincristine (VCR) in tumor cells and especially in VCR-resistant sublines of P388 leukemia (P388/VCR) and human myelogenous leukemia.
  • HY-B1369
    Imipenem monohydrate

    N-Formimidoyl thienamycin monohydrate

    Bacterial Antibiotic Infection
    Imipenem monohydrate, a member of the carbapenem class of antibiotics isolated from the soil organism Streptomyces cattleya, is an intravenous β-lactam antibiotic effective against a wide range of Gram-positive and Gram-negative bacteria, including several multi-drug resistant bacterial species. Imipenem acts as cell wall-targeting antibiotic.
  • HY-128910
    MC-VC(S)-PABQ-Tubulysin M

    Drug-Linker Conjugates for ADC Cancer
    MC-VC(S)-PABQ-Tubulysin M is a drug-linker conjugate for ADC with potent antitumor activity by using Tubulysin M (a tubulin inhibitor), linked via the ADC linker MC-VC(S)-PABQ. MC-VC(S)-PABQ-Tubulysin M is effective against multidrug-resistant lymphoma cell lines and tumors.
  • HY-N0315
    Allicin

    Diallyl thiosulfinate

    Bacterial Antibiotic Infection
    Allicin (diallyl thiosulfinate) is isolated from garlic including Diallyl monosulfide, Diallyl disulfide, Diallyl trisulfide, Diallyl tetrasulfide, and Methyl allyl disulphide etc. They accounts for 98% of the extract. Allicin (diallyl thiosulfinate) has highly potent antimicrobial activity, and inhibits growth of a variety of microorganisms, among them antibiotic-resistant strains.
  • HY-12458
    Pyrindamycin A

    DNA/RNA Synthesis Cancer Infection
    Pyrindamycin A is an antibiotic that inhibits DNA synthesis. Pyrindamycin A shows antitumor activities against murine leukemia, exhibits stronger cytotoxic activities towards murine and human tumor cell lines and especially towards doxorubicin-resistant cells, inhibits P388 and P388/ADR cells with the same IC50 of 3.9 μg/ml.
  • HY-B0593A
    Ceftazidime pentahydrate

    GR20263 pentahydrate

    Bacterial Antibiotic Infection
    Ceftazidime pentahydrate (GR20263 pentahydrate) is a third generation cephalosporin administered intravenously or intramuscularly. Ceftazidime pentahydrate has a broad spectrum of in vitro activity against Gram-positive and Gram-negative aerobic bacteria. Ceftazidime pentahydrate is particularly active against Enterobacteriaceae (including beta-lactamase-positive strains) and is resistant to hydrolysis by most beta-lactamases.
  • HY-10426
    XCT790

    Estrogen Receptor/ERR Autophagy Cancer
    XCT-790 is a potent and selective inverse agonist for ERRα with an IC50 value of 0.37 μM. XCT-790 induces cell death in chemotherapeutic resistant cancer cells. XCT-790 (Compound 12) is inactive against ERRγ and the estrogen receptors ERα and ERβ.
  • HY-13678
    Meropenem

    SM 7338

    Bacterial Antibiotic Infection
    Meropenem (SM 7338) is a carbapenem antibiotic with broad-spectrum antibacterial activity. Meropenem has activity against susceptible and resistant N. gonorrhoeae (MIC value of 0.02-0.06 mg/mL), H. influenzae (MIC value of 0.03-0.12 mg/mL), and H. ducreyi (MIC value of 0.015-0.12 mg/mL).
  • HY-139201
    Poly-D-lysine hydrobromide (MW 30000-70000)

    Others Cancer
    Poly-D-lysine hydrobromide (MW 30000-70000) is a synthetic polymeric substrate and is one of the most widely used substrate in neural cell culture. Poly-D-lysine hydrobromide (MW 30000-70000) removes proteinase K-resistant PrP from prion-infected SN56 neuroblastoma cells without affecting PrP C.
  • HY-106410A
    Zabofloxacin hydrochloride

    DW-224a

    Bacterial Topoisomerase Infection
    Zabofloxacin hydrochloride (DW-224a) is a potent and seletive inhibitor of the bacterial type II and IV topoisomerases. Zabofloxacin hydrochloride has excellent activity against gram-positive pathogens including Steptococcus aureusStreptococcus pyogenes and S.pneumonia. Zabofloxacin hydrochloride is a novel fluoronaphthyridone quinolone that is considered as an alternative antibiotic for treatment of quinolone-susceptible (QSSP) and quinolone-resistant gonorrhea (QRSP).
  • HY-128780B
    SPR206 acetate

    Bacterial Antibiotic Infection
    SPR206 acetate is a polymyxin analog with antibiotic activity against Gram-negative pathogens, including multidrug-resistant (MDR) variants. SPR206 acetate has an anti-bacterial infection effect by interacting with the bacterium’s outer membrane. The MIC values of SPR206 acetate against Pseudomonas aeruginosa Pa14 and Acinetobacter baumannii NCTC13301 are both 0.125 mg/L.
  • HY-12554
    Terlipressin

