Search Result
Results for "
A549
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
7
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-160927
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Drug Derivative
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Cancer
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Docosahexaenoyl Serinol (Compound 1) inhibits proliferation of lung cancaer cells A549, with 77.4% inhibition rate at 3 μM .
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- HY-172116
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- HY-146105
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Apoptosis
MDM-2/p53
MMP
Bcl-2 Family
Reactive Oxygen Species
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Cancer
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Anticancer agent 65 (compound 4c) shows excellent activity in cancer cell lines, especially A549 cells, with an IC50 of 1.07 μM. Anticancer agent 65 induces S-phase arrest in A549 cells and increases the expression level of p53 and p21. Anticancer agent 65 causes apoptosis, ROS generation and collapse of MMP in A549 cells .
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- HY-169370
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- HY-126422
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Others
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Cancer
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cis-Tiliroside, a kaempferol derivative, is a flavonoid glycoside. cis-Tiliroside exhibits better cytotoxic activity than trans-Tiliroside in A549 cell line .
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- HY-149890
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Apoptosis
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Cancer
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Anticancer agent 130 (compound 8d) is an anticancer agent that can significantly induce apoptosis in A549 cells .
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- HY-162745
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PROTACs
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Cancer
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SMARCA2 degrader-20 is a PROTAC SMARCA2 degrader with a DC50 less than 100 nM in A549 cells .
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- HY-P1935
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- HY-145314
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Integrin
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Cancer
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TC113 is a c(RGDyK)-Based conjugate of Gemcitabine (GEM). TC113 could be internalized by A549 cells through integrin αvβ3. TC113 shows potent antiproliferative properties against WM266.4 and A549 cells .
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- HY-170568
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Microtubule/Tubulin
Apoptosis
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Cancer
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Tubulin polymerization-IN-73 (Compound 37) is an inhibitor for microtubule polymerization with an IC50 of 1.8 μM. Tubulin polymerization-IN-73 arrests the cell cycle at G2/M phase, induces apoptosis in A549 cell, inhibits the proliferation of A549 WT and A549/T resistant cell with IC50 of 0.023 μM and 0.057 μM. Tubulin polymerization-IN-73 exhibits antitumor efficacy in mouse model .
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- HY-162614
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PD-1/PD-L1
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Cancer
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Rogersonin E can be isolated from an Ophiocordyceps-associated fungus, Clonostachys rogersoniana. Rogersonin E downregulates the expression of PD-L1 protein in MDA-MB-231 and A549 cells .
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- HY-N11470
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Others
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Cancer
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1,1′-Disinomenine is an alkaloid that can be isolated from the stems of Sinomenium acutum. 1,1′-Disinomenine shows weak inhibition against A549 and Hela cells .
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- HY-173007
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Akt
PI3K
Anaplastic lymphoma kinase (ALK)
CDK
Apoptosis
Mitochondrial Metabolism
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Cancer
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ALK/PI3K/AKT-IN-1 (Compound 45) inhibits the proliferation of cancer cell A549, H1975 and PC9 with an IC50 of 0.44, 0.83 and 1.51 μM. ALK/PI3K/AKT-IN-1 increases the expression of p21 and p27, inhibits the activity of CDK2 and p-Rb, arrests the cell cycle at G1 phase. ALK/PI3K/AKT-IN-1 inhibits the ALK/PI3K/AKT signaling pathway, promotes the depolarization of mitochondrial membrane potential, and inducing apoptosis in A549 cell. ALK/PI3K/AKT-IN-1 inhibits the formation and growth of A549 cell spheroids .
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- HY-156453
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PAK
Apoptosis
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Cancer
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PAK4-IN-3(compound 27e) is aPAK4inhibitor, with theIC50of 10 nM.PAK4-IN-3shows antiproliferative activity against A549 cells with anIC50value of 0.61μM, and inducesapoptosisof A549 cells in a concentration-dependent manner and blocked the cell cycle at phase G0/G1 .
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- HY-169273
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PROTACs
SWI/SNF Complex
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Cancer
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PROTAC SMARCA2 degrader-22 (Compound 5) is a PROTAC degrader for SMARCA2 with a degradation efficacy of 94% at 100 nM. PROTAC SMARCA2 degrader-22 inhibits the proliferation of cell A549 with an EC50 < 250 nM .
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- HY-145865
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Apoptosis
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Cancer
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Antiproliferative against-3 (comp 33) shows a prominent activity against Hela (IC50 = 0.21 µM), A549 (IC50 = 0.39 µM), and MCF-7 (IC50 = 0.33 µM), respectively. Antiproliferative against-3 (comp 33) also dose dependently induces apoptosis by arresting A549 cells at G1 phase .
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- HY-W548095
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Drug Derivative
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Cancer
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Anticancer agent 170 (compound 3a) is a keton derivative of Deguelin (HY-13425), and shows potency anti-cancer activity against A549, with the IC50 of 6.62 μM .
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- HY-N7585
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Others
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Others
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Ustusolate C is a drimane sesquiterpene that can be isolated from Aspergillus ustus 094102
. Ustusolate C exhibits moderate cytotoxicity against A549 cells with an IC50 of 10.5 μM .
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- HY-146274
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c-Met/HGFR
Apoptosis
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Cancer
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c-Met-IN-10 (compound 26a) is a highly potent c-Met kinase inhibitor with an IC50 value of 16 nM. c-Met-IN-10 has inhibitory activity against cancer cells A549, H460 and HT-29 with IC50s of 0.56 ~ 1.59 μM. c-Met-IN-10 suppresses the colony formation on HT-29 cells, induces HT-29 and A549 cells apoptosis, and inhibits A549 cells motility. c-Met-IN-10 can be used for researching anticancer .
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- HY-163920
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PROTACs
HDAC
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Cancer
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Degrader-1 (compound Z16) is a potent and selective HDAC8 PROTAC degrader with an DC50 of 0.27 nM in A549 cells .
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- HY-147027
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PARP
Caspase
Apoptosis
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Cancer
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PARP-1-IN-2 (compound 11g) is a potent and BBB-penetrated PARP1 inhibitor, with an IC50 of 149 nM. PARP1-IN-2 shows significantly potent anti-proliferative activity against Human lung adenocarcinoma epithelial cell line A549. PARP1-IN-2 can induce A549 cells apoptosis .
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- HY-172194
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CDK
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Cancer
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CDK7-IN-33 (Compound 148) is the inhibitor for CDK7 with a Ki of 21.75 nM. CDK7-IN-33 inhibits the proliferation of CDK7 WT expressing A549 with pIC50 of 7.37 .
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- HY-155396
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PROTACs
HDAC
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Cancer
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PRO-HD1 is a PROTAC HDAC6 degrader. PRO-HD1 degrades HDAC6 in A549 cells, and inhibits proliferation of Jurkat cells (IC50: 5.8 μM) .
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- HY-162956
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SARS-CoV
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Infection
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SARS-CoV-2-IN-97 (Compound CO-01) is an inhibitor for SARS-CoV-2 Nsp15 endoribonuclease with an IC50 of 53.5 μM. SARS-CoV-2-IN-97 exhibits low cytotoxicity in A549-AT cell with IC50 of 134 μM .
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- HY-149839
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Apoptosis
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Cancer
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Antitumor agent-112 (compound 3a) is a potent antitumor agent. Antitumor agent-112 induces apoptosis. Antitumor agent-112 has cytotoxic activity on A549 cells with an IC50 value of 91.35 μM .
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- HY-145363
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Integrin
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Cancer
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Sulodexide (pIC50 = 8.2 nM) selectively binds to the αvβ5 integrin in K562 and A549 cell lines and exhibits a significant inhibitory effect .
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- HY-N3687
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Others
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Cancer
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Dasycarpol (compound 2) is a product of microbial transformation of fraxinellone by Aspergillus niger (AS 3.421). Dasycarpol shows moderate cytotoxicity against A549 cells ,with the IC50 of 20 ug/mL .
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- HY-169272
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PROTACs
Epigenetic Reader Domain
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Cancer
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PROTAC SMARCA2 degrader-21 (Compound I-5) is a PROTAC degrader for SMARCA, that degrades SMARCA2 with a DC50 of 10-50 nM in A549 cell, and degrades SMARCA2 and SMARCA4 in MV411 with DC50 of <1 nM and >100 nM, respectively .
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- HY-N10201
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Endogenous Metabolite
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Cancer
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Cytoglobosin C, a cytochalasan derivative, shows potent cytotoxicity against both SGC-7901 and A549 cell lines (IC50<10 μM) .
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- HY-N4029
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Others
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Cancer
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Humulene oxide II is an essential oil component from Zingiber striolatum Diels flowers, leaves and stems. Humulene oxide II has cytotoxicity against A549, PC-3 and K562 cell lines .
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- HY-146462
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Apoptosis
ROS Kinase
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Cancer
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Anticancer agent 59 (compound 11) has inhibitory activity against kinds of cancer cell lines, especially in A549 with IC50 of 0.2 μM. Anticancer agent 59 induces apoptosis and an increase of Ca 2+ and ROS in cancer cells. Anticancer agent 59 significantly decreases mitochondrial membrane potential. Anticancer agent 59 can suppress tumor growth in A549 mouse xenograft model .
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- HY-170559
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EGFR
Apoptosis
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Cancer
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EGFR-IN-141 (Compound 8I) is the inhibitor for EGFR with an IC50 of 2.67 nM. EGFR-IN-141 exhibits cytotoxicity in cancer cell A549 with an IC50 of 13.75 μM. EGFR-IN-141 induces apoptosis and mitochondrial membrane depolarization, and exhibits potential antitumor efficacy .
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- HY-N2199
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Apoptosis
Autophagy
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Cancer
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Sotetsuflavone is a flavonoid that can be isolated from Cycas revolute. Sotetsuflavone inhibits migration and invasion of A549 cells by reversing EMT, and induces cell apoptosis and autophagy. Sotetsuflavone inhibits HIF-1α, VEGF, angiostatin, MMP-9, and MMP-13 expression in A549 cells. Sotetsuflavone also protects mice against Crohn's disease (CD)-like colitis. Sotetsuflavone can be used for research of NSCLC .
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- HY-154978
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Others
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Cancer
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Cisplatin-resistant cells-IN-1 (Compound 8) has high cytotoxicity against Cisplatin (HY-17394)-resistant cells. Cisplatin-resistant cells-IN-1 reduces the metabolic activity effectively in the low nanomolar range (IC50: 0.14–1.79 μM in A549/A549-R, K562/K562-R, and MCF-7/MCF-7TamR cells) .
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- HY-156033
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EGFR
Apoptosis
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Cancer
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EGFR-IN-88 (Compound 4i) is an EGFR inhibitor (IC50: 87 nM). EGFR-IN-88 shows cytotoxicity against A549 cell with an IC50? of 3.902? μM. EGFR-IN-88 can induce cell apoptosis .
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- HY-N7589
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Carolignan M
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Others
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Cancer
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Demethylcarolignan E is a phenylpropanoid ester that can be isolated from the stems of Hibiscus taiwanensi. Demethylcarolignan E has cytotoxicity against human cancer lines A549 and MCF-7 (IC50: <10 μg/mL) .
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- HY-169270
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Epigenetic Reader Domain
PROTACs
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Cancer
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PROTAC SMARCA2 degrader-19 (Compound 46) is a PROTAC degrader for SMARCA2, that degrades SMARCA2 in cell A549 and MV411 with a DC50 < 100 nM. PROTAC SMARCA2 degrader-19 degrades SMARCA4 in cell MV411 with a DC50 > 1000 nM .
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- HY-N2429
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COX
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Inflammation/Immunology
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Sphondin possesses an inhibitory effect on IL-1β-induced increase in the level of COX-2 protein and PGE2 release in A549 cells .
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- HY-N10082
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Others
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Cancer
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Trigoxyphin A is a oxygenated daphnane-type diterpenoids. Trigoxyphin A exhibites strong cytotoxic activity against HL60 and A549 with IC50s of 0.27 and 7.5 μM, respectively .
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- HY-161891
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EGFR
Akt
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Cancer
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EGFR/Akt-IN-1 (compound 17) is a potent inhibitor of EGFR/Akt, with the IC50s of 12.89 μM and 10.88 μM in A549 cells, respectively. EGFR/Akt-IN-1 arrestes the cell cycle at the S phase .
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- HY-172110
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EGFR
Akt
p38 MAPK
ERK
Apoptosis
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Cancer
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Apoptosis inducer 35 (Compound 6) is a multi-targeted inhibitor, that reduces the expressions of EGFR, AKT, ERK and P38-MAPKα. Apoptosis inducer 35 inhibits the proliferation of cancer cell A549 and Jurkat, arrests the cell cycle at S phase, and induces apoptosis .
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- HY-163713
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SARS-CoV
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Infection
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SARS-CoV-2-IN-89 (Compound 2) is a SARS-CoV-2 inhibitor. SARS-CoV-2-IN-89 enhances IFN-I responses to SARS-CoV-2 infection in A549.hACE2 cells .
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- HY-N8025
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Others
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Cancer
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Nephthenol is a terpenoid that can be isolated from Nephthea brassica. Nephthenol exhibits cytotoxicity in cells A549, HT-29, KB and P-388 with IC50s of 2.72, 3.01, 1.84, and 0.42 µg/mL, respectively .
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- HY-152147
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PROTACs
HDAC
Apoptosis
DNA/RNA Synthesis
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Cancer
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SZUH280 is a potent and selective PROTAC HDAC8 degrader with a DC50 of 0.58 μM in A549 cells. SZUH280 induces cancer cell apoptosis. SZUH280 hampers DNA damage repair in cancer cells, promoting cellular radiosensitization .
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- HY-75564
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Endogenous Metabolite
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Cancer
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Cyclo(Ala-Gly), a metabolite of a mangrove endophytic fungus, Penicillium thomi, exhibits cytotoxicity against A549, HepG2 and HT29 cells. The IC50 values range from 9.5 to 18.1 μM .
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- HY-N11912
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Biochemical Assay Reagents
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Cancer
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Soladulcoside A is a steroidal glycoside and antineoplastic agent that can be obtained from the whole plant of Solanum nigrum. Soladulcoside A can inhibit A549 cells and has the potential to study cancers such as non-small cell lung cancer (NSCLC) .
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- HY-156355
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Others
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Cancer
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Sec61-IN-5 (Compound 16c) is a Sec61 inhibitor. Sec61 shows cytotoxicity in A549 cells (IC50: 0.27 nM). Sec61-IN-5 inhibits Sec61-dependent secretory function (IC50: 0.08 nM) .
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- HY-156110
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Insulin Receptor
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Cancer
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IGF2BP1-IN-1 (Compound A11) is a IGF2BP1 inhibitor and inhibits downstream signaling. IGF2BP1-IN-1 binds to IGF2BP1 protein with a KD value of 2.88 nM. IGF2BP1-IN-1 inhibits cancer cells proliferation (IC50: 9 nM for A549 cell, 34 nM for HCT116). IGF2BP1-IN-1 induces cancer cell apoptosis. GF2BP1-IN-1 inhibits tumor growth in A549 xenograft mouse model .
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- HY-168236
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PROTACs
Epigenetic Reader Domain
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Cancer
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PROTAC SMARCA2 degrader-28 (Compound 158) is a PROTAC degrader for SMARCA2, that degrades SMARCA2 with a DC50 of 3 nM in HiBiT A549 cells. (Pink: Ligand for target protein (HY-168237); Black: Linker (HY-168238); Blue: Ligand for E3 ligase (HY-W087383))
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- HY-170549
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VEGFR
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Cancer
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VEGFR-2-IN-60 (compound 5c) is a potent VEGFR-2 inhibitor with an IC50 of 1.07 nM. VEGFR-2-IN-60 exhibits cytotoxic activity against HCC1806, Hela, and A549 cell lines .
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- HY-W471938
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Drug Derivative
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Cancer
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Antiproliferative agent-35 (Compound 4) is an anticancer agent derivated from Esculetin (HY-N0284). Antiproliferative agent-35 inhibits the proliferation of B16 and A549 cells, with IC50s of 13.2 and 9.2 μM resspectively .
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- HY-130624
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HSP
Apoptosis
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Cancer
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Hsp90-Cdc37-IN-2 (Compound 41) is an inhibitor for the interaction between heat shock protein 90 (Hsp90) and cyclin 37 (Cdc37). Hsp90-Cdc37-IN-2 inhibits the proliferation of cancer cell A549, MCF-7, HOS and HepG2 with IC50 of 0.41-0.94 μM. Hsp90-Cdc37-IN-2 decreases the mitochondrial membrane potential, induces apoptosis, and arrest cell cycle at G0/G1 phase in A549 .
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- HY-131344
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mTOR
Autophagy
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Cancer
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mTOR inhibitor-8 is an mTOR inhibitor and autophagy inducer. mTOR inhibitor-8 inhibits the activity of mTOR via FKBP12 and induces autophagy of A549 human lung cancer cells .
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- HY-155200
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EGFR
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Cancer
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EGFR-IN-84 (Compound 6g) is an EGFR inhibitor (IC50: 24 nM). EGFR-IN-84 inhibits A549 cell growth (IC50: 1.537 μM). EGFR-IN-84 can be used for research of lung cancer .
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- HY-149842
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Akt
Apoptosis
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Cancer
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AKT-IN-18, an inhibitor of Akt, inhibits Akt with an IC50 of 69.45 μΜ in A549 cells. AKT-IN-18 induces apoptosis and can be used in non-small cell lung cancer study .
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- HY-156878
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Others
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Cancer
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Antiproliferative agent-39 (Compound 12) inhibits proliferation of A549, SNU-638, Col2, HT1080, MCF-7 with IC50s of 11, 25, 14, 11, 6.3 μM respectively .
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- HY-157402
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Topoisomerase
EGFR
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Cancer
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Topoisomerase II/EGFR-IN-1 is topoisomerase II/EGFR dual inhibitor. Topoisomerase II/EGFR-IN-1 has superior cytotoxic activity to MCF-7, A549 and HCT-116 cell lines, displays strong apoptotic activity and can be used for the research of cancer .
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- HY-126841
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Photosensitizer
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Cancer
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5-Methoxysterigmatocystin is a mycotoxin with cytotoxic and genotoxic properties. 5-Methoxysterigmatocystin exhibits cytotoxicity against cancer cells A549 and HepG2 (IC50 of 5.5 and 0.7 μM), and induces DNA damage. 5-Methoxysterigmatocystin is a photosensitizer, which utilizes the visible to generate singlet oxygen ( 1O2) .
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- HY-164389
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Ras
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Cancer
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SML-10-70-1 is a ligand for RAS, which covalently modifies the K-Ras G12C mutant protein, and inhibits the phosphorylation of ERK and Akt. SML-10-70-1 inhibits the proliferation of cancer cells H23, H358 and A549 with IC50 of 26.6-47.6 μM .
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- HY-N4048
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Others
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Cancer
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Heudelotinone is a dinorditerpenoid that can be isolated from the stem bark and roots of Ricinodendron heudelotii. Heudelotinone shows cytotoxicity against SMMC-7721, A549 and Hela cells with IC50s of 21.68, 16.04 and 10.67 μM, respectively .
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- HY-162891
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EGFR
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Cancer
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EGFR-IN-123 (compound D06) is a potent EGFR inhibitor. EGFR-IN-123 inhibits PC-9G, A549, A431 and HCT116 cells with IC50s of 0.74, 1.36, 1.20 and 2.53 μM, respectively .
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- HY-115960
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Others
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Cancer
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Anticancer agent 35 (compound 10), a sulfonylurea derivative, is a potent anticancer agent. Anticancer agent 35 inhibits A549, A431, PACA2 cell growth with IC50s of 18.1 µg/mL, 4.0 µg/mL, 18.9 µg/mL, respectively .
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- HY-163692
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Microtubule/Tubulin
Apoptosis
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Cancer
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Tubulin polymerization-IN-64 (Compound 8a) is an inhibitor for tubulin polymerization by occupying the colchicine binding site of tubulin, with IC50 of 6.9 μM. Tubulin polymerization-IN-64 inhibits proliferations of cancer cells A549, HeLa, HCT116 and HT-29, with IC50s of 2.42, 10.33, 6.28, 5.33 μM, respectively. Tubulin polymerization-IN-64 arrests cell cycle at G2/M phase, induces apoptosis in A549 .
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- HY-N12563
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c-Myc
Apoptosis
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Cancer
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γ-Sitosterol is an inhibitor for c-Myc. γ-Sitosterol inhibits the proliferation of cancer cell MCF-7 and A549 with IC50 of 240.73 μg/mL and 696.6 μg/mL, arrests the cell cycle at G2/M phase, and induces apoptosis. γ-Sitosterol upregulates the expression of cell cycle regulators cyclin B/E .
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- HY-162034
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FAK
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Cancer
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FAK-IN-17 is a focal adhesion kinase (FAK) inhibitor. FAK-IN-17 possesses anticancer activity against A549 and MDA-MB-231 cell lines with IC50 values of 130 nM and 94 nM .
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- HY-147882
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Bacterial
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Infection
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Anti-MRSA agent 6 (compound 3q6) is a potent anti-methicillin-resistant Staphylococcus aureus (anti-MRSA) agent. Anti-MRSA agent 6 shows low cytoxicity for MCF-7, A549 cells .
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- HY-158429
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PROTACs
Cytochrome P450
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Cancer
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PROTAC CYP1B1 degrader-2 (compound PV2) is a von Hippel-Landau (VHL) E3 ligase-based CYP1B1 degrader with the DC50 of 1.0 nM at 24 h in A549/Taxol cells. PROTAC CYP1B1 degrader-2 inhibits growth, migration, and invasion of A549/Taxol cell(Sturcture Note:(Blue: VHL ligand (HY-112078), Black: linker (HY-W007700), Pink: CYP1B1 ligand (HY-159006) .
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- HY-149840
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Apoptosis
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Cancer
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Antitumor agent-113 shows cytotoxic effects on A549 cells with IC50 value of 46.60 μM and induces apoptosis. Antitumor agent-113 can be used in non-small cell lung cancer study .
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- HY-145861
-
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Histone Demethylase
Apoptosis
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Cancer
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LSD1-IN-14 is a potent and selective LSD1 inhibitor (IC50=0.89 μM). LSD1-IN-14 can significantly inhibit the proliferation of A549 and THP-1 cells and induce the apoptosis of tumor cells .
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- HY-158436
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Microtubule/Tubulin
Autophagy
Apoptosis
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Cancer
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Antitumor agent-155 (Compound 13) inhibits microtubule polymerization, induces autophagy and apoptosis. Antitumor agent-155 shows cytotoxicity against HCT116, A549, AGS, SK-MES-1 cells with IC50s of 0.227, 0.253, 0.574, 0.423 μM respectively .
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- HY-161403
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Cytochrome P450
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Cancer
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CYP1B1-IN-8 (Compound 14b) is a CYP1B1 inhibitor (IC50: 4.14 × 10 –5 nM). CYP1B1-IN-8 reduces the resistance in A549 cells to Paclitaxel (HY-B0015), and inhibits cell migration and invasion .
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- HY-118528
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TGF-β Receptor
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Cancer
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TP0427736 is a selective inhibitor of ALK5 with an IC50 of 2.72 nM. TP0427736 inhibits Smad2/3 phosphorylation in A549 cells. TP0427736 decreases the growth inhibition of human outer root sheath cells .
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- HY-168607
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TGF-beta/Smad
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Cancer
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ALK5-IN-83 (compound 13b) is a ALK5 inhibitor with the IC50 of 0.13 μM. ALK5-IN-83 inhibits TGF-β1-induced Smad2 phosphorylation and cell motility in A549 cells .
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- HY-172397
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Bacterial
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Infection
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Mycobacterium Tuberculosis-IN-7 (Compound 4c) inhibits M. tuberculosis H37Ra with MIC of 5.34 μg/mL. Mycobacterium Tuberculosis-IN-7 exhibits slight cytotoxicity in cancer cell Vero, A549, and HepG2 (IC50s >50 μM) .
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- HY-162885
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Proteasome
JAK
STAT
Interleukin Related
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Cancer
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YSY01A is a proteasome inhibitor that can suppress cancer cell survival by inducing apoptosis (Apoptosis). Its IC50 values are 51.0 nM for HEK293T, 9.2 nM for A549, 5.2 nM for MCF-7, 8.9 nM for MGC-803, and 35.4 nM for PC-3M cells. Additionally, YSY01A eliminates constitutive STAT3 signaling by downregulating gp130 and JAK2 in human A549 lung cancer cells. YSY01A holds promise for research in the field of cancer therapy .
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-
- HY-124429
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ERK
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Cancer
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FQI1 is a Late SV40 Factor (LSF) inhibitor. FQI1 inhibits cell proliferation, with IC50s of 3, 0.79, 6.3 μM for NIH/3T3, HeLa, A549 cells. FQI1 can be used for cancer research .
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- HY-144394
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Apoptosis
c-Met/HGFR
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Cancer
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Antitumor agent-45 (Compound 21) could induce and stimulate A549 cells apoptosis in G0/G1 and G2/M phase. Antitumor agent-45 (Compound 21) inhibits c-Met expression to regulate the growth of tumor cells .
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- HY-163880
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EGFR
Ras
p38 MAPK
Reactive Oxygen Species
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Cancer
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EGFR-IN-119 (Compound 5l) is an inhibitor for EGFR with an IC50 of 84.3 nM. EGFR-IN-119 inhibits the cytotoxicity in lung cancer cell A549 with an IC50 of 1.34 μM. EGFR-IN-119 downregulates the expressions of EGFR, KRAS, and MAP2K genes, exhibits antioxidant activity through reduction of reactive oxygen species (ROS), and hyperpolarizes the mitochondrial membrane potential .
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- HY-158019
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DNA/RNA Synthesis
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Cancer
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Anticancer agent 196 (compound 1) shows cell cytotoxicity with IC50 values of 7.69 µM and 54.2 µM for HL-60 cells and A549 cells, respectively. Anticancer agent 196 can induce DNA damage .
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- HY-172211
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Amylases
Glycosidase
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Metabolic Disease
Cancer
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α-Amylase/α-Glucosidase-IN-17 (Compound 3) is an inhibitor of α-amylase and α-glucosidase, with IC50 values of 14.61 μM and 25.38 μM, respectively. α-Amylase/α-Glucosidase-IN-17 has certain inhibitory activity against A549 cancer cells. α-Amylase/α-Glucosidase-IN-17 has anti-tumor and anti-diabetic effects .
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- HY-158020
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DNA/RNA Synthesis
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Cancer
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Anticancer agent 197 (compound 2b) shows cell cytotoxicity with IC50 values of 10.03 µM and 73.54 µM for HL-60 cells and A549 cells, respectively. Anticancer agent 197 can induce DNA damage .
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- HY-115941
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HDAC
Microtubule/Tubulin
Apoptosis
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Cancer
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HDAC-IN-9 is a potent and selective tubulin and HDAC dual inhibitor. HDAC-IN-9 inhibits the invasion and migration of A549 cells. HDAC-IN-9 shows potent antitumor and antiangiogenic effect in vitro and in vivo .
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- HY-147030
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PARP
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Cancer
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PARP1-IN-8 (compound 11c) is a potent and BBB-penetrated PARP1 inhibitor, with an IC50 of 97 nM. PARP1-IN-8 shows significantly potent anti-proliferative activity against Human lung adenocarcinoma epithelial cell line A549 .
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-
- HY-162342
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Topoisomerase
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Cancer
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Topoisomerase I inhibitor 14 (Compound 4h) is an inhibitor for Topoisomerase I. Topoisomerase I inhibitor 14 inhibits proliferation of A549 and C6 with IC50s of 4.56 μM and 13.17 μM, without significant toxicity in healthy cells NIH3T3 (IC50 is 74.44 μM), which exhibits anticancer potency .
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- HY-N7980
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NF-κB
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Cancer
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Rubipodanone A, a naphthohydroquinone dimer, shows cytotoxicity against A549, BEL-7402, HeLa, HepG2, SGC-7901 and U251 cells. Rubipodanone A also shows obvious activating effect at 20 and 40 μM for NF-κB .
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- HY-129334
-
|
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Telomerase
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Cancer
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Macrocalin B is a diterpenoid, which can be isolated from Isodon xerophilus. Macrocalin B inhibits the proliferation of cancer cells K562, HL-60, A549, MKN, CA and HCT with IC50 of 2.81-171 μM. Macrocalin B inhibits the telomerase in K562 with an IC50 in nanomolar level .
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- HY-W159754
-
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p-Hydroxyallylbenzene
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Cholinesterase (ChE)
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Cancer
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Chavicol (p-Hydroxyallylbenzene, compound 6) can inhibit acetylcholinesterase (Cholinesterase (ChE)), with an IC50 of 7.42 μM. Chavicol has anti-cancer activity and can suppress the growth, survival, migration, and invasion of cancer cells. Chavicol cytotoxic effect is significant, approximately 31 μg/mL in A-549 cells .
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- HY-18200A
-
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E5555 hydrochloride; ER-172594-00 hydrochloride
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Protease Activated Receptor (PAR)
JAK
Apoptosis
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Cardiovascular Disease
Cancer
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Atopaxar hydrochloride (E5555 hydrochloride) is the hydrochloride salt form of Atopaxar (HY-18200). Atopaxar hydrochloride is an orally active, selective and reversible antagonist for thrombin receptor protease-activated receptor-1 (PAR-1). Atopaxar hydrochloride is the inhibitor for Janus kinase 1 (JAK1) and JAK2, which inhibits the JAK-STAT with EC50 of 5.90 μM in A549. Atopaxar hydrochloride inhibits the cell viability of A549 (IC50=7.02 μM), arrests the cell cycle at G1 phase and induces apoptosis. Atopaxar hydrochloride exhibits antiplatelet and antitumor activities. Atopaxar hydrochloride can be used for the research of atherothrombotic disease .
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- HY-P3397A
-
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GHSR
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Cancer
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JV-1-36 acetate is a growth hormone-releasing hormone (GHRH) antagonist. JV-1-36 acetate inhibits the production of reactive oxygen species in A549 lung cancer cells. JV-1-36 can be used to study the effect of GHRH antagonists in vitro .
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- HY-146319
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- HY-P3397
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GHSR
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Cancer
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JV-1-36 is a growth hormone-releasing hormone (GHRH) antagonist. JV-1-36 inhibits the production of reactive oxygen species in A549 lung cancer cells. JV-1-36 can be used to study the effect of GHRH antagonists in vitro .
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-
- HY-159576
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O-Me B1939; O-Me E7389; O-Me ER-086526
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ADC Cytotoxin
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Cancer
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O-Me Eribulin is a derivative of Eribulin and is an ADC cytotoxin that can be used for ADC synthesis. O-Me Eribulin can inhibit the cell viability of SKBR3, MDA-MB-468, and A549 cells, with IC50 values of 0.2052, 0.1827, and 0.5151 nM, respectively. O-Me Eribulin can be used for tumor research .
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- HY-172112
-
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VEGFR
Apoptosis
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Cancer
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VEGFR-2-IN-64 (Compound 28) is the inhibitor for VEGFR2 with IC50 of 27.8 nM. VEGFR-2-IN-64 inhibits the proliferation of cancer cell A549, T-47D and Caco-2, exhibits anti-migration and anti-cloning activities in cell T-47D, induces apoptosis in T-47D .
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- HY-159176
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Cytochrome P450
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Cancer
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Antitumor agent-183 (compound 3f) has antitumor activity with metabolic stability. Antitumor agent-183 inhibits cancer cell growth, with IC50s less than 5 nM for A549, HCT116, and HS578T cells. The albumin-bound nanoparticle formulation of Antitumor agent-183 has prolonged retention in the tumor tissues .
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- HY-161863
-
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Microtubule/Tubulin
Reactive Oxygen Species
Apoptosis
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Cancer
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Tubulin polymerization-IN-67 (Compound 5h) is an inhibitor for tubulin polymerization on colchicine binding site with an IC50 of 2.92 μM. Tubulin polymerization-IN-67 inhibits the proliferation of cancer cells HT29, A549, U2OS, MG-63 and HeLa with IC50s of 0.12-4.13 μM. Tubulin polymerization-IN-67 arrests the cell cycle at G2/M phase, induces apoptosis in cell U2OS, inhibits the cell migration of A549. Tubulin polymerization-IN-67 reduces the mitochondrial membrane potential (MMP) and increase intracellular ROS, inhibits the angiogenesis in HUVECs. Tubulin polymerization-IN-67 exhibits antitumor efficacy in mice
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- HY-163198
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ASCT
mTOR
Apoptosis
Autophagy
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Cancer
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ASCT2-IN-1 (compound 20k) is an ASCT2 inhibitor with IC50 values of 5.6 μM and 3.5 μM in cells A549 and HEK293, respectively. ASCT2-IN-1 induces cell apoptosis. ASCT2-IN-1 inhibits tumor growth .
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- HY-161654
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PROTACs
Ras
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Cancer
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PROTAC SOS1 degrader-10 (Compound 11o) is a degrader for son of sevenless 1 (SOS1) in a CRBN and proteasome dependent manner. PROTAC SOS1 degrader-10 degrades SOS1 in KRAS mutant cancer cells SW620, A549 and DLD-1, with DC50s of 2.23, 1.85 and 7.53 nM, respectively. PROTAC SOS1 degrader-10 inhibits the proliferations of cells SW620, A549 and DLD-1, with IC50s of 36.7, 52.2 and 107 nM, respectively. PROTAC SOS1 degrader-10 inhibits phosphorylation of ERK. (Pink: SOS1 ligand (HY-161655); Black: linker (HY-161656); Blue: E3 ligase ligand (HY-W249500))
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- HY-N10853
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Others
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Cancer
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3′,5-Dihydroxy-4′,6,7-trimethoxyflavanone is a nature product that could be isolated from the fruits of Vitex rotundifolia. 3′,5-Dihydroxy-4′,6,7-trimethoxyflavanone has potent cytotoxic activity against A549 and HepG-2 cell lines .
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-
- HY-147538
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Apoptosis
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Cancer
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|
Antitumor agent-64 (Compound 8d) is a diosgenin derivative. Antitumor agent-64 exhibits potent cytotoxic activity against A549 cell line. Antitumor agent-64 induces A549 cells apoptosis via the mitochondria-related pathway .
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- HY-N10965
-
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Others
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Cancer
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Gambogic acid B is an active compound. Gambogic acid B can be isolated from the resin of Garcinia hanburyi.. Gambogic acid B has cytotoxicity against A549, HCT116 and MDA‑MB‑231 cells with IC50 values of 1.60 μM, 6.88 μM and 0.87 μM, respectively .
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-
- HY-157564
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Apoptosis
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Cancer
|
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Antitumor agent-135 (Compound 13) is a potent antitumor agent. Antitumor agent-135 induces cell apoptosis, with IC50s of 3.79 , 10.55, 1.14, and 4.14 μM for NSCLC cell lines (A549, H460, PC-9, and PC-9/GR) .
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-
- HY-142945
-
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Ras
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Cancer
|
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KRAS G12C inhibitor 43 (compound 59) is a potent KRAS G12C inhibitor. KRAS G12C inhibitor 43 shows antimigration and anti-proliferative activity with IC50s of 0.001-1 µM, >1 µM, >1 µM for H358, A549, HCC cells ,respectively .
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-
- HY-159123
-
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MAP4K
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Cancer
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KHK-6 is an inhibitor for serine/threonine kinase hematopoietic progenitor kinase 1 (HPK 1) with an IC50 of 20 nM. KHK-6 enhances CD3/CD28-induced cytokine production, enhances CD69, CD25 and HLA-DR markers on CD4+ and CD8+ T cells, and enhances T cell-mediated killing activity of SKOV3 and A549 cells .
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-
- HY-161284
-
|
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MMP
|
Cancer
|
|
MMP-9/10-IN-1 (Compound 6b) is a potent dual MMP-9/10 Inhibotor with IC50s of 0.076 and 0.139 μM against NSCLC and A549 cells, respectively. MMP-9/10-IN-1 has anti-invasive and anti-angiogenic activities when in combination with Sorafenib (HY-10201) .
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-
- HY-161450
-
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PROTACs
Ras
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Cancer
|
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LHF418 is an effective SOS1 PROTAC degrader with a DC50 value of 209.4 nM in A549 cells. LHF418 can effectively inhibit RAS signaling and colony formation in KRAS-driven cancer cells. (Structural note: (Blue: Cereblon ligand (HY-A0003), Black: linker; Pink: SOS1 binder SOS1 Ligand intermediate-3 (HY-161452)) .
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- HY-115983
-
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CD47
Apoptosis
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Cancer
|
|
DMUP is a potent CD47-SIRPα axis inhibitor. DMUP induces apoptosis and increases the macrophage phagocytosis in A549 cells. DMUP decreases the expression of CD47 and SIRPα protein. DMUP shows antitumor activity .
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-
- HY-155359
-
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Microtubule/Tubulin
|
Cancer
|
|
Tubulin polymerization-IN-55 is a potent inhibitor of Tubulin Polymerization. Tubulin polymerization-IN-55 has antiproliferative activity against A549, K562, HepG2, MDA-MB-231 and HFL-1 with IC50 s of 8, 3, 9, 24 and 62 nM, respectively .
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-
- HY-159449
-
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PROTACs
Epigenetic Reader Domain
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Cancer
|
|
PROTAC SMARCA2 degrader-5 (Compound I-425) is a PROTAC degrader for catalytic subunit of the SWI/SNF complex SMARCA2. PROTAC SMARCA2 degrader-5 degrades SMARCA2 in MV411 and in A549 with DC50 <100 nM, degrades SMARCA4 with DC50 of 100-500 nM . (Pink: Ligand for target protein (HY-159531); Black: Linker (HY-159538); Blue: Ligand for E3 ligase (S,R,S)-AHPC (HY-125845))
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-
- HY-157413
-
|
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EGFR
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Cancer
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|
YS-67 is a potent inhibitor of EGFR with an IC 50 of 5.2 nM. YS-67 significantly inhibits p-EGFR and p-AKT. YS-67 inhibits the proliferation of A549, PC-9, and A431cells with IC 50s of 4.1, 0.5, and 2.1 μM, respectively .
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-
- HY-138537
-
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IKK
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Cancer
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|
NF-κB-IN-1, a 4-arylidene crucumin analogue, is a potent NF-κB signaling pathway inhibitor. NF-κB-IN-1 directly inhibits IKK to block NF-κB activation. NF-κB-IN-1 effectively inhibits the viability of lung cancer cells and attenuates the clonogenic activity of A549 cells .
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-
- HY-N0985
-
|
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Others
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Cancer
|
|
1,4,5,6-Tetrahydroxy-7,8-diprenylxanthone is a xanthone that can be isolated from Garcinia xanthochymus. 1,4,5,6-Tetrahydroxy-7,8-diprenylxanthone shows moderate cytotoxicities against MDA-MB-435S and A549 cell lines with IC50s of 1.3 and 3.86 μg/ml, respectively .
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-
- HY-147862
-
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EGFR
Apoptosis
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Cancer
|
|
EGFR-IN-62 (compound 9h) is a potent and reversible EGFR kinase inhibitor, with IC50 values of 10 nM (L858R/T790 M), 29 nM (WT), and 242 nM (L858R/T790 M/C797S), respectively. EGFR-IN-62 shows antiproliferative activity against A549 and H1975 cell lines, with IC50 values of 2.53 and 1.56 μM, respectively. EGFR-IN-62 induces dose-dependent apoptosis process, G1/G0-phase arrestation, and the inhibition of motility on A549 and/or H1975 cell lines .
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-
- HY-P3116
-
|
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Bacterial
|
Cancer
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|
Thiocoraline is a depsipeptide that can be isolated by marine Micromonospora. Thiocoraline has antitumor activity with IC50s of 0.002, 0.002, 0.01 and 0.002 μg/mL in P388, A549, HT-29 and MEL-28 cells, respectively. Thiocoraline also a strong antimicrobial activity against Gram-positive microorganisms .
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-
- HY-163871
-
|
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PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
PROTAC SMARCA2/4-degrader-18 (Compound I-348) is a PROTAC degrader for catalytic subunit of the SWI/SNF complex SMARCA2 and SMARCA4. PROTAC SMARCA2/4-degrader-18 degrades SMARCA2 in A549 with DC50 <100 nM, degrades SMARCA4 in MV411 with DC50 <100 nM. (Pink: Ligand for Target Protein (HY-159531); Black: Linker (HY-76547); Blue: Ligand for E3 Ligase (HY-125845))
|
-
- HY-163870
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
PROTAC SMARCA2/4-degrader-17 (Compound I-345) is a PROTAC degrader for catalytic subunit of the SWI/SNF complex SMARCA2 and SMARCA4. PROTAC SMARCA2/4-degrader-17 degrades SMARCA2 in A549 with DC50 <100 nM, degrades SMARCA4 in MV411 with DC50 <100 nM. (Pink: Ligand for Target Protein (HY-159545); Black: Linker (HY-W053507); Blue: Ligand for E3 Ligase (HY-125845))
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-
- HY-162743
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
PROTAC SMARCA2/4-degrader-29 (Compound I-279) is a PROTAC degrader for catalytic subunit of the SWI/SNF complex SMARCA2 and SMARCA4. PROTAC SMARCA2/4-degrader-29 degrades SMARCA2 in A549 with DC50 <100 nM, degrades SMARCA4 in MV411 with DC50 <100 nM. (Pink: ligand for target protein (HY-163926); Black: linker (HY-159682); Blue: ligand for E3 ligase (HY-W382038)) .
|
-
- HY-162744
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
PROTAC SMARCA2/4-degrader-31 (Compound I-280) is a degrader for catalytic subunit of the SWI/SNF complex SMARCA2 and SMARCA4. PROTAC SMARCA2/4-degrader-31 degrades SMARCA2 in A549 with DC50 <100 nM, degrades SMARCA4 in MV411 with DC50 <100 nM. (Pink: Ligand for target protein (HY-163926); Black: Linker (HY-159682); Blue: Ligand for E3 ligase (HY-W382038)) .
|
-
- HY-163868
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
PROTAC SMARCA2/4-degrader-15 (Compound I-335) is a PROTAC degrader for catalytic subunit of the SWI/SNF complex SMARCA2 and SMARCA4. PROTAC SMARCA2/4-degrader-15 degrades SMARCA2 in A549 with DC50 <100 nM, degrades SMARCA4 in MV411 with DC50 <100 nM. (Pink: Ligand for Target Protein (HY-159545); Black: Linker (HY-N3024); Blue: Ligand for E3 Ligase (HY-125845))
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-
- HY-W778562
-
|
|
Others
|
Cancer
|
|
10-Deacetyl-13-oxobaccatin III is an taxane that can be isolated from Taxus sumatrana. 10-Deacetyl-13-oxobaccatin III (30 μg/mL) shows cytotoxicity against A498, NCI-H226, A549, PC-3 cells, with inhibition a rate of 29.7%, 49.2%, 43.9%, 65.3% .
|
-
- HY-146061
-
|
|
Ras
|
Cancer
|
|
KRAS G12C inhibitor 48 (compound 6e) is a potent KRAS G12C inhibitor with an IC50 of 639.91 nM. KRAS G12C inhibitor 48 (0-50 µM) shows anti-proliferative activity with IC50s of 0.796, 6.33, 16.14 µM for H358, H23, A549 cells, respectively .
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-
- HY-158090
-
|
|
Others
|
Cancer
|
|
Triptolide palmitate is the derivative of Triptolide (HY-32735). Triptolide palmitate exhibits cytotoxicity against cancer cell MCF-7 and A549, with IC50 of 7.5 and 6.4 μM. Triptolide palmitate exhibits a half-time T1/2 of 50.4 min in Sprague Dawley rats. Triptolide palmitate can be utilizd as drug carrier .
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-
- HY-139425
-
-
- HY-161668
-
|
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Ligands for E3 Ligase
Ferroptosis
|
Cancer
|
|
Ru-Poma is a Ru(II)-based photosensitizer, which attenuates Cisplatin (HY-17394)-resistant tumor through photodynamic therapy (PDT). Ru-Poma photodegrades CRBN through a Pomalidomide (HY-10984) moiety. Ru-Poma induces ferroptosis, through an increase in lipid peroxide, downregulation of GPX4 and GAPDH expression. Ru-Poma exhibits cytotoxicity in A549, with IC50 of 18.46 μM and 0.37 μM in dark and upon irradiation, respectively .
|
-
- HY-162601
-
|
|
Histone Methyltransferase
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
D-01 is a dual-targeting inhibitor of HIF-1α and EZH2 (IC50: 4.86 μM and 0.99 μM respectively). D-01 inhibits the expression of H3K27me3 protein. D-01 inhibits the migration, clone and the invasion of A549 cells, and also inhibits tube formation of HUVECs. D-01 can be used for research of lung cancer .
|
-
- HY-163877
-
|
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PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
PROTAC SMARCA2/4-degrader-19 (Compound I-412) is a PROTAC degrader for catalytic subunit of the SWI/SNF complex SMARCA2 and SMARCA4. PROTAC SMARCA2/4-degrader-19 degrades SMARCA2 in MV411 and in A549 with DC50 <100 nM, degrades SMARCA4 in MV411 with DC50 <100 nM. (Pink: Ligand for Target Protein (HY-163949); Black: Linker (HY-W006635); Blue: Ligand for E3 Ligase (HY-125845))
|
-
- HY-163873
-
|
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PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
PROTAC SMARCA2/4-degrader-20 (Compound I-405) is a PROTAC degrader for catalytic subunit of the SWI/SNF complex SMARCA2. PROTAC SMARCA2/4-degrader-20 degrades SMARCA2 in A549 and MV411 with DC50 <100 nM, degrades SMARCA4 in MV411 with DC50 of 100-500 nM. (Pink: Ligand for Target Protein (HY-159545); Black: Linker (HY-W006635); Blue: Ligand for E3 Ligase (HY-163932))
|
-
- HY-159461
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
PROTAC SMARCA2/4-degrader-9 (Compound I-503) is a PROTAC degrader for catalytic subunit of the SWI/SNF complex SMARCA2 and SMARCA4. PROTAC SMARCA2 degrader-9 degrades SMARCA2 in MV411 and in A549 with DC50 <100 nM, degrades SMARCA4 in MV411 with DC50 <100 nM . (Pink: Ligand for target protein (HY-159545); Black: Linker (HY-W006635); Blue: Ligand for E3 ligase (S,R,S)-AHPC (HY-125845))
|
-
- HY-162748
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
PROTAC SMARCA2/4-degrader-30 (Compound I-291) is a PROTAC degrader for catalytic subunit of the SWI/SNF complex SMARCA2 and SMARCA4. PROTAC SMARCA2/4-degrader-30 degrades SMARCA2 in A549 and in MV411 with DC50 <100 nM, degrades SMARCA4 in MV411 with DC50 <100 nM. (Pink: ligand for target protein (HY-163926); Black: linker (HY-159684); Blue: ligand for E3 ligase (HY-W382038)) .
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-
- HY-115947
-
|
|
Drug Derivative
|
Cancer
|
|
Anticancer agent 33 (compound 3), a Squamocin and Bullatacin derivative, is a potent anticancer agent. Anticancer agent 33 shows high potency to inhibit 4T1 breast cancer cell line (A549, HeLa, HepG2 and MCF-7 cells) growth with IC50s of 1.9-5.4 µM .
|
-
- HY-B1014
-
-
- HY-149352
-
|
|
Thymidylate Synthase
|
Cancer
|
|
DG1 (Compound 8Nc) is a Thymidylate Synthase (TS) inhibitor that affects cancer angiogenesis and metabolic reprogramming in NSCLC cells. DG1 can effectively inhibit the expression of CD26, ET-1, FGF-1 and EGF. DG1 also effectively inhibits the proliferation of cancer tissue in the A549 xenograft mouse model .
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-
- HY-N10208
-
|
|
Endogenous Metabolite
|
Cancer
|
|
Aspericin C is a pyran derivative found in the marine-derived fungus Rhizopus sp. 2-PDA-61. Aspericin C shows cytotoxic activities against P388, A549, HL-60, and BEL-7420 cell lines (IC50=14.6, 7.1, 61.4, and 24.2 μM, respectively) .
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-
- HY-143301
-
|
|
Topoisomerase
|
Cancer
|
|
Topoisomerase I inhibitor 4 (compound 7a) is a topoisomerase I inhibitor. Topoisomerase I inhibitor 4 inhibits HepG2, A549, MCF-7 and HeLa cancer cells proliferation with IC50s of 1.20, 2.09, 1.56 and 1.92 μM, respectively. Topoisomerase I inhibitor 4 can be used for the research of cancer .
|
-
- HY-168247
-
|
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PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
PROTAC BRM/BRG1 degrader-2 (Example.004) is a PROTAC BRM/BRG1 degrader (DC50: < 10 nM in A549 cell; IC50: 15 nM for A549). Blue: E3 ligase ligand (HY-112078), Black: linker (HY-168249), Pink: BRM/BRG1 inhibitor (HY-168248) .
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-
- HY-155039
-
|
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Drug Derivative
|
Cancer
|
|
Antitumor agent-105 (Compound 37) is an antitumor agent. Antitumor agent-105 has antitumor activity against A549, H1299, H460, HCT116, MDA-MB-231 cells, with IC50 values of 6.7, 8.3, 4.3, 4.4, 6.7 μM respectively .
|
-
- HY-145963
-
|
|
GLUT
|
Cancer
|
|
DRB18 is a potent pan-class GLUT inhibitor. DRB18 alters energy-related metabolism in A549 cells by changing the abundance of metabolites in glucose-related pathways. DRB18 can eventually lead to G1/S phase arrest and increase oxidative stress and necrotic cell death. DRB18 has anti-tumor activity .
|
-
- HY-N8954
-
|
|
Others
|
Cancer
|
|
Kaempferol 7-O-neohesperidoside is a ?avonoid glycoside that can be isolated from Litchi chinensis. Kaempferol 7-O-neohesperidoside exhibits significant cytotoxic activity against A549, LAC, Hep-G2, and HeLa cell lines with IC50s of 0.53, 7.93, 0.020, and 0.051 μM, respectively .
|
-
- HY-168300
-
|
|
Reactive Oxygen Species
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Antiangiogenic agent 7 (Compound 1) can induce cell apoptosis, increase Reactive Oxygen Species, and inhibit the intracellular enzyme thioredoxin reductase. Antiangiogenic agent 7 has anti-cancer activity, with an IC50 of 0.08-3.5 μM against cervical cancer cells HeLa, prostate cancer cells PC-3, and non-small cell lung cancer A549. Antiangiogenic agent 7 inhibits tumor growth in mouse xenograft models .
|
-
- HY-159455
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
PROTAC SMARCA2/4-degrader-4 (Compound I-434) is a PROTAC degrader for catalytic subunit of the SWI/SNF complex SMARCA2 and SMARCA4. PROTAC SMARCA2/4-degrader-4 degrades SMARCA2 in MV411 and in A549 with DC50 <100 nM, degrades SMARCA4 in MV411 with DC50 <100 nM. (Pink: Ligand for target protein (HY-159472); Black: Linker (HY-159478); Blue: Ligand for E3 ligase (S,R,S)-AHPC (HY-125845))
|
-
- HY-159456
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
PROTAC SMARCA2/4-degrader-5 (Compound I-437) is a PROTAC degrader for catalytic subunit of the SWI/SNF complex SMARCA2 and SMARCA4. PROTAC SMARCA2/4-degrader-5 degrades SMARCA2 in MV411 and in A549 with DC50 <100 nM, degrades SMARCA4 in MV411 with DC50 of 100-500 nM. (Pink: Ligand for target protein (HY-159545); Black: Linker (HY-159557); Blue: Ligand for E3 ligase (S,R,S)-AHPC (HY-125845))
|
-
- HY-159460
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
PROTAC SMARCA2/4-degrader-8 (Compound I-502) is a PROTAC degrader for catalytic subunit of the SWI/SNF complex SMARCA2. PROTAC SMARCA2/4-degrader-8 degrades SMARCA2 with DC50 <100 nM in A549 and in MV411, degrades SMARCA4 with DC50<100 nM in MV411(Pink: Ligand for target protein (HY-159545); Black: Linker (HY-W063924); Blue: Ligand for E3 ligase (S,R,S)-AHPC (HY-125845))
|
-
- 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-169262
-
|
|
Phospholipase
Apoptosis
|
Cancer
|
|
PLD-IN-1 (Compound 3r) is an orally active inhibitor for phospholipase D with an IC50 of 1.97 μM. PLD-IN-1 reduces the expression of CD24, CD47 and PD-L1, enhances the calreticulin expression, and thus modulates the immune evasion mechanism in lung cancer cells by promoting the phagocytosis of cancer cells by macrophages. PLD-IN-1 inhibits the cell viability of lung cancer cell A549, HCC44, H460 and HCC15 with IC50 of 18.44, 22.31, 24.85 and 21.45 μM, respectively. PLD-IN-1 can induce apoptosis and inhibits migration in cell A549. PLD-IN-1 enhances the level of pro-inflammatory M1 macrophages and decreases the level of anti-inflammatory M2 macrophages, exhibits antitumor efficacy in mouse model .
|
-
- HY-W011391
-
|
|
Apoptosis
ASCT
|
Cancer
|
|
GPNA hydrochloride is a well known substrate of the enzyme γ-glutamyltransferase (GGT). GPNA hydrochloride is a specific glutamine (Gln) transporter ASCT2 inhibitor. GPNA hydrochloride also inhibit Na +-dependent carriers, such as SNAT family (SNAT1/2/4/5), and the Na +-independent leucine transporters LAT1/2. GPNA reversibly induces apoptosis in A549 cells .
|
-
- HY-170653
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
Anticancer agent 262 (compound 3h) is a DNA intercalating anticancer agent, with an IC50 of 5.7 µM against A549 cancer cells .
|
-
- HY-129765
-
|
|
Reactive Oxygen Species
|
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-130723
-
|
|
AMPK
|
Cancer
|
|
AMPK activator 2 (compound 7a), a fluorine-containing proguanil derivative, up-regulates AMPK signal pathway and downregulates mTOR/4EBP1/p70S6K. AMPK activator 2 inhibits proliferation and migration of human cancer cell lines (UMUC3, T24, A549) .
|
-
- HY-N13139
-
|
|
Others
|
Cancer
|
|
Dexylosyltubeimoside Ⅲ (compound 3) is a cyclic disoside that can be isolated from Actinostemma lobatum MAXIM. Dexylosyltubeimoside Ⅲ has in vitro anticancer activity and inhibits the growth of human esophageal cancer cell line ECA109 (IC50=22.37 μM), lung cancer cell line A549 (IC50=27.27 μM) and gastric cancer cell line MGC-803 (IC50=36.85 μM) .
|
-
- HY-159820
-
|
|
Others
|
Cancer
|
|
Veonetinib (example 3) is a potent inhibitor of tyrosine kinase, with the IC50 of 0.1 μM and 0.4 μM in A549 cells and LOVO cells, respectively .
|
-
- HY-116038
-
|
|
Others
|
Cancer
|
|
Kulinone has cytotoxic effects against A549, H460 and HGC27 with IC50 values of 6.2, 7.8, 5.6 μg/mL .
|
-
- HY-103662
-
-
- HY-170813
-
|
|
CDK
|
Infection
|
|
P162-0948 is a selective CDK8 inhibitor with an IC50 value of 50.4 nM. P162-0948 reduces cell migration and protein expression of EMT-related proteins in A549 human alveolar epithelial cell lines. P162-0948 reduces phosphorylation of Smad, which suggests disruption of the TGF-β/Smad signaling pathway. P162-0948 is promising for research of pulmonary fibrosis .
|
-
- HY-152100
-
|
|
Autophagy
|
Cancer
|
|
CUR5g is a potent autophagy inhibitor. CUR5g selectively inhibits autophagosome degradation in cancer cells by blocking autophagosome-lysosome fusion. CUR5g blocks the recruitment of STX17 to autophagosomes via a UVRAG-dependent mechanism, resulting in the inability of autophagosomes to fuse with lysosomes. CUR5g improves the anticancer effect of Cisplatin (HY-17394) against A549 cells both in vitro and in vivo .
|
-
- HY-169409
-
|
|
VEGFR
|
Cancer
|
|
VEGFR-2-IN-59 (Compound 3h) is an inhibitor for VEGFR2 with an IC50 of 3.73 µM. VEGFR-2-IN-59 exhibits cytotoxicity in cancer cell A549, HT-29, A375, MCF7 and NHDF with IC50 of 20.91, 19.70, 9.63, 17.43 and 20.71 μM. VEGFR-2-IN-59 inhibits formation of tubular structure and exhibits anti-angiogenic property .
|
-
- HY-159512
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
EGFR kinase inhibitor 7 (compound 18i) is an EGFR inhibitor (IC50=42.3 nM) with anticancer activity. EGFR kinase inhibitor 7 has significant in vitro cytotoxicity and apoptosis induction ability. EGFR kinase inhibitor 7 has antiproliferative activity against human colon cancer cell line HCT116 and human non-small cell lung cancer cell line A549, with IC50 values of 4.82 µM and 1.43 µM, respectively .
|
-
- HY-N12079
-
|
|
Biochemical Assay Reagents
|
Cancer
|
|
(2,4-Dichloro-3,5-dimethoxyphenyl) methyl 6-O-β-D-glucopyranosyl-β-D-glucopyranoside is an anticancer agent that inhibits the proliferation of lung cancer A549 cells (IC50=29 μΜ). (2,4-Dichloro-3,5-dimethoxyphenyl) methyl 6-O-β-D-glucopyranosyl-β-D-glucopyranoside can be obtained from Lilium regale and can be used in cancer research .
|
-
- HY-135453
-
|
|
Bacterial
|
Infection
|
|
(-)-Pinocembrin exhibits anti-mycobacterium activity against mycobacteriuum tuberculosis H37Ra with an IC50 value of 1.11 mg/mL in dormant phase and 1.21 mg/mL in active phase, respectively. (-)-Pinocembrin has potent antiproliferative activity with IC50 values of 1.88-11.00 mg/mL against THP-1, A549, Panc-1, HeLa and MCF7 cell lines .
|
-
- HY-146543
-
|
|
Ras
|
Cancer
|
|
KRAS inhibitor-13 (compound 5-6) is a potent KRAS G12C inhibitor with an IC50 of 0.883 µM. KRAS inhibitor-13 shows p-ERK inhibition activities with IC50s of 5.9, >100 µM in MIA PaCA-2, A549 cells, respectively. KRAS inhibitor-13 has the potential for the research of pancreatic, colorectal, and lung cancers .
|
-
- HY-143466
-
|
|
FAK
ULK
AMPK
Apoptosis
Autophagy
|
Cancer
|
|
ULK1-IN-2 (compound 3s) is a potent ULK1 inhibitor. ULK1-IN-2 shows highest cytotoxic effect against cancer cell lines, with IC50 of 1.94 μM in A549. ULK1-IN-2 can induce apoptosis and simultaneously block autophagy, and can be used to study NSCLC (Non-small cell lung cancer) .
|
-
- HY-151802
-
|
|
TrxR
|
Cancer
|
|
CPUL1 is a TrxR inhibitor, which shows proliferation-inhibitory and anti-metastatic activity against A549 cells. CPUL1 influences EMT (epithelial-mesenchymal transition) via inducing ROS-mediated ERK/JNK signaling by inhibiting TrxR1 enzyme activity. CPUL1 in combination with α-Lipoic Acid (HY-N0492) or Dithiodipropionic acid (HY-W014395) is more effective .
|
-
- HY-N12364
-
|
|
Others
|
Cancer
|
|
Bufoserotonin C is a new indole alkaloid from the traditional Chinese medicine Chansu that has antitumor activity, with IC 50 of 34.3 μM in A549 cells .
|
-
- HY-N9003
-
|
|
Others
|
Cancer
|
|
Dihydroprehelminthosporol (Compound 1) from the
fungusVeronaea sp.of the separated. Dihydroprehelminthosporol on
human cancer cell line A549 and SK-0A-3 has cytotoxicity .
|
-
- HY-156405
-
|
|
Fat Mass and Obesity-associated Protein (FTO)
Autophagy
|
Metabolic Disease
|
|
FTO-IN-10 (compound 7) is a potent human demethylase FTO (the fat mass and obesity-associated protein) inhibitor with an IC50 of 4.5 μM. FTO-IN-10 enters the FTO’s structural domain II binding pocket through hydrophobic and hydrogen bonding interactions. FTO-IN-10 induces DNA damage and autophagic cell death in A549 cells .
|
-
- HY-155231
-
|
|
Elastase
|
Cancer
|
|
Neutrophil elastase inhibitor 4 (compound 4f) is a competitive human neutrophil elastase (HNE) inhibitor (IC50: 42.30 nM, Ki: 8.04 nM). Neutrophil elastase inhibitor 4 induces T47D cell apoptosis. Neutrophil elastase inhibitor 4 inhibits cell proliferation with IC50s of 21.25, 34.17, 29.93, 99.11 nM for T47D, RPMI 8226, A549, and HSF cells .
|
-
- HY-115959
-
|
|
Bacterial
|
Inflammation/Immunology
Cancer
|
|
Anticancer agent 34 (compound 9), a sulfonylurea derivative, is a potent antimicrobial and anticancer agent. Anticancer agent 34 inhibits the microbial growth of B. mycoides, E. coli, and C. albicans with a MIC between 0.156 and 0.039 mg/ml. Anticancer agent 34 inhibits A549, PC3 cell growth with IC50s of 8.4 µg/ml, 7.8 µg/ml, respectively .
|
-
- HY-115961
-
|
|
Bacterial
|
Inflammation/Immunology
Cancer
|
|
Anticancer agent 36 (compound 11), a sulfonylurea derivative, is a potent antimicrobial and anticancer agent. Anticancer agent 36 inhibits the microbial growth of B. mycoides, E. coli, and C. albicans with a MIC between 0.156 and 0.039 mg/L. Anticancer agent 36 inhibits A549, PC3 cell growth with IC50s of 19.7 µg/mL, 11.9 µg/mL, respectively .
|
-
- HY-146533
-
|
|
Ras
|
Cancer
|
|
KRAS inhibitor-12 (compound 6-1) is a potent KRAS G12C inhibitor with an IC50 of 0.537 µM. KRAS inhibitor-12 shows p-ERK inhibition activities with IC50s of 1.3, 3.7 µM in MIA PaCA-2, A549 cells, respectively. KRAS inhibitor-12 has the potential for the research of pancreatic, colorectal, and lung cancers .
|
-
- HY-146545
-
|
|
Ras
|
Cancer
|
|
KRAS inhibitor-15 (compound 3-19) is a potent KRAS G12C inhibitor with an IC50 of 0.954 µM. KRAS inhibitor-15 shows p-ERK inhibition activities with IC50s of 2.03, >33.3 µM in MIA PaCA-2, A549 cells, respectively. KRAS inhibitor-15 has the potential for the research of pancreatic, colorectal, and lung cancers .
|
-
- HY-146476
-
|
|
Ras
|
Cancer
|
|
KRAS inhibitor-18 (compound 3-10) is a potent KRAS G12C inhibitor with an IC50 of 4.74 µM. KRAS inhibitor-18 shows p-ERK inhibition activities with IC50s of 66.4, 11.1 µM in MIA PaCA-2, A549 cells, respectively. KRAS inhibitor-18 has the potential for the research of pancreatic, colorectal, and lung cancers .
|
-
- HY-146546
-
|
|
Ras
|
Cancer
|
|
KRAS inhibitor-16 (compound 3-11) is a potent KRAS G12C inhibitor with an IC50 of 0.457 µM. KRAS inhibitor-16 shows p-ERK inhibition activities with IC50s of 3.06, 11.1 µM in MIA PaCA-2, A549 cells, respectively. KRAS inhibitor-16 has the potential for the research of pancreatic, colorectal, and lung cancers .
|
-
- HY-146475
-
|
|
Ras
|
Cancer
|
|
KRAS inhibitor-17 (compound 3-9) is a potent KRAS G12C inhibitor with an IC50 of 3.37 µM. KRAS inhibitor-17 shows p-ERK inhibition activities with IC50s of 9.25, >33.3 µM in MIA PaCA-2, A549 cells, respectively. KRAS inhibitor-17 has the potential for the research of pancreatic, colorectal, and lung cancers .
|
-
- HY-146544
-
|
|
Ras
|
Cancer
|
|
KRAS inhibitor-14 (compound 3-22) is a potent KRAS G12C inhibitor with an IC50 of 0.249 µM. KRAS inhibitor-14 shows p-ERK inhibition activities with IC50s of 1.12, >33.3 µM in MIA PaCA-2, A549 cells, respectively. KRAS inhibitor-14 has the potential for the research of pancreatic, colorectal, and lung cancers .
|
-
- HY-147864
-
|
|
c-Fms
c-Kit
Apoptosis
|
Cancer
|
|
c-Fms-IN-12 (Compound 4g) is an FMS kinase inhibitor. c-Fms-IN-12 can also inhibits c-KIT. c-Fms-IN-12 is a potential broad-spectrum anticancer agent against multiple cancer types. c-Fms-IN-12 induces A549 cell apoptosis .
|
-
- HY-163860
-
|
|
EGFR
|
Cancer
|
|
EGFR-TK-IN-3 (3) is an EGFR TK inhibitor, with an IC50 of 2.33 μM against Erlotinib (HY-50896)-resistant A549 cells .
|
-
- HY-N10852
-
|
|
Others
|
Cancer
|
|
Shikokianin, a diterpenoid, shows significant cytotoxicity against HL-60 and A-549 cells with IC50 values of 3.4 μM and 18.8 μM, respectively .
|
-
- HY-163616
-
|
|
Apoptosis
|
Cancer
|
|
Anticancer agent 221 (Compound 4h) is an orally active anticancer agent and an antioxidant agent. Anticancer agent 221 exhibits cytotoxicity to cancer cells A549 (IC50=22.09 µg/mL) and MCF-7 (IC50=6.40 µg/mL), and induces apoptosis. Anticancer agent 221 exhibits antioxidant efficacy with an IC50 of 42.46 μM in DPPH experiment. Anticancer agent 221 exhibits antitumor efficacy against breast cancer in mouse models .
|
-
- HY-N12078
-
|
|
Biochemical Assay Reagents
|
Cancer
|
|
4-Chloro-3-methoxy-5-methylphenyl 6-O-(6-deoxy-β-L-mannopyranosyl)-β-D-glucopyranoside (compound 3) is an anticancer agent and natural product that can effectively inhibit lung cancer proliferation of A549 cells. 4-Chloro-3-methoxy-5-methylphenyl 6-O-(6-deoxy-β-L-mannopyranosyl)-β-D-glucopyranoside is available from Lilium regale and has potential for use in cancer research .
|
-
- HY-120581
-
|
|
PGE synthase
|
Cancer
|
|
ML388 is a potent and selective hydroxyprostaglandin dehydrogenase (HPGD) inhibitor with an IC50 of 34 nM. ML388 induces PGE2 production in A549 cells and LNCaP prostate cancer cells .
|
-
- HY-12757
-
|
|
BCRP
|
Cancer
|
|
YHO-13177, a acrylonitrile derivative, is an orally active, potent and specific inhibitor of breast cancer resistance protein (BCRP) and ABCG2 with an IC50 value of 10 nM. YHO-13177 potentiates the cytotoxicity of SN-38 in HCT116 and A549 cells that express BCRP. YHO-13177 combined with Irinotecan (HY-16562) significantly suppresses the tumor growth in an HCT116/BCRP xenograft model .
|
-
- HY-163691
-
|
|
Carbonic Anhydrase
|
Cancer
|
|
Antitumor agent-163 (Compound 3) is a photosensitizer used in Molecular-Targeted Photodynamic Therapy (MT-PDT) targeting carbonic anhydrase IX (CAIX). Antitumor agent-163 inactivates CAIX protein via singlet oxygen under 540 nm wavelength light, without affecting internal standard proteins such as α-tubulin, β-actin, and proliferating cell nuclear antigen (PCNA). Antitumor agent-163 induces cell membrane damage, inhibits cell viability (IC50 is 0.2 and 0.05 μM for A549 and U87MG). Antitumor agent-163 exhibits antitumor efficacy in mouse model .
|
-
- HY-162341
-
|
|
Topoisomerase
|
Cancer
|
|
Topoisomerase I inhibitor 15 (compound 4b) is an inhibitor of topoisomerase I with anticancer activity. Topoisomerase I inhibitor 15 inhibits A549 cells with an IC50 of 7.34 μM .
|
-
- HY-153259
-
|
|
PARP
|
Cancer
|
TNKS1/2-IN-2 (Compound 21) is a potent and selective tankyrases inhibitor. TNKS1/2-IN-2 exhibits IC50 values of 4 nM and 63 nM against TNK1 and TNK2 in the enzymatic assay, respectively. TNKS1/2-IN-2 inhibits proliferation of A549 and H292 cell lines with IC50 values of 39.5 nM and 12.8 nM, respectively. TNKS1/2-IN-2 can be used for the research of cancer .
|
-
- HY-151901
-
|
|
SARS-CoV
|
Infection
|
|
SARS-CoV-2 Mpro-IN-5 is a dual Inhibitor of Main Protease (M Pro) and Cathepsin L (CatL), with IC50s of 1800 nM and 145 nM respectively. SARS-CoV-2 Mpro-IN-5 has antiviral activity against SARS-CoV2. SARS-CoV-2 Mpro-IN-5 blocks SARS-CoV2 replication in hACE2 expressing A549 cells with IC50 value of 14.7 nM .
|
-
- HY-151900
-
|
|
SARS-CoV
Virus Protease
|
Infection
|
|
SARS-CoV-2 Mpro-IN-4 is a dual Inhibitor of Main Protease (M Pro) and Cathepsin L (CatL), with IC50s of 900 nM and 60 nM respectively. SARS-CoV-2 Mpro-IN-4 has antiviral activity against SARS-CoV2. SARS-CoV-2 Mpro-IN-4 blocks SARS-CoV2 replication in hACE2 expressing A549 cells with IC50 value of 8.2 nM .
|
-
- HY-N6969A
-
|
|
Adrenergic Receptor
|
Cancer
|
|
Dicentrine hydrochloride is a drug with anti-inflammatory and anti-cancer activity. Dicentrine hydrochloride exerts its effects by enhancing TNF-α-induced apoptosis in A549 lung adenocarcinoma cells. Dicentrine hydrochloride increases caspase-8, -9, -3 and poly(ADP-ribose) polymerase (PARP) activities. Dicentrine hydrochloride inhibits TNF-α-induced invasion and migration of A549 cells. Dicentrine hydrochloride significantly inhibited the TNF-α-activated TAK1, p38, JNK and Akt signaling pathways, and reduced the transcriptional activities of NF-κB and AP-1 .
|
-
- HY-N6955
-
|
|
Others
|
Cancer
|
|
Eupalinilide B is a guaiane type sesquiterpene lactone that can be found in Eupatorium lindleyanum. Eupalinilide B shows potent cytotoxicity against P-388 and A-549 tumor cell lines .
|
-
- HY-162108
-
|
|
Apoptosis
|
Cancer
|
|
Antitumor agent-128 (compound 1a) is an antitumor agent that elicits cell cycle arrest in both the G2/M and S phases, triggering apoptosis in A549 cells .
|
-
- HY-N10113
-
|
Muconomycin B
|
Apoptosis
Arenavirus
Fungal
Antibiotic
Reactive Oxygen Species
|
Infection
Cancer
|
|
Verrucarin J (Muconomycin B) is a metabolite of the Myrothecium fungus family. Verrucarin J generates reactive oxygen species (ROS) and induces apoptosis of cancer cell lines, such as A549, HCT 116 and SW-620 cells. Verrucarin J shows activities against Candida albicans and Mucor miehei. Verrucarin J inhibits arenavirus Junin (JUNV) yield with an IC50 of 1.2 ng/mL .
|
-
- HY-146537
-
|
|
Ras
|
Cancer
|
|
KRAS G12C inhibitor 47 (compound 8-1-1) is a potent KRAS G12C inhibitor with an IC50 of 0.172 µM. KRAS G12C inhibitor 47 shows p-ERK inhibition activities with IC50s of 0.046, 69.8 µM in MIA PaCA-2, A549 cells, respectively. KRAS G12C inhibitor 47 has the potential for the research of pancreatic, colorectal, and lung cancers .
|
-
- HY-145291
-
|
|
Topoisomerase
Apoptosis
|
Cancer
|
|
CPT-Se4, a selenoproagent of Camptothecin (CPT), shows improved potency in killing cancer cells and inhibiting tumor growth. CPT-Se4 decreases the GSH/GSSG ratio and total thiols, elevates the ROS level in Hep G2 cells, and eventually induces apoptosis of cancer cells. CPT-Se4 shows cytotoxicity against HeLa, Hep G2, A549, and SMMC-7721 cells (IC50= 2.54-6.4 μM) .
|
-
- HY-155203
-
|
|
Apoptosis
Reactive Oxygen Species
Ferroptosis
|
Cancer
|
|
Anticancer agent 154 (Compound 8h) increases the levels of reactive oxygen species and leads to mitochondrial damage. Anticancer agent 154 induces cell apoptosis and DNA damage. Anticancer agent 154 also induces ferroptosis by reducing the GSH level and GPX4 expression and increasing the lipid peroxidation level. Anticancer agent 154 inhibits cancer cell (HT29, H1975, A549, and MCF-7) proliferation with IC50s of 1.0-1.9 μM .
|
-
- HY-145290
-
|
|
Topoisomerase
Apoptosis
|
Cancer
|
|
CPT-Se3, a selenoproagent of Camptothecin (CPT), shows improved potency in killing cancer cells and inhibiting tumor growth. CPT–Se3 decreases the GSH/GSSG ratio and total thiols, elevates the ROS level in Hep G2 cells, and eventually induces apoptosis of cancer cells. CPT-Se3 shows cytotoxicity against HeLa, Hep G2, A549, and SMMC-7721 cells (IC50= 2.19-4.7 μM) .
|
-
- HY-146715
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
IDO/Tubulin-IN-2 (HT2) is a potent TDO and tubulin inhibitor. IDO/Tubulin-IN-2 also shows potent activity against U87, HepG2, A549, HCT-116, and LO2 cancer cell lines, with IC50 values of 0.43, 0.036, 0.041, 0.095 and 1.04 μM, respectively. IDO/Tubulin-IN-2 remarkably promotes the antitumor activity .
|
-
- HY-N0753
-
|
|
Others
|
Cancer
|
|
Eupalinolide B is a germacrane sesquiterpene isolated from Eupatorium lindleyanum. Eupalinolide B demonstrates potent cytotoxicity against A-549, BGC-823 and HL-60 tumour cell lines .
|
-
- HY-149841
-
|
|
Akt
|
Cancer
|
|
AKT-IN-17 is a AKt inhibitor. AKT-IN-17 inhibits AKt in A549 cells, leading to Apoptosis. AKT-IN-17 can be used in non-small cell lung cancer study .
|
-
- HY-N9101
-
|
|
Others
|
Cancer
|
|
4,4'-Dihydroxy-3,3',9-trimethoxy-9,9'-epoxylignan is a lignans that can be isolated from the Viburnum foetidum. 4,4'-Dihydroxy-3,3',9-trimethoxy-9,9'-epoxylignan has cytotoxicity against A549, SK-OV-3, SKMEL-2 and HCT15 cell line with IC50s of 67.14, 67.38, 64.11 and 76.31 μg/mL, respectively .
|
-
- HY-N1056
-
|
Zerumbetol
|
Others
|
Cancer
|
|
Yunnancoronarin A (Zerumbetol) can be isolated from Hedychium forrestii. Yunnancoronarin A is cytotoxic, with IC50 values of 11.08 and 2.19 μM against lung adenocarcinoma cells A549 and leukemia cells K562, respectively .
|
-
- HY-161628
-
|
|
Topoisomerase
|
Cancer
|
|
Tapcin is a dual inhibitor for topoisomerase I and topoisomerase II, with IC50 of 203 and 71 nM. Tapcin inhibits proliferations of cancer cells A-375, HeLa, Huh7.5, U2-OS, A549, Caco-2 and HT29, with IC50s of 441, 1.04, 40.5, 0.002, 0.006, 0.287 and 0.842 nM, respectively. Tapcin exhibits antitumor activity in HT29 xenograft model .
|
-
- HY-165114
-
|
|
Endogenous Metabolite
|
Cancer
|
|
6-Hydroxyramulosin is a fungal metabolite with antiancer effects. 6-Hydroxyramulosin shows cytotoxic effects against A549 and T24, showing IC50 values of 14.2 µg/mL and 15.3 µg/mL, respectively .
|
-
- HY-111320
-
|
|
Bacterial
Antibiotic
|
Cancer
|
|
Chrysomycin B is an antibiotic isolated from a strain of Streptomyces. Chrysomycin B causes DNA damage in the human lung adenocarcinoma A549 cell line and inhibits topoisomerase II. Chrysomycin B suppresses the growth of transplantable tumors in mice.
|
-
- HY-149390
-
|
|
TrxR
|
Cancer
|
|
TrxR1-IN-1 (Compound 5j) is a TrxR1 inhibitor (IC50: 8.8 μM). TrxR1-IN-1 has anticancer activity, with IC50s of MCF-7 (1.5 μM), HeLa (1.7 μM), BGC-823 (2.4 μM), SW-480 (2.8 μM), A549 (2.1 μM). TrxR1-IN-1 has antioxidant activity, and scavenges DPPH radical .
|
-
- HY-146461
-
|
|
Apoptosis
Caspase
ROS Kinase
|
Cancer
|
|
Anticancer agent 58 (compound 16) has inhibitory activity against kinds of cancer cell lines, especially in A549 and T24 with IC50s of 0.6 μM and 0.7 μM, respectively. Anticancer agent 58 induces apoptosis by activating caspase 3/8/9 activity, and induces an increase of Ca 2+ and ROS in cancer cells. Anticancer agent 58 significantly decreases mitochondrial membrane potential. Anticancer agent 58 can suppress tumor growth in T24 mouse xenograft model .
|
-
- HY-162808
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
GTSE1-IN-1 (compound Y18) is an orally active GTSE1 inhibitor with anticancer activity. GTSE1-IN-1 significantly inhibits cancer cell proliferation by inhibiting the transcription and expression of GTSE1, causing DNA damage and persistently inducing cell cycle arrest and cell senescence. In addition, GTSE1-IN-1 significantly inhibits the adhesion, migration and invasion of colorectal cancer HCT116 cells and non-small cell lung cancer A549 cells in vitro .
|
-
- HY-169403
-
|
|
STAT
Apoptosis
Reactive Oxygen Species
|
Cancer
|
|
NW16 is an orally active inhibitor for STAT3 with Kd of 11.0 μM. NW16 arrests the cell cycle at S phase, induces apoptosis in HCT116, and inhibits the proliferation of cancer cell HCT116, A549, and B16 with IC50s of 0.28, 1.22, and 9.86 μM, respectively. NW16 induces the production of ROS, inhibits the PI3K/AKT signaling pathway, and thus exhibits antitumor efficacy in mouse model .
|
-
- HY-148572
-
|
|
Indoleamine 2,3-Dioxygenase (IDO)
NAMPT
|
Cancer
|
|
NAMPT/IDO1-IN-1 is an orally active dual inhibitor of NAMPT and IDO1 with IC50s of 57.7 nM and 233 nM, respectively. NAMPT/IDO1-IN-1 blocks NAD+ biosynthesis, inhibits proliferation and migration of Paclitaxel (HY-B0015)- and FK866 (HY-50876)-resistant NSCLC cell lines (A549/R cells). NAMPT/IDO1-IN-1 has shown antitumor effects in mice and enhanced A549/R cell sensitivity to paclitaxel .
|
-
- HY-162640
-
|
|
ROR
|
Cancer
|
|
ROR1-IN-1 (Compound 19h) is an inhibitor for receptor tyrosine kinase-like orphan receptor 1 (ROR 1) with Ki of 0.10 μM. ROR1-IN-1 inhibits proliferation of cancer cells H1975, A549 and MDA-MB-231, with IC50 of 0.36 μM, 1.37 μM and 0.47 μM. ROR1-IN-1 exhibits antitumor efficacy in mice and good pharmacokinetic characteristics in rat models .
|
-
- HY-W068682
-
|
Hemipyocyanine; 1-Phenazinol; Hemi-pyocyanin
|
Amylases
Bacterial
|
Infection
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
1-Hydroxyphenazine (Hemipyocyanine; 1-Phenazinol; Hemi-pyocyanin) is an inhibitor for α-Amylase with an IC50 of 3.1 μg/mL . 1-Hydroxyphenazine exhibits anticancer and anti-inflammatory activity against cells A549, 1321N1 and RAW264.7, antifungal and antibacterial activity against strains Candida albicans, Aspergillus fumigatus, Escherichia coli and Xanthomonas campestris .
|
-
- HY-N10898
-
|
|
Lipoxygenase
|
Inflammation/Immunology
Cancer
|
|
(-)-Dihydroguaiaretic acid is a Lipoxygenase inhibitor that has antioxidant activity. (-)-Dihydroguaiaretic acid inhibits the oxidation of unsaturated fatty acids and removes free radicals. (-)-Dihydroguaiaretic acid also has anticancer activity with an IC50 value of 7.49 μM (A549 cells) .
|
-
- HY-150582
-
|
|
c-Met/HGFR
c-Kit
FLT3
Apoptosis
|
Cancer
|
|
c-Met-IN-14 (compound 26af) is a selective inhibitor of c-Met kinase from N-sulfonylamidine-based derivatives, with an IC50 value of 2.89 nM. c-Met-IN-14 shows anticancer activity by blocking phosphorylation of c-Met, and arrests cell cycle at G2/M phase. c-Met-IN-14 induces apoptosis of A549 cells in a dose-dependent manner .
|
-
- HY-N12589
-
|
|
Others
|
Cancer
|
|
8-epi-Helenalin is a semitterpene lactone with anti-tumor activity that can be isolated from Inula britannicaL. var. chinensis (Rupr.) Reg. and the ED50 values of 8-epi-Helenalin for HL-60, A549, MCF7, HCT-15, SK-OV-3 and Malme-3M are 12.2 μM, 53.8 μM, 9.1 μM, 8.7 μM, 18.7 μM and 8.3 μM, respectively. 8-epi-Helenalin can be used for anti-tumor studies .
|
-
- HY-147860
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-61 (compound 22a) is a potent EGFR kinase inhibitor, with IC50 values of 42 nM (L858R/T790 M), 137 nM (L858R/T790 M/C797S), and 743 nM (WT), respectively. EGFR-IN-61 shows antiproliferative activity against A549 and H1975 cell lines, with IC50 values of 2.14 and 1.82 μM, respectively .
|
-
- HY-161641
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin polymerization-IN-62 (Compound 14b) is an inhibitor for microtubule polymerization (IC50 is 7.5 μM) and a degrader for α- and β-tubulin. Tubulin polymerization-IN-62 inhibits proliferation of cancer cells MCF-7, A549 and HCT-116, with IC50 of 32, 60 and 29 nM, respectively. Tubulin polymerization-IN-62 arrests the cell cycle at G2/M phase, inhibits the migration of MCF-7. Tubulin polymerization-IN-62 exhibits antitumor efficacy with a tumor growth inhibition rate (TGI) of 74.27% in 4T1 homograft mouse model .
|
-
- HY-N11662
-
|
|
Others
|
Cancer
|
|
Euphoheliosnoid A (Compound 24) is a diterpenoid that can significantly enhance the killing activity of natural killer (NK) cells towards H1299-luci cells and A549-luci cells at the concentration of 2.5 μM .
|
-
- HY-N6252
-
|
|
Others
|
Cancer
|
|
Gypenoside XLVI is one of the major dammarane-type triterpenoid saponins from Gynostamma pentaphallum . Gypenoside XLVI has a tetracyclic triterpene structure and possess potent non-small cell lung carcinoma A549 cell inhibitory activity .
|
-
- HY-N10904
-
|
|
Others
|
Cancer
|
|
Broussonol E is a diprenylated flavonol. Broussonol E can be isolated from the leaves of Broussonetia kazinoki. Unlike some dinonylated flavonol derivatives, Broussonol E has no cytotoxicity to human tumor cell lines (A549, HCT-8, KB) .
|
-
- HY-162307
-
|
|
PROTACs
Keap1-Nrf2
|
Cancer
|
|
Nrf2 degrader 1 (compound 1) is a PROTAC Nrf2 degrader with anticancer effects. Nrf2 degrader 1 inhibits cancer cells growth for A549 and LK-2 cells with IC50 values of 100 nM and 40 nM, respectively .
|
-
- HY-147348
-
|
|
Biochemical Assay Reagents
|
Cancer
|
|
4-Formylcolchicine is a potent anticancer agent. 4-Formylcolchicine shows cytotoxicity activity with IC50 values of 1.007, 0.128, 0.054 μM for A549, HT-29, HCT116 cells, respectively .
|
-
- HY-156450
-
|
|
ERK
|
Cancer
|
|
ERK5-IN-5 (compound 4a) is an ERK5 kinase inhibitor with anticancer activity. ERK5-IN-5 exhibits good anti-proliferative activity with the IC50 value of 6.23 µg/mL for A549 cells .
|
-
- HY-B0239
-
|
|
Antibiotic
Bacterial
HIF/HIF Prolyl-Hydroxylase
VEGFR
Autophagy
Apoptosis
Beclin1
JNK
Akt
MMP
|
Infection
Cancer
|
|
Chloramphenicol is an orally active, potent and broad-spectrum antibiotic. Chloramphenicol shows antibacterial activity. Chloramphenicol represses the oxygen-labile transcription factor and hypoxia inducible factor-1 alpha (HIF-1α) in hypoxic A549 and H1299 cells. Chloramphenicol suppresses the mRNA levels of vascular endothelial growth factor (VEGF) and glucose transporter 1, eventually decreasing VEGF release. Chloramphenicol can be used for anaerobic infections and lung cancer research .
|
-
- HY-108016
-
|
Encordin
|
Src
PI3K
JNK
STAT
EGFR
Apoptosis
Autophagy
|
Cancer
|
|
Peruvoside is a potent inhibitor of Src, PI3K, JNK, STAT, and EGFR. Peruvoside induces apoptosis and autophagy and possesses a broad spectrum of anticancer activity in breast, lung, liver cancers and leukemia. Peruvoside is a broad-spectrum and potent antiviral activity against positive-sense RNA viruses. Peruvoside sensitizes Gefitinib (HY-50895)-resistant tumour cells (A549, PC9/gef and H1975) to Gefitinib .
|
-
- HY-155051
-
|
|
Apoptosis
Histone Methyltransferase
|
Cancer
|
|
Antiproliferative agent-25 (Compound 3s4) is a selective PRMT5 inhibitor (IC50: 0.11 μM). Antiproliferative agent-25 up-regulates hnRNP E1 protein level. Antiproliferative agent-25 forms H-bond interactions with SAM and E444 residue of PRMT5. Antiproliferative agent-25 has antiproliferative effects against A549 cells by inducing apoptosis and inhibiting cell migration. Antiproliferative agent-25 has high clearances with T1/2 of only 21.8 and 4.7 min in human and rat liver microsomes .
|
-
- HY-N15267
-
|
|
FAK
Akt
mTOR
|
Cancer
|
|
Ovalitenone is a flavonoid compound that can be isolated from the plant Millettia peguensis. It shows no cytotoxic effects on lung cancer H460 and A549 cells, but it significantly inhibits anchorage-independent growth, CSC-like phenotypes, colony formation, and the migration and invasion capabilities of cancer cells. Ovalitenone can significantly reduce the levels of N-cadherin, snail, and slug, while increasing E-cadherin, thus inhibiting the EMT pathway. Additionally, Ovalitenone suppresses the signaling pathways regulated by focal adhesion kinase (FAK), ATP-dependent tyrosine kinase (AKT), mammalian target of rapamycin (mTOR), and cell division cycle 42 (Cdc42) .
|
-
- HY-147708
-
|
|
Calcium Channel
|
Cancer
|
|
T-Type calcium channel inhibitor 2 (compound 6g) is a potent T-type calcium channel inhibitor with IC50s of 31.0, 83.1, 69.3 µM for Cav3.1 (α1G), Cav3.2 (α1H), Cav3.3 (α1I) (α1H), respectively. T-Type calcium channel inhibitor 2 shows cytotoxicity for A549, HCT-116 cells with IC50s of 5.0, 6.4 µM, respectively .
|
-
- HY-113796
-
|
|
Others
|
Cancer
|
|
Kopsoffinol, a bisindole alkaloid, shows in vitro growth inhibitory activity against human PC-3, HCT-116, MCF-7, and A549 cells and moderate effects in reversing multidrug-resistance in vincristine-resistant human KB cells .
|
-
- HY-N4251
-
|
(-)-Periplocoside M
|
Others
|
Cancer
|
|
Periplocoside M (compound 8) is a natural product isolated from the root bark of Periploca sepium. Periplocoside M shows antitumor activity against human A-549 and HepG2 cell lines, with the IC50 of 4.84 and 7.06 μM .
|
-
- HY-156451
-
|
|
ERK
|
Cancer
|
|
ERK5-IN-6 (compound 5J) is an ERK5 kinase inhibitor with anticancer activity. ERK5-IN-6 exhibits good anti-proliferative activity with the IC50 value of 4.56 µg/mL for A549 cells .
|
-
- HY-146432
-
|
|
Apoptosis
Raf
Ras
ROS Kinase
MDM-2/p53
|
Cancer
|
|
Antitumor agent-60 (compound 20) is a potent antitumor agent, targeting RAS-RAF signaling pathway and binding to CRAF with a Kd value of 3.93 μM. Antitumor agent-60 induces apoptosis by blocking cell cycle at G2/M phase. Antitumor agent-60 enhances the level of p53 and ROS. Antitumor agent-60 causes oval and irregular nucleus in cancer cells. Antitumor agent-60 can suppress the growth of tumor to some extent in A549 xenograft model .
|
-
- HY-147947
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin polymerization-IN-30 (compound 6e) is a potent Tubulin polymerization inhibitor. Tubulin polymerization-IN-30 is a colchicine binding site inhibitor. Tubulin polymerization-IN-30 can disrupt intracellular microtubule organization, arrest cell cycle at the G2/M phase. Tubulin polymerization-IN-30 exhibits the high potency against the cancer cell lines including SGC-7901, A549 and HeLa, with IC50 values of 2.16, 2.21, and 0.403 μM .
|
-
- HY-163874
-
|
|
PROTACs
|
Cancer
|
|
SMARCA2 degrader-13 (compound I-406) is a PROTAC degrader targeting SMARCA2; it degrades SMARCA2 proteins in A549 cells with an DC50 <100 nM, and a maximum degradation rate (Dmax%) >90 after 24 h of treatment .
|
-
- HY-163866
-
|
|
PROTACs
|
Cancer
|
|
SMARCA2 degrader-3 (compound I-323) is a PROTAC degrader targeting SMARCA2; it degrades SMARCA2 proteins in A549 cells with an DC50 <100 nM, and a maximum degradation rate (Dmax%) >90 after 24 h of treatment .
|
-
- HY-N7535
-
|
|
Others
|
Cancer
|
|
Chlorovaltrate K is a chlorinated valepotriate with anticancer effects. Chlorovaltrate K shows moderate cytotoxicity against A549, PC-3M, HCT-8 and Bel 7402 cell lines with IC50 values of 2.32-8.26 μM .
|
-
- HY-163867
-
|
|
PROTACs
|
Cancer
|
|
SMARCA2 degrader-4 (compound I-332) is a PROTAC degrader targeting SMARCA2; it degrades SMARCA2 proteins in A549 cells with an DC50 <100 nM, and a maximum degradation rate (Dmax%) >90 after 24 h of treatment .
|
-
- HY-N8934
-
|
|
Others
|
Cancer
|
|
6β-Hydroxytomentosin, a sesquiterpenoid, can be found in flowers of Inula japonica. 6β-Hydroxytomentosin exhibits weak cytotoxicities against A549, SK-OV-3, HepG-2 and HT-29 cell lines .
|
-
- HY-163865
-
|
|
PROTACs
|
Cancer
|
|
SMARCA2 degrader-2 (compound I-322) is a PROTAC degrader targeting SMARCA2; it degrades SMARCA2 proteins in A549 cells with an DC50 <100 nM, and a maximum degradation rate (Dmax%) >90 after 24 h of treatment .
|
-
- HY-162747
-
|
|
PROTACs
|
Cancer
|
|
PROTAC SMARCA2 degrader-17 (compound I-290) is a PROTAC degrader targeting SMARCA2; it degrades SMARCA2 proteins in A549 cells with an DC50 <100 nM, and a maximum degradation rate (Dmax%) >90 after 24 h of treatment .
|
-
- HY-162742
-
|
|
PROTACs
|
Cancer
|
|
PROTAC SMARCA2 degrader-16 (compound I-278) is a PROTAC degrader targeting SMARCA2; it degrades SMARCA2 proteins in A549 cells with an DC50 <100 nM, and a maximum degradation rate (Dmax%) >90 after 24 h of treatment .
|
-
- HY-N13163
-
|
|
Others
|
Cancer
|
|
2-Epitripdiolide is a diterpenoid compound derived from Tripterygium hypoglaucum with significant antitumor activity. Its IC50 values against A549, KB, KBvin, and MDA-MB-231 cells are 1.34, 0.4, 4.4, and 1.2 nM, respectively .
|
-
- HY-159462
-
|
|
PROTACs
|
Cancer
|
|
PROTAC SMARCA2 degrader-10 (compound I-507) is a PROTAC degrader targeting SMARCA2; it degrades SMARCA2 proteins in A549 cells with an DC50 <100 nM, and a maximum degradation rate (Dmax%) >90 after 24 h of treatment .
|
-
- HY-159450
-
|
|
PROTACs
|
Cancer
|
|
PROTAC SMARCA2 degrader-6 (compound I-427) is a PROTAC degrader targeting SMARCA2; it degrades SMARCA2 proteins in A549 cells with an DC50 <100 nM, and a maximum degradation rate (Dmax%) >90 after 24 h of treatment .
|
-
- HY-N1841
-
|
3'-Hydroxyrocaglamide
|
Others
|
Cancer
|
|
Rocaglamide D (3'-Hydroxyrocaglamide) (compound 1) is a lignan that can be found in Aglaia odorata. Rocaglamide D shows cytotoxicity with IC50s of 0.32, 0.12, 0.25 µM for HeLa, SGC-7901, A549 cells, respectively .
|
-
- HY-162746
-
|
|
PROTACs
|
Cancer
|
|
PROTAC SMARCA2 degrader-9 (compound I-285) is a PROTAC degrader targeting SMARCA2; it degrades SMARCA2 proteins in A549 cells with an DC50 <100 nM, and a maximum degradation rate (Dmax%) >90 after 24 h of treatment .
|
-
- HY-168714
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Microtubule inhibitor 12 (Compound 2k) is an inhibitor for microtubule polymerization with an IC50 of 22.23 μM. Microtubule inhibitor 12 arrests the cell cycle of B16-F10 at G2/M phase, induces apoptosis in B16-F10, and inhibits cell migration. Microtubule inhibitor 12 inhibits the proliferation of cancer cells B16-f10, A549, HepG2 and MCF-7, with IC50s of 0.098, 0.135, 0.109, and 0.259 μM, respectively. Microtubule inhibitor 12 exhibits antitumor efficacy in mouse model .
|
-
- HY-155050
-
|
|
Apoptosis
Histone Methyltransferase
|
Cancer
|
|
PRMT5-IN-31 (Compound 3m) is a selective PRMT5 inhibitor (IC50: 0.31 μM). PRMT5-IN-31 up-regulates hnRNP E1 protein level. PRMT5-IN-31 occupies the substrate site of PRMT5 and forms essential interactions with amino acid residues. PRMT5-IN-31 has antiproliferative effects against A549 cells by inducing apoptosis and inhibiting cell migration. PRMT5-IN-31 has high metabolic stability on human liver microsomes (T1/2: 132.4 min) .
|
-
- HY-169369
-
|
XJZ-06-462
|
MDM-2/p53
Autophagy
Apoptosis
|
Cancer
|
|
TRAP-1 (XJZ-06-462) is ap53 transcriptional activator that effectively activates mutant p53 and triggers the transcription of p53 target genes. TRAP-1 rapidly upregulates p21 and other p53 target genes in pancreatic cell lines with p53Y220C. TRAP-1 inhibits cell proliferation, with IC50 values of 3.94 and 0.531 μM in BxPC-3 and A549 cells, respectively. TRAP-1 regulates autophagy in lung cancer cells and offers protective effects against oxidative stress and cell apoptosis .
|
-
- HY-162041
-
|
|
Survivin
|
Cancer
|
|
AQIM-I is an inhibitor of survivin via inhibits survivin expression and colony formation. AQIM-I induces ROS production, apoptosis, cell cycle arrest, DNA damage, and autophagy. AQIM-I inhibits nonsmall cell lung cancer cells A549 with an IC50 value of 9 nM .
|
-
- HY-119767
-
|
|
VEGFR
Apoptosis
|
Cancer
|
|
Jolkinolide A is a diterpenoid, can be extracted from the roots of Euphorbia fischeriana Steud. Jolkinolide A exhibits anti-tumor activity, by affecting on angiogenesis of tumor tissues. Jolkinolide A significantly inhibits the Akt-STAT3-mTOR signaling pathway and reduces the expression of VEGF in A549 cells .
|
-
- HY-164384
-
|
|
PI3K
Akt
mTOR
Apoptosis
|
Cancer
|
|
DFX117 is a selective, orally active inhibitor for PI3Kα and c-Met tyrosine kinase. DFX117 inhibits PI3K/Akt/mTOR pathway, inhibits the proliferation of NCI-H1975, NCI-H1993, and HCC827 with IC50s 0.02-0.08 µM. DFX117 arrests cell cycle at G0/G1 phase, induces apoptosis in A549 and NCI-H1975. DFX117 exhibits antitumor efficacy in mice .
|
-
- HY-161852
-
|
|
PI3K
Apoptosis
|
Cancer
|
|
PI3K-IN-55 (Compound 6a) is a potent inhibitor for PI3K. PI3K-IN-55 affects PI3K/Akt/p53 signaling pathway, inhibits the proliferation of cancer cells A549, Hela, HepG2, MCF-7 and HT-29, with IC50s of 1.03-6.78 μM. PI3K-IN-55 induces apoptosis in cell MCF-7 .
|
-
- HY-157299
-
|
|
PDHK
|
Cancer
|
|
PDK-IN-3 (compound 1) is a potent pan inhibitor of PDK with IC50s of 109.3, 135.8, 458.7 nM and 8.67 μM against PDK 1-4, respectively. PDK-IN-3 also induces proliferation and apoptosis in A549 cells .
|
-
- HY-N0781
-
|
|
Apoptosis
|
Cancer
|
|
Linderalactone is an important sesquiterpene lactone isolated from Lindera aggregata. Linderalactone inhibits cancer growth by modulating the expression of apoptosis-related proteins and inhibition of JAK/STAT signalling pathway. Linderalactone also inhibits the proliferation of the lung cancer A-549 cells with an IC50 of 15 μM .
|
-
- HY-N3615
-
|
|
Others
|
Cancer
|
|
Confluentin can be isolated from Rhododendron dauricum. Confluentin shows weak cytotoxicity against human tumor cells (IC50: 15.05, 17.08, 18.48, and 23.01 μM for HL-60, SMMC-7712, A-549, and MCF-7) .
|
-
- HY-N12617
-
|
|
Bacterial
Apoptosis
|
Infection
Cancer
|
|
Bipolaricin R (Compound 6) is a compound that can be isolated from Bipolaris maydis. Bipolaricin R exhibits noticeable antimicrobial ability against Bacillus cereus, Staphylococcus aureus, and Staphylococcus epidermidis. Bipolaricin R has excellent antiproliferation and apoptosis induction effects against A549 cell line .
|
-
- HY-163434
-
|
|
EGFR
Histone Methyltransferase
|
Cancer
|
|
PRMT5/EGFR-IN-1 (Compound 10p) is an orally active dual PRMT5/EGFR inhibitor, with IC50s of 15.47 and 19.31 μM, respectively. PRMT5/EGFR-IN-1 exhibits antiproliferative activity against A549, MCF7, HeLa, and MDA-MB-231 cell lines. PRMT5/EGFR-IN-1 has favorable in vivo PK and PD properties. PRMT5/EGFR-IN-1 can significantly inhibit the growth of MCF7 orthotopic xenograft tumors .
|
-
- HY-168251
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
PROTAC BRM/BRG1 degrader-3 (compound 304) is a PROTACs-based BRM/BRG1 degrader with a DC50 of less than 1 nM for BRM degradation in SW1573 cells and a DC50 of greater than 1 nM for BRG1 degradation in SW1573 cells. PROTAC BRM/BRG1 degrader-3 has anti-tumor activity and anti-proliferative activity against A549 cells (IC50=0.6 nM). (Structure Note: PINK, Target protein ligand (HY-168252); Blue, E3 (HY-168253); Black, linker (HY-69260)).
|
-
- HY-161786
-
|
|
Bcl-2 Family
Apoptosis
Reactive Oxygen Species
|
Cancer
|
|
Bcl-2-IN-20 (Compound 81) is an inhibitor for Bcl-2 with IC50 <10 μM (79.1% inhibition at 9 μM). Bcl-2-IN-20 exhibits cytotoxicity in SK-MEL-28 (IC50>10 μM), A549 (IC50=6.1 μM), HepG2 (IC50>10 μM), MCF-7 (IC50=8.9 μM), HCT116 (IC50>10 μM) and HEK-293 (IC50=14.1 μM). Bcl-2-IN-20 promotes the ROS production, induces apoptosis and DNA damage .
|
-
- HY-158156
-
|
|
NF-κB
Apoptosis
|
Cancer
|
|
NF-κB-IN-16 (compound 9) is a complex (Pt(IV) complex) of NF-κB inhibitor and Cisplatin (HY-17394), which has high efficacy and low toxicity in anti-tumor activity. active. NF-κB-IN-16 can cause DNA damage, induce mitochondrial dysfunction, produce reactive oxygen species, and induce apoptosis through the mitochondrial pathway and endoplasmic reticulum stress. NF-κB-IN-16 potently inhibits the NF-κB/MAPK signaling pathway and disrupts PI3K/AKT signaling. NF-κB-IN-16 also exhibits excellent in vivo antitumor efficiency and low toxicity in A549 or A549/CDDP xenograft models .
|
-
- HY-163363
-
|
|
Adrenergic Receptor
|
Cancer
|
|
β-AR antagonist 2 (compound 43) is an antagonist of β-AR (IC50: 0.17 μM). β-AR-IN-1 inhibits the growth of mouse A549 xenograft tumors and shows cardioprotective efficacy against DOX-induced HF in C57 mice .
|
-
- HY-N10351
-
|
|
Apoptosis
|
Cancer
|
|
27-O-(tert-Butyldimethylsilyl)withaferin A (compound 9a), a natural withanolide, is an apoptosis inducer. 27-O-(tert-Butyldimethylsilyl)withaferin A shows antiproliferative activity against HeLa, A-549 and MCF-7 human cancer cell lines, and against normal Vero cells .
|
-
- HY-B0239R
-
|
|
Antibiotic
Bacterial
HIF/HIF Prolyl-Hydroxylase
VEGFR
Autophagy
Apoptosis
Beclin1
JNK
Akt
MMP
|
Infection
Cancer
|
|
Chloramphenicol (Standard) is the analytical standard of Chloramphenicol. This product is intended for research and analytical applications. Chloramphenicol is an orally active, potent and broad-spectrum antibiotic. Chloramphenicol shows antibacterial activity. Chloramphenicol represses the oxygen-labile transcription factor and hypoxia inducible factor-1 alpha (HIF-1α) in hypoxic A549 and H1299 cells. Chloramphenicol suppresses the mRNA levels of vascular endothelial growth factor (VEGF) and glucose transporter 1, eventually decreasing VEGF release. Chloramphenicol can be used for anaerobic infections and lung cancer research .
|
-
- HY-107513
-
|
|
mGluR
|
Neurological Disease
Cancer
|
|
BAY 36-7620 is a potent and noncompetitive antagonist of mGlu1 Receptor (IC50=0.16 μM) with inverse agonist activity. BAY 36-7620 inhibits tumor growth and prolongs the survival of mice with tumors by inhibiting mGlu1 receptor. BAY 36-7620 suppresses AKT phosphorylation in A549 tumors. BAY 36-762 has neuroprotective effect in acute subdural hematoma rat model.BAY 36-7620 is used in non-small cell lung cancer and breast cancer research .
|
-
- HY-147504
-
|
|
Apoptosis
Caspase
Bcl-2 Family
|
Cancer
|
|
Anticancer agent 63 (compound 3h) shows active in reducing the viability of different cancer cell lines, including SW480, HeLa, A549 and MCF-7, with IC50 values at 24 h of 4.9, 11.5, 9.4, and 3.4 μM, respectively. Anticancer agent 63 induce apoptosis in MCF-7 cells via down-regulating the expression of Bcl-2 and up-regulating the expression of IL-2 and Caspase-3. Anticancer agent 63 also shows antioxidant activity .
|
-
- HY-161858
-
|
|
PI3K
Akt
Apoptosis
|
Cancer
|
|
EpskA21 is an inhibitor for PI3K/AKT signaling pathway, and inhibits the proliferation of cancer cells MCF-7, A549, MIA-PaCa-2, Panc-1 and HepG2, with IC50 of 1.3-7.24 μM. EpskA21 inhibits the cell migration, arrests the cell cycle at G2/M (MCF-7) and S (MIA-PaCa-2) phase, and induces apoptosis in MCF-7 and MIA-PaCa-2. EpskA21 causes the mitochondrial dysfunction .
|
-
- HY-128062
-
|
|
LIM Kinase (LIMK)
|
Cancer
|
|
LIMK1 inhibitor BMS-4 is a LIM Kinase (LIMK) inhibitor targeting to LIMK1/2. LIMK1 inhibitor BMS-4 inhibits phosphorylation of cofilin, the LIMK substrate. However, LIMK1 inhibitor BMS-4 is noncytotoxic on A549 cells .
|
-
- HY-163875
-
|
|
PROTACs
|
Cancer
|
|
SMARCA2 degrader-14 (compound I-408) is a PROTAC degrader targeting SMARCA2 and SMARCA4; it degrades SMARCA2/4 proteins in A549 cells with the DC50s <100 nM, and the maximum degradation rate (Dmax%) >90 after 24 h of treatment .
|
-
- HY-163876
-
|
|
PROTACs
|
Cancer
|
|
SMARCA2 degrader-15 (compound I-409) is a PROTAC degrader targeting SMARCA2 and SMARCA4; it degrades SMARCA2/4 proteins in A549 cells with the DC50s <100 nM, and the maximum degradation rate (Dmax%) >90 after 24 h of treatment .
|
-
- HY-W667666
-
|
|
Others
|
Others
|
|
Anthragallol 1,2-dimethyl ether (compound 11) can be isolated from O. umbellata. Anthragallol 1,2-dimethyl ether has cytotoxicity, with IC50 values of 5.9 and 8.8 μg/ml against A549 cells and MDA-MB-231 cells, respectively .
|
-
- HY-W026772
-
|
|
Fluorescent Dye
Reactive Oxygen Species
TNF Receptor
Interleukin Related
SOD
|
Inflammation/Immunology
|
|
Fluorene is an orally active polycyclic aromatic hydrocarbon (PAH) and a precursor to other fluorene-based compounds. Fluorene and its derivatives serve as dye precursors for fluorene synthesis. In A549 cells, Fluorene induces oxidative stress and inflammatory responses by increasing ROS and SOD generation, exacerbating lipid peroxidation, modulating antioxidant enzyme activity, and upregulating the expression of pro-inflammatory factors TNF-α and IL-6. In vivo, Fluorene exhibits anxiolytic activity. Fluorene holds potential for research in inflammation and neurological disorders .
|
-
- HY-115537
-
|
|
Apoptosis
|
Cancer
|
|
NAE-IN-M22 is a potent, selective and reversible inhibitor of NEDD8 activating enzyme (NAE), with potency in micromolar range. NAE-IN-M22 inhibits multiple cancer cell lines and induces apoptosis in A549 cells. NAE-IN-M22 also can inhibit tumor growth in vivo .
|
-
- HY-161098
-
|
|
Apoptosis
|
Cancer
|
|
Apoptosis inducer 14 (Compd 7f), a chemotherapeutic agent, induces intrinsic and extrinsic apoptotic death mediated P53. Apoptosis inducer 14 exhibits IC50 values of 193.93 μg/mL, 6.76 μg/mL and 222.67 μg/mL in A549, HCT116 and HF84 cells, respectively .
|
-
- HY-162079
-
|
|
MMP
Apoptosis
|
Cancer
|
|
Anticancer agent 183 (compound 4h) inhibits the matrix metalloproteinase-9 (MMP-9) viability than 75% at 100 μg/mL. Anticancer agent 183 has anticancer activity with an IC50 value of <0.14 μM on the A549 cell line. Anticancer agent 183 induces apoptotic .
|
-
- HY-N6578
-
|
|
Others
|
Cancer
|
|
3-epi-Isocucurbitacin B (Compound 5) is a cucurbitane triterpene derived from Trichosanthes kirilowii. 3-epi-Isocucurbitacin B shows significant cytotoxicity to human tumor cells A-549, SK-OV-3, SK-MEL-2, XF-498 and HCT15 .
|
-
- HY-161332
-
|
|
Ferroptosis
Pyroptosis
Apoptosis
Reactive Oxygen Species
|
Cancer
|
|
Antitumor agent-143 (compound 2c) is an antitumor agent that blocks cell proliferation of A549 cells during the S phase and induces an early apoptosis. Antitumor agent-143 induces cell death via ferroptosis, apoptosis by a ROS-mediated mitochondrial dysfunction pathway and GSDMD-mediated pyroptosis .
|
-
- HY-161769
-
|
|
PROTACs
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
|
HL435 is a heterobifunctional molecule that degrades BRD4 by linking to JQ1, with DC50 of 11.9 nM and 21.9 nM, in MDA-MB-231 and MCF-7 cells, respectively. HL435 inhibits the proliferation of MDA-MB-231, MCF-7, 22Rv1 and A549, arrests the cell cycle and induces apoptosis. HL435 exhibits antitumor activity in mouse model. (Pink: ligand for target protein JQ-1 (HY-78695); Black: linker (HY-W004640); blue: ligand for E3 ligase HL389 (HY-161770))
|
-
- HY-134008
-
|
|
Apoptosis
Bcl-2 Family
Caspase
|
Cancer
|
|
Protoapigenone is an antineoplastic agent isolated from ferns. Protoapigenone has significant inhibitory activity against Hep G2, Hep 3B, MCF-7, A549 and MDAMB-231, with IC50s values of 1.60, 0.23, 0.78, 3.88 and 0.27 μg/mL respectively .
|
-
- HY-159459
-
|
|
PROTACs
|
Cancer
|
|
PROTAC SMARCA2/4-degrader-32 (compound I-446) is a PROTAC degrader targeting SMARCA2 and SMARCA4; it degrades SMARCA2/4 proteins in A549 cells with the DC50s <100 nM, and the maximum degradation rate (Dmax%) >90 after 24 h of treatment .
|
-
- HY-163869
-
|
|
PROTACs
|
Cancer
|
|
PROTAC SMARCA2/4-degrader-16 (compound I-337) is a PROTAC degrader targeting SMARCA2 and SMARCA4; it degrades SMARCA2/4 proteins in A549 cells with the DC50s <100 nM, and the maximum degradation rate (Dmax%) >90 after 24 h of treatment .
|
-
- HY-123898
-
|
|
Tyrosinase
Endogenous Metabolite
|
Cancer
|
|
Cepharadione B (compound 22) is a natural compound isolated from the leaves of Piper sanctum. Cepharadione B is a tyrosinase inhibitor with an IC50 value of 170 μM, and inhibits cell growth in A-549, SK-OV-3, SK-MEL-2, XF-498 and HCT-15 cells .
|
-
- HY-16952
-
|
(±)-Bepridil; Org 5730
|
Calcium Channel
Sodium Channel
SARS-CoV
|
Infection
Cardiovascular Disease
|
|
Bepridil ((±)-Bepridil) is a calcium channel blocking agent used as antiarrhythmic agent. Bepridil inhibits both calcium and sodium currents, has research potential in certain ischemia-induced ventricular arrhythmias. Bepridil also has strong inhibition of SARS-CoV-2 from entry and replication inside Vero E6 and A549 cells .
|
-
- HY-N10354
-
|
|
Apoptosis
|
Cancer
|
|
27-Methyl withaferin A (comppund 26) is an apoptosis inducer with anticancer effects. 27-Methyl withaferin A shows antiproliferative effects against HeLa, A-549 and MCF-7 human tumor cell lines with IC50 values of 3.2 μM, 4.2 μM and 1.4 μM, respectively .
|
-
- HY-159458
-
|
|
PROTACs
|
Cancer
|
|
SMARCA2/4-degrader-7 (compound I-439) is a PROTAC degrader targeting SMARCA2 and SMARCA4; it degrades SMARCA2/4 proteins in A549 cells with the DC50s <100 nM, and the maximum degradation rate (Dmax%) >90 after 24 h of treatment .
|
-
- HY-146148
-
|
|
Histone Demethylase
|
Cancer
|
|
KDM4C-IN-1 (Compound 4d) is a potent KDM4C inhibitor with an IC50 of 8 nM. KDM4C-IN-1 inhibits the growth of HepG2 and A549 cells with IC50s of 0.8 µM and 1.1 µM, respectively .
|
-
- HY-159452
-
|
|
PROTACs
|
Cancer
|
|
SMARCA2/4-degrader-1 (compound I-430) is a PROTAC degrader targeting SMARCA2 and SMARCA4; it degrades SMARCA2/4 proteins in A549 cells with the DC50s <100 nM, and the maximum degradation rate (Dmax%) >90 after 24 h of treatment .
|
-
- HY-159453
-
|
|
PROTACs
|
Cancer
|
|
SMARCA2/4-degrader-2 (compound I-431) is a PROTAC degrader targeting SMARCA2 and SMARCA4; it degrades SMARCA2/4 proteins in A549 cells with the DC50s <100 nM, and the maximum degradation rate (Dmax%) >90 after 24 h of treatment .
|
-
- HY-161824
-
|
|
Others
|
Cancer
|
|
Antiproliferative agent-52 (Compound 4a) is an antiproliferative agent that exhibits significant antiproliferative activity against four human tumor cell lines (A549, A2780, SKOV3, HCC827), with IC50 values ranging from 5.83 to 8.63 nM. Antiproliferative agent-52 can be used in cancer research .
|
-
- HY-162741
-
|
|
PROTACs
|
Cancer
|
|
PROTAC SMARCA2/4-degrader-33 (compound I-277) is a PROTAC degrader targeting SMARCA2 and SMARCA4; it degrades SMARCA2/4 proteins in A549 cells with the DC50s <100 nM, and the maximum degradation rate (Dmax%) >90 after 24 h of treatment .
|
-
- HY-147802
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
EGFR-IN-59 (Compound 8c) is a EGFR inhibitor (IC50=190 nM) and apoptosis inducer. EGFR-IN-59 exhibits cytotoxicity against non-small lung cancer cell lines (A549) and normal lung fibroblasts (WI38) with IC50s of 8.62 and 52.6 µM, respectively. EGFR-IN-59 can be used for the research of various cancers such as non-small cell lung cancer (NSCLC), head and neck cancer, breast cancer and colorectal cancer .
|
-
- HY-146080
-
|
|
Apoptosis
|
Cancer
|
|
Antitumor agent-61 (Compound 9b), Irinotecan (Ir) derivative, is a potential antitumor agent. Antitumor agent-61 displays potent activity with IC50s of 0.92, 1.39, 1.75, 2.20, 3.05 and 3.23 μM against five human cancer cells SK-OV-3, SK-OV-3/CDDP, U2OS, MCF-7, A549 and MG-63, respectively. Antitumor agent-61 induces SK-OV-3 cells apoptosis through mitochondrion pathways .
|
-
- HY-150644
-
|
|
Aldose Reductase
|
Cancer
|
|
S07-2010 is a potent pan-AKR1C (aldo-keto reductase family 1 member C) inhibitor, with IC50 values of 0.19, 0.36, 0.47, and 0.73 μM for AKR1C3, AKR1C4, AKR1C1 and AKR1C2, respectively. S07-2010 induces apoptosis in A549/DDP cells. S07-2010 strengthens the cytotoxicity of chemotherapeutic agents in drug-resistant cells. S07-2010 significantly inhibits the proliferation of drug-resistant cells .
|
-
- HY-N13078
-
|
|
Others
|
Cancer
|
|
3-epi-Resibufogenin (compound 2) is an anticancer agent that can be produced by biotransformation of Resibufogenin (HY-N0815) from Actinomucor elegans AS 3.2778. 3-epi-Resibufogenin exhibits cytotoxicity against cancer cells with IC50 values ??of 42.5 μM (A549) and 48.4 μM (H1299), respectively .
|
-
- HY-100864
-
|
|
PGE synthase
|
Inflammation/Immunology
|
|
mPGES1-IN-3 (Compound 17d) is a potent and selective microsomal prostaglandin E2 synthase-1 (mPGES-1) inhibitor, which exhibits excellent mPGES-1 enzyme (IC50: 8 nM), cell (A549 IC50: 16.24 nM) and human whole blood potency (IC50: 249.9 nM) .
|
-
- HY-N13162
-
|
|
Others
|
Cancer
|
|
Hemsleyadin D is a triterpenoid compound derived from Hemsleya penxianensis with antitumor activity. Its IC50 values against K562, MGC-803, U118, HepG2, A549, and MCF-7 cells are 93.9, 47.1, 25.9, 56.1, 66.3, and 67.6 μM, respectively .
|
-
- HY-161845
-
|
|
Drug Derivative
|
Cancer
|
|
Anticancer agent 240 (compound 9b) is an 8-quinolinesulfonamide derivative with a cytotoxicity activity. Anticancer agent 240 shows inhibitory activity in Caco-2, SNB-19, A-549, and SKOV-3 cell line IC50 values of 0.26, 0.38, 0.40 and 4.16 μM .
|
-
- HY-163742
-
|
|
SARS-CoV
|
Infection
|
|
SARS-CoV-2 Mpro-IN-22 (compound 4), a hydrolysable tannin, is a potent SARS-CoV-2 main protease (Mpro) inhibitor with an IC50 value of 1.2 µg/mL. SARS-CoV-2 Mpro-IN-22 does not show any significant cytotoxic activity against A549 and HUVEC cell lines .
|
-
- HY-163034
-
|
|
Apoptosis
Reactive Oxygen Species
|
Cancer
|
|
Antitumor photosensitizer-5 (Ru2) is a photosensitizer which effectively target tumor mitochondria with an IC50 of 0.3 μM for phototoxicity to A549 cells. Under 460 nm light irradiation, antitumor photosensitizer-5 induces the generation of reactive oxygen species and NADH depletion, causes mitochondrial damage and activation of caspase-3, inducing apoptosis and suppressing cell migration. Antitumor photosensitizer-5 has the potential to prevent the growth of malignant tumors, therefore, shows the potential to be applied to photodynamic therapy .
|
-
- HY-139272
-
|
|
Drug Derivative
|
Cancer
|
|
Eicosapentaenoyl 1-propanol-2-amide is an amide derivative of Eicosapentaenoic Acid (HY-B0660). Eicosapentaenoyl 1-propanol-2-amide inhibits the 98.4% proliferation of cancer cell A549 at 3 μM. Eicosapentaenoyl 1-propanol-2-amide can be used in cancer research .
|
-
- HY-N0781R
-
|
|
Apoptosis
|
Cancer
|
|
Linderalactone (Standard) is the analytical standard of Linderalactone. This product is intended for research and analytical applications. Linderalactone is an important sesquiterpene lactone isolated from Lindera aggregata. Linderalactone inhibits cancer growth by modulating the expression of apoptosis-related proteins and inhibition of JAK/STAT signalling pathway. Linderalactone also inhibits the proliferation of the lung cancer A-549 cells with an IC50 of 15 μM .
|
-
- HY-W317408
-
|
|
Biochemical Assay Reagents
|
Others
|
|
(+)-Menthyl acetate is a compound isolated from natural Cunila angustifolia Benth essential oil. The selectivity of (+)-Menthyl acetate is higher than that of MCF-7 cell line, IC50=34.0 μg?mL -1, and lower than that of SK-Mel-28 cell line, IC50=279.9 μg?mL -1, on A549 cell without fatal .
|
-
- HY-156098
-
|
|
c-Met/HGFR
|
Cancer
|
|
c-Met-IN-19 (Compound 21j) is a c-Met inhibitor (IC50: 1.99 nM). c-Met-IN-19 shows cytotoxicity against A549, HT-29, SGC-7901, MDA-MB-231 cells with IC50s of 0.25, 0.36, 0.98, 0.76 μM .
|
-
- HY-161313
-
|
|
Histone Methyltransferase
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
DYB-03 is an oral active HIF-1α/EZH2 inhibitor. DYB-03 inhibits migration, invasion, and angiogenesis of lung cancer cells and HUVECs in vitro and in vivo. DYB-03 induces apoptosis in 2-ME2 - and GSK126 -resistant of A549 and H460 cells .
|
-
- HY-111125
-
|
|
Parasite
Reactive Oxygen Species
Apoptosis
|
Infection
Cancer
|
|
AMRI-59 is a potent inhibitor of PrxI used for parasitic infections. AMRI-59 can increase cellular ROS, leading to activation of signaling pathways mediated by mitochondria and apoptosis signal-regulated kinase 1, thereby leading to apoptosis in A549 human lung adenocarcinoma. AMRI-59 exhibits significant antitumor activity without apparent acute toxicity .
|
-
- HY-N3179
-
|
|
Others
|
Others
|
|
Norcepharadione B is an alkaloid that can be isolated from Houttuynia cordata. Norcepharadione B exhibits moderate cytotoxicity against A-549, SK-OV-3, SK-MEL-2, XF-498 and HCT-15 cell line with ED50s of 40, 26.4, 40, 14.2 and 38.2 μg/mL, respectively .
|
-
- HY-152468
-
|
|
Apoptosis
|
Cancer
|
|
Antitumor agent-83 is an activator of pro-apoptotic protein BAX and has significant anti-proliferation effect on tumor cells. Antiumor agent-83 mediates cell Apoptosis by inducing the conformational activation of BAX and has inhibitory effect on A549 cell cycle. Antiumor agent-83 has good metabolic stability and CYPs spectrum in vitro .
|
-
- HY-125158
-
|
|
Aurora Kinase
Apoptosis
|
Cancer
|
|
HOI-07 is a selective Aurora B kinase inhibitor. HOI-07 blocks phosphorylation of histone H3 on Ser10 in
lung cancer cells. HOI-07 induces cell-cycle arrest, and apoptosis. HOI-07 has antitumor activity, and suppresses the tumor growth of A549, 143B and KHOS xenografts .
|
-
- HY-130723A
-
|
|
AMPK
|
Cancer
|
|
AMPK activator 2 (compound 7a) hydrochloride, a fluorine-containing proguanil derivative, up-regulates AMPK signal pathway and downregulates mTOR/4EBP1/p70S6K. AMPK activator 2 hydrochloride inhibits proliferation and migration of human cancer cell lines (UMUC3, T24, A549) .
|
-
- HY-149436
-
|
|
CDK
|
Cancer
|
|
CDK2/Bcl2-IN-1 (compound 1), a saponin and a CDK-2 inhibitor (IC50=117.6 nM) with promising cytotoxicity against cancer cells. CDK2/Bcl2-IN-1 also inhibits Bcl-2, and induces apoptosis in A549 lung cancer cells .
|
-
- HY-146977
-
|
|
PDK-1
|
Cancer
|
|
LDHA/PDKs-IN-1 (compound 20e) is a potent and dual inhibitor of PDKs and LDHA with IC50s of 0.8 and 0.15 μM, respectively. LDHA/PDKs-IN-1 reduces A549 cell proliferation with an EC50 of 13.2 μM and decreases the lactate formation, and increases oxygen consumption. LDHA/PDKs-IN-1 has the potential for the research of cancer diseases .
|
-
- HY-N1614
-
|
|
Others
|
Others
|
|
1 α-hydroxytorilin (compound 3) is a sesquiterpenoid. 1 α-hydroxytorilin can be isolated from Torilis japonica. 1α-hydroxytorilin has cytotoxicity against human A549, SK-OV-3, SK-MEL-2, and HCT15 tumor cells with ED50 values of 20.52, 18.24, 17.48, 42.54 μg/mL, respectively .
|
-
- HY-N0074
-
|
|
COX
|
Inflammation/Immunology
|
|
Byakangelicol, isolated from Angelica dahurica, inhibits interleukin-1beta (IL-1beta) -induced prostaglandin E2 (PGE2) release in A549 cells mediated by suppression of cyclooxygenase-2 (COX-2) expression and the activity of COX-2 enzyme. Byakangelicol has therapeutic potential as an anti-inflammatory agent on airway inflammation .
|
-
- HY-N3210
-
|
|
Others
|
Cancer
|
|
Nb-Demethylechitamine is an alkaloid isolated from the methanol extract of Alstonia rostrata twigs. Nb-Demethylechitamine has in vitro cytotoxic activity against several human cancer cell lines, including human myeloid leukemia HL-60, liver cancer SMMC-7721, lung cancer A-549, breast cancer MCF-7, and colon cancer SW480 cells .
|
-
- HY-146978
-
|
|
PDK-1
|
Cancer
|
|
LDHA/PDKs-IN-2 (compound 20k) is a potent and dual inhibitor of PDKs and LDHA with IC50s of 1.6 and 0.7 μM, respectively. LDHA/PDKs-IN-2 reduces A549 cell proliferation with an EC50 of 15.7 μM and decreases the lactate formation, and increases oxygen consumption. LDHA/PDKs-IN-2 has the potential for the research of cancer diseases .
|
-
- HY-N0538
-
|
Xylite
|
Autophagy
Endogenous Metabolite
Bacterial
Atg7
Atg8/LC3
|
Metabolic Disease
Cancer
|
|
Xylitol can be classified as a polyol and sugar alcohol, exhibiting inhibitory activity on cancer cell proliferation. It induces autophagy (Autophagy) and cell death in A549 cells by activating the autophagy signaling pathway, as evidenced by the increased expression of LC3-II and Atg5-Atg12 upon Xylitol treatment. Additionally, Xylitol inhibits acetaldehyde production by Candida species, thereby reducing their carcinogenic potential. In vivo, Xylitol induces alterations in the gut microbiota of mice, which may enhance cholesterol accumulation and upregulate hepatic ChREBP, while also slowing tumor growth in the B16F10 melanoma C57BL/6 mouse model .
|
-
- HY-157292
-
|
|
Apoptosis
Reactive Oxygen Species
|
Cancer
|
|
2E-3-F16 is a anticancer agent. 2E-3-F16 exhibits tumor cell selectivity between NCI-H446 cancer cells and HBE cells. 2E-3-F16 enhances the sensitivity of A549 cells to Cisplatin (HY-17394) .
|
-
- HY-170910
-
|
|
HSP
|
Cancer
|
|
Hsp90-IN-39 (Compound 16t) is a HSP90 inhibitor with notable selectivity for the HSP90α isoform. Hsp90-IN-39 demonstrates significant antiproliferative activity in various cancer cell lines, including MCF-7, HCT116, SKBr3, K562, and A549. Hsp90-IN-39 holds potential for cancer research .
|
-
- HY-157419
-
|
7-(4-Ethylphenyl)-FL118
|
Apoptosis
|
Cancer
|
|
FL77-24, a FL118 analog and apoptosis inducer, possesses antitumor activity, with IC50 values of 99.4 nM, 118 nM, <6.4 nM, 28.5 nM and <6.4 nM in HCT116, HepG2, MCF-7, A549 and HeLa cells, respectively. FL77-24 mainly causes cell cycle arrest in S and G2/M phases .
|
-
- HY-N12349
-
|
|
Others
|
Others
|
|
Glucozaluzanin C is a lignan isolated from the MeOH extract of the roots of Ainsliaea acerifolia (Compositae). Glucozaluzanin C has ED50 value of 2.45 μg/mL, 1.37μg/mL, 0.40 μg/mL, 1.41 μg/mL, 1.43 μg/mL for A549 cells, SK-OV-3 cells, SK-MEL-2 cells, XF498 cells, HCT15 cells, respectively .
|
-
- HY-N12135
-
|
|
Others
|
Cancer
|
|
15α-Hydroxy-20-oxo-6,7-seco-ent-kaur-16-en-1,7α(6,11α)-diolide (compound 2) is an enantio-kaurene diterpenoid (ent -kaurene diterpenoid), which can be isolated from Rubescens rubescens. 15α-Hydroxy-20-oxo-6,7-seco-ent-kaur-16-en-1,7α(6,11α)-diolide has cellular activity against EC-1, U87, A549, MCF-7 and HeLa cell lines Toxicity, IC50s are 37.69 μM, 79.362 μM, 80.07 μM, 197.35 μM, 462.13 μM, and 180.09 μM respectively .
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-
- HY-111140
-
|
|
PGE synthase
Lipoxygenase
|
Inflammation/Immunology
|
|
YS121 is a dual inhibitor of microsomal prostaglandin E2 synthase-1 (mPGES-1; IC50=3.4 μM) and 5-lipoxygenase (5-LOX; IC50=6.5 μM). YS121 dose- dependently reduces PGE2 production with EC50=12 μM in IL-1β-stimulated A549 cells .
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-
- HY-168606A
-
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MDM-2/p53
|
Cancer
|
|
p53-MDM2-IN-7 (compound 6d) (hydrochloride) is a p53-MDM2 inhibitor. p53-MDM2-IN-7 has an IC50 value of 8.13 μM against A549 cells. p53-MDM2-IN-7 can be used in anti-cancer research .
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-
- HY-162896
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
And1 degrader 1 (Compound A15) is a degrader of the acidic nucleoplasmic DNA-binding protein 1 (And1), which can significantly induce the degradation of And1 in NSCLC cells. And1 degrader 1 (5 μM) combined with Olaparib (HY-10162) (1 μM) effectively inhibits the proliferation of A549 and H460 cells. And1 degrader 1 can be used in cancer research .
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-
- HY-149302
-
|
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Apoptosis
Autophagy
Histone Acetyltransferase
|
Cancer
|
MC4033 shows IC50s of 39.4 μM, 52.1 μM, 41 μM and 30.1 μM in HCT116, H1299, A549 and U937, respectively .
MC4033 (25, 50, 100, and 200 μM, 72 h) reduces the level of H4K16Ac in HT29 cells, suggesting its ability to inhibit KAT8 in cells .
|
-
- HY-170883
-
|
|
Photosensitizer
|
Cancer
|
|
Type-I/-II Photosensitizer-1 (compound 8b) is a photosensitizer with anticancer activity. Type-I/-II Photosensitizer-1 exhibits significant phototoxicity against both A549 and 4T1 tumor cells. Type-I/-II Photosensitizer-1 shows a strong oxygen-independent antitumor effect under laser irradiation (IC50=1.50-1.76 μM) .
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-
- HY-170846
-
|
|
FGFR
VEGFR
Bcr-Abl
FLT3
Cytochrome P450
|
Inflammation/Immunology
|
|
FGFRs-IN-1 (Compound A16) is the orally active inhibitor for FGFR, that inhibits FGFR1/2/3/4 with IC50s of 2.3, 7, 11, and 163 nM, respectively. FGFRs-IN-1 also inhibits VEGFR1/2/3, Abl, and Flt3 with IC50s of 61, 176, 112, 26, and 353 nM, respectively. FGFRs-IN-1 exhibits weak inhibitory efficacy against CYP enzymes. FGFRs-IN-1 reduces the expression of α-SMA and collagen I, and inhibits epithelial-mesenchymal transition (EMT) in TGF-β1 stimulated A549 cell. FGFRs-IN-1 exhibits anti-inflammatory activity in Bleomycin (HY-17565)-induced mouse pulmonary fibrosis model and CCl4 (HY-Y0298)-induced mouse liver fibrosis model .
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-
- HY-N0084
-
|
Betulinic aldehyde; Betunal
|
Bacterial
|
Infection
Cardiovascular Disease
Cancer
|
|
Betulinaldehyde (Betunal) Has anti-cancer and anti-staphylococcus aureus activity. Betulinaldehyde Suppressible Akt, MAPK sum STAT3 Signal path, increase self-transfer, Suppression A549 Cellular vitality, increase and transfer. Betulinaldehyde suppresses PLCγ1/Ca 2+/MMP9 signal pathway, has a key effect on vascular plasticity, and is available for cardiovascular disease (CVD) research .
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-
- HY-N12606
-
|
|
Fungal
|
Infection
|
|
Neodidymelliosides A (compound 1)It is a secondary metabolite of fungi and has a significant inhibitory effect on Staphylococcus aureus and Candida albicans biofilms. Neodidymelliosides AIt also has anti-cancer activity and can inhibit KB3.1 (cervix),PC-3 (prostate),MCF-7(breast),SKOV-3 (ovary),A431 (skin )and A549 (lung )Cell viability of cell lines .
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-
- HY-118528A
-
|
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TGF-β Receptor
|
Endocrinology
|
|
TP0427736 hydrochloride is a potent inhibitor of ALK5 kinase activity with an IC50 of 2.72 nM and this effect is 300-fold higher than the inhibitory effect on ALK3 (IC50=836 nM). TP0427736 hydrochloride also inhibits Smad2/3 phosphorylation in A549 cells induced by TGF-β1 with an IC50 value of 8.68 nM. TP0427736 hydrochloride can be used for the research of androgenic alopecia (AGA) .
|
-
- HY-P10711
-
|
|
Autophagy
|
Cancer
|
|
ALA-A2 is an anticancer peptide discovered in alpha-lactalbumin that selectively kills cancer cells by inducing Autophagy. ALA-A2 has cell-penetrating capabilities, allowing it to effectively enter cells without relying on membranolytic effects. In A549 lung cancer cells, ALA-A2 demonstrates significant dose-dependent anticancer activity. ALA-A2 holds promise for research in cancer therapy and autophagy regulation .
|
-
- HY-168113
-
|
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Others
|
Cancer
|
|
Antiproliferative agent-60 (compound 8c) is a 11-Azaartemisinin derivative with superior anticancer activities. Antiproliferative agent-60 shows IC50 values of 7.7 μM, 42.5 μM, and 15.5 μM for epidermoid carcinoma (KB), HepG2, and A549 cells, respectively. Antiproliferative agent-60 exhibits significant tumor selectivity, up to 32-fold higher compared to Hek293 normal cells .
|
-
- HY-163006
-
|
|
EGFR
c-Met/HGFR
|
Cancer
|
|
EGFR/c-Met-IN-1 (compound TS-41) is a dual-target inhibitor of EGFR/c-Met. The IC50 for inhibiting EGFR L858R and c-Met is 68.1 nM and 0.26 nM respectively. . EGFR/c-Met-IN-1 induces apoptosis and cell cycle arrest in A549-P cells, downregulating the phosphorylation of EGFR, c-Met, and downstream AKT. EGFR/c-Met-IN-1 inhibits tumor growth in vitro and in vivo .
|
-
- HY-151486
-
|
|
GLUT
|
Cancer
|
|
GLUT1-IN-1 is a glucose transporter 1 (GLUT1) inhibitor and has a GLUT1-specific inactivation ability. GLUT1-IN-1 exhibits concentration-dependent cytotoxicity for HeLa, A549 and HepG2 cells with IC50 values of 5.49 μM, 11.14 μM, and 8.73 μM, respectively. GLUT1-IN-1 can be used for the research of photodynamic therapy (PDT) and severals cancer .
|
-
- HY-162721
-
|
|
Others
|
Cancer
|
|
Anticancer agent 242 (7) possesses anticancer activity in A2780 (IC50 = 0.24 μM, ovarian adenocarcinoma), A2780cis (IC50 = 0.45 μM, resistant derivative of A2780), CCD18Co (IC50 = 0.59 μM, non-malignant human fibroblasts), A549 (IC50 = 0.32 μM, lung carcinoma), HT29 (IC50 = 0.26 μM, colorectal adenocarcinoma), and MCF7 (IC50 = 0.55 μM, breast adenocarcinoma) .
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-
- HY-N8508
-
|
|
Apoptosis
Cytochrome P450
PARP
JNK
Bcl-2 Family
Caspase
|
Cancer
|
|
Myrothecine A is a trichothecene mycotoxin found in M. roridum. Myrothecine A induces apoptosis, promotes the cytochrome c release, PARP-cleavage and phosphorylation of JNK, increases Bax and cleaved caspase-3, -5, and -8 levels. Myrothecine A has anticancer activities and promotes the maturation of DC cells in the microenvironment. Myrothecine A inhibits proliferation of A549, MCF-7, HepG2, and SMMC-7721 cancer cells with IC50s of 95, 70, 60, and 25 µM, respectively .
|
-
- HY-157154
-
|
|
SARS-CoV
|
Infection
|
|
MAT-POS-e194df51-1 is an orally active, non-covalent and non-peptide SARS-CoV-2 main protease (M pro) inhibitor with an IC50 value of 37nM. MAT-POS-e194df51-1 is cytotoxic with EC50 values of 64 nM and 126 nM in A549-ACE2-TMPRSS2 cells and HeLa -ACE2 cells, respectively .
|
-
- HY-170508
-
|
|
Cytochrome P450
|
Endocrinology
|
|
Aromatase-IN-4 (Compound 6a) is an aromatase (Aromatase) inhibitor. Aromatase-IN-4 exhibits anticancer activity, with GI50 values of 2.95 μM, 3.35 μM, 2.27 μM, 8.46 nM, and 1.56 μM against the MDAMB-231, MCF-7, A-549, NCI-H23, and A-498 cell lines, respectively . Aromatase-IN-4 effectively blocks aromatase-dependent estrogen production .
|
-
- HY-164056
-
|
|
EGFR
|
Cancer
|
|
EGFR T790M/L858R-IN-8 (compound 9) is a potent inhibitor of EGFR, targeting mutant EGFR T790M/L858R with IC50 of 56.8 μM. The anti-proliferative effect of EGFR T790M/L858R-IN-8 on cancer cell lines A549, A431, and NHI-H1975 is not significant .
|
-
- HY-101450
-
|
|
EGFR
|
Cancer
|
|
PF-6274484 is a potent EGFR inhibitor with Kis of 0.14 nM and 0.18 nM for EGFR-L858R/T790M and WT EGFR, respectively. PF-6274484 inhibits EGFR-L858R/T790M autophosphorylation in H1975 tumor cells and EGFR WT in A549 tumor cells with IC50s of 6.6 and 5.8 nM, respectively .
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-
- HY-146366
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 26 (compound 3c) is a potent inhibitor of tubulin. Tubulin inhibitor 26 is an indazole derivative compound. Tubulin inhibitor 26 shows noteworthy low nanomolar potency against HepG2, HCT116, SW620, HT29 and A549 cancer cell lines. Tubulin inhibitor 26 arrests tumor cell in G2/M phase and induced cell apoptosis. Tubulin inhibitor 26 suppresses tumor growth in vivo without affecting the mice body weight .
|
-
- HY-171038
-
|
|
STAT
|
Inflammation/Immunology
|
|
STAT3-IN-39 (compound 10K) is an orally active STAT3 inhibitor that exhibits excellent inhibitory activity against STAT3 phosphorylation, with an IC50 of 0.47 μM in NIH-3T3 cells. STAT3-IN-39 inhibits the TGF-β1-induced fibrotic response and blocks the epithelial-mesenchymal transition in A549. STAT3-IN-39 can be utilized in research related to idiopathic pulmonary fibrosis .
|
-
- HY-119631
-
|
|
Bacterial
|
Infection
|
|
Nornidulin is a depsidone originally isolated from A. nidulans that has antibacterial activity against M. tuberculosis and M. ranoe as well as antifungal activity against T. tonsurans and M. audouini. It also inhibits the growth of methicillin-resistant S. aureus (MRSA; MIC=2 μg/mL).2 Nornidulin has cytotoxic activity in MOLT-3 cells (IC50=35.7 μM) but not HuCCA-1, HepG2, or A549 cells (IC50s=>116.4 μM).
|
-
- HY-W127820
-
|
Tetrakis(2-N-methylpyridyl)porphine chloride
|
Biochemical Assay Reagents
Fluorescent Dye
|
Others
|
|
H2TMpyP-2 (tetrakis(2-N-methylpyridyl)porphine) chloride is an active photosensitizer with strong absorption properties in the visible to near-infrared region and excellent singlet oxygen quantum yield. Captisol-TMPyP complexes can be used in supramolecular nanosynthesis to increase singlet oxygen production, improve photostability and better photosensitization, and support photodynamic therapy activity. The Captisol:TMPyP complex also exhibited antibacterial activity against Escherichia coli and was cytotoxic against lung cancer A549 cells .
|
-
- HY-170895
-
|
|
HSP
Na+/K+ ATPase
|
Cancer
|
|
Hsp90-IN-38 (compound 20m) is a HSP90 (heat shock protein) inhibitor. Hsp90-IN-38 exhibits strong HSP90 binding affinity with a Kd of 87 nM. Hsp90-IN-38 inhibits ATPase with an IC50 of 0.13 μM. Hsp90-IN-38 inhibits HCT116, MCF-7, SKBr3, K562 and A549 cells with IC50s of 0.187, 0.072, 0.105, 0.403 and 031 μM, respectively .
|
-
- HY-161825
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulin polymerization-IN-66 (Compound 13) inhibits colony formation and tubulin polymerization. Tubulin polymerization-IN-66 induces apoptosis. Tubulin polymerization-IN-66 inhibits cell viability of A549, A2780, SKOV3, HCC827 cells, with IC50s of 0.84, 0.38, 0.31, 0.34 nM respectively. Tubulin polymerization-IN-66 is also active against the Paclitaxel (HY-B0015)-resistant cancer cell line A2780/T and its parental cell line A2780 .
|
-
- HY-156080
-
|
|
PI3K
Akt
|
Cancer
|
|
PI3K-IN-48 is a PI3K inhibitor with IC50 value of 1.55 ± 0.18 μM for A549 cells. PI3K-IN-48 can induce G0/G1 phase arrest, cell apoptosis, and down-regulate expression of p-PI3K and p-Akt. PI3K-IN-48 can be used for human lung cancers diseases research .
|
-
- HY-115407
-
|
|
Bacterial
|
Infection
Cancer
|
|
Cochliodone A is an active compound extracted from cultures of the deep-sea derived fungus Chaetomium sp. and has antibacterial and anticancer activity. Cochliodone A is toxic to a variety of bacteria, with MICs of 15.3 μg/mL (V. vulnificus), 32.7 μg/mL (V. rotiferianus), 15.9 μg/mL (S. aureus ATCC 43300), and 16.3 μg/mL (S . aureus CGMCC 1.12409). Cochliodone A also inhibits a variety of cancer cell lines, with IC50s of 28.1 μM (A549), 20.7 μM (HeLa), and 23.2 μM (Hep G2) .
|
-
- HY-B0239S2
-
|
|
JNK
Apoptosis
VEGFR
MMP
Bacterial
Akt
Autophagy
HIF/HIF Prolyl-Hydroxylase
Antibiotic
Beclin1
|
Cancer
|
|
Threo-Chloramphenicol-d6 is the deuterium labeled Chloramphenicol[1]. Chloramphenicol is an orally active, potent and broad-spectrum antibiotic. Chloramphenicol shows antibacterial activity. Chloramphenicol represses the oxygen-labile transcription factor and hypoxia inducible factor-1 alpha (HIF-1α) in hypoxic A549 and H1299 cells. Chloramphenicol suppresses the mRNA levels of vascular endothelial growth factor (VEGF) and glucose transporter 1, eventually decreasing VEGF release. Chloramphenicol can be used for anaerobic infections and lung cancer research[2][3][4].
|
-
- HY-N13176
-
|
|
Autophagy
Apoptosis
PI3K
Akt
mTOR
FAK
|
Cancer
|
Stellettin B is a triterpenoid compound that can be isolated from the marine sponge Jaspis stellifera. Stellettin B induces G1 phase arrest, apoptosis, and autophagy in human non-small cell lung cancer A549 cells by blocking the PI3K/Akt/mTOR pathway. Stellettin B can reduce the migration and invasion of liver cancer cells by decreasing the activation of the MAPK and FAK/PI3K/AKT/mTOR signaling pathways. Stellettin B can be used in the study of various tumors .
|
-
- HY-156444
-
|
|
HDAC
CDK
Apoptosis
|
Cancer
|
|
HDAC1/CDK7-IN-1 (compound 8e) is a dual CDK7 and HDAC1 inhibitor with IC50s of 893 nM and 248 nM, respectively. HDAC1/CDK7-IN-1 inhibits the growth cells of MDA-MB-231, MCF-7, A549, and HCT-116 cancer cells. HDAC1/CDK7-IN-1 induces cell cycle arrest and apoptosis in HCT-116 cells, as well as hindered the migration of HCT-116 cells .
|
-
- HY-157398
-
|
|
EGFR
|
Cancer
|
|
EGFR T790M/L858R-IN-3 (compound B1) is a EGFR L858R/T790M inhibitor with IC50 value of 13?nM. EGFR T790M/L858R-IN-3 shows anti-tumour activity in H1975 cells with an IC50 value of 0.087 μΜ. EGFR T790M/L858R-IN-3 inhibits cell migration in A549 cells and induces apoptosis in H1975 cells .
|
-
- HY-149918
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Antiproliferative agent-23 is a microtubule-destabilizing agent (MDA) and efficiently disturbes the tubulin-microtubule system. Antiproliferative agent-23 induces apoptosis via a mitochondrion-dependent pathway by downregulating the Bcl-2 protein, upregulating Bax and Cyt c proteins, and activating the caspase cascade. Antiproliferative agent-23 initiates reactive oxygen species (ROS)-mediated endoplasmic reticulum stress in A549/CDDP cells (cisplatin resistant cancer cell line) via the PERK/ATF4/CHOP signaling pathway. Antiproliferative agent-23 has anti-tumor activity .
|
-
- HY-121255
-
|
(R)-Cryptopleurine; NSC 19912
|
TMV
|
Cancer
|
|
(–)-Cryptopleurine is an alkaloid that has been found in Lauraceae and has diverse biological activities. It inhibits the growth of human A375 melanoma, A431 epidermoid carcinoma, A549 lung, MES-SA uterine sarcoma, and MCF-7 breast cancer cells (IC50=3 nM for all).2 (–)-Cryptopleurine inhibits hypoxia-induced gene expression in a hypoxia response element (HRE) reporter assay (IC50=8.7 nM).3 (–)-Cryptopleurine (500 μg/mL) prevents lesion formation in tobacco (N. tabacum) plants infected with tobacco mosaic virus (TMV). It also inhibits protein synthesis by yeast and mammalian ribosomes.
|
-
- HY-N8504
-
|
NSC 260179; Spectinabilin
|
Bacterial
|
Infection
|
|
Neoaureothin is a bacterial metabolite that has been found in Streptomyces. It is an androgen receptor (AR) antagonist that inhibits binding of dihydrotestosterone (DHT) to ARs (IC50=13 μM) and inhibits DHT-induced expression of prostate-specific antigen in LNCaP cells (IC50=1.75 nM). Neoaureothin is cytotoxic to A549, HCT116, and HepG2 cells (IC50s=34.3, 47, and 37.2 μg/mL, respectively). It also has nematocidal activity against the pine wood nematode B. xylophilus (LC50=0.84 μg/mL) and increases survival of P. densiflora trees inoculated with B. xylophilus.
|
-
- HY-162819
-
|
|
Apoptosis
|
Cancer
|
|
Apoptosis inducer 26 (compound [AgCl(dap2SH)(PPh3)2]) is an autophagy inducer based on mononuclear Ag(I) ligands, with antibacterial and anticancer activities against a variety of bacterial strains and cancer cell lines. Apoptosis inducer 26 can effectively inhibit the growth of both Gram(+) and Gram(-) bacteria by causing the accumulation of Ag(I) ions in the bacterial periplasm. Apoptosis inducer 26 can intercalate between base pairs of CT DNA and induce apoptosis in A549 cells. Apoptosis inducer 26 also has the ability to scavenge free radicals, which can protect against oxidative stress .
|
-
- HY-B0530A
-
|
γ-pipradol hydrochloride
|
Reactive Oxygen Species
mAChR
NADPH Oxidase
|
Cancer
|
|
Azacyclonol (γ-pipradol) hydrochloride is a compound with promising anticancer activity, showing effectiveness in inhibiting NOX-derived ROS in A549 human lung cancer cells. Azacyclonol hydrochloride exhibits enhanced proliferation inhibition against androgen-refractory cancer cell lines, specifically DU145 and PC-3. Azacyclonol hydrochloride demonstrates antitumor activity in DU145-xenografted chorioallantoic membrane tumor models. Azacyclonol hydrochloride also acts as a ligand for the M3 muscarinic acetylcholine receptor, which is overexpressed in ARPC. Azacyclonol hydrochloride effectively blocks carbachol-induced proliferation and NOX activity in DU145 cells. Azacyclonol hydrochloride can also be utilized for the treatment of chronic schizophrenia.
|
-
- HY-144791
-
|
|
Bcl-2 Family
MDM-2/p53
Caspase
Apoptosis
|
Cancer
|
|
Bcl-2-IN-6 (compound 10) is a potent Bcl-2 (B-cell lymphoma-2) inhibitor. Bcl-2-IN-7 down-regulates the expression of Bcl-2, and increases the expression of p53, Bax, and caspase-7 mRNA. Bcl-2-IN-7 induces cell cycle arrest and apoptosis in breast cancer MCF-7 cells. Bcl-2-IN-7 shows good anticancer activity, with IC50 values of 20.91, 22.30, 42.29, and 48.00 μM against MCF-7, LoVo, HepG2, and A549 cell lines, respectively .
|
-
- HY-144792
-
|
|
Bcl-2 Family
MDM-2/p53
Caspase
Apoptosis
|
Cancer
|
|
Bcl-2-IN-7 (compound 6) is a potent Bcl-2 (B-cell lymphoma-2) inhibitor. Bcl-2-IN-7 down-regulates the expression of Bcl-2, and increases the expression of p53, Bax, and caspase-7 mRNA. Bcl-2-IN-7 induces cell cycle arrest and apoptosis in breast cancer MCF-7 cells. Bcl-2-IN-7 shows good anticancer activity, with IC50 values of 20.17, 22.64, 45.57, and 51.50 μM against MCF-7, LoVo, HepG2, and A549 cell lines, respectively .
|
-
- HY-155816
-
|
|
PROTACs
|
Cancer
|
|
PROTAC NSD3 degrader-1 (compound 56) is a PROTAC targeting to Nuclear receptor binding SET domain protein NSD3. PROTAC NSD3 degrader-1 specifically induces NSD3 degradation with DC50 values of 1.43 and 0.94 μM in lung cancer cells NCI-H1703 and A549, respectively. PROTAC NSD3 degrader-1 suppresses the methylation of H3K36, induces apoptosis, and causes cell-cycle arrest. PROTAC NSD3 degrader-1 also downregulates the expression of NSD3-associated genes such as CDC25A, ALDH1A1, and IGFBP.
|
-
- HY-170438
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-139 (compound PD 18) is an epidermal growth factor receptor (EGFR) inhibitor, with IC50s of 12.88 (wild type), 10.84 (L858R/T790M), 42.68 (L858R/T790M/C797S) nM, respectively. EGFR-IN-139 displays strong anticancer activity against A549 and H1975 cancer cell lines, which are highly expressed EGFR. EGFR-IN-139 has a strong selectivity to cancer cells. EGFR-IN-139 can be used for nonsmall cell lung cancer (NSCLC) research[1].
|
-
- HY-P10819
-
|
|
Histone Demethylase
Apoptosis
|
Cancer
|
|
S9-CMC1 TFA is a covalent peptide lysine-specific demethylase 1 (LSD1) inhibitor with an IC50 value of 2.53 μM. S9-CMC1 TFA specifically recognizes Cys360 in the enzyme-active region. S9-CMC1 TFA inhibits LSD1 activity, increasing H3K4me1 and H3K4me2 levels, leading to G1 cell cycle arrest and apoptosis and inhibiting cell proliferation. S9-CMC1 TFA significantly inhibits tumor growth in A549 xenograft animal models .
|
-
- HY-169921
-
|
|
c-Myc
Apoptosis
|
Cancer
|
|
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 .
|
-
- HY-147825
-
|
|
EGFR
Raf
Apoptosis
|
Cancer
|
|
EGFR/BRAFV600E-IN-1 (Compound 23) is a potent EGFR and BRAF V600E dual inhibitor with IC50s of 0.08 and 0.15 µM, respectively. EGFR/BRAFV600E-IN-1 induces apoptosis and cell cycle arrest in both pre-G1 and G2/M phases. EGFR/BRAFV600E-IN-1 exhibits antiproliferative activity againist A-549, MCF-7, Panc-1, HT-29 with IC50s of 1.2, 0.79, 1.3, and 1.23 µM, respectively .
|
-
- HY-170968
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
EGFR-IN-150 is an EGFR inhibitor that effectively suppresses the phosphorylation of mutant epidermal growth factor receptor (EGFR) and its downstream AKT signaling pathway, thereby exerting antitumor effects and inducing HMOX1 expression to trigger ferroptosis. EGFR-IN-150 exhibits an IC50 of 0.386 μM against the non-small cell lung cancer (NSCLC) cell line H1975, and significantly inhibits colony formation and migration of both H1975 and A549 cells while inducing apoptosis. In addition, EGFR-IN-150 markedly suppresses tumor growth in the H1975 cell-derived xenograft (CDX) mouse model. EGFR-IN-150 holds promise for research related to non-small cell lung cancer .
|
-
- HY-155759
-
|
|
NF-κB
Interleukin Related
Caspase
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
HMGB1-IN-2 (compound 15) is an inhibitor of highly conserved nuclear protein (HMGB1), showing NO inhibitory effect with IC50 value of 20.2 μM in RAW264.7 cells. HMGB1-IN-2 (30 μM) decreases the level of IL-1 β, TNF-α, caspase-1 p20, inhibits the phosphorylation of NF-κB p65, exhibits anti-apoptotic activity. HMGB1-IN-2 (15 mg/kg; ip) relives kidney injury in septic acute kidney injury mouse. HMGB1-IN-2 inhibits Huh7 cells and A549 cells with IC50s of 77.0 μM, and 82.0 μM, respectively .
|
-
- HY-149388
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Anticancer agent 139 (Compound 6h) has potent anticancer activity. Anticancer agent 139 displayed a π–cationic interaction with the residue Lys352 of Tublin. Anticancer agent 139 has good anticancer activity against SNB-19, OVCAR-8, and NCI-H40 with PGIs of 86.61, 85.26, and 75.99, respectively. Anticancer agent 139 also has moderate anticancer activity against HOP-62, SNB-75, ACHN, NCI/ADR-RES, 786-O, A549/ATCC, HCT-116, and MDA-MB-231 with PGIs of 67.55, 65.46, 59.09, 59.02, 57.88, 56.88, 56.53, 56.4, and 51.88 respectively .
|
-
- HY-170524
-
|
|
SARS-CoV
DNA Methyltransferase
|
Infection
|
|
TDI-015051 is an orally active inhibitor for SARS-CoV-2 nonstructural protein 14 (NSP14) with an IC50 ≤0.15 nM. TDI-015051 inhibits SARS-CoV-2 NSP14 in Huh-7.5 cell (EC50=11.4 nM) and in ACE2-TMPRSS2 expressing A549 cell (EC50=64.7 nM). TDI-015051 also inhibits other coronaviruses like α-hCoV-NL63, α-hCoV-229E and β-hCoV-MERS with IC50s of 1.7, 2.6 and 3.6 nM, respectively. TDI-015051 binds to the SAH-stabilized cap binding pocket, inhibits viral RNA methylation and viral replication, and exhibits anti-infectious activity in mouse models .
|
-
- HY-138185
-
|
SF 2738A
|
Bacterial
Apoptosis
|
Cancer
|
|
Collismycin A is a bacterial metabolite originally isolated from Streptomyces that has diverse biological activities, including antibacterial, antiproliferative, and neuroprotective properties. It is active against a variety of bacteria (MICs=6.25 and 100 μg/mL) and fungi (MICs=12.5-100 μg/mL). It inhibits proliferation of A549 lung, HCT116 colon, and HeLa cervical cancer cells (IC50s=0.3, 0.6, and 0.3 μM, respectively) and NIH373 fibroblasts (IC50=56.6 μM) but not MDA-MD-231 breast cancer cells (IC50=>100 μM). Collismycin A forms a complex with Fe(II) and Fe(III) at a 2:1 ratio, and the addition of iron ions inhibits the antiproliferative effect of collismycin A on HeLa cells, an effect that does not occur with the addition of zinc, manganese, copper, or magnesium ions.3 Collismycin A (1 μM) prevents apoptosis in the brain region of zebrafish larvae in a model of neuronal cell death induced by all-trans retinoic acid.
|
-
- HY-170932
-
|
|
EGFR
COX
Apoptosis
|
Cancer
|
|
EGFR/COX-2-IN-1 is an EGFR/COX-2 inhibitor. EGFR/COX-2-IN-1 inhibits EGFR WT, EGFR T790M, COX-1 and COX-2 with IC50s of 0.12, 0.076, 20.1 and 1.52 μM respectively. EGFR/COX-2-IN-1 inhibits and with IC50s of , respectively. EGFR/COX-2-IN-1 inhibits MCF-7, HT-29 and A-549 with IC50s of 1.20, 5.14 and 14.81 μM, respectively. EGFR/COX-2-IN-1 displays Apoptosis induction by up-regulating Bax and down-regulating Bcl-2 protein levels. EGFR/COX-2-IN-1 results in a significant increase in the percentage of cells at the G2/M in MFC-7 cells. EGFR/COX-2-IN-1 exhibits broad-spectrum antitumor effects .
|
-
- HY-159087
-
|
|
PROTACs
|
Cancer
|
|
RGB110 (Compound 10d) is a PROTAC inhibitor for D-dopachrome tautomerase with an IC50 of 5.9 μM. RGB110 causes no degradation of D-DT. (Pink: ligand for target protein (HY-159164); Black: linker (HY-W125017); Blue: ligand for E3 ligase CRBN (HY-10984))
|
-
- HY-N14995
-
-
- HY-134563
-
|
|
Caspase
Apoptosis
|
Cancer
|
|
Z-Asp(OMe)-Gln-Met-Asp(OMe)-FMK is an inhibitor for caspase-3, and inhibits Dihydroartemisinin (HY-N0176) and Dictamnine (HY-N0849) co-induced apoptosis .
|
-
- HY-173034
-
|
|
Phosphatase
Apoptosis
|
Cancer
|
|
PTP1B-IN-30 (Compound 3j) is the inhibitor for PTP1B with an IC50 of 0.51 µM. PTP1B-IN-30 inhibits the proliferation of cancer cell T47D with an IC50 of 21.21 µM, arrests the cell cycle at S phase, and induces apoptosis in T47D .
|
-
- HY-163628
-
|
|
SARS-CoV
|
Infection
|
|
SARS-CoV-2 Mpro-IN-20 (compound MPI100) is a SARS-CoV-2 main protease inhibitor. SARS-CoV-2 Mpro-IN-20 shows antiviral activity with the EC50 of 3.4 μM .
|
-
- HY-163414
-
|
|
Carbonic Anhydrase
|
Cancer
|
|
hCAIX/XII-IN-11 (Compound 6c) is an inhibitor of hCA IX and hCA XII with a Ki value of 0.7 μM for both the isoforms. hCAIX/XII-IN-11 can be used for anticancer research .
|
-
- HY-137918
-
|
|
Src
TGF-β Receptor
Anaplastic lymphoma kinase (ALK)
|
Others
|
|
TGF-βRI inhibitor 3 (Compound 9ac) is a selective TGF-β inhibitor. TGF-βRI inhibitor 3 can effectively inhibit the TGF-β signaling pathway. TGF-βRI inhibitor 3 has IC50 values of 13 μM and 0.63 μM for c-Src kinase and ALK5 kinase, respectively .
|
-
- HY-136945
-
|
|
IFNAR
|
Cancer
|
|
StA-IFN-1 is an inhibitor for type I interferon (IFN), that inhibits the activation of IFNβ with an IC50 of 4.1 μM .
|
-
- HY-112914
-
|
|
mTOR
Autophagy
|
Cancer
|
|
mTOR inhibitor-1 (Compound C-4) is an ATP-Competitive mTOR inhibitor which can suppress cells proliferation and inducing autophagy .
|
-
- HY-128840
-
|
|
PROTACs
MDM-2/p53
|
Cancer
|
|
PROTAC MDM2 Degrader-1 (Compound 15a) is a MDM2 PROTAC degrader. The structures of both Linker ends of PROTAC MDM2 Degrader-1 are MDM2 ligands. PROTAC MDM2 Degrader-1 can not only block the binding of p53-MDM2, but also degrade the target MDM2 protein by utilizing the function of the E3 ligase of MDM2 itself, thus exerting an anti-tumor effect. (Pink: MDM2 ligand 2 (HY-128836); Black: Linker (HY-128844); Blue: E3 ligase Ligand 15 (HY-128836))
|
-
- HY-161400
-
|
|
TGF-β Receptor
|
Cancer
|
|
TGFβRII-IN-2 (Compound 3n) is an inhibitor for transforming growth factor-β type II receptor (TGFβRII) with IC50 of 2.4 μM, which blocks endothelial-to-mesenchymal transition and cell migration in different cancer cell lines without perturbing the microtubule network .
|
-
- HY-172100
-
|
|
Apoptosis
Reactive Oxygen Species
p38 MAPK
|
Cancer
|
|
p38-α MAPK-IN-8 (Compound 13) is a lipophilic cationic derivative. p38-α MAPK-IN-8 is cytotoxic to various tumor cells, and can induce cell cycle arrest, apoptosis, increase reactive oxygen species (ROS) production, and induce mitochondrial membrane potential depolarization. The antitumor activity of p38-α MAPK-IN-8 may be related to p38α MAPK pathway, which can be used in the study of cancer .
|
-
- HY-W010320
-
|
2-Ethyl-3-hydroxy-4H-pyran-4-one
|
Heme Oxygenase (HO)
|
Others
|
|
Ethyl maltol (2-Ethyl-3-hydroxy-4H-pyran-4-one) is an orally active and important food additive and flavor enhancer. Ethyl maltol is less toxic to rats and dogs. Ethyl maltol can enhance copper-mediated cytotoxicity and induce apoptosis in lung epithelial cells .
|
-
- HY-19715
-
-
- HY-149001
-
|
|
PARP
|
Cancer
|
|
PARP1-IN-9 (Compound 5c) is a PARP1 inhibitor with an IC50 of 30.51 nM. PARP1-IN-9 induces cell apoptosis and shows anticancer activity. PARP1-IN-9 has higher potency than Olaparib (HY-10162) .
|
-
- HY-111783
-
|
|
DNA-PK
ATM/ATR
PI3K
Apoptosis
|
Cancer
|
|
AZD-7648 is a potent, orally active, selective DNA-PK inhibitor with an IC50 of 0.6 nM. AZD-7648 induces apoptosis and shows antitumor activity .
|
-
- HY-151981
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-74 (Compound 21) is a potent EGFR inhibitor with an IC50 of 138 nM against EGFR L858R/T790M. EGFR-IN-74 induces cancer cell apoptosis .
|
-
- HY-16941
-
|
|
Others
|
Cancer
|
|
Damulin A is a saponin found in G. pentaphyllum with anti-cancer activities .
|
-
- HY-170760
-
|
|
Bacterial
|
Infection
|
|
Antibacterial agent 258 (Compound 11e) is an antibacterial agent, that destory the bacteria cell membrane, and inhibits various gram-positive bacteria (MIC for Staphylococcus aureus is 1-2 μg/mL). Antibacterial agent 258 exhibits low hemolytic activity and low cytotoxicity. Antibacterial agent 258 exhibits anti-infectious efficacy in mouse models .
|
-
- HY-161766
-
|
|
TRP Channel
|
Cancer
|
|
L687 is a potent activator of TRPC3/C6/C7 that can induce cellular uptake of oligonucleotides .
|
-
- HY-161775
-
|
|
RET
Trk Receptor
|
Cancer
|
|
RET/TRKA-IN-1 (Compound 13) is a dual inhibitor for RET (IC50=0.375 µM) and TRKA. RET/TRKA-IN-1 inhibits cell viability of LC-2 and KM12, with GI50 of 0.72 and 0.25 μM. RET/TRKA-IN-1 arrests the cell cycle at G1 phase .
|
-
- HY-110115
-
|
|
Mps1
|
Cancer
|
|
TC-Mps1-12 is a potent and selective monopolar spindle 1 (Mps1) inhibitor, with an IC50 of 6.4 nM .
|
-
- HY-172253
-
|
|
Apoptosis
|
Cancer
|
|
(5R)-Dimethylbenzene-camptothecin (Compound 6a) is a camptothecin derivative. (5R)-Dimethylbenzene-camptothecin is cytotoxic to tumor cells and can induce apoptosis and cell cycle arrest. (5R)-Dimethylbenzene-camptothecin has anti-tumor activity .
|
-
- HY-122942
-
-
- HY-156914
-
|
|
IGF-1R
Src
|
Cancer
|
|
IGF-1R/SRC-IN-1 (Compound 3b) is an inhibitor for IGF-1R (IC50 is 63 μM) and SRC .
|
-
- HY-172155
-
|
|
MEK
|
Cancer
|
|
MEK1/2-IN-3 (Compound M15) is a MEK1 inhibitor with an IC50 of 10.29 nM. MEK1/2-IN-3 can inhibit the proliferation and migration, induce apoptosis of tumor cells. MEK1/2-IN-3 has good liver microsomal stability. MEK1/2-IN-3 can be used for the research of solid tumors .
|
-
- HY-13525
-
|
|
Biochemical Assay Reagents
|
Metabolic Disease
Cancer
|
|
CP-91149 is a GP (glycogen phosphorylase) inhibitor. CP-91149 promotes glycogen resynthesis, but not its overaccumulation. CP-91149 has the potential for Type II (insulin-dependent) diabetes study .
|
-
- HY-150004
-
|
|
c-Met/HGFR
HDAC
Apoptosis
|
Cancer
|
|
c-Met/HDAC-IN-3 (Compound 15f) is a dual c-Met and HDAC inhibitor with IC50 values of 12.50 nM and 26.97 nM against c-Met and HDAC1, respectively. c-Met/HDAC-IN-3 induces apoptosis and cause cell cycle arrest in G2/M phase .
|
-
- HY-170436
-
|
|
Photosensitizer
Apoptosis
|
Cancer
|
|
NFh-NMe-2 is a photosensitizer, that interacts with nitroreductase, generates singlet oxygen in tumor cells, exhibits cytotoxicity in cancer cells, and induces apoptosis. NFh-NMe-2 exhibits antitumor efficacy in mouse models .
|
-
- HY-160438B
-
|
|
Bcl-2 Family
Survivin
|
Cancer
|
|
PBX-7011 TFA is a derivative of camptothecin (HY-16560), which inhibits expressions of the cancer related survival genes DDX5, Survivin, Mcl-1 and XIAP in cells FaDu, degrades DDX5 proteins and exhibits anticancer activity .
|
-
- HY-170886
-
|
|
SARS-CoV
Virus Protease
|
Infection
|
|
SARS-CoV-2 Mpro-IN-36 (Compound 6d) is an inhibitor of SARS-CoV-2 M pro with an IC50 of 110 nM. SARS-CoV-2 Mpro-IN-36 exhibits antiviral activity with an EC50 of 1.6 μM .
|
-
- HY-160788
-
-
- HY-N12996
-
|
|
Others
|
Others
|
|
Sitosterone is a steroid that can be isolated from stem bark of syzygium aqueum. Sitosterone shows cytotoxicity .
|
-
- HY-N0203R
-
|
|
Apoptosis
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Atractylenolide III (Standard) is the analytical standard of Atractylenolide III. This product is intended for research and analytical applications. Atractylenolide III (ICodonolactone) is the main component of Atractylodes rhizome and has the activity of inducing apoptosis in lung cancer cells. Atractylenolide III is an orally active gastroprotective agent .
|
-
- HY-160220S
-
|
|
Ras
|
Cancer
|
|
KRAS inhibitor-23 (Isomer 2 of compound i) is a potent inhibitor of KRAS that plays an important role in cancer research .
|
-
- HY-161388
-
|
|
Ferroptosