Search Result
Results for "
drug resistant
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
4
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-W016420
-
MK-0955 sodium
|
Bacterial
Antibiotic
|
Infection
Cancer
|
Fosfomycin (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-B1924
-
Desmethyl-vancomycin hydrochloride
|
Bacterial
Antibiotic
|
Infection
|
Norvancomycin hydrochloride is suitable for endocarditis, osteomyelitis, pneumonia, sepsis or soft tissue infections caused by Staphylococcus aureus (including methicillin-resistant strains and multi-drug-resistant strains).
|
-
-
- HY-B1075
-
MK-0955 calcium
|
Bacterial
Antibiotic
|
Infection
Cancer
|
Fosfomycin (MK-0955) calcium is a blood-brain barrier penetrating, broad-spectrum antibiotic by irreversibly inhibiting an early stage in cell wall synthesis. Fosfomycin 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-B0609
-
MK-0955 tromethamine
|
Bacterial
Antibiotic
|
Infection
Cancer
|
Fosfomycin (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-N0402
-
-
-
- HY-161602
-
|
EGFR
|
Cancer
|
EGFR/HER2-IN-13 (Compd 38) is an inhibitor of mutant EGFR/HER2s which are resistant to other drugs. EGFR/HER2-IN-13 can be used for cancer research .
|
-
-
- HY-161603
-
|
EGFR
|
Cancer
|
EGFR/HER2-IN-14 (Compd 46) is an inhibitor of mutant EGFR/HER2s which are resistant to other drugs. EGFR/HER2-IN-14 can be used for cancer research .
|
-
-
- HY-N2894
-
|
Parasite
|
Infection
|
Piperolactam A is a natural product that can be isolated from root of Piper betle. Piperolactam A exhibits promising leishmanicidal action against wild type and drug resistant strains of Leishmania donovani .
|
-
-
- HY-B1075A
-
MK-0955
|
Bacterial
Antibiotic
|
Infection
|
Fosfomycin (MK-0955) is a broad-spectrum antibiotic. Fosfomycin can cross blood-brain barrier penetrating, and irreversibly inhibits an early stage in cell wall synthesis. Fosfomycin shows anti-bacteria activity for a range of bacteria, including multidrug-resistant (MDR), extensively drug-resistant (XDR), and pan-drug-resistant (PDR) bacteria .
|
-
-
- HY-132972
-
|
TrxR
|
Cancer
|
TrxR-IN-2, a potential thioredoxin reductase (TrxR) inhibitor, represents a promising candidate drug for the chemoresearch of drug-resistant hepatocellular carcinoma.
|
-
-
- HY-B0317F
-
|
Calcium Channel
|
Infection
|
Amlodipine hydrochloride is a biologically active drug used to lower blood pressure and prevent chest pain. Amlodipine hydrochloride has shown synergistic effects with antimicrobial drugs in in vitro studies, especially against carbene peptide-resistant Acinetobacter baumannii. Amlodipine hydrochloride can be used in combination with other antibiotics to enhance the inhibitory effect against resistant bacteria. The use of amlodipine hydrochloride helps reduce the dosage requirements of the drug, reduce toxic effects, and delay the emergence of drug resistance .
|
-
-
- HY-100358
-
|
Parasite
|
Infection
|
AQ-13 dihydrochloride is an aminoquinoline antimalarial agent that is effective against drug-resistant strains of Plasmodium falciparum.
|
-
-
- HY-117742
-
|
Others
|
Others
|
DA-7867 is an antibacterial compound with activity against a wide range of bacteria, including drug-resistant bacteria. DA-7867 shows promising antibacterial activity against some clinically important pathogens, including drug-resistant bacteria. It is an amide analog of Tedizolid, reflecting the potential use of tetrazoles in the development of new antibacterial agents.
|
-
-
- HY-N8388
-
|
Bacterial
|
Infection
|
Collinin is a anti-tubercular agent, it can be isolated from leaves of Z. schinifolium. Collinin has an excellent anti-tuberculosis effect against multidrug-resistant (MDR), extensively drug-resistant (XDR) strains .
|
-
-
- HY-141862
-
|
Influenza Virus
|
Infection
|
Zanamivir–cholesterol conjugate is a long-acting neuraminidase inhibitor with potent efficacy against drug-resistant influenza viruses.
|
-
-
- HY-N11874
-
|
Others
|
Infection
|
Staphyloferrin A is a siderophore protein that can be combined with antibiotics to study drug-resistant bacteria that cause skin diseases .
|
-
-
- HY-B1075AS
-
MK-0955 (benzylamine)-13C3
|
Bacterial
Antibiotic
|
Infection
|
(Rac)-Fosfomycin (benzylamine)- 13C3 is the 13C labeled Fosfomycin[1]. Fosfomycin (MK-0955) is a broad-spectrum antibiotic. Fosfomycin can cross blood-brain barrier penetrating, and irreversibly inhibits an early stage in cell wall synthesis. Fosfomycin shows anti-bacteria activity for a range of bacteria, including multidrug-resistant (MDR), extensively drug-resistant (XDR), and pan-drug-resistant (PDR) bacteria[2][3].
|
-
-
- HY-B1075R
-
|
Bacterial
Antibiotic
|
Infection
Cancer
|
Fosfomycin (calcium) (Standard) is the analytical standard of Fosfomycin (calcium). This product is intended for research and analytical applications. Fosfomycin (MK-0955) calcium is a blood-brain barrier penetrating, broad-spectrum antibiotic by irreversibly inhibiting an early stage in cell wall synthesis. Fosfomycin 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-N10430
-
|
HIV
|
Infection
|
Patentiflorin A is a potent, broadspectrum HIV-1 inhibitor. Patentiflorin A also inhibits HIV drug-resistant strains .
|
-
-
- HY-146394
-
|
HBV
DNA/RNA Synthesis
|
Infection
|
HBV-IN-22 (Compound LC5f) is an inhibitor of HBV DNA replication with IC50 values of 0.71 μM and 0.84 μM against wild-type and agent resistant HBV strains, respectively .
|
-
-
- HY-107468
-
|
HIV Protease
|
Infection
Inflammation/Immunology
|
PL-100 is a potent HIV-1 protease inhibitor with a Ki of 36 pM and an EC50 of 16 nM. PL-100 inhibits viral replication by suppressing HIV-1 protease activity and demonstrates excellent antiviral efficacy against drug-resistant HIV strains. PL-100 can be used in research on drug-resistant HIV disease .
|
-
-
- HY-149762
-
|
Bacterial
|
Infection
|
IMBI (compound 32) is an antibacterial agent that inhibits quorum sensing (QS) against drug-resistant pathogens. IMBI inhibits biofilm formation of Salmonella marcescens and restores or increases its susceptibility to antimicrobial drugs .
|
-
-
- HY-B1924R
-
|
Bacterial
Antibiotic
|
Infection
|
Norvancomycin (hydrochloride) (Standard) is the analytical standard of Norvancomycin (hydrochloride). This product is intended for research and analytical applications. Norvancomycin hydrochloride is suitable for endocarditis, osteomyelitis, pneumonia, sepsis or soft tissue infections caused by Staphylococcus aureus (including methicillin-resistant strains and multi-drug-resistant strains).
|
-
-
- HY-N13147
-
|
Antibiotic
Bacterial
|
Infection
|
Tetromycin C5 is an antibiotic, that exhibits board-spectrum antibacterial activity against gram-positive bacteria and their drug-resistant bacteria .
|
-
-
- HY-16672
-
|
Bacterial
|
Infection
|
AVX 13616 shows the potent in vivo antibacterial activity of Avexa’s lead antibacterial candidate; particularly against drug-resistant Staphylococcus pathogens.
|
-
-
- HY-122073
-
|
Bacterial
|
Infection
|
Furalazine is an antimicrobial agent. Furalazine shows activity against drug-resistant strains of cholera bacteria. Furalazine has the potential for the research of cholera .
|
-
-
- HY-162926
-
|
Bacterial
|
Infection
|
Antituberculosis agent-12 (compound 3408) is a narrow-spectrum antituberculosis prodrug phosphate that has the ability to inhibit drug-resistant tuberculosis infection .
|
-
-
- HY-142545
-
|
Bacterial
|
Infection
|
Antibacterial agent 68 (compound 4d) is an antibacterial agent against drug-resistant Escherichia coli. Antibacterial agent 68 has low cytotoxicity and exerts strong antibacterial activities against multidrug-resistant Escherichia coli at low concentrations as 0.007 mM .
|
-
-
- HY-150554
-
|
Bacterial
|
Infection
|
Antitubercular agent-29 (compound 6xa) is a potent agent resistant (DR) Mycobacterium tuberculosis (Mtb) inhibitor with MIC of 0.03 μg/mL against agent-susceptible (DS)-Mtb strains, MIC of 0.03-0.06 μg/mL against DR-Mtb strains, and favourable selectivity (SI>40) against Vero cells .
|
-
-
- HY-151598
-
|
Bacterial
|
Infection
|
Pks13-TE inhibitor 2 (compound 32) is a 13-Thioesterase (Pks13-TE) inhibitor (IC50=1.30 μM). Pks13-TE inhibitor 2 shows good anti-tuberculosis activity against both agent-sensitive and drug-resistant Mtb strains (MIC=0.0039-0.0078 μg/mL). Pks13-TE inhibitor 2 can be used in studies of multidrug-resistant TB and extensively drug-resistant TB .
|
-
-
- HY-151599
-
|
Bacterial
|
Infection
|
Pks13-TE inhibitor 3 (compound 23) is a 13-Thioesterase (Pks13-TE) inhibitor (IC50=1.55 μM). Pks13-TE inhibitor 3 shows good anti-tuberculosis activity against both agent-sensitive and drug-resistant Mtb strains (MIC=0.0625-0.25 μg/mL). Pks13-TE inhibitor 3 can be used in studies of multidrug-resistant TB and extensively drug-resistant TB .
|
-
-
- HY-139863
-
|
Bacterial
|
Infection
|
Antibacterial agent 62 is a novel redox cycling antituberculosis chemotype with potent bactericidal activity against growing and nutrient-starved phenotypically drug-resistant nongrowing bacteria.
|
-
-
- HY-151102
-
|
Antibiotic
Bacterial
|
Infection
|
Fabimycin is a FabI inhibitor with potent antibacterial activity against gram-negative bacteria. Fabimycin is effective against drug-resistant gram-negative Infections in vivo .
|
-
-
- HY-P10027
-
|
Antibiotic
Bacterial
|
Infection
|
Clovibactin is an antibiotic for drug-resistant bacterial pathogens without detectable resistance. Clovibactin TFA inihibits cell wall synthesis by targeting pyrophosphate of peptidoglycan precursors .
|
-
-
- HY-147017
-
GSK286
|
Bacterial
|
Infection
Inflammation/Immunology
|
GSK2556286 (GSK286) is an orally active inhibitor of M. tuberculosis. GSK2556286 inhibits growth within human macrophages (IC50 = 0.07 μM). GSK2556286 is effective against both multidrug-resistant (MDR) or extensively drug-resistant (XDR) and agent-sensitive (DS) M. tuberculosis.
|
-
-
- HY-114315
-
|
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-149089
-
|
Bacterial
|
Infection
|
Antibacterial agent 138 has excellent antibacterial activity to multi-drug resistant bacteria. Antibacterial agent 138 inhibits bacterial protein synthesis but bacterial cell walls .
|
-
-
- HY-144215
-
|
HBV
|
Inflammation/Immunology
|
TLR8 agonist 4 showed effective inhibition on wild-type and drug-resistant (lamivudine and entecavir) HBV strains. The IC50 values are 0.15 and 0.10 respectively μM.
|
-
-
- HY-155283
-
|
Beta-lactamase
Bacterial
|
Infection
|
Zndm19 is a New Delhi Metallo-β-lactamase-1 (NDM-1) inhibitor. Zndm19 can be used for the research of drug-resistant bacterial infections .
|
-
-
- HY-N6054
-
|
Parasite
Topoisomerase
|
Infection
Inflammation/Immunology
|
Niranthin, a lignan with a wide spectrum of pharmacological activities. Niranthin is a potent and non-competitive inhibitor of heterodimeric type IB topoisomerase of L. donovani. Niranthin can be used for the research of drug-resistant leishmaniasis research.
|
-
-
- HY-16371
-
IDN 5109; BAY 59-8862
|
Microtubule/Tubulin
|
Cancer
|
Ortataxel (IDN 5109; BAY 59-8862) is a derivative of Paclitaxel (HY-B0015). Ortataxel exhibits activity against multiple drug-sensitive and resistant cancer cell lines .
|
-
-
- HY-N9386
-
-
-
- HY-145912
-
-
-
- HY-10844
-
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-155190
-
|
Bacterial
|
Infection
|
Antitubercular agent-39 (Compound P1) is a potent antitubercular agent. Antitubercular agent-39 is active against drug-resistant strains and drug-susceptible clinical isolates. Antitubercular agent-39 inhibits Mtb strain H37Rv with a MIC less than 1 μM .
|
-
-
- HY-122324A
-
(-)-(R)-Tylophorine; (-)-DCB-3500; (-)-NSC-717335
|
Others
|
Cancer
|
(-)-Tylophorine ((-)-(R)-Tylophorine) is a potent cytotoxic agent with activity against both drug-sensitive and multidrug-resistant cancer cell lines. (-)-Tylophorine has been explored in biomedical research for its anticancer applications .
|
-
-
- HY-N6611
-
|
IGF-1R
|
Infection
Inflammation/Immunology
Cancer
|
Chimaphilin is an IGF-1R inhibitor (IC50: 0.086 μM). Chimaphilin has antifungal, antioxidant and anticancer activities. Chimaphilin inhibits the growth of both drug-sensitive and drug-resistant osteosarcoma cell lines. Chimaphilin can induce cancer cell apoptosis. Chimaphilin is a main component of pyrola .
|
-
-
- HY-111023
-
TG-873870 malate
|
Antibiotic
Bacterial
|
Infection
|
Nemonoxacin (TG-873870) malate is a nonfluorinated quinolone antibiotic. Nemonoxacin malate has broad-spectrum activity against Gram-positive, Gram-negative and atypical pathogens. Nemonoxacin malate can inhibit drug-resistant Streptococcus pneumoniae and (HY-121544) Methicillin-resistant Staphylococcus aureus. Nemonoxacin malate can be used for the research of community-acquired pneumonia .
|
-
-
- HY-10392
-
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-111746
-
|
Parasite
|
Infection
|
CWHM-1008 is a potent and orally active antimalarial agent, with EC50 values of 46 and 21 nM against agent-sensitive Plasmodium falciparum 3D7 and drug-resistant Dd2 strains, respectively .
|
-
- HY-149585
-
|
Fungal
|
Infection
|
Chitin synthase inhibitor 14 (compound 4n) is chitin synthase (CHS) inhibitor. Chitin synthase inhibitor 14 has antifungal activity while possessed the potency against drug-resistant fungal variants .
|
-
- HY-P10210
-
|
Antibiotic
Bacterial
|
Infection
|
Paenilagicin is a Gram-positive active antibiotic with a unique diphosphorylated prenyl binding mechanism that does not induce drug resistance. Paenilagicin exhibits a MIC value of 2 μg/mL against multidrug-resistant Gram-positive bacteria .
|
-
- HY-161689
-
|
Bacterial
|
Infection
|
Antibacterial agent 220 is a potent antibacterial agent that can directly destroy bacterial cell membranes. Antibacterial agent 220 effectively combats Gram-positive and and Gram-negative pathogens, including drug-resistant strains .
|
-
- HY-14814
-
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-127079
-
|
Microtubule/Tubulin
|
Cancer
|
Epothilone F is a Microtubule/Tubulin-stabilizing agent with anti-tumor activity. Epothilone F inhibits the proliferation of breast cancer cells, non-small cell lung cancer cells, drug-resistant ovarian cancer cells .
|
-
- HY-118731
-
|
Reverse Transcriptase
|
Infection
|
TNK-6123 is a potent Emivirine (HY-15353) analogue with improved activity against drug-resistant HIV mutants. TNK-6123 improves activity against Lys103Asn mutant RT .
|
-
- HY-144391
-
|
Fungal
Antibiotic
|
Inflammation/Immunology
|
Chitin synthase inhibitor 1 is a potent and selective chitin synthase (CHS) inhibitor (IC50=0.12 mM). Chitin synthase inhibitor 1 has potent antifungal activity against drug-resistant fungi variants .
|
-
- HY-155691
-
|
HIV Protease
|
Infection
|
HIV-1 protease-IN-12 (compound 35b) is a HIV-1 protease inhibitor with an IC50 of 0.51 nM. HIV-1 protease-IN-12 also inhibits drug-resistant variant .
|
-
- HY-P10027A
-
|
Antibiotic
Bacterial
|
Infection
|
Clovibactin TFA is the TFA salt form of Clovibactin (HY-P10027). Clovibactin TFA is an antibiotic for drug-resistant bacterial pathogens without detectable resistance. Clovibactin TFA inihibits cell wall synthesis by targeting pyrophosphate of peptidoglycan precursors .
|
-
- HY-P10526
-
|
Bacterial
|
Infection
|
CRAMP (1-39) is an antimicrobial peptide. CRAMP (1-39) has shown potent bactericidal effects against multiple strains of Neisseria meningitidis in vitro. CRAMP (1-39) can be used to study drug-resistant bacterial infections .
|
-
- HY-149346
-
|
Bacterial
|
Infection
|
Mtb-IN-2 (compound 10c) is an antimicrobial agent against Mycobacterium tuberculosis (Mtb), without cytotoxicity. Mtb-IN-2 significantly decreases colony-forming units (CFU) in spleen of murine tuberculosis models, and distinguishes both drug-sensitive and drug-resistant Mtb H37Rv strains. Mtb-IN-2 affects methionine metabolism but not folate pathway directly.
|
-
- HY-146811
-
|
Bacterial
|
Inflammation/Immunology
|
HSGN-94 is a potent antimicrobial agent with lipoteichoic acid (LTA) biosynthesis inhibition. HSGN-94 inhibits drug-resistant Gram-positive bacteria with MIC values of 0.25-2 μg/mL. HSGN-94 inhibits biofilm formation of MRSA and Vancomycin-resistant Enterococci. HSGN-94 also inhibits pro-inflammatory cytokines, exhibits in vivo efficacy in an MRSA murine wound infection model .
|
-
- HY-14749AR
-
|
Parasite
|
Infection
|
Pyronaridine (tetraphosphate) (Standard) is the analytical standard of Pyronaridine (tetraphosphate). This product is intended for research and analytical applications. Pyronaridine tetraphosphate is an orally active Mannich base anti-malarial agent. Pyronaridine tetraphosphate is active against P. falciparum and Echinococcus granulosus infection .
|
-
- HY-14749A
-
|
Parasite
|
Infection
|
Pyronaridine tetraphosphate is an orally active Mannich base anti-malarial agent. Pyronaridine tetraphosphate is active against P. falciparum and Echinococcus granulosus infection .
|
-
- HY-14749
-
|
Parasite
|
Infection
|
Pyronaridine is an orally active Mannich base anti-malarial agent. Pyronaridine is active against P. falciparum and Echinococcus granulosus infection .
|
-
- HY-147988
-
|
DNA/RNA Synthesis
Bacterial
|
Infection
|
DNA Gyrase-IN-5 (Compound 8I-w) is a potent DNA gyrase inhibitor with an IC50 of 0.10 μM. DNA Gyrase-IN-5 shows antibacterial activities against wild type and drug-resistant strains .
|
-
- HY-155690
-
|
HIV Protease
|
Infection
|
HIV-1 protease-IN-11 (compound 34a) is a HIV-1 protease inhibitor with an IC50 of 0.41 nM. HIV-1 protease-IN-11 also exhibits significant activity against drug-resistant variant .
|
-
- HY-149936
-
|
HIV Protease
|
Infection
|
HIV-1 protease-IN-8 (compound 34b) is a potent HIV-1 protease inhibitor with an IC50 value of 0.32 nM. HIV-1 protease-IN-8 displays IC50s of 0.29 μM and 1.90 μM for wild-type HIV-1 (HIV-1NL4-3) and drug-resistant variant (HIV-1MDR), respectively. HIV-1 protease-IN-8 displays robust antiviral activity against both wild-type HIV-1 and drug-resistant variant .
|
-
- HY-167701
-
|
Others
|
Cancer
|
OBHSA is a selective estrogen receptor degrader (SERD) with specific degradation activity against estrogen receptor α (ERα). OBHSA has a significant inhibitory effect on the proliferation of various breast cancer cells, including tamoxifen-sensitive and drug-resistant breast cancer cells. OBHSA blocks the cell cycle by degrading cyclin D1, thereby overcoming tamoxifen resistance. OBHSA also triggers excessive activation of the unfolded protein response (UPR) by inducing an increase in intracellular reactive oxygen species, ultimately leading to cell apoptosis. OBHSA shows great potential in the development of novel inhibitory drugs against endocrine-resistant breast cancer .
|
-
- HY-14814A
-
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-117407
-
|
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-130603
-
DCZ0415
4 Publications Verification
|
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-143408
-
|
Bacterial
|
Infection
|
OYYF-175, an antimicrobial antifolate, is a dihydrofolate reductase (DHFR) inhibitor with an IC50 of 2.36 nM for Escherichia coli DHFR. OYYF-175 exhibits potent broad-spectrum antibacterial activities, especially against multi-drug resistant Gram-Negative-strains .
|
-
- HY-10844R
-
|
Bacterial
Antibiotic
|
Infection
Cancer
|
Pretomanid (Standard) is the analytical standard of Pretomanid. This product is intended for research and analytical applications. 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-155545
-
|
Fungal
|
Infection
|
Antifungal agent 60 (compound 16) is an inhibitor of ergosterol biosynthesis with broad-spectrum antifungal activity. Antifungal agent 60 inhibits 7 human pathogenic fungal species, 2 fluconazole-resistant C. albicans isolates and 2 multi-drug resistant Candida auris isolates. Antifungal agent 60 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-10844S
-
|
Isotope-Labeled Compounds
Bacterial
Antibiotic
|
Infection
Cancer
|
Pretomanid-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[1][2].
|
-
- HY-10844S1
-
PA-824-d5; (S)-PA 824-d5
|
Antibiotic
Bacterial
Isotope-Labeled Compounds
|
Infection
Cancer
|
Pretomanid-d5 is deuterated labeled Pretomanid (HY-10844). 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-150644
-
|
Others
|
Cancer
|
S07-2010 is a potent pan-AKR1C (aldo-keto reductase family 1 member C) inhibitor, with IC50 values of 0.19, 0.36, 0.47, and 0.73 μM for AKR1C3, AKR1C4, AKR1C1 and AKR1C2, respectively. S07-2010 induces apoptosis in A549/DDP cells. S07-2010 strengthens the cytotoxicity of chemotherapeutic agents in drug-resistant cells. S07-2010 significantly inhibits the proliferation of drug-resistant cells .
|
-
- HY-122268
-
|
HIV
|
Infection
|
QYL-685 is a Z-methenylcyclopropane nucleoside analog containing 2,6-diaminopurine, which has strong antiviral activity against HIV-1. QYL-685 showed activity against Zidovudine (HY-17413) resistant and Didanosine (HY-B0249) resistant HIV-1 infected clones in vitro. QYL-685 can be developed as a therapeutic drug for HIV-1 infection .
|
-
- HY-116794
-
2,2-Diphenylethyl isothiocyanate
|
Apoptosis
JNK
MDM-2/p53
Caspase
|
Cancer
|
SF5 (2,2-Diphenylethyl isothiocyanate) is a sulforaphane analog. SF5 inhibits apoptosis by the JNK-p53-caspase pathway. SF5 can be used as a new renal protective agent for drug-resistant acute renal disease .
|
-
- HY-N6054R
-
|
Parasite
Topoisomerase
|
Infection
Inflammation/Immunology
|
Niranthin (Standard) is the analytical standard of Niranthin. This product is intended for research and analytical applications. Niranthin, a lignan with a wide spectrum of pharmacological activities. Niranthin is a potent and non-competitive inhibitor of heterodimeric type IB topoisomerase of L. donovani. Niranthin can be used for the research of drug-resistant leishmaniasis research.
|
-
- HY-162508
-
|
Bacterial
|
Infection
|
KSK-104 has potent antibacterial activity against Mycobacterium tuberculosis (MIC=0.78 μM). The role of KSK-104 is mainly involved in the synthesis and recovery pathways of pyridoxal 5'-phosphate (PLP), PLP-dependent enzymes and oxidative stress networks. KSK-104, as a candidate molecule for novel anti-tuberculosis drugs, can be used to develop research against drug-resistant mycobacterium tuberculosis .
|
-
- HY-108024
-
KAF156; GNF156
|
Parasite
|
Infection
|
Ganaplacide (KAF156) is a first-in-class,
orally active imidazolopiperazine antimalarial agent.
Ganaplacide is active against a broad range of Plasmodium
species, including drug-resistant parasites. Ganaplacide is parasiticidal
against both asexual and sexual blood stages as well as the liver stages of the
parasite .
|
-
- HY-126143
-
|
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-108024A
-
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-N7305
-
|
P-glycoprotein
|
Cancer
|
Jatrophane 5 is a natural product of Jatropha carcas L. Jatrophane 5 has powerful inhibition of P-gp, higher than R(+)-verapamil (HY-14275) and Tariquidar (HY-10550) in colorectal multi-drug resistant cells (DLD1-TxR) .
|
-
- HY-124112
-
|
Parasite
|
Infection
|
PAM 1392 is active orally against Plasmodium berghei in mice, P. cynofologi and P. knowlesi in monkeys and Trypanosoma cruzi in tissue cultures of mice, and hemolytic streptococci in vitro. PAM 1392 has antimalarial and antitrypanosomal activities, which is proming for rasearch of drug-resistant malaria .
|
-
- HY-144694
-
|
HSP
HDAC
Fungal
|
Infection
|
HDAC/HSP90-IN-3 (compound J5) is a potent and selective fungal Hsp90 and HDAC dual inhibitor, with IC50 values of 0.83 and 0.91 μM, respectively. HDAC/HSP90-IN-3 shows antifungal activity against azole resistant C. albicans. HDAC/HSP90-IN-3 can suppress important virulence factors and down-regulate drug-resistant genes ERG11 and CDR1 .
|
-
- HY-15456
-
|
c-Met/HGFR
|
Cancer
|
NVP-BVU972 is an selective and potent Met inhibitor, with an IC50 of 14 nM. NVP-BVU972 also exhibits good anti-proliferative activity against Met with drug-resistant mutations and inhibits phosphorylation. NVP-BVU972 can be used in study of cancer .
|
-
- HY-12930
-
SPR719
4 Publications Verification
VXc-486
|
Topoisomerase
Bacterial
|
Infection
|
SPR719 (VXc-486) is a gyrase B inhibitor, with bactericidal activity. SPR719 potently inhibits multiple agent-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-14814S
-
RX-3341-d5; WQ-3034-d5; ABT492-d5
|
Isotope-Labeled Compounds
Bacterial
Antibiotic
|
Infection
|
Delafloxacin-d5 is deuterium labeled Delafloxacin. 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[1].
|
-
- HY-137960
-
|
Bacterial
|
Inflammation/Immunology
Cancer
|
O,O-Dimethyl-cannabigerol is a natural product from Cannabis sativa. O,O-Dimethyl-cannabigerol has an antibacterial effect on drug-resistant strains of Staphylococcus aureus (MIC ranging from 1 to 2 μg/mL) . O,O-Dimethyl-cannabigerol is a nonpsychoactive constituent .
|
-
- HY-114604
-
|
Others
|
Others
|
Propioxatin B is a tricyclic sesquiterpenoid compound isolated from the root of vetiver grass. It has anti-tuberculosis activity and inhibitory effects on a variety of drug-resistant mutants of Mycobacterium tuberculosis. In computer simulation docking studies, it showed binding affinity with bacterial DNA gyrase and has a certain safety in vivo.
|
-
- HY-123390
-
|
Bcr-Abl
Akt
|
Cancer
|
DB07107 is a potent agent resistant T315I mutant Bcr-Abl tyrosine kinase inhibitor. DB07107 is also a potent Akt1 inhibitor with an IC50 value of 360 nM .
|
-
- HY-12892
-
|
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 agent sensitive and multi-agent 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-160621
-
|
FGFR
|
Cancer
|
CXF-009 is a selective and covalent FGFR4 inhibitor, with the IC50 of 48 nM. CXF-009 targeting Cys477 and Cys552 of FGFR4, and can be used for the study of hepatocellular carcinoma .
|
-
- HY-147871
-
|
Bacterial
|
Infection
|
Antimycobacterial agent-3 (Compound 1h) is an antimycobacterial agent against both agent-sensitive MTB strain H37Rv and drug-resistant clinical isolates (MIC: < 0.029–0.110 μM). Antimycobacterial agent-3 shows low cell cytotoxicity .
|
-
- HY-162959
-
|
Bacterial
Topoisomerase
DNA/RNA Synthesis
|
Infection
|
BWC0977 is a potent bacterial topoisomerase inhibitor that inhibits bacterial DNA replication via inhibition of DNA gyrase and topoisomerase IV. BWC0977 exhibits a minimum inhibitory concentration (MIC90) of 0.03-2 µg/mL against MDR (Multi-Drug Resistant) Gram-negative bacteria .
|
-
- HY-168188
-
|
Cytochrome P450
|
Infection
|
CYP51-IN-21 (Compound A33) is a potent CYP51 inhibitor. CYP51-IN-21 shows excellent antifungal activities against pathogenic fungi and drug-resistant strains. CYP51-IN-21 inhibits the formation of fungal biofilm .
|
-
- HY-155054
-
|
Parasite
|
Infection
|
Cysteine protease inhibitor-3 (Compound 15) is a Cysteine protease inhibitor. Cysteine protease inhibitor-3 inhibits Pf3D7, PfW2, PfFP2 and PfFP3 with IC50s of 0.74 μM, 1.05 μM, 3.5 μM, and 4.9 μM, respectively. Cysteine protease inhibitor-3 has anti-plasmodial efficacy against both drug-sensitive and drug-resistant parasites .
|
-
- HY-P10540
-
|
Bacterial
|
Infection
|
Pantinin-2 is a cysteine-free toxic peptide found in the emperor scorpion (paninus imperator). Pantinin-2 has high activity against Gram-positive bacteria but weak activity against Gram-negative bacteria. Pantinin-2 also exhibits activity against Candida tropicalis and has relatively mild hemolytic activity against human erythrocytes. Pantinin-2 can be used in the development of antimicrobial drugs for drug-resistant pathogens .
|
-
- HY-14814R
-
|
Bacterial
Antibiotic
|
Infection
|
Delafloxacin (Standard) is the analytical standard of Delafloxacin. This product is intended for research and analytical applications. 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-117974
-
ETX2514
|
Bacterial
|
Infection
|
Durlobactam sodium salt (ETX2514) is a broad-spectrum β-lactamase inhibitor with IC50s of 4, 14 and 190 nM for Class A KPC-2, Class C AmpC and Class D OXA-24, respectively. For the treatment of drug-resistant Gram-negative bacteria including Acinetobacter baumannii .
|
-
- HY-162324
-
|
Survivin
|
Cancer
|
MX106-4C is a survivin inhibitor that selectively kills ABCB1-positive colorectal cancer cells. MX106-4C can exert synergistic anticancer effects with Doxorubicin or resensitize drug-resistant ABCB1 cells to Doxorubicin .
|
-
- HY-162822
-
|
P-glycoprotein
|
Cancer
|
P-gp modulator-5 (compound 25) is a modulator of P-gp and can inhibit the proliferation of multidrug resistant (MDR) tumors. P-gp modulator-5 inhibits the activity of drug efflux pumps in MDR cells, leading to a large accumulation of ROS and altered cell cycle profiles .
|
-
- HY-138627B
-
|
Others
|
Cancer
|
AST5902 mesylate is a principal metabolite of Alflutinib, exhibiting significant antineoplastic activity. AST5902 mesylate contributes to the overall pharmacological effects in the treatment of non-small cell lung cancer. AST5902 mesylate is involved in the response to activating EGFR mutations and can help overcome EGFR T790M drug-resistant mutations.
|
-
- HY-19895
-
|
Others
|
Infection
|
DS-8587 is a new fluoroquinolone with significant antibacterial activity. The MIC value of DS-8587 against clinically isolated amoxicillin-resistant Bacillus strains is superior to ciprofloxacin and levofloxacin. The antibacterial activity of DS-8587 is less affected by adeA/adeB/adeC or abeM efflux pumps, and has more advantages than ciprofloxacin. DS-8587 has a lower single-step mutation frequency than ciprofloxacin. DS-8587 may be an effective drug for inhibiting amoxicillin-resistant Bacillus infections .
|
-
- HY-150967
-
|
Bacterial
|
Infection
|
MmpL3-IN-1 (compound 32) is a potent Mycobacterial membrane protein large 3 (MmpL3) inhibitor. MmpL3-IN-1 has anti-tuberculosis activity with the MIC<0.016 μg/mL in M. tuberculosis and can be used in studies of drug-resistant tuberculosis .
|
-
- HY-151417
-
|
Fungal
|
Infection
|
Chitin synthase inhibitor 7 (compound 9c) is a potent chitin synthase (CHS) inhibitor with an IC50 value of 0.37 mM. Chitin synthase inhibitor 7 has broad-spectrum antifungal activity against drug-resistant fungi. Chitin synthase inhibitor 7 can be used in the research of fungi infection .
|
-
- HY-151416
-
|
Fungal
|
Infection
|
Chitin synthase inhibitor 6 (compound 9b) is a potent chitin synthase (CHS) inhibitor with an IC50 value of 0.21 mM. Chitin synthase inhibitor 6 has broad-spectrum antifungal activity against drug-resistant fungi. Chitin synthase inhibitor 6 can be used in the research of fungi infection .
|
-
- HY-149053
-
|
P-glycoprotein
|
Cancer
|
OY-101 is an orally active, potent and specific P-glycoprotein (P-gp) inhibitor. OY-101 can sensitize drug-resistant tumors and effectively reverse tumor multidrug resistance. OY-101 is improvements in water-solubility, cytotoxicity, and reversal activity compared to Tetrandrine (HY-13764) .
|
-
- HY-13574
-
VX 710-3
|
P-glycoprotein
|
Cancer
|
Biricodar dicitrate (VX 710-3) is the dicitrate salt form of Biricodar (HY-13574A). Biricodar dicitrate is an inhibitor for P-glycoprotein and multidrug resistance-associated protein 1 (MRP-1), which increases the accumulation of chemotherapy drugs within cancer cells and shows effective chemosensitizing activity in multidrug resistant cells .
|
-
- HY-168108
-
|
Fungal
|
Infection
|
Antifungal agent 115 (compound 8n) is a non-competitive chitin synthase (CHS) inhibitor with an IC50 of 93 μM. Antifungal agent 115 demonstrates good selectivity and broad-spectrum antifungal activity, exhibiting significant efficacy against drug-resistant fungi. Antifungal agent 115 can be utilized in fungi infection research .
|
-
- HY-139848
-
|
P-glycoprotein
|
Cancer
|
WS-898 is a highly effective ABCB1 inhibitor capable of reversing paclitaxel (PTX) resistance in drug-resistant SW620/Ad300, KB-C2, and HEK293/ABCB1 cells (IC50 = 5.0, 3.67, and 3.68 nM, respectively).
|
-
- HY-144341
-
|
Bacterial
|
Infection
|
DprE1-IN-1 is a potent, orally active DprE1 inhibitor with favorable hepatocyte stability, low cytotoxicity and low hERG channel inhibition. DprE1-IN-1 displays potent activity against both agent-susceptible and clinically isolated drug-resistant Tuberculosis strains with MICs10 CFU reduction in macrophages.
|
-
- HY-16566
-
Kanamycin A
|
Antibiotic
Bacterial
|
Infection
Inflammation/Immunology
|
Kanamycin (Kanamycin A) is an orally active antibacterial (gram-negative/positive bacteria) agent, inhibits translocation and causes misencoding by binding to the 70 S ribosomal subunit. Kanamycin shows good inhibitory activity to both M. tuberculosis (sensitive and drug-resistant ) and K. pneumonia, which can be used in studies of tuberculosis and pneumonia .
|
-
- HY-P5550
-
|
Influenza Virus
|
Infection
|
Urumin has antiviral activity against the human influenza A virus. Urumin inhibits the growth of PR8 influenza virus (IC50: 3.8 μM). Urumin targets the conserved stalk of H1 hemagglutini, and is effective at neutralizing drug-resistant H1 influenza viruses. Urumin protects naive mice from lethal influenza infection .
|
-
- HY-P10411
-
|
Bacterial
|
Infection
|
BING is an antimicrobial peptide that can be isolated from Japanese medaka fish. BING shows a broad-spectrum toxicity against pathogenic bacteria including drug-resistant strains. BING induces a deregulation of periplasmic peptidyl-prolyl isomerases in gram-negative bacteria, and reduces the RNA level of cpxR, which plays a crucial role in the development of antimicrobial resistance .
|
-
- HY-P10539
-
|
Bacterial
|
Infection
|
Hp1404 is a novel cationic antimicrobial peptide. Hp1404 has specific inhibitory activity against Gram-positive bacteria, including Staphylococcus aureus (MRSA) resistant to Laburnetin (HY-N7382). Hp1404 has antimicrobial activity, low toxicity, and is not prone to drug resistance, and can be used in the research of antimicrobial agents .
|
-
- HY-16566A
-
Kanamycin A sulfate
|
Bacterial
Antibiotic
|
Infection
|
Kanamycin (Kanamycin A) sulfate is an orally active antibacterial (gram-negative/positive bacteria) agent, inhibits translocation and causes misencoding by binding to the 70 S ribosomal subunit. Kanamycin sulfate shows good inhibitory activity to both M. tuberculosis (sensitive and drug-resistant ) and K. pneumonia, which can be used in studies of tuberculosis and pneumonia .
|
-
- HY-128910
-
|
Drug-Linker Conjugates for ADC
Microtubule/Tubulin
|
Cancer
|
MC-VC(S)-PABQ-Tubulysin M is a synthetic ADC drug-linker conjugate composed of the tubulin polymerization inhibitor Tubulysin M (an ADC Cytotoxin) (HY-N7053) and MC-VC(S)- PABQ (an ADC linker) is connected. MC-VC(S)-PABQ-Tubulysin M is effective against multidrug-resistant lymphoma cell lines and tumors .
|
-
- HY-124952
-
|
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-A0248B
-
|
Antibiotic
Bacterial
|
Infection
|
Polymyxin B2 is a polypeptide antibiotic that has antibacterial activity, particularly against gram-negative bacteria. Polymyxin B2 kills the bacteria by binding to lipopolysaccharide molecules on the bacterial cell membrane, disrupting the integrity of the cell membrane and causing the cell contents to leak. Polymyxin B2 can be used in antibiotic development and treatment of drug-resistant strains .
|
-
- HY-150045
-
|
Topoisomerase
Bacterial
|
Infection
|
TP0480066 is a selective topoisomerase II inhibitor with IC50s of 1.10 and 62.89 nM for DNA gyrase and topo IV, respectively. TP0480066 shows good activity of againsting various bacterial species including drug-resistant strains. TP0480066 also exhibits potent inhibitory activity to N. gonorrhoeae, can be used in study of gonorrhea .
|
-
- HY-157464
-
|
Others
|
Cancer
|
[Ru(phen)2(4-Me-Sal)]BF4 (compound 10), a Ru(II)-based polypyridyl complexe, displays outstanding antiproliferative activity against drug-sensitive CCRF-CEM and multidrug-resistant CEM/ADR5000 leukemia cells (IC50=0.52 μM and 5.56 μM, respectively) .
|
-
- HY-161984
-
|
HDAC
|
Infection
Others
|
HDAC-IN-76 (compound 6i) is a histone deacetylase (HDAC) inhibitor. HDAC-IN-76 IC50 values of 30 nM and 98 nM for Pf3D7 (chloroquine (HY-17589A) drug-susceptible strain) and PfDd2 (chloroquine (HY-17589A) drug-resistant strain), has a highly potent antimalarial activity against asexual blood-stage Plasmodium, respectively, and exhibits selective inhibition against parasites, with IC50 values of 7 nM and 9 nM for human HDAC1 and HDAC6, respectively, while inhibiting PfHDAC1 .
|
-
- HY-117746
-
|
Others
|
Infection
|
KSK120 is a potent inhibitor of drug-resistant infections with specific activity against Chlamydia trachomatis (C. trachomatis). KSK120 inhibits the developmental cycle of C. trachomatis, thereby reducing the infectivity of progeny bacteria. KSK120 targets the glucose-6-phosphate (G-6P) metabolic pathway of C. trachomatis, showing its potential application in antimicrobial inhibition. The mechanism of KSK120 may involve inhibition of the transcriptional machinery, which provides new ideas for the development of specific drugs against C. trachomatis infection .
|
-
- HY-N7634
-
|
Farnesyl Transferase
Parasite
|
Infection
Cancer
|
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-157045
-
|
ATP Synthase
|
Infection
|
ATP Synthesis-IN-1 (Compound 4), quinoline derivative, is a potent inhibitor of PA ATP synthesis activity. ATP Synthesis-IN-1 has PA ATP synthesis inhibition with IC50 value of 11.1μg/mL. ATP Synthesis-IN-1 also has antibacterial activity. ATP Synthesis-IN-1 can be used for the research of drug-resistant PA infection .
|
-
- HY-163030
-
|
Elastase
NF-κB
p38 MAPK
Bacterial
|
Infection
Inflammation/Immunology
|
LasB-IN-1 (compound 5f) is a potent and orally active inhibitor of LasB (IC50 = 8.7 μM). LasB-IN-1 effectively attenuates elastase production and biofilm formation by P. aeruginosa while alleviating the inflammatory response through downregulating MAPK and NF-κB pathways. LasB-IN-1 is potential to be a novel anti-infective candidate against drug-resistant infections .
|
-
- HY-109014
-
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-P3349
-
|
Bacterial
|
Infection
|
c[Arg-Arg-Arg-Arg-Nal-Nal-Nal] (Compound 9C) shows broad-spectrum activity against drug-resistant Gram-positive and Gram-negative bacteria, with MICs of 3.1, 3,1, 12.5, and 25 μg/mL for MRSA (ATCC BAA-1556), S. aureus (ATCC 29213), P. aeruginosa (ATCC 27883), and E. coli (ATCC 25922), respectively .
|
-
- HY-151606
-
|
Akt
|
Cancer
|
Akt3 degrader 1 (compound 12l) is a selective Akt3 degrader that overcomes Osimertinib (HY-15772)-induced resistance in H1975OR NSCLC cells. Akt3 degrader 1 also has anti-proliferative activity and significantly inhibits tumour growth in mice. Akt3 degrader 1 can be used in the study of drug-resistant non-small cell lung cancer .
|
-
- HY-122209
-
|
HBV
|
Infection
|
DVR-01 is a HBV inhibitor with EC50 values of 1.7 and 1.6 μM in AML12HBV10 and HepDES19 cells, respectively. DVR-01 shows antiviral activity against drug-resistant HBV mutants with EC50s of 2.403-3.273 μM. DVR-01 can be used for the research of HBV infection and related diseases .
|
-
- HY-U00244A
-
P2647 hydrochloride; BZQ hydrochloride; Benzoquinamide hydrochloride
|
Adrenergic Receptor
|
Cancer
|
Benzquinamide (P2647) is an antiemetic which can bind to the α2A, α2B, and α2C adrenergic receptors (α2-AR) with Ki values of 1,365, 691, and 545 nM, respectively. Benzquinamide also inhibits P-glycoprotein mediated drug efflux and potentiates anticancer agent cytotoxicity in multidrug resistant cells .
|
-
- HY-155510
-
|
Bacterial
|
Infection
|
DprE1-IN-5 (Compound 10) is a DprE1 inhibitor. DprE1-IN-5 has anti-TB activity against Mtb H37Rv strain (MIC: 4 μM). DprE1-IN-5 also has antimycobacterial activity against drug-resistant strains. DprE1-IN-5 has high microsomal stability .
|
-
- HY-138072
-
|
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-P3348
-
|
Bacterial
|
Infection
|
c[Arg-Arg-Arg-Arg-Dip-Dip-Dip] (Compound 8C) shows broad-spectrum activity against drug-resistant Gram-positive and Gram-negative bacteria, with MICs of 3.1, 3,1, 12.5, and 12.5 μg/mL for MRSA (ATCC BAA-1556), S. aureus (ATCC 29213), P. aeruginosa (ATCC 27883), and E. coli (ATCC 25922), respectively .
|
-
- HY-103255
-
|
Apoptosis
|
Cancer
|
CFM-4 is a potent small molecular antagonist of CARP-1/APC-2 binding. CFM-4 prevents CARP-1 binding with APC-2, causes G2M cell cycle arrest, and induces apoptosis with an IC50 range of 10-15 μM. CFM-4 also suppresses growth of drug-resistant human breast cancer cells .
|
-
- HY-151422
-
|
Fungal
|
Infection
Cancer
|
Chitin synthase inhibitor 12 is a chitin synthase inhibitor. Chitin synthase inhibitor 12 shows excellent inhibitory activity with an IC50 value of 0.16 mM. Chitin synthase inhibitor 12 also is a broad-spectrum antifungal agent and has significantly antifungal activity against drug-resistant fungal variants, such as C. albicans and C. neoformans. Chitin synthase inhibitor 12 can be used for the research of invasive fungal infections (IFIs) .
|
-
- HY-151420
-
|
Fungal
|
Infection
Cancer
|
Chitin synthase inhibitor 10 is a chitin synthase inhibitor. Chitin synthase inhibitor 10 shows excellent chitin synthase inhibitory activity with an IC50 value of 0.11 mM. Chitin synthase inhibitor 10 also is an antifungal agent and has significantly antifungal activity against drug-resistant fungal variants, such as C. albicans and C. neoformans. Chitin synthase inhibitor 10 can be used for the research of invasive fungal infections (IFIs) .
|
-
- HY-155512
-
|
Bacterial
|
Infection
|
DprE1-IN-7 (Compound 64) is a DprE1 inhibitor. DprE1-IN-7 has anti-TB activity against Mtb H37Rv strain (MIC: 1 μM). DprE1-IN-7 also has antimycobacterial activity against drug-resistant strains. DprE1-IN-7 has high microsomal stability and medium clearance .
|
-
- HY-155511
-
|
Bacterial
|
Infection
|
DprE1-IN-6 (Compound 56) is a DprE1 inhibitor. DprE1-IN-6 has anti-TB activity against Mtb H37Rv strain (MIC: 1 μM). DprE1-IN-6 also has antimycobacterial activity against drug-resistant strains. DprE1-IN-6 has high microsomal stability and medium clearance .
|
-
- HY-B1268
-
Dioctyl sulfosuccinate sodium salt
|
HSV
|
Others
|
Docusate Sodium (Dioctyl sulfosuccinate sodium salt) is one of the main components in stool softeners. Docusate Sodium is a sulfated surfactant and may inactivate viral pathogens by disrupting viral envelopes and/or denaturing/disassociating proteins. Docusate Sodium is effective in vitro against wild type and drug-resistant strains of HSV type 1 and 2. Docusate Sodium is an obesogen. Docusate Sodium with developmental exposure leads to increased adult adiposity, inflammation, metabolic disorder and dyslipidemia in offspring fed a standard diet in mice .
|
-
- HY-110354
-
G28UCM
|
Fatty Acid Synthase (FASN)
Bacterial
Antibiotic
|
Infection
Cancer
|
UCM05 (G28UCM) is a potent inhibitor of fatty acid synthase (FASN) shows activity against HER2+ breast cancer xenografts and is active in anti-HER2 drug-resistant cell lines. UCM05 is a Filamentous temperature-sensitive protein Z (FtsZ) inhibitor and inhibits the growth of the Gram-positive bacterium B. subtilis with MIC values of 100 μM but lack activity on the Gram-negative bacterium E. coli.
|
-
- HY-155152
-
|
P-glycoprotein
BCRP
|
Cancer
|
P-gp/BCRP-IN-2 (compound 15) is an oxadiazole derivative and a dual inhibitor of the ABC transporter P-glycoprotein (IC50: 1.6 nM) and BCRP (IC50: 600 nM). P-gp/BCRP-IN-2 also enhances the anti-proliferative effects of Doxorubicin (HY-15142A) in drug-resistant human adenocarcinoma colon cancer cell lines HT29/DX and MDCK-MDR1 cells .
|
-
- HY-146595
-
|
Bacterial
|
Infection
|
FtsZ-IN-1 is a potent FtsZ inhibitor with quinolinium ring. FtsZ-IN-1 has stronger antibacterial activity against Gram-positive bacteria with MICs of 0.5-8 μg/mL. FtsZ-IN-1 significantly causes cell elongation of B. subtilis by enhancing FtsZ polymerization. FtsZ-IN-1 exhibits low hemolytic toxicity and low tendency to induce agent resistance. FtsZ-IN-1 has against drug-resistant bacteria activity .
|
-
- HY-144069
-
|
Trk Receptor
Apoptosis
|
Cancer
|
Pan-Trk-IN-3 (Compound 11g) is a potent inhibitor of pan-Trk and their drug-resistant mutants with IC50 values of 2, 3, 2, 21, 26, 5, 7 and 6 nM against TrkA, TrkB, TrkC, TrkA G595R, TrkA G667C, TrkA G667S, TrkA F589L and TrkC G623R, respectively. Pan-Trk-IN-3 displays excellent antitumor activity and induces apoptosis .
|
-
- HY-P5704
-
|
Bacterial
|
Infection
|
K11 is an antimicrobial peptide. K11 is active against MDR/XDR K. pneumoniae isolates (MIC: 8-512 μg/mL), and inhibits bacterial biofilm formation. K11 can act synergistically with antibiotics (Chloramphenicol (HY-B0239), Meropenem (HY-13678), Rifampicin (HY-B0272), etc.) against drug-resistant K. pneumoniae. K11 has high thermal and wide pH stability .
|
-
- HY-105048A
-
|
Bacterial
|
Infection
|
Omiganan pentahydrochloride is a cationic peptide compound with a broad antibacterial profile. Omiganan pentahydrochloride is capable of inhibiting a variety of bacteria, including yeast, and is active against both gram-positive and gram-negative bacteria. Omiganan pentahydrochloride is able to interact with the bacterial cell membrane, causing the destruction of the cell membrane and the death of the bacteria. Omiganan pentahydrochloride can be used for the study of antimicrobial activity against pathogens commonly associated with catheter-associated infections, including strains with drug-resistant phenotypes .
|
-
- HY-16764A
-
JNJ-Q2 hydrochloride
|
Bacterial
|
Infection
Inflammation/Immunology
|
Acorafloxacin hydrochloride (JNJ-Q2 hydrochloride) is a broad-spectrum fluoroquinolone anti-bacterial drug being developed for the treatment of acute bacterial skin and skin-structure infections and community-acquired pneumonia .
Acorafloxacin hydrochloride (Avarofloxacin ) is an aminoethylidenylpiperidine fluoroquinolone that demonstrates antibacterial effect against numerous Gram-positive bacteria with a mean 0.12 mg/L MIC90 value .
Acorafloxacin hydrochloride (JNJ-Q2) has potential for treatment of methicillin-resistant Staphylococcus aureus (MRSA) infections .
|
-
- HY-125810
-
|
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 . 4'-Ethynyl-2'-deoxyadenosine is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-18944
-
|
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-138671
-
|
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-12108
-
|
HIV Integrase
HIV
|
Infection
|
S 1360 is a potent and selective inhibitor of HIV-1 integrase. S 1360 inhibits the catalytic activity of purified integrase (
IC50: 20 nM). The EC50, and CC50 of S 1360
in MTT assay (MT-4 cells infected with HIV-1 IIIB) are 200 nM and 12 μM, respectively. S 1360 has antiviral activity against both X4 tropic and R5 tropic strains, as well as NRTI, NNRTI and PI drug-resistant variants .
|
-
- HY-118013
-
|
Others
|
Infection
|
NDM-1 inhibitor-2 is an inhibitor of New Delhi metallo-β-lactamase-1 (NDM-1) and has the ability to inhibit NDM-1 activity. NDM-1 inhibitor-2 exhibits a good inhibitory effect on drug-resistant bacterial strains that overexpress NDM-1. When NDM-1 inhibitor-2 is used in combination with the carbapenem antibiotic meropenem, a favorable synergistic effect can be produced .
|
-
- HY-158106
-
|
CDK
|
Cancer
|
AZD8421 is a selective CDK2 inhibitor (IC50: 9 nM) with selectivity for CDK1, CDK4 and CDK6. AZD8421 inhibits cancer cell proliferation by inhibiting pRB phosphorylation, inducing cell cycle arrest and senescence. AZD8421 demonstrated promising single efficacy and synergy with CDK4/6 inhibitors such as Palbociclib (HY-50767) in in vivo breast and ovarian models. AZD8421 also has potent single-agent inhibitory activity against drug-resistant breast cancer cells.
|
-
- HY-B1268R
-
|
HSV
|
Others
|
Docusate (Sodium) (Standard) is the analytical standard of Docusate (Sodium). This product is intended for research and analytical applications. Docusate Sodium (Dioctyl sulfosuccinate sodium salt) is one of the main components in stool softeners. Docusate Sodium is a sulfated surfactant and may inactivate viral pathogens by disrupting viral envelopes and/or denaturing/disassociating proteins. Docusate Sodium is effective in vitro against wild type and drug-resistant strains of HSV type 1 and 2. Docusate Sodium is an obesogen. Docusate Sodium with developmental exposure leads to increased adult adiposity, inflammation, metabolic disorder and dyslipidemia in offspring fed a standard diet in mice .
|
-
- HY-P2312
-
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-B0766
-
SY801
|
Autophagy
Apoptosis
HBV
HCV
HSP
Reactive Oxygen Species
Bcl-2 Family
Glutathione S-transferase
p38 MAPK
NF-κB
Microtubule/Tubulin
ERK
JNK
TNF Receptor
Interleukin Related
CDK
Cyclin G-associated Kinase (GAK)
mTOR
P-glycoprotein
Ferroptosis
|
Infection
Inflammation/Immunology
Cancer
|
Bicyclol (SY801) is an orally active derivative of the traditional Chinese medicine Schisandra chinensis, which has antiviral, anti-inflammatory, immunomodulatory, antioxidant, anti-steatosis, anti-fibrotic and anti-tumor activities. Bicyclol regulates the expression of heat shock proteins and plays an anti-apoptosis role in hepatocytes. Bicyclol reduces the activation of NF-κB and the levels of inflammatory factors in hepatocytes infected with hepatitis C virus (HCV) by inhibiting the activation of the ROS-MAPK-NF-κB pathway, and prevents ferroptosis in acute liver injury. Bicyclol can change the expression of Mdr-1, GSH/GST and Bcl-2, increase the intracellular concentration of anticancer drugs, and sensitize drug-resistant cells to anticancer drugs. Bicyclol inhibits the proliferation of human malignant hepatoma cells by regulating the PI3K/AKT pathway and the Ras/Raf/MEK/ERK pathway. Bicyclol can be used in the study of chronic hepatitis, acute liver injury, nonalcoholic fatty liver disease, liver fibrosis and hepatocellular carcinoma .
|
-
- HY-153356
-
|
Apoptosis
|
Cancer
|
MRT-2359 is a potent, orally active and selective GSPT1 depressant (IC50: >30 nM and <300 nM) that specifically induces apoptosis dependent on protein translation. MRT-2359 exhibits significant and preferred anti-proliferative activity in a variety of cancer cell lines, especially MYC-driven cell lines, such as non-small cell lung cancer (NSCLC) and small cell lung cancer (SCLC) with high expression of N-Myc or L-Myc. MRT-2359 inhibits the growth of drug-resistant NSCLC and SCLC cells, making it suitable for cancer research .
|
-
- HY-164477
-
|
Androgen Receptor
|
Cancer
|
FL442 is an Androgen Receptor (AR) modulator. FL442 exhibits strong inhibitory effects in AR-dependent prostate cancer cells, showing similar inhibitory efficiency to traditional antiandrogen drugs Bicalutamide (HY-14249) and Enzalutamide (HY-70002), while maintaining antiandrogenic activity against the AR mutant F876L, which is highly resistant to Enzalutamide. Pharmacokinetic studies of FL442 in mice reveal a long half-life (8 hours), good targeting (prostate tissue), and metabolic stability, and it effectively inhibits LNCaP tumor growth at low plasma concentrations (30 ng/mL) .
|
-
- HY-153857
-
|
FLT3
|
Cancer
|
PHI-101 is an orally active FLT3 inhibitor that overcomes resistance to multiple drug-resistant mutations. PHI-101 potently inhibits FLT3 single activating mutations (ITD or TKD mutants) and has inhibitory activity against FLT3 double (ITD/D835Y or ITD/F691L) and triple (ITD/D835Y/F691L) resistance mutations. PHI-101 has potential for research in relapsed or refractory acute myeloid leukemia (AML) .
|
-
- HY-101522
-
|
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-19542
-
C6-Cer; N-Hexanoylsphingosine
|
Apoptosis
|
Cancer
|
C6 Ceramide (C6-Cer) is a short-chain, cell-permeable ceramide pathway activator with anticancer activity. C6 Ceramide-mediated miR-29b expression participates in the progression of multiple myeloma through suppressing the proliferation, migration and angiogenesis of endothelial cells by targeting Akt signal pathway. C6 Ceramide exhibits multiple anti-cancer properties including cell cycle arrest, Apoptosis, inhibition of tumor growth and enhances the effects of chemotherapy in drug-resistant cancer cells. C6-ceramide can be used as an adjuvant for chemotherapeutic agents, to enhance anti-tumor effects .
|
-
- HY-135748A
-
|
Toll-like Receptor (TLR)
Apoptosis
|
Infection
Cancer
|
Poly (I:C):Kanamycin (1:1) sodium is an isometric complex of Poly (I:C) (HY-135748) and Kanamycin (HY-16566). Poly(I:C) sodium, a synthetic analog of double-stranded RNA, is a TLR3 and retinoic acid-inducible gene I receptor (RIG-I and b>MDA5) agonist. Poly(I:C) sodium can be used as a vaccine adjuvant to enhance innate and adaptive immune responses and induce apoptosis in cancer cells . Kanamycin is an orally active antibacterial agent (Gram-negative/positive bacteria) that inhibits translocation and causes miscoding by binding to the 70S ribosomal subunit. Kanamycin shows good inhibitory activity against Mycobacterium tuberculosis (susceptible and drug-resistant) and Klebsiella pneumoniae, and can be used in the research of tuberculosis and pneumonia .
|
-
- HY-162464
-
|
PROTACs
SARS-CoV
|
Infection
|
MPD2 is a Cereblon-binding ligand-based PROTAC that degrades MPro, the main protease of SARS-CoV-2. MPD2 effectively reduced MPro protein levels in 293T cells in a time-dependent manner (DC50=296 nM). MPD2 exhibited potent antiviral activity against multiple SARS-CoV-2 strains and had enhanced potency against Nirmatrelvir (HY-138687) resistant strains. MPD2 provides a new direction for antiviral drug development against SARS-CoV-2 and other emerging coronavirus pathogens (Sturcture Note:(Blue: Cereblon ligand (HY-14658), Black: linker (HY-W275882);Red: SARS-CoV-2 MPro Inhibitor MP18 (HY-158763)) .
|
-
- HY-121656
-
|
Others
|
Cancer
|
AKR1C2/3-IN-2 is a potential AKR1C3 inhibitor with selective AKR1C3 activity. AKR1C2/3-IN-2 is able to block AKR1C3-mediated testosterone (T) production and PSA induction, affecting the endocrine activity of prostate cancer cells. AKR1C2/3-IN-2 shows selectivity over other AKR1C enzymes, indicating its potential application in inhibiting drug-resistant prostate cancer. AKR1C2/3-IN-2 has no inhibitory activity against COX isomerases, further emphasizing its specificity as a prostate cancer inhibitory compound .
|
-
-
-
HY-L169
-
|
409 compounds
|
Resistance refers to the decrease in the effectiveness of drugs in treating diseases or symptoms. Due to the increasing global antibiotic resistance, it may threaten our ability to treat common infectious diseases. Drug resistance is also the main cause of chemotherapy failure in malignant tumors. In approximately 50% of cases, drug resistance exists even before chemotherapy begins. There are many mechanisms of anticancer drug resistance, including increased protein expression that leads to drug removal, mutations in drug binding sites, recovery of tumor protein production, and pre-existing genetic heterogeneity in tumor cell populations. In addition, the issue of drug resistance seems to have affected the development of new anticancer drugs. Drug resistance may be caused by various conditions, such as mutations, epigenetic modifications, and upregulation of drug efflux protein expression. Overcoming multidrug resistance in cancer treatment is becoming increasingly important.
MCE designs a unique collection of 409 anti-drug-resistant compounds. It is a good tool to be used for research on cancer and other diseases.
|
-
-
HY-L142
-
|
103 compounds
|
Tuberculosis (TB), usually caused by bacteria (Mycobacterium tuberculosis), is an infectious disease that mainly affects the lungs. According to the statistics of the World Health Organization (WHO), 10 million people suffer from tuberculosis every year, and 1.5 million people die of tuberculosis every year, which makes tuberculosis the number one killer of infectious diseases.
Tuberculosis can be cured through the standard 6-month course of treatment of four kinds of antibiotics. Common drugs include rifampicin and isoniazid. In some cases, TB bacteria do not respond to standard drugs, that is, patients with drug-resistant tuberculosis. The treatment of drug-resistant tuberculosis takes longer and is more complex. In the face of the resurgence of tuberculosis in the world and the rapid emergence of multi drug resistant tuberculosis, it is very important to develop new anti-tuberculosis drugs or new clinical treatment schemes for existing anti mycobacterium drugs.
MCE supplies a unique collection of 103 compounds with clear anti-tuberculosis activity. MCE Anti-tuberculosis Compound Library is a useful tool for anti-tuberculosis related research and anti-tuberculosis drug development p>
|
-
-
HY-L049
-
|
1,401 compounds
|
Antibacterial agents are a group of materials that fight against pathogenic bacteria. Thus, by killing or reducing the metabolic activity of bacteria, their pathogenic effect in the biological environments will be minimized. The most widely used antibacterial agents exert their effects on bacterial cell wall synthesis, protein synthesis, DNA replication and metabolic pathways. However, resistance to antimicrobial agents has become a major source of morbidity and mortality worldwide. The main mechanisms of resistance are limiting uptake of a drug, modification of a drug target, inactivation of a drug, and active efflux of a drug. Therefore, it is an urgent need to develop new drugs targeted at resistant organisms.
MCE offers a unique collection of 1,401 compounds with validated antibacterial activities. MCE antibacterial compound library is an effective tool for drug repurposing screening, combination screening and biological investigation.
|
-
-
HY-L065
-
|
2,913 compounds
|
Chinese herbal therapy is an important part of Traditional Chinese Medicine (TCM). It has been used for centuries in China, where herbs are considered fundamental therapy for many acute and chronic conditions. Many studies indicated TCM exerted an overall regulatory effect via multi-component and multi-target network. Active components from Traditional Chinese Medicine possess many medicinal properties such as antioxidant, anti-cancer, and anti-bacterial effects, which makes it an important source of new drugs. Nearly 200 modern medicines have been developed either directly or indirectly from the plants used as medicines in China. For example, artemisinin, used in multidrug resistant malaria, was first isolated from the Chinese herb Artemisia annua L. Today, scientists continue to identify compounds in Chinese herbal remedies that may be useful in the development of new therapeutic agents applicable in Western medicine.
MCE designs a unique collection of 2,913 active compounds of Chinese Herbal Medicines. MCE Traditional Chinese Medicine Active Compound Library is a useful tool for discovery new drugs from TCM.
|
Cat. No. |
Product Name |
Type |
-
- HY-69174
-
|
Microbial Culture
|
1-Amino-2,5-anhydro-1-deoxy-D-mannitol is a potent antibacterial compound with antibacterial activity against a variety of Gram-positive bacteria, including methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococci (VRE). The application potential of 1-Amino-2,5-anhydro-1-deoxy-D-mannitol lies in its ability to effectively combat common drug-resistant bacterial infections. 1-Amino-2,5-anhydro-1-deoxy-D-mannitol may become an emerging antibacterial agent in clinical inhibition.
|
Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P10027A
-
|
Antibiotic
Bacterial
|
Infection
|
Clovibactin TFA is the TFA salt form of Clovibactin (HY-P10027). Clovibactin TFA is an antibiotic for drug-resistant bacterial pathogens without detectable resistance. Clovibactin TFA inihibits cell wall synthesis by targeting pyrophosphate of peptidoglycan precursors .
|
-
- HY-P10027
-
|
Antibiotic
Bacterial
|
Infection
|
Clovibactin is an antibiotic for drug-resistant bacterial pathogens without detectable resistance. Clovibactin TFA inihibits cell wall synthesis by targeting pyrophosphate of peptidoglycan precursors .
|
-
- HY-P10210
-
|
Antibiotic
Bacterial
|
Infection
|
Paenilagicin is a Gram-positive active antibiotic with a unique diphosphorylated prenyl binding mechanism that does not induce drug resistance. Paenilagicin exhibits a MIC value of 2 μg/mL against multidrug-resistant Gram-positive bacteria .
|
-
- HY-P1653
-
|
Peptides
|
Cancer
|
EC-1456 is a folate-tubulysin conjugate with significant anti-proliferative activity against FR-positive tumors, including models which were anticancer drug resistant. EC-1456 can be utilized in cancer research .
|
-
- HY-P10526
-
|
Bacterial
|
Infection
|
CRAMP (1-39) is an antimicrobial peptide. CRAMP (1-39) has shown potent bactericidal effects against multiple strains of Neisseria meningitidis in vitro. CRAMP (1-39) can be used to study drug-resistant bacterial infections .
|
-
- HY-P10540
-
|
Bacterial
|
Infection
|
Pantinin-2 is a cysteine-free toxic peptide found in the emperor scorpion (paninus imperator). Pantinin-2 has high activity against Gram-positive bacteria but weak activity against Gram-negative bacteria. Pantinin-2 also exhibits activity against Candida tropicalis and has relatively mild hemolytic activity against human erythrocytes. Pantinin-2 can be used in the development of antimicrobial drugs for drug-resistant pathogens .
|
-
- HY-W729138
-
|
Peptides
|
Others
|
Fmoc-D-homoArg(Et)2-OH (hydrochloride) is a Fmoc-protected derivative of D-Homoarginine (HArg) that renders peptides and proteins resistant to proteolysis by trypsin. Fmoc-D-homoArg(Et)2-OH (hydrochloride) can be used as a cleavable ADC linker to synthesize antibody-drug conjugates (ADCs) .
|
-
- HY-P5550
-
|
Influenza Virus
|
Infection
|
Urumin has antiviral activity against the human influenza A virus. Urumin inhibits the growth of PR8 influenza virus (IC50: 3.8 μM). Urumin targets the conserved stalk of H1 hemagglutini, and is effective at neutralizing drug-resistant H1 influenza viruses. Urumin protects naive mice from lethal influenza infection .
|
-
- HY-P10411
-
|
Bacterial
|
Infection
|
BING is an antimicrobial peptide that can be isolated from Japanese medaka fish. BING shows a broad-spectrum toxicity against pathogenic bacteria including drug-resistant strains. BING induces a deregulation of periplasmic peptidyl-prolyl isomerases in gram-negative bacteria, and reduces the RNA level of cpxR, which plays a crucial role in the development of antimicrobial resistance .
|
-
- HY-P10539
-
|
Bacterial
|
Infection
|
Hp1404 is a novel cationic antimicrobial peptide. Hp1404 has specific inhibitory activity against Gram-positive bacteria, including Staphylococcus aureus (MRSA) resistant to Laburnetin (HY-N7382). Hp1404 has antimicrobial activity, low toxicity, and is not prone to drug resistance, and can be used in the research of antimicrobial agents .
|
-
- HY-A0248B
-
|
Antibiotic
Bacterial
|
Infection
|
Polymyxin B2 is a polypeptide antibiotic that has antibacterial activity, particularly against gram-negative bacteria. Polymyxin B2 kills the bacteria by binding to lipopolysaccharide molecules on the bacterial cell membrane, disrupting the integrity of the cell membrane and causing the cell contents to leak. Polymyxin B2 can be used in antibiotic development and treatment of drug-resistant strains .
|
-
- HY-P3349
-
|
Bacterial
|
Infection
|
c[Arg-Arg-Arg-Arg-Nal-Nal-Nal] (Compound 9C) shows broad-spectrum activity against drug-resistant Gram-positive and Gram-negative bacteria, with MICs of 3.1, 3,1, 12.5, and 25 μg/mL for MRSA (ATCC BAA-1556), S. aureus (ATCC 29213), P. aeruginosa (ATCC 27883), and E. coli (ATCC 25922), respectively .
|
-
- HY-P3348
-
|
Bacterial
|
Infection
|
c[Arg-Arg-Arg-Arg-Dip-Dip-Dip] (Compound 8C) shows broad-spectrum activity against drug-resistant Gram-positive and Gram-negative bacteria, with MICs of 3.1, 3,1, 12.5, and 12.5 μg/mL for MRSA (ATCC BAA-1556), S. aureus (ATCC 29213), P. aeruginosa (ATCC 27883), and E. coli (ATCC 25922), respectively .
|
-
- HY-P5704
-
|
Bacterial
|
Infection
|
K11 is an antimicrobial peptide. K11 is active against MDR/XDR K. pneumoniae isolates (MIC: 8-512 μg/mL), and inhibits bacterial biofilm formation. K11 can act synergistically with antibiotics (Chloramphenicol (HY-B0239), Meropenem (HY-13678), Rifampicin (HY-B0272), etc.) against drug-resistant K. pneumoniae. K11 has high thermal and wide pH stability .
|
-
- HY-105048A
-
|
Bacterial
|
Infection
|
Omiganan pentahydrochloride is a cationic peptide compound with a broad antibacterial profile. Omiganan pentahydrochloride is capable of inhibiting a variety of bacteria, including yeast, and is active against both gram-positive and gram-negative bacteria. Omiganan pentahydrochloride is able to interact with the bacterial cell membrane, causing the destruction of the cell membrane and the death of the bacteria. Omiganan pentahydrochloride can be used for the study of antimicrobial activity against pathogens commonly associated with catheter-associated infections, including strains with drug-resistant phenotypes .
|
-
- HY-P2312
-
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-P5377
-
Cathepsin K substrate
|
Peptides
|
Others
|
Abz-HPGGPQ-EDDnp (Cathepsin K substrate) is a biological active peptide. (Cathepsins are a class of globular lysosomal proteases, playing a vital role in mammalian cellular turnover. They degrade polypeptides and are distinguished by their substrate specificities. Cathepsin K is the lysosomal cysteine protease involved in bone remodeling and resorption. It has potential as a drug target in autoimmune diseases and osteoporosis.This FRET peptide can be used to monitor selectively cathepsin K activity in physiological fluids and cell lysates. Abz-HPGGPQ-EDDnp [where Abz represents o-aminobenzoic acid and EDDnp represents N -(2, 4-dinitrophenyl)-ethylenediamine], a substrate initially developed for trypanosomal enzymes, is efficiently cleaved at the Gly-Gly bond by cathepsin K. This peptide is resistant to hydrolysis by cathepsins B, F, H, L, S and V, Ex/Em=340 nm/420 nm.)
|
Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
Cat. No. |
Product Name |
Chemical Structure |
-
- HY-10844S
-
|
Pretomanid-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[1][2].
|
-
-
- HY-B1075AS
-
|
(Rac)-Fosfomycin (benzylamine)- 13C3 is the 13C labeled Fosfomycin[1]. Fosfomycin (MK-0955) is a broad-spectrum antibiotic. Fosfomycin can cross blood-brain barrier penetrating, and irreversibly inhibits an early stage in cell wall synthesis. Fosfomycin shows anti-bacteria activity for a range of bacteria, including multidrug-resistant (MDR), extensively drug-resistant (XDR), and pan-drug-resistant (PDR) bacteria[2][3].
|
-
-
- HY-10844S1
-
|
Pretomanid-d5 is deuterated labeled Pretomanid (HY-10844). 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-14814S
-
|
Delafloxacin-d5 is deuterium labeled Delafloxacin. 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[1].
|
-
Cat. No. |
Product Name |
|
Classification |
-
- HY-125810
-
|
|
Alkynes
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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 . 4'-Ethynyl-2'-deoxyadenosine is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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