    Vasopressin Receptor Endocrinology Inflammation/Immunology Cardiovascular Disease
    Terlipressin is a vasopressin analogue with potent vasoactive properties. Terlipressin is a highly selective vasopressin V1 receptor agonist that reduces the splanchnic blood flow and portal pressure and controls acute variceal bleeding. Terlipressin exerts anti-inflammatory and anti-oxidative effects. Terlipressin has the potential for hepatorenal syndrome and norepinephrine-resistant septic shock research.
  • HY-124952
    iKIX1

    Fungal Infection
    iKIX1 is an antifungal agent and resensitizes drug-resistant C. glabrata to azole antifungals in vitro. iKIX1 inhibits the interaction between the KIX domain of the mediator subunit CgGal11A and the activation domain of CgPdr1, the IC50 and Ki values are 190.2 μM and 18 μM, respectively. iKIX1 is used for the study of multidrug resistance and C. glabrata infection.
  • HY-12554A
    Terlipressin acetate

    Vasopressin Receptor Endocrinology Inflammation/Immunology Cardiovascular Disease
    Terlipressin acetate is a vasopressin analogue with potent vasoactive properties. Terlipressin acetate is a highly selective vasopressin V1 receptor agonist that reduces the splanchnic blood flow and portal pressure and controls acute variceal bleeding. Terlipressin acetate exerts anti-inflammatory and anti-oxidative effects. Terlipressin acetate has the potential for hepatorenal syndrome and norepinephrine-resistant septic shock research.
  • HY-118341
    Clitocine

    Apoptosis Bcl-2 Family Cancer
    Clitocine, an adenosine nucleoside analog isolated from mushroom, is a potent and efficacious readthrough agent. Clitocine acts as a suppressor of nonsense mutations and can induce the production of p53 protein in cells harboring p53 nonsense-mutated alleles. Clitocine can induce apoptosis in multidrug-resistant human cancer cells by targeting Mcl-1. Anticancer activity.
  • HY-107662
    TCS PrP Inhibitor 13

    Apoptosis Cancer Infection
    TCS PrP Inhibitor 13, an antiprion agent, is a cellular prion protein (PrP C) inhibitor. TCS PrP Inhibitor 13, as a protease-resistant form of prion protein (PrP-res) accumulation inhibitor, shows an IC50 value of 3 nM in both ScN2a and F3 cell lines. TCS PrP Inhibitor 13 induces Schwannoma cells apoptosis.
  • HY-106410
    Zabofloxacin

    DW-224a Free base

    Bacterial Topoisomerase Infection
    Zabofloxacin (DW-224a Free base) is a potent and seletive inhibitor of the bacterial type II and IV topoisomerases. Zabofloxacin has excellent activity against gram-positive pathogens including Steptococcus aureusStreptococcus pyogenes and S.pneumonia. Zabofloxacin is a novel fluoronaphthyridone quinolone that is considered as an alternative antibiotic for treatment of quinolone-susceptible (QSSP) and quinolone-resistant gonorrhea (QRSP).
  • HY-133119
    PK150

    Bacterial Infection
    PK150, an analogue of Sorafenib, shows oral bioavailability and antibacterial activity against several pathogenic strains at submicromolar concentrations. PK150 inhibits Gram-positive Methicillin-sensitive S. aureus (MSSA), Methicillin-resistant S. aureus (MRSA), Vancomycin intermediate S. aureus (VISA) with MICs of 0.3, 0.3-1, 0.3 µM, respectively.
  • HY-N1074
    Warangalone

    Scandenolone

    Parasite PKA Infection Inflammation/Immunology
    Warangalone is an anti-malarial compound which can inhibit the growth of both strains of parasite 3D7 (chloroquine sensitive) and K1 (chloroquine resistant) with IC50s of 4.8 μg/mL and 3.7 μg/mL, respectively. Warangalone can also inhibit cyclic AMP-dependent protein kinase catalytic subunit (cAK) with an IC50 of 3.5 μM.
  • HY-15148
    Tipranavir

    PNU-140690

    HIV Protease HIV SARS-CoV Infection
    Tipranavir (PNU-140690) inhibits the enzymatic activity and dimerization of HIV-1 protease, exerts potent activity against multi-protease inhibitor (PI)-resistant HIV-1 isolates with IC50s of 66-410 nM. Tipranavir inhibits SARS-CoV-2 3CL pro activity.
  • HY-N2346
    Tubulysin E

    Microtubule/Tubulin Apoptosis Cancer
    Tubulysin E is a highly cytotoxic peptide isolated from the myxobacterial species Archangium geophyra and Angiococcus disciformis. Tubulysin displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the lower nanomolar range. Tubulysin E is a cytotoxic activity tubulysin which inhibits tubulin polymerization and leads to cell cycle arrest and apoptosis.
  • HY-121300
    Kendomycin

    (-)-TAN2162

    Antibiotic Bacterial Endothelin Receptor CGRP Receptor Cancer Infection
    Kendomycin ((−)-TAN 2162) is a polyketide antibiotic with remarkable antibacterial and cancer cells cytotoxic activities. Kendomycin tends to be bacteriostatic rather than bactericidal and inhibits the growth of the methicillin-resistant Staphylococcus aureus (MRSA) strain COL at a low concentration (MIC of 5 μg/mL). Kendomycin is a potent antagonist of the endothelin receptor and a calcitonin receptor agonist which plays its role as an anti-osteoporotic agent.
  • HY-B0509
    Amikacin hydrate

    BAY 41-6551 hydrate

    Bacterial Antibiotic Infection
    Amikacin hydrate (BAY 41-6551 hydrate) is an aminoglycoside antibiotic and a semisynthetic analog of kanamycin. Amikacin hydrate is bactericidal, acting directly on the 30S and 50S bacerial ribosomal subunits to inhibit protein synthesis. Amikacin hydrate is very active against most Gram-negative bacteria including gentamicin- and tobramycin-resistant strains. Amikacin hydrate also inhibits the infections caused by susceptible Nocardia and nontuberculous mycobacteria.
  • HY-124679
    DS86760016

    Bacterial Infection
    DS86760016 is a potent leucyl-tRNA synthetase (LeuRS) inhibitor with activity against multidrug-resistant (MDR) Gram-negative bacteria, such as Escherichia coli, Klebsiella pneumoniae, and Pseudomonas aeruginosa. DS86760016 inhibits LeuRS enzymes from Escherichia coli, Pseudomonas aeruginosa, and Acinetobacter baumannii, with IC50s of 0.38, 0.62, and 0.16 μM, respectively.
  • HY-13678A
    Meropenem trihydrate

    SM 7338 trihydrate

    Bacterial Antibiotic Infection
    Meropenem trihydrate (SM 7338 trihydrate) is a carbapenem antibiotic with broad-spectrum antibacterial activity. Meropenem trihydrate has activity against susceptible and resistant N. gonorrhoeae (MIC value of 0.02-0.06 mg/mL), H. influenzae (MIC value of 0.03-0.12 mg/mL), and H. ducreyi (MIC value of 0.015-0.12 mg/mL).
  • HY-N7049
    Tubulysin F

    Microtubule/Tubulin Apoptosis Cancer
    Tubulysin F is a highly cytotoxic peptide isolated from the myxobacterial species Archangium geophyra and Angiococcus disciformis. Tubulysin displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the lower nanomolar range. Tubulysin F is a cytotoxic activity tubulysin which inhibits tubulin polymerization and leads to cell cycle arrest and apoptosis.
  • HY-N7052
    Tubulysin I

    Microtubule/Tubulin Apoptosis Cancer
    Tubulysin I is a highly cytotoxic peptide isolated from the myxobacterial species Archangium geophyra and Angiococcus disciformis. Tubulysin displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the lower nanomolar range. Tubulysin I is a cytotoxic activity tubulysin which inhibits tubulin polymerization and leads to cell cycle arrest and apoptosis.
  • HY-107818
    4-Hydroxychalcone

    NF-κB Inflammation/Immunology Cardiovascular Disease
    4-Hydroxychalcone is a chalcone metabolite with anti-angiogenic and anti-inflammatory activities. 4-Hydroxychalcone suppresses angiogenesis by suppression of growth factor pathway with no signs of cytotoxicity. 4-Hydroxychalcone inhibits TNF-α induced NF-κB pathway activation and activates BMP signaling, reduces resistant hypertension (RH) by attenuating hyperaldosteronism and renal injury in mice.
  • HY-N7050
    Tubulysin G

    Microtubule/Tubulin Apoptosis Cancer
    Tubulysin G is a highly cytotoxic peptide isolated from the myxobacterial species Archangium geophyra and Angiococcus disciformis. Tubulysin displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the lower nanomolar range. Tubulysin G is a cytotoxic activity tubulysin which inhibits tubulin polymerization and leads to cell cycle arrest and apoptosis.
  • HY-125374
    Larotaxel

    XRP9881

    Apoptosis Cancer
    Larotaxel (XRP9881) is a taxane analogue with preclinical activity against taxane-resistant breast cancer. Larotaxel (XRP9881) exerts its cytotoxic effect by promoting tubulin assembly and stabilizing microtubules, ultimately leading to cell death by apoptosis. It presents the ability to cross the blood brain barrier and has a much lower affinity for P-glycoprotein 1 than Docetaxel.
  • HY-N2347
    Tubulysin C

    Microtubule/Tubulin Apoptosis Cancer
    Tubulysin C is a highly cytotoxic peptide isolated from the myxobacterial species Archangium geophyra and Angiococcus disciformis. Tubulysin displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the lower nanomolar range. Tubulysin C is a cytotoxic activity tubulysin which inhibits tubulin polymerization and leads to cell cycle arrest and apoptosis.
  • HY-A0248A
    Polymyxin B1

    Bacterial Infection
    Polymyxin B1 is a potent antimicrobial lipopeptide first derived from Bacilus polymyxa. Polymyxin B1 is the major component in Polymyxin B (HY-A0248). Polymyxin B1 can induce lysis of bacterial cells through interaction with their membranes. Polymyxin B1 has the potential for multidrug-resistant Gram-negative bacterial infections treatment.
  • HY-P1649
    SPR741

    NAB741

    Bacterial Antibiotic Infection
    SPR741 (NAB741) is a cationic peptide derived from polymyxin B and is a potentiator molecule. SPR741 increases the permeability of the outer membrane of Gram-negative bacteria and is used to treat severe Gram-negative bacteria infections. SPR741 inhibits multidrug-resistant Gram-negative bacteria. The spectrum of activity of the antibiotic can be widened when used in combination with SPR741.
  • HY-N7634
    Tectol

    Farnesyl Transferase Parasite Cancer Infection
    Tectol, isolated from Lippia sidoides, exhibits significant activity against human leukemia cell lines HL60 and CEM. Tectol is a farnesyltransferase (FTase) inhibitor with IC50s of 2.09 and 1.73 μM for human and T. brucei FTase, respectively. Tectol inhibits drug-resistant strain of P. falciparum (FcB1) with an IC50 of 3.44 μM.
  • HY-P1036
    Compstatin

    Complement System Others
    Compstatin, a 13-residue cyclic peptide, is a potent inhibitor of the complement system C3 with species specificity. Compstatin binds to baboon C3 and is resistant to proteolytic cleavage in baboon blood (similar to humans). Compstatin inhibits only the activation of primates’ complement system. Compstatin exhibits IC50 values of 63 μM and 12 μM for classical and alterative complement pathway, respectively.
  • HY-B0537A
    Pentamidine dihydrochloride

    MP-601205 dihydrochloride

    Parasite Fungal Phosphatase Bacterial Antibiotic Cancer Infection
    Pentamidine dihydrochloride (MP-601205 dihydrochloride) is an antimicrobial agent and interferes with DNA biosynthetics. Pentamidine dihydrochloride inhibits parasite Leishmania infantum with an IC50 of 2.5 μM. Pentamidine dihydrochloride is a potent and selective protein tyrosine phosphatases (PTPases) and phosphatase of regenerating liver (PRL) inhibitor. Pentamidine dihydrochloride has the potential for Gambian trypanosomiasis, antimony-resistant leishmaniasis, and Pneumocystis carinii pneumonia treatment. Antitumor and antibacterial activities.
  • HY-N7053
    Tubulysin M

    Microtubule/Tubulin Apoptosis Cancer
    Tubulysin M is a highly cytotoxic peptide isolated from the myxobacterial species Archangium geophyra and Angiococcus disciformis. Tubulysin displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the lower nanomolar range. Tubulysin M is a cytotoxic activity tubulysin which inhibits tubulin polymerization and leads to cell cycle arrest and apoptosis.
  • HY-P1649B
    SPR741 acetate

    NAB741 acetate

    Bacterial Antibiotic Infection
    SPR741 acetate (NAB741 acetate) is a cationic peptide derived from polymyxin B and is a potentiator molecule. SPR741 acetate increases the permeability of the outer membrane of Gram-negative bacteria and is used to treat severe Gram-negative bacteria infections. SPR741 acetate inhibits multidrug-resistant Gram-negative bacteria. The spectrum of activity of the antibiotic can be widened when used in combination with SPR741 acetate.
  • HY-B0537
    Pentamidine

    MP-601205

    Parasite Fungal Phosphatase Bacterial Antibiotic Cancer Infection
    Pentamidine (MP-601205) is an antimicrobial agent and interferes with DNA biosynthetics. Pentamidine inhibits parasite Leishmania infantum with an IC50 of 2.5 μM. Pentamidine is a potent and selective protein tyrosine phosphatases (PTPases) and phosphatase of regenerating liver (PRL) inhibitor. Pentamidine has the potential for Gambian trypanosomiasis, antimony-resistant leishmaniasis, and Pneumocystis carinii pneumonia treatment. Antitumor and antibacterial activities.
  • HY-N7051
    Tubulysin H

    Microtubule/Tubulin Apoptosis Cancer
    Tubulysin H is a highly cytotoxic peptide isolated from the myxobacterial species Archangium geophyra and Angiococcus disciformis. Tubulysin displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the lower nanomolar range. Tubulysin H is a cytotoxic activity tubulysin which inhibits tubulin polymerization and leads to cell cycle arrest and apoptosis.
  • HY-100348
    EPI-001

    Androgen Receptor PPAR Apoptosis Cancer
    EPI-001, a selective inhibitor of Androgen Receptor (AR), targets transactivation unit 5 (Tau-5) of the AR. EPI-001 can inhibit transactivation of the AR amino-terminal domain (NTD), with an IC50 of ~6 μM. EPI-001 is also a selective modulator of PPARγ. EPI-001 is active against castration-resistant prostate cancer.
  • HY-B0509B
    Amikacin disulfate

    BAY 41-6551 disulfate

    Bacterial Antibiotic Infection
    Amikacin disulfate (BAY 41-6551 dissulfate) is an aminoglycoside antibiotic and a semisynthetic analog of kanamycin. Amikacin disulfate is bactericidal, acting directly on the 30S and 50S bacerial ribosomal subunits to inhibit protein synthesis. Amikacin disulfate is very active against most Gram-negative bacteria including gentamicin- and tobramycin-resistant strains. Amikacin disulfate also inhibits the infections caused by susceptible Nocardia and nontuberculous mycobacteria.
  • HY-11079
    A-803467

    Sodium Channel Inflammation/Immunology Neurological Disease
    A-803467 is a potent and selective tetrodotoxin-resistant Nav1.8 sodium channel blocker (IC50=8 nM). A-803467 has shown significant anti-nociception in neuropathic and inflammatory pain models. A-803467 enhances the chemosensitivity of conventional anticancer agents through interaction with the ATP-binding cassette subfamily G member 2 (ABCG2) transporter.
  • HY-107813
    Amikacin sulfate

    BAY 41-6551 sulfate

    Bacterial Antibiotic Infection
    Amikacin sulfate (BAY 41-6551 sulfate) is an aminoglycoside antibiotic and a semisynthetic analog of kanamycin. Amikacin sulfate is bactericidal, acting directly on the 30S and 50S bacerial ribosomal subunits to inhibit protein synthesis. Amikacin sulfate is very active against most Gram-negative bacteria including gentamicin- and tobramycin-resistant strains. Amikacin sulfate also inhibits the infections caused by susceptible Nocardia and nontuberculous mycobacteria.
  • HY-16559A
    Riviciclib

    P276-00 free base

    CDK Cancer
    Riviciclib (P276-00 free base) is a potent cyclin-dependent kinase (CDK) inhibitor, which inhibits CDK9-cyclinT1, CDK4-cyclin D1, and CDK1-cyclinB with IC50s of 20 nM, 63 nM, and 79 nM, respectively. Riviciclib shows antitumor activity on cisplatin-resistant cells.
  • HY-128914
    Tubulysin

    Microtubule/Tubulin Cancer
    Tubulysin family of secondary metabolites are originally isolated from the myxobacteria Archangium geophyra and Angiococcus disciformis. These compounds are potent microtubule destabilizing agents with IC50 values in the picomolar range against many cancer cell lines, including those with multidrug resistant properties. Tubulysins have limited therapeutic utility due to severe toxicity, so Tubulysins are ideal candidates to be incorporated into molecule drug conjugate (SMDC) delivery system.
  • HY-138072
    EMI1

    EGFR Cancer
    EMI1 is an EGFR ex19del/T790M/C797S and EGFR L858R/T790M/C797S inhibitor. EMI1 can be used for the research of mutant EGFR-associated, drug-resistant non-small-cell lung cancer (NSCLC).
  • HY-A0035
    Faropenem

    Antibiotic Infection
    Faropenem is a potent and orally active beta-lactam antibiotic. Faropenem demonstrates broad-spectrum in vitro antimicrobial activity against many gram-positive and -negative aerobes and anaerobes. Faropenem is resistant to hydrolysis by nearly all beta-lactamases, including extended-spectrum beta-lactamases and AmpC beta-lactamases. Faropenem is developed as an oral prodrug, faropenem medoxomil, for the research of respiratory tract infections.
  • HY-16559
    Riviciclib hydrochloride

    P276-00

    CDK Apoptosis Cancer
    Riviciclib hydrochloride (P276-00) is a potent cyclin-dependent kinase (CDK) inhibitor, which inhibits CDK9-cyclinT1, CDK4-cyclin D1, and CDK1-cyclinB with IC50s of 20 nM, 63 nM, and 79 nM, respectively. Riviciclib hydrochloride (P276-00) shows antitumor activity on cisplatin-resistant cells.
  • HY-B0537B
    Pentamidine isethionate

    MP-601205 isethionate

    Parasite Fungal Phosphatase Bacterial Antibiotic Infection Cancer
    Pentamidine isethionate (MP-601205 isethionate) is an antimicrobial agent and interferes with DNA biosynthetics. Pentamidine isethionate inhibits parasite Leishmania infantum with an IC50 of 2.5 μM. Pentamidine isethionate is a potent and selective protein tyrosine phosphatases (PTPases) and phosphatase of regenerating liver (PRL) inhibitor. Pentamidine isethionate has the potential for Gambian trypanosomiasis, antimony-resistant leishmaniasis, and Pneumocystis carinii pneumonia treatment. Antitumor and antibacterial activities.
  • HY-P1036A
    Compstatin TFA

    Complement System Others
    Compstatin TFA, a 13-residue cyclic peptide, is a potent inhibitor of the complement system C3 with species specificity. Compstatin TFA binds to baboon C3 and is resistant to proteolytic cleavage in baboon blood (similar to humans). Compstatin TFA inhibits only the activation of primates’ complement system. Compstatin TFA exhibits IC50 values of 63 μM and 12 μM for classical and alterative complement pathway, respectively.
  • HY-P1649A
    SPR741 TFA

    NAB741 TFA

    Bacterial Antibiotic Infection
    SPR741 TFA (NAB741 TFA) is a cationic peptide derived from polymyxin B and is a potentiator molecule. SPR741 TFA increases the permeability of the outer membrane of Gram-negative bacteria and is used to treat severe Gram-negative bacteria infections. SPR741 TFA inhibits multidrug-resistant Gram-negative bacteria. The spectrum of activity of the antibiotic can be widened when used in combination with SPR741 TFA.
  • HY-N6680
    Virginiamycin S1

    Bacterial Antibiotic Infection
    Virginiamycin S1 is a cyclic hexadepsipeptide antibiotic, inhibits bacterial protein synthesis at the level of aminoacyl-tRNA binding and peptide bond formation. Virginiamycin S1 belongs to the type B compounds in the streptogramin family and is produced by Streptomyces virginiae, shows a strong bactericidal activity against a wide range of Gram-positive bacteria. Virginiamycin S1 together with virginiamycin M1 is more effective in treat multidrug-resistant bacterial infections[1][2].
  • HY-139554
    Zifanocycline

    KBP-7072

    Bacterial Infection
    Zifanocycline (KBP-7072) is a semisynthetic third-generation aminomethylcycline antibiotic that inhibits the normal function of the bacterial ribosome. Zifanocycline exhibits a broad spectrum of in vitro antibacterial activity against Gram-positive and Gram-negative bacteria, including many multidrug-resistant pathogens. Zifanocycline is available in both oral and injectable formulations. Zifanocycline can be used for the research of acute bacterial skin and skin structure infections, community-acquired bacterial pneumonia, and complicated intra-abdominal infections.
  • HY-N2348
    Tubulysin D

    Microtubule/Tubulin Apoptosis Cancer
    Tubulysin D is one of the most potent derivatives among the tubulysins isolated from the myxobacterial species Archangium geophyra and Angiococcus disciformis. Tubulysin D is a novel tetrapeptide that displays potent antitumor activity and leads to cell cycle arrest and apoptosis by inhibiting tubulin polymerization with an IC50 of 1.7 μM. Tubulysin displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the lower nanomolar range.
  • HY-128449
    Cephradine monohydrate

    Cefradine monohydrate

    Bacterial Antibiotic TOPK Infection Inflammation/Immunology
    Cephradine (Cefradine) monohydrate is a broad-spectrum and orally active cephalosporin. Cephradine monohydrate is active against both grampositive and gram-negative pathogens and effective in eradicating most penicillinase-producing organisms known to be resistant to penicillin G, penicillin V, and ampicillin. Cephradine monohydrate has been used in the research of genitourinary, gastrointestinal and respiratory tract infections, and in infections of the skin and soft tissues. Cephradine monohydrate blocks solar-ultraviolet induced skin inflammation through direct inhibition of TOPK.
  • HY-131003
    Taletrectinib

    DS-6051b; AB-106

    ROS Cancer
    Taletrectinib (DS-6051b) is a potent, orally active, and new-generation selective ROS1/NTRK inhibitor. Taletrectinib potently inhibits recombinant ROS1, NTRK1, and NTRK3 with IC50s of 0.207, 0.622, 2.28, and 0.98 nM, respectively. Taletrectinib also inhibits ROS1 G2032R and other Crizotinib-resistant ROS1 mutants.
  • HY-15298C
    Grazoprevir sodium salt

    MK-5172 sodium salt

    HCV HCV Protease SARS-CoV Infection
    Grazoprevir sodium salt (MK-5172 sodium salt) is a selective inhibitor of Hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants, with Kis of 0.01 nM (gt1b), 0.01 nM (gt1a), 0.08 nM (gt2a), 0.15 nM (gt2b), 0.90 nM (gt3a), respectively. Grazoprevir sodium salt inhibits SARS-CoV-2 3CL pro activity.
  • HY-131003A
    Taletrectinib free base

    DS-6051b free base; AB-106 free base

    ROS Cancer
    Taletrectinib (DS-6051b) free base is a potent, orally active, and new-generation selective ROS1/NTRK inhibitor. Taletrectinib free base potently inhibits recombinant ROS1, NTRK1, and NTRK3 with IC50s of 0.207, 0.622, 2.28, and 0.98 nM, respectively. Taletrectinib free base also inhibits ROS1 G2032R and other Crizotinib-resistant ROS1 mutants.
  • HY-15298B
    Grazoprevir hydrate

    MK-5172 hydrate

    HCV HCV Protease SARS-CoV Infection
    Grazoprevir hydrate (MK-5172 hydrate) is a selective inhibitor of Hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants, with Kis of 0.01 nM (gt1b), 0.01 nM (gt1a), 0.08 nM (gt2a), 0.15 nM (gt2b), 0.90 nM (gt3a), respectively. Grazoprevir hydrate inhibits SARS-CoV-2 3CL pro activity.
  • HY-120355A
    AP14145 hydrochloride

    Potassium Channel Cardiovascular Disease
    AP14145 hydrochloride is a potent KCa2 (SK) channel negative allosteric modulator with an IC50 of 1.1 μM for KCa2.2 (SK2) and KCa2.3 (SK3) channels. AP14145 hydrochloride inhibition strongly depends on two amino acids, S508 and A533 in the channel. AP14145 hydrochloride prolonged atrial effective refractory period (AERP) in rats and demonstrates antiarrhythmic effects in a Vernakalant-resistant porcine model of atrial fibrillation (AF).
  • HY-N1365
    Isoscopoletin

    6-Hydroxy-7-methoxycoumarin

    HBV Cancer Infection
    Isoscopoletin (6-Hydroxy-7-methoxycoumarin) is an active constituent in Artemisia argyi leaves. Isoscopoletin shows substantial inhibition against cell proliferation, with IC50s of 4.0 μM and 1.6 μM for human CCRF-CEM leukaemia cells and multidrug resistant subline CEM/ADR5000, respectively. Isoscopoletin (6-Hydroxy-7-methoxycoumarin) possesses inhibitory activity against HBV replication.
  • HY-18944
    FIT-039

    CDK HSV CMV DNA/RNA Synthesis Infection
    FIT-039 is a selective, ATP-competitive and orally active CDK9 inhibitor with an IC50 of 5.8 μM for CKD9/cyclin T1. FIT-039 does not inhibit other CDKs and other kinases. FIT-039 inhibits replication of HSV-1 (IC50 of 0.69 μM), HSV-2, human adenovirus, and human CMV. FIT-039 is a promising antiviral agent for inhibiting drug-resistant HSVs and other DNA viruses.
  • HY-15298
    Grazoprevir

    MK-5172

    HCV Protease HCV SARS-CoV Infection
    Grazoprevir (MK-5172) is a selective inhibitor of Hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants, with Kis of 0.01 nM (gt1b), 0.01 nM (gt1a), 0.08 nM (gt2a), 0.15 nM (gt2b), 0.90 nM (gt3a), respectively. Grazoprevir inhibits SARS-CoV-2 3CL pro activity.
  • HY-19617A
    EGFR-IN-1 hydrochloride

    EGFR Cancer
    EGFR-IN-1 hydrochloride is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 hydrochloride potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 hydrochloride displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity.
  • HY-15148S
    Tipranavir-d4

    HIV Protease HIV SARS-CoV Infection
    Tipranavir-d4 (PNU-140690-d4) is the deuterium labeled Tipranavir. Tipranavir (PNU-140690) inhibits the enzymatic activity and dimerization of HIV-1 protease, exerts potent activity against multi-protease inhibitor (PI)-resistant HIV-1 isolates with IC50s of 66-410 nM. Tipranavir inhibits SARS-CoV-2 3CL pro activity.
  • HY-15298A
    Grazoprevir potassium salt

    MK-5172 potassium salt

    HCV HCV Protease SARS-CoV Infection
    Grazoprevir potassium salt (MK-5172 potassium salt) is a selective inhibitor of Hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants, with Kis of 0.01 nM (gt1b), 0.01 nM (gt1a), 0.08 nM (gt2a), 0.15 nM (gt2b), 0.90 nM (gt3a), respectively. Grazoprevir potassium salt inhibits SARS-CoV-2 3CL pro activity.
  • HY-P2312
    Human β-defensin-3

    HβD-3

    Antibiotic Bacterial Infection
    Human β-defensin-3 (HβD-3) is an antibiotic anti-microbial peptide produced by epithelial cells with antimicrobial activities and reduces the effect of inflammatory cytokine responses. Human β-defensin-3 is against different microbes with IC90 values of 6-25 μg/ml.
  • HY-138671
    DprE1-IN-4

    Bacterial Infection
    DprE1-IN-4 is a potent and orally active noncovalent DprE1 inhibitor with an IC50 of 0.90 μg/mL. DprE1-IN-4 exhibits potent in vitro activity against M. tuberculosis H37Rv and drug-resistant tuberculosis strain with MIC values of 0.12 μg/mL and 0.24 μg/mL, respectively. DprE1-IN-4 displays acceptable pharmacokinetic property and shows significant bactericidal activity in an acute mouse model of tuberculosis.
  • HY-16764
    Avarofloxacin

    JNJ-Q2

    Bacterial Infection Inflammation/Immunology
    Avarofloxacin (JNJ-Q2) is a broad-spectrum fluoroquinolone antibacterial drug being developed for the treatment of acute bacterial skin and skin-structure infections and community-acquired pneumonia. Avarofloxacin (JNJ-Q2) is an aminoethylidenylpiperidine fluoroquinolone that demonstrates antibacterial effect against numerous Gram-positive bacteria with a mean 0.12 mg/L MIC90 value. Avarofloxacin (JNJ-Q2) has potential for treatment of methicillin-resistant Staphylococcus aureus (MRSA) infections.
  • HY-42424
    (S,R,S)-AHPC-Me hydrochloride

    VHL ligand 2 hydrochloride; E3 ligase Ligand 1

    Ligand for E3 Ligase Cancer
    (S,R,S)-AHPC-Me hydrochloride (VHL ligand 2 hydrochloride) is the (S,R,S)-AHPC-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC-Me hydrochloride can be used to synthesize ARV-771, a von Hippel-Landau (VHL) E3 ligase-based BET PROTAC degrader. ARV-771 potently degrades BET protein in castration-resistant prostate cancer (CRPC) cells with a DC50 <1 nM.
  • HY-42424A
    (S,R,S)-AHPC-Me dihydrochloride

    VHL ligand 2 dihydrochloride; E3 ligase Ligand 1 dihydrochloride

    Ligand for E3 Ligase Cancer
    (S,R,S)-AHPC-Me dihydrochloride (VHL ligand 2 dihydrochloride) is the (S,R,S)-AHPC-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC-Me dihydrochloride can be used to synthesize ARV-771, a von Hippel-Landau (VHL) E3 ligase-based BET PROTAC degrader. ARV-771 potently degrades BET protein in castration-resistant prostate cancer (CRPC) cells with a DC50 <1 nM.
  • HY-N2214
    7-O-Methylaloeresin A

    Bacterial Inflammation/Immunology
    7-O-Methylaloeresin A is 5-methylchromone glycoside isolated from Commiphora socotrana (Burseraceae). 7-O-Methylaloeresin A exhibits good activity against multiple drug resistant Staphylococcus aureus (NCTC 11994) and Salmonella typhimurium (ATCC 1255) with MIC values of 0.72 and 0.18 mM, respectively. 7-O-Methylaloeresin A has antioxidant activities, gives IC50 values of 0.026  mM and 0.021  mM for DPPH and 2-deoxyribose degradation assay, respectively.
  • HY-19617B
    EGFR-IN-1 TFA

    EGFR Cancer
    EGFR-IN-1 TFA is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 TFA potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 TFA displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity.
  • HY-19617
    EGFR-IN-1

    EGFR Cancer
    EGFR-IN-1 (compound 24) is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity.
  • HY-112078
    (S,R,S)-AHPC-Me

    VHL ligand 2; E3 ligase Ligand 1A

    Ligand for E3 Ligase Cancer
    (S,R,S)-AHPC-Me (VHL ligand 2) is the (S,R,S)-AHPC-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC-Me can be used to synthesize ARV-771, a von Hippel-Landau (VHL) E3 ligase-based BET PROTAC degrader. ARV-771 potently degrades BET protein in castration-resistant prostate cancer (CRPC) cells with a DC50 <1 nM.
  • HY-136522
    S2116

    Histone Demethylase Apoptosis Cancer
    S2116, a N-alkylated tranylcypromine (TCP) derivative, is a potent lysine-specific demethylase 1 (LSD1) inhibitor. S2116 increases H3K9 methylation and reciprocal H3K27 deacetylation at super-enhancer regions. S2116 induces apoptosis in TCP-resistant T-cell acute lymphoblastic leukemia (T-ALL) cells by repressing transcription of the NOTCH3 and TAL1 genes. S2116 significantly retardes the growth of T-ALL cells in xenotransplanted mice.
  • HY-123823
    Nitroaspirin

    NCX 4016

    COX Apoptosis Cancer
    Nitroaspirin (NCX 4016) is a nitric oxide (NO) donor and a nitro-derivative of Aspirin, which combines with Nitroaspirin to inhibit cyclooxygenase. Nitroaspirin (NCX 4016) has antithrombotic and anti-platelet properties and acts as a direct and irreversible inhibitor of COX-1. Nitroaspirin (NCX 4016) causes significant induction of cell cycle arrest and apoptosis in Cisplatin-resistant human ovarian cancer cells via down-regulation of EGFR/PI3K/STAT3 signaling and modulation of Bcl-2 family proteins.
  • HY-18299
    Purvalanol B

    NG 95

    CDK Parasite Cancer Infection
    Purvalanol B (NG 95) is a potent, selective, reversible and ATP-competitive inhibitor CDK, with IC50s of 6 nM, 6 nM, 9 nM, 6 nM for cdc2-cyclin B, CDK2-cyclin A, CDK2-cyclin E and CDK5-p35, respectively. Purvalanol B shows selectivity for CDK over a range of other protein kinases (IC50>1000 nM). Purvalanol B inhibits the growth a chloroquine-resistant strain of P. falciparum.
  • HY-136523
    S2157

    Histone Demethylase Apoptosis Cancer
    S2157, a N-alkylated tranylcypromine (TCP) derivative, is a potent lysine-specific demethylase 1 (LSD1) inhibitor. S2157 increases H3K9 methylation and reciprocal H3K27 deacetylation at super-enhancer regions. S2157 induces apoptosis in TCP-resistant T-cell acute lymphoblastic leukemia (T-ALL) cells by repressing transcription of the NOTCH3 and TAL1 genes. S2157 efficiently pass through the blood-brain barrier and can almost completely eradicate CNS leukemia in mice transplanted with T-ALL cells.
  • HY-16787
    ICA-121431

    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-101522
    CHMFL-EGFR-202

    EGFR BMX Kinase Btk MEK Cancer
    CHMFL-EGFR-202 is a potent, irreversible inhibitor of epidermal growth factor receptor (EGFR) mutant kinase, with IC50s of 5.3 nM and 8.3 nM for drug-resistant mutant EGFR T790M and WT EGFR kinases, respectively. CHMFL-EGFR-202 exhibits ∼10-fold selectivity for EGFR L858R/T790M against the EGFR wild-type in cells. CHMFL-EGFR-202 adopts a covalent “DFG-in-C-helix-out” inactive binding conformation with EGFR, with strong antiproliferative effects against EGFR mutant-driven nonsmall-cell lung cancer (NSCLC) cell lines.
  • HY-136265
    BC-LI-0186

    Aminoacyl-tRNA Synthetase Cancer
    BC-LI-0186 is a potent and selective inhibitor of Leucyl-tRNA synthetase (LRS; LeuRS) and Ras-related GTP-binding protein D (RagD) interaction (IC50=46.11 nM). BC-LI-0186 competitively binds to the RagD interacting site of LRS (Kd=42.1 nM) and has on effects on LRS-Vps34, LRS-EPRS, RagB-RagD association, mTORC1 complex formation or the activities of 12 kinases. BC-LI-0186 can effectively suppress the activity of cancer-associated MTOR mutants and the growth of rapamycin-resistant cancer cells. BC-LI-0186 is a promising agent for lung cancer research.