Search Result
Results for "
selective cytotoxicity
" in MedChemExpress (MCE) Product Catalog:
3
Biochemical Assay Reagents
2
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-129905
-
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LLOMe hydrochloride; Leu-Leu methyl ester hydrochloride; H-Leu-Leu-OMe hydrochloride
|
Endogenous Metabolite
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Inflammation/Immunology
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L-Leucyl-L-Leucine methyl ester (LLOMe) hydrochloride, a dipeptide condensation product of L-leucine methyl ester generated by human monocytes or polymorphonuclear leukocytes, selectively eliminates lymphocytes with cytotoxic potential. L-Leucyl-L-Leucine methyl ester hydrochloride also can induce endolysosomal pathway stress .
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- HY-133122
-
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TNF Receptor
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Inflammation/Immunology
Cancer
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UCB-9260, an orally active compound, inhibits TNF signaling by stabilising an asymmetric form of the trimer. UCB-9260 is selective for TNF over other superfamily members, and binds TNF with a similar Kd of 13 nM .
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-
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- HY-P9948
-
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Campath-IH
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Apoptosis
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Cancer
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Alemtuzumab (Campath-IH) is a humanized monoclonal antibody against CD52. Alemtuzumab does not cross-react with murine CD52. Alemtuzumab selectively targets the CD52 antigen to induce profound lymphocyte depletion, followed by recovery of T and B cells with regulatory phenotypes. Alemtuzumab is capable of complement-dependent cytotoxicity and antibody-dependent cell-mediated cytotoxicity (ADCC), as well as induction of apoptosis. Alemtuzumab has the potential for B-cell chronic lymphocytic leukaemia research .
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-
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- HY-101374A
-
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(+)-BRD4780
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Imidazoline Receptor
Caspase
Mitochondrial Metabolism
Lactate Dehydrogenase
|
Cardiovascular Disease
Neurological Disease
Cancer
|
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AGN 192403 (BRD4780) hydrochloride is a potent and selective imidazoline-1 receptor antagonist with a Ki value of 42 nM. AGN 192403 hydrochloride is also a TMED9 inhibitor. AGN 192403 hydrochloride shows protective effects on oxidative cytotoxicity and mitochondrial inhibitor-induced cytotoxicity in astrocytes. AGN 192403 hydrochloride mitigates the proliferation and migration of differentiated glioma tumor cells. AGN 192403 hydrochloride can be used for glioma tumor and neurological diseases research .
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-
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- HY-12456
-
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Antibiotic
ADC Payload
DNA Alkylator/Crosslinker
Necroptosis
Apoptosis
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Cancer
|
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Duocarmycin SA is an orally active antitumor antibiotic with an IC50 of 10 pM . Duocarmycin SA is an extremely potent cytotoxic agent capable of inducing a sequence-selective alkylation of duplex DNA. Duocarmycin SA demonstrates synergistic cytotoxicity against glioblastoma multiforme (GBM) cells treated with proton radiation in vitro .
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- HY-13767
-
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SR259075; SR4233; Win59075; SML 0552; SR 259075; Tirazone
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DNA/RNA Synthesis
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Cancer
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Tirapazamine (SR259075) is an anticancer agent that shows selective cytotoxicity for hypoxic cells in solid tumors, thereby inducing single-and double-strand breaks in DNA, base damage, and cell death. Tirapazamine is an anticancer and bioreductive agent.Tirapazamine (SR259075) can enhance the cytotoxic effects of ionizing radiation in hypoxic cells .
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- HY-P9961
-
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GSK1841157; OMB-157
|
CD20
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Cancer
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Ofatumumab is a fully human anti-CD20 monoclonal antibody that induces antibody-dependent cell-mediated cytotoxicity (ADCC) and complement-dependent cytotoxicity (CDC) in CD20-expressing B lymphocytes. Ofatumumab has strong lytic activity against CD20-positive B lymphocytes and eliminates CD20-positive tumor cells through ADCC and CDC. Ofatumumab is particularly effective against drug-resistant cells with low CD20 expression and can be applied to the research of chronic lymphocytic leukemia (CLL) .
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-
-
- HY-12406
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VLX600
2 Publications Verification
|
Oxidative Phosphorylation
Mitochondrial Metabolism
Autophagy
|
Cancer
|
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VLX600 is an iron-chelating inhibitor of oxidative phosphorylation (OXPHOS). VLX600 causes mitochondrial dysfunction and induces a strong shift to glycolysis. VLX600 displays selective cytotoxic activity against malignant cell and induces autophagy. Anticancer activity .
|
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-
- HY-114322
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VZ185
2 Publications Verification
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
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VZ185 is a potent, fast, and selective von Hippel-Lindau based dual degrader probe of BRD9 and BRD7 with DC50s of 4.5 and 1.8 nM, respectively. VZ185 is cytotoxic in EOL-1 and A-402 cells, with EC50s of 3 nM and 40 nM, respectively .
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-
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- HY-111606
-
-
-
- HY-18976
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-
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- HY-P990026
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-
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- HY-132247
-
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Estrogen Receptor/ERR
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Cancer
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ErSO is a selective anticipatory unfolded protein response (a-UPR) activator. ErSO acts through ERα to elicit strong and sustained cytotoxic activation of the a-UPR. ErSO can be used for the research of cancer .
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- HY-10996A
-
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FGFR
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Neurological Disease
Cancer
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KHS101 hydrochloride is a selective neuronal differentiation inducer that can cross the blood-brain barrier. KHS101 hydrochloride exhibits selective cytotoxicity against glioblastoma multiforme (GBM). KHS101 hydrochloride interacts with transforming acidic coiled-coil protein (TACC3). KHS101 hydrochloride can be used in GBM research .
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- HY-135470
-
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P-7138
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Bacterial
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Infection
|
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Nifurpirinol (P-7138) is a selective prosubstrate of bacterial nitroreductase (NTR). NTR catalyzes the reduction of nifurpirinol to generate cytotoxic metabolites that induce apoptosis in target cells. Nifurpirinol selectively ablates NTR-expressing cells such as pancreatic β cells, osteoblasts, dopaminergic neurons, and podocytes in transgenic zebrafish models. Nifurpirinol can be used in regeneration studies and disease modeling such as focal segmental glomerulosclerosis (FSGS) .
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- HY-121087
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BCI-215
3 Publications Verification
|
Phosphatase
|
Cancer
|
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BCI-215 is a potent and tumor cell-selective dual specificity MAPK phosphatase (DUSP-MKP) inhibitor. BCI-215 has cytotoxicity for tumor cells but not normal cells .
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- HY-P1103
-
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CXCR
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Cancer
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CTCE-9908 is a potent and selective CXCR4 antagonist. CTCE-9908 induces mitotic catastrophe, cytotoxicity and inhibits migration in CXCR4-expressing ovarian cancer cells .
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- HY-D2318
-
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Fluorescent Dye
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Others
|
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Flipper-TR 5 is a Flipper probe containing a terminal carboxylate for retention on the plasma membrane. Flipper-TR 5 selectively labels the cytoplasmic membrane, and exhibits excellent mechanical sensitivity, negligible cytotoxicity and controllable phototoxicity .
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- HY-100746
-
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Autophagy
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Cancer
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STF-62247 is an autophagy inducer that selectively cytotoxic to VHL-deficient renal cell carcinoma (IC50 of 0.625 μM and 16 μM in RCC4 and RCC4/VHL cells, respectively) .
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- HY-157131
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TRP Channel
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Neurological Disease
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TRPV2-selective blocker 1 is a TRPV2-selective blocker that inhibits calcium influx and ionic currents. TRPV2-selective blocker 1 exhibits an IC50 of 6.3 μM against rat TRPV2, and shows no activity against TRPV1, TRPV3 or TRPV4 channels. TRPV2-selective blocker 1 attenuates macrophage phagocytosis, LPS-induced macrophage migration, and calcium microdomains generated by peripheral TRPV2. TRPV2-selective blocker 1 is non-cytotoxic and can be used to investigate the function of TRPV2 during immune processes .
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- HY-W028690
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DNMDP
4 Publications Verification
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Phosphodiesterase (PDE)
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Cancer
|
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DNMDP, a phosphodiesterase 3A (PDE3A) inhibitor, is a potent and selective cancer cell cytotoxic agent. DNMDP binding to PDE3A promotes an interaction between PDE3A and Schlafen 12 (SLFN12). DNMDP shows clear cell-selective cytotoxicity .
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- HY-173072
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- HY-17605A
-
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GS-9883 sodium
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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-N1039A
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Others
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Cancer
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Manool is a diterpene from Salvia officinalis. Manool induces selective cytotoxicity in cancer cells. Manool arrests the cancer cells at the G(2)/M phase of the cell cycle .
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- HY-P991061
-
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CHS-114; SRF-114
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CCR
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Cancer
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Tagmokitug (CHS-114; SRF-114) is a fully human IgG1 antibody targeting CCR8. Tagmokitug selectively binds to human CCR8 (Kd = 502 pM) and mediates the death of CCR8-expressing cells via antibody-dependent cellular cytotoxicity and antibody-dependent cellular phagocytosis. Tagmokitug selectively eliminates intratumoral regulatory T cells, induces tumor growth inhibition, remodels the tumor immune microenvironment, and promotes the differentiation of cytotoxic CD8 + T cell subsets. Tagmokitug can be used for the research of solid tumors .
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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-118762
-
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Cathepsin
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Cancer
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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 .
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- HY-13562
-
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AQ4N
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NO Synthase
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Cancer
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Banoxantrone (AQ4N), as a prototype hypoxia selective cytotoxin, can be reduced to AQ4, a potent topoisomerase II inhibitor. Banoxantrone selectively kills hypoxic cells via an iNOS-dependent mechanism. Banoxantrone shows a potent cytotoxicity and hypoxia-selective effect enhanced by radiation .
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- HY-121088
-
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P-glycoprotein
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Cardiovascular Disease
Others
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Ceefourin 2 is a potent and highly selective inhibitor of MRP4. Ceefourin 2 inhibits the transport of MRP4 substrates but is not selective for other ABC transporters. Ceefourin 2 shows lower cytotoxicity and higher microsomal and acid stability .
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- HY-149290
-
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Prostaglandin Receptor
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Cancer
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AMX12006 is a potent, selective and orally active EP4 antagonist with an IC50 value of 4.3 nM. AMX12006 shows cytotoxic and antitumor activity .
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- HY-130013
-
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Fluorescent Dye
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Others
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HKYellow-AM (6/12-mixture) is a yellow fluorescent probe that can detect ONOO- in living cells and tissues with high selectivity and sensitivity without cytotoxicity .
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- HY-123554
-
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Apoptosis
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Cancer
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Flavagline FL3 is a flavagline with potent and selective cytotoxicity in cancer cells.Flavagline FL3 induces apoptosis of HL60 and Hela cells by triggering the translocation of Apoptosis Inducing Factor (AIF) and caspase-12 to the nucleus .
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- HY-122751
-
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Phosphodiesterase (PDE)
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Cancer
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(R)-DNMDP is a potent and selective cancer cell cytotoxic agent. (R)-DNMDP, the R-form of DNMDP, binds PDE3A directly. (R)-DNMDP has a 500-fold lower EC50 compared to the (S)-enantiomer in HeLa cell line .
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- HY-178946
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IRE1
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Cancer
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IA107 is a potent, selective, and allosteric IRE1α RNase (IC50 = 16 nM (non phosphorylated), IC50 = 9 nM (phosphorylated)) inhibitor. IA107 can inhibit endoplasmic reticulum stress-induced XBP1 mRNA splicing and protein expression, and has no cytotoxicity .
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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-75577
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Drug Intermediate
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Cancer
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4-Amino-3-methoxybenzoic acid is a drug intermediate that can be used to construct benzothiazole compounds with anti-breast cancer activity .
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- HY-101374
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-
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- HY-135275
-
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Bcl-2 Family
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Cancer
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BCL-XL-IN-4 (compound 10) is a potent and selective BCL-XL inhibitor with Ki values of 0.042, 170 nM for BCL-XL, BCL-2, respectively. BCL-XL-IN-4 shows cytotoxicity .
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- HY-146819
-
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Carbonic Anhydrase
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Cancer
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Compound 9 is the most effective against tumor specific Ca ix/ca XII (ki=29.1 and 8.8 nm), so it is possible to evaluate its cytotoxicity and selectivity to HepG-2, HCT-116 and MCF-7 cancer cell lines in vitro, and its IC50 values to tumor cells are 1.78, 1.94 and 3.07, respectively μ M. It showed that it had obvious cytotoxicity.
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- HY-17605AR
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GS-9883 sodium (Standard)
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Reference Standards
HIV Integrase
HIV
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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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- HY-105314
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Others
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Cancer
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LY-33169 is an antitumor agent. LY-33169 had selective cytotoxicity against Colon Adenocarcinoma-38, Human Colon-116, Human Prostate LNCaP, and Human Breast WSU-Br-1 cells .
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- HY-146548
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Apoptosis
Bcl-2 Family
Caspase
PARP
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Cancer
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Anticancer Agent 43 is a potent anticancer agent. Anticancer Agent 43 induces apoptosis by caspase 3, PARP1, and Bax dependent mechanisms. Anticancer Agent 43 induces DNA damage .
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- HY-16984
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Itk
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Inflammation/Immunology
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GNE-4997 is a potent and selective interleukin-2-inducible T-cell kinase (ITK) inhibitor with a Ki of 0.09 nM, and the correlation between the basicity of solubilizing elements in GNE-4997 and off-target antiproliferative effects reduces cytotoxicity .
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- HY-147971
-
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Parasite
Topoisomerase
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Infection
Cancer
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Anticancer agent 75 is a potent anticancer agent. Anticancer agent 75 shows cytotoxicity and selectivity in cancer cell lines. Anticancer agent 75 shows cytotoxicity to normal human kidney cell lines is at least 35 times lower than that of the Doxorubicin standard. Anticancer agent 75 shows good activity of antiplasmodial .
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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-178940
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Apoptosis
Checkpoint Kinase (Chk)
CDK
DNA/RNA Synthesis
Bcl-2 Family
Caspase
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Cancer
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Apoptosis inducer 49 is a selective apoptosis inducer with high specificity against CCRF-CEM leukemia cells (IC50 = 2.68 μM). Apoptosis inducer 49 enhances RNA synthesis and replication stress, activates the Chk1-p21 axis, leading to S-phase arrest. Apoptosis inducer 49 can inhibit Bcl-2 and activate caspase-3. Apoptosis inducer 49 can be used for the study of Leukemia .
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- HY-P1103A
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CXCR
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Cancer
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CTCE-9908 TFA is a potent and selective CXCR4 antagonist. CTCE-9908 TFA induces mitotic catastrophe, cytotoxicity and inhibits migration in CXCR4-expressing ovarian cancer cells .
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- HY-111402
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Erizomycin; NSC 246134
|
Bacterial
Antibiotic
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Infection
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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 .
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- HY-101280
-
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NAMPT
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Cancer
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LB-60-OF61 is a NAMPT inhibitor and is a cytotoxic compound with a selectivity towards MYC overexpressing cell lines .
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- HY-101280A
-
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NAMPT
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Cancer
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LB-60-OF61 hydrochloride is a potent NAMPT (nicotinamide phosphoribosyltransferase) inhibitor. LB-60-OF61 hydrochloride is a cytotoxic compound with a selectivity towards MYC overexpressing cell lines .
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- HY-115905
-
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Parasite
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Infection
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Antimalarial agent 9 (Compound 11) is a potent antimalarial agent. Antimalarial agent 9 is a quinoline-imidazole derivative compound. Antimalarial agent 9 exhibits significant antimalarial efficacy in-vitro against both CQ-sensitive (IC50-0.14 μM) and MDR strain (IC50-0.41 μM) with minimal cytotoxicity and high selectivity .
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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-117412
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Drug Derivative
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Cancer
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KCG 1 is a potent and selective anti-tumor agent that displays anti-prollferative and cytotoxic effects on epithelial tumoral cells .
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- HY-142908
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Endogenous Metabolite
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Cancer
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Maximiscin, a fungal metabolite, induces DNA damage and shows selective cytotoxic activity against a subtype of triple-negative breast cancer.
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- HY-N9737
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Others
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Neurological Disease
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(−)-Acutumine is a tetracyclic chloroalkaloid that exhibits selective cytotoxicity to cultured human T cells and memory-enhancing properties in the Wistar rat model .
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- HY-122014
-
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Topoisomerase
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Others
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39625 is a camptothecin ketone analogue, a stable, potent and selective topoisomerase I inhibitor, active against purified topoisomerase I and cytotoxic to cancer cells.
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- HY-147968
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Others
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Cancer
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Anticancer agent 74 is a moderate anticancer agent. Anticancer agent 74 has lower selectivity and cytotoxicity than doxorubicin to normal cell .
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- HY-161171
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Parasite
Ephrin Receptor
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Cancer
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Antimalarial agent 37 (compound 33) is a selective inhibitor against Type Ⅱ kinase with antiplasmodial activity. Antimalarial agent 37 exhibited cytotoxicity and selectivity towards cancer cells HepG2 and MCF 7 .
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- HY-142694
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E1/E2/E3 Enzyme
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Cardiovascular Disease
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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 .
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- HY-142691
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-
- HY-142692
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- HY-N3065
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Others
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Cancer
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Pierreione B is a pyranoisoflavone, that can be isolated from the leaves and twigs of Antheroporum pierrei. Pierreione B demonstrates solid tumor selectivity with minimal cytotoxicity .
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- HY-155278
-
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Others
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Cancer
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Anticancer agent 162 (compound 1d) is an effective anticancer agent. Anticancer agent 162 induces oncosis of Hela cells with lipophilicity and cytotoxicity selectivity .
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- HY-154842
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- HY-146029
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Apoptosis
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Cancer
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Apoptosis inducer 3 (Compound 3) is an apoptosis inducer that selectively triggers apoptosis and late-apoptosis. Apoptosis inducer 3 shows cytotoxicity against cancer cells .
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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-146154
-
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EGFR
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Cancer
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EGFR-IN-58 (Compound 4a) is a potent, ATP-competitive, and selective EGFR inhibitor. EGFR-IN-58 shows potent cytotoxicity against melanoma, colon, and blood cancers .
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- HY-162515
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Mitochondrial Metabolism
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Cancer
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8-OAc is a potent and selective mitochondrial electron transport chain (ETC) complex I inhibitor. 8-OAc exhibits cytotoxicity against cancer cell lines .
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- HY-129301
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BCRP
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Cancer
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CCTA-1523 is a potent, selective, reversible and orally active ABCG2 inhibitor. CCTA-1523 shows cytotoxicity. CCTA-1523 shows anticancer activity .
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- HY-N3113
-
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Others
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Cancer
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Panaxyne is a polyacetylene, that can be isolated from the roots of cultivated-wild ginseng. Panaxyne shows significant and selective cytotoxicity against SK-OV-3, with an ED50 of 1.40 µM .
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- HY-161983
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Influenza Virus
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Infection
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Neuraminidase-IN-22 (compound 3e) is a potent, selective and orally active neuraminidase inhibitor with an IC50 value of 0.03 µM. Neuraminidase shows cytotoxicity and anti-influenza A virus activity .
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- HY-163755
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- HY-N10491
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P-glycoprotein
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Cancer
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Spongionellol A is a MDR1 (p-glycoprotein) inhibitor. Spongionellol A has high cytotoxic activity and selectivity in prostate cancer cells by inducing caspase‑dependent apoptosis. Spongionellol A can be used in the research of cancers, such as prostate cancer .
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- HY-163195
-
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Microtubule/Tubulin
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Cancer
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Tubulin inhibitor 40 (compound 45) is a tubulin inhibitor with IC50 of 1.2 μM. Tubulin inhibitor 40 shows selective cytotoxicity towards cancer cells. Tubulin inhibitor 40 processes antitumor activity .
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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-118722
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DNA/RNA Synthesis
Cytochrome P450
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Cancer
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RB-90740 is a type of biological reducing agent. RB-90740 is activated through metabolic reduction and generates cytotoxic products, thereby selectively killing tumor cells (usually in a hypoxic environment). RB-90740 has selective toxicity towards hypoxic cells, which is mainly achieved by causing DNA strand breaks and activating reducing enzymes (such as Cytochrome P450). RB-90740 does not initially exhibit cytotoxicity similar to its in vitro properties in hypoxic cells in mouse models. RB-90740 can be used to study the tumor physiological environment
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- HY-161453
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Cholinesterase (ChE)
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Neurological Disease
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ChE-IN-32 (compound 5d) is a potent and selective hBChE inhibitor with an IC50 value of 0.109 µM. BChE-IN-32 shows cytotoxicity. BChE-IN-32 has the potential for the research of Alzheimer's disease .
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- HY-A0162R
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Antibiotic
Reference Standards
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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- HY-19481
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HCV
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Infection
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HCV-371 is a highly selective, potent, and low cytotoxicity HCV NSSB (EC50 = 4.8-6.1 μM) polymerase allosteric inhibitor. HCV-371 can be used for research on hepatitis C virus infection .
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- HY-169246
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CDK
Apoptosis
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Cancer
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CDK2-IN-32 (Compound 5g) is a selective CDK2 inhibitor with an IC50 of 0.21 μM. CDK2-IN-32 shows cytotoxicity against Vero cells with an IC50 of 28.52 μM .
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- HY-146782
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EGFR
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Cancer
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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 .
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- HY-173446
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PARP
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Cancer
|
|
PARP1-IN-38 (compound ent-6_P) is a potent PARP1 inhibitor with an IC50 of 10 μM. PARP1-IN-38 shows selective cytotoxic activity in BRCA mutant cancer cells
|
-
- HY-149347
-
|
|
Bacterial
|
Infection
|
|
Mtb-IN-3 (compound 10c) is an inhibitor of Mycobacterium tuberculosis (Mtb). Mtb-IN-3 shows selective, potent in vitro antimycobacterial activity without cytotoxicity. Mtb-IN-3 inhibits colony-forming in spleen in the murine tuberculosis model .
|
-
- HY-N11919
-
|
|
Others
|
Cancer
|
|
Anticancer agent 149 (compound 3) is an anticancer agent isolated from the rhizome of Dioscorea dioscorea (DM). Anticancer agent 149 exhibits selective cytotoxic activity against MCF-7 cells (IC50=31.41 μM) .
|
-
- HY-146438
-
|
|
PPAR
|
Cancer
|
|
PPARγ agonist 3 (Compound 18a) is a potent and selective agonist of PPARγ. PPARγ agonist 3 is not cytotoxic neither on non-resistant nor on resistant cells. PPARγ agonist 3 exerts antitumor potency only in combination with Imatinib .
|
-
- HY-146428
-
|
|
Bacterial
|
Infection
|
|
Anti-MRSA agent 4 (compound 7a) is a potent and selective growth inhibitor of Gram-positive Methicillin-resistant Staphylococcus aureus (MRSA), with MIC ≤ 0.26 µM. Anti-MRSA agent 4 exhibits no cytotoxic and no hemolytic activity in HEK293 cells .
|
-
- HY-151295
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
Antitumor agent-75 is a novel potent antitumor agent. Antitumor agent-75 has cytotoxic effects on cancer and normal human cell lines. Antitumor agent-75 shows a highly selective cytotoxic effect against human lung adenocarcinoma (cell line A549) when combined with Antitumor agent-74 (HY-151292), the IC50 value of 2.8 μM. Antitumor agent-75 can be used for the research of cancer .
|
-
- HY-146439
-
|
|
PPAR
|
Cancer
|
|
PPARγ agonist 4 (Compound 18b) is a potent and selective agonist of PPARγ. PPARγ agonist 4 is not cytotoxic neither on non-resistant nor on resistant cells. PPARγ agonist 4 exerts antitumor potency only in combination with Imatinib .
|
-
- HY-101280R
-
|
|
NAMPT
Reference Standards
|
Cancer
|
|
LB-60-OF61 (Standard) is the analytical standard of LB-60-OF61 (HY-101280). This product is intended for research and analytical applications. LB-60-OF61 is a NAMPT inhibitor and is a cytotoxic compound with a selectivity towards MYC overexpressing cell lines .
|
-
- HY-179506
-
|
|
MDM-2/p53
Apoptosis
|
Cancer
|
|
P53 Activator 16 (Compound JC16) is a p53 activator. P53 Activator 16 exhibits selective cytotoxicity and pro-apoptotic (apoptosis) activity towards p53-Y220C mutant cancer cells, while having little effect on wild-type or P53-deficient cells. P53 Activator 16 induces the conformational transition of cell p53-Y220C from the mutant form to the wild-type form, accompanied by the transcriptional activation of p53 target genes, without increasing the overall level of p53 protein. P53 Activator 16 can be used for the study of p53 mutant cancers .
|
-
- HY-W551344
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
dCTPase-IN-1 is a highly selective deoxycytidine triphosphate pyrophosphatase 1 (dCTPase) inhibitor with an IC50 of 20 nM. dCTPase-IN-1 functionally inhibits dCTPase, exhibits a synergistic effect in enhancing cytotoxicity, and has no inherent cytotoxicity. dCTPase-IN-1 can be used for the research of leukemia .
|
-
- HY-181493
-
|
|
VEGFR
Reactive Oxygen Species (ROS)
Apoptosis
|
Cancer
|
|
VEGFR-2-IN-81 is a thiazole-based isoquinolin-1(2H)-one derivative and an VEGFR-2 inhibitor with IC50 of 1.94 μM. VEGFR-2-IN-81 exhibits significant selective cytotoxicity against colorectal cancer cells (IC50 = 7.75 μM). VEGFR-2-IN-81 exerts anti-colorectal cancer effects by inducing apoptosis, elevating intracellular ROS levels and reducing mitochondrial transmembrane potential. VEGFR-2-IN-81 can be used for the research of colorectal cancer, lung cancer, breast cancer, liver cancer .
|
-
- HY-165043
-
|
DG(20:4/0:0/20:4); 1,3-Diarachidonin
|
Biochemical Assay Reagents
|
Others
|
|
1,3-Diarachidonoyl glycerol (DG(20:4/0:0/20:4)) is a compound that is being studied for its selective cell killing mechanism, and it has a selective killing effect on cells transformed by the E1A gene of adenovirus type 12. Its killing effect is attributed to lipid peroxidation, and its structural characteristics are crucial to the specificity of this cytotoxicity, which ultimately exerts cytotoxic effects by destroying the cell membrane.
|
-
- HY-123724
-
|
|
Others
|
Others
|
|
Ravidomycin is a compound with antibacterial and cytotoxic activities. New analogs have been isolated from microorganisms. These analogs differ in antibacterial selectivity compared with known compounds.
|
-
- HY-180357
-
|
|
Checkpoint Kinase (Chk)
Reactive Oxygen Species (ROS)
DNA/RNA Synthesis
|
Cancer
|
|
Graviquinone is a Chk1 inhibitor. Graviquinone exhibits potent cytotoxicity against various cancer cell lines. Graviquinone possesses the characteristics of bypassing ABCB1-mediated multidrug resistance, selectively damaging cancer cell DNA, and regulating the DNA damage response. Graviquinone can also enhance cytotoxicity by increasing ROS levels in cancer cells. Graviquinone can be used for cancer research .
|
-
- HY-W041672
-
|
|
PARP
|
Cancer
|
|
PD128763 is a selective poly(ADP-ribose) polymerase inhibitor. PD128763 results in an enhancement of Streptozotocin (HY-13753)-induced cytotoxicity. PD128763 can be used in leukemia research .
|
-
- HY-183281
-
|
|
TRP Channel
|
Others
|
|
TRPV3 antagonist-1 is a selective TRPV3 channel antagonist with an IC50 of 11.97 μM. TRPV3 antagonist-1 shows selectivity over hTRPV1, hTRPV4, hTRPA1, and hTRPM8. TRPV3 antagonist-1 shows low cytotoxicity .
|
-
- HY-N16734
-
|
|
Others
|
Cancer
|
|
Norviburtinal is a non-selective cytotoxic and pro-angiogenic agent. Norviburtinal has an IC50 of 3.25 μg/mL on G361 melanoma cells and an effective concentration of 50 μg/mL on zebrafish embryos. Norviburtinal promotes capillary sprout formation in zebrafish subintestinal vessels (SIV) and has both cytotoxic and pro-angiogenic activities. Norviburtinal can be used in research on promoting angiogenesis related to melanoma, lung cancer, and wound healing .
|
-
- HY-182785
-
|
|
Photosensitizer
|
Cancer
|
|
Photosensitizer-10 is a glutathione (GSH)-activatable photosensitizer. Photosensitizer-10 shows minimal photoactivity in the absence of glutathione, and generates a highly active species upon reaction with glutathione to induce photo-cytotoxicity. Photosensitizer-10 exhibits selective photo-cytotoxicity toward cancer cells with elevated intracellular glutathione levels while sparing normal cells. Photosensitizer-10 can be used for the research of cancer, such as lung carcinoma and skin carcinoma .
|
-
- HY-182029
-
|
|
G-quadruplex
|
Cancer
|
|
G-quadruplex ligand 5 is a G-quadruplex (G4) ligand. G-quadruplex ligand 5 selectively stabilizes cancer-associated G4 oligonucleotides and shows cytotoxicity toward cancer cells. G-quadruplex ligand 5 can be used for the research of cancer .
|
-
- HY-173350
-
|
|
Arf Family GTPase
Apoptosis
|
Cancer
|
|
Ran-IN-1 is a specific inhibitor of Ran GTPase. Ran-IN-1 selectively induces cytotoxicity and apoptosis in aneuploid ovarian cancer cells and also inhibits DNA repair. Ran-IN-1 exhibits antitumor activity and is useful for research on tumors such as epithelial ovarian cancer .
|
-
- HY-159582
-
|
|
CXCR
|
Cardiovascular Disease
|
|
ACKR3 agonist 1 (compound 27) is a selective ACKR3 agonist (EC50=69 nM, Emax=82%) that inhibits platelet aggregation. ACKR3 agonist 1 is metabolically stable and non-cytotoxic, and has the potential to inhibit platelet-mediated thrombosis .
|
-
- HY-N6642
-
|
|
PPAR
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Ankaflavin, isolated from Monascus-Fermented red rice, is an orally active PPARγ agonist. Ankaflavin exhibits selective cytotoxic effect and induces cell death through apoptosis on cancer cells. Ankaflavin has anti-inflammatory, anti-cancer, antiatherosclerotic, and hypolipidemic effects .
|
-
- HY-U00279
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
Nitracrine inhibits RNA synthesis and covalently, reversibly binds to DNA but also forms covalent adducts with DNA in vivo. Nitracrine, a 1-nitroacridine derivative, is a potent hypoxia-selective agent in vitro and antitumor agent. Nitracrine has cytotoxicity towards most cells .
|
-
- HY-U00279A
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
Nitracrine dihydrochloride hydrate inhibits RNA synthesis and covalently, reversibly binds to DNA but also forms covalent adducts with DNA in vivo. Nitracrine dihydrochloride hydrate, a 1-nitroacridine derivative, is a potent hypoxia-selective agent in vitro and antitumor agent. Nitracrine dihydrochloride hydrate has cytotoxicity towards most cells .
|
-
- 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-149939
-
|
|
Parasite
|
Infection
|
|
Antimalarial agent 26 is an orally active 1,4-naphthoquinones derivative with antimalarial activities. Antimalarial agent 26 shows cytotoxicity against P. falciparum and selectivity over mammalian cell lines. Antimalarial agent 26 inhibits P. burghei induced parasitemia in vivo .
|
-
- 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-129905A
-
|
LLOMe hydrobromide; Leu-Leu methyl ester hydrobromide; H-Leu-Leu-OMe hydrobromide
|
Endogenous Metabolite
|
Inflammation/Immunology
|
|
L-Leucyl-L-Leucine methyl ester (LLOMe) hydrobromide, a dipeptide condensation product of L-leucine methyl ester generated by human monocytes or polymorphonuclear leukocytes, selectively eliminates lymphocytes with cytotoxic potential. L-Leucyl-L-Leucine methyl ester hydrobromide also can induce endolysosomal pathway stress .
|
-
- HY-177729
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
PROTAC BRD9 Degrader-9 (Compound 16) is an efficient and selective targeting BRD9 PROTAC degrader. PROTAC BRD9 Degrader-9 does not cause significant cytotoxicity. PROTAC BRD9 Degrader-9 can be used for cancer research
|
-
- HY-P10860
-
|
|
Factor Xa
|
Cardiovascular Disease
|
|
cMCoFx1 is a potent and selective FXIIa cyclic peptide inhibitor. cMCoFx1 has high binding affinity (KD: 900 pM) and inhibitory activity (Ki: 370 pM) for FXIIa. cMCoFx1 can effectively inhibit endogenous clotting pathways, and cMCoFx1 is stable in serum and non-cytotoxic .
|
-
- 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-157168
-
|
|
Trk Receptor
|
Neurological Disease
|
|
TrkA-IN-6 (compound R48) is a hydrazone-like, selective inhibitor of tropomyosin kinase type A receptor kinase (TrkA). TrkA-IN-6 exhibited a higher cytotoxic effect on U87 GBM cells than Temozolomide (HY-17364), with an IC50 of 68.99 μM .
|
-
- HY-146043
-
|
|
Parasite
|
Infection
|
|
Antiparasitic agent-5 (compound 8h) has selectively antiparasitic activity against Leishmania infantum (L. infantum) with an IC50 value of 2.50 μM. Antiparasitic agent-5 also has certain cytotoxicity against HepG2 (CC50 = 6.78 μM) .
|
-
- 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-D2988
-
|
|
Fluorescent Dye
Bacterial
|
Infection
|
|
BIN-3 is a novel near-infrared fluorescent probe. BIN-3 has excellent biocompatibility, no cytotoxicity, and no hemolysis. BIN-3 can be used for highly sensitive and selective imaging of drug-resistant bacterial infections expressing β-lactam enzymes in live mice .
|
-
- HY-182649
-
|
|
HDAC
Apoptosis
Microtubule/Tubulin
|
Cancer
|
|
NN-429 is a selective HDAC6 inhibitor. NN-429 induces apoptosis, increases the acetylation level of α-tubulin, and exhibits cytotoxicity against cancer cells. NN-429 is applicable to research related to acute myeloid leukemia, multiple myeloma and lymphoma .
|
-
- HY-146044
-
|
|
Parasite
|
Infection
|
|
Antiparasitic agent-6 (compound 5b) has selectively antiparasitic activity against Leishmania infantum (L. infantum) with an IC50 value of 3.89 μM. Antiparasitic agent-6 also has certain cytotoxicity against HepG2 (CC50 = 13.64 μM) .
|
-
- HY-146045
-
|
|
Parasite
|
Infection
|
|
Antiparasitic agent-7 (compound 5d) has selectively antiparasitic activity against Leishmania infantum (L. infantum) with an IC50 value of 2.85 μM. Antiparasitic agent-7 also has certain cytotoxicity against HepG2 (CC50 = 10.61 μM) .
|
-
- HY-164546
-
|
|
STAT
Apoptosis
|
Cancer
|
WB436B is a highly selective STAT3 inhibitor. WB436B can selectively inhibit STAT3-Tyr705 phosphorylation and the expression of STAT3 target genes, showing cytotoxic effects on pancreatic cancer cells and inducing apoptosis. WB436B can suppress tumor growth and metastasis in pancreatic cancer mouse models, extending the survival of tumor-bearing mice .
|
-
- HY-128063
-
|
|
CXCR
|
Inflammation/Immunology
|
|
CXCR3 antagonist 1 (compound 6c) is a selective and non-cytotoxic CXCR3 antagonist (IC50=0.06 µM). CXCR3 antagonist 1 has potential in researching inflammatory diseases (including inflammatory bowel disease, multiple sclerosis, rheumatoid arthritis, and diabetes) .
|
-
- 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-N10492
-
|
|
P-glycoprotein
|
Cancer
|
|
Spongionellol A analog 1, an analog of Spongionellol A (HY-10491), is a MDR1 (p-glycoprotein) inhibitor. Spongionellol A analog 1 has high cytotoxic activity and selectivity in prostate cancer cells by inducing caspase?dependent apoptosis. Spongionellol A analog 1 can be used in the research of cancers, such as prostate cancer .
|
-
- HY-147788
-
|
|
Dihydroorotate Dehydrogenase
|
Cancer
|
|
hDHODH-IN-9 (Compound 3k) is a potent inhibitor of hDHODH with an IC50 of 0.34 μM. hDHODH-IN-9 demonstrates high cytotoxic activity against MCF-7 and A375 cells and good selectivity. hDHODH-IN-9 has the potential for the research of cancer diseases .
|
-
- HY-181558
-
|
|
Others
|
Cancer
|
|
Anticancer agent 303 is a selective, orally active anticancer agent belonging to the pyrazolopyridine derivatives. Anticancer agent 303 exhibits low cytotoxicity to healthy cells, with a selective window of approximately 2-fold between cancer cells and healthy cells. Anticancer agent 303 produces detectable systemic exposure in mice following intraperitoneal or oral administration. Anticancer agent 303 effectively inhibits the proliferation of prostate cancer and breast cancer cells .
|
-
- HY-U00279B
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
Nitracrine hydrochloride is a platinum-based antineoplastic drug with selective toxicity to hypoxic cells. Nitracrine hydrochloride exhibits significant cytotoxicity against the Chinese hamster ovary cell line AA8 under hypoxic conditions. Nitracrine hydrochloride exerts its effect by binding to the insertion of DNA and forming covalent adducts. The cytotoxicity of Nitracrine hydrochloride under hypoxic conditions is related to its reductive metabolism to form alkylated substances. At the same time, it may enhance the reactivity to DNA through the insertion of DNA, thereby improving the efficacy. Nitracrine hydrochloride can also inhibit RNA synthesis, contributing to its anti-tumor effect .
|
-
- 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-101096
-
|
MK-8998; CX-8998; JZP385
|
Calcium Channel
|
Neurological Disease
Cancer
|
|
Suvecaltamide (MK-8998) is a selective T-type calcium channel inhibitor with oral efficacy. Suvecaltamide exhibits no cytotoxicity in myeloma cell lines and does not affect the antitumor efficacy of Bortezomib (BTZ). Suvecaltamide reverses BTZ-induced peripheral neuropathy (CIPN) in mouse and rat models, and helps inhibit myeloma growth .
|
-
- HY-157159
-
|
|
Btk
|
Cancer
|
|
BTK-IN-28 (compound PID-4) is a potent BTK inhibitor with anticancer activity. BTK-IN-28 has inhibitory effects on BTK and downstream signaling cascades and selectively inhibits Burkitt lymphoma RAMOS proliferation. BTK-IN-28 has no significant cytotoxicity towards non-tumor cells .
|
-
- HY-105846
-
|
|
DNA/RNA Synthesis
Bacterial
Antibiotic
|
Cancer
|
|
Nogalamycin is an anthracyclinone antibiotic. Nogalamycin is a potent antibiotic against Gram-positive bacteria, also has cytotoxicity against certain tumor cells. Nogalamycin is produced by Streptomyces nogalater var. Nogalater. Nogalamycin selectively inhibits RNA synthesis after binding to DNA template. Nogalamycin can be used for researching anticancer .
|
-
- HY-N10132
-
|
|
nAChR
|
Infection
Neurological Disease
|
|
Microgrewiapine A is an antagonist of nAChR. Microgrewiapine A inhibits hα4β2 and hα3β4 activity with 60% and 70% inhibition, respectively. Microgrewiapine A has selective cytotoxic against HT-29 human colon cancer cells with an IC50 of 6.8 μM .
|
-
- HY-P991942
-
|
BAY3375968; TPP-23411
|
CCR
|
Inflammation/Immunology
Cancer
|
|
Lanerkitug (BAY3375968) is a fully human monoclonal IgG1 anti-human CCR8 antibody. Lanerkitug selectively depletes human CCR8 + Tregs via antibody dependent cellular cytotoxicity (ADCC) and antibody dependent cellular phagocytosis (ADCP). Lanerkitug can be used in the research of solid tumors .
|
-
- HY-179560
-
|
|
Polo-like Kinase (PLK)
MDM-2/p53
|
Cancer
|
|
PMV6-PEG4-BI2536 is a p53-Y220C-PLK1 dual-functional compound, composed of a high-affinity p53-Y220C mutant binder (Kd ≈ 2.5 nM) and a potent PLK1 kinase inhibitor (IC50 = 0.83 nM). PMV6-PEG4-BI2536 triggers TP53 Y220C cell G2/M arrest and apoptosis through PLK1 mislocalization and kinase inhibition, independent of p53 transcriptional reactivation. PMV6-PEG4-BI2536 can be used for the study of TP53 mutant cancers .
|
-
- HY-146738
-
|
|
Akt
|
Cancer
|
|
GSD-11 is a potent and selective anti-austerity agent. GSD-11 inhibits the cell migration and colony formation of PANC-1 cells. GSD-11 inhibits the Akt/mTOR signaling pathway. GSD-11 has the potential for the research of pancreatic cancer[1].
|
-
- 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-175427
-
|
|
Bacterial
Antibiotic
|
Infection
|
|
Amycolatopsin C is a glycosylated macrolactone with antibacterial activity. Amycolatopsin C selectively inhibits the growth of Mycobacterium bovis (BCG) and Mycobacterium tuberculosis (H37Rv) compared to other Gram-positive and Gram-negative bacteria. Amycolatopsin C demonstrates low levels of cytotoxicity toward mammalian cells and can be utilized in antibacterial research .
|
-
- 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-P10772
-
|
|
Peptide-Drug Conjugates (PDCs)
EBV
|
Cancer
|
|
L2P4 is a peptide-based and EBNA1 targeting fluorescent probe, which inhibits the EBNA1 homodimer formation and selectively inhibits EBV+ tumor growth. L2P4 exhibits cytotoxicity in EBV-positive C666-1 cell with LC50 of 46.4 μM .
|
-
- HY-161156
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
Cancer
|
|
BChE-IN-26 (Compound 7b) is a selective AChE and BChE inhibitor with Ki value of 35 μM and 1.6 μM. BChE-IN-26 has cytotoxicity to human neuroblastoma (SH-SY5Y) cell line. BChE-IN-26 can be used for the research of Alzheimer’s disease .
|
-
- HY-135909
-
TH1217
1 Publications Verification
ZINC1775962367
|
SARS-CoV
|
Infection
Cancer
|
|
TH1217 (ZINC1775962367) is a potent and selective dCTPase pyrophosphatase 1 (dCTPase) inhibitor, with an IC50 of 47 nM. TH1217 enhances the cytotoxic effect of cytidine analogues in leukemia cells. TH1217 also could modulate SARS-Cov-2 interactors, so it shows activity of against COVID-19 .
|
-
- HY-W001187
-
|
|
Mitochondrial Metabolism
DNA/RNA Synthesis
Reactive Oxygen Species (ROS)
|
Cancer
|
|
Tempo is a nitric oxide radical and a selective scavenger of ROS in mitochondria. Tempo is also an organocatalyst that disproportionates superoxide and oxidizes primary alcohols to aldehydes in a catalytic cycle. Tempo has mutagenic and antioxidant effects and can induceDNA strand breaks. Tempo also exerts cytotoxic and mutagenic properties in mouse lymphoma cells .
|
-
- HY-N0069
-
|
Solamargin; δ-Solanigrine
|
P-glycoprotein
Apoptosis
|
Cancer
|
|
Solamargine, a derivative from the steroidal solasodine in Solanum species, exhibits anticancer activities in numerous types of cancer. Solamargine induces non-selective cytotoxicity and P-glycoprotein inhibition. Solamargine significantly inhibits migration and invasion of HepG2 cells by down-regulating MMP-2 and MMP-9 expression and activity .
|
-
- HY-105916
-
|
|
mGluR
|
Cancer
|
|
NSC 303861 is an L-glutamine receptor antagonist. NSC 303861 selectively inhibits glutamine dependent enzymes in purine nucleotide synthesis without affecting pyrimidine synthase. NSC 303861 has significant cytotoxicity against liver cancer 3924A cells (LC50 = 6 µM). NSC 303861 can be used for cancer research .
|
-
- HY-108447
-
|
|
Ser/Thr Protease
SARS-CoV
PAI-1
|
Infection
Cancer
|
|
BC-11 hydrobromide is a selective TMPRSS2 inhibitor (TMPRSS2 is a key host cellular factor for viral entry and SARS-CoV-2 pathogenesis), and a selective urokinase (uPA) inhibitor (IC50=8.2 μM). BC-11 hydrobromide is cytotoxic to triple-negative MDA-MB231 breast cancer cells. BC-11 hydrobromide is used in research on viral infections and cancer .
|
-
- HY-124675
-
MYCMI-6
1 Publications Verification
NSC354961
|
c-Myc
Apoptosis
|
Cancer
|
|
MYCMI-6 (NSC354961) is a potent and selective endogenous MYC:MAX protein interactions inhibitor. MYCMI-6 blocks MYC-driven transcription and binds selectively to the MYC bHLHZip domain with a Kd of 1.6 μM. MYCMI-6 inhibits tumor cell growth in a MYC-dependent manner (IC50<0.5 μM). MYCMI-6 is not cytotoxic to normal human cells. MYCMI-6 induces apoptosis .
|
-
- HY-P992450
-
|
|
TNF Receptor
|
Cancer
|
|
REGN6569 is a fully human IgG1 monoclonal antibody targeting glucocorticoid-induced tumor necrosis factor receptor-related protein (GITR) with high specificity for GITR. REGN6569 exerts stronger in vitro antibody-dependent cell-mediated cytotoxicity (ADCC) against regulatory T cells expressing GITR. REGN6569 selectively depletes regulatory T cells via antibody-dependent cell-mediated cytotoxicity and increases the proportion of proliferative natural killer (NK) cells in peripheral blood. REGN6569 is applicable for advanced solid malignancies. Isotype control: HY-P99001 .
|
-
- HY-P10772A
-
|
|
Peptide-Drug Conjugates (PDCs)
EBV
|
Cancer
|
|
L2P4 TFA is a peptide-based and EBNA1 targeting fluorescent probe, which inhibits the EBNA1 homodimer formation and selectively inhibits EBV+ tumor growth. L2P4 TFA exhibits cytotoxicity in EBV-positive C666-1 cell with LC50 of 46.4 μM .
|
-
- HY-175763
-
|
|
RGS Protein
|
Neurological Disease
Metabolic Disease
|
|
Z55660043 is a Regulator of G protein signaling-14 (RGS14) inhibitor with an IC50 of 2.3 μM. Z55660043 selectively and non-covalently inhibits RGS14 GTPase-accelerating protein (GAP) activity without measurable cytotoxicity. Z55660043 can be used for central nervous system and metabolic disorders research .
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-
- HY-184105
-
|
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Indoleamine 2,3-Dioxygenase (IDO)
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Cancer
|
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IDO1-IN-36 (Compound 5a) is a selective, mixed-type IDO1 inhibitor with an IC50 of 0.72 μM against hIDO1. IDO1-IN-36 exhibits extremely low cytotoxicity in cancer cells. IDO1-IN-36 can be used for the research of breast cancer .
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-
- HY-135900
-
|
|
ADC Payload
Bacterial
|
Cancer
|
|
Aniline-MPB-amino-C3-PBD is a cytotoxic agent comprised non-alkylating group. Aniline-MPB-amino-C3-PBD is a sequence-selective DNA minor-groove binding agent. Aniline-MPB-amino-C3-PBD acts as the payload for ADCs. Antimicrobial activity .
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-
- HY-16712
-
|
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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) .
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-
- HY-108263
-
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CGP52421
|
FLT3
|
Cancer
|
|
3-Hydroxy Midostaurin (CGP 52421), a metabolite of PKC412, effectively inhibits FMS-like tyrosine kinase-3 (FLT3) autophosphorylation with IC50s of approximately 132 nM and 9.8 μM in culture medium and plasma, respectively. 3-Hydroxy Midostaurin is less selective but more cytotoxic than PKC412 .
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-
- HY-N2332
-
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MLA
|
nAChR
|
Neurological Disease
|
|
Methyllycaconitine (MLA) is a potent, selective, CNS-penetrant, competitive α7nAChR antagonist. Methyllycaconitine alleviates amyloid-β peptides-induced cytotoxicity in SH-SY5Y cells. Methyllycaconitine prevents methamphetamine-induced effects in mouse striatum. Methyllycaconitine can be used for neurological disease research, such as Alzheimer’s disease .
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-
- HY-114563
-
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dFdG
|
Drug Derivative
|
Cancer
|
|
LY 223592 (Compound I-a) is a Gemcitabine (HY-17026) derivative. LY 223592 has the biological activity of highly selective inhibition of lung cancer cell proliferation (IC50 = 5.6 nM in A549 cells) and low cytotoxicity to normal cells. LY 223592 can be used for the research of cancer, such as non-small cell lung cancer (NSCLC) .
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- HY-156694
-
-
- HY-179621
-
|
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Cholinesterase (ChE)
Amyloid-β
|
Neurological Disease
|
|
EQ-04 is a highly selective positive allosteric modulator (PAM) of α7 nAChR. EQ-04 has no direct inhibitory activity on AChE and BChE. EQ-04 inhibits Aβ aggregation. EQ-04 has safe cytotoxicity and potent neuroprotective activity. EQ-04 can be used for the study of Alzheimer's disease.
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- HY-180819
-
|
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Cholinesterase (ChE)
|
Neurological Disease
|
|
AChE/BChE-IN-33 (Compound 3N) is a dual-target inhibitor of AChE and BChE, with IC50 values of 12.81 and 44.54 nM respectively. AChE/BChE-IN-33 exhibits selective cytotoxicity against SH-SY5Y cells. AChE/BChE-IN-33 can be used for the study of Alzheimer's disease and neuroblastoma .
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-
- HY-147040
-
|
|
c-Met/HGFR
Apoptosis
|
Cancer
|
|
ABN401 is an orally active and selective ATP-competitive c-MET inhibitor with an IC50 of 10 nM. ABN401 is cytotoxic to MET-addicted cancer cells with the IC50 of 2-43 nM. ABN401 has bioavailability in rats and dogs of 42.1-56.2% and 27.4-37.7%, respectively. ABN401 has antitumor activity .
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-
- HY-152118
-
|
|
Cytochrome P450
|
Cancer
|
|
CYP1B1-IN-4 is a 2,4-diarylthiazole compound with selectively CYP1B1 inhibition (IC50=0.2 nM). CYP1B1-IN-4 has little cytotoxicity and high stability in both human and rat liver microsomes .
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-
- HY-155035
-
|
|
17β-HSD
|
Cancer
|
|
S07-1066 is an aldo-keto reductase 1C3 (AKR1C3) inhibitor, synergizing doxorubicin (DOX) cytotoxicity. S07-1066 selectively blocks AKR1C3-mediated reduction of DOX, and reverses the DOX resistance in overexpressing AKR1C3 cells .
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-
- 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 .
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-
- HY-P2149
-
|
|
Mitosis
|
Infection
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Concanavalin A can be coupled to agarose to form Concanavalin A (agarose) (HY-P2149A). Concanavalin A (ConA) is a selective, competitive binding agent that targets specific carbohydrate structures containing glucose and mannose; it acts as a mitogen and exhibits varying degrees of cytotoxicity, hepatotoxicity, and teratogenicity. Concanavalin A is also utilized for in vivo blood glucose monitoring in the context of diabetes .
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-
- HY-146980
-
|
|
Apoptosis
GLUT
|
Cancer
|
|
GLUT4-IN-2 is a potent and selective GLUT4 inhibitor with IC50s of 11.4 µM and 6.8 µM for GLUT1 and GLUT4, respectively. GLUT4-IN-2 induces cell apoptosis and cell cycle arrest at G0/G1phase. GLUT4-IN-2 shows potent antitumor activity .
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-
- HY-120638
-
|
|
Topoisomerase
|
Cancer
|
|
BMS-250749 is a topoisomerase I (Top I) inhibitor of the fluoroglycosyl-3,9-difluoroindolecarbazole class. BMS-250749 exhibits potent cytotoxicity and selectivity, and shows curative antitumor activity against Lewis lung cancer. BMS-250749 exhibits broad-spectrum antitumor activity superior to CPT-11 in certain preclinical xenograft models. .
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-
- HY-159511
-
|
|
Hedgehog
|
Cancer
|
|
Hedgehog IN-7 (Compound 8g), a purine derivative, acts as an inhibitor of Hedgehog, capable of reducing the expression of Hedgehog genes and inhibiting Hedgehog signaling. Hedgehog IN-7 has significant cytotoxicity and selectivity towards the Hedgehog pathway-dependent pancreatic cancer cell Mia-PaCa-2 cells and can be used in the research of pancreatic cancer .
|
-
- 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 .
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-
- HY-135470R
-
|
P-7138 (Standard)
|
Reference Standards
Bacterial
|
Infection
|
|
Nifurpirinol (P-7138) (Standard) is the analytical standard of Nifurpirinol (HY-135470). This product is intended for research and analytical applications. Nifurpirinol (P-7138) is a selective prosubstrate of bacterial nitroreductase (NTR). NTR catalyzes the reduction of nifurpirinol to generate cytotoxic metabolites that induce apoptosis in target cells. Nifurpirinol selectively ablates NTR-expressing cells such as pancreatic β cells, osteoblasts, dopaminergic neurons, and podocytes in transgenic zebrafish models. Nifurpirinol can be used in regeneration studies and disease modeling such as focal segmental glomerulosclerosis (FSGS) .
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-
- HY-179019
-
|
|
HDAC
Microtubule/Tubulin
Apoptosis
Caspase
|
Neurological Disease
Cancer
|
|
HDAC-IN-94 is a potent, selective HDAC6 inhibitor (IC50 = 4.5 nM). HDAC-IN-94 shows >1000-fold selectivity over HDAC8 and shows minimal activity against other isoforms (HDAC1-3/10). HDAC-IN-94 induces α-tubulin hyperacetylation, apoptosis, and G2/M cell cycle arrest, exhibiting potent anti-tumor efficacy with low cytotoxicity. HDAC-IN-94 can be used for neuroblastoma and glioblastoma research .
|
-
- HY-133129
-
MS1943
4 Publications Verification
|
HyT
Histone Methyltransferase
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
MS1943 is an orally active selective HyT degrader of EZH2 that effectively reduces EZH2 levels in cells. MS1943 has anticancer activity and exhibits cytotoxic effects in a variety of TNBC cells while sparing normal cells. In addition, MS1943 maintains high potency (IC50=120 nM) in inhibiting EZH2 methyltransferase activity and is highly selective for EZH2. (Structure Note: RED, EZH2 ligand (HY-148458); Blue, Hyt (HY-W001578)) .
|
-
- HY-10015
-
|
5-(4-Phenoxybutoxy)psoralen
|
Potassium Channel
|
Inflammation/Immunology
|
|
PAP-1 (5-(4-Phenoxybutoxy)psoralen) is a potent, selective, and orally active Kv1.3 blocker (EC50=2 nM). PAP-1 blocks Kv1.3 in a use-dependent manner and acts by preferentially binding to the C-type inactivated state of the channel. PAP-1 exhibits 23-fold selectivity over Kv1.5 (EC50=45 nM), and further displays 33- to 125-fold selectivity over all other Kv1-family channels. PAP-1 does not exhibit cytotoxic or phototoxic effects .
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-
- HY-146083
-
|
|
Drug Derivative
|
Cancer
|
|
(Z)-p-cyano-α-Cyanostilbene (compound 11), a phenantrene derivative, has antiproliferative activity. (Z)-p-cyano-α-Cyanostilbene shows significant selectivity against HeLa (IC50=0.21 µM) and HepG2 (IC50=0.230 µM) cells without cytotoxic against normal skin fibroblasts (IC50>100 µM) .
|
-
- HY-182266
-
|
|
Mitochondrial Metabolism
Apoptosis
Reactive Oxygen Species (ROS)
DNA/RNA Synthesis
|
Cancer
|
|
FBP is a mitochondria-targeted, selective anticancer agent. FBP induces oxidative stress and mitochondrial dysfunction, leading to Apoptosis. FBP generates ROS and causes double-strand DNA breaks in cancer cells. FBP exhibits cytotoxic efficacy against cancer cells, with cervical cancer cells being the most sensitive. FBP can be used for the research of cervical cancer, lung cancer, melanoma and breast cancer .
|
-
- HY-161247
-
|
|
5-HT Receptor
|
Metabolic Disease
|
|
5HT2A antagonist 2 is an orally active, selective antagonist for 5HT2A with IC50 of 14 nM. 5-HT2A antagonist 2 exhibits good chemical, hepatocyte, and plasma stability, without significant cytotoxicity in cell lines VERO, HFL-1, L929, NIH3T3, CHO-K1 .
|
-
- HY-158378
-
|
R-AST-OH
|
Glutaminase
|
Cancer
|
|
Trivalent hydroxyarsinothricn (R-AST-OH) is a covalent and irreversible kidney-type glutaminase (KGA) inhibitor. Trivalent hydroxyarsinothricn binds to the glutamine binding site and forms a covalent bond with an active site cysteine residue. Trivalent hydroxyarsinothricn selectively kills triple-negative breast cancer (TNBC) cells and is not cytotoxic to the control cell line. KGA is the enzyme that controls glutamine metabolism and is correlated with tumor malignancy .
|
-
- HY-151361
-
|
|
AMPK
|
Cancer
|
|
AMPK-IN-3 (compound 67) is a potent and selective AMPK inhibitor with IC50s of 60.7, 107 and 3820 nM for AMPK (α2), AMPK (α1) and KDR, respectively. AMPK-IN-3 inhibits AMPK does not affect cell viability or cause significant cytotoxicity in K562 cells. AMPK-IN-3 can be used in study of cancer .
|
-
- HY-117512
-
|
|
Dopamine Transporter
Serotonin Transporter
|
Neurological Disease
|
|
UWA-101 hydrochloride is a selective and non-cytotoxic DAT/SERT inhibitor, with EC50 values of 3.6 µM and 2.3 µM for inhibiting DAT and SERT, respectively. UWA-101 hydrochloride can alleviate the side effects of dopaminergic agents (such as L-DOPA), such as motor disorders, and lacks psychotropic activity. UWA-101 hydrochloride can be used for research on neurodegenerative diseases such as Parkinson's disease .
|
-
- HY-15582
-
|
|
Microtubule/Tubulin
ADC Payload
|
Cancer
|
|
Auristatin E is a cytotoxic microtubule polymerization inhibitor with potent and selective antitumor activity. Auristatin E is a cytotoxin in antibody-drug conjugates (ADC). Auristatin E inhibits cell division by blocking the polymerisation of tubulin, promising for research in B-cell malignancies. Auristatin E, a synthetic analogue of the Dolastatin 10 (HY-15580), is linear peptides comprised of four amino acids .
|
-
- HY-103086
-
|
|
Raf
Autophagy
Apoptosis
|
Cancer
|
|
INU-152 is a potent and selective B-Raf inhibitor. INU-152 reduces tumor cell proliferation, enhances autophagy, and induces apoptosis by inhibiting B-Raf activity. INU-152 exhibits significant cytotoxicity against cancer cells transformed with v-Ha-ras (Ras-NIH 3T3). INU-152 can be utilized in cancer research .
|
-
- HY-173403
-
|
|
TrxR
Reactive Oxygen Species (ROS)
Apoptosis
|
Cancer
|
|
TrxR-IN-8 (Compound 6f) is a selective TrxR inhibitor (IC50: 10.2 μM). TrxR-IN-8 induces apoptosis through oxidative stress by stimulating the production of reactive oxygen species (ROS), reducing intracellular thiols, and lowering the glutathione/glutathione ratio. TrxR-IN-8 exhibits significant cytotoxicity against non-small cell lung cancer (NSCLC) cells .
|
-
- HY-175856
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
AChE-IN-95 (Compound 7) is a highly selective competitive acetylcholinesterase (AChE) inhibitor (IC50=17.87 μM, Ki=19.48 μM). AChE-IN-95 exhibits strong cytotoxicity against SH-SY5Y neuroblastoma cells. AChE-IN-95 is promising for research of Alzheimer’s disease and neurodegenerative disorders .
|
-
- HY-N2332A
-
|
MLA citrate
|
nAChR
|
Neurological Disease
|
|
Methyllycaconitine (MLA) citrate is a potent, selective, CNS-penetrant, competitive α7nAChR antagonist. Methyllycaconitine citrate alleviates amyloid-β peptides-induced cytotoxicity in SH-SY5Y cells. Methyllycaconitine citrate prevents methamphetamine-induced effects in mouse striatum. Methyllycaconitine citrate can be used for neurological disease research, such as Alzheimer’s disease .
|
-
- HY-P5891
-
|
|
PKC
|
Cardiovascular Disease
|
|
TAT-SAMβA is the peptide consist of RNAENFDRF (SAMβA; HY-P3429) conjugated to the cell penetrating TAT protein-derived peptide TAT47–57. TAT-SAMβA is a selective antagonist of Mfn1-βIIPKC association. TAT-SAMβA protects mouse embryonic fibroblast cells (MEFs) against oxidative stress-induced cytotoxicity .
|
-
- HY-116572
-
|
|
Reactive Oxygen Species (ROS)
JNK
Apoptosis
Caspase
|
Cancer
|
|
TASIN-1 hydrochloride is a selective inhibitor of truncated APC TR (adenomatous polyposis coli gene) that exerts cytotoxic effects by inhibiting cholesterol biosynthesis. TASIN-1 hydrochloride specifically targets colorectal cancer (CRC) cells carrying APC truncated mutations, while having no significant toxicity to wild-type APC cells. TASIN-1 hydrochloride exerts cytotoxic effects by targeting Emopamil binding protein (EBP) to inhibit cholesterol biosynthesis, triggering endoplasmic reticulum (ER) stress, reactive oxygen species (ROS) generation, and JNK-mediated apoptosis, and inhibiting Akt survival signaling. TASIN-1 hydrochloride can be used to prevent and intervene in APC mutant colorectal cancer .
|
-
- HY-116572A
-
|
|
Reactive Oxygen Species (ROS)
JNK
Apoptosis
Caspase
|
Cancer
|
|
TASIN-1 is a selective inhibitor of truncated APC TR (adenomatous polyposis coli gene) that exerts cytotoxic effects by inhibiting cholesterol biosynthesis. TASIN-1 specifically targets colorectal cancer (CRC) cells carrying APC truncated mutations, while having no significant toxicity to wild-type APC cells. TASIN-1 exerts cytotoxic effects by targeting Emopamil binding protein (EBP) to inhibit cholesterol biosynthesis, triggering endoplasmic reticulum (ER) stress, reactive oxygen species (ROS) generation, and JNK-mediated apoptosis, and inhibiting Akt survival signaling. TASIN-1 can be used to prevent and intervene in APC mutant colorectal cancer .
|
-
- HY-106031
-
|
|
Topoisomerase
DNA/RNA Synthesis
|
Cancer
|
|
F-14512 is an anticancer agent that utilizes the polyamine transport system (PTS) to selectively deliver polyamine-containing drugs to cancer cells. F-14512 enhances the affinity of polyamines for DNA, thereby inhibiting topoisomerase II and achieving selective cellular uptake. F-14512 exhibits significant cytotoxicity against cells with high PTS activity and induces DNA damage. F-14512 demonstrates potent antitumor activity in the MX1 breast tumor xenograft model. F-14512 can be used to study breast cancer .
|
-
- HY-106031A
-
|
|
Topoisomerase
DNA/RNA Synthesis
|
Cancer
|
|
F-14512 hydrochloride is an anticancer agent that utilizes the polyamine transport system (PTS) to selectively deliver polyamine-containing drugs to cancer cells. F-14512 hydrochloride enhances the affinity of polyamines for DNA, thereby inhibiting topoisomerase II and achieving selective cellular uptake. F-14512 hydrochloride exhibits significant cytotoxicity against cells with high PTS activity and induces DNA damage. F-14512 hydrochloride demonstrates potent antitumor activity in the MX1 breast tumor xenograft model. F-14512 hydrochloride could be used to study breast cancer .
|
-
- HY-W014622
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
CRT0044876 is a potent and selective apurinic/apyrimidinic endonuclease 1 (APE1) inhibitor (IC50=~3 μM). CRT0044876 inhibits the AP endonuclease, 3′-phosphodiesterase and 3′-phosphatase activities of APE1, and is a specific inhibitor of the exonuclease III family of enzymes to which APE1 belongs. CRT0044876 potentiates the cytotoxicity of several DNA base-targeting compounds .
|
-
- HY-N0069R
-
|
Solamargin (Standard); δ-Solanigrine (Standard)
|
P-glycoprotein
Reference Standards
Apoptosis
|
Cancer
|
|
Solamargine (Standard) is the analytical standard of Solamargine. This product is intended for research and analytical applications. Solamargine, a derivative from the steroidal solasodine in Solanum species, exhibits anticancer activities in numerous types of cancer. Solamargine induces non-selective cytotoxicity and P-glycoprotein inhibition. Solamargine significantly inhibits migration and invasion of HepG2 cells by down-regulating MMP-2 and MMP-9 expression and activity .
|
-
- HY-169265
-
|
|
Bcl-2 Family
|
Others
|
|
BRD-K20733377 is an inhibitor for Bcl-2, and exhibits selective cytotoxicity against senescent cells, that inhibits the viability of Etoposide (HY-13629)-induced IMR-90 senescent cell with an IC50 of 10.7 μM. BRD-K20733377 reduces the mRNA expression of aging-related genes p16, p21 and KI67 in aged mouse model .
|
-
- HY-163632
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-112 (SPP10) is an EGFR kinase inhibitor which exhibits IC50s of 2.31 ± 0.3, 3.16 ± 0.8, and 4.2 ± 0.2 μM, against MCF-7, H69AR, and PC-3 cancer cells, respectively. EGFR-IN-112 also demonstrates selective cytotoxicity against cancer cells .
|
-
- HY-112481
-
|
|
|
Inflammation/Immunology
|
|
IKK2-IN-5 is a selective IKK-2 inhibitor with an IC50 of 0.025 μM. IKK2-IN-5 inhibits the production of TNF-α in LPS (HY-D1056)-stimulated human peripheral blood mononuclear cells. IKK2-IN-5 exhibits extremely low cytotoxicity against human peripheral blood mononuclear cells .
|
-
- HY-B0543
-
|
Thiosinamine; N-Allylthiourea
|
Reactive Oxygen Species (ROS)
|
Cancer
|
|
Allylthiourea can selectively inhibit the oxidation of ammonia. Allylthiourea is commonly used to inhibit nitrification by targeting ammonia monooxygenase and chelating copper in the active site to suppress its activity. Allylthiourea also exhibits anticancer activity, showing cytotoxicity against the MCF-7 cell line with an IC50 of 5.22 mM. Allylthiourea can be utilized in research related to micropollutant biodegradability and cancer studies .
|
-
- HY-175806
-
|
|
TrxR
Reactive Oxygen Species (ROS)
Ferroptosis
|
Cancer
|
|
CS47 is a Thioredoxin Reductase 1 (TRXR1) inhibitor and ferroptosis inducer. CS47 binds non-covalently to sites between the FAD and NADPH pockets of TRXR1. CS47 drives glutathione depletion, lipid reactive oxygen species accumulation, HMOX1-dependent iron overload, and selective cytotoxicity in lung cancer cells. CS47 can be used for the research of lung cancer .
|
-
- HY-148170
-
|
|
EBV
DNA/RNA Synthesis
Nucleoside Antimetabolite/Analog
|
Infection
|
|
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 .
|
-
- HY-181637
-
|
|
Drug Derivative
|
Endocrinology
|
|
4-DMA-3'-OH-Chalcone (compound 24) is a synthetic chalcone derivative and selective cytotoxic agent.4-DMA-3'-OH-Chalcone reduces viability of endometriotic cells, while preserving or enhancing viability of eutopic endometrial cells.4-DMA-3'-OH-Chalcone can be used for the research of endometriosis .
|
-
- HY-P2149A
-
|
|
Mitosis
|
Others
Metabolic Disease
|
|
Concanavalin A (agarose) is composed of Concanavalin A (HY-P2149) conjugated with agarose. Concanavalin A (ConA) is a selective competitive binder targeting the specific carbohydrate structures of glucose and mannose, inducing mitosis, and exhibiting certain cytotoxicity, hepatotoxicity, and teratogenicity. Concanav in A (agarose) can be used for in vivo blood glucose monitoring in diabetes, and for "fishing out" specific glycoproteins or removing sugar impurities from complex samples .
|
-
- HY-W001187R
-
|
|
Mitochondrial Metabolism
DNA/RNA Synthesis
Reactive Oxygen Species (ROS)
Reference Standards
|
Cancer
|
|
Tempo (Standard) is the analytical standard of Tempo. This product is intended for research and analytical applications. Tempo is a nitric oxide radical and a selective scavenger of ROS in mitochondria. Tempo is also an organocatalyst that disproportionates superoxide and oxidizes primary alcohols to aldehydes in a catalytic cycle. Tempo has mutagenic and antioxidant effects and can induceDNA strand breaks. Tempo also exerts cytotoxic and mutagenic properties in mouse lymphoma cells [4].
|
-
- HY-W017378R
-
|
|
Drug Intermediate
Reference Standards
|
Others
|
|
Solamargine (Standard) is the analytical standard of Solamargine. This product is intended for research and analytical applications. Solamargine, a derivative from the steroidal solasodine in Solanum species, exhibits anticancer activities in numerous types of cancer. Solamargine induces non-selective cytotoxicity and P-glycoprotein inhibition. Solamargine significantly inhibits migration and invasion of HepG2 cells by down-regulating MMP-2 and MMP-9 expression and activity .
|
-
- HY-144632
-
|
|
Fungal
|
Infection
|
|
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 .
|
-
- HY-182241
-
|
|
c-Myc
Early 2 Factor (E2F)
TNF Receptor
MDM-2/p53
Reactive Oxygen Species (ROS)
Apoptosis
|
Cancer
|
|
JR4-187 is an orally active, copper-dependent anticancer agent. JR4-187 downregulates genes involved in oxidative phosphorylation, MYC targets and E2F targets in cancer cells, while upregulates genes involved in the TNF-α signaling pathway, p53 pathway and KRAS signaling pathway, and downregulates CTR1 protein . JR4-187 induces ROS production, apoptosis, copper-dependent cytotoxicity, and exhibits selective cytotoxicity against KRAS-mutant cancer cells. JR4-187 is well tolerated in mouse models of pancreatic cancer. JR4-187 can be used in research related to cancers such as pancreatic ductal adenocarcinoma, colon cancer and rectal cancer .
|
-
- HY-101997
-
|
|
Orthopoxvirus
Apoptosis
Caspase
Bcl-2 Family
Akt
|
Infection
Cancer
|
|
BEPP hydrochloride is a double-stranded RNA-dependent protein kinase (PKR) modulator. BEPP hydrochloride enhances the phosphorylation levels of PKR and eIF2α, activates caspase-3, upregulates the pro-apoptotic protein BAX, and downregulates the anti-apoptotic protein Bcl-2. BEPP hydrochloride inhibits vaccinia virus replication and exhibits selective cytotoxicity in cells expressing PKR. BEPP hydrochloride can be used in research related to cancer and viral infections .
|
-
- HY-181959
-
|
|
Eukaryotic Initiation Factor (eIF)
|
Cancer
|
|
APL-4098 is an orally active, selective, ATP-competitive GCN2 inhibitor with a Ki of 4.39 nM and a Kd of 2.9 nM. APL-4098 reduces the phosphorylation level of eIF2α and the expression level of ATF4. APL-4098 impairs mitochondrial function and exerts cytotoxic effects on primary acute myeloid leukemia cells. APL-4098 is applicable to research related to acute myeloid leukemia .
|
-
- HY-149376
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 38 (compound 14) is a tetrazole-based Tubulin inhibitor with antiproliferative potencies. Tubulin inhibitor 38 (100 nM，24 h) mediates mitotic arrest，blocks cell cycle at G2/M phase and induces apoptosis. Tubulin inhibitor 38 exhibits high cytotoxicity with high selectivity index among HeLa，MCF7，and U87 MG cells .
|
-
- HY-145734A
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
AMXI-5001 hydrochloride is a potent, orally active, and dual parp1/2 and microtubule polymerization inhibitor. MXI-5001 hydrochloride exhibits selective antitumor cytotoxicity across a wide variety of human cancer cells with much lower IC50s than existing clinical PARP1/2 inhibitors. AMXI-5001 hydrochloride induces complete regression of established tumors, including exceedingly large tumors .
|
-
- HY-177285
-
|
|
Kinesin
ADC Payload
|
Cancer
|
|
NVP-BQS481 (Compound 1) is a selective Kinesin spindle protein-5 (Eg5) inhibitor with an IC50< 0.5 nM. NVP-BQS481 has significant antimitotic and antitumor activity (IC50: 0.0.9 nM for SK-OV-3ip cells). NVP-BQS481 can be used as a cytotoxic payload for synthesis of antibody-drug conjugates (ADCs) .
|
-
- HY-101096R
-
|
MK-8998 (Standard); CX-8998 (Standard); JZP385 (Standard)
|
Calcium Channel
Reference Standards
|
Neurological Disease
Cancer
|
|
Suvecaltamide (Standard) is the analytical standard of Suvecaltamide (HY-101096). This product is intended for research and analytical applications. Suvecaltamide (MK-8998) is a selective T-type calcium channel inhibitor with oral efficacy. Suvecaltamide exhibits no cytotoxicity in myeloma cell lines and does not affect the antitumor efficacy of Bortezomib (BTZ). Suvecaltamide reverses BTZ-induced peripheral neuropathy (CIPN) in mouse and rat models, and helps inhibit myeloma growth .
|
-
- HY-145734
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
AMXI-5001 is a potent, orally active, and dual parp1/2 and microtubule polymerization inhibitor. MXI-5001 exhibits selective antitumor cytotoxicity across a wide variety of human cancer cells with much lower IC50s than existing clinical PARP1/2 inhibitors. AMXI-5001 induces complete regression of established tumors, including exceedingly large tumors .
|
-
- HY-175270
-
|
|
MAGL
Keap1-Nrf2
NF-κB
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
MAGL-IN-22 (Compound 40) is a reversible, competitive, selective and BBB-penetrable MAGL inhibitor with an IC50 of 0.34 μM for hMAGL. MAGL-IN-22 has significant antioxidant and anti-inflammatory activity, and activates the Nrf2 pathway and significantly inhibits NFκB-mediated inflammation, without inducing cytotoxic effects. MAGL-IN-22 can be used for neurodegenerative diseases, chronic pain and cancers research .
|
-
- HY-112453
-
|
|
Parasite
|
Infection
|
|
IMDNQ1 is a Trypanosoma cruzi inhibitor derived from 1,4-naphthoquinone substituted with cyclic imide. IMDNQ1 effectively inhibits the proliferation of Trypanosoma cruzi epimastigotes, while also reducing the viability of mouse fibroblasts. The selectivity index between the antiproliferative activity and cytotoxicity of IMDNQ1 is 60.25, indicating a certain level of safety. IMDNQ1 can be widely used in studies related to Chagas disease .
|
-
- HY-181054
-
|
|
Bcl-2 Family
Apoptosis
Reactive Oxygen Species (ROS)
|
Cancer
|
|
Mcl-1-IN-21 is a selective Mcl-1 protein inhibitor. Mcl-1-IN-21 can induce apoptosis, elevate intracellular ROS, reduce mitochondrial membrane potential, exert cytotoxicity against human cervical cancer cells, and inhibit tumor growth in a human cervical cancer xenograft mouse model. Mcl-1-IN-21 can be used for the research of cervical cancer .
|
-
- 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-18051
-
|
|
Calcium Channel
|
Cancer
|
|
CXL 017 is a sarco/endoplasmic reticulum Ca 2+-ATPase (SERCA) inhibitor. CXL 017 can inhibit the ATPase activity of SERCA by competing with ATP for binding. CXL 017 exhibits selective cytotoxicity against multidrug-resistant acute myeloid leukemia cells HL60/MX2. CXL 017 can be used in the research of tumors such as multidrug-resistant acute myeloid leukemia .
|
-
- HY-129765
-
|
|
Reactive Oxygen Species (ROS)
|
Cancer
|
|
Thiobenzanilide 63T (63T) is a small molecule that selectively induces cancer cell death in a caspase-independent pathway. Thiobenzanilide 63T induces reactive oxygen species and lipid peroxidation. Thiobenzanilide 63T demonstrates strong cytotoxic activity against a lung-derived cancer cell line. Thiobenzanilide 63T decreases the expression of heme oxygenase (HO-1) in A549 cells .
|
-
- HY-144712
-
|
|
G-quadruplex
Apoptosis
|
Cancer
|
|
L5-DA is a G-quadruplex (G4) ligand and selectively stabilized for G4s over ds26. L5-DA exhibits significant cytotoxicity against HeLa cells (IC50=4.3 μM). L5-DA stabilizes G4s in HeLa cells, induces apoptosis, and cell cycle arrest .
|
-
- HY-179046
-
|
|
VEGFR
|
Cancer
|
VEGFR-2-IN-78 (Compound 6b) is a potent VEGFR-2 inhibitor with an IC50 of 0.21 μM. VEGFR-2-IN-78 exhibits selective cytotoxicity against A-498 and MDA-MB-231 cells. VEGFR-2-IN-78 has antioxidant activity. VEGFR-2-IN-78 can be used in anti-angiogenesis research .
|
-
- HY-153519
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
WWL0245 is a potent and seletive BRD4 PROTAC. WWL0245 selectively degrades BRD4 with sub-nanomolar DC50 (<1 nM) than BRD2/3 and PLK1 ( DC50>1 μM). WWL0245 shows excellent selective cytotoxicity in the BETi sensitive cancer cell lines, including AR-positive prostate cancer cell lines. WWL0245 is a promising drug candidate for AR-positive prostate cancer research and a valuable tool compound to study the biological function of BRD4 .
|
-
- HY-W1126504
-
|
MC339
|
Notch
|
Cancer
|
|
ETN029 (MC339) is a selective DLL3 ligand. ETN029 labeled with 225Ac has dose-dependent cytotoxicity in SCLC, NEPC and metastatic melanoma cells and increases the phosphorylation of H2AX expression. ETN029 labeled with 177Lu shows rapid uptake persistent tumor retention and favorable tumor-to-kidney ratio. ETN029 can be used for cancers like SCLC and NEPC imaging and research .
|
-
- HY-182542
-
|
|
OAT
|
Cancer
|
|
SOAT-IN-3 is a selective inhibitor of sodium-dependent organic anion transporter (SOAT/SLC10A6). SOAT-IN-3 reduces intracellular estradiol synthesis, the process of dehydroepiandrosterone (DHEA) production from DHEAS, and DHEAS-induced cancer cell proliferation. SOAT-IN-3 shows no cytotoxicity against breast cancer cells at the tested concentrations. SOAT-IN-3 can be used in the research of breast cancer .
|
-
- HY-156640
-
|
LP-168
|
EGFR
|
Cancer
|
|
Rocbrutinib is an orally available, highly selective Bruton's tyrosine kinase (BTK) inhibitor, with an IC50 of 0.11 nM against wild-type BTK and an IC50 of 1.0 nM against C481S-mutated BTK. Rocbrutinib reduces the viability of leukemia cells, induces cytotoxicity and inhibits cell migration. Rocbrutinib can be used in research related to chronic lymphocytic leukemia, non-Hodgkin's lymphoma and mantle cell lymphoma .
|
-
- HY-N9674
-
|
|
Others
|
Cancer
|
|
Epimedonin H is a selective prenylated 2-phenoxychromone compound with no significant cytotoxicity against five human cancer cell lines, including HL-60 and SMMC-7721 (IC50 > 10 μM). Epimedonin H can be used in potential activity screening studies in the field of natural product chemistry. Epimedonin H can be extracted from the dried aerial parts of Epimedium brevicornum (a plant of the genus Epimedium in the Berberidaceae family) .
|
-
- HY-19541A
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
I-CBP112 hydrochloride is a selective inhibitor of CBP/P300 that directly binds their bromodomains (Kds = 142 and 625 nM, respectively). I-CBP112 significantly reduces the leukemia-initiating potential of MLL-AF9(+) acute myeloid leukemia cells in a dose-dependent manner in vitro and in vivo. I-CBP112 increases the cytotoxic activity of BET bromodomain inhibitor JQ1 as well as doxorubicin .
|
-
- HY-183716
-
|
|
Drug Derivative
|
Cancer
|
|
Mito-TP-2 is a triptolide (HY-32735) derivative. Mito-TP-2 exhibits concentration-dependent cytotoxicity in cancer cells. Mito-TP-2 is selectively driven and accumulated into the mitochondria of tumor cells by mitochondrial transmembrane potential and exerts specific mitochondrial toxicity. Mito-TP-2 can be used for the research of liver cancer, breast cancer, and non-small cell lung cancer .
|
-
- HY-159730
-
|
|
Aminotransferases (Transaminases)
|
Inflammation/Immunology
Cancer
|
|
ERG245 is a selective amino acid aminotransferase (BCAT1) inhibitor with a human IC50 of 0.5 nM. ERG245 enhances oxidative phosphorylation (OXPHOS) in CD8 + T cells by specifically inhibiting BCAT1 activity, thereby increasing the cytotoxicity of CD8 + T cells. ERG245 shows anti-inflammatory and anti-tumor activities. ERG245 can be used for the researches of cancer anf inflammation, such as colitis and colon cancer .
|
-
- HY-183718
-
|
|
PROTACs
Anaplastic lymphoma kinase (ALK)
|
Neurological Disease
Cancer
|
|
M4K3250 is a selective ALK2 PROTAC degrader with a pDC50 of 7.9. M4K3250 induces the formation of a ternary complex between ALK2 and the E3 ubiquitin ligase CRBN, thereby causing ALK2 degradation and inhibiting ALK2 activity. M4K3250 exhibits cytotoxicity in glioblastoma cells. M4K3250 can be used in studies related to glioblastoma .
|
-
- 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-182347
-
|
|
Parasite
|
Infection
|
|
LSPN954 (compound 4i) is an indole-based peptidomimetic antiplasmodial agent that exhibits submicromolar activity against both sensitive and multidrug-resistant *Plasmodium falciparum* strains, with low cytotoxicity to human cells and a high selectivity index. LSPN954 shows slow-acting inhibitory activity, allowing the initial development of *Plasmodium* followed by morphological changes, and its activity is independent of the inhibition of plastid-dependent isoprenoid biosynthesis. LSPN954 can be used in malaria research .
|
-
- HY-121337
-
|
R-40244
|
Environmental Pollutants
Apoptosis
Bcl-2 Family
|
Others
|
|
Flurochloridone (R-40244) is a selective preemergence and persistent herbicide. Flurochloridone induces endoplasmic reticulum (ER) stress and activated unfolded protein response (UPR) signaling pathways. Flurochloridone impairs cell viability and induces cytotoxicity and apoptosis mediated by ER stress via activating eIF2α-ATF4/ATF6-CHOP-Bim/Bax signaling pathways in TM4 cells .
|
-
- 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-149040
-
|
(S)-OBI-3424; (S)-TH-3424; AST-3424
|
17β-HSD
|
Cancer
|
|
Odafosfamide ((S)-OBI-3424) is a highly selective prodrug bis-alkylating agent activated by aldehyde-keto reductase 1C3 (AKR1C3(). Odafosfamide is highly cytotoxic to cell lines with high AKR1C3 expression. Odafosfamide exhibits antitumor activity in a variety of tumors with high AKR1C3 expression (such as liver cancer, non-small cell lung cancer, and leukemia). Odafosfamide can be used in cancer research .
|
-
- HY-147646
-
|
|
CDK
Apoptosis
|
Cancer
|
|
CDK1/Cyc B-IN-1 (Compound 5) is a selective CDK1/Cyc B complex inhibitor with an IC50 of 97 nM. CDK1/Cyc B-IN-1 triggers apoptosis and G2/M cell cycle arrest. CDK1/Cyc B-IN-1 shows broad-spectrum cytotoxic action against cancer cell lines .
|
-
- HY-182767
-
|
|
Na+/HCO3- Cotransporter
|
Cancer
|
|
SOAT-IN-2 is a selective sodium-dependent organic anion transporter (SOAT, SLC10A6) inhibitor. SOAT-IN-2 blocks sodium-dependent cellular uptake of sulfated steroid Dehydroepiandrosterone sulfate (DHEAS, HY-113416). SOAT-IN-2 reduces intracellular estradiol synthesis, DHEA (HY-14650) formation, and DHEAS-stimulated cancer cell proliferation without inducing cytotoxicity. SOAT-IN-2 can be used for the research of breast cancer .
|
-
- HY-173526
-
|
|
Bacterial
Calcium Channel
|
Infection
|
|
H052 is a selective Staphylococcus aureus α-hemolysin (Hla) inhibitor. H052 binds to Hla monomers, disrupts the interaction with host cell membranes to block pore formation, inhibiting calcium ion influx, cytotoxicity, and inflammatory responses. H052 exhibits potency (EC50=30 nM in U937 cells) against Hla-induced calcium influx. H052 is promising for research of lung infections caused by S. aureus .
|
-
- HY-172873
-
|
|
HDAC
Caspase
Apoptosis
|
Cancer
|
|
HDSI-18 is an orally active HDAC6 selective inhibitor (IC50: 1.6 nM). HDSI-18 is cytotoxic to K562, MV4-11, MOLM-13, THP-1, and Jurkat cells (IC50: 0.48, 0.58, 0.91, 1.79, and 4.31 μM, respectively). HDSI-18 activates Caspase-3, induces mitochondrial depolarization and apoptosis, and has antitumor activity .
|
-
- HY-100707
-
|
|
DNA-PK
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
IC 86621 is a potent DNA-dependent protein kinase (DNA-PK) inhibitor, with an IC50 of 120 nM. IC 86621 also acts as a selective and reversible ATP-competitive inhibitor.IC 86621 inhibits DNA-PK mediated cellular DNA double-strand break (DSB) repair (EC50=68 µM). IC 86621 increases DSB-induced antitumor activity without cytotoxic effects. IC 86621 can protects rheumatoid arthritis (RA) T cells from apoptosis .
|
-
- HY-P990914
-
|
GS-1811; JTX-1811
|
CCR
|
Inflammation/Immunology
Cancer
|
|
Denikitug (GS-1811; JTX-1811) is a humanized monoclonal antibody against CCR8 receptor with a KD of 16.8 pM. Denikitug specifically binds to human CCR8, inhibits CCL1-induced downstream CCR8 signaling. Denikitug selectively depletes cells expressing CCR8 via antibody-dependent cellular cytotoxicity (ADCC). Denikitug promotes anti-tumor immunity and can be used for the research of cancer and immunology .
|
-
- HY-161240
-
|
|
Monoamine Oxidase
|
Neurological Disease
Inflammation/Immunology
|
|
MAO-B-IN-30 (compound IS7) is a potent, selective and cross the blood-brain barrier MAO-B inhibitor with IC50 values of 19.176, 0.082 µM for MAO-A and MAO-B, respectively. MAO-B-IN-30 shows antiproliferative activity and non-cytotoxic. MAO-B-IN-30 reduces TNF-alpha, IL-6, NF-kB levels. MAO-B-IN-30 has the potential for the research of Parkinson's disease .
|
-
- HY-130783
-
|
|
Fluorescent Dye
|
Others
|
|
LysoFP-NO2 is a turn-on fluorescent probe for carbon monoxide (CO) that localizes to the lysosome. In the presence of lysosomal CO, lysoFP-NO2 is transformed into lysoFP-NH2, which is highly fluorescent. LysoFP-NO2 is selective for CO over various reactive nitrogen, oxygen, and sulfur species. It displays excitation/emission maxima of 440/528 nm, respectively, and is not cytotoxic to HepG2 cells for up to five hours when used at a concentration of 30 μM.
|
-
- HY-155479
-
|
|
Bacterial
|
Infection
|
|
PqsR-IN-3 (compound 16e) is a selective inhibitor of the pqs system (IC50=3.7 μM) and its associated virulence factor pyocyanin (IC50=2.7 μM). PqsR-IN-3 inhibits bacterial biofilm synthesis and is significantly cytotoxic against Pseudomonas aeruginosa. PqsR-IN-3 has synergistic effects with several antibiotics, such as Ciprofloxacin (HY-B0356) and Tobramycin (HY-B0441) .
|
-
- HY-157942
-
|
|
Cytochrome P450
|
Cancer
|
|
CYP1B1-IN-7 (compound 2a) is a selective inhibitor of CYP1B1 (IC50: 75 nM). CYP1B1-IN-7 also reverses resistance (IC50: 29 μM) and exhibits cytotoxicity in the CYP1B1-overexpressing MCF-7 cell line that is resistant to Docetaxel (HY-B0011) .
|
-
- HY-153225
-
|
|
HIV
Reverse Transcriptase
|
Infection
|
|
PYR01 is a non-nucleoside reverse transcriptase inhibitor and a killing activator targeting HIV infected cells. PYR01 has cytokilling and antiviral properties of HIV-1 infection with the IC50 values of 27.5nM and 39.7nM, respectively. PYR01 leads to selective cytotoxicity by promoting HIV-1 Gag-Pol dimerization and HIV-1 protease intracellular activation. PYR01 can be used in the study of HIV .
|
-
- HY-10015R
-
|
5-(4-Phenoxybutoxy)psoralen (Standard)
|
Reference Standards
Potassium Channel
|
Inflammation/Immunology
|
|
PAP-1 (Standard) is the analytical standard of PAP-1. This product is intended for research and analytical applications. PAP-1 (5-(4-Phenoxybutoxy)psoralen) is a potent, selective, and orally active Kv1.3 blocker (EC50=2 nM). PAP-1 blocks Kv1.3 in a use-dependent manner and acts by preferentially binding to the C-type inactivated state of the channel. PAP-1 exhibits 23-fold selectivity over Kv1.5 (EC50=45 nM), and further displays 33- to 125-fold selectivity over all other Kv1-family channels. PAP-1 does not exhibit cytotoxic or phototoxic effects .
|
-
- HY-178330
-
|
|
Others
Topoisomerase
|
Infection
|
|
IKE16 is a fungi-selective eukaryotic topoisomerase II inhibitor, with an IC50 value of 13.68 μM. IKE16 suppresses both the DNA relaxation activity and the decatenation activity of yTOPOII selectively. IKE16 shows moderate activity against standard fungal strains (Candida albicans ATCC 10231, Saccharomyces cerevisiae ATCC 89763) with a minimum inhibitory concentration (MIC) of 2 μg/mL against S. cerevisiae ATCC 89763. IKE16 exhibits high cytotoxicity against human cells, with an EC50 of 0.07 μM in HepG2 and 0.045 μM in HEK-293. IKE16 can be used for the study of antifungal infection .
|
-
- HY-179014
-
|
|
DNA Glycosylase
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
OGG1 activator-1 (Compound 30) is a selective 8-oxoguanine DNA glycosylase-1 (OGG1) activator with an AC50 value of 0.58 μM. OGG1 activator-1 does not activate nor inhibit the key downstream repair enzyme APE1, and shows > 150-fold selectivity for the activation effect on OGG1. OGG1 activator-1 exhibits extremely high metabolic stability and almost no cytotoxicity. OGG1 activator-1 can be used for the study of oxidative stress-related diseases (such as neurodegenerative diseases, fibrotic diseases, cancer, inflammation, etc.) .
|
-
- HY-183683
-
|
|
Proteasome
Apoptosis
|
Cancer
|
|
DQ-9 is a selective immunoproteasome β5i inhibitor (IC50=0.0019 μM). DQ-9 generates additional inhibitory substances via iron-mediated intracellular activation, and induces oxidative stress, carbon-centered free radicals and macromolecular damage through its artemisinin domain. DQ-9 induces apoptosis in leukemia and multiple myeloma cells. DQ-9 exhibits selective cytotoxicity against leukemia and multiple myeloma cells by elevating the labile iron pool. DQ-9 can be used in the research of hematological malignancies (leukemia, multiple myeloma, mantle cell lymphoma, acute myeloid leukemia) .
|
-
- HY-114778
-
|
SHR3162; Fuzuloparib
|
PARP
|
Cancer
|
|
Fluzoparib (SHR3162) is a potent and orally active PARP1 inhibitor (IC50=1.46±0.72 nM, a cell-free enzymatic assay) with superior antitumor activity. Fluzoparib selectively inhibits the proliferation of homologous recombination repair (HR)-deficient cells, and sensitizes both HR-deficient and HR-proficient cells to cytotoxic agents. Fluzoparib exhibits good pharmacokinetic properties in vivo and can be used for BRCA1/2-mutant relapsed ovarian cancer research .
|
-
- HY-176954
-
|
|
Proton Pump
Ras
Autophagy
Apoptosis
|
Cancer
|
|
RSC-1255 is a potent and selective Vacuolar H⁺-ATPase (V-ATPase) inhibitor that directly binds the mammalian V-ATPase complex with a Kd = 23 nM. RSC-1255 exhibits preferential cytotoxicity toward KRAS-mutant cancer cells, especially KRAS G13D and KRAS G12V cells. RSC-1255 induces apoptosis and blocks lysosomal acidification, autophagy, and macropinocytosis in cancer cells. RSC-1255 can be used for the study of KRAS-driven lung and colon cancers .
|
-
- HY-N3017
-
|
|
Antibiotic
|
Neurological Disease
Inflammation/Immunology
|
|
Artemitin is a flavonoid neuroanesthetic agent with moderate cytotoxicity. Artemitint has selective inhibitory activity against Meth-A sarcoma cells with an ED50 of 5-10 μg/mL, and has no significant effect on LLC lung cancer cells. Artemitin exerts anticancer activity by affecting cell proliferation signaling pathways, and also has potential anti-inflammatory and neuroprotective effects. Artemitin exhibits a dose-dependent antinociceptive effect in the mouse hot plate test, with an ED50 of 1.6 μg/kg, and has analgesic activity .
|
-
- HY-P992349
-
|
|
CD20
Apoptosis
|
Cancer
|
|
DXL625 is an autophilic CD20-targeting agent. DXL625 triggers downstream apoptosis signaling pathways dependent on intact lipid rafts and extracellular Ca 2+. DXL625 induces caspase-mediated apoptosis in cancer cells and selectively targets cells in the actively proliferative S phase. DXL625 mediates complement-dependent cytotoxicity in cancer cells and primary B lymphocytes. DXL625 can be used in research related to Burkitt's lymphoma and B-cell lymphoma .
|
-
- HY-181756
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
LGF308 is a PROTAC degrader of BRD4 that exhibits selective cytotoxicity toward cancer cells over normal cells. LGF308 mediates the formation of a ternary complex between BRD4 and DCAF11 to achieve BRD4 degradation. LGF308 induces tumor cell apoptosis by upregulating apoptosis-related proteins. LGF308 inhibits tumor cell proliferation and migration in breast cancer and triple-negative breast cancer cell lines. LGF308 can be used for the research of breast cancer .
|
-
- 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-141599
-
|
ADCT 301
|
Antibody-Drug Conjugates (ADCs)
Interleukin Related
|
Cancer
|
|
Camidanlumab tesirine (ADCT 301) is an ADC comprising HuMax-TAC, a human IgG1 mAb directed against human CD25, stochastically conjugated through a dipeptide cleavable linker to a pyrrolobenzodiazepine (PBD) dimer warhead. Camidanlumab tesirine has a drug–antibody ratio (DAR) of 2.3. Camidanlumab tesirine binds human CD25 with picomolar affinity. Camidanlumab tesirine has highly potent and selective cytotoxicity against a panel of CD25-expressing human lymphoma cell lines .
|
-
- HY-P11019
-
|
|
CXCR
Calcium Channel
|
Cancer
|
|
IS4 is a selective CXCR4 competitive antagonist, with an IC50 of 0.65 nM in THP-1 cells and 38.75 nM in Jurkat cells. IS4 is stable in serum and non-cytotoxic. IS4 competitively binds to CXCR4 with CXCL12, thereby inhibiting CXCL12-induced intracellular Ca 2+ release and cancer cell migration. IS4 can be used in the research on the prevention of metastasis of breast cancer, prostate cancer, leukemia, and other diseases .
|
-
- HY-W391625
-
|
(Rac)-Epiligulyl oxide
|
Fungal
|
Cancer
|
|
(Rac)-Dehydrocostus Lactone ((Rac)-Epiligulyl oxide) is a natural product with antiparasitic activity. (Rac)-Dehydrocostus Lactone can significantly inhibit the growth of Trypanosoma brucei rhodesiense. (Rac)-Dehydrocostus Lactone exhibits a broad spectrum of biological effects, including anti-inflammatory, anticancer, antiviral and antimicrobial activities. (Rac)-Dehydrocostus Lactone also has antifungal, antioxidant, antidiabetic, antiulcer and antihelminthic effects. (Rac)-Dehydrocostus Lactone exhibits different IC(50) values in cytotoxicity tests and has a high selectivity index .
|
-
- HY-P4284
-
|
|
Proteasome
ClpP
Bacterial
|
Infection
|
|
Z-GGF-CMK is an Antibacterial agent, an inhibitor of the ClpP1P2 serine protease complex (with an IC50 of 50 μM against intracellular ClpP1P2 protease activity in Mycobacterium bovis BCG), and a selective inhibitor of the mycobacterial Proteasome (with an IC50 of 50 μM against the proteasome in M. bovis BCG). Z-GGF-CMK inhibits the growth of mycobacteria. Z-GGF-CMK exhibits cytotoxic activity against liver cancer cells. Z-GGF-CMK can be used in the research of tuberculosis .
|
-
- HY-N18126
-
|
|
Others
|
Cancer
|
|
13b,14-Dihydrorutaecarpine is a cytotoxin derived from dihydrorutaecarpine. 13b,14-Dihydrorutaecarpine exerts selective cytotoxicity against central nervous system (CNS) and prostate cancer cell lines (GI50=0.02 μM and 0.2 μM). 13b,14-Dihydrorutaecarpine can be used in the research of central nervous system (CNS) cancer, ovarian cancer, prostate cancer and renal cancer .
|
-
- HY-B0543R
-
|
Thiosinamine (Standard); N-Allylthiourea (Standard)
|
Reference Standards
Reactive Oxygen Species (ROS)
|
Cancer
|
|
Allylthiourea (Standard) is the analytical standard of Allylthiourea. This product is intended for research and analytical applications. Allylthiourea can selectively inhibit the oxidation of ammonia. Allylthiourea is commonly used to inhibit nitrification by targeting ammonia monooxygenase and chelating copper in the active site to suppress its activity. Allylthiourea also exhibits anticancer activity, showing cytotoxicity against the MCF-7 cell line with an IC50 of 5.22 mM. Allylthiourea can be utilized in research related to micropollutant biodegradability and cancer studies [4].
|
-
- HY-146000
-
|
|
Influenza Virus
|
Inflammation/Immunology
|
|
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 .
|
-
- HY-178014
-
|
|
Salt-inducible Kinase (SIK)
Src
|
Others
|
|
SIK1-IN-1 (Compound 27) is a selective Salt-inducible kinase 1 (SIK1) inhibitor with an IC50 of 0.7 nM for SIK1 over SIK2 and SIK3. SIK1-IN-1 has no cytotoxicity against HEK293 cells and PBMCs (maximum concentration of 30 μM). SIK1-IN-1 also has potent inhibitory activities for 392 kinases, in particular tyrosine kinases, such as FGR, HCK and LYN) .
|
-
- 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-15582S
-
|
|
Isotope-Labeled Compounds
Microtubule/Tubulin
ADC Payload
|
Cancer
|
|
Auristatin E-d8 is the deuterium labeled Auristatin E (HY-15582). Auristatin E is a cytotoxic microtubule polymerization inhibitor with potent and selective antitumor activity. Auristatin E is a cytotoxin in antibody-drug conjugates (ADC). Auristatin E inhibits cell division by blocking the polymerisation of tubulin, promising for research in B-cell malignancies. Auristatin E, a synthetic analogue of the Dolastatin 10 (HY-15580), is linear peptides comprised of four amino acids .
|
-
- HY-132258A
-
|
IMGN853 (solution)
|
Antibody-Drug Conjugates (ADCs)
Antifolate
|
Cancer
|
|
Mirvetuximab soravtansine (IMGN853) solution is an anti-folate receptor α (FRα) antibody drug-conjugate (ADC) consisting of the cytotoxic maytansinoid, DM4, covalently linked to the humanized monoclonal antibody M9346A, and the drug-linker conjugate for ADC is sulfo-SPDB-DM4 (HY-101141). Mirvetuximab soravtansine selectively binds to folate receptor 1 (FOLR1). Mirvetuximab soravtansine has an anti-proliferative effect via growth arrest and augmented DNA damage .
|
-
- 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-179504
-
|
|
Phosphodiesterase (PDE)
TNF Receptor
|
Inflammation/Immunology
|
|
PDE4B-IN-6 (compound 4i) is a potent and selective PDE4B inhibitor with an IC50 of 7.42 nM. PDE4B-IN-6 shows ~195- and ~169-fold selectivity for PDE4B over PDE4A (IC50 = 1540 nM) and PDE4C (IC50 = 1260 nM), respectively. PDE4B-IN-6 increases cAMP level and suppresses TNF-α expression. PDE4B-IN-6 shows favorable antioxidant profiles and low cytotoxicity. PDE4B-IN-6 can be used for chronic obstructive pulmonary disease (COPD) research .
|
-
- HY-153385
-
|
|
Molecular Glues
Epigenetic Reader Domain
|
Cancer
|
|
TMX1 is a covalent, selective BRD4 molecular glue degrader. TMX1 binds to the JQ1-binding site of BRD4BD2, forms covalent bonds with Cys58 of DCAF16 and Cys87 of GAK in a BRD4BD2-dependent template-assisted manner, stabilizes the BRD4-TMX1-DCAF16 ternary complex, and promotes the ubiquitination of BRD4 via the CRL4DCAF16 ubiquitin ligase complex. TMX1 induces selective degradation of BRD4, mild degradation of BRD2 and BRD3, as well as DCAF16-dependent cytotoxicity .
|
-
- HY-156240
-
|
|
E1/E2/E3 Enzyme
Keap1-Nrf2
|
Metabolic Disease
|
|
DI-1548 is a potent, selective, and irreversible covalent inhibitor of DCN1 (IC50 = 4.6 nM). DI-1548 potently and selectively inhibits cullin 3 neddylation at nanomolar concentrations, and exhibits no obvious effect on the neddylation of other cullin members (including cullin 1, 2, 4A, 4B, and 5). DI-1548 exhibits no cytotoxicity. DI-1548 covalently binds to DCN1, disrupting the DCN1-UBC12 interaction, causing the collapse of the neddylation complex, inactivating CRL3, leading to NRF2 accumulation and upregulation of its target genes, and ultimately protecting mice from liver damage. DI-1548 can be used in liver injury research .
|
-
- HY-W751180
-
|
CGP52421-13C6
|
Isotope-Labeled Compounds
FLT3
|
Cancer
|
|
3-Hydroxy Midostaurin- 13C6 (CGP52421- 13C6) is the 13C-labeled 3-Hydroxy Midostaurin (HY-108263). 3-Hydroxy Midostaurin (CGP 52421), a metabolite of PKC412, effectively inhibits FMS-like tyrosine kinase-3 (FLT3) autophosphorylation with IC50s of approximately 132 nM and 9.8 μM in culture medium and plasma, respectively. 3-Hydroxy Midostaurin is less selective but more cytotoxic than PKC412 .
|
-
- HY-D2186
-
|
|
Biochemical Assay Reagents
|
Others
|
|
BTD probe-1 is a benzothiazine-based chemoproteomic probe and selective protein S-sulfenic acid (Cys-SOH) labeling agent. BTD probe-1 labels protein S-sulfenic acids in vitro in cell and tissue samples, and in situ in intact cells, enabling detection or enrichment of modified proteins/peptides. BTD probe-1 exhibits no cytotoxicity in cells at concentrations ≤1 mM. BTD probe-1 enables global, site-specific mapping and quantification of cysteine S-sulfenylation in complex proteomes with lower input material .
|
-
- HY-158721
-
|
Marinamide
|
Endogenous Metabolite
Parasite
|
Infection
Cancer
|
|
Penicinoline (Marinamide) (Compound 1), a pyrrolyl 4-quinolinone alkaloid, is a microbial secondary metabolite. Penicinoline can be isolated from endophytic fungus Penicillium sp. Penicinoline has antimalarial activity against Chloroquine (HY-17589A) sensitive strain (pf3d7) and against Chloroquine resistant strain (pfDd2) of plasmodium falciparum. Penicinoline also has strong insecticidal activity against Aphis gossypii and selective anticancer effect with significant cytotoxicity for 95-D and HepG2 cells .
|
-
- HY-180546
-
|
|
CDK
|
Cancer
|
|
CDK2-IN-53 (compound 9) is a CDK2 inhibitor with anticancer activity. CDK2-IN-53 selectively inhibits the proliferation of HCT-116 and MCF-7cells with IC50 values of 13.89 and 7.65 μM, respectively, while showing lower cytotoxicity toward normal lung fibroblast (WI-38) cells (IC50 = 71.24 μM). CDK2-IN-53 can be used for cancer research, such as colon and breast cancer .
|
-
- HY-153094
-
|
|
HIV
HIV Integrase
|
Infection
|
|
BDM-2 is an IN-LEDGF allosteric inhibitor (INLAI) of HIV-1 integrase (IN refers to integrase) (IC50=47 nM) with potent anti-Retroviral (ARV) activity. BDM-2 shows IN multimerization activation effect with an AC50 value of 20 nM. BDM-2 blocks the interaction between the catalytic core domain of IN (IN-CCD) and the Integrase binding domain of LEDGF/p75 (IBD), with an IC50 value of 0.15 μM. BDM-2 exhibits highly selective and favorable cytotoxicity .
|
-
- HY-181841
-
|
|
Toll-like Receptor (TLR)
HIV
|
Infection
|
|
TLR8 agonist 10 is a selective TLR8 agonist with an EC50 of 0.019 μM in humans. TLR8 agonist 10 activates TLR8-mediated signaling pathways. As a latency-reversing agent, TLR8 agonist 10 reactivates latent HIV-1 reservoirs. TLR8 agonist 10 activates innate cytotoxic natural killer cells to target HIV-infected CD4 + T cells. TLR8 agonist 10 is applicable to research related to HIV-1 infection .
|
-
- HY-145685
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
RECQL5-IN-1 (Compound 4a) acts as an orally effective RECQL5 inhibitor (targeting both enzymatic and nonenzymatic domain). RECQL5-IN-1 is a potent inhibitor of RECQL5 helicase activity (IC50=46.3 nM), stabilizes the interaction between RECQL5-RAD51 proteins, causes RAD51 aggregation and homologous recombination repair (HRR) inhibition, thereby exhibiting selective cytotoxicity in RECQL5-expressing cancer cells .
|
-
- HY-174404
-
|
|
Topoisomerase
Apoptosis
Bcl-2 Family
|
Cancer
|
|
Topoisomerase II inhibitor 23 is a potent topoisomerase II inhibitor (IC50 = 0.94 μM). Topoisomerase II inhibitor 23 shows high selectivity and exceptional cytotoxic activity in MCF-7, HepG2, and HCT116 cells. Topoisomerase II inhibitor 23 induces cell cycle arrest at the G1 phase, leading to inhibition of cell proliferation. Topoisomerase II inhibitor 2 induces apoptosis by up-regulating the pro-apoptotic Bax level and down-regulating the anti-apoptotic Bcl-2 level.
|
-
- HY-112146
-
MMG-11
5 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-P991942A
-
|
BAY3375968 (FUT8-KO); TPP-23411 (FUT8-KO)
|
CCR
|
Cancer
|
|
Lanerkitug (FUT8-KO) (BAY3375968 (FUT8-KO)) is an anti-CCR8 monoclonal antibody expressed by CHO cells with the fucosyltransferase 8 gene (FUT8) knocked out. Fucose deficiency enhances the ADCC effect of the antibody. Lanerkitug (HY-P991942) selectively depletes human CCR8+Tregs via antibody dependent cellular cytotoxicity (ADCC) and antibody dependent cellular phagocytosis (ADCP). Lanerkitug can be used in the research of solid tumors .
|
-
- 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-183866
-
|
Maleimide-KGDEVD-doxorubicin
|
HSP
IFNAR
|
Cancer
|
|
MPD-1 (Maleimide-KGDEVD-doxorubicin) is a peptide drug conjugate (PDC). MPD-1 enhances CD8 + T cell tumor infiltration, and activates antigen-presenting cells. MPD-1 enables dual-trigger payload release, amplifies cytotoxicity via in situ feedback, and selectively delivers payload to tumor microenvironments via enhanced albumin metabolism and macropinocytosis. MPD-1 exhibits antitumor efficacy in mouse colorectal cancer models. MPD-1 can be used for the research of colorectal cancer .
|
-
- HY-122224
-
|
|
Sigma Receptor
|
Cancer
|
|
SW43 is a Sigma-2 selective ligand and agonist. SW43 is an ideal molecule for the development of cancer-targeted drug compounds. SW43 conjugated with DOX-L-NETA ( 89Y) exhibits antitumor activity in a VX2 cancer liver tumor allograft rabbit model. SW 43 conjugated with SW IV-52s to form SW III-123 activates the NF-κB pathway, has potent cytotoxicity against ovarian cancer cell lines, and induces apoptosis .
|
-
- 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-121382
-
|
|
Cholinesterase (ChE)
Apoptosis
Necroptosis
|
Neurological Disease
Cancer
|
|
Gypsogenin is a selective mixed-type BChE inhibitor (Ki=19.99 μM) that also exhibits significant cytotoxicity against various human cancer cell lines. Gypsogenin inhibits tumor growth by inducing cell cycle arrest and triggering apoptosis. Gypsogenin displays antibacterial activity against bacteria such as Bacillus subtilis and Bacillus thuringiensis, and often serves as a key parent nucleus for the synthesis of anticancer compounds. Gypsogenin is widely used in research on Alzheimer's disease and various cancers including colon cancer, melanoma, and leukemia .
|
-
- HY-121337R
-
|
R-40244 (Standard)
|
Reference Standards
Apoptosis
Bcl-2 Family
|
Others
|
|
Flurochloridone (Standard) is the analytical standard of Flurochloridone. This product is intended for research and analytical applications. Flurochloridone (R-40244) is a selective preemergence and persistent herbicide. Flurochloridone induces endoplasmic reticulum (ER) stress and activated unfolded protein response (UPR) signaling pathways. Flurochloridone impairs cell viability and induces cytotoxicity and apoptosis mediated by ER stress via activating eIF2α-ATF4/ATF6-CHOP-Bim/Bax signaling pathways in TM4 cells .
|
-
- 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-174373
-
|
|
SARS-CoV
Angiotensin-converting Enzyme (ACE)
|
Infection
|
|
SARS-CoV-2-IN-113 (Compound 24) is a sulfonohydrazide derivative against SARS-CoV-2 infection with an IC50 of 8.320 μM. SARS-CoV-2-IN-113 exerts potent antiviral effects by inhibiting the entry and replication of SARS-CoV-2, and downregulating the expression of genes and proteins such as Spike, ACE-2, and RdRp. SARS-CoV-2-IN-113 has high selectivity and low cytotoxicity, and can be used in the research of SARS-CoV-2 .
|
-
- HY-162116
-
|
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
Cancer
|
|
TLR7 agonist 18 (Compound 21a) is a selective Toll-like receptor 7 (TLR7) agonist with an EC50 of 7.8 μM. TLR7 agonist 18 is not cytotoxic to hTLR7 cotransfected HEK293 cell lines and can induce the secretion of several cytokines, including IL-1β, IL-12p70, IL-8, and TNF-α. TLR7 agonist 18 can be used in vaccine, asthma, allergy and anti-cancer research .
|
-
- HY-124084
-
|
|
Stearoyl-CoA Desaturase (SCD)
|
Cancer
|
|
SW203668 is an irreversible stearoyl CoA desaturase (SCD) inhibitor with an IC50 of 54 nM. SW203668 covalently binds and inhibits SCD, depletes unsaturated fatty acids, and triggers cell death in sensitive cells. SW203668 requires demethylation by CYP4F11 to form its active SCD-inhibiting form; differential CYP4F11 expression drives selective cytotoxicity. SW203668 exerts cytotoxicity toward CYP4F11-expressing non-small cell lung cancer (NSCLC) cells and spares CYP4F11-lacking NSCLC cells. SW203668 inhibits tumor growth in immunodeficient mice bearing CYP4F11-expressing NSCLC xenografts and spares mouse skin sebocytes. SW203668 can be used for the research of non-small cell lung cancer .
|
-
- HY-W129441
-
|
N-Ac-4-S-CAP
|
DNA/RNA Synthesis
Tyrosinase
Thymidylate Synthase
|
Others
|
|
N-Acetyl-4-S-mercaptoaminophenol (N-Ac-4-S-CAP) is a compound that is selectively cytotoxic to melanocytes of black mouse hair follicles. It can cause 98% depigmentation of black mouse hair follicles. N-Ac-4-S-CAP can produce visible changes in hair follicle melanocytes 4 hours after intraperitoneal injection, including aggregation of melanin granules and nuclear condensation. Electron microscopy observations showed that it caused progressive destruction of melanocytes, including swelling of membranous organelles, nuclear condensation, and cytoplasmic vacuolation, ultimately leading to complete cell necrosis. N-Ac-4-S-CAP has a specific cytotoxic effect on melanocytes that actively produce eumelanin, but may not affect precursor or dormant melanocytes. These properties suggest that N-Ac-4-S-CAP may have potential application value in the treatment of melanoma or skin whitening.
|
-
- HY-P99159
-
|
|
Interleukin Related
|
Cancer
|
|
Ivuxolimab is a fully human IgG2 agonist targeting OX40 (CD134), which selectively binds to the OX40 receptor on the surface of activated CD4 + and CD8 + T cells without inducing antibody-dependent cytotoxicity. Ivuxolimab can promote T cell proliferation, survival and cytokine (such as IFN-γ, IL-2) secretion, inhibit regulatory T cell function, and enhance anti-tumor immune response. Ivuxolimab can be used in the study of melanoma, hepatocellular carcinoma, head and neck squamous cell carcinoma, etc .
|
-
- HY-13561
-
|
M475271
|
Src
Apoptosis
|
Cancer
|
|
AZM475271 (M475271) is an orally active and selective Src kinase inhibitor. AZM475271 inhibits phosphorylation of c-Src kinase, Lck, c-yes (IC50s = 0.01, 0.03, 0.08 μM, respectively). AZM475271 induces apoptosis. AZM475271 reduces tumor cell proliferation and migration in vitro and in vivo, and reduces microvessel density (MVD). AZM475271 inhibits tumor growth and metastasis. AZM475271 sensitizes tumor cells to the cytotoxic effects of Gemcitabine (HY-17026) .
|
-
- HY-183767
-
-
- HY-401209
-
|
|
α-synuclein
DNA/RNA Synthesis
|
Neurological Disease
|
|
Synucleozid-2.0 is a blood-brain barrier-permeable inhibitor that binds to the IRE of SNCA mRNA, with a EC50 of 2.9 µM and a Kd value of 1.8 µM. Synucleozid-2.0 selectively binds to and stabilizes the A bulge and adjacent closed base pairs in the 5' UTR IRE of SNCA mRNA, blocks the translation process and reduces intracellular levels of α-synuclein. Synucleozid-2.0 exerts cytoprotective effects against cytotoxicity induced by α-synuclein preformed fibrils. Synucleozid-2.0 is applicable to the research of Parkinson's disease .
|
-
- HY-147717
-
|
|
CDK
|
Cancer
|
|
CDK8-IN-7 (compound 12) is a potent and selective cyclin-dependent kinase 8 (CDK8) inhibitor with an Kd of 3.5 nM. CDK8-IN-7 shows cytotoxicity for MOLM-13, OCI-AML3, MV4-11, NRK and H9c2 cells with IC50s of 5.9, 4.8, 5.4, 16.2, 12.5-25 µM, respectively. CDK8-IN-7 has the potential for the research of AML-cancer .
|
-
- HY-100155
-
|
|
Sigma Receptor
Apoptosis
Autophagy
|
Cancer
|
|
4-IBP is a selective σ₁ receptor agonist with high affinity for the σ₁ receptor (Ki =1.7 nM) and moderate affinity for the σ₂ receptor (Ki = 25.2 nM). 4-IBP can make cancer cells more sensitive to the cytotoxic effects of pro-apoptotic and pro-autophagic compounds. 4-IBP significantly reduces the migration ability of a variety of cancer cells. 4-IBP is mainly used in glioblastoma, non-small cell lung cancer and prostate cancer research .
|
-
- HY-174444
-
|
|
PROTACs
HDAC
|
Cancer
|
|
PROTAC HDAC degrader-2 is a selective IIb HDACs PROTAC degrader, with DC50s of 13 nM for HDAC6, 29 nM for HDAC10, respectively. PROTAC HDAC degrader-2 exhibits low cytotoxicity against hematological and solid cancer cell lines. PROTAC HDAC degrader-2 can be used for the chemical knockdown of class IIb HDACs. ( Pink: HDAC ligand : (HY-174471), Blue: E3 ligase CRBN Ligand (HY-131717), E3 ligase ligand-linker conjugate (HY-174473)) .
|
-
- HY-181044
-
|
|
Lipoxygenase
COX
|
Inflammation/Immunology
Cancer
|
|
COX-2/5-LOX-IN-6 (Compound 4c) is a potent and selective 5-LOX (IC50 = 0.10 μM) and COX-2 (IC50: 2.88 μM) inhibitor. COX-2/5-LOX-IN-6 displays potent anticancer activity against ovarian cancer. COX-2/5-LOX-IN-6 would not cause cytotoxic effects in noncancerous cells. COX-2/5-LOX-IN-6 is a potential anti-inflammatory agent .
|
-
- HY-157569
-
|
|
PD-1/PD-L1
|
Cancer
|
|
PD1-PDL1-IN 2 (ZE132) is a potent and selective PD-1/PD-L1 inhibitor, which has robust anti-tumour activity in vivo. PD1-PDL1-IN 2 promotes cytotoxic T-cell tumour infiltration and induces IL-2 expression. In addition, PD1-PDL1-IN 2 elicits strong inhibitory effects on the mRNA expression of TGF-β .
|
-
- HY-183670
-
|
|
JAK
STAT
Apoptosis
|
Infection
Cancer
|
|
JAK2-IN-21 is a Janus kinase 2 (JAK2) inhibitor with an IC50 of 12.25 nM. JAK2-IN-21 inhibits the JAK2/STAT3/STAT5 tumor-promoting signaling pathway and reduces JAK2 protein expression. JAK2-IN-21 exhibits selective cytotoxicity against HPV-positive cancer cells and induces cancer cell apoptosis. JAK2-IN-21 can be used in the research of HPV-positive cervical cancer .
|
-
- HY-178372
-
|
|
Glutathione S-transferase
|
Inflammation/Immunology
Cancer
|
|
GSTO1-IN-4 is a selective, potent GSTO1-1 inhibitor (IC50 = 0.04 μM; KI = 0.16 μM). GSTO1-IN-4 shows low inhibition to GSTO2-2, GSTA1-1 and GSTP1-1. GSTO1-IN-4 shows a capacity to attenuate inflammation in mice and to significantly enhance the cytotoxicity of Cisplatin (HY-17394). GSTO1-IN-4 can be used for the study of inflammation and breast cancer .
|
-
- HY-150772
-
|
|
Microtubule/Tubulin
HDAC
Apoptosis
Mitochondrial Metabolism
|
Cancer
|
|
Tubulin/HDAC-IN-1 is a dual tubulin and HDAC-IN-1 inhibitor through CH/π interaction with tubulin and hydrogen bond interaction with HDAC8. Tubulin/HDAC-IN-1 inhibits tubulin polymerization and selectively inhibits HDAC8 (IC50: 150 nM). Tubulin/HDAC-IN-1 has cytotoxicity against various human cancer cells, also arrests cell cycle in the G2/M phase and induces cell apoptosis. Tubulin/HDAC-IN-1 can be used in the research of hematologic and solid tumors such as neuroblastoma, leukemia .
|
-
- HY-179032
-
|
|
VEGFR
PI3K
Akt
mTOR
Apoptosis
|
Cancer
|
|
VEGFR-2-IN-77 (Compound 10) is a VEGFR-2 inhibitor with an IC50 value of 139 nM. VEGFR-2-IN-77 inhibits the PI3K/AKT/mTOR pathway. VEGFR-2-IN-77 exhibits selective cytotoxicity, being particularly sensitive to leukemia and prostate cancer cells. VEGFR-2-IN-77 causes cell cycle arrest and apoptosis, inhibiting cell migration and invasion. VEGFR-2-IN-77 can be used for the study of leukemia and prostate cancer.
|
-
- 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-186140
-
|
|
SHP1
Phospholipase
ERK
Interleukin Related
|
Inflammation/Immunology
Cancer
|
|
SHP1‑IN‑2 is a selective and orally active SHP1 inhibitor. SHP1‑IN‑2 covalently binds to Cys480 of SHP1. SHP1‑IN‑2 elicits potent antitumor immunity and suppresses syngeneic tumor growth. SHP1‑IN‑2 blocks tumor progression in a svngeneic cancer model by
activating natural killer cells and cytotoxic CD8 ＋ T cells, along with reduced T cel
l. SHP1‑IN‑2 can be used for cancer‑related research .
|
-
- HY-N3434
-
|
|
Drug Derivative
Reactive Oxygen Species (ROS)
|
Cancer
|
|
Kaempferol 3,7,4'-trimethyl ether is an O-methylated kaempferol flavonol aglycone distributed in Siparuna gigantotepala, Aframomum arundinaceum and Siparuna guianensis. Kaempferol 3,7,4'-trimethyl ether exhibits antioxidant activity. Kaempferol 3,7,4'-trimethyl ether suppresses the proliferation of leukemia cells and exerts selective cytotoxicity against both drug‑sensitive and multi‑factorial drug‑resistant cancer cells. Kaempferol 3,7,4'-trimethyl ether can be applied in the research of multidrug‑resistant cancers .
|
-
- HY-170366
-
|
|
VEGFR
Apoptosis
|
Cancer
|
|
VEGFR-2-IN-58 (Compound 7b) inhibits VEGFR-2 with an IC50 of 42.5 nM. VEGFR-2-IN-58 displays selective cytotoxicity against cancer cells. VEGFR-2-IN-58 shows cellular growth arrest at the G2/M phase in cancer cells. VEGFR-2-IN-58 induces cancer cells Apoptosis, increasing BAX expression and reducing Bcl2 expression. VEGFR-2-IN-58 inhibits wound closure in cancer cells .
|
-
- HY-178775
-
|
|
PI4K
Parasite
MAP4K
PI3K
|
Infection
|
|
PI4K-IN-3 (Compound 27) is an orally active PI4K inhibitor with an IC50 of 1.9 nM for Plasmodium vivax PI4K. PI4K-IN-3 has no hERG channel inhibition and mammalian cytotoxicity. PI4K-IN-3 has significant selectivity against the human MINK1 and MAP4K4 kinases but with low selectivity against human PI3Kα and PI4Kβ. PI4K-IN-3 has potent antimalarial activity and significantly reduces parasitaemia in NSG mice mouse models of Plasmodium falciparum malaria .
|
-
- HY-124084A
-
|
|
Stearoyl-CoA Desaturase (SCD)
|
Cancer
|
|
SW203668 TFA is an irreversible stearoyl CoA desaturase (SCD) inhibitor with an IC50 of 54 nM. SW203668 TFA covalently binds and inhibits SCD, depletes unsaturated fatty acids, and triggers cell death in sensitive cells. SW203668 TFA requires demethylation by CYP4F11 to form its active SCD-inhibiting form; differential CYP4F11 expression drives selective cytotoxicity. SW203668 TFA exerts cytotoxicity toward CYP4F11-expressing non-small cell lung cancer (NSCLC) cells and spares CYP4F11-lacking NSCLC cells. SW203668 TFA inhibits tumor growth in immunodeficient mice bearing CYP4F11-expressing NSCLC xenografts and spares mouse skin sebocytes. SW203668 TFA can be used for the research of non-small cell lung cancer .
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- HY-185426
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SC-011
|
Antibody-Drug Conjugates (ADCs)
|
Cancer
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ABBV-011 (SC-011) is a SEZ6-targeted, antibody-drug conjugate (ADC). ABBV-011 binds cell surface-expressed SEZ6 by anti-SEZ6 antibody Turmetabart (HY-P991041), triggers ADC-receptor complex internalization into lysosomes, releases Calicheamicin (HY-19609) payload, and mediates cytotoxicity. ABBV-011 induces tumor regression and mediates selective killing of SEZ6-positive cells. ABBV-011 can be used for the research of small cell lung cancer .
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- HY-173488
-
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NF-κB
HIF/HIF Prolyl-Hydroxylase
Keap1-Nrf2
|
Cancer
|
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NF-κB/HIF-1α-IN-1 (compound 9c) is a potent blocker of the NF-κB activation pathway and demonstrates selective anti-fibrotic activity. NF-κB/HIF-1α-IN-1 shows no significant cytotoxicity in NCI tumor cell lines. In rat models. NF-κB/HIF-1α-IN-1 has been shown to effectively ameliorate liver fibrosis by inhibiting the expression levels of NF-κB and HIF-1α, while simultaneously inducing the activation of Nrf2 .
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- HY-402805
-
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DYRK
CDK
Tau Protein
|
Cancer
|
|
DYRK2-IN-2 (Compound C17) is a selective inhibitor of DYRK2, with its IC50 value being 40.3 nM. The inhibitory activity of DYRK2-IN-2 on DYRK1A (IC50 = 1842 nM), DYRK1B (IC50 = 1335 nM), DYRK4 (IC50 = 1931 nM), DYRK3 (IC50 = 112 nM), and CLKs (IC50 = 540-6496 NM) is relatively low. DYRK2-IN-2 inhibits the phosphorylation of Tau protein at Thr212 and shows moderate cytotoxicity in HT22 cells. DYRK2-IN-2 can be used in cancer research .
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- HY-162562
-
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PCSK9
|
Metabolic Disease
Inflammation/Immunology
|
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E28362 is an orally active lipid-lowering agent and a selective PCSK9 antagonist. E28362 blocks the interaction between PCSK9 and LDLR, and induces PCSK9 degradation via the ubiquitin-proteasome pathway. E28362 significantly increases the levels of cell surface and total LDLR proteins, enhances low-density lipoprotein uptake, thereby effectively reducing plasma lipids, hepatic cholesterol and triglyceride levels. E28362 shows no obvious cytotoxicity at high concentrations, and significantly attenuates atherosclerotic lesions in animal models. E28362 is an important molecule in research of hyperlipidemia and atherosclerosis .
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- HY-183941
-
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PAK
|
Cancer
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SPU-106 is a p21 activated kinase 4 (PAK4) inhibitor with a target IC50 of 21.36 μM. SPU-106 selectively binds to the C-terminal kinase domain of PAK4 to inhibit its kinase activity. SPU-106 inhibits the PAK4/LIMK1/cofilin and PAK4/SCG10 signaling pathways. SPU-106 inhibits invasion of gastric cancer cells and lacks cytotoxicity against cancer cells. SPU-106 can be used for the research of gastric cancer .
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- HY-110374
-
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Epigenetic Reader Domain
Apoptosis
|
Cancer
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NVS-CECR2-1, a non-BET family Bromodomain (BRD) inhibitor, is a potent and selective cat eye syndrome chromosome region, candidate 2 (CECR2) inhibitor. NVS-CECR2-1 binds to CECR2 BRD with high affinity (IC50=47 nM; KD=80 nM). NVS-CECR2-1 exhibits cytotoxic activity and induces apoptosis against various cancer cells by targeting CECR2 as well as via CECR2-independent mechanism . NVS-CECR2-1 is a chemical probe.
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- HY-18957C
-
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BGB-283 hydrochloride
|
Endogenous Metabolite
|
Cancer
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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 .
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- HY-180781
-
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ADAMTS
|
Inflammation/Immunology
Cancer
|
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ADAMTS-5-IN-4 (Compound 4b) is a selective ADAMTS5 inhibitor with an IC₅₀ of 9.4 μM. ADAMTS-5-IN-4 significantly inhibits the degradation of Aggrecan in the implants of the osteoarthritis model. ADAMTS-5-IN-4 effectively inhibits the pseudopod elongation and directional migration of ovarian cancer cells. ADAMTS-5-IN-4 shows significant cytotoxicity to HEK293T cells, human chondrocytes, and porcine chondrocyte implants. ADAMTS-5-IN-4 can be used for the study of osteoarthritis and ovarian cancer .
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- HY-178479
-
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Indoleamine 2,3-Dioxygenase (IDO)
Cytochrome P450
|
Inflammation/Immunology
Cancer
|
|
IDO1-IN-30 (Compound (R)-100) is a potent and highly selective IDO1 inhibitor. IDO1-IN-30 has an IC50 of 4.8 nM to IDO1 in SKOV3 cells. IDO1-IN-30 does not show significant cytotoxicity at 25 µM in HepG2 cells. IDO1-IN-30 can eliminate inhibition of CYP450 enzymes (such as 3A4, 2C9, 2D6). IDO1-IN-30 can be used for research on cancer and inflammatory conditions .
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- HY-177345
-
|
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Sigma Receptor
Apoptosis
Caspase
|
Cancer
|
|
SV119 is a selective sigma-2 (σ₂) receptor ligand (Ki ≈ 5-10 nM). SV119 induces apoptosis in various human cancer cell lines by activating caspase-3 and promoting mitochondrial depolarization. SV119 can enhance the effects of chemotherapeutic agents such as Paclitaxel (HY-B0015), increasing their cytotoxicity against tumor cells. SV119 significantly inhibits tumor growth in mouse xenograft models, both alone and in combination. SV119 is useful in the research of cancers such as breast, prostate, and pancreatic cancer .
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- HY-181419
-
|
|
Bacterial
|
Infection
|
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Antimycobacterial agent-16 is a pyrazinamide derivative and antimycobacterial agent with a selectivity index >25 against HepG2 cells.Antimycobacterial agent-16 does not undergo hydrolysis by mycobacterial pyrazinamidase.Antimycobacterial agent-16 exerts activity against Mycobacterium tuberculosis H37Rv, multidrug-resistant Mycobacterium tuberculosis strains, and Mycobacterium kansasii.Antimycobacterial agent-16 shows no inhibitory activity against mycobacterial enoyl-ACP reductase (InhA).Antimycobacterial agent-16 has low cytotoxicity against HepG2 cells.Antimycobacterial agent-16 can be used for the research of tuberculosis .
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- HY-157936
-
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iGluR
|
Neurological Disease
|
|
GluN2B-NMDAR antagonist-2 (compound S-58) is a potent, selective and cross the blood-brain barrier NMDAR-GluN2B antagonist with an IC50 value of 74.01, nM. GluN2B-NMDAR antagonist-2 shows mild cytotoxicity. GluN2B-NMDAR antagonist-2 decreases the cerebral infarction rates and neurologic deficit scores. GluN2B-NMDAR antagonist-2 has the potential for the research of stroke .
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- HY-P5446
-
|
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Bacterial
|
Others
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BMAP-18 is a biological active peptide. (BMAP-18 is a truncated form of the antimicrobial peptide BMAP-27. Bovine myeloid antimicrobial peptide-27 (BMAP-27) belongs to the Cathelicidin family of peptides which displays rapid bactericidal activity against Staphylococcus aureus, Streptococcus uberis, and Escherichia coli. BMAP-27 is cytotoxic to human erythrocytes and neutrophils, although at higher than microbicidal concentrations. BMAP-18 displays much higher cell selectivity as compared to parental BMAP-27 because of its decreased hemolytic activity and retained antimicrobial activity.)
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- HY-163783
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Casein Kinase
|
Infection
|
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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 .
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- HY-133135
-
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CHIKV
Nucleoside Antimetabolite/Analog
|
Infection
|
CHIKV-IN-1 (Compound 3a) is a compound that inhibits the Chikungunya virus (CHIKV) with an EC50 of 0.12 μM. CHIKV-IN-1 is a potent inhibitor of the S-adenosyl-L-homocysteine hydrolase (SAH hydrolase), with an IC50 of 0.36 μM. CHIKV-IN-1 is only effective against CHIKV and some other alphaviruses, but has no activity against other RNA viruses such as SARS-CoV, MERS-CoV, and ZIKV. CHIKV-IN-1 has extremely low cytotoxicity (CC₅₀ > 250 μM), and it has an extremely high selectivity index (SI > 2083). CHIKV-IN-1 can be used in research on anti-Chikungunya virus .
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- HY-N13838
-
|
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Bacterial
|
Infection
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8,9-Dehydro-7,9-diisobutyryloxythymol is a Thymol (HY-N6810) derivative, as well as an antibacterial agent. 8,9-Dehydro-7,9-diisobutyryloxythymol can be found in the aerial parts of Ageratina adenophora, with selective activity against Gram-positive bacterial strains including Bacillus cereus. 8,9-Dehydro-7,9-diisobutyryloxythymol does not exhibit detectable in vitro cytotoxic activity against human cancer cell lines. 8,9-Dehydro-7,9-diisobutyryloxythymol can be used for the research of bacterial infection .
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- HY-182800
-
|
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Molecular Glues
Casein Kinase
|
Cancer
|
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IBA-11 is a selective CRBN-dependented CK1α molecular glue degrader. IBA-11 binds to the canonical tri-tryptophan pocket of CRBN, forming a ternary complex with CK1α to mediate its degradation. IBA-11 induces CRBN-dependent ubiquitin-proteasome system-mediated degradation of CK1α. IBA-11 exhibits cytotoxicity against cancer cells. IBA-11 demonstrates in vitro metabolic stability in rat liver microsomes and minimal hERG inhibition. IBA-11 can be used for the research of cancer, such as acute myeloid leukemia .
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- HY-149230
-
|
|
Deubiquitinase
|
Cancer
|
|
USP28-IN-4 is a USP28 inhibitor (IC50=0.04 μM) with high selectivity over USP2, USP7, USP8, USP9x, UCHL3 and UCHL5. USP28-IN-4 shows cytotoxicity against cancer cells, down-regulates the cellular level of c-Myc through ubiquitin-proteasome system. USP28-IN-4 also decreases the ankyrase-1/2 level in vitro. USP28-IN-4 enhance the sensitivity of colorectal cancer cells to Regorafenib (HY-10331) .
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- HY-142118A
-
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AP 12009 sodium
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TGF-beta/Smad
|
Cancer
|
|
Trabedersen (AP 12009) sodium is an orally active synthetic antisense phosphorothioate oligodeoxynucleotide that selectively targets human TGFβ2 mRNA. Trabedersen sodium blocks TGFβ2 protein production, enters the nucleus without a transfection vector, and exerts dose-dependent antitumor effects. By reversing TGFβ2-induced immunosuppression and enhancing immune cytotoxicity, Trabedersen sodium exhibits significant antiproliferative, antimigratory, and antimetastatic activities, with favorable safety profiles. Trabedersen sodium is widely used in research related to various solid tumors, including anaplastic astrocytoma, glioblastoma, colorectal tumor, and melanoma .
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- HY-12759
-
|
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Histone Methyltransferase
|
Cancer
|
|
CARM1-IN-1 (compound 7g) is a highly potent and selective inhibitor of CARM1 (IC50=8.6 μM, CARM1/PABP1), with low inhibitory activity against PRMT1 and SET7 (IC50 >667 μM). CARM1-IN-1 inhibits the methylation activity of CARM1 and the methylation levels of different substrates, such as PABP1, CA150, SmB, and H3. CARM1-IN-1 also inhibits the promoter activity of prostate-specific antigen (PSA) without significant cytotoxicity .
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- HY-149229
-
|
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Deubiquitinase
|
Cancer
|
|
USP28-IN-3 is a USP28 inhibitor (IC50=0.1 μM) with high selectivity over USP2, USP7, USP8, USP9x, UCHL3 and UCHL5. USP28-IN-3 shows cytotoxicity against cancer cells, down-regulates the cellular level of c-Myc through ubiquitin-proteasome system. USP28-IN-3 also decreases the ankyrase-1/2 level in vitro. USP28-IN-3 enhance the sensitivity of colorectal cancer cells to Regorafenib (HY-10331) .
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- HY-169830
-
|
|
Drug Derivative
Apoptosis
|
Cancer
|
|
2-(Cyclohexylmethyl)-plumbagin is a derivative of the naphthoquinone compound Plumbagin (HY-N1497). Under nutrient-deprived conditions, 2-(Cyclohexylmethyl)-plumbagin selectively exhibits cytotoxicity against PANC-1 human pancreatic cancer cells (PC50 = 0.11 µM) and reduces the phosphorylation of Akt and mTOR in PANC-1 cells. 2-(Cyclohexylmethyl)-plumbagin also induces apoptosis (Apoptosis) in PANC-1 cells at a concentration of 1 µM. Additionally, 2-(Cyclohexylmethyl)-plumbagin reduces tumor volume and weight in a xenograft MiaPaCa-2 pancreatic cancer mouse model .
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- HY-12759A
-
|
|
Histone Methyltransferase
|
Cancer
|
|
CARM1-IN-1 (compound 7g) hydrochloride is a highly potent and selective inhibitor of CARM1 (IC50=8.6 μM, CARM1/PABP1), with low inhibitory activity against PRMT1 and SET7 (IC50 >667 μM). CARM1-IN-1 hydrochloride inhibits the methylation activity of CARM1 and the methylation levels of different substrates, such as PABP1, CA150, SmB, and H3. CARM1-IN-1 hydrochloride also inhibits the promoter activity of prostate-specific antigen (PSA) without significant cytotoxicity .
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- HY-149228
-
|
|
Deubiquitinase
|
Cancer
|
|
USP28-IN-2 is a USP28 inhibitor (IC50=0.3 μM) with high selectivity over USP2, USP7, USP8, USP9x, UCHL3 and UCHL5. USP28-IN-2 shows cytotoxicity against cancer cells, down-regulates the cellular level of c-Myc through ubiquitin-proteasome system. USP28-IN-2 also decreases the ankyrase-1/2 level in vitro. USP28-IN-2 enhance the sensitivity of colorectal cancer cells to Regorafenib (HY-10331) .
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- HY-142118
-
|
AP 12009
|
TGF-beta/Smad
|
Cancer
|
|
Trabedersen (AP 12009) is an orally active synthetic antisense phosphorothioate oligodeoxynucleotide that selectively targets human TGFβ2 mRNA. Trabedersen blocks TGFβ2 protein production, enters the nucleus without a transfection vector, and exerts dose-dependent antitumor effects. By reversing TGFβ2-induced immunosuppression and enhancing immune cytotoxicity, Trabedersen exhibits significant antiproliferative, antimigratory, and antimetastatic activities, with favorable safety profiles. Trabedersen is widely used in research related to various solid tumors, including anaplastic astrocytoma, glioblastoma, colorectal tumor, and melanoma .
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- HY-121382R
-
|
|
Reference Standards
Apoptosis
Cholinesterase (ChE)
Necroptosis
|
Cardiovascular Disease
|
|
Cinosulfuron (Standard) is the analytical standard of Cinosulfuron. This product is intended for research and analytical applications. Gypsogenin is a selective mixed-type BChE inhibitor (Ki=19.99 μM) that also exhibits significant cytotoxicity against various human cancer cell lines. Gypsogenin inhibits tumor growth by inducing cell cycle arrest and triggering apoptosis. Gypsogenin displays antibacterial activity against bacteria such as Bacillus subtilis and Bacillus thuringiensis, and often serves as a key parent nucleus for the synthesis of anticancer compounds. Gypsogenin is widely used in research on Alzheimer's disease and various cancers including colon cancer, melanoma, and leukemia .
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-
- HY-P11757
-
|
|
EGFR
|
Cancer
|
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Cyclo[K(N3)larllt] is a seven-membered cyclic peptide targeting EGFR, with a Kd value of 5.09 μM, and exhibits binding selectivity toward homologous proteins HER2 and HER3. Cyclo[K(N3)larllt] has no cytotoxicity and shows no growth inhibitory effect on cancer cells overexpressing EGFR. Cyclo[K(N3)larllt] can serve as a ligand for EGFR-targeted fluorescent conjugates, which is applicable to the detection of cancers with EGFR overexpression. Cyclo[K(N3)larllt] can be used in the research of colorectal cancer .
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![Cyclo[K(N3)larllt]](//file.medchemexpress.com/product_pic/hy-p11757.gif)
- HY-D1244
-
|
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Fluorescent Dye
|
Cardiovascular Disease
Inflammation/Immunology
|
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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-174444A
-
|
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PROTACs
HDAC
|
Cancer
|
|
PROTAC HDAC degrader-2 TFA is the trifluoroacetate salt of PROTAC HDAC degrader-2. PROTAC HDAC degrader-2 is a selective IIb HDACs PROTAC degrader, with DC50s of 13 nM for HDAC6, 29 nM for HDAC10, respectively. PROTAC HDAC degrader-2 exhibits low cytotoxicity against hematological and solid cancer cell lines. PROTAC HDAC degrader-2 can be used for the chemical knockdown of class IIb HDACs. ( Pink: HDAC ligand : (HY-174471), Blue: E3 ligase CRBN Ligand (HY-131717), E3 ligase ligand-linker conjugate (HY-174473)) .
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- HY-103241
-
|
|
Amyloid-β
ATM/ATR
Phosphatase
Apoptosis
|
Neurological Disease
Cancer
|
|
Ro 90-7501 is an amyloid β42 (Aβ42) fibril assembly inhibitor that reduces Aβ42-induced cytotoxicity (EC50 of 2 μM). Ro 90-7501 inhibits ATM phosphorylation and DNA repair. RO 90-7501 selectively enhances toll-like receptor 3 (TLR3) and RIG-I-like receptor (RLR) ligand-induced IFN-β gene expression and antiviral response . Ro 90-7501 also inhibits protein phosphatase 5 (PP5) in a TPR-dependent manner . Ro 90-7501 has significant radiosensitizing effects on cervical cancer cells .
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- HY-181588
-
|
|
Nuclear Hormone Receptor 4A/NR4A
|
Neurological Disease
Inflammation/Immunology
|
|
NR4A agonist-2 is a selective pan-NR4A agonist designed based on Vidofludimus (HY-14908), with a Kd of 0.10 μM against NR4A1, and EC50 values of 0.098 μM, 0.092 μM and 0.09 μM against Nur77, Nurr1, NOR-1, respectively. NR4A agonist-2 exhibits 47-fold selectivity over DHODH, and shows no cytotoxic activity at concentrations up to 10 μM. By binding to a specific surface pocket in the ligand-binding domain of Nurr1, NR4A agonist-2 inhibits the formation of Nurr1 homodimers, activates response elements such as NBRE, NurRE, DR5, and then potently induces the expression of neuroprotective genes including BDNF, SOD2, thereby exerting neuroprotective activity. NR4A agonist-2 can be used in the research of neurodegenerative diseases such as Parkinson's disease, dementia and multiple sclerosis .
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- HY-179535
-
|
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TAM Receptor
Discoidin Domain Receptor
TGF-β Receptor
Hedgehog
|
Cancer
|
|
Axl-IN-21 is an orally active and selective AXL inhibitor (Kd = 2.7 nM, IC50 = 4.0 nM). Axl-IN-21 displays kinase selectivity and retains strong activity against cancer-related mul-kinases (Mer with Kd = 1.4 nM, DDR1 with IC50 = 22.2 nM, HIPK4 with Kd = 11.0 nM and LOK with Kd =10 nM). Axl-IN-21 overcomes tumor microenvironment-driven resistance by blocking CAF-derived GAS6-induced AXL/STAT3/ABCG1 signaling, restoring chemosensitivity and inhibiting drug efflux in gastric cancer (GC). Axl-IN-21 suppresses TGF-β1-induced epithelial-mesenchymal transition (EMT), migration, and invasion in MDA-MB-231 cells. Axl-IN-21 exhibits no significant cytotoxicity in non-cancerous cells. Axl-IN-21 can be research for triple negative breast cancer and gastric cancer [1] [2] .
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- HY-P99144A
-
|
|
PD-1/PD-L1
|
Inflammation/Immunology
Cancer
|
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Anti-Mouse PD-1 Antibody (S-5001) is a selective inhibitor targeting PD-1, blocking the PD-1/PD-L1 immune checkpoint axis through competitive binding to PD-1. Anti-Mouse PD-1 Antibody (S-5001) works by reversing the tumor immunosuppressive microenvironment and reactivating the anti-tumor activity of cytotoxic T lymphocytes. It can be used in research on tumors such as melanoma and HPV-positive oropharyngeal squamous cell carcinoma. Anti-Mouse PD-1 Antibody (S-5001) is often combined with photothermal therapy, chemotherapy, etc., to enhance efficacy .
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-
- HY-160696
-
|
|
CD73
|
Cancer
|
|
ORIC-533 is an orally active, highly selective, AMP-competitive CD73 inhibitor that potently blocks adenosine production with sub-nanomolar affinity (Ka=0.03 nM). In multiple myeloma, ORIC-533 restores and enhances the cytotoxicity of the immune system against tumor cells through multiple immunological mechanisms, including reversing the immunosuppressive microenvironment, inducing immunogenic cell death, and activating dendritic cells, T cells and NK cells, with no direct toxicity to normal cells. The combination of ORIC-533 with Daratumumab (HY-P9915) synergistically enhances anti-tumor efficacy, significantly increases intratumoral CD8 + T cell infiltration and inhibits tumor growth in vivo .
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-
- HY-183317
-
|
|
Indoleamine 2,3-Dioxygenase (IDO)
Interleukin Related
Apoptosis
Caspase
PARP
|
Cancer
|
|
IDO1-IN-34 is a selective IDO1 inhibitor with an IC50 of 0.093 μM. IDO1-IN-34 exhibits cytotoxicity against various cancer cell lines. IDO1-IN-34 inhibits the kynurenine (kynurenine) pathway and activates IL-2. IDO1-IN-34 induces cell apoptosis via the endogenous mitochondrial pathway, while increasing the levels of cytochrome c, caspase-3, caspase-9 and PARP-1. IDO1-IN-34 can be used for research on liver cancer, lung cancer, breast cancer, prostate cancer, colon cancer and leukemia .
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-
- HY-182302
-
|
|
Drug Derivative
HSP
|
Cancer
|
|
SMTIN-P01 is a TRAP1 inhibitor that is selective for cytosolic Hsp90 and accumulates in mitochondria. SMTIN-P01 binds to the ATP-binding site of TRAP1 as an ATP mimic, thereby inhibiting ATPase and foldase activities. SMTIN-P01 induces mitochondrial membrane depolarization and proteolytic degradation in cancer cells. SMTIN-P01 exhibits significant cytotoxicity, but shows extremely low toxicity to primary mouse hepatocytes, and does not interfere with SIRT3-related functions or the levels of cytosolic Hsp90 substrates. SMTIN-P01 has important application value in cancer-related research .
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-
- HY-W010451
-
|
Hydroxyhydroquinone
|
PERK
Eukaryotic Initiation Factor (eIF)
Potassium Channel
Apoptosis
|
Cardiovascular Disease
Cancer
|
|
1,2,4-Trihydroxybenzene (Hydroxyhydroquinone) is an ER stress inducer that targets proteins such as PKR-like ER kinase PERK to induce cytotoxicity. 1,2,4-Trihydroxybenzene selectively activates eIF2α phosphorylation, activates the PERK-eIF2α signaling pathway and induces stress granule formation. 1,2,4-Trihydroxybenzene subsequently exacerbates oxidative stress and causes DNA double-strand breaks, destroying organelles such as mitochondria and ER, and inducing cell death. 1,2,4-Trihydroxybenzene also has the potential to exhibit anti-tumor effect, increase blood pressure, and relieve spasm .
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-
- HY-103322
-
|
|
PKA
Potassium Channel
|
Metabolic Disease
Cancer
|
|
6-Bnz-cAMP sodium, a derivative of cyclic adenosine monophosphate (cAMP), is a selective PKA activator with inhibitory activity against the bTREK-1 K + channel. 6-Bnz-cAMP sodium does not activate the Epac signaling pathway. It inhibits the bTREK-1 K + channel via a voltage-independent, ATP-dependent mechanism that is independent of the PKA/Epac/calmodulin kinase/MAP kinase pathway. 6-Bnz-cAMP sodium activates CREB phosphorylation to regulate osteoblast-specific gene expression, induces osteoblast differentiation, promotes extracellular matrix mineralization, supports osteoblast proliferation, and shows no cytotoxicity toward osteoblasts. It can be used in studies related to bone tissue repair and regeneration .
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-
- HY-179571
-
|
PPTD
|
Reactive Oxygen Species (ROS)
Ferroptosis
|
Cancer
|
|
ZIP 14-IN-1 (PPTD) is a selective and orally active ZIP14 inhibitor. ZIP 14-IN-1 inhibits ZIP14 while sparing ZIP8 (SLC39A8). ZIP 14-IN-1 efficiently blocks ZIP14-mediated uptake of multiple divalent metals (zinc, iron, manganese and cadmium). ZIP 14-IN-1 binds to a pocket formed at the dimer interface of ZIP14, obstructing the metal transport pathway. ZIP 14-IN-1 effectively reverses the consequent elevation of reactive oxygen species (ROS) and lipid peroxidation, attenuating metal-induced cytotoxicity. ZIP 14-IN-1 can be uses for cancer cachexia research .
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-
- HY-182636
-
|
|
Deubiquitinase
Aldehyde Dehydrogenase (ALDH)
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
MT16-001 is a cell-permeable UCHL1 inhibitor with an IC50 value of 580 nM. MT16-001 also exhibits considerable inhibitory activity against USP30, and shows selectivity for other UCH family deubiquitinases (DUBs) as well as the broader proteome. MT16-001 binds covalently to the cysteine residue at the active site of UCHL1, and forms covalent interactions with ALDH2, ALDH9A1 and GATD3A in intact cells. Meanwhile, as a cytotoxic agent, it displays a steep dose-response curve in human embryonic kidney cells. MT16-001 can be used for research on various cancers, liver fibrosis and pulmonary fibrosis .
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-
- HY-178497
-
|
|
PROTACs
Ras
p38 MAPK
TNF Receptor
|
Inflammation/Immunology
Cancer
|
|
ZJK-807 is a highly effective and selective PROTAC degrader targeting KRASG12D (DC50 = 79.5 nM in AsPC-1 cells). ZJK-807 shows minimal impact on wild-type KRAS or other mutants (G12C/S/V, G13D), inducing mutant-specific cytotoxicity. ZJK-807 suppresses RAS/MAPK signaling and uniquely modulates TNF signaling and eukaryotic ribosome biogenesis. ZJK-807 can be used for the study of KRAS-driven pancreatic cancer. Yellow: KRASG12D ligand (HY-W087383); Green: E3 ligase CRBN ligand (HY-178507); Black: Linker (HY-178506) .
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-
- HY-158426
-
2-APQC
1 Publications Verification
|
Sirtuin
|
Cardiovascular Disease
|
|
2-APQC is an orally active and selective agonist of Sirtuin-3 (SIRT3) (Kd=2.756 μM), antagonizes Isoproterenol/ISO (HY-B0468)-induced cytotoxicity. 2-APQC activates the SIRT3-PYCR1 axis to enhance mitochondrial proline metabolism and inhibit the ROS-p38MAPK pathway by inhibiting signaling pathways such as mTOR-p70S6K, JNK, and TGF-β/Smad3. 2-APQC also activates the AMPK-Parkin axis to alleviate myocardial hypertrophy and fibrosis and protect cardiac function. 2-APQC can be used in the study of heart failure .
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- HY-N7183
-
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NF-κB
GSK-3
β-catenin
Wnt
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Cancer
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9-Hydroxycanthin-6-one is a β-carboline alkaloid. 9-Hydroxycanthin-6-one can be isolated from the roots of E. longifolia. 9-Hydroxycanthin-6-one inhibits TNF-α-induced activation of the NF-κB pathway. 9-Hydroxycanthin-6-one activates GSK3β independently of CK1α, drives phosphorylation and degradation of β-catenin, and inhibits the Wnt signaling pathway. 9-Hydroxycanthin-6-one exerts selective cytotoxicity against Wnt-dependent colon cancer cells. 9-Hydroxycanthin-6-one can be used in studies related to colon cancer .
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-
- HY-162386
-
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Cuproptosis
Mitochondrial Metabolism
|
Cancer
|
|
UM4118 is a potent copper-selective non-genotoxic copper ionophore that induces cuproptosis in acute myeloid leukemia cells. UM4118 exhibits stronger activity against SF3B1G12C mutant acute myeloid leukemia cells. UM4118 transports extracellular copper into cells, elevates intracellular and mitochondrial copper levels, and triggers lipoylated DLAT aggregation, proteotoxic stress, iron-sulfur cluster protein depletion, reduced lipoylated protein levels, and maximal mitochondrial respiratory damage. UM4118 cytotoxicity can be enhanced by supplementation with extracellular copper, abolished by copper chelation, and shows synthetic lethal effects in the absence of iron-sulfur cluster biosynthesis/transport genes. UM4118 can be used for the study of acute myeloid leukemia .
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- HY-123599
-
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DNA/RNA Synthesis
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Cancer
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IACS-4619 (compound 4) is a highly selective 2-aminopyrimidine-based MTH1 (MutT homolog 1) inhibitor (IC50=0.2 nM). IACS-4619 inhibits MTH1 by blocking its hydrolysis of oxidized purine nucleotides such as 8-oxo-dGTP, thereby preventing MTH1 from inhibiting the incorporation of oxidized nucleotides into DNA. IACS-4619 significantly inhibits endogenous MTH1 activity in MTH1-overexpressing U2OS cells, but without antiproliferative or cytotoxic effects on various human cancer and normal cell lines. IACS-4619 can be used in oncology research related to the MTH1 target .
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- HY-P992457
-
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Glycoprotein VI
Interleukin Related
|
Cancer
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SAR444200 is a nanobody T-cell engager targeting GPC3 (glypican-3) and TCRαβ (T-cell receptor αβ). SAR444200 has a KD of 0.023 nM for human GPC3 and a KD of 5.2 nM for human TCRαβ. SAR444200 mediates T-cell-dependent cytotoxicity, with high selectivity and killing activity against GPC3-positive tumor cells. SAR444200 binds to GPC3 in a dual-epitope manner, and binds to TCRαβ via its N-terminal nanobody, forming an artificial immunological synapse between T cells and tumor cells. SAR444200 can be used for the research of GPC3 + solid tumors, including liver cancer, lung squamous cell carcinoma and melanoma .
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- HY-100155R
-
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Sigma Receptor
Reference Standards
Apoptosis
Autophagy
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Cancer
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4-IBP (Standard) is the analytical standard of 4-IBP (HY-100155). This product is intended for research and analytical applications. 4-IBP is a selective σ₁ receptor agonist with high affinity for the σ₁ receptor (Ki =1.7 nM) and moderate affinity for the σ₂ receptor (Ki = 25.2 nM). 4-IBP can make cancer cells more sensitive to the cytotoxic effects of pro-apoptotic and pro-autophagic compounds. 4-IBP significantly reduces the migration ability of a variety of cancer cells. 4-IBP is mainly used in glioblastoma, non-small cell lung cancer and prostate cancer research .
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- HY-169921
-
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c-Myc
Apoptosis
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Cancer
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|
c-Myc inhibitor 15 (Compound A5) is a selective c-Myc inhibitor that exerts anticancer effects by disrupting the interaction between c-Myc and Max, leading to the degradation of c-Myc protein and the induction of apoptosis. Its IC50 values are 4.08 μM and 7.86 μM in A549 and NCI-H1299 lung cancer cell lines, respectively, demonstrating strong cytotoxic activity. In a syngeneic tumor model, c-Myc inhibitor 15 exhibited outstanding antitumor efficacy, achieving a tumor growth inhibition rate of 76.4% and significantly reducing c-Myc protein expression levels. c-Myc inhibitor 15 holds promise for research related to c-Myc-driven lung cancers .
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- HY-D3197
-
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Fluorescent Dye
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Inflammation/Immunology
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CDg16 is a selective fluorescent dye targeting SLC18B1 (λabs/λem=458/544 nm) that is actively transported into lysosomal vesicles of activated macrophages independent of the endocytic pathway. CDg16 enables highly specific vesicle localization in live cells. CDg16 exhibits no cytotoxicity and accurately distinguishes activated M1 and M2 subsets from different origins. CDg16 shows low background staining in non-activated cells and normal organs, making it suitable for time-lapse imaging. In preclinical animal models of inflammatory sites, atherosclerotic plaques and liver inflammation, CDg16 allows visualization of activated macrophages. CDg16 can be used to study inflammation-related diseases and atherosclerosis .
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- HY-173522
-
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Kinesin
Microtubule/Tubulin
|
Cancer
|
|
KIF2C-IN-1 is a cell-penetrating, selective KIF2C inhibitor with fluorescent properties (Ex/Em = 410/510 nm). KIF2C-IN-1 exhibits notable cytotoxicity and weak inhibitory effects on KIF2A/B. KIF2C-IN-1 prohibits the dissociation of KIF2C from microtubules. KIF2C-IN-1 inhibiting KIF2C reverses cross-resistance to microtubule-targeting agents. KIF2C-IN-1 reduces tumorigenesis in chemoresistant triple-negative breast cancer (TNBC) model in mice with the combination of Paclitaxel (HY-B0015) .
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-
- HY-171124
-
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AZD9592
|
Antibody-Drug Conjugates (ADCs)
EGFR
c-Met/HGFR
Topoisomerase
DNA/RNA Synthesis
|
Cancer
|
|
Tilatamig samrotecan (AZD9592) is an anti-EGFR/c-MET antibody-drug conjugate (ADC). Tilatamig samrotecan consists of an anti-EGFR/c-MET antibody with the drug-linker conjugate being AZ14170133 (HY-145399) (a topoisomerase I (TOP1i) inhibitor payload). Tilatamig samrotecan induces multiple DNA damage response pathway markers (like ATM, ATR, γH2AX). Tilatamig samrotecan selectively binds to EGFR and c-MET, delivering the cytotoxic payload. Tilatamig samrotecan exerts anti-tumor activity in vivo. Tilatamig samrotecan can be used for non-small cell lung cancer (NSCLC) and head and neck squamous cell carcinoma (HNSCC) research .
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-
- HY-114796
-
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Lipoxygenase
|
Inflammation/Immunology
|
|
tHGA is a compound with anti-inflammatory activity and has the activity to inhibit soybean 15-LOX. tHGA showed significant inhibitory effects in experiments on human leukocytes, with an IC50 value of 0.42 μM, which is close to the effect of commonly used standard NDGA. tHGA concentration-dependently inhibits the synthesis of 5-LOX products, especially the cysteine leukotriene LTC(4), with an IC50 value of 1.80 μM. and showed no cytotoxicity. The anti-inflammatory effects of tHGA do not appear to be through redox or metal chelation mechanisms, as the compound was negative in these bioactivity tests. tHGA works through a dual LOX/COX inhibition mechanism and has higher selectivity for 5-LOX and COX-2, with an IC50 value of 0.40 μM .
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-
- HY-N17778
-
|
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Others
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Cancer
|
|
(2R,3R)-7,3',4'-Trihydroxy-5-methoxy-flavanonol is a flavonoid and a selective inhibitor of human liver cancer cell growth, with an IC50 of 38.6 μg/mL (121.5 μM). (2R,3R)-7,3',4'-Trihydroxy-5-methoxy-flavanonol inhibits cancer cell growth with dose-dependent cytotoxic activity, and its anticancer activity is comparable to that of Cisplatin (HY-17394). (2R,3R)-7,3',4'-Trihydroxy-5-methoxy-flavanonol can be used in research on liver cancer and other types of cancer.
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-
- HY-137381
-
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N6-Benzoyl-cAMP
|
PKA
Potassium Channel
|
Metabolic Disease
|
|
6-Bnz-cAMP, a derivative of cyclic adenosine monophosphate (cAMP), is a selective PKA activator with inhibitory activity against the bTREK-1 K + channel. 6-Bnz-cAMP does not activate the Epac signaling pathway. 6-Bnz-cAMP inhibits the bTREK-1 K + channel via a voltage-independent, ATP-dependent mechanism that is independent of the PKA/Epac/calmodulin kinase/MAP kinase pathway. 6-Bnz-cAMP activates CREB phosphorylation to regulate osteoblast-specific gene expression, induces osteoblast differentiation, promotes extracellular matrix mineralization, supports osteoblast proliferation, and shows no cytotoxicity toward osteoblasts. 6-Bnz-cAMP can be used in studies related to bone tissue repair and regeneration .
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-
- HY-W615446
-
|
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Glutathione S-transferase
Interleukin Related
|
Inflammation/Immunology
Cancer
|
|
GSTO1-IN-3 is a potent GSTO1-1 inhibitor with an IC50 of 0.11 μM, and shows selectivity over GSTO2-2, GSTA1-1 and GSTP1-1 (IC50 > 100 μM). GSTO1-IN-3 enhances the cytotoxicity of Cisplatin (HY-17394) against human breast cancer cells. GSTO1-IN-3 inhibits IL-1β release in mouse bone marrow-derived macrophage (BMDM) cells. GSTO1-IN-3 attenuates inflammation in mice. GSTO1-IN-3 can be used for breast cancer and inflammation research .
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-
- HY-P991944
-
|
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CCR
|
Cancer
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ZL-1218 is a selective humanized IgG1 antibody, targeting CCR8. ZL-1218 induces antibody-dependent cellular cytotoxicity (ADCC), leading to NK cell-mediated depletion of CCR8-expressing regulatory T cells (Tregs). ZL-1218 blocks the binding of the CCR8 ligand CCL1 to CCR8 and reduces Treg recruitment by inhibiting the chemotaxis of CCR8 + cells. ZL-1218 reduces intratumoral Treg levels in a dose-dependent manner. ZL-1218 exerts enhanced antitumor activity when combined with the anti-PD-1 antibody. ZL-1218 can be used for solid tumour research .
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- HY-P10466A
-
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Sec61
SARS-CoV
Interleukin Related
TNF Receptor
IFNAR
|
Infection
Inflammation/Immunology
|
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KZR-8445 TFA, a cyclic depsipeptide, is a client-selective Sec61 inhibitor. KZR-8445 TFA binds to the fully opened Sec61 lateral gate, blocks lumenal plug domain access, stabilizes lateral gate helices, traps select signal peptides, and disrupts secretory and membrane protein biogenesis. KZR-8445 TFA inhibits pro-inflammatory cytokine secretion in primary immune cells. KZR-8445 TFA inhibits SARS-CoV-2 replication, virus-induced cytotoxicity, and spike protein biogenesis. KZR-8445 TFA blocks disease progression in a mouse model of rheumatoid arthritis. KZR-8445 TFA can be used for the researches of rheumatoid arthritis and SARS-CoV-2 infection .
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- HY-P10466
-
|
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Sec61
SARS-CoV
Interleukin Related
TNF Receptor
IFNAR
|
Infection
Inflammation/Immunology
|
|
KZR-8445, a cyclic depsipeptide, is a client-selective Sec61 inhibitor. KZR-8445 binds to the fully opened Sec61 lateral gate, blocks lumenal plug domain access, stabilizes lateral gate helices, traps select signal peptides, and disrupts secretory and membrane protein biogenesis. KZR-8445 inhibits pro-inflammatory cytokine secretion in primary immune cells. KZR-8445 inhibits SARS-CoV-2 replication, virus-induced cytotoxicity, and spike protein biogenesis. KZR-8445 blocks disease progression in a mouse model of rheumatoid arthritis. KZR-8445 can be used for the researches of rheumatoid arthritis and SARS-CoV-2 infection .
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- HY-169920
-
|
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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) .
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-
- HY-P992448
-
|
|
PD-1/PD-L1
|
Cancer
|
|
RC98 is a monoclonal antibody targeting programmed cell death ligand 1 (PD-L1) and acts as a selective PD-L1 inhibitor. RC98 binds specifically to human and cynomolgus monkey PD-L1. RC98 blocks the interaction between PD-L1 and its receptor PD-1 to reverse T-cell inactivation mediated by PD-1/PD-L1 signaling. RC98 enhances the cytotoxic T-lymphocyte-mediated anti-tumor immune response against PD-L1-expressing tumor cells. RC98 can be used for the research of tumor immunity and solid tumors .
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-
- HY-179507
-
|
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MDM-2/p53
Apoptosis
|
Cancer
|
|
p53 Activator 17 is a p53-Y220C activator. p53 Activator 17 exhibits selective cytotoxicity and pro-apoptotic activity in p53-Y220C mutant cancer cell lines, with minimal effects in wild-type or p53-null cells. p53 Activator 17 induces a mutant-to-wild-type conformational shift in cellular p53-Y220C, accompanied by transcriptional activation of canonical p53 target genes, including BBC3 (PUMA) and MDM2. p53 Activator 17 can be used for the study of hepatocellular carcinoma and breast cancer .
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- HY-D3190
-
|
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Fluorescent Dye
Apoptosis
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Inflammation/Immunology
|
|
BODIPY-DOX is a conjugate composed of BODIPY and Doxorubicin (HY-15142A), as well as a pH-activated fluorescent probe for M1 macrophages and an apoptosis inducer. BODIPY-DOX undergoes pH-induced hydrazone bond cleavage in acidic M1 macrophage phagosomes, thereby releasing cytotoxic Doxorubicin (Dox) and inhibiting the function of pro-inflammatory M1 macrophages. BODIPY-DOX highly selectively inhibits the production of relevant pro-inflammatory cytokines by mouse and human monocyte-derived M1 macrophages, while exerting minimal effects on M2 or unactivated macrophages. Therefore, BODIPY-DOX enables simultaneous fluorescent tracing, differentiation and elimination of specific macrophage subsets, and exhibits the potential to regulate tissue regeneration in zebrafish models .
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- HY-174374
-
|
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Topoisomerase
|
Cardiovascular Disease
|
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Topobexin is a TOP2B-selective inhibitor with IC50 values of 0.19 μM and 4.8 μM for TOP2B and TOP2A (DNA decatenation assay). Topobexin binds to non-homologous residues in the obex pocket and targets the ATPase domain of TOP2B. Topobexin prevents anthracycline-induced DNA double-strand break formation, apoptotic signaling mediated by caspase 3/7, 8 and 9, cardiomyocyte morphological changes, mitochondrial depolarization/loss, left ventricular systolic dysfunction, extracellular matrix remodeling, fibrotic alterations, and increases in plasma cardiac troponin T and BNP. Topobexin does not impair the antiproliferative effects of anthracyclines in cancer cells, exhibits no intrinsic cytotoxicity in cardiomyocytes, and is well tolerated in rabbits. Topobexin can be used in studies related to anthracycline-induced cardiotoxicity .
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-
- HY-P11590
-
|
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EGFR
|
Cancer
|
|
WGYRGFYC (WC8) is a selective HER2-targeting peptide that binds specifically to HER2 by mimicking the antigen-binding site of trastuzumab. The DOTA precursor of WGYRGFYC has a KD of 61.20 nM for HER2. WGYRGFYC enables specific and highly sensitive detection of HER2 expression in HER2-positive breast cancer cells and tumor tissues, and monitors the dynamic downregulation of HER2 expression. WGYRGFYC rapidly distributes to target tissues and is efficiently cleared from non-target tissues via the kidneys, generating an ideal tumor-to-background ratio in imaging; it is a component of the PET radiotracer Ga-DOTA-WC8. WGYRGFYC exhibits no significant cytotoxicity in breast cancer cells, and can be used for non-invasive imaging diagnosis and therapeutic efficacy evaluation of HER2-positive breast cancer .
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- HY-N6784
-
|
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ATP Synthase
Bacterial
Apoptosis
Antibiotic
|
Infection
Neurological Disease
|
|
Oligomycin B is an antibiotic that acts as a non-selective inhibitor of ATP Synthase. Oligomycin B increases mitochondrial membrane potential. Oligomycin B induces apoptosis and necrosis. Oligomycin B impairs the motility of Plasmopara viticola zoospores and induces their lysis. Oligomycin B inhibits Magnaporthe oryzae (wheat blast fungus) and suppresses the development of wheat blast. Oligomycin B reduces hyphal growth and spore germination of Botrytis cinerea, and protects Arabidopsis thaliana against Botrytis cinerea infection. Oligomycin B exacerbates cytotoxic brain edema in rats with cerebral cortical contusion, increases intracranial pressure and brain water content, and aggravates mitochondrial damage in these rats. Oligomycin B is used in studies related to grape downy mildew, traumatic brain injury, wheat blast, and gray mold .
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- HY-103241R
-
|
|
Reference Standards
Amyloid-β
ATM/ATR
Phosphatase
Apoptosis
|
Neurological Disease
Cancer
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Ro 90-7501 (Standard) is the analytical standard of Ro 90-7501 (HY-103241). This product is intended for research and analytical applications. Ro 90-7501 is an amyloid β42 (Aβ42) fibril assembly inhibitor that reduces Aβ42-induced cytotoxicity (EC50 of 2 μM). Ro 90-7501 inhibits ATM phosphorylation and DNA repair. RO 90-7501 selectively enhances toll-like receptor 3 (TLR3) and RIG-I-like receptor (RLR) ligand-induced IFN-β gene expression and antiviral response . Ro 90-7501 also inhibits protein phosphatase 5 (PP5) in a TPR-dependent manner . Ro 90-7501 has significant radiosensitizing effects on cervical cancer cells .
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-
- HY-174866
-
|
|
Histone Acetyltransferase
Epigenetic Reader Domain
PROTACs
|
Cancer
|
|
BT-O2C is a highly selective p300 PROTAC degrader. BT-O2C can significantly degrade the level of p300 in HAP1 cells. BT-O2C has significant cytotoxicity in CIC:DUX4 sarcoma (CDS) cell lines (IC50 ranges from 152 to 221 nM) and significantly reduces the expression of CDS target genes (ETV1, ETV4, ETV5). BT-O2C can be used for research on cancer. (Pink: p300 Ligand (HY-174868); Blue: CRBN Ligand (HY-W023573); Black: Linker; CRBN Ligand+Linker (HY-174869)) .
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-
- HY-119062
-
|
|
MetAP
CDK
|
Cancer
|
|
A-800141 is an orally active, selective, sulfonamide-based MetAP2 inhibitor (IC50=12 nM) that binds reversibly to MetAP2 and interacts with its manganese ions. A-800141 induces the production of N-terminal methionine-unprocessed GAPDH variants, which in turn triggers G1-phase cell cycle arrest, elevates p21 levels, and reduces the levels of phosphorylated Rb and total cyclin A. A-800141 exhibits anti-angiogenic and tumor growth inhibitory effects, and produces synergistic effects when combined with cytotoxic inhibitors or BCL-2 inhibitors. A-800141 has been widely used in scientific research related to B-cell lymphoma, neuroblastoma, prostate cancer, colon cancer, melanoma and other fields .
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-
- HY-179034
-
|
|
Carbonic Anhydrase
c-Met/HGFR
Apoptosis
|
Cancer
|
|
CAIX/XII-IN-16 (Compound 5d) is a selective inhibitor of CA IX/XII and c-Met. CAIX/XII-IN-16‘s Ki values for hCA IX, hCA XII and CA I are 10.6, 31.8 and 2361 nM respectively, and its IC50 value for c-Met is 0.49 μM. CAIX/XII-IN-16 exhibits significantly enhanced cytotoxicity against colon cancer cells under hypoxic conditions. CAIX/XII-IN-16 causes cell cycle arrest and induces apoptosis (apoptosis). CAIX/XII-IN-16 significantly enhances the efficacy of Oxaliplatin (HY-17371) and 5-Fluorouracil (HY-90006). CAIX/XII-IN-16 can be used for studies on chemotherapy resistance related to hypoxia .
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-
- HY-156096
-
|
|
HDAC
Histone Methyltransferase
Caspase
Apoptosis
DNA/RNA Synthesis
|
Cancer
|
|
HDAC3-IN-2 (compound 4i) is a pyrazinyl hydrazide-based HDAC3 inhibitor (IC50: 14 nM) that efficiently targets triple-negative breast cancer cells. HDAC3-IN-2 is cytotoxic with an IC50 of 0.55 μM against 4T1 and an IC50 of 0.74 μM against MDA-MB-231. HDAC3-IN-2 has anti-tumor efficacy in vivo in tumor-bearing mouse models, selectively increasing the acetylation levels of H3K9, H3K27 and H4K12, increasing the contents of apoptosis-related caspase-3, caspase-7 and cytochrome c, and reducing Proliferation-related Bcl-2, CD44, EGFR, and Ki-67 levels .
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-
- HY-183569
-
|
|
c-Fms
Akt
PERK
Aminotransferases (Transaminases)
Apoptosis
TNF Receptor
Interleukin Related
|
Metabolic Disease
|
|
CSF1R-IN-27 is a CSF1R inhibitor with oral effectiveness, kinome-wide selective profile, low cellular cytotoxicity, and CSF1R IC50 values of 19 nM, 88 nM, 173 nM, 797 nM, 1448 nM, and >3000 nM. CSF1R-IN-27 suppresses M-CSF-induced phosphorylation of CSF1R, AKT, and ERK in macrophages, and inhibits hepatic p-CSF1R/p-AKT/p-ERK signaling. CSF1R-IN-27 reduces serum transaminase levels, improves hepatic histopathology, alleviates inflammatory cell infiltration, and decreases circulating TNF-α and IL-6 levels. CSF1R-IN-27 can be used for the research of acute liver injury .
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-
- HY-175638
-
|
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Carbonic Anhydrase
Apoptosis
Bcl-2 Family
CDK
|
Cancer
|
|
Carbonic anhydrase-IN-35 is a selective carbonic anhydrase (CA) inhibitor. Carbonic anhydrase-IN-35 potently inhibits tumor-associated hCA IX (Ki = 0.6 nM) and hCA XII (Ki = 2.2 nM). Carbonic anhydrase-IN-35 induces apoptosis in MCF-7 cells by elevating Bax, reducing Bcl-2, and downregulating CDK4/6. Carbonic anhydrase-IN-35 exhibits potent cytotoxicity against MCF-7 (IC50 = 0.3975 μM normoxic/0.6575 μM hypoxic), MCF-7-ADR (IC50> = 0.3975 μM normoxic/4.488 μM hypoxic), MDA-MB-231, and 4T1 breast cancer cells. Carbonic anhydrase-IN-35 can be used for the study of breast cancer .
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-
- HY-P5640
-
|
|
Bacterial
Parasite
|
Infection
|
|
Tritrpticin is a porcine-derived antimicrobial peptide with properties such as membrane disruption and hemolysis. Tritrpticin disrupts the cell membranes of bacteria, fungi and Jurkat T cell leukemia cells and induces their death. Tritrpticin also enhances the efficacy of Metronidazole (HY-B0318) against *Trichomonas vaginalis*, reduces plasma endotoxin and inflammatory cytokine levels, restricts bacterial growth in blood and visceral tissues, decreases the mortality rate of septic shock in rats and enhances the therapeutic effect of ertapenem. Tritrpticin exhibits selective cytotoxicity against Jurkat T cell leukemia cells, while showing low toxicity to normal peripheral blood mononuclear cells and red blood cells, and can serve as a template for antimicrobial peptide design. Tritrpticin can be applied to research related to bacterial infections, fungal infections, trichomoniasis, septic shock and leukemia .
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-
- HY-181556
-
|
|
JNK
TGF-beta/Smad
Cadherin
|
Inflammation/Immunology
|
|
JNK3-IN-10 is a blood-brain barrier-impermeable JNK3 inhibitor (IC50=0.257 nM) with over 400-fold selectivity over JNK1. JNK3-IN-10 blocks the JNK3-mediated signaling pathway downstream of TGF-β1, inhibits TGF-β1-induced phosphorylation of c-Jun, reduces the expression of pro-fibrotic markers, and restores the expression of the epithelial protein E-cadherin. JNK3-IN-10 exhibits low cytotoxicity, anti-fibrotic, cytoprotective and renoprotective effects, and alleviates albuminuria, glomerulosclerosis and podocyte foot process fusion. JNK3-IN-10 can be used for the research of chronic kidney disease, glomerulosclerosis and adriamycin-induced nephropathy .
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-
- HY-179021
-
|
|
COX
Lipoxygenase
|
Cancer
|
|
COX-2/15-LOX-IN-7 is a potent, selective and orally active dual inhibitor of COX-2 and 15-LOX with IC50 values of 0.022 and 1.19 μM. COX-2/15-LOX-IN-7 also inhibits COX-1 with an IC50 value of 28.081μM. COX-2/15-LOX-IN-7 has low cytotoxicity against human colorectal cancer HT-29 and HCT116 cell lines (IC50 >100 μM for both). COX-2/15-LOX-IN-7 exhibits non-ulcerogenic performance. COX-2/15-LOX-IN-7 can be used for the research of cancer .
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-
- HY-174301
-
|
|
Deubiquitinase
DNA Methyltransferase
MDM-2/p53
|
Cancer
|
|
USP7-IN-18 is a naphthalene derivative. USP7-IN-18 is a selective USP7 inhibitor (IC50 : 130.9 nM), with no or very weak inhibition of the other 8 DUBs including USP47. USP7-IN-18 specifically binds to the catalytic domain of USP7, blocking its deubiquitinase activity. USP7-IN-18 causes degradation of the oncogenic proteins MDM2 and DNMT1, and also degrades the novel target PCLAF. USP7-IN-18 activates the p53-p21 pathway. USP7-IN-18 exerts anti-tumor effects in colon cancer animal models and reshapes the tumor immune microenvironment. USP7-IN-18 achieves both direct cytotoxic and immune-synergistic anti-tumor actions.
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-
- HY-125938
-
|
Cycloartenol ferulate; Cycloartenol ferulic acid ester
|
Drug Derivative
Apoptosis
Reactive Oxygen Species (ROS)
JAK
STAT
|
Inflammation/Immunology
Cancer
|
|
Cycloartenyl ferulate (Cycloartenol ferulate; Cycloartenol ferulic acid ester) is a derivative of γ-oryzanol (HY-B2194) with multiple biological activities including antioxidant, anti-inflammatory, and anti-tumor properties. Cycloartenyl ferulate selectively binds to IFNγR1 (binding affinity Kd = 0.5 μM) to activate the canonical JAK1/2-STAT1 signaling pathway. Cycloartenyl ferulate inhibits paraquat (PQ)-triggered apoptosis and ROS in HK2 cells. Cycloartenyl ferulate enhances the activation and cytolytic activity of natural killer (NK) cells by upregulating the expression of NK cell activation receptors (NKG2D, NKp30, NKp44) and the release of cytotoxic molecules and cytokine IFNγ. Cycloartenyl ferulate exerts anti-cancer effects in tumor mice models. Cycloartenyl ferulate can be used for the study of cancer and allergic inflammation intervention .
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-
- HY-177990
-
|
|
STAT
MMP
Apoptosis
|
Cancer
|
|
STAT3-IN-52 (Compound 9) is a selective and orally active signal transducer and activator of transcription 3 (STAT3) inhibitor. STAT3-IN-52 binds to the pY705 site of STAT3 (Ki = 440 nM), blocking the phosphorylation and dimerization of STAT3. STAT3-IN-52 shows strong cytotoxicity against various cancer cells, such as breast cancer MDA-MB-231 (IC50 = 0.7 μM), medulloblastoma UW426, pancreatic cancer BKPC3 cells. STAT3-IN-52 can induce cell apoptosis, inhibit the STAT3 nuclear transport and DNA binding activity and downregulate the expression of the STAT3 target gene MMP9. STAT3-IN-52
can be used for research related to STAT3 abnormal activation in cancer .
|
-
- HY-183831
-
|
|
MDM-2/p53
PARP
Caspase
Apoptosis
|
Cancer
|
|
GPS167 is a CLK kinase inhibitor that potently and selectively inhibits recombinant human CLK1, CLK2 and CLK4. By inhibiting CLK-mediated phosphorylation of SRSF10, GPS167 upregulates the protein-binding ability of CLK1 and CLK4 with SRSF10, downregulates oncogenic BCLAF1-L and upregulates tumor-suppressive BCLAF1-S, regulates alternative splicing of genes such as MDM2 and MDM4, stabilizes p53 protein and induces DNA damage, ultimately triggering tumor cell apoptosis. GPS167 can block the epithelial-mesenchymal transition process of tumors, activate intracellular double-stranded RNA-mediated antiviral immune responses, and produce synergistic cytotoxicity when combined with microtubule-targeting drugs. GPS167 can be used in research related to various cancers including colorectal cancer .
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-
- HY-W010451R
-
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Hydroxyhydroquinone (Standard)
|
Reference Standards
PERK
Potassium Channel
Apoptosis
Eukaryotic Initiation Factor (eIF)
|
Cardiovascular Disease
Cancer
|
|
1,2,4-Trihydroxybenzene (Hydroxyhydroquinone) (Standard) is the analytical standard of 1,2,4-Trihydroxybenzene (HY-W010451). This product is intended for research and analytical applications. 1,2,4-Trihydroxybenzene (Hydroxyhydroquinone) is an ER stress inducer that targets proteins such as PKR-like ER kinase PERK to induce cytotoxicity. 1,2,4-Trihydroxybenzene selectively activates eIF2α phosphorylation, activates the PERK-eIF2α signaling pathway and induces stress granule formation. 1,2,4-Trihydroxybenzene subsequently exacerbates oxidative stress and causes DNA double-strand breaks, destroying organelles such as mitochondria and ER, and inducing cell death. 1,2,4-Trihydroxybenzene also has the potential to exhibit anti-tumor effect, increase blood pressure, and relieve spasm .
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-
- HY-123597
-
|
DDUG; NCI C04808
|
Autophagy
Checkpoint Kinase (Chk)
|
Cancer
|
|
NSC 109555 is an ATP-competitive inhibitor of checkpoint kinase 2 (Chk2; IC50=200 nM in a cell-free kinase assay). It is selective for Chk2 over Chk1 and 16 kinases in a panel but does inhibit Brk, c-Met, IGFR, and LCK with IC50 values of 210, 6,000, 7,400, and 7,100 nM, respectively. NSC 109555 inhibits Chk2 autophosphorylation and phosphorylation of the Chk2 substrate histone H1 in vitro (IC50=240 nM). It inhibits the growth of, and induces autophagy in, L1210 leukemia cells in vitro.2 NSC 109555 (1,250 nM) potentiates gemcitabine-induced cytotoxicity in MIA PaCa-2, CFPAC-1, PANC-1, and BxPC-3 pancreatic cancer cells, as well as reduces gemcitabine-induced increases in Chk2 phosphorylation and enhances gemcitabine-induced production of reactive oxygen species (ROS) in MIA PaCa-2 cells.
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-
- HY-175459
-
|
|
PROTACs
FAK
|
Inflammation/Immunology
Cancer
|
|
PROTAC FAK degrader 3 is a selective FAK PROTAC degrader (DC50 = 1.08 nM). PROTAC FAK degrader 3 induces FAK degradation dependent on the ubiquitin-proteasome system and its binding to FAK and CRBN. PROTAC FAK degrader 3 upregulates MHC-I gene transcription and tumor cell surface expression by inhibiting the non-catalytic activity of FAK, leading to increased antigen presentation and activation of cytotoxic CD8 T cells. PROTAC FAK degrader 3 enhances in vivo anti-tumor activity by promoting MHC-I expression and enhancing T cell activation. PROTAC FAK degrader 3 can be used in cancer research targeting FAK degradation in ovarian cancer, hepatocellular carcinoma, and other cancers. (Pink: FAK-IN-3:HY-143407, Blue: Thalidomide-4-OH:HY-103596, Blue + Black: FAK ligand-3: HY-W939883, Black: Linker) .
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-
- HY-W680886
-
|
|
Monoamine Transporter
Serotonin Transporter
Dopamine Transporter
5-HT Receptor
|
Neurological Disease
|
|
6-APDB is a class of monoamine neurotransmitter releaser and Monoamine Transporter modulator that exerts selective effects on human monoamine transporters and acts as a partial agonist at 5-HT2 family receptors. For NET, 6-APDB has an IC50 of 0.56 μM and a Ki of 18 μM; for SERT, it has an IC50 of 2.3 μM and a Ki of 23 μM; for DAT, it has an IC50 of 33 μM and a Ki of >30 μM, and affinity for rat and mouse TAAR1, with Ki values of 1.0 μM and 0.21 μM, respectively. 6-APDB inhibits norepinephrine and 5-HT reuptake, mediates the release of three types of monoamine neurotransmitters, shows a dose-dependent biphasic locomotor effect in mice, and fully substitutes the discriminative stimulus effect of MDMA. 6-APDB shows no significant cytotoxicity at high concentrations, and possesses empathogenic psychoactivity, potential hallucinogenic effects, and behavioral effects associated with intermittent abuse .
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-
- HY-182044
-
|
|
Ras
Apoptosis
PARP
Caspase
CDK
|
Cancer
|
|
MRTX849-amide-C4-(o)-carborane is a KRAS G12C inhibitor with mutation selectivity for cells expressing KRAS G12C. MRTX849-amide-C4-(o)-carborane shows low intrinsic cytotoxicity in cancer cells. MRTX849-amide-C4-(o)-carborane covalently binds to Cys12 of KRAS G12C, recruits Hsp70, promotes ubiquitination, and induces proteasome-dependent degradation of the target protein. MRTX849-amide-C4-(o)-carborane inhibits the activity of the downstream ERK signaling pathway and induces apoptosis signaling in cancer cells. MRTX849-amide-C4-(o)-carborane is applicable for the research of KRAS G12C-positive cancers .
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-
- 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 .
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-
- HY-151738
-
|
|
ADC Linker
|
Others
|
|
Fmoc-Aeg(N3)-OH is a click chemistry reagent containing an Azide. Alkylating the Nitrogen of an amide bond results in peptoid structures, which leads to conformational restrains, like N-methylation and allows backbone derivatisation. Altering cytotoxicity, bacterial cell selectivity and receptor pharmacology through formation of peptoid derivatives have been published for Cilengitide, Piscidin 1, and MC3, MC4 and MC5 receptor agonist. This building block enables design of macrocycles through intermolecular crosslinking or backbone stabilization through intermolecular ring-closure. This compound is a potential building block for the construction of (customized) peptide nucleic acids (PNAs) and for peptoid synthesis . Fmoc-Aeg(N3)-OH 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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-
- HY-179612
-
|
|
SARS-CoV
Cathepsin
Proteasome
|
Infection
|
|
SARS-CoV-2 3CLpro-IN-34 (Compound 55) is a highly efficient non-covalent inhibitor of the SARS-CoV-2 3CL pro protease (b. SARS-CoV-2 3CL pro protease) with an IC50 of 1.9 μM. SARS-CoV-2 3CLpro-IN-34 can inhibit the 3CL pro protein of SARS-CoV-1, with its IC50 being 3.2 μM, and it shows high selectivity towards host cysteine proteases (such as cathepsins L/K and calpain). SARS-CoV-2 3CLpro-IN-34 exhibits antiviral activity in cells infected with SARS-CoV-2, with its EC50 being 25 μM, and it is not affected by P-gp inhibitors and shows no significant cytotoxicity. SARS-CoV-2 3CLpro-IN-34 can be used for research on SARS-CoV-2 infection .
|
-
- HY-173148
-
|
|
SARS-CoV
|
Infection
|
|
TKB272 is an orally active and selective antiviral agent targeting the main protease (Mpro) of SARS-CoV-2. It effectively blocks the infection and replication of various SARS-CoV-2 strains, including Omicron variants such as XBB.1.5 and EG.5.1. The enzymatic inhibitory activity of TKB272 shows an IC50 of 0.7 µM (against SARS-CoV-2WK-521 Mpro), and its antiviral activity at the cellular level reaches an EC50 as low as 2.6 nM (against BQ.1.1 strain in HeLahACE2-TMPRSS2 cells), with a cytotoxicity CC50 of 98 µM, indicating no apparent toxicity. In addition, TKB272 significantly suppresses the replication of SARS-CoV-2XBB.1.5 in B6.Cg-Tg(K18-hACE2)2-Prlmn/J transgenic mouse models. TKB272 holds promise for research in the field of SARS-CoV-2 infection .
|
-
- HY-P99014
-
|
ARGX-110
|
Fc Receptor (FcR)
NF-κB
|
Inflammation/Immunology
Cancer
|
|
Cusatuzumab (ARGX-110) is a selective competitive blocker targeting CD70 (with an equilibrium dissociation constant of 17 pM for binding to human CD70). Cusatuzumab also possesses enhanced antibody-dependent cell-mediated cytotoxicity (ADCC) activity. It is a humanized IgG1 monoclonal antibody, artificially synthesized through humanization and genetic engineering modifications (CH2 region mutation to enhance effector function). Cusatuzumab has a dual mechanism of action: firstly, it competitively blocks the interaction between CD70 and CD27, inhibiting the CD27-NF-κB signaling pathway, reducing regulatory T cell (Treg) activation and tumor cell proliferation; secondly, by enhancing binding to FcγRIIIa, it mediates ADCC and antibody-dependent cellular phagocytosis (ADCP), directly lysing CD70-positive tumor cells. Cusatuzumab can efficiently eliminate leukemia stem cells (LSCs), induce tumor cell differentiation and apoptosis, restore immune surveillance, and target CD70-positive tumors. Cusatuzumab is used in the study of acute myeloid leukemia (AML) .
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-
- HY-128586A
-
|
|
NEDD8-activating Enzyme
Carbonic Anhydrase
Apoptosis
|
Cancer
|
|
TAS4464 hydrochloride is a long-acting, highly selective covalent inhibitor targeting NEDD8-activating enzyme (NAE) (IC50=0.955 nM), and also inhibits CAII with an IC50 of 0.73 μM, which is less potent than MLN4924 (HY-70062). The IC50 values of TAS4464 hydrochloride against other E1 enzymes UAE and SAE are 449 nM and 1280 nM, respectively. TAS4464 hydrochloride targets NEDD8 in an ATP-dependent manner to inhibit NAE, blocks the neddylation pathway, causes accumulation of CRL ubiquitin ligase substrates (such as CDT1, p27, phosphorylated IκBα), and further induces tumor cell apoptosis. TAS4464 hydrochloride exhibits antiproliferative and cytotoxic effects, and has broad-spectrum antitumor activity against various hematologic and solid tumor cell lines as well as patient-derived tumor cells. TAS4464 hydrochloride has a wide therapeutic window, without obvious toxicity. TAS4464 hydrochloride can be used in the research of hematologic malignancies (leukemia, lymphoma, multiple myeloma, etc.) and solid tumors (small cell lung cancer, colorectal cancer, sarcoma, endometrial cancer, ovarian cancer, etc.) .
|
-
- HY-128586
-
|
|
Apoptosis
Carbonic Anhydrase
NEDD8-activating Enzyme
|
Cancer
|
|
TAS4464 is a long-acting, highly selective covalent inhibitor targeting NEDD8-activating enzyme (NAE) (IC50=0.955 nM), and also inhibits CAII with an IC50 of 0.73 μM, which is less potent than MLN4924 (HY-70062). The IC50 values of TAS4464 against other E1 enzymes UAE and SAE are 449 nM and 1280 nM, respectively. TAS4464 targets NEDD8 in an ATP-dependent manner to inhibit NAE, blocks the neddylation pathway, causes accumulation of CRL ubiquitin ligase substrates (such as CDT1, p27, phosphorylated IκBα), and further induces tumor cell apoptosis. TAS4464 exhibits antiproliferative and cytotoxic effects, and has broad-spectrum antitumor activity against various hematologic and solid tumor cell lines as well as patient-derived tumor cells. TAS4464 has a wide selcetive window, without obvious toxicity. TAS4464 can be used in the research of hematologic malignancies (leukemia, lymphoma, multiple myeloma, etc.) and solid tumors (small cell lung cancer, colorectal cancer, sarcoma, endometrial cancer, ovarian cancer, etc.) .
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-
| Cat. No. |
Product Name |
Type |
-
- HY-D1244
-
|
|
Fluorescent Dyes
|
|
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-D2318
-
|
|
Fluorescent Dyes
|
|
Flipper-TR 5 is a Flipper probe containing a terminal carboxylate for retention on the plasma membrane. Flipper-TR 5 selectively labels the cytoplasmic membrane, and exhibits excellent mechanical sensitivity, negligible cytotoxicity and controllable phototoxicity .
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-
- HY-D2186
-
|
|
Fluorescent Dyes
|
|
BTD probe-1 is a benzothiazine-based chemoproteomic probe and selective protein S-sulfenic acid (Cys-SOH) labeling agent. BTD probe-1 labels protein S-sulfenic acids in vitro in cell and tissue samples, and in situ in intact cells, enabling detection or enrichment of modified proteins/peptides. BTD probe-1 exhibits no cytotoxicity in cells at concentrations ≤1 mM. BTD probe-1 enables global, site-specific mapping and quantification of cysteine S-sulfenylation in complex proteomes with lower input material .
|
-
- HY-130013
-
|
|
Fluorescent Dyes
|
|
HKYellow-AM (6/12-mixture) is a yellow fluorescent probe that can detect ONOO- in living cells and tissues with high selectivity and sensitivity without cytotoxicity .
|
-
- HY-D2988
-
|
|
Fluorescent Dyes
|
|
BIN-3 is a novel near-infrared fluorescent probe. BIN-3 has excellent biocompatibility, no cytotoxicity, and no hemolysis. BIN-3 can be used for highly sensitive and selective imaging of drug-resistant bacterial infections expressing β-lactam enzymes in live mice .
|
-
- HY-D3197
-
|
|
Fluorescent Dyes
|
|
CDg16 is a selective fluorescent dye targeting SLC18B1 (λabs/λem=458/544 nm) that is actively transported into lysosomal vesicles of activated macrophages independent of the endocytic pathway. CDg16 enables highly specific vesicle localization in live cells. CDg16 exhibits no cytotoxicity and accurately distinguishes activated M1 and M2 subsets from different origins. CDg16 shows low background staining in non-activated cells and normal organs, making it suitable for time-lapse imaging. In preclinical animal models of inflammatory sites, atherosclerotic plaques and liver inflammation, CDg16 allows visualization of activated macrophages. CDg16 can be used to study inflammation-related diseases and atherosclerosis .
|
-
- HY-D3190
-
|
|
Fluorescent Dyes
|
|
BODIPY-DOX is a conjugate composed of BODIPY and Doxorubicin (HY-15142A), as well as a pH-activated fluorescent probe for M1 macrophages and an apoptosis inducer. BODIPY-DOX undergoes pH-induced hydrazone bond cleavage in acidic M1 macrophage phagosomes, thereby releasing cytotoxic Doxorubicin (Dox) and inhibiting the function of pro-inflammatory M1 macrophages. BODIPY-DOX highly selectively inhibits the production of relevant pro-inflammatory cytokines by mouse and human monocyte-derived M1 macrophages, while exerting minimal effects on M2 or unactivated macrophages. Therefore, BODIPY-DOX enables simultaneous fluorescent tracing, differentiation and elimination of specific macrophage subsets, and exhibits the potential to regulate tissue regeneration in zebrafish models .
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| Cat. No. |
Product Name |
Type |
-
- HY-P2149
-
|
|
Biochemical Assay Reagents
|
|
Concanavalin A can be coupled to agarose to form Concanavalin A (agarose) (HY-P2149A). Concanavalin A (ConA) is a selective, competitive binding agent that targets specific carbohydrate structures containing glucose and mannose; it acts as a mitogen and exhibits varying degrees of cytotoxicity, hepatotoxicity, and teratogenicity. Concanavalin A is also utilized for in vivo blood glucose monitoring in the context of diabetes .
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-
- HY-P2149A
-
|
|
Biochemical Assay Reagents
|
|
Concanavalin A (agarose) is composed of Concanavalin A (HY-P2149) conjugated with agarose. Concanavalin A (ConA) is a selective competitive binder targeting the specific carbohydrate structures of glucose and mannose, inducing mitosis, and exhibiting certain cytotoxicity, hepatotoxicity, and teratogenicity. Concanav in A (agarose) can be used for in vivo blood glucose monitoring in diabetes, and for "fishing out" specific glycoproteins or removing sugar impurities from complex samples .
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-
- HY-75577
-
|
|
Biochemical Assay Reagents
|
|
4-Amino-3-methoxybenzoic acid is a drug intermediate that can be used to construct benzothiazole compounds with anti-breast cancer activity .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P1103
-
|
|
CXCR
|
Cancer
|
|
CTCE-9908 is a potent and selective CXCR4 antagonist. CTCE-9908 induces mitotic catastrophe, cytotoxicity and inhibits migration in CXCR4-expressing ovarian cancer cells .
|
-
- HY-P4284
-
|
|
Proteasome
ClpP
Bacterial
|
Infection
|
|
Z-GGF-CMK is an Antibacterial agent, an inhibitor of the ClpP1P2 serine protease complex (with an IC50 of 50 μM against intracellular ClpP1P2 protease activity in Mycobacterium bovis BCG), and a selective inhibitor of the mycobacterial Proteasome (with an IC50 of 50 μM against the proteasome in M. bovis BCG). Z-GGF-CMK inhibits the growth of mycobacteria. Z-GGF-CMK exhibits cytotoxic activity against liver cancer cells. Z-GGF-CMK can be used in the research of tuberculosis .
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-
- HY-P10772
-
|
|
Peptide-Drug Conjugates (PDCs)
EBV
|
Cancer
|
|
L2P4 is a peptide-based and EBNA1 targeting fluorescent probe, which inhibits the EBNA1 homodimer formation and selectively inhibits EBV+ tumor growth. L2P4 exhibits cytotoxicity in EBV-positive C666-1 cell with LC50 of 46.4 μM .
|
-
- HY-P10772A
-
|
|
Peptide-Drug Conjugates (PDCs)
EBV
|
Cancer
|
|
L2P4 TFA is a peptide-based and EBNA1 targeting fluorescent probe, which inhibits the EBNA1 homodimer formation and selectively inhibits EBV+ tumor growth. L2P4 TFA exhibits cytotoxicity in EBV-positive C666-1 cell with LC50 of 46.4 μM .
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-
- HY-P5640
-
|
|
Bacterial
Parasite
|
Infection
|
|
Tritrpticin is a porcine-derived antimicrobial peptide with properties such as membrane disruption and hemolysis. Tritrpticin disrupts the cell membranes of bacteria, fungi and Jurkat T cell leukemia cells and induces their death. Tritrpticin also enhances the efficacy of Metronidazole (HY-B0318) against *Trichomonas vaginalis*, reduces plasma endotoxin and inflammatory cytokine levels, restricts bacterial growth in blood and visceral tissues, decreases the mortality rate of septic shock in rats and enhances the therapeutic effect of ertapenem. Tritrpticin exhibits selective cytotoxicity against Jurkat T cell leukemia cells, while showing low toxicity to normal peripheral blood mononuclear cells and red blood cells, and can serve as a template for antimicrobial peptide design. Tritrpticin can be applied to research related to bacterial infections, fungal infections, trichomoniasis, septic shock and leukemia .
|
-
- HY-P1103A
-
|
|
CXCR
|
Cancer
|
|
CTCE-9908 TFA is a potent and selective CXCR4 antagonist. CTCE-9908 TFA induces mitotic catastrophe, cytotoxicity and inhibits migration in CXCR4-expressing ovarian cancer cells .
|
-
- HY-P5446
-
|
|
Bacterial
|
Others
|
|
BMAP-18 is a biological active peptide. (BMAP-18 is a truncated form of the antimicrobial peptide BMAP-27. Bovine myeloid antimicrobial peptide-27 (BMAP-27) belongs to the Cathelicidin family of peptides which displays rapid bactericidal activity against Staphylococcus aureus, Streptococcus uberis, and Escherichia coli. BMAP-27 is cytotoxic to human erythrocytes and neutrophils, although at higher than microbicidal concentrations. BMAP-18 displays much higher cell selectivity as compared to parental BMAP-27 because of its decreased hemolytic activity and retained antimicrobial activity.)
|
-
- HY-A0162R
-
|
|
Antibiotic
Reference Standards
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-P10860
-
|
|
Factor Xa
|
Cardiovascular Disease
|
|
cMCoFx1 is a potent and selective FXIIa cyclic peptide inhibitor. cMCoFx1 has high binding affinity (KD: 900 pM) and inhibitory activity (Ki: 370 pM) for FXIIa. cMCoFx1 can effectively inhibit endogenous clotting pathways, and cMCoFx1 is stable in serum and non-cytotoxic .
|
-
- HY-P5891
-
|
|
PKC
|
Cardiovascular Disease
|
|
TAT-SAMβA is the peptide consist of RNAENFDRF (SAMβA; HY-P3429) conjugated to the cell penetrating TAT protein-derived peptide TAT47–57. TAT-SAMβA is a selective antagonist of Mfn1-βIIPKC association. TAT-SAMβA protects mouse embryonic fibroblast cells (MEFs) against oxidative stress-induced cytotoxicity .
|
-
- HY-P11019
-
|
|
CXCR
Calcium Channel
|
Cancer
|
|
IS4 is a selective CXCR4 competitive antagonist, with an IC50 of 0.65 nM in THP-1 cells and 38.75 nM in Jurkat cells. IS4 is stable in serum and non-cytotoxic. IS4 competitively binds to CXCR4 with CXCL12, thereby inhibiting CXCL12-induced intracellular Ca 2+ release and cancer cell migration. IS4 can be used in the research on the prevention of metastasis of breast cancer, prostate cancer, leukemia, and other diseases .
|
-
- HY-P11757
-
|
|
EGFR
|
Cancer
|
|
Cyclo[K(N3)larllt] is a seven-membered cyclic peptide targeting EGFR, with a Kd value of 5.09 μM, and exhibits binding selectivity toward homologous proteins HER2 and HER3. Cyclo[K(N3)larllt] has no cytotoxicity and shows no growth inhibitory effect on cancer cells overexpressing EGFR. Cyclo[K(N3)larllt] can serve as a ligand for EGFR-targeted fluorescent conjugates, which is applicable to the detection of cancers with EGFR overexpression. Cyclo[K(N3)larllt] can be used in the research of colorectal cancer .
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-
- HY-P10466A
-
|
|
Sec61
SARS-CoV
Interleukin Related
TNF Receptor
IFNAR
|
Infection
Inflammation/Immunology
|
|
KZR-8445 TFA, a cyclic depsipeptide, is a client-selective Sec61 inhibitor. KZR-8445 TFA binds to the fully opened Sec61 lateral gate, blocks lumenal plug domain access, stabilizes lateral gate helices, traps select signal peptides, and disrupts secretory and membrane protein biogenesis. KZR-8445 TFA inhibits pro-inflammatory cytokine secretion in primary immune cells. KZR-8445 TFA inhibits SARS-CoV-2 replication, virus-induced cytotoxicity, and spike protein biogenesis. KZR-8445 TFA blocks disease progression in a mouse model of rheumatoid arthritis. KZR-8445 TFA can be used for the researches of rheumatoid arthritis and SARS-CoV-2 infection .
|
-
- HY-P10466
-
|
|
Sec61
SARS-CoV
Interleukin Related
TNF Receptor
IFNAR
|
Infection
Inflammation/Immunology
|
|
KZR-8445, a cyclic depsipeptide, is a client-selective Sec61 inhibitor. KZR-8445 binds to the fully opened Sec61 lateral gate, blocks lumenal plug domain access, stabilizes lateral gate helices, traps select signal peptides, and disrupts secretory and membrane protein biogenesis. KZR-8445 inhibits pro-inflammatory cytokine secretion in primary immune cells. KZR-8445 inhibits SARS-CoV-2 replication, virus-induced cytotoxicity, and spike protein biogenesis. KZR-8445 blocks disease progression in a mouse model of rheumatoid arthritis. KZR-8445 can be used for the researches of rheumatoid arthritis and SARS-CoV-2 infection .
|
-
- HY-P11590
-
|
|
EGFR
|
Cancer
|
|
WGYRGFYC (WC8) is a selective HER2-targeting peptide that binds specifically to HER2 by mimicking the antigen-binding site of trastuzumab. The DOTA precursor of WGYRGFYC has a KD of 61.20 nM for HER2. WGYRGFYC enables specific and highly sensitive detection of HER2 expression in HER2-positive breast cancer cells and tumor tissues, and monitors the dynamic downregulation of HER2 expression. WGYRGFYC rapidly distributes to target tissues and is efficiently cleared from non-target tissues via the kidneys, generating an ideal tumor-to-background ratio in imaging; it is a component of the PET radiotracer Ga-DOTA-WC8. WGYRGFYC exhibits no significant cytotoxicity in breast cancer cells, and can be used for non-invasive imaging diagnosis and therapeutic efficacy evaluation of HER2-positive breast cancer .
|
| Cat. No. |
Product Name |
Target |
Research Area |
Image |
-
- HY-P9948
-
|
Campath-IH
|
Apoptosis
|
Cancer
|
|
Alemtuzumab (Campath-IH) is a humanized monoclonal antibody against CD52. Alemtuzumab does not cross-react with murine CD52. Alemtuzumab selectively targets the CD52 antigen to induce profound lymphocyte depletion, followed by recovery of T and B cells with regulatory phenotypes. Alemtuzumab is capable of complement-dependent cytotoxicity and antibody-dependent cell-mediated cytotoxicity (ADCC), as well as induction of apoptosis. Alemtuzumab has the potential for B-cell chronic lymphocytic leukaemia research .
|
-
(5)
-
- HY-P99014
-
|
ARGX-110
|
Fc Receptor (FcR)
NF-κB
|
Inflammation/Immunology
Cancer
|
|
Cusatuzumab (ARGX-110) is a selective competitive blocker targeting CD70 (with an equilibrium dissociation constant of 17 pM for binding to human CD70). Cusatuzumab also possesses enhanced antibody-dependent cell-mediated cytotoxicity (ADCC) activity. It is a humanized IgG1 monoclonal antibody, artificially synthesized through humanization and genetic engineering modifications (CH2 region mutation to enhance effector function). Cusatuzumab has a dual mechanism of action: firstly, it competitively blocks the interaction between CD70 and CD27, inhibiting the CD27-NF-κB signaling pathway, reducing regulatory T cell (Treg) activation and tumor cell proliferation; secondly, by enhancing binding to FcγRIIIa, it mediates ADCC and antibody-dependent cellular phagocytosis (ADCP), directly lysing CD70-positive tumor cells. Cusatuzumab can efficiently eliminate leukemia stem cells (LSCs), induce tumor cell differentiation and apoptosis, restore immune surveillance, and target CD70-positive tumors. Cusatuzumab is used in the study of acute myeloid leukemia (AML) .
|
-
(5)
-
- HY-P99144A
-
|
|
PD-1/PD-L1
|
Inflammation/Immunology
Cancer
|
|
Anti-Mouse PD-1 Antibody (S-5001) is a selective inhibitor targeting PD-1, blocking the PD-1/PD-L1 immune checkpoint axis through competitive binding to PD-1. Anti-Mouse PD-1 Antibody (S-5001) works by reversing the tumor immunosuppressive microenvironment and reactivating the anti-tumor activity of cytotoxic T lymphocytes. It can be used in research on tumors such as melanoma and HPV-positive oropharyngeal squamous cell carcinoma. Anti-Mouse PD-1 Antibody (S-5001) is often combined with photothermal therapy, chemotherapy, etc., to enhance efficacy .
|
-
(5)
-
- HY-P9961
-
|
GSK1841157; OMB-157
|
CD20
|
Cancer
|
|
Ofatumumab is a fully human anti-CD20 monoclonal antibody that induces antibody-dependent cell-mediated cytotoxicity (ADCC) and complement-dependent cytotoxicity (CDC) in CD20-expressing B lymphocytes. Ofatumumab has strong lytic activity against CD20-positive B lymphocytes and eliminates CD20-positive tumor cells through ADCC and CDC. Ofatumumab is particularly effective against drug-resistant cells with low CD20 expression and can be applied to the research of chronic lymphocytic leukemia (CLL) .
|
-
(5)
-
- HY-P990026
-
-
(5)
-
- HY-P99159
-
|
|
Interleukin Related
|
Cancer
|
|
Ivuxolimab is a fully human IgG2 agonist targeting OX40 (CD134), which selectively binds to the OX40 receptor on the surface of activated CD4 + and CD8 + T cells without inducing antibody-dependent cytotoxicity. Ivuxolimab can promote T cell proliferation, survival and cytokine (such as IFN-γ, IL-2) secretion, inhibit regulatory T cell function, and enhance anti-tumor immune response. Ivuxolimab can be used in the study of melanoma, hepatocellular carcinoma, head and neck squamous cell carcinoma, etc .
|
-
(5)
-
- HY-P991061
-
|
CHS-114; SRF-114
|
CCR
|
Cancer
|
|
Tagmokitug (CHS-114; SRF-114) is a fully human IgG1 antibody targeting CCR8. Tagmokitug selectively binds to human CCR8 (Kd = 502 pM) and mediates the death of CCR8-expressing cells via antibody-dependent cellular cytotoxicity and antibody-dependent cellular phagocytosis. Tagmokitug selectively eliminates intratumoral regulatory T cells, induces tumor growth inhibition, remodels the tumor immune microenvironment, and promotes the differentiation of cytotoxic CD8 + T cell subsets. Tagmokitug can be used for the research of solid tumors .
|
-
(5)
-
- HY-P990914
-
|
GS-1811; JTX-1811
|
CCR
|
Inflammation/Immunology
Cancer
|
|
Denikitug (GS-1811; JTX-1811) is a humanized monoclonal antibody against CCR8 receptor with a KD of 16.8 pM. Denikitug specifically binds to human CCR8, inhibits CCL1-induced downstream CCR8 signaling. Denikitug selectively depletes cells expressing CCR8 via antibody-dependent cellular cytotoxicity (ADCC). Denikitug promotes anti-tumor immunity and can be used for the research of cancer and immunology .
|
-
(5)
-
- HY-141599
-
|
ADCT 301
|
Antibody-Drug Conjugates (ADCs)
Interleukin Related
|
Cancer
|
|
Camidanlumab tesirine (ADCT 301) is an ADC comprising HuMax-TAC, a human IgG1 mAb directed against human CD25, stochastically conjugated through a dipeptide cleavable linker to a pyrrolobenzodiazepine (PBD) dimer warhead. Camidanlumab tesirine has a drug–antibody ratio (DAR) of 2.3. Camidanlumab tesirine binds human CD25 with picomolar affinity. Camidanlumab tesirine has highly potent and selective cytotoxicity against a panel of CD25-expressing human lymphoma cell lines .
|
-
(5)
-
- HY-P991942
-
|
BAY3375968; TPP-23411
|
CCR
|
Inflammation/Immunology
Cancer
|
|
Lanerkitug (BAY3375968) is a fully human monoclonal IgG1 anti-human CCR8 antibody. Lanerkitug selectively depletes human CCR8 + Tregs via antibody dependent cellular cytotoxicity (ADCC) and antibody dependent cellular phagocytosis (ADCP). Lanerkitug can be used in the research of solid tumors .
|
-
(5)
-
- HY-P992450
-
|
|
TNF Receptor
|
Cancer
|
|
REGN6569 is a fully human IgG1 monoclonal antibody targeting glucocorticoid-induced tumor necrosis factor receptor-related protein (GITR) with high specificity for GITR. REGN6569 exerts stronger in vitro antibody-dependent cell-mediated cytotoxicity (ADCC) against regulatory T cells expressing GITR. REGN6569 selectively depletes regulatory T cells via antibody-dependent cell-mediated cytotoxicity and increases the proportion of proliferative natural killer (NK) cells in peripheral blood. REGN6569 is applicable for advanced solid malignancies. Isotype control: HY-P99001 .
|
-
(5)
-
- HY-P992349
-
|
|
CD20
Apoptosis
|
Cancer
|
|
DXL625 is an autophilic CD20-targeting agent. DXL625 triggers downstream apoptosis signaling pathways dependent on intact lipid rafts and extracellular Ca 2+. DXL625 induces caspase-mediated apoptosis in cancer cells and selectively targets cells in the actively proliferative S phase. DXL625 mediates complement-dependent cytotoxicity in cancer cells and primary B lymphocytes. DXL625 can be used in research related to Burkitt's lymphoma and B-cell lymphoma .
|
-
(5)
-
- HY-P991942A
-
|
BAY3375968 (FUT8-KO); TPP-23411 (FUT8-KO)
|
CCR
|
Cancer
|
|
Lanerkitug (FUT8-KO) (BAY3375968 (FUT8-KO)) is an anti-CCR8 monoclonal antibody expressed by CHO cells with the fucosyltransferase 8 gene (FUT8) knocked out. Fucose deficiency enhances the ADCC effect of the antibody. Lanerkitug (HY-P991942) selectively depletes human CCR8+Tregs via antibody dependent cellular cytotoxicity (ADCC) and antibody dependent cellular phagocytosis (ADCP). Lanerkitug can be used in the research of solid tumors .
|
-
(5)
-
- HY-P992181
-
|
MEDI1116; VIB-1116; HZN-1116
|
Inhibitory Antibodies
|
Inflammation/Immunology
|
|
AMG-329 (MEDI1116) is a human immunoglobulin G1λ monoclonal antibody targeting FLT3L. AMG-329 selectively binds to FLT3L, blocks FLT3L-FLT3 interaction, neutralizes soluble and cell-bound human FLT3L activity. AMG-329 reduces circulating relative proportions of plasmacytoid dendritic cells, conventional dendritic cells, and classical monocytes. AMG-329 does not induce antibody dependent cellular cytotoxicity. AMG-329 can be used for the research of sjögren’s disease .
|
-
(5)
-
- HY-P992457
-
|
|
Glycoprotein VI
Interleukin Related
|
Cancer
|
|
SAR444200 is a nanobody T-cell engager targeting GPC3 (glypican-3) and TCRαβ (T-cell receptor αβ). SAR444200 has a KD of 0.023 nM for human GPC3 and a KD of 5.2 nM for human TCRαβ. SAR444200 mediates T-cell-dependent cytotoxicity, with high selectivity and killing activity against GPC3-positive tumor cells. SAR444200 binds to GPC3 in a dual-epitope manner, and binds to TCRαβ via its N-terminal nanobody, forming an artificial immunological synapse between T cells and tumor cells. SAR444200 can be used for the research of GPC3 + solid tumors, including liver cancer, lung squamous cell carcinoma and melanoma .
|
-
(5)
-
- HY-P991944
-
|
|
CCR
|
Cancer
|
|
ZL-1218 is a selective humanized IgG1 antibody, targeting CCR8. ZL-1218 induces antibody-dependent cellular cytotoxicity (ADCC), leading to NK cell-mediated depletion of CCR8-expressing regulatory T cells (Tregs). ZL-1218 blocks the binding of the CCR8 ligand CCL1 to CCR8 and reduces Treg recruitment by inhibiting the chemotaxis of CCR8 + cells. ZL-1218 reduces intratumoral Treg levels in a dose-dependent manner. ZL-1218 exerts enhanced antitumor activity when combined with the anti-PD-1 antibody. ZL-1218 can be used for solid tumour research .
|
-
(5)
-
- HY-P992448
-
|
|
PD-1/PD-L1
|
Cancer
|
|
RC98 is a monoclonal antibody targeting programmed cell death ligand 1 (PD-L1) and acts as a selective PD-L1 inhibitor. RC98 binds specifically to human and cynomolgus monkey PD-L1. RC98 blocks the interaction between PD-L1 and its receptor PD-1 to reverse T-cell inactivation mediated by PD-1/PD-L1 signaling. RC98 enhances the cytotoxic T-lymphocyte-mediated anti-tumor immune response against PD-L1-expressing tumor cells. RC98 can be used for the research of tumor immunity and solid tumors .
|
-
(5)
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-129905
-
-
-
- HY-129905A
-
-
-
- HY-N0069
-
-
-
- HY-N3017
-
-
-
- HY-N6784
-
|
|
Structural Classification
Microorganisms
Antifungal
Macrolide Antibiotics
Antibiotics
Disease Research
Source Classification
|
ATP Synthase
Bacterial
Apoptosis
Antibiotic
|
|
Oligomycin B is an antibiotic that acts as a non-selective inhibitor of ATP Synthase. Oligomycin B increases mitochondrial membrane potential. Oligomycin B induces apoptosis and necrosis. Oligomycin B impairs the motility of Plasmopara viticola zoospores and induces their lysis. Oligomycin B inhibits Magnaporthe oryzae (wheat blast fungus) and suppresses the development of wheat blast. Oligomycin B reduces hyphal growth and spore germination of Botrytis cinerea, and protects Arabidopsis thaliana against Botrytis cinerea infection. Oligomycin B exacerbates cytotoxic brain edema in rats with cerebral cortical contusion, increases intracranial pressure and brain water content, and aggravates mitochondrial damage in these rats. Oligomycin B is used in studies related to grape downy mildew, traumatic brain injury, wheat blast, and gray mold .
|
-
-
- HY-N6642
-
-
-
- HY-W010451
-
|
Hydroxyhydroquinone
|
Cardiovascular Disease
Microorganisms
Classification of Application Fields
Phenols
Polyphenols
Disease Research Fields
Source Classification
|
PERK
Eukaryotic Initiation Factor (eIF)
Potassium Channel
Apoptosis
|
|
1,2,4-Trihydroxybenzene (Hydroxyhydroquinone) is an ER stress inducer that targets proteins such as PKR-like ER kinase PERK to induce cytotoxicity. 1,2,4-Trihydroxybenzene selectively activates eIF2α phosphorylation, activates the PERK-eIF2α signaling pathway and induces stress granule formation. 1,2,4-Trihydroxybenzene subsequently exacerbates oxidative stress and causes DNA double-strand breaks, destroying organelles such as mitochondria and ER, and inducing cell death. 1,2,4-Trihydroxybenzene also has the potential to exhibit anti-tumor effect, increase blood pressure, and relieve spasm .
|
-
-
- HY-N1039A
-
-
-
- HY-121382
-
-
-
- HY-N3434
-
-
-
- HY-125938
-
|
Cycloartenol ferulate; Cycloartenol ferulic acid ester
|
Triterpenes
Monophenols
other families
Classification of Application Fields
Terpenoids
Phenols
Plants
Inflammation/Immunology
Disease Research Fields
Source Classification
|
Drug Derivative
Apoptosis
Reactive Oxygen Species (ROS)
JAK
STAT
|
|
Cycloartenyl ferulate (Cycloartenol ferulate; Cycloartenol ferulic acid ester) is a derivative of γ-oryzanol (HY-B2194) with multiple biological activities including antioxidant, anti-inflammatory, and anti-tumor properties. Cycloartenyl ferulate selectively binds to IFNγR1 (binding affinity Kd = 0.5 μM) to activate the canonical JAK1/2-STAT1 signaling pathway. Cycloartenyl ferulate inhibits paraquat (PQ)-triggered apoptosis and ROS in HK2 cells. Cycloartenyl ferulate enhances the activation and cytolytic activity of natural killer (NK) cells by upregulating the expression of NK cell activation receptors (NKG2D, NKp30, NKp44) and the release of cytotoxic molecules and cytokine IFNγ. Cycloartenyl ferulate exerts anti-cancer effects in tumor mice models. Cycloartenyl ferulate can be used for the study of cancer and allergic inflammation intervention .
|
-
-
- HY-N7183
-
|
|
Structural Classification
Alkaloids
Simaroubaceae
Other Alkaloids
Plants
Source Classification
|
NF-κB
GSK-3
β-catenin
Wnt
|
|
9-Hydroxycanthin-6-one is a β-carboline alkaloid. 9-Hydroxycanthin-6-one can be isolated from the roots of E. longifolia. 9-Hydroxycanthin-6-one inhibits TNF-α-induced activation of the NF-κB pathway. 9-Hydroxycanthin-6-one activates GSK3β independently of CK1α, drives phosphorylation and degradation of β-catenin, and inhibits the Wnt signaling pathway. 9-Hydroxycanthin-6-one exerts selective cytotoxicity against Wnt-dependent colon cancer cells. 9-Hydroxycanthin-6-one can be used in studies related to colon cancer .
|
-
-
- HY-111402
-
|
Erizomycin; NSC 246134
|
Natural Products
Microorganisms
Source Classification
|
Bacterial
Antibiotic
|
|
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-158721
-
|
Marinamide
|
Structural Classification
Alkaloids
Microorganisms
Indole Alkaloids
Source Classification
|
Endogenous Metabolite
Parasite
|
|
Penicinoline (Marinamide) (Compound 1), a pyrrolyl 4-quinolinone alkaloid, is a microbial secondary metabolite. Penicinoline can be isolated from endophytic fungus Penicillium sp. Penicinoline has antimalarial activity against Chloroquine (HY-17589A) sensitive strain (pf3d7) and against Chloroquine resistant strain (pfDd2) of plasmodium falciparum. Penicinoline also has strong insecticidal activity against Aphis gossypii and selective anticancer effect with significant cytotoxicity for 95-D and HepG2 cells .
|
-
-
- HY-142908
-
-
-
- HY-N9737
-
-
-
- HY-N3065
-
-
-
- HY-N3113
-
-
-
- HY-N10491
-
|
|
Microorganisms
Diterpenoids
Source Classification
|
P-glycoprotein
|
|
Spongionellol A is a MDR1 (p-glycoprotein) inhibitor. Spongionellol A has high cytotoxic activity and selectivity in prostate cancer cells by inducing caspase‑dependent apoptosis. Spongionellol A can be used in the research of cancers, such as prostate cancer .
|
-
-
- HY-N11919
-
-
-
- HY-N10492
-
|
|
Microorganisms
Diterpenoids
Source Classification
|
P-glycoprotein
|
|
Spongionellol A analog 1, an analog of Spongionellol A (HY-10491), is a MDR1 (p-glycoprotein) inhibitor. Spongionellol A analog 1 has high cytotoxic activity and selectivity in prostate cancer cells by inducing caspase?dependent apoptosis. Spongionellol A analog 1 can be used in the research of cancers, such as prostate cancer .
|
-
-
- HY-N10132
-
-
-
- HY-175427
-
|
|
Microorganisms
Macrolide Antibiotics
Antibiotics
Source Classification
|
Bacterial
Antibiotic
|
|
Amycolatopsin C is a glycosylated macrolactone with antibacterial activity. Amycolatopsin C selectively inhibits the growth of Mycobacterium bovis (BCG) and Mycobacterium tuberculosis (H37Rv) compared to other Gram-positive and Gram-negative bacteria. Amycolatopsin C demonstrates low levels of cytotoxicity toward mammalian cells and can be utilized in antibacterial research .
|
-
-
- HY-N0069R
-
-
-
- HY-121382R
-
|
|
Triterpenes
Structural Classification
Terpenoids
Plants
Caryophyllaceae
Source Classification
Gypsophila perfoliata Linn.
|
Reference Standards
Apoptosis
Cholinesterase (ChE)
Necroptosis
|
|
Cinosulfuron (Standard) is the analytical standard of Cinosulfuron. This product is intended for research and analytical applications. Gypsogenin is a selective mixed-type BChE inhibitor (Ki=19.99 μM) that also exhibits significant cytotoxicity against various human cancer cell lines. Gypsogenin inhibits tumor growth by inducing cell cycle arrest and triggering apoptosis. Gypsogenin displays antibacterial activity against bacteria such as Bacillus subtilis and Bacillus thuringiensis, and often serves as a key parent nucleus for the synthesis of anticancer compounds. Gypsogenin is widely used in research on Alzheimer's disease and various cancers including colon cancer, melanoma, and leukemia .
|
-
-
- HY-W010451R
-
|
Hydroxyhydroquinone (Standard)
|
Structural Classification
Microorganisms
Phenols
Polyphenols
Source Classification
|
Reference Standards
PERK
Potassium Channel
Apoptosis
Eukaryotic Initiation Factor (eIF)
|
|
1,2,4-Trihydroxybenzene (Hydroxyhydroquinone) (Standard) is the analytical standard of 1,2,4-Trihydroxybenzene (HY-W010451). This product is intended for research and analytical applications. 1,2,4-Trihydroxybenzene (Hydroxyhydroquinone) is an ER stress inducer that targets proteins such as PKR-like ER kinase PERK to induce cytotoxicity. 1,2,4-Trihydroxybenzene selectively activates eIF2α phosphorylation, activates the PERK-eIF2α signaling pathway and induces stress granule formation. 1,2,4-Trihydroxybenzene subsequently exacerbates oxidative stress and causes DNA double-strand breaks, destroying organelles such as mitochondria and ER, and inducing cell death. 1,2,4-Trihydroxybenzene also has the potential to exhibit anti-tumor effect, increase blood pressure, and relieve spasm .
|
-
-
- HY-123724
-
-
-
- HY-N16734
-
-
-
- HY-N2332
-
-
-
- HY-N9674
-
-
-
- HY-N18126
-
-
-
- HY-N13838
-
|
|
Triterpenes
Structural Classification
Pongamia pinnata (L.) Pierre
Terpenoids
Plants
Compositae
Source Classification
|
Bacterial
|
|
8,9-Dehydro-7,9-diisobutyryloxythymol is a Thymol (HY-N6810) derivative, as well as an antibacterial agent. 8,9-Dehydro-7,9-diisobutyryloxythymol can be found in the aerial parts of Ageratina adenophora, with selective activity against Gram-positive bacterial strains including Bacillus cereus. 8,9-Dehydro-7,9-diisobutyryloxythymol does not exhibit detectable in vitro cytotoxic activity against human cancer cell lines. 8,9-Dehydro-7,9-diisobutyryloxythymol can be used for the research of bacterial infection .
|
-
-
- HY-N17778
-
|
|
Structural Classification
Flavonols
Flavonoids
Leguminosae
Genista corsica (Loisel.) DC.
Plants
Source Classification
|
Others
|
|
(2R,3R)-7,3',4'-Trihydroxy-5-methoxy-flavanonol is a flavonoid and a selective inhibitor of human liver cancer cell growth, with an IC50 of 38.6 μg/mL (121.5 μM). (2R,3R)-7,3',4'-Trihydroxy-5-methoxy-flavanonol inhibits cancer cell growth with dose-dependent cytotoxic activity, and its anticancer activity is comparable to that of Cisplatin (HY-17394). (2R,3R)-7,3',4'-Trihydroxy-5-methoxy-flavanonol can be used in research on liver cancer and other types of cancer.
|
-
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-15582S
-
|
|
|
Auristatin E-d8 is the deuterium labeled Auristatin E (HY-15582). Auristatin E is a cytotoxic microtubule polymerization inhibitor with potent and selective antitumor activity. Auristatin E is a cytotoxin in antibody-drug conjugates (ADC). Auristatin E inhibits cell division by blocking the polymerisation of tubulin, promising for research in B-cell malignancies. Auristatin E, a synthetic analogue of the Dolastatin 10 (HY-15580), is linear peptides comprised of four amino acids .
|
-
-
- HY-W751180
-
|
|
|
3-Hydroxy Midostaurin- 13C6 (CGP52421- 13C6) is the 13C-labeled 3-Hydroxy Midostaurin (HY-108263). 3-Hydroxy Midostaurin (CGP 52421), a metabolite of PKC412, effectively inhibits FMS-like tyrosine kinase-3 (FLT3) autophosphorylation with IC50s of approximately 132 nM and 9.8 μM in culture medium and plasma, respectively. 3-Hydroxy Midostaurin is less selective but more cytotoxic than PKC412 .
|
-
| Cat. No. |
Product Name |
|
Classification |
-
- HY-151738
-
|
|
|
Azide
|
|
Fmoc-Aeg(N3)-OH is a click chemistry reagent containing an Azide. Alkylating the Nitrogen of an amide bond results in peptoid structures, which leads to conformational restrains, like N-methylation and allows backbone derivatisation. Altering cytotoxicity, bacterial cell selectivity and receptor pharmacology through formation of peptoid derivatives have been published for Cilengitide, Piscidin 1, and MC3, MC4 and MC5 receptor agonist. This building block enables design of macrocycles through intermolecular crosslinking or backbone stabilization through intermolecular ring-closure. This compound is a potential building block for the construction of (customized) peptide nucleic acids (PNAs) and for peptoid synthesis . Fmoc-Aeg(N3)-OH 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-159511
-
|
|
|
Azide
|
|
Hedgehog IN-7 (Compound 8g), a purine derivative, acts as an inhibitor of Hedgehog, capable of reducing the expression of Hedgehog genes and inhibiting Hedgehog signaling. Hedgehog IN-7 has significant cytotoxicity and selectivity towards the Hedgehog pathway-dependent pancreatic cancer cell Mia-PaCa-2 cells and can be used in the research of pancreatic cancer .
|
-
- HY-P11757
-
|
|
|
Azide
|
|
Cyclo[K(N3)larllt] is a seven-membered cyclic peptide targeting EGFR, with a Kd value of 5.09 μM, and exhibits binding selectivity toward homologous proteins HER2 and HER3. Cyclo[K(N3)larllt] has no cytotoxicity and shows no growth inhibitory effect on cancer cells overexpressing EGFR. Cyclo[K(N3)larllt] can serve as a ligand for EGFR-targeted fluorescent conjugates, which is applicable to the detection of cancers with EGFR overexpression. Cyclo[K(N3)larllt] can be used in the research of colorectal cancer .
|
| Cat. No. |
Product Name |
|
Classification |
-
- HY-142118
-
|
AP 12009
|
|
Antisense Oligonucleotides
|
|
Trabedersen (AP 12009) is an orally active synthetic antisense phosphorothioate oligodeoxynucleotide that selectively targets human TGFβ2 mRNA. Trabedersen blocks TGFβ2 protein production, enters the nucleus without a transfection vector, and exerts dose-dependent antitumor effects. By reversing TGFβ2-induced immunosuppression and enhancing immune cytotoxicity, Trabedersen exhibits significant antiproliferative, antimigratory, and antimetastatic activities, with favorable safety profiles. Trabedersen is widely used in research related to various solid tumors, including anaplastic astrocytoma, glioblastoma, colorectal tumor, and melanoma .
|
-
- HY-142118A
-
|
AP 12009 sodium
|
|
Antisense Oligonucleotides
|
|
Trabedersen (AP 12009) sodium is an orally active synthetic antisense phosphorothioate oligodeoxynucleotide that selectively targets human TGFβ2 mRNA. Trabedersen sodium blocks TGFβ2 protein production, enters the nucleus without a transfection vector, and exerts dose-dependent antitumor effects. By reversing TGFβ2-induced immunosuppression and enhancing immune cytotoxicity, Trabedersen sodium exhibits significant antiproliferative, antimigratory, and antimetastatic activities, with favorable safety profiles. Trabedersen sodium is widely used in research related to various solid tumors, including anaplastic astrocytoma, glioblastoma, colorectal tumor, and melanoma .
|
-
- HY-148170
-
|
|
|
Nucleoside Analogs
Uridine
|
|
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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![Cyclo[K(N3)larllt]](http://file.medchemexpress.com/product_pic/hy-p11757.gif)
