Search Result
Results for "
low cytotoxicity
" in MedChemExpress (MCE) Product Catalog:
5
Biochemical Assay Reagents
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-147652
-
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DNA Stain
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Others
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G-quadruplex DNA fluorescence probe 1 (Compound E1) is a selective G-quadruplex DNA targeting fluorescent probe. G-quadruplex DNA fluorescence probe 1 can pass through membrane and enter living cells with low cytotoxicity .
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- HY-146985
-
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Cathepsin
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Neurological Disease
Cancer
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Cathepsin X-IN-1 (compound 25) is a potent Cathepsin X inhibitor with an IC50 of 7.13 µM. Cathepsin X-IN-1 decreases PC-3 cell migration with low cytotoxic .
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-
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- HY-147820
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-
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- HY-146759
-
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CD73
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Cancer
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ZM514 is a potent CD73 inhibitor with IC50s of 1.39 μM and 14.65 μM for hCD73 and mCD73, respectively. ZM514 has low cytotoxicity. ZM514 can be used for researching anticancer .
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- HY-141646
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Fluorescent Dye
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Others
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MIT-PZR is a mitochondria-targeted,? low cytotoxicity fluorescent probe that can be used in live cells and in vivo imaging. Ex / Em = 485 / 705 nm
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-
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- HY-146706
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Bacterial
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Infection
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PqsR-IN-2 (Compound 19) is a potent PqsR (Pseudomonas aeruginosa quorum sensing transcriptional regulator) inhibitor. PqsR-IN-1 attenuates pyocyanin production and has very low cytotoxicity .
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- HY-146705
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Bacterial
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Infection
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PqsR-IN-1 (Compound 18) is a potent PqsR (Pseudomonas aeruginosa quorum sensing transcriptional regulator) inhibitor. PqsR-IN-1 attenuates pyocyanin production and has very low cytotoxicity .
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-
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- HY-146197
-
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Apoptosis
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Cancer
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Apoptotic agent-1 (Compound 8a) is an apoptotic agent with high antiproliferative activity against cancer cells and low cytotoxic effect. Apoptotic agent-1 induces over-expression of Fas receptor and Cyto C genes .
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- HY-146668
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Cholinesterase (ChE)
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Neurological Disease
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AChE/BChE-IN-8 (Compound 5a) is an uncompetitive AChE and mixed BChE inhibitor with Ki values of 0.788 μM and 2.364 μM against Electrophorus electricus AChE (EeAChE) and equine BChE (eqBChE), respectively. AChE/BChE-IN-8 can cross the BBB and has low cytotoxicity .
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- HY-131983
-
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Influenza Virus
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Infection
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Neuraminidase-IN-2 is an anti-influenza compounds with IC50 values of 0.28, 0.27, 11.50, 0.089 and 23.44 µM for H1N1, 09H1N1, H3N2, H5N1 and H5N2, respectively. Neuraminidase-IN-2 has antiviral activity and low cytotoxicity .
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- HY-17605A
-
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GS-9883 sodium
|
HIV Integrase
HIV
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Infection
|
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Bictegravir sodium is a potent inhibitor of HIV-1 integrase, with an IC50 of 7.5 nM. Bictegravir sodium exhibits potent and selective anti-HIV activity and low cytotoxicity .
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- HY-126275
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ROCK
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Cancer
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HSD1590 is potent ROCK inhibitor, with IC50s of 1.22 and 0.51 nM for ROCK1 and ROCK2, respectively. HSD1590 exhibits single digit nanomolar binding to ROCK (Kds<2 nM). HSD1590 displays low cytotoxicity .
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- HY-147871
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|
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Bacterial
|
Infection
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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 .
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- HY-151560
-
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Dihydroorotate Dehydrogenase
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Cancer
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hDHODH-IN-11 is a potent human dihydroorotate dehydrogenase (hDHODH) inhibitor with an IC50 value of 7.2 nM. hDHODH-IN-11 has low cytotoxicity. hDHODH-IN-11 can be used in research of acute myeloid leukemia (AML) .
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- HY-147532
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Cannabinoid Receptor
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Cancer
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CB2R probe 1 is a safe and green CB2R (cannabinoid 2 receptor) fluorescent probe with an Ki of 130 nM. CB2R probe 1 shows low cytotoxicity in cancer cells .
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- HY-147883
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Bacterial
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Infection
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Antitubercular agent-27 (compound 1) is a potent antitubercular agent with an IC50 value of 3.2 µM, an MIC value of 7.8 µM, an IC90 value of 7.0 µM. Antitubercular agent-27 shows antimycobacterial activity for resistant isolates of Mycobacterium tuberculosis H37Rv. Antitubercular agent-27 shows effective intracellular antimycobacterial activity and low cytotoxicity .
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- HY-147884
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Bacterial
|
Infection
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Antitubercular agent-28 (compound 2) is a potent antitubercular agent with an IC50 value of 1.5 µM, an MIC value of 4.5 µM, an IC90 value of 2.5 µM. Antitubercular agent-28 shows antimycobacterial activity for resistant isolates of Mycobacterium tuberculosis H37Rv. Antitubercular agent-28 shows effective intracellular antimycobacterial activity and low cytotoxicity .
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- HY-144341
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Bacterial
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Infection
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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.
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- HY-17605AR
-
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HIV Integrase
HIV
|
Infection
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Bictegravir (sodium) (Standard) is the analytical standard of Bictegravir (sodium). This product is intended for research and analytical applications. Bictegravir sodium is a potent inhibitor of HIV-1 integrase, with an IC50 of 7.5 nM. Bictegravir sodium exhibits potent and selective anti-HIV activity and low cytotoxicity .
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- HY-168100
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Bacterial
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Infection
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LpxC-IN-14 (compound 6i) is a potent LpxC inhibitor. LpxC-IN-14 shows antibacterial activity. LpxC-IN-14 shows low cytotoxicity. LpxC-IN-14 shows acceptable plasma protein binding .
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- HY-146299
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Bacterial
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Infection
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Mt KARI-IN-2 (compound 5b) is a potent Mycobacterium tuberculosis ketol-acid reductoisomerase (Mtb KARI) inhibitor with a Ki value of 2.02 μM. Mt KARI-IN-2 has inhibitory activity against Mtb H37Rv (MIC = 0.78 μM) and low cytotoxicity (HEK IC50 > 86 μg/mL) .
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- HY-147505
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Bacterial
Fungal
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Infection
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Antitubercular agent-21 (Compound 15) is an antitubercular agent with an MIC of o.4 µg/mL against M. tuberculosis H37Rv. Antitubercular agent-21 exhibits lower activity against other microorganism such as bacteria gram-positive, gram-negative or fungi. Antitubercular agent-21 shows low cytotoxicity .
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- HY-146300
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Bacterial
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Infection
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Mt KARI-IN-4 (compound 5c) is a potent Mycobacterium tuberculosis ketol-acid reductoisomerase (Mtb KARI) inhibitor with a Ki value of 5.48 μM. Mt KARI-IN-4 has inhibitory activity against Mtb H37Rv (MIC = 0.78 μM) and low cytotoxicity (HEK IC50 > 72 μg/mL) .
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- HY-146301
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Bacterial
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Infection
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Mt KARI-IN-5 (compound 6c) is a potent Mycobacterium tuberculosis ketol-acid reductoisomerase (Mtb KARI) inhibitor with a Ki value of 4.72 μM. Mt KARI-IN-5 has inhibitory activity against Mtb H37Rv (MIC = 1.56 μM) and low cytotoxicity (HEK IC50 > 64 μg/mL)
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- HY-147738
-
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Fluorescent Dye
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Others
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SQM-NBD is a potent and selectiveAIE fluorescent probe. SQM-NBD exhibits excellent sensitivity to Cys and Hcy with the LOD of 54 nM and 72 nM, respectively.SQM-NBD has good cell permeability and low cytotoxicity. SQM-NBD has the potential for Cys/Hcy identification under physiological and pathological conditions .
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- HY-148172
-
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HIV
HBV
Nucleoside Antimetabolite/Analog
|
Infection
|
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L-Fd4A is an adenine derivative. L-Fd4A has anti-human immunodeficiency virus (HIV) (EC50=1.5 μM) and anti-hepatitis B virus (HBV) (EC50=1.7 μM) activity. L-Fd4A has low cytotoxicity .
|
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- HY-146388
-
|
|
Bacterial
ATP Synthase
|
Infection
|
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Mtb ATP synthase-IN-1 (compound 6ab) is a potent Mycobacterium tuberculosis (Mtb) ATP synthase inhibitor, with MIC of 0.452-0.499 μg/mL against Mtb. Mtb ATP synthase-IN-1 has good metabolic stability, low cytotoxicity (Vero IC50 > 64 μg/mL), and acceptable oral bioavailability. Mtb ATP synthase-IN-1 can be used for researching anti-mycobacterium .
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- HY-15221
-
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Apoptosis
Histone Demethylase
MDM-2/p53
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Cardiovascular Disease
Cancer
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Methylstat is a potent histone demethylases inhibitor. Methylstat shows anti-proliferative activity with low cytotoxicity. Methylstat induces apoptosis and cell cycle arrest at G0/G1 phase. Methylstat increases the expression of p53 and p21 protein levels. Methylstat inhibits angiogenesis induced by various cytokines. Methylstat can be used as a chemical probe for addressing its role in angiogenesis .
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- HY-144334
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DNA/RNA Synthesis
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Infection
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CHIKV-IN-3 is a potent against two low-passage CHIKV inhibitor with EC50 values of 1.55 and 0.14 µM for CHIKV-122508 and CHIKV-6708, respectively. CHIKV-IN-3 acts on the host cells to interfere with the viral replication. CHIKV-IN-3 displays minimal cytotoxic liability(CC50 > 100 µM). Prophylactic effect .
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- HY-161461
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Amylases
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Neurological Disease
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E234G HYPE-IN-1 (Compound I2.10) is an inhibitor of AMPylation directed by the Huntingtin-interacting protein E (HYPE), possessing low micromolar bioactivity, low cytotoxicity, and blood-brain barrier permeability. E234G HYPE-IN-1 can inhibit the AMPylation of B-cell immunoglobulin-binding protein (BiP), the primary substrate of HYPE. E234G HYPE-IN-1 is suitable for development as a HYPE-specific therapeutic agent for clinical conditions such as neurodegenerative diseases and diabetes .
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- HY-146017
-
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HIV
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Infection
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HIV-1 inhibitor-22 (compound 11a) is a potent HIV-1 non-nucleoside reverse transcriptase (RT) inhibitor, with an IC50 value of 3.63 μM for HIV-1 RT. HIV-1 inhibitor-22 has antiretroviral activity against HIV-1 WT and K103N strains with EC50s of 0.304 μM and 0.201 μM, also has low cytotoxicity (CC50 > 227 μM)
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- HY-146226
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Enterovirus
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Infection
|
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Viral 2C protein inhibitor 1 (compound 6aw) is a potent and broad-spectrum enterovirus antiviral agent, inhibiting viral 2C protein. Viral 2C protein inhibitor 1 inhibits multiple strains of EV-D68, EV-A71 and CVB3 with EC50s of 0.1~3.6 µM, and exhibits high selectivity index and relatively low cytotoxicity .
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- HY-146015
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HIV
|
Infection
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HIV-1 inhibitor-21 (compound 9b) is a potent HIV-1 non-nucleoside reverse transcriptase (RT) inhibitor, with an IC50 value of 0.55 μM for HIV-1 RT. HIV-1 inhibitor-21 has antiretroviral activity against HIV-1 WT and K103N strains with EC50s of 12.7 nM and 10.4 nM, and has relatively low cytotoxicity (MT-4 cells CC50 =10.2 μM) .
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- HY-144632
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Fungal
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Infection
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Antifungal agent 22 (compound D16) is a potential and orally active antifungal agent for CM (cryptococcal meningitis), with an IC50 of 0.5 μg/mL. Antifungal agent 22 can penetrate the blood-brain barrier and kill the C. neoformans H99 cells by destroying the integrity of fungal cell membranes. Antifungal agent 22 shows selective anti-Cryptococcus activity with good metabolic stability and low cytotoxicity .
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- HY-146000
-
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Influenza Virus
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Inflammation/Immunology
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Influenza virus-IN-3 (compound 9) is a potent and selective influenza virus inhibitor with IC50s of 0.88, 0.10, 5.5, 0.51 µM for H5N1, H5N2, H5N6, H5N8, respectively. Influenza virus-IN-3 shows antiviral and NA (neuraminidase enzyme)-inhibitory activity. Influenza virus-IN-3 shows low cytotoxicity with an CC50 of >200 µM .
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- HY-148170
-
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EBV
DNA/RNA Synthesis
Nucleoside Antimetabolite/Analog
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Infection
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L-I-OddU, a L-5'-halo- dioxolane nucleoside analogue, is a potent and selective anti-Epstein-Barr virus (EBV) agent with an EC50 value of 0.03μM. L-I-OddU has low cytotoxicity with a CC50 value of 1000 nM. L-I-OddU has antiviral activity by suppressing replicative EBV DNA and viral protein synthesis .
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- HY-146001
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Influenza Virus
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Inflammation/Immunology
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Influenza virus-IN-4 (compound 11e) is a potent influenza virus neuraminidase inhibitor with IC50s of 3.4, 0.094, 0.79, 0.077 µM for H5N1, H5N2, H5N6, H5N8, respectively. Influenza virus-IN-4 shows NA (neuraminidase enzyme)-inhibitory activity. Influenza virus-IN-4 shows low cytotoxicity with an CC50 of >200 µM. Influenza virus-IN-4 shows no obvious toxicity at the dose of 1500 mg/kg in mice .
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- HY-146957
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Virus Protease
Flavivirus
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Cancer
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ZIKV-IN-1 is a potent zika virus inhibitor with an EC50 of 2.8 μM and EC90 of 6.8 μM. ZIKV-IN-1 shows anti-ZIKV activity with low cytotoxicity. ZIKV-IN-1 shows a strong affinity to ZIKV RdRp domain . ZIKV-IN-1 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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- HY-130612
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Epigenetic Reader Domain
PROTACs
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Cancer
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PROTAC BRD2/BRD4 degrader-1 (compound 15) is a potent and selective BET protein BRD4 and BRD2 degrader, connected by ligands for Cereblon and BET. PROTAC BRD2/BRD4 degrader-1 rapidly induces reversible, long-lasting, and unexpectedly selective removal of BRD4 and BRD2 over BRD3. It effectively inhibits solid tumors with low cytotoxic effect. PROTAC BRD2/BRD4 degrader-1 is composed of the BET inhibitor, a linker, and the ligand thalidomide for cereblon (CRBN)/cullin 4A .
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- HY-147881
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Influenza Virus
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Infection
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Anti-Influenza agent 3 (compound 11h) is a potent anti-influenza agent with EC50 values of 3.29, 2.45 µM for A/HK/68 (H3N2, M2-WT), A/WSN/33 (H1N1, M2-S31N) strain, respectively. Anti-Influenza agent 3 shows low cytotoxicity for MDCK epithelial cells. Anti-Influenza agent 3 inhibits the M2 WT and S31N ion channel conductivity .
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- HY-146740
-
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PD-1/PD-L1
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Cancer
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PD-1/PD-L1-IN-27 is a potent PD-1/PD-L1 inhibitor with an IC50 value of 134 nM. PD-1/PD-L1-IN-27 shows antitumor effects with low T cell cytotoxicity. PD-1/PD-L1-IN-27 has the ability to activate CD8 + T cells and reduces T cell exhaustion .
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- HY-16117A
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-
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- HY-N6622
-
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Others
|
Others
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Tazettine is an alkaloid with low cytotoxicity to mammalian cell lines (CC50 >100 μg/mL) .
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- HY-155067
-
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Bacterial
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Infection
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Antitubercular agent-38 is an orally active Benzothiazinones (BTZs) derivate, with potent antituberculosis activity. Antitubercular agent-38 exhibits low cardiac toxicity, low cell cytotoxicity .
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- HY-147806
-
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Parasite
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Infection
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Antiparasitic agent-8 (Compound 9) is an antiparasitic agent against Hymenolepis nana with low cytotoxicity .
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- HY-155071
-
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Bacterial
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Infection
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MmpL3-IN-2 is an MmpL3 inhibitor with low cytotoxicity and moderate metabolic stability for tuberculosis research .
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- HY-100039
-
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HIV
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Infection
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YYA-021 is a small-molecule CD4 mimic that inhibits HIV entry, with high anti-HIV activity and low cytotoxicity .
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- HY-142545
-
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Bacterial
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Infection
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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 .
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- HY-151977
-
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Tyrosinase
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Cancer
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Tyrosinase-IN-7 is a potent tyrosinase inhibitor with an IC50 value of 1.57 µM. Tyrosinase-IN-7 inhibits cell growth with low cytotoxicity .
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- HY-151979
-
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Tyrosinase
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Cancer
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Tyrosinase-IN-8 is a potent tyrosinase inhibitor with an IC50 value of 1.6 µM. Tyrosinase-IN-8 inhibits cell growth with low cytotoxicity .
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- HY-152150
-
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Ser/Thr Protease
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Metabolic Disease
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Thrombin inhibitor 7 is a potent FXIIa inhibitor with IC50 values of 28 nM, >132 µM for FXIIa and FXIa, respectively. Thrombin inhibitor 7 shows low cytotoxicity .
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- HY-151356
-
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Bacterial
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Infection
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Antibacterial agent 122 (compound 15) is a thiourea derivative with anti-mycobacterial activity and low cytotoxicity. Antibacterial agent 122 can be used for tuberculosis-related studies .
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- HY-141426
-
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Enterovirus
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Infection
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MDL-860 is a broad-spectrum antipicornavirus compound that has low cytotoxicity toward human cells. MDL-860 can be used for the research of virus infection .
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- HY-146417
-
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Flavivirus
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Infection
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Antiviral agent 19 (Compound 3) is a selective inhibitor against Zika virus infection with an EC50 of 1.3 µM. Antiviral agent 19 has low cytotoxicity .
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- HY-N2193
-
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Flavivirus
Dengue Virus
Apoptosis
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Infection
Cancer
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Hirsutine, an indole alkaloid of Uncaria rhynchophylla, exhibits anti-cancer activity. Hirsutine induces apoptosis and is a potent Dengue virus inhibitor exhibiting low cytotoxicity .
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- HY-W008864
-
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β-Octaacetyllactose
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Antibiotic
Fungal
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Infection
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Lactose octaacetate shows mild to moderate antifungal activity against some fungi, but it has low or no activity against bacteria and yeast. Lactose octaacetate shows low cytotoxicity to MDBK cells, Hep-2 and MDCK cells. Lactose octaacetate has antiviral activity against PV-1 .
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- HY-146418
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Flavivirus
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Infection
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Antiviral agent 20 (Compound 17b) is a selective inhibitor against Zika virus infection with an EC50 of 4.5 µM. Antiviral agent 20 has low cytotoxicity .
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- HY-161893
-
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Bacterial
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Infection
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Anti-MRSA agent 15 (Compound 9o10) exhibits antibacterial activity, that inhibits methicillin-resistant Staphylococcus aureus (MRSA) with a MIC of 0.0625 μg/mL. Anti-MRSA agent 15 exhibits low hemolysis and low cytotoxicity. Anti-MRSA agent 15 exhibits anti-infective in mice .
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- HY-146348
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Bacterial
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Infection
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Tuberculosis inhibitor 5 (Compound 11i) is a potent antimycobacterial biphenyl analogue without noticeable cytotoxicity. Tuberculosis inhibitor 5 is an anti-tuberculosis agent .
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- HY-161013
-
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Others
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Others
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Antiproliferative agent-44 (compound 3) is a potent inhibitor of proliferation, with the IC50 values ranging from 2.02 to 1.61 μM .
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- HY-152109
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- HY-N11056
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Antibiotic
VSV
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Infection
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Justicidin C is an antiviral lignan. Justicidin C shows strong antiviral activity against vesicular stomatitis virus and low cytotoxicity against rabbit lung cells (RL-33) .
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- HY-149013
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Bacterial
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Infection
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Anti-MRSA agent 5 (B14) is a potent MRSAagent with MIC50 values of 0.38 μg/mL and has low hERG activity with an IC50 values of >40 μM. Anti-MRSA agent 5 (B14) also has low cytotoxicity to mammal cells and unlikely to acquire bacterial resistance .
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- HY-122274
-
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Parasite
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Infection
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MMV666693 is a translation inhibitor specific for Plasmodium falciparum. MMV666693 has low cytotoxicity in human fibroblasts (IC50>32 µM) and can be used in the development of antimalarial drugs .
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- HY-158336
-
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Ferroptosis
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Cancer
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E/Z-FETPY is an organo-diiron(I) complex with strong cytotoxicity in cancer cell lines. E/Z-FETPY induces ferroptosis in low-differentiated cell lines, such as A2780 cells .
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- HY-170760
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Bacterial
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Infection
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Antibacterial agent 258 (Compound 11e) is an antibacterial agent, that destory the bacteria cell membrane, and inhibits various gram-positive bacteria (MIC for Staphylococcus aureus is 1-2 μg/mL). Antibacterial agent 258 exhibits low hemolytic activity and low cytotoxicity. Antibacterial agent 258 exhibits anti-infectious efficacy in mouse models .
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- HY-133207
-
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Microtubule/Tubulin
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Cancer
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Myoseverin B is a microtubule assembly inhibitor capable of inhibiting the polymerization of tubulin (IC50 = 2 μM) and exhibiting low cytotoxicity in most cell types. Myoseverin B can be used in research as an antitumor agent .
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- HY-152669
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Bacterial
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Infection
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Urease-IN-5 is an inhibitor of urease with an IC50 value of 1.473 µM. Urease-IN-5 has low cytotoxicity and inhibitory activity on P. vulgaris with an IC50 value of 17.78 µg/mL .
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- HY-161258
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Bacterial
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Infection
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Antibacterial agent 181 (Compound 3f) is a potent ciprofloxacin cationic antibacterial agent with low cytotoxicity. The MIC values of Antibacterial agent 181 against Staphylococcus aureus and Escherichia coli are both 2 μg/mL .
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- HY-155734
-
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SARS-CoV
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Infection
|
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SARS-CoV-2-IN-55(compound 65) is a low cytotoxicity inhibtor of SARS-CoV-2 with an IC50 value of 0.3 μM, by the direct interaction with VSV-S pseudoparticles .
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- HY-P4836
-
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Parasite
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Infection
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LL-37 FK-13 is an antimicrobial agent, that inhibits Trichomonas vaginalis. LL-37 FK-13 exhibits slight hemolytic effects on human erythrocytes and low cytotoxicity to human fibroblasts .
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- HY-152668
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Bacterial
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Infection
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Urease-IN-4 is an effective inhibitor of urease with an IC50 value of 1.64 µM. Urease-IN-4 has low cytotoxicity and shows inhibitory activity on P. vulgaris with an IC50 value of 15.27 µg/mL .
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- HY-N10877
-
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Others
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Cancer
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Chlorajapolide F is a nature product that could be isolated from the aerial part of Chloranthus japonicas. Chlorajapolide F has low cytotoxic activity against NCI-H460 and SMMC-7721 cell lines .
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- HY-163431
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URAT1
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Inflammation/Immunology
|
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URAT1 inhibitor 10 (Compound 23a) is a URAT1 inhibitor. URAT1 inhibitor 10 has oral efficacy and low cytotoxicity. URAT1 inhibitor 10 has high selectivity for OAT1 .
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- HY-118942
-
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ARC 111
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Topoisomerase
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Cancer
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Topovale (ARC 111) is a topoisomerase I inhbitor. Topovale is an antitumor agent, and shows low nM cytotoxicity against a panel of cancer cells. Topovale induces reversible topoisomerase I (TOP1) cleavage complexes in tumor cells .
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- HY-143762
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Influenza Virus
|
Infection
|
|
Cap-dependent endonuclease-IN-12 (EXP-35) is a potent Cap-dependent endonuclease inhibitor with low cytotoxicity. Cap-dependent endonuclease-IN-12 shows inhibitory activity against H1N1 .
|
-
- HY-157554
-
-
- HY-111402
-
|
Erizomycin; NSC 246134
|
Bacterial
Antibiotic
|
Infection
|
|
Pyridomycin (Erizomycin) is a selective and low cytotoxic inhibitor of Mycobacterium tuberculosis that effectively targets InhA. Pyrdomycin is also an antibiotic that can be obtained from metabolites of Dactylosporangium fulvum. Pyrdomycin can be used in the study of bacterial infections such as tuberculosis .
|
-
- HY-151448
-
|
|
Virus Protease
|
Infection
|
|
ZIKV-IN-5 (compound 5c) is a low-cytotoxicity and acid-stable anti-ZIKV agent (EC50=0.71 μM). ZIKV-IN-5 effectively inhibits the activity of ZIKV NS5 MTase .
|
-
- HY-149243
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
BChE-IN-16 (compound 87) is a highly potent BChE inhibitor with an IC50 of 3.8 nM for hBChE. BChE-IN-16 has low cytotoxicity, potential CNS permeability, unique adaptability and can be used in Alzheimer's disease (AD) research.
|
-
- HY-A0162R
-
|
|
Antibiotic
Bacterial
|
Infection
|
|
Bictegravir (sodium) (Standard) is the analytical standard of Bictegravir (sodium). This product is intended for research and analytical applications. Bictegravir sodium is a potent inhibitor of HIV-1 integrase, with an IC50 of 7.5 nM. Bictegravir sodium exhibits potent and selective anti-HIV activity and low cytotoxicity .
|
-
- HY-149353
-
|
|
Bacterial
|
Infection
|
|
Antibacterial agent 145 (compound 1b) is an antibacterial agent depending on bacterial iron uptake pathway. Antibacterial agent 145 disrupts cytoplasmic membrane integrity and inhibits cell metabolism but exhibits low cytotoxic effects to normal cells .
|
-
- HY-155546
-
|
|
Bacterial
|
Infection
|
|
Antimicrobial agent-22 (THI 6c) is a multi-target broad-spectrum antibacterial agent. Antimicrobial agent-22 has low cytotoxicity, hemolytic property, rapid bactericidal ability and good anti-biofilm activity .
|
-
- HY-150754
-
|
|
Bacterial
|
Infection
|
|
FtsZ-IN-4 is an orally active FtsZ (filamenting temperature-sensitive mutant Z) inhibitor, exhibits excellent antibacterial activity. FtsZ-IN-4 shows good pharmaceutical properties with low cytotoxicity (CC50 >20 μg/mL) .
|
-
- HY-118762
-
|
|
Cathepsin
|
Cancer
|
|
KGP94 is a selective inhibitor of cathepsin L with an IC50 of 189 nM . KGP94 inhibits migration and invasion of metastatic carcinoma and shows low cytotoxicity (GI50=26.9 µM) against various human cell lines .
|
-
- HY-155813
-
|
|
SARS-CoV
|
Infection
|
|
MPI60 is a potent SARS-CoV-2 M Pro inhibitor with high antiviral potency, low cellular cytotoxicity, and high in vitro metabolic stability. MPI60 can be used for SARS-CoV-2 research .
|
-
- HY-151447
-
|
|
Virus Protease
|
Infection
|
|
ZIKV-IN-4 (compound 5b) is a low-cytotoxicity and acid-stable anti-ZIKV agent (EC50=3.49 μM). ZIKV-IN-4 effectively inhibits the activity of ZIKV NS5 MTase .
|
-
- HY-134154
-
|
PAzePC; Azelaoyl PC; 1-Palmitoyl-2-Azelaoyl PC
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Oxidized low-density lipoprotein (oxLDL) particles contain low molecular weight species which are cytotoxic and pro-atherogenic. Many of these substances were isolated and purified from oxLDL and identified as phosphatidylcholine species containing a fragmented, oxidized short-chain fatty acid remnant at the sn-2 position. PAz-PC (Azelaoyl PC) is one of the predominant oxLDL species and may be one of the important structural determinants of oxLDL.
|
-
- HY-19135
-
|
|
HIV Protease
|
Infection
|
|
A-77003 is an inhibitor for HIV protease, with IC50 of 0.1 to 0.2 μg/ml, for HIV-1 and HIV-2 protease. A-77003 exhibits high levels of antiretroviral activity and low cytotoxicity in vitro .
|
-
- HY-161330
-
|
|
Bacterial
|
Infection
|
|
Anti-MRSA agent 10 (Compound 2d) is a Cephalosporin (HY-144229) derivative and exhibits antibacterial activity. Anti-MRSA agent 10 is slightly drug resistane and exhibits low cytotoxicity in cells HUVEC and HBZY-1 .
|
-
- HY-137498
-
|
|
Filovirus
|
Infection
|
|
EBOV/MARV-IN-1 is a potent inhibitor of Ebola virus (EBOV) and Marburg virus (MARV), with broad-spectrum activity (EC50=0.31, and 0.82 µM, respectively) and low cytotoxicity (SI>100) in HeLa cells .
|
-
- HY-136213
-
|
|
Fluorescent Dye
|
Others
|
|
Endoplasmic reticulum dye 1 is a promising live cell imaging agent for the detection of exocytotic events at the plasma membrane. Endoplasmic reticulum dye 1 shows low cytotoxicity, resistance to photobleaching , which is ideal for imaging either short- or long-time courses .
|
-
- HY-168335
-
|
|
Dihydroorotate Dehydrogenase
|
Others
|
|
hDHODH-IN-16 (Compound 3t) is a human dihydroorotate dehydrogenase (hDHODH) inhibitor, with an IC50 of 0.11 μM. hDHODH-IN-16 shows very low cytotoxicity to healthy HaCaT cells, with an IC50 value greater than 200 µM .
|
-
- HY-147760
-
|
|
DYRK
|
Metabolic Disease
|
|
Dyrk1A-IN-2 (Compound 63) is a DYRK1A inhibitor with an EC50 of 37 nM. Dyrk1A-IN-2 exhibits highly potent human β-cell replication-promoting activity and low cytotoxicity .
|
-
- HY-162914
-
|
|
SARS-CoV
|
Infection
|
|
SARS-CoV-2-IN-96 (compound 12b) is an inhibitor of HCoV-OC43 (EC50= 97 nM) and SARS-CoV-2 (EC50= 45 nM) and low cytotoxicity (CC50> 10 μM) in Huh7 cells .
|
-
- HY-W110888
-
|
|
GLUT
|
Neurological Disease
|
|
Brilliant Yellow, a diazo-containing sulfonic aci, is also a potent VGLUT-specific inhibitor. Brilliant Yellow is membrane-impermeable. However, there are some Brilliant Yellow analogs with low cytotoxicity and cell penetration. Brilliant Yellow analogs work on glutamatergic transmission in hippocampal neurons .
|
-
- HY-146286
-
|
|
Apoptosis
|
Cancer
|
|
Anticancer agent 44 (compound 2a) is a potent anticancer agent. Anticancer agent 44 shows cytotoxicity activity in cancer cells. Anticancer agent 44 induces apoptosis. Anticancer agent 44 shows low toxicity towards activated lymphocytes of human blood .
|
-
- HY-149207
-
|
|
Tyrosinase
|
Metabolic Disease
|
|
Tyrosinase-IN-11 is a potent tyrosinase inhibitor with IC50s of 50 nM and 64 nM for L-tyrosinase and L-dopa, respectively. Tyrosinase-IN-11 has significant antioxidant activity and low cytotoxicity. Tyrosinase-IN-11 has the potential for skin hyperpigmentation research .
|
-
- HY-149431
-
|
|
HSP
Potassium Channel
|
Cancer
|
|
NDNA4 (compound 17) is a selective inhibitor of Hsp90α (IC50: 0.34 μM). NDNA4 is a permanently charged analog with low membrane permeability and low cytotoxicity against Ovcar-8 and MCF-10A ((IC50 >100 μM)). NDNA4 prevents disruption of hERG channel maturation without generating a heat shock response or causing degradation of Hsp90α-dependent client proteins .
|
-
- HY-146290
-
|
|
Apoptosis
|
Cancer
|
|
Anticancer agent 46 (compound 2b) is a potent and selective anticancer agent. Anticancer agent 46 shows cytotoxicity activity in cancer cells. Anticancer agent 46 induces apoptosis. Anticancer agent 46 shows low toxicity towards activated lymphocytes of human blood .
|
-
- HY-119993
-
|
BMH-23
|
DNA/RNA Synthesis
|
Cancer
|
|
AR03 (BMH-23) is an apurinic/apyrimidinic endonuclease 1 (Ape1) inhibitor with an IC50 of 2.1 µM. AR03 has low affinity for double-stranded DNA. AR03 potentiates the cytotoxicity of methyl methanesulfonate and temozolomide in SF767 cells .
|
-
- HY-144731
-
|
|
HIV
|
Inflammation/Immunology
|
|
gp120-IN-2 (compound 4i) is a potent HIV-1 gp120 inhibitor with an IC50 of 7.5 µM and CC50 of 112.93 µM. gp120-IN-2 shows anti-HIV-1 activity. gp120-IN-2 shows cytotoxicity in a dose dependent manner in SUP-T1 cells .
|
-
- HY-146138
-
|
|
EGFR
VEGFR
Casein Kinase
Topoisomerase
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
EGFR-IN-57 (Compound 25a) is a potent, orally active EGFR-TK inhibitor with an IC50 of 0.054 µM. EGFR-IN-57 also inhibits VEGFR-2, CK2α, topoisomerase IIβ and tubulin polymerization with IC50 values of 0.087, 0.171, 0.13 and 3.61 µM, respectively. EGFR-IN-57 induces cell cycle arrest at G2/M and pre-G1 phases. EGFR-IN-57 induces cancer cell apoptosis .
|
-
- HY-146888
-
|
|
HIV Protease
|
Infection
|
|
HIV-1 protease-IN-2 is a potent HIV-1 protease inhibitor with an IC50 of 2.53 nM. HIV-1 protease-IN-2 shows antiviral activity against DRV (Darunavir)-sensitive or DRV-resistant HIV-1 variants .
|
-
- HY-114197
-
-
- HY-155247
-
|
|
Tyrosinase
|
Others
|
|
Tyrosinase-IN-14 (compound 7m) is a tyrosinase inhibitor that reduces the catalytic activity of tyrosinase by changing its secondary structure. Tyrosinase-IN-14 has low cytotoxicity and anti-browning activity in fruits. Tyrosinase-IN-14 effectively inhibits banana browning during storage .
|
-
- HY-W663230
-
|
|
Parasite
|
Infection
|
|
Eugenitin is a polyketide isolated from the fungus Mycoleptodiscus indicus that is related to the South American medicinal plant. Eugenitin inhibits Leishmania major with LD50=39.9 μM. Eugenitin has low cytotoxicity (IC50 >131 μM) against several human cancer cell lines .
|
-
- HY-115989
-
|
|
HCV
|
Infection
|
|
HCV-IN-38 is a potent, selective and orally active HCV inhibitor (EC50=15 nM, SI=431). HCV-IN-38 has high anti-HCV activity and low cytotoxicity. HCV-IN-38 has a good safety and oral pharmacokinetic profile .
|
-
- HY-N2346
-
|
|
ADC Cytotoxin
Microtubule/Tubulin
|
Cancer
|
|
Tubulysin E is a highly cytotoxic anti-microtubule toxin (anti-microtubule toxins) that is synthesized as an ADC cytotoxin (ADC Cytotoxin). Tubulysin E can be isolated from the myxobacteria Archangium geophyra and Angiococcus disciformis. Tubulysin E displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the low nanomolar range. Tubulysin E inhibits microtubule/Tubulin polymerization and leads to cell cycle arrest and apoptosis .
|
-
- HY-N7049
-
|
|
ADC Cytotoxin
Microtubule/Tubulin
|
Cancer
|
|
Tubulysin F is a highly cytotoxic anti-microtubule toxin (anti-microtubule toxins) that is synthesized as an ADC cytotoxin (ADC Cytotoxin). Tubulysin F can be isolated from the myxobacteria Archangium geophyra and Angiococcus disciformis. Tubulysin F displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the low nanomolar range. Tubulysin F inhibits microtubule/Tubulin polymerization and leads to cell cycle arrest and apoptosis .
|
-
- HY-N7052
-
|
|
ADC Cytotoxin
Microtubule/Tubulin
|
Cancer
|
|
Tubulysin I is a highly cytotoxic anti-microtubule toxin (anti-microtubule toxins) that is synthesized as an ADC cytotoxin (ADC Cytotoxin). Tubulysin I can be isolated from the myxobacteria Archangium geophyra and Angiococcus disciformis. Tubulysin I displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the low nanomolar range. Tubulysin I inhibits microtubule/tubulin polymerization and leads to cell cycle arrest and apoptosis .
|
-
- HY-N7053
-
|
|
ADC Cytotoxin
Microtubule/Tubulin
|
Cancer
|
|
Tubulysin M is a highly cytotoxic anti-microtubule toxin (anti-microtubule toxins) that is synthesized as an ADC cytotoxin (ADC Cytotoxin). Tubulysin M can be isolated from the myxobacteria Archangium geophyra and Angiococcus disciformis. Tubulysin M displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the low nanomolar range. Tubulysin M inhibits microtubule/tubulin polymerization and leads to cell cycle arrest and apoptosis .
|
-
- HY-N7050
-
|
|
ADC Cytotoxin
Microtubule/Tubulin
|
Cancer
|
|
Tubulysin G is a highly cytotoxic anti-microtubule toxin (anti-microtubule toxins) that is synthesized as an ADC cytotoxin (ADC Cytotoxin). Tubulysin G can be isolated from the myxobacteria Archangium geophyra and Angiococcus disciformis. Tubulysin G displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the low nanomolar range. Tubulysin G inhibits microtubule/tubulin polymerization and leads to cell cycle arrest and apoptosis .
|
-
- HY-N2348
-
|
|
ADC Cytotoxin
Microtubule/Tubulin
|
Cancer
|
|
Tubulysin D is a highly cytotoxic anti-microtubule toxin (anti-microtubule toxins) that is synthesized as an ADC cytotoxin (ADC Cytotoxin). Tubulysin D can be isolated from the myxobacteria Archangium geophyra and Angiococcus disciformis. Tubulysin D displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the low nanomolar range. Tubulysin D inhibits microtubule/Tubulin polymerization and leads to cell cycle arrest and apoptosis .
|
-
- HY-N2347
-
|
|
ADC Cytotoxin
Microtubule/Tubulin
|
Cancer
|
|
Tubulysin C is a highly cytotoxic anti-microtubule toxin (anti-microtubule toxins) that is synthesized as an ADC cytotoxin (ADC Cytotoxin). Tubulysin C can be isolated from the myxobacteria Archangium geophyra and Angiococcus disciformis. Tubulysin C displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the low nanomolar range. Tubulysin C inhibits microtubule/Tubulin polymerization and leads to cell cycle arrest and apoptosis .
|
-
- HY-N7051
-
|
|
ADC Cytotoxin
Microtubule/Tubulin
|
Cancer
|
|
Tubulysin H is a highly cytotoxic anti-microtubule toxin (anti-microtubule toxins) that is synthesized as an ADC cytotoxin (ADC Cytotoxin). Tubulysin H can be isolated from the myxobacteria Archangium geophyra and Angiococcus disciformis. Tubulysin H displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the low nanomolar range. Tubulysin H inhibits microtubule/tubulin polymerization and leads to cell cycle arrest and apoptosis .
|
-
- HY-147537
-
|
|
Parasite
|
Infection
|
|
Antileishmanial agent-9 (compound 16c) has potent and selective activity against Leishmania donovani (L. donovani) with an IC50 value of 4.01 μM. Antileishmanial agent-9 has relatively low cytotoxicity in L-6 cells (IC50 = 40.1 μM) .
|
-
- HY-153468
-
|
|
Sodium Channel
|
Cancer
|
|
ErSO-TFPy activates the sodium channel TRPM4, causes an imbalance of intracellular calcium and sodium ions. ErSO-TFPy exhibits low nanomolar cytotoxicity in ERα+ breast cancer cell lines (IC50 = 5-25 nM) through induction of necrosis. ErSO-TFPy exhbits antitumor efficacy in mouse models .
|
-
- HY-147536
-
|
|
Parasite
|
Infection
|
|
Antileishmanial agent-8 (compound 18) has potent and selective activity against Leishmania donovani (L. donovani) with an IC50 value of 5.64 μM. Antileishmanial agent-8 has relatively low cytotoxicity in L-6 cells (IC50=73.9 μM) .
|
-
- HY-W011762
-
|
|
Apoptosis
|
Cancer
|
|
VK3-OCH3 is a potent antitumor agent. VK3-OCH3 shows cytotoxicity for neuroblastoma cell lines and low cytotoxicity for normal cell lines. VK3-OCH3 induces apoptosis and cell cycle arrest at G2/M phase in IMR-32 cells. VK3-OCH3 shows antitumor activity .
|
-
- HY-155053
-
|
|
Flavivirus
DNA/RNA Synthesis
|
Inflammation/Immunology
|
|
ZIKV-IN-6 (compound 22) is an inhibitor of Zika virus (ZIKV), with low cytotoxicity (CC50＞50 μM). ZIKV-IN-6 binds to ZIKV RdRp directly and inhibits viral RNA synthesis by ZIKV NS5. ZIKV-IN-6 suppresses the excessive inflammatory response and pyroptosis .
|
-
- HY-146104
-
|
|
Bacterial
|
Infection
|
|
Antimycobacterial agent-1 (compound 33) has selectively antimycobacterial activity against Mycobacterium tuberculosis (M. tuberculosis) H37Ra with a MIC value of 1 μg/ml. Antimycobacterial agent-1 has relatively low cytotoxicity in normal cells (Vero cells IC50 = 143.2 μg/ml) .
|
-
- HY-N7934
-
|
(-)-Trachelogenin
|
HCV
|
Infection
Neurological Disease
Inflammation/Immunology
|
|
Trachelogenin ((-)-Trachelogenin) is an HCV entry inhibitor without genotype specificity, and with low cytotoxicity. Trachelogenin inhibits HCVcc infection and HCVpp cell entry in a dose-dependent manner with an IC50 of 0.325 and 0.259 μg/mL in HCVcc and HCVpp models, respectively. Trachelogenin exhibits effective antiviral, anti-inflammatory and analgesic effects .
|
-
- HY-W009245
-
|
|
HIV
|
Infection
Cancer
|
|
Bz-RS-iSer(3-Ph)-OMe (compound 2), a Taxol derivative, inhibits HSV replication cycle at low cytotoxicity, blocks mitotic divisions of Vero cells, influences M-MSV induced tumor size and affects immune response by inhibiting PHA-induced T lymphocyte proliferation .
|
-
- HY-144822
-
|
|
Bacterial
|
Infection
|
|
Anti-MRSA agent 2 (compound 14) has highly inhibitory activity against Methicillin-resistant Staphylococcus aureus (MRSA) with MIC of 0.098 μg/ml, and relatively low cytotoxicity in normal cells. Anti-MRSA agent 2 has strong ability to destroy bacterial membrane and bind to genomic DNA .
|
-
- HY-139181
-
|
|
HDAC
|
Cancer
|
|
NR160 is a selective HDAC6 inhibitor with an IC50 value of 30 nM. NR160 shows low cytotoxicity against leukemia cell line. NR160 augments the apoptosis induction of Bortezomib (HY-10227) (proteasome inhibitor), Epirubicin (HY-13624) and Daunorubicin (HY-13062A) significantly .
|
-
- HY-153690
-
|
|
TNF Receptor
|
Others
|
|
Progranulin modulator-1 (Compound 60) is an orally active enhancer of progranulin (PGRN) secretion. Progranulin modulator-1 enhances the potency of BV-2 cell to increase PGRN levels, has inhibitory effect on hERG and Low cytotoxicity, the PGRN EC50 and hERG IC50 were 83 and 3100 nM, respectively .
|
-
- HY-144446
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
BuChE-IN-1 (Compound 23) is a potent inhibitor of butyrylcholinesterase (BuChE). Butyrylcholinesterase (BuChE) is recently regarded as a biomarker in progressed Alzheimer’s disease (AD). BuChE-IN-1 shows low cytotoxicity and high blood brain barrier (BBB) permeability. BuChE-IN-1 is a promising BuChE inhibitor for the research of AD .
|
-
- HY-149009
-
|
|
Bcl-2 Family
Apoptosis
|
Cancer
|
|
Bcl-2-IN-9 is a novel proapoptotic Bcl-2 inhibitor with IC50 value of 2.9 μM and low cytotoxic. Bcl-2-IN-9 mediates apoptosis by down-regulating expression of Bcl-2 in cancer cells and has a high selectivity against leukemia cells .
|
-
- HY-163693
-
|
|
Fungal
|
Infection
|
|
Antifungal agent 104 (Compound 5e) exhibits antifungal activity against Sclerotinia sclerotiorum, Rhizoctonia solani and Botrytis cinerea, with EC50 of 1.52 μg/mL, 0.06 μg/mL and 15.69 μg/mL, respectively. Antifungal agent 104 exhibits low cytotoxicity to human renal cell 239A (6.28-100 mM) .
|
-
- HY-162422
-
|
|
Fluorescent Dye
Pyroptosis
|
Cancer
|
|
Mito-DK is a small-molecule fluorescent dye with the capability of crosstalk-free response to polarity and mtDNA as well as mitochondrial morphology. Mito-DK has high photostability, low cytotoxicity, and good mitochondria-targeting properties. Mito-DK can be used for real-time tracking and multidimensional assessing of mitochondria-related pyroptosis in cancer cells .
|
-
- HY-151897
-
|
|
HDAC
|
Cancer
|
|
HDAC-IN-49 is a potent unselective HDAC (HDAC) inhibitor with IC50s of 13 nM, 14 nM, 21 nM, 1880 nM, and 10 nM for HDAC1, HDAC2, HDAC3, HDAC4, and HDAC6. HDAC-IN-49 demonstrates prominent antileukemic activity with low cytotoxic activity toward healthy cells .
|
-
- HY-162956
-
|
|
SARS-CoV
|
Infection
|
|
SARS-CoV-2-IN-97 (Compound CO-01) is an inhibitor for SARS-CoV-2 Nsp15 endoribonuclease with an IC50 of 53.5 μM. SARS-CoV-2-IN-97 exhibits low cytotoxicity in A549-AT cell with IC50 of 134 μM .
|
-
- HY-W010649R
-
-
- HY-142694
-
|
|
E1/E2/E3 Enzyme
|
Cardiovascular Disease
|
|
DCN1-UBC12-IN-2 is a potent and specific DCN1-UBC12 inhibitor (IC50=9.55 nM). DCN1-UBC12-IN-2 could specifically target DCN1-UBC12 interaction and relieve Ang II-induced cardiac fibroblast activation .
|
-
- HY-142691
-
-
- HY-144730
-
|
|
HIV
|
Inflammation/Immunology
|
|
gp120-IN-1 (compound 4e) is a potent HIV-1 gp120 inhibitor with an IC50 of 2.2 µM and CC50 of 100.90 µM. gp120-IN-1 shows anti-HIV-1 activity. gp120-IN-1 shows cytotoxicity in a dose dependent manner in SUP-T1 cells. gp120-IN-1 shows inhibition of gp120-mediated virus enter into cells .
|
-
- HY-146298
-
|
|
Bacterial
|
Infection
|
|
Mt KARI-IN-1 (Lead compound) is a potent Mycobacterium tuberculosis ketol-acid reductoisomerase (Mtb KARI) inhibitor with a Ki value of 3.06 μM .
|
-
- HY-142692
-
-
- HY-147721
-
|
|
Bacterial
|
Infection
|
|
Dihydropteroate synthase-IN-1 (compound 5g) is a potent dihydropteroate synthase (DHPS) inhibitor. Dihydropteroate synthase-IN-1 shows antimicrobial activities and antifungal activity. Dihydropteroate synthase-IN-1 inhibits cytochromes P450. Dihydropteroate synthase-IN-1 can bu used as diagnostic radio imaging material .
|
-
- HY-W010649
-
|
|
HSP
Epigenetic Reader Domain
ATP-binding cassette (ABC) transporters
Bacterial
Fungal
Antibiotic
|
Infection
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Isoxazole is a member of the five-membered heterocycle drug scaffold. Isoxazole has been used as a BET bromodomain inhibitor and can improve β-cell function in a diabetic mouse model. Isoxazole and its derivatives exhibit broad biological activities (such as antimicrobial, antibacterial, antifungal, antiviral, anticancer, anti-inflammatory, immunomodulatory, analgesic, anti-tuberculosis, and anti-diabetic effects). For example, the bicyclic Isoxazole can act as an HSP90 inhibitor, and the tricyclic Isoxazole is promising as a selective multidrug resistance protein (MRP1) inhibitor .
|
-
- HY-169166
-
|
|
HIV Protease
|
Infection
|
|
HIV-1 protease-IN-14 (compound 5ae) is a potent HIV-1 protease inhibitor with Ki values of 0.28, 56.9 nM for WT HIV-1 PR, R41T HIV-1 PR, respectively. HIV-1 protease-IN-14 shows low cytotoxicity .
|
-
- HY-146496
-
|
|
Bacterial
|
Infection
|
|
Antitubercular agent-20 (Compound 2d) is an orally active antitubercular agent. Antitubercular agent-20 shows excellent activity against MTB H37Rv and MDR-MTB strains (MIC: ＜0.016 µg/ml). Antitubercular agent-20 has low cytotoxicity and good tolerance in BALB/c mice .
|
-
- HY-172264
-
|
|
Antibiotic
Bacterial
DNA/RNA Synthesis
|
Infection
|
|
XT17 is an anthrone compound with broad-spectrum antibacterial activity. It exerts its antibacterial effect by disrupting the cell wall and inhibiting DNA synthesis. XT17 exhibits weak hemolytic activity, low cytotoxicity against mammalian cell lines, and a low frequency of drug resistance. Meanwhile, XT17 shows in vivo efficacy in a mouse corneal infection model induced by Staphylococcus aureus or Pseudomonas aeruginosa. Further docking studies have confirmed that XT17 can form a stable complex with bacterial gyrase. XT17 can be used in the research of the anti - infection field .
|
-
- HY-148842
-
|
|
Liposome
|
Others
|
|
C14-4 is an ionizable lipid utilized for the synthesis of lipid nanoparticles (LNPs). C14-4 enhances mRNA delivery, enabling the effective transport of mRNA to primary human T cells, which in turn induces functional protein expression. C14-4 demonstrates high transfection efficiency while maintaining low cytotoxicity .
|
-
- HY-144663
-
|
|
Bacterial
Thymidylate Synthase
|
Infection
|
|
MtTMPK-IN-1 (compound 3) is a potent Mycobacterium tuberculosis thymidylate kinase (MtTMPK) inhibitor with an IC50 value of 2.5 μM. MtTMPK-IN-1 has moderate to weak activity against Mtb H37Rv and low cytotoxicity in human fibroblast cells MRC-5. MtTMPK-IN-1 can be used for researching tuberculosis .
|
-
- HY-18620
-
DZ2002
1 Publications Verification
|
STAT
PI3K
NF-κB
MEK
ERK
Bacterial
Antibiotic
Akt
|
Inflammation/Immunology
|
|
DZ2002 is an orally active, reversible and low-cytotoxic type III SAHH inhibitor (Ki=17.9 nM), with good immunosuppressive activity. DZ2002 prevents the development of experimental dermal fibrosis by reversing the profibrotic phenotype of various cell types. DZ2002 can be used in studies of autoimmune diseases such as lupus syndrome and systemic sclerosis .
|
-
- HY-144823
-
|
|
Bacterial
|
Infection
|
|
Anti-MRSA agent 3 (compound 18) has highly inhibitory activity against Methicillin-resistant Staphylococcus aureus (MRSA) with MIC of 0.098 μg/ml, and low cytotoxicity in normal cells. Anti-MRSA agent 3 has relatively strong ability to destroy bacterial cell wall and membrane, high binding affinity to bacterial genomic DNA .
|
-
- HY-151593
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
dBRD4-BD1 is a selective and durable BRD4 degrader with an DC50 value of 280 nM (Dmax=77%). dBRD4-BD1 upregulates BRD2/3 protein level and shows low cytotoxicity than iBRD4-BD1 .
|
-
- HY-146495
-
|
|
Bacterial
|
Infection
|
|
Antitubercular agent-19 (Compound 1c) is an antitubercular agent. Antitubercular agent-19 shows excellent activity against MTB H37Rv and MDR-MTB strains (MIC: ＜0.016 µg/ml). Antitubercular agent-19 shows low cytotoxicity and relatively high acute lethal toxicity in BALB/c mice .
|
-
- HY-D0716
-
|
Fluo-3-pentaacetoxymethyl ester
|
Fluorescent Dye
|
Others
|
|
Fluo-3 AM is a fluorecent Ca 2+ chelator, with high affinity for calcium. Fluo-3 AM can specifically identify intracellular calcium ions, with high sensitivity, low cytotoxicity, increased AM acetylmethyl ester can enter the cell well, after being sheared by the intracellular esterase stay in the cell to bind to calcium ions, produce strong fluorescence .
|
-
- HY-146308
-
|
|
HIV
|
Infection
|
|
HIV-1 inhibitor-26 (compound 9a) is a potent HIV-1 reverse transcriptase (RT) inhibitor with an IC50 value of 1.4 μM. HIV-1 inhibitor-26 has low cytotoxicity with a CC50 of 1486 μM in PBMCs. HIV-1 inhibitor-26 can be used for researching AIDS .
|
-
- HY-149014
-
|
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
|
|
OX2R-IN-1 (compound 15) is a low cytotoxicity profile OX2R-IN-1 antagonist (a potential OX2R binder) with an IC50 value of 484 μM. OX2R-IN-1 (compound 15) can cross the BBB into the brain with a short half-life .
|
-
- HY-156325
-
|
|
SARS-CoV
|
Infection
|
|
SARS-CoV-2-IN-62 (Compound R3b) is an inhibitor of SARS-CoV-2 replication and has low cytotoxicity. SARS-CoV-2-IN-62 inhibits viral replication in Vero E6 cells and Calu-3 cells, with EC50 values of 2.97 μM and 3.82 μM, respectively .
|
-
- HY-168959
-
|
|
Parasite
|
Infection
|
|
Antiparasitic agent-25 (Compounds 11) is an orally active antiparasitic agent. Antiparasitic agent-25 inhibits both parasite invasion and replication ability and has irreversible action against Toxoplasma gondii, significantly reducing the replication rate of Toxoplasma gondii with an IC50 value of 6.33 μM, and demonstrates low cytotoxicity with a CC50 value of 285 μM .
|
-
- HY-156337
-
|
|
SARS-CoV
|
Infection
|
|
SARS-CoV-2-IN-63 (Compound R3e) is an inhibitor of SARS-CoV-2 replication and has low cytotoxicity. SARS-CoV-2-IN-63 inhibits viral replication in Vero E6 cells and Calu-3 cells, with EC50 values of 1.99 μM and 1.92 μM, respectively .
|
-
- HY-116170
-
|
|
Aldose Reductase
|
Cancer
|
|
SN34037 is a specific inhibitor of Aldo-keto reductase 1C3 (AKR1C3, EC 1.1.1.188) with the ability to inhibit the cytotoxic activity of PR-104A. SN34037-sensitive coumberone reduction provides a rapid and specific assay for AKR1C3 activity. SN34037 inhibits the aerobic cytotoxicity of PR-104A in TF1 erythroleukemia cells with high AKR1C3 expression, but not in Nalm6 pre-B acute lymphoblastic leukemia cells with low AKR1C3 expression .
|
-
- HY-146681
-
|
|
PAK
|
Cancer
|
|
PAK1-IN-1 is a potent and selective PAK1 inhibitor with an IC50 of 9.8 nM. PAK1-IN-1 inhibits the migration and invasion of PAK1-related tumour cells in a dose-dependent manner .
|
-
- HY-147772
-
-
- HY-144754
-
|
|
VEGFR
Apoptosis
|
Cancer
|
|
VEGFR-2-IN-13 (Compound 19a) is a potent VEGFR-2 inhibitor with an IC50 of 3.4 nM. VEGFR-2-IN-13 disrupts the HepG2 cell cycle by arresting the G2/M phase and induces apoptosis .
|
-
- HY-118362
-
|
|
Bacterial
|
Infection
|
|
Netzahualcoyonol is a quinone methyl triterpene isolated from the roots of Salacia multiflora (Lam.) DC. Netzahualcoyonol exhibits antibacterial and anti-biofilm activities. Netzahualcoyonol inhibits Gram-positive bacteria (MIC=3.26–52 μM). Additionally, Netzahualcoyonol demonstrates cytotoxicity against Hep G2 cells (IC50 = 1.95 μM) but exhibits low toxicity towards Vero cells .
|
-
- HY-139989
-
|
|
HIV
|
Infection
|
|
NBD-14270, a pyridine analogue, is a potent HIV-1 entry antagonist with an IC50 of 180 nM against 50 HIV-1 Env-pseudotyped viruses. NBD-14270 binds to HIV-1 gp120 and shows potent antiviral activity. NBD-14270 shows low cytotoxicity (CC50>100 μM) .
|
-
- HY-172461
-
|
|
Monoamine Oxidase
Cholinesterase (ChE)
|
Neurological Disease
|
|
MAO-IN-6 (Compound 3f) is a BBB permeable and reversible MAO-B inhibitor with an IC50 of 0.09 μM. MAO-IN-6 also exhibits certain inhibitory activities against AChE and BChE, with IC50 values of 4.48 μM and 17.03 μM, respectively. MAO-IN-6 has low cytotoxicity and can be used in the research of Alzheimer's disease .
|
-
- HY-121300
-
|
(-)-TAN2162
|
Antibiotic
Bacterial
Endothelin Receptor
CGRP Receptor
|
Infection
Cancer
|
|
Kendomycin ((−)-TAN 2162) is a polyketide antibiotic with remarkable antibacterial and cancer cells cytotoxic activities. Kendomycin tends to be bacteriostatic rather than bactericidal and inhibits the growth of the methicillin-resistant Staphylococcus aureus (MRSA) strain COL at a low concentration (MIC of 5 μg/mL). Kendomycin is a potent antagonist of the endothelin receptor and a calcitonin receptor agonist which plays its role as an anti-osteoporotic agent .
|
-
- HY-146421
-
|
|
NO Synthase
NF-κB
Reactive Oxygen Species
|
Inflammation/Immunology
|
|
Anti-inflammatory agent 21 (compound 9o) is an orally active and low cytotoxic anti-inflammatory agent, with an IC50 value of 0.76 μM for NO. Anti-inflammatory agent 21 acts via accumulation ROS and blocks the NF-κB/MAPK signaling pathway. Anti-inflammatory agent 21 can ameliorate cartilage destruction and inflammatory cell infiltration in arthritis rats model .
|
-
- HY-N0367
-
|
(E)-Anethole
|
Endogenous Metabolite
|
Cardiovascular Disease
Metabolic Disease
Endocrinology
Cancer
|
|
Trans-Anethole ((E)-Anethole) is an orally active phenylpropene derivative found in Foeniculum vulgare that is estrogenic at low concentrations and cytotoxic at high concentrations in tumor cell lines. Trans-Anethole also has anti-aflatoxin, anti-thrombotic and anti-diabetic activities. Trans-Anethole is an important odor component in plants such as fennel, myrtle, liquorice, and camphor .
|
-
- HY-146158
-
|
WX-081
|
Bacterial
Potassium Channel
Antibiotic
|
Infection
|
|
Fudapirine, an anti-tuberculosis agent, displays excellent anti-mycobacterial activity against M. tuberculosis H37Rv and low cytotoxicity. Fudapirine exhibits potent activity with MIC50s of 0.083 and 0.11 μg/mL for agent susceptible tuberculosis (DS-TB) and multidrug resistant tuberculosis (MDR-TB) strains. Fudapirine also inhibits hERG channel with the IC50 of 1.89 μM.
|
-
- HY-N6640
-
|
20-Hydroxyeedysone 2-acetate
|
Amyloid-β
|
Neurological Disease
|
|
2-O-Acetyl-20-hydroxyecdysone, an ecdysterones in insects and terrestrial plants, inhibits amyloid-β42 (Aβ42)-induced cytotoxicity. 2-O-Acetyl-20-hydroxyecdysone could decrease Aβ oligomer formation through promotion of fibrogenesis, transforming Aβ oligomers to the low-toxicity fibrils .
|
-
- HY-101902
-
|
Quin-2 acetoxymethyl ester
|
Fluorescent Dye
|
Others
|
|
Quin-2AM is a fluorecent Ca 2+ chelator, with high affinity for calcium. Quin-2AM can specifically identify intracellular calcium ions, with high sensitivity, low cytotoxicity, increased AM acetylmethyl ester can enter the cell well, after being sheared by the intracellular esterase stay in the cell to bind to calcium ions, produce strong fluorescence .
|
-
- HY-147556
-
|
|
Potassium Channel
|
Cancer
|
|
SK3 Channel-IN-1 (compound 7a) is a potent and specific SK3 channel modulator. SK3 Channel-IN-1 has efficient effect on breast cancer MDA-MB-435 cell migration while exhibiting low cytotoxicity in other cell lines. SK3 Channel-IN-1 can modulate ion channels’activity in cancer .
|
-
- HY-P4836A
-
|
|
Parasite
|
Infection
|
|
LL-37 FK-13 TFA is the TFA salt form of LL-37 FK-13 (HY-P4836). LL-37 FK-13 TFA is an antimicrobial agent, that inhibits Trichomonas vaginalis. LL-37 FK-13 TFA exhibits minimal hemolytic effects on human erythrocytes and low cytotoxicity to human fibroblasts .
|
-
- HY-D1498
-
|
|
Fluorescent Dye
|
Others
|
|
Mag-Fluo-4 AM is a fluorecent Ca 2+ chelator, with high affinity for calcium. Mag-Fluo-4 AM can specifically identify intracellular calcium ions, with high sensitivity, low cytotoxicity, increased AM acetylmethyl ester can enter the cell well, after being sheared by the intracellular esterase stay in the cell to bind to calcium ions, produce strong fluorescence .
|
-
- HY-156087G
-
|
|
Apoptosis
Necroptosis
|
Cancer
|
|
Cholicamideβ (GMP) is a GMP grade of Cholicamideβ. Cholicamideβ (compound 6) is a self-assembling, small molecule, cancer vaccine adjuvant. Cholicamideβ can form virus-like particles with low cytotoxicity. Cholicamideβ, upon binding to peptide antigens, enhances antigen presentation by dendritic cells and induces antigen-specific T cells. Cholicamideβ can induce apoptosis and necrosis .
|
-
- HY-161404
-
|
|
Bacterial
|
Infection
|
|
Antibacterial agent 202 (compound 45c) is a low cytotoxicity bacterial inhibitor with good activity against Gram-negative bacteria, including Escherichia coli, Klebsiella pneumonia, especially Pseudomonas aeruginosa, (MIC (minimum inhibitory concentration)=7.8-31.25 μM). Antibacterial agent 202 can exert antibacterial activity by destroying the integrity of cell membranes and can be used in the research of bacterial infections .
|
-
- HY-149223
-
|
|
Bacterial
|
Infection
|
|
FtsZ-IN-5 is a potent FtsZ inhibitor, to promote FtsZ polymerization and inhibit GTPase activity of FtsZ. Thus, FtsZ-IN-5 inhibits bacterial division to lead to death of bacterial cells. FtsZ-IN-5 shows bactericidal activity with no significant tendency to trigger bacterial resistance as well as rapid bactericidal properties. And FtsZ-IN-5 shows low hemolytic activity and cytotoxicity to mammalian cells .
|
-
- HY-149226
-
|
|
Bacterial
|
Infection
|
|
FtsZ-IN-8 is a potent FtsZ inhibitor, to promote FtsZ polymerization and inhibit GTPase activity of FtsZ. Thus, FtsZ-IN-8 inhibits bacterial division to lead to death of bacterial cells. FtsZ-IN-8 shows bactericidal activity with no significant tendency to trigger bacterial resistance as well as rapid bactericidal properties. And FtsZ-IN-8 shows low hemolytic activity and cytotoxicity to mammalian cells .
|
-
- HY-N8374
-
|
|
Parasite
|
Infection
|
|
Pheanthine (Compound 2) is an antiplasmodial agent, that inhibits chloroquine-resistant Plasmodium falciparum K-1 (IC50 is 0.8 μM) and chloroquine-sensitive P. falciparum strain NF54 A19A (IC50 of 0.03 μM). Pheanthine exhibits low cytotoxicity in human lung fibrosblast (MRC-5, IC50 is 11.2 μM) and macrophages (PMM, IC50 is 8 μM) .
|
-
- HY-156087
-
|
|
Apoptosis
Necroptosis
|
Cancer
|
|
Cholicamideβ (GMP) is a GMP grade of Cholicamideβ. Cholicamideβ (compound 6) is a self-assembling, small molecule, cancer vaccine adjuvant. Cholicamideβ can form virus-like particles with low cytotoxicity. Cholicamideβ, upon binding to peptide antigens, enhances antigen presentation by dendritic cells and induces antigen-specific T cells. Cholicamideβ can induce apoptosis and necrosis .
|
-
- HY-149225
-
|
|
Bacterial
|
Infection
|
|
FtsZ-IN-7 is a potent FtsZ inhibitor, to promote FtsZ polymerization and inhibit GTPase activity of FtsZ. Thus, FtsZ-IN-7 inhibits bacterial division to lead to death of bacterial cells. FtsZ-IN-7 shows bactericidal activity with no significant tendency to trigger bacterial resistance as well as rapid bactericidal properties. And FtsZ-IN-7 shows low hemolytic activity and cytotoxicity to mammalian cells .
|
-
- HY-149224
-
|
|
Bacterial
|
Infection
|
|
FtsZ-IN-6 is a potent FtsZ inhibitor, to promote FtsZ polymerization and inhibit GTPase activity of FtsZ. Thus, FtsZ-IN-6 inhibits bacterial division to lead to death of bacterial cells. FtsZ-IN-6 shows bactericidal activity with no significant tendency to trigger bacterial resistance as well as rapid bactericidal properties. And FtsZ-IN-6 shows low hemolytic activity and cytotoxicity to mammalian cells .
|
-
- HY-151482
-
|
|
SARS-CoV
|
Infection
|
|
SARS-CoV-2 Mpro-IN-2 (compound GC-14) is a selective, low cytotoxic and non-covalent M pro inhibitor (IC50=0.40 μM) with good anti-SARS-CoV-2 activity (EC50=1.1 μM). SARS-CoV-2 Mpro-IN-2 can be used in COVID-19 studies .
|
-
- HY-157382
-
|
|
Cholinesterase (ChE)
Amyloid-β
MMP
|
Neurological Disease
|
|
AChE-IN-51 (compound 8C) is an orally active, non-competitive inhibitor of AChE and BChE (IC50: 84 nM, 97 nM). It also inhibits MMP-2 and amyloid Aβ1-42 aggregates (IC50: 724 nM, 302 nM). AChE-IN-51 has low cytotoxicity and in silico predicted blood-brain barrier permeability. Can be used for research on diseases such as Alzheimer's disease (AD) .
|
-
- HY-163435
-
|
|
Apoptosis
Caspase
PARP
Bcl-2 Family
|
Cancer
|
|
Anticancer agent 201 (Compound 2f) has IC50 values in the low micromolar range for multiple tumor cell lines. Anticancer agent 201 is highly cytotoxic to CCRF-CEM cells in vitro, inducing apotosis by activating caspase-3 in the intrinsic mitochondrial pathway and lysis of PARP, as well as reducing the expression of Bcl-2 and Bcl-XL proteins. Anticancer agent 201 can be used in cancer research .
|
-
- HY-N3497
-
|
|
NF-κB
DNA/RNA Synthesis
Parasite
Apoptosis
|
Infection
Cancer
|
|
Isochamaejasmin is a biflavonoid with anti-cancer, antiplasmodial and insecticidal activities. Isochamaejasmin displays a potent NF-κB (NF-κB) activation activity. Isochamaejasmin could cause DNA damage and induce apoptosis via the mitochondrial pathway in AW1 cells . Isochamaejasmin also has a moderate antiplasmodial activity (IC50 of 7.3 μM for P. falciparum) and relatively low cytotoxicity (CC50 of 29.0 μM) .
|
-
- HY-155540
-
|
|
SARS-CoV
|
Infection
|
|
SARS-CoV-2 3CLpro-IN-14 (compound 11j) is an orally active SARS-CoV-2 3CLpro inhibitor. SARS-CoV-2 3CLpro-IN-14 shows significant anti-SARS-CoV-2 activity (EC50 = 0.18 μM) and low cytotoxicity (CC50 > 50 μM) in Vero E6 cells .
|
-
- HY-15096
-
|
FJ-776
|
Fluorescent Dye
HSP
|
Cancer
|
|
MKT-077 (FJ-776), a highly water-soluble mitochondrial dye, has significant antitumor activity . MKT-077 exhibits low cytotoxicity, and inhibits broad-spectrum human cancer cell lines (colon cancer, breast cancer, pancreatic cancer). MKT-077 inhibits the growth of tumor in nude mice enograft tumor model. Ex/Em=488/543 nm .
|
-
- HY-126726
-
|
|
Biochemical Assay Reagents
|
Others
|
|
Oxidized low-density lipoprotein (oxLDL) particles contain low molecular weight species that are cytotoxic and proatherogenic. Many of these species were recently isolated and purified from oxLDL and identified as phosphatidylcholine species containing fragmented oxidized short-chain fatty acid residues at the sn-2 position. 1-(Palmitoyl)-2-(5-keto-6-octene-dioyl)phosphatidylcholine or KOdiA-PC is one of the most potent CD36 ligands of the oxLDL species. KOdiA-PC confers CD36 scavenger receptor binding affinity to LDL at a frequency of only 2 to 3 KOdiA-PC molecules/LDL particle and may be one of the more important structural determinants of oxLDL.
|
-
- HY-158379
-
|
|
Parasite
|
Infection
|
|
Antiparasitic agent-22 (Compound 24) is a pan antiparasitic agent, that inhibits T. Brucei, L. infantum, L. tropica promastigotes (IC50 of 2.41, 5.95, 8.98 μM), L. infantum amastigotes (IC50 of 8.18 μM) and P. falciparum W2 strain (IC50 of 0.155 μM). Antiparasitic agent-22 exhibits low cytotoxicity against THP1, with CC50 of 64.16 μM .
|
-
- HY-155981
-
|
|
SARS-CoV
|
Infection
|
|
SARS-CoV-2 3CLpro-IN-18 (Compound 3C) is a covalent SARS-CoV-2 3CLpro inhibitor (IC50s: 0.478 μM). SARS-CoV-2 3CLpro-IN-18 inhibits SARS-CoV-2 in Vero E6 cells (EC50= 2.499 μM) with low cytotoxicity (CC50 > 200 μM) .
|
-
- HY-146557
-
|
|
Bacterial
|
Infection
|
|
Antitubercular agent-16 (Compound 5q) is an antitubercular agent with MIC90 values of 0.40, 20.11, 23.51, 19.62, 10.93 and 13.62 μg/mL against M. tuberculosis H37Rv, CF16, CF61, CF76, CF152 and CF161, respectively. Antitubercular agent-16 shows low cytotoxicity against macrophages and pulmonary fibroblasts .
|
-
- HY-N0674A
-
|
13-Methylpalmatine chloride
|
Bcl-2 Family
Caspase
PARP
p38 MAPK
Parasite
Autophagy
|
Infection
Cancer
|
|
Dehydrocorydaline chloride (13-Methylpalmatine chloride) is an alkaloid that regulates protein expression of Bax, Bcl-2; activates caspase-7, caspase-8, and inactivates PARP . Dehydrocorydaline chloride elevates p38 MAPK activation. Anti-inflammatory and anti-cancer activities . Dehydrocorydaline chloride shows strong anti-malarial effects (IC50 =38 nM), and low cytotoxicity (cell viability > 90%) using P. falciparum 3D7 strain .
|
-
- HY-161260
-
|
|
P-glycoprotein
|
Cancer
|
|
P-gp inhibitor 20 (compound H27) is a low cytotoxicity P-glycoprotein (P-gp) inhibitor. P-gp inhibitor 20 inhibits the efflux function of P-gp in a dose-dependent manner (without affecting the expression of P-gp), thereby reversing the multidrug resistance (MDR) of MCF-7/ADR cells, with an IC50 value of 46.6 nM. P-gp inhibitor 20 can be used for cancer research .
|
-
- HY-146556
-
|
|
Bacterial
|
Infection
|
|
Antitubercular agent-15 (Compound 5n) is an antitubercular agent with MIC90 values of 0.73, 7.69, 9.38, 18.80, 7.53 and 7.31 μg/mL against M. tuberculosis H37Rv, CF16, CF61, CF76, CF152 and CF161, respectively. Antitubercular agent-15 shows low cytotoxicity against macrophages and pulmonary fibroblasts .
|
-
- HY-157940
-
|
|
Endothelin Receptor
|
Infection
|
|
Methylsolfonyl 25(S)-Δ7-dafachronic acid (compound 3) is a selective ssDAF-12 agonist with the IC50 of 0.41 μM. Methylsolfonyl 25(S)-Δ7-dafachronic acid shows low cell cytotoxicity in HepG2 cells with IC50 of >200 μM. Methylsolfonyl 25(S)-Δ7-dafachronic acid can be used for study of parasitism .
|
-
- HY-161985
-
|
|
PPAR
|
Metabolic Disease
|
|
PPARγ-IN-3 (compound 9ga) is a potent and orally active PPARγ inhibitor. PPARγ-IN-3 reduces triglyceride (TG) accumulation with low cytotoxicity. PPARγ-IN-3 preventes the excessive growth of body weight and lessened fat mass as well as liver mass, decreases lipid accumulation in the liver and blood. PPARγ-IN-3 has the potential for the research of diet-induced obesity .
|
-
- HY-129149
-
|
|
HMG-CoA Reductase (HMGCR)
|
Metabolic Disease
|
|
Ganoderic acid SZ is a natural product with 3-hydroxy-3-methylglutaryl-CoA reductase inhibitory activity. Ganoderic acid SZ shows stronger activity than the positive control atorvastatin in inhibiting HMG-CoA reductase. Ganoderic acid SZ exhibits significant inhibition of yeast-derived α-glucosidase with IC50 values achieved at very low concentrations. Ganoderic acid SZ also exhibits cytotoxicity against K562 cells with IC?? values in the range of 10-20 μM .
|
-
- HY-170688
-
|
|
Bacterial
Reactive Oxygen Species
|
Infection
|
|
Antibacterial agent 119 (Compound 21 g) is an antibacterial candidate against Methicillin (HY-121544)-resistant Staphylococcus aureus (MICs less than 1 μg/mL against tested strains). Antibacterial agent 119 induces ROS production. Antibacterial agent 119 also acts on the bacterial cell membrane to cause membrane breakage. Antibacterial agent 119 exhibits potent antibacterial activity with low cytotoxicity, rapid bactericidal ability, and good in vivo antibacterial activity .
|
-
- HY-146057
-
|
|
Bacterial
|
Infection
|
|
Antituberculosis agent-2 (Compound 8d) is an antituberculosis agent against agent-sensitive and multidrug-resistant tuberculosis. Antituberculosis agent-2 shows anti-tuberculosis activity with MIC values of 0.454, 1.757 and 1.644 μg/mL against M. tuberculosis H37Rv, 13946 and 14862, respectively. Antituberculosis agent-2 displays favorable mouse and human microsomal stability, low cytotoxicity, and acceptable oral bioavailability .
|
-
- HY-135646
-
|
|
Influenza Virus
|
Infection
Inflammation/Immunology
|
|
Eleutheroside B1, a coumarin compound, has a wide spectrum of anti-human influenza virus efficacy, with an IC50 value of 64-125 µg/ml. Eleutheroside B1 mediates its anti-influenza activity through POLR2A and N-glycosylation. Eleutheroside B1 inhibits the mRNA expression of several chemokine genes and the influenza nucleoprotein (NP) gene, and exhibits low cytotoxicity. Antiviral and anti-inflammatory activities .
|
-
- HY-146018
-
|
|
HIV
|
Infection
|
|
HIV-1 inhibitor-23 (compound 12a) is a highly potent HIV-1 non-nucleoside reverse transcriptase inhibitor, with EC50s of 24.9 nM and 10.4 nM for HIV-1 WT and HIV-1 K103N, respectively. HIV-1 inhibitor-23 has low cytotoxicity (CC50 > 221 μM) and a favorable in vitro microsomal stability .
|
-
- HY-115829
-
|
|
HIV
|
Infection
|
|
APA-H-MPO hydrochloride is an inhibitor of PCAF bromodomain/Tat-AcK50 interaction with potential for anti-HIV/AIDS. APA-H-MPO hydrochloride can effectively inhibit the binding of PCAF bromodomain to Tat-AcK50. APA-H-MPO hydrochloride showed low cytotoxicity in preliminary cell studies. APA-H-MPO hydrochloride is considered a potential candidate for a promising inhibitory strategy targeting the host cell protein PCAF BRD to block HIV replication .
|
-
- HY-N0674B
-
|
13-Methylpalmatine (hydroxyl)
|
Bcl-2 Family
Caspase
PARP
p38 MAPK
Parasite
Autophagy
|
Infection
Inflammation/Immunology
Cancer
|
|
Dehydrocorydaline (13-Methylpalmatine) hydroxyl is an alkaloid that regulates protein expression of Bax, Bcl-2; activates caspase-7, caspase-8, and inactivates PARP. Dehydrocorydaline hydroxyl elevates p38 MAPK activation. Anti-inflammatory and anti-cancer activities. Dehydrocorydaline hydroxyl shows strong anti-malarial effects (IC50=38 nM), and low cytotoxicity (cell viability > 90%) using P. falciparum 3D7 strain.
|
-
- HY-116971
-
|
|
Histone Methyltransferase
Apoptosis
|
Cancer
|
|
DCG066 is an inhibitor of lysine methyltransferase G9a. DCG066 can bind directly to G9a and inhibit methyltransferase activity in vitro. DCG066 decreases di-methylation levels of histone H3 lysine 9 (H3K9Me2), inhibits cell proliferation and induces cell apoptosis. DCG066 displays low cytotoxicity in leukemia cell lines with high levels of G9a expression, including K562 .
|
-
- HY-N0674
-
|
13-Methylpalmatine
|
Bcl-2 Family
Caspase
PARP
p38 MAPK
Parasite
Autophagy
|
Infection
Cancer
|
|
Dehydrocorydaline (13-Methylpalmatine) is an alkaloid that regulates protein expression of Bax, Bcl-2; activates caspase-7, caspase-8, and inactivates PARP . Dehydrocorydaline elevates p38 MAPK activation. Anti-inflammatory and anti-cancer activities . Dehydrocorydaline shows strong anti-malarial effects (IC50=38 nM), and low cytotoxicity (cell viability > 90%) using P. falciparum 3D7 strain .
|
-
- HY-146782
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-49 is a potent and selective EGFR inhibitor with IC50s of 65.0 nM and 13.6 nM for EGFR T790M and EGFR T790M/L858R, respectively. EGFR-IN-49 induces late apoptosis in a dose-dependent manner .
|
-
- HY-145820
-
|
|
Apoptosis
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 14 is a potent NQO2 (quinone oxidoreductase 2) inhibitor with an IC50 of 1.0 μM. Tubulin inhibitor 14 also inhibits tubulin polymerization and the formation of endothelial cell capillary-like tubes. Tubulin inhibitor 14 is a microtubule-destabilizing agent with potential tumor-selectivity and antiangiogenic and vascular disrupting features .
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-
- HY-N0367R
-
|
|
Endogenous Metabolite
|
Cardiovascular Disease
Metabolic Disease
Endocrinology
Cancer
|
|
Trans-Anethole (Standard) is the analytical standard of Trans-Anethole. This product is intended for research and analytical applications. Trans-Anethole ((E)-Anethole) is an orally active phenylpropene derivative found in Foeniculum vulgare that is estrogenic at low concentrations and cytotoxic at high concentrations in tumor cell lines. Trans-Anethole also has anti-aflatoxin, anti-thrombotic and anti-diabetic activities. Trans-Anethole is an important odor component in plants such as fennel, myrtle, liquorice, and camphor .
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-
- HY-16712
-
|
|
TGF-β Receptor
|
Cancer
|
|
LDN-214117 is an orally active ALK2 inhibitor with well-tolerated and good brain penetration. LDN-214117 has a high selectivity and low cytotoxicity for ALK2 with an IC50 value of 24 nM. LDN-214117 also is a specific bone morphogenetic proteins (BMPs) signaling inhibitor and has relatively selective inhibition for BMP6 with an IC50 value of 100 nM. LDN-214117 can be used for the research of fibrodysplasia ossificans progressiva (FOP), diffuse intrinsic pontine glioma (DIPG) [2]
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-
- HY-146005
-
|
|
Microtubule/Tubulin
|
Neurological Disease
Inflammation/Immunology
|
|
Tau-aggregation and neuroinflammation-IN-1 is a potent tau-aggregation and neuroinflammation inhibitor. Tau-aggregation and neuroinflammation-IN-1 exhibits remarkable inhibitory activities against AcPHF6 and full-length tau aggregation. Tau-aggregation and neuroinflammation-IN-1 has a low cytotoxicity and reduced NO release in LPS-stimulated BV2 cells. Tau-aggregation and neuroinflammation-IN-1 can reverse okadaic acid-induced memory impairment in rats .
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-
- HY-152552
-
|
|
α-synuclein
|
Neurological Disease
|
|
α-Synuclein inhibitor 8 is an active inhibitor of α-Synuclein with an IC50 value of 2.5 µM. α-Synuclein inhibitor 8 has highly inhibition on the aggregation and disaggregation of α-Synuclein fibers. α-Synuclein inhibitor 8 reduces the formation of inclusions in neurons that can repairs damage neurons and improves Parkinson’s disease (PD)-like symptoms. α-Synuclein inhibitor 8 has high antioxidant activity and low cytotoxicity .
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-
- HY-156119
-
|
|
Mixed Lineage Kinase
Necroptosis
|
Metabolic Disease
Cancer
|
|
MLKL-IN-6 (compound P28) is a mixed lineage kinase inhibitor targeting Mixed Lineage Kinase domain-like (MLKL). MLKL-IN-6 inhibits cell necrosis. MLKL-IN-6 inhibits MLKL phosphorylation and oligomerization during cell necrosis, inhibits immune cell death, and reduces the expression of adhesion factors. MLKL-IN-6 has low cytotoxicity, and it inhibits hepatic stellate cell activation, reduces liver fibrosis marker levels, and has anti-fibrotic effects .
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-
- HY-N4238
-
|
13-Methylpalmatine nitrate
|
Bcl-2 Family
Caspase
PARP
p38 MAPK
Parasite
Autophagy
|
Infection
Cancer
|
|
Dehydrocorydaline nitrate (13-Methylpalmatine nitrate) is an alkaloid. Dehydrocorydaline regulates protein expression of Bax, Bcl-2; activates caspase-7, caspase-8, and inactivates PARP . Dehydrocorydaline nitrate elevates p38 MAPK activation. Anti-inflammatory and anti-cancer activities. . Dehydrocorydaline nitrate shows strong anti-malarial effects (IC50 =38 nM), and low cytotoxicity (cell viability > 90%) using P. falciparum 3D7 strain .
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-
- HY-151917
-
|
|
Apoptosis
Carbonic Anhydrase
Phosphodiesterase (PDE)
|
Cancer
|
|
Enpp/Carbonic anhydrase-IN-2 (compound 1i) is a potent Enpp and carbonic anhydrase inhibitor with IC50s of 1.13, 1.07, 0.74, 0.33, 0.68 for NPP1, NPP2, NPP3, CA-IX, CA-XII respectively. Enpp/Carbonic anhydrase-IN-2 shows antiproliferative activity for cancer cells and low cytotoxic against normal cells. Enpp/Carbonic anhydrase-IN-2 induces Apoptosis .
|
-
- HY-124623
-
|
|
Parasite
|
Infection
|
|
DNDI-8219 (compound 58) is a potent selective and orally active trypanocidal agent, possessing inhibitory activity against Trypanosoma cruzi (T. cruzi) with an IC50 of 0.4 μM. DNDI-8219 has low cytotoxicity (L6 cells IC50 > 100 μM). DNDI-8219 can effectively cure chronic T. cruzi infection and markedly reduce parasite burdens in mouse model. DNDI-8219 has good solubility, metabolic stability and safety.
|
-
- HY-W814315
-
|
CH5424802 analog; RO5424802 analog; RG7853 analog
|
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
|
Alectinib analog (CH5424802 analog) is a selective ALK inhibitor with activity in blocking resistance gating mutations. The synthetic optimization of alectinib analog allows it to be combined with specific peptides to improve the ability to target cancer cells. Alectinib analog exhibits low micromolar IC50 values in antiproliferation and shows good cytotoxic effects. The inhibitory activity of alectinib analog is closely related to its stability and release of active ingredients. Alectinib analog demonstrated the ability to inhibit vascular septal length or width in an in vivo zebrafish model .
|
-
- HY-149709
-
|
|
ICMT
|
Cancer
|
|
ICMT-IN-35 (compound 10n) is a FTPA-triazole compound and ICMT inhibitor (IC50=0.8 μM). ICMT-IN-35 is taken up by mammalian cells and can prevent K-Ras membrane localization and induce K-Ras mislocalization. Furthermore, ICMT-IN-35 is selectively cytotoxic against ICMT +/+ MEF cells and has low micromolar activity (IC50=0.8 μM) against metastatic pancreatic cancer cell lines .
|
-
- HY-151916
-
|
|
Apoptosis
Carbonic Anhydrase
Phosphodiesterase (PDE)
|
Cancer
|
|
Enpp/Carbonic anhydrase-IN-1 (compound 1e) is a potent Enpp and carbonic anhydrase inhibitor with IC50s of 1.36, 1.35, 3.00, 0.88, 1.02 μM for NPP1, NPP2, NPP3, CA-II, CA-IX respectively. Enpp/Carbonic anhydrase-IN-1 shows antiproliferative activity for cancer cells and low cytotoxic against normal cells. Enpp/Carbonic anhydrase-IN-1 induces Apoptosis .
|
-
- HY-12755
-
|
CID-2950007
|
Ras
Apoptosis
|
Cancer
|
|
ML141 (CID-2950007) is a potent, allosteric, selective and reversible non-competitive inhibitor of Cdc42 GTPase. ML141 inhibits Cdc42 wild type and Cdc42 Q61L mutant with EC50s of 2.1 and 2.6 μM, respectively. ML141 shows low micromolar potency and selectivity against other members of the Rho family of GTPases (Rac1, Rab2, Rab7). ML141 do not show cytotoxicity in multiple cell lines .
|
-
- HY-149058
-
|
|
Influenza Virus
|
Infection
|
|
Neuraminidase-IN-13 (Compound 10) is a neuraminidase inhibitor with antiviral activity and low cytotoxicity. Neuraminidase-IN-13 significantly inhibits NDV infection of Vero cells by preventing the release of viral particles from infected cells . Neuraminidase-IN-13 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
|
-
- HY-154978
-
|
|
Others
|
Cancer
|
|
Cisplatin-resistant cells-IN-1 (Compound 8) has high cytotoxicity against Cisplatin (HY-17394)-resistant cells. Cisplatin-resistant cells-IN-1 reduces the metabolic activity effectively in the low nanomolar range (IC50: 0.14–1.79 μM in A549/A549-R, K562/K562-R, and MCF-7/MCF-7TamR cells) .
|
-
- HY-112146
-
MMG-11
2 Publications Verification
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
MMG-11 is a potent and selective human TLR2 antagonist with low cytotoxicity. MMG-11 inhibits both TLR2/1 and TLR2/6 signaling with IC50s of 1.7 µM for Pam3CSK4-induced hTLR2/1 and 5.7 µM for Pam2CSK4-induced hTLR2/6 responses .
|
-
- HY-146352
-
|
|
HIV
|
Infection
Inflammation/Immunology
|
|
HIV-1 inhibitor-28 (compound 14j2) is a highly potent and selective HIV-1 inhibitor with an EC50 of 58 nM for WT HIV-1 strain and an IC50 of 3.37 μM for HIV-1 WT reverse transcription (RT). HIV-1 inhibitor-28 exhibits relatively low cytotoxicity in MT-4 cells (CC50 = 38.6 μM). HIV-1 inhibitor-28 can be used for researching AIDS .
|
-
- HY-146339
-
|
|
HIV
|
Infection
Inflammation/Immunology
|
|
HIV-1 inhibitor-27 (compound 5) is a potent HIV-1 inhibitor with IC50s of 16 μM, 0.5 μM and 0.39 μM for HIV-1 YU2, NL4-3 and 89.6 strain, respectively. HIV-1 inhibitor-27 has low cytotoxicity with a CC50 of 128 μM in TZM-bl cells. HIV-1 inhibitor-27 can be used for researching AIDS .
|
-
- HY-161674
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
Monoamine Oxidase B inhibitor 4 (compound 1l) is a selective inhibitor of human monoamine oxidase-B (hMAO-B) (IC50=8.3 nM). Monoamine Oxidase B inhibitor 4 also has anti-neuroinflammatory and low neurotoxicity. Monoamine Oxidase B inhibitor 4 can inhibit the release of NO, TNF-α and IL-1β stimulated by LPS and Aβ1-42, and can also attenuate Aβ(1-42)-induced cytotoxicity .
|
-
- HY-112146A
-
|
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
MMG-11 quarterhydrate is a potent and selective human TLR2 antagonist with low cytotoxicity. MMG-11 quarterhydrate inhibits both TLR2/1 and TLR2/6 signaling with IC50s of 1.7?μM for Pam3CSK4-induced hTLR2/1 and 5.7?μM for Pam2CSK4-induced hTLR2/6 responses .
|
-
- HY-144098
-
|
|
Parasite
HDAC
|
Others
|
|
HDAC8-IN-2 (compound 5o) is a potent HDAC8 inhibitor, with IC50 values of 0.27 and 0.32 μM for smHDAC8 (Schistosoma mansoni histone deacetylase 8) and hHDAC8, respectively. HDAC8-IN-2 shows significant killing of the schistosome larvae. HDAC8-IN-2 markedly impairs egg laying of adult worm pairs .
|
-
- HY-144316
-
|
|
Cholinesterase (ChE)
GSK-3
|
Neurological Disease
|
|
ZLWH-23 is a selective AChE inhibitor (IC50=0.27 μM) with GSK-3β inhibitory property (IC50=6.78 μM). ZLWH-23 possesses selectivity for AChE over BChE (IC50=20.82 μM) and for GSK-3β over multi-kinases. ZLWH-23 has the potential for the research of Alzheimer's disease .
|
-
- HY-D1583
-
|
DBCO-Cy5; Cyanine5 dibenzocyclooctyne
|
Fluorescent Dye
|
Others
|
|
Cyanine5 DBCO (DBCO-Cy5) is a low-toxicity azide reactive probe (NIR fluorescent dye), for imaging azide-labeled biomolecules via a copper-free "click-through" reaction. Cyanine5 DBCO has no apparent cytotoxicity or animal toxicity and shows no damage to the physiological functions of cells other than the target cells (azide-labeled cells). Cyanine5 DBCO can be used to label and track cells in vitro and in vivo (Ex=635 nm, Em=650-700 nm) .
|
-
- HY-146353
-
|
|
HIV
|
Infection
Inflammation/Immunology
|
|
HIV-1 inhibitor-29 (compound 14d2) is a potent HIV-1 inhibitor with an EC50 of 2.18 μM for HIV-1 IIIB. HIV-1 inhibitor-29 has high anti-resistance profile toward F227L/V106A strain (EC50 = 0.974 μM), and exhibits low cytotoxicity in MT-4 cells (CC50 = 211 μM). HIV-1 inhibitor-29 can be used for researching AIDS .
|
-
- HY-162492
-
|
|
Influenza Virus
|
Infection
|
|
Influenza A virus-IN-14 (Compound 37) is an inhibitor for influenza virus type A (IAV), which inhibits H1N1 with an EC50 of 23 nM. Influenza A virus-IN-14 exhibits low cytotoxicity with CC50 of more than 100 μM. Influenza A virus-IN-14 inhibits cytopathic effect and improves the survival rates of cell Calu3. Influenza A virus-IN-14 exhibits synergistic activity with the neuraminidase inhibitor Oseltamivir (HY-13317). Influenza A virus-IN-14 exhibits poor pharmacokinetic properties in CD-1 mouse .
|
-
- HY-146019
-
|
|
HIV
|
Infection
|
|
HIV-1 inhibitor-24 (compound S-12a) is a highly potent HIV-1 reverse transcriptase, with an IC50 value of 9.5 nM. HIV-1 inhibitor-24 has high antiretroviral activity against WT HIV-1 with an EC50 of 1.6 nM, and exhibits relatively low cytotoxicity with a CC50 of 9.07 μM in MT-4 cells. HIV-1 inhibitor-24 is well tolerated at a dose of 2 g/kg in mice and has a significant cardiovascular safety .
|
-
- HY-155527
-
|
|
SARS-CoV
|
Infection
|
|
SARS-CoV-2 Mpro-IN-9 (compound c7) is a nonpeptidic, noncovalent SARS-CoV-2 M pro inhibitor (IC50=0.085 μM), with improved physicochemical and drug metabolism and pharmacokinetics (DMPK) properties. SARS-CoV-2 Mpro-IN-9 inhibits viral replication (EC50=1.10 μM) in SARS-CoV-2-infected Vero E6 cells, while exhibits low cytotoxic effects (CC50>50 μM) .
|
-
- HY-139781
-
|
|
PD-1/PD-L1
|
Cancer
|
|
PD-L1-IN-1 is a potent PD-L1 inhibitor with an IC50 of 115 nM. PD-L1-IN-1 strongly binds with the PD-L1 protein and challenged it in a co-culture of PD-L1 expressing cancer cells (PC9 and HCC827 cells) and peripheral blood mononuclear cells enhanced antitumor immune activity of the latter. PD-L1-IN-1 significantly increased interferon γ release and apoptotic induction of cancer cells, with low cytotoxicity in healthy cells .
|
-
- HY-136910
-
|
USP7-IN-7
|
Deubiquitinase
MDM-2/p53
|
Cancer
|
|
USP7-797 (USP7-IN-7) is an orally available, selective USP7 inhibitor (IC50=0.5 nmol/L) with antitumor activity. USP7-797 reduces the level of MDM2, thereby increasing the stability and activity of p53, leading to cell cycle arrest and apoptosis. USP7-797 has low nanomolar cytotoxicity against p53 mutant cancer cell lines, p53 wild-type hematological tumors, and neuroblastoma cell lines .
|
-
- HY-146749
-
|
|
FLT3
Trk Receptor
Apoptosis
|
Cancer
|
|
FLT3/TrKA-IN-1 is a potent FLT3/TrKA dual kinase inhibitor with the IC50s of 43.8 nM, 97.2 nM, 92.5 nM and 23.6 nM for FLT3, FLT3-ITD, FLT3-TKD and TrKA, respectively. FLT3/TrKA-IN-1 induces cell cycle arrest at the G0/G1 phase as well as apoptosis and shows antiproliferative activity in vitro. FLT3/TrKA-IN-1 has the potential for the research of Acute myeloid leukemia (AML) .
|
-
- HY-147750
-
|
|
Phosphodiesterase (PDE)
|
Neurological Disease
Cancer
|
|
TDP1 Inhibitor-2 (compound 5) is a potent inhibitor for TDP1 (tyrosyl-DNA phosphodiesterase 1), with an IC50 of 99 nM. TDP1 Inhibitor-2 also can inhibit SCAN1 (spinocerebellar ataxia syndrome with axonal neuropathy), with an IC50 of 3.5 μM .
|
-
- HY-144393
-
|
|
BCRP
|
Cancer
|
|
P-gp/BCRP-IN-1 (compound 19) is a potential, relatively safe, orally active and efficient efflux transporter (P-gp and BCRP) inhibitor. P-gp/BCRP-IN-1 exerts resistance reversal by inhibiting the efflux function of P-gp and BCRP. P-gp/BCRP-IN-1 can overcome the resistance and improve the oral bioavailability of PTX (Paclitaxel) .
|
-
- HY-18957C
-
|
BGB-283 hydrochloride
|
Endogenous Metabolite
|
Cancer
|
|
Lifirafenib hydrochloride (BGB-283 hydrochloride) is a novel, reversible B-RAFV600E inhibitor with antitumor activity. Lifirafenib has shown potent antitumor activity against solid tumors with B-RAFV600E mutations, such as melanoma, thyroid cancer, and low-grade serous ovarian cancer. Lifirafenib exhibits selective cytotoxicity in vitro, preferentially inhibiting the proliferation of cancer cells with B-RAFV600E and EGFR mutations/amplification. Lifirafenib can achieve dose-dependent inhibition of tumor growth in animal models, accompanied by partial and complete tumor shrinkage .
|
-
- HY-151799
-
|
|
p62
E1/E2/E3 Enzyme
Apoptosis
|
Cancer
|
|
P62-RNF168 agonist-1 (compound 5a) is a low cytotoxicity P62-RNF168 agonist that enhances the interaction between P62 and RNF168. P62-RNF168 agonist-1 induces a reduction in H2A ubiquitination mediated by RNF168 and impairs homologous recombination-mediated DNA repair. P62-RNF168 agonist-1 also inhibits the growth of xenograft tumors in mice in a dose-dependent manner .
|
-
- HY-158138
-
|
|
PARP
Topoisomerase
Apoptosis
|
Cancer
|
|
TOPOI/PARP-1-IN-1 (Compound B6) is an orally active, low cytotoxic TOPOI/PARP dual inhibitor with an IC50 value of 0.09 μM for PARP1. TOPOI/PARP-1-IN-1 can effectively inhibit the proliferation and migration of cancer cells. TOPOI/PARP-1-IN-1 also causes cell cycle arrest in the G0/G1 phase and induces apoptosis. The tumor growth inhibition rate (TGI) of TOPOI/PARP-1-IN-1 in mice is 75.4% .
|
-
- HY-163783
-
|
|
Casein Kinase
|
Infection
|
|
CSNK2-IN-1 is a potent and selective CSNK2 inhibitor with IC50 of 1.7 nM and 0.66 nM for CSNK2A1 and CSNK2A2, respectively. CSNK2-IN-1 has antiviral activity against beta-coronaviruses such as SARS-CoV-2 and MHV. CSNK2-IN-1 has good solubility, metabolic stability, and low cytotoxicity, but its plasma concentration in vivo decreases rapidly and is insufficient to achieve pharmacological effects. CSNK2-IN-1 can be used in the research of antiviral drug development .
|
-
- HY-D1701
-
|
|
Fluorescent Dye
|
Others
|
|
Calcium is an important part of the human body, usually in the form of calcium, a large number of bones and teeth of the human body, a small amount of blood and tissues.
MCE calcium ion detection probe can specifically identify intracellular calcium ions, with high sensitivity, low cytotoxicity, increased AM acetylmethyl ester can enter the cell well, after being sheared by the intracellular esterase stay in the cell to bind to calcium ions, produce strong fluorescence, in addition, Mag-indo-1/AM and Mag-Fluo-4 AM at a certain concentration (usually 5 mM) can effectively identify intracellular magnesium ions .
|
-
- HY-157404
-
|
|
Pim
|
Cancer
|
|
Pim-1/2 kinase inhibitor 2 (compound 5b) is a competitive PIM-1 and PIM-2 kinase inhibitor with IC50s of 1.31 μM and 0.67 μM, respectively. Pim-1/2 kinase inhibitor 2 shows in-vitro low cytotoxicity against normal human lung fibroblast Wi-38 cell line and potent in-vitro anticancer activity against myeloid leukaemia (NFS-60), liver (HepG-2), prostate (PC-3), and colon (Caco-2) cancer cell lines .
|
-
- HY-101898
-
|
Indo-1 Acetoxymethyl ester
|
Fluorescent Dye
|
Others
|
|
Calcium is an important part of the human body, usually in the form of calcium, a large number of bones and teeth of the human body, a small amount of blood and tissues.
MCE calcium ion detection probe can specifically identify intracellular calcium ions, with high sensitivity, low cytotoxicity, increased AM acetylmethyl ester can enter the cell well, after being sheared by the intracellular esterase stay in the cell to bind to calcium ions, produce strong fluorescence, in addition, Mag-indo-1/AM and Mag-Fluo-4 AM at a certain concentration (usually 5 mM) can effectively identify intracellular magnesium ions .
|
-
- HY-144737
-
|
|
Bacterial
TNF Receptor
|
Infection
Inflammation/Immunology
|
|
Anti-inflammatory agent 15 (compound 29) is a potent antimycobacterial and anti-inflammatory agent. Anti-inflammatory agent 15 inhibits Mtb H37Rv and M299 growth, with MIC50 (minimum inhibitory concentration 50%) of 2.3 and 7.8 μM, respectively. Anti-inflammatory agent 15 inhibits NO through the suppression of iNOS expression, and also inhibited the production of TNF-α and IL-1β. Anti-inflammatory agent 15 can be used for tuberculosis (TB) research .
|
-
- HY-144727
-
|
|
Bacterial
TNF Receptor
|
Infection
Inflammation/Immunology
|
|
Anti-inflammatory agent 11 (compound 16) is a potent antimycobacterial and anti-inflammatory agent. Anti-inflammatory agent 11 inhibits Mtb H37Rv and M299 growth, with MIC50 (minimum inhibitory concentration 50%) of 1.3 and 6.9 μM, respectively. Anti-inflammatory agent 11 inhibits NO through the suppression of iNOS expression, and also inhibited the production of TNF-α and IL-1β. Anti-inflammatory agent 11 can be used for tuberculosis (TB) research .
|
-
- HY-D1244
-
|
|
Fluorescent Dye
|
Cardiovascular Disease
Inflammation/Immunology
|
|
CO probe 1 (probe 2) is a highly efficient fluorescent CO probe (Ex=493 nm) with an allyl ether reaction site. In the presence of PdCl₂, CO reduces Pd 2+ to Pd 0, triggering a Tsuji-Trost reaction that removes the allyl protecting group, releases fluorescein, and generates a significant fluorescence signal. CO probe 1 has high selectivity, rapid response (fluorescence enhancement of 150 times within 20 minutes), and low cytotoxicity, and can be used for real-time imaging of CO in living cells. CO probe 1 may be used to study pathological mechanisms involving CO signaling regulation, such as inflammation, vascular disease, or cancer .
|
-
- HY-147514
-
|
|
Apoptosis
Caspase
PARP
Bcl-2 Family
|
Cancer
|
|
Anticancer agent 64 (compound 5m) shows cytotoxic activity in CCRF-CEM cells, with IC50 of 2.4 μM. Anticancer agent 64 shows good anticancer activity through apoptosis induction. Anticancer agent 64 induces caspase 3 and 7 activation and PARP cleavage. Anticancer agent 64 induces significant effect of mitochondria depolarization .
|
-
- HY-169920
-
|
|
HIV
Reverse Transcriptase
|
Infection
|
|
HIV-1 inhibitor-79 (Compound 3k) is an HIV inhibitor that exhibits significant inhibitory activity against HIV-1 and its common mutant strains (with IC50 values of 1.9, 1.9, 8.7, and 11 nM against HIV-1, K103, L100I, and E138K, respectively), and has low cytotoxicity and a high selectivity index (CC50 = 21.95 μM, SI = 11478). Additionally, HIV-1 inhibitor-79 also shows antiviral activity against HIV-2, with an EC50 value of 6.14 μM, and significantly inhibits the activity of HIV-1 reverse transcriptase (IC50 = 25 nM) .
|
-
- HY-143464
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
BChE-IN-4 is a potent and cross the blood-brain barrier BChE inhibitor. BChE-IN-4 attenuates learning and memory deficits caused by cholinergic deficit in mouse model. BChE-IN-4 has the potential for the research of alzheimer’s disease .
|
-
- HY-130178
-
|
|
Endogenous Metabolite
|
Infection
|
|
CL-385319 is an N-substituted piperidine compound with inhibitory activity against H5N1 avian influenza A virus infection. CL-385319 exhibited an IC50 of 27.03±2.54 μM against infection of highly pathogenic H5N1 virus in Madin-Darby canine kidney cells (MDCK). CL-385319 had low cytotoxicity with a CC50 of 1.48 mM and was able to inhibit the entry of pseudoviruses carrying H5N1 strains from different sources, but had no inhibitory effect on the entry of VSV-G pseudotyped particles. Pseudoviruses with the M24A mutation in HA1 or the F110S mutation in HA2 were resistant to CL-385319, indicating that these two residues in the cavity region may be critical for the binding of CL-385319 .
|
-
- HY-146019A
-
|
|
HIV
|
Infection
|
|
HIV-1 inhibitor-25 (compound R-12a) is a highly potent HIV-1 reverse transcriptase, with an IC50 value of 0.1061 μM. HIV-1 inhibitor-25 has high antiretroviral activity against WT HIV-1 with an EC50 of 13.6 nM, and exhibits relatively low cytotoxicity with a CC50 of 33.13 μM in MT-4 cells. HIV-1 inhibitor-25 also has inhibitory activity against HIV-1 mutant strains (L100I, K103N, Y181C, Y188L, E138K, F227L+V106A) with EC50 of 0.1961 ~ 5.8136 μM. HIV-1 inhibitor-25 can be used for researching AIDS .
|
-
- HY-121642
-
|
|
Others
|
Others
|
|
SL-017 is a novel photoacoustic sensitizer and a derivative of photofrin B. It can be taken up by cells to the maximum extent within 30 minutes and is mainly localized in mitochondria. After being activated by visible light or ultrasound, SL-017 can significantly increase the production of reactive oxygen species (ROS). Low concentrations of SL-017 can rapidly cause the loss of mitochondrial membrane potential. SL-017 can also cause mitochondrial fragmentation, a process that occurs after the loss of membrane potential. Epoxyeicosatrienoic acids (EETs) can alleviate the loss of mitochondrial membrane potential caused by SL-017, but the antioxidant ascorbic acid has no such effect. These characteristics indicate that SL-017 mainly targets mitochondria and exerts its cytotoxic effect by triggering the collapse of mitochondrial membrane potential, generating ROS, and causing mitochondrial fragmentation. As a novel photoacoustic sensitizer, SL-017 has potential application value in photodynamic therapy and sonodynamic therapy.
|
-
- HY-W327027
-
|
|
Fluorescent Dye
|
Others
|
|
7-(2,4-Dinitrophenoxy)-4-methyl-2H-chromen-2-one (Compound 1) is a fluorescent probe for the detection of hydrogen sulfide (H2S). 7-(2,4-Dinitrophenoxy)-4-methyl-2H-chromen-2-one has a low detection limit (4×10 -6 mol/L), good selectivity and high sensitivity. 7-(2,4-Dinitrophenoxy)-4-methyl-2H-chromen-2-one shows almost no cytotoxicity at concentrations of 150 µg/mL. 7-(2,4-Dinitrophenoxy)-4-methyl-2H-chromen-2-one has the excitation peak of 331 nm, and the emission peak about 385 nm in DMSO solvent. Upon the addition of increasing amounts of HS -, the fluorescence intensity increases obviously at about 392 nm .
|
-
- HY-150979
-
|
|
Fluorescent Dye
|
Cancer
|
|
Gd-NMC-3 is a near-infrared fluorescence/magnetic resonance (NIRF/MR) bimodal imaging probe. Gd-NMC-3 shows high resolution and sensitivity in tumor imaging with good biocompatibility, indicating huge application potential .
|
-
| Cat. No. |
Product Name |
Type |
-
- HY-136213
-
|
|
Dyes
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Endoplasmic reticulum dye 1 is a promising live cell imaging agent for the detection of exocytotic events at the plasma membrane. Endoplasmic reticulum dye 1 shows low cytotoxicity, resistance to photobleaching , which is ideal for imaging either short- or long-time courses .
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- HY-D0716
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Fluo-3-pentaacetoxymethyl ester
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Fluorescent Dyes/Probes
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Fluo-3 AM is a fluorecent Ca 2+ chelator, with high affinity for calcium. Fluo-3 AM can specifically identify intracellular calcium ions, with high sensitivity, low cytotoxicity, increased AM acetylmethyl ester can enter the cell well, after being sheared by the intracellular esterase stay in the cell to bind to calcium ions, produce strong fluorescence .
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- HY-D1498
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Fluorescent Dyes/Probes
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Mag-Fluo-4 AM is a fluorecent Ca 2+ chelator, with high affinity for calcium. Mag-Fluo-4 AM can specifically identify intracellular calcium ions, with high sensitivity, low cytotoxicity, increased AM acetylmethyl ester can enter the cell well, after being sheared by the intracellular esterase stay in the cell to bind to calcium ions, produce strong fluorescence .
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- HY-15096
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MKT-077
Maximum Cited Publications
10 Publications Verification
FJ-776
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Dyes
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MKT-077 (FJ-776), a highly water-soluble mitochondrial dye, has significant antitumor activity . MKT-077 exhibits low cytotoxicity, and inhibits broad-spectrum human cancer cell lines (colon cancer, breast cancer, pancreatic cancer). MKT-077 inhibits the growth of tumor in nude mice enograft tumor model. Ex/Em=488/543 nm .
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- HY-D1583
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DBCO-Cy5; Cyanine5 dibenzocyclooctyne
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Fluorescent Dyes/Probes
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Cyanine5 DBCO (DBCO-Cy5) is a low-toxicity azide reactive probe (NIR fluorescent dye), for imaging azide-labeled biomolecules via a copper-free "click-through" reaction. Cyanine5 DBCO has no apparent cytotoxicity or animal toxicity and shows no damage to the physiological functions of cells other than the target cells (azide-labeled cells). Cyanine5 DBCO can be used to label and track cells in vitro and in vivo (Ex=635 nm, Em=650-700 nm) .
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- HY-101898
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Indo-1 Acetoxymethyl ester
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Fluorescent Dyes/Probes
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Calcium is an important part of the human body, usually in the form of calcium, a large number of bones and teeth of the human body, a small amount of blood and tissues.
MCE calcium ion detection probe can specifically identify intracellular calcium ions, with high sensitivity, low cytotoxicity, increased AM acetylmethyl ester can enter the cell well, after being sheared by the intracellular esterase stay in the cell to bind to calcium ions, produce strong fluorescence, in addition, Mag-indo-1/AM and Mag-Fluo-4 AM at a certain concentration (usually 5 mM) can effectively identify intracellular magnesium ions .
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- HY-141646
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Fluorescent Dyes/Probes
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MIT-PZR is a mitochondria-targeted,? low cytotoxicity fluorescent probe that can be used in live cells and in vivo imaging. Ex / Em = 485 / 705 nm
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- HY-101902
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Quin-2 acetoxymethyl ester
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Fluorescent Dyes/Probes
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Quin-2AM is a fluorecent Ca 2+ chelator, with high affinity for calcium. Quin-2AM can specifically identify intracellular calcium ions, with high sensitivity, low cytotoxicity, increased AM acetylmethyl ester can enter the cell well, after being sheared by the intracellular esterase stay in the cell to bind to calcium ions, produce strong fluorescence .
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- HY-156087G
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Fluorescent Dye
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Cholicamideβ (GMP) is a GMP grade of Cholicamideβ. Cholicamideβ (compound 6) is a self-assembling, small molecule, cancer vaccine adjuvant. Cholicamideβ can form virus-like particles with low cytotoxicity. Cholicamideβ, upon binding to peptide antigens, enhances antigen presentation by dendritic cells and induces antigen-specific T cells. Cholicamideβ can induce apoptosis and necrosis .
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- HY-D1701
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Fluorescent Dyes/Probes
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Calcium is an important part of the human body, usually in the form of calcium, a large number of bones and teeth of the human body, a small amount of blood and tissues.
MCE calcium ion detection probe can specifically identify intracellular calcium ions, with high sensitivity, low cytotoxicity, increased AM acetylmethyl ester can enter the cell well, after being sheared by the intracellular esterase stay in the cell to bind to calcium ions, produce strong fluorescence, in addition, Mag-indo-1/AM and Mag-Fluo-4 AM at a certain concentration (usually 5 mM) can effectively identify intracellular magnesium ions .
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- HY-D1244
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Fluorescent Dyes/Probes
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CO probe 1 (probe 2) is a highly efficient fluorescent CO probe (Ex=493 nm) with an allyl ether reaction site. In the presence of PdCl₂, CO reduces Pd 2+ to Pd 0, triggering a Tsuji-Trost reaction that removes the allyl protecting group, releases fluorescein, and generates a significant fluorescence signal. CO probe 1 has high selectivity, rapid response (fluorescence enhancement of 150 times within 20 minutes), and low cytotoxicity, and can be used for real-time imaging of CO in living cells. CO probe 1 may be used to study pathological mechanisms involving CO signaling regulation, such as inflammation, vascular disease, or cancer .
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- HY-150979
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Fluorescent Dyes/Probes
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Gd-NMC-3 is a near-infrared fluorescence/magnetic resonance (NIRF/MR) bimodal imaging probe. Gd-NMC-3 shows high resolution and sensitivity in tumor imaging with good biocompatibility, indicating huge application potential .
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| Cat. No. |
Product Name |
Type |
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- HY-W110888
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Biochemical Assay Reagents
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Brilliant Yellow, a diazo-containing sulfonic aci, is also a potent VGLUT-specific inhibitor. Brilliant Yellow is membrane-impermeable. However, there are some Brilliant Yellow analogs with low cytotoxicity and cell penetration. Brilliant Yellow analogs work on glutamatergic transmission in hippocampal neurons .
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- HY-148842
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Drug Delivery
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C14-4 is an ionizable lipid utilized for the synthesis of lipid nanoparticles (LNPs). C14-4 enhances mRNA delivery, enabling the effective transport of mRNA to primary human T cells, which in turn induces functional protein expression. C14-4 demonstrates high transfection efficiency while maintaining low cytotoxicity .
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- HY-126726
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Drug Delivery
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Oxidized low-density lipoprotein (oxLDL) particles contain low molecular weight species that are cytotoxic and proatherogenic. Many of these species were recently isolated and purified from oxLDL and identified as phosphatidylcholine species containing fragmented oxidized short-chain fatty acid residues at the sn-2 position. 1-(Palmitoyl)-2-(5-keto-6-octene-dioyl)phosphatidylcholine or KOdiA-PC is one of the most potent CD36 ligands of the oxLDL species. KOdiA-PC confers CD36 scavenger receptor binding affinity to LDL at a frequency of only 2 to 3 KOdiA-PC molecules/LDL particle and may be one of the more important structural determinants of oxLDL.
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- HY-W008864
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β-Octaacetyllactose
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Cell Assay Reagents
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Lactose octaacetate shows mild to moderate antifungal activity against some fungi, but it has low or no activity against bacteria and yeast. Lactose octaacetate shows low cytotoxicity to MDBK cells, Hep-2 and MDCK cells. Lactose octaacetate has antiviral activity against PV-1 .
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- HY-156087G
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Biochemical Assay Reagents
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Cholicamideβ (GMP) is a GMP grade of Cholicamideβ. Cholicamideβ (compound 6) is a self-assembling, small molecule, cancer vaccine adjuvant. Cholicamideβ can form virus-like particles with low cytotoxicity. Cholicamideβ, upon binding to peptide antigens, enhances antigen presentation by dendritic cells and induces antigen-specific T cells. Cholicamideβ can induce apoptosis and necrosis .
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| Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P4836A
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Parasite
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Infection
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LL-37 FK-13 TFA is the TFA salt form of LL-37 FK-13 (HY-P4836). LL-37 FK-13 TFA is an antimicrobial agent, that inhibits Trichomonas vaginalis. LL-37 FK-13 TFA exhibits minimal hemolytic effects on human erythrocytes and low cytotoxicity to human fibroblasts .
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- HY-144334
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|
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DNA/RNA Synthesis
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Infection
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CHIKV-IN-3 is a potent against two low-passage CHIKV inhibitor with EC50 values of 1.55 and 0.14 µM for CHIKV-122508 and CHIKV-6708, respectively. CHIKV-IN-3 acts on the host cells to interfere with the viral replication. CHIKV-IN-3 displays minimal cytotoxic liability(CC50 > 100 µM). Prophylactic effect .
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- HY-P4836
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|
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Parasite
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Infection
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LL-37 FK-13 is an antimicrobial agent, that inhibits Trichomonas vaginalis. LL-37 FK-13 exhibits slight hemolytic effects on human erythrocytes and low cytotoxicity to human fibroblasts .
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- HY-A0162R
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|
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Antibiotic
Bacterial
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Infection
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Bictegravir (sodium) (Standard) is the analytical standard of Bictegravir (sodium). This product is intended for research and analytical applications. Bictegravir sodium is a potent inhibitor of HIV-1 integrase, with an IC50 of 7.5 nM. Bictegravir sodium exhibits potent and selective anti-HIV activity and low cytotoxicity .
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| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
|
Classification |
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- HY-149058
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Azide
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Neuraminidase-IN-13 (Compound 10) is a neuraminidase inhibitor with antiviral activity and low cytotoxicity. Neuraminidase-IN-13 significantly inhibits NDV infection of Vero cells by preventing the release of viral particles from infected cells . Neuraminidase-IN-13 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
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| Cat. No. |
Product Name |
|
Classification |
-
- HY-148842
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|
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Cationic Lipids
Cationic Lipids
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C14-4 is an ionizable lipid utilized for the synthesis of lipid nanoparticles (LNPs). C14-4 enhances mRNA delivery, enabling the effective transport of mRNA to primary human T cells, which in turn induces functional protein expression. C14-4 demonstrates high transfection efficiency while maintaining low cytotoxicity .
|
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- HY-148172
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Nucleosides and their Analogs
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L-Fd4A is an adenine derivative. L-Fd4A has anti-human immunodeficiency virus (HIV) (EC50=1.5 μM) and anti-hepatitis B virus (HBV) (EC50=1.7 μM) activity. L-Fd4A has low cytotoxicity .
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- HY-148170
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Nucleosides and their Analogs
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L-I-OddU, a L-5'-halo- dioxolane nucleoside analogue, is a potent and selective anti-Epstein-Barr virus (EBV) agent with an EC50 value of 0.03μM. L-I-OddU has low cytotoxicity with a CC50 value of 1000 nM. L-I-OddU has antiviral activity by suppressing replicative EBV DNA and viral protein synthesis .
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- HY-156087
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|
|
|
Adjuvant
|
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Cholicamideβ (GMP) is a GMP grade of Cholicamideβ. Cholicamideβ (compound 6) is a self-assembling, small molecule, cancer vaccine adjuvant. Cholicamideβ can form virus-like particles with low cytotoxicity. Cholicamideβ, upon binding to peptide antigens, enhances antigen presentation by dendritic cells and induces antigen-specific T cells. Cholicamideβ can induce apoptosis and necrosis .
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