Search Result
Results for "
drug resistant
" in MedChemExpress (MCE) Product Catalog:
3
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-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-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-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-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-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-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-N0402
-
-
-
- HY-100358
-
|
Parasite
|
Infection
|
AQ-13 dihydrochloride is an aminoquinoline antimalarial agent that is effective against drug-resistant strains of Plasmodium falciparum.
|
-
-
- 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-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-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-N10430
-
|
HIV
|
Infection
|
Patentiflorin A is a potent, broadspectrum HIV-1 inhibitor. Patentiflorin A also inhibits HIV drug-resistant strains .
|
-
-
- 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-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-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-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-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-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-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-N9386
-
-
-
- HY-145912
-
-
-
- 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-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-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-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-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-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-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-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-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-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-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-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-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
2 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-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-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-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-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-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-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-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-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-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-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
3 Publications Verification
VXc-486
|
|
|
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-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-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-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-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-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-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-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-161023
-
|
Others
|
Cancer
|
Importin β1-IN-1 (compound DD1-Br) is an orally active Importin β1 inhibitor (KD = 0.219 μM). Importin β1-IN-1 exhibits antiproliferative activity on castration-resistant prostate cancer (CRPC) cells. Importin β1-IN-1 alone or in combination with enzalutamide completely prevented tumor growth in a mouse model of drug-resistant CRPC. Importin β1-IN-1 can be used in cancer research .
|
-
- 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-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-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
-
|
|
|
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-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-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-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-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-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-L169
-
|
325 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 325 anti-drug-resistant compounds. It is a good tool to be used for research on cancer and other diseases.
|
-
-
HY-L142
-
|
94 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 94 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
|
-
-
HY-L049
-
|
1306 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 1306 compounds with validated antibacterial activities. MCE antibacterial compound library is an effective tool for drug repurposing screening, combination screening and biological investigation.
|
-
-
HY-L065
-
|
2845 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 2845 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 |
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-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-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-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-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 |
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Classification |
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- HY-125810
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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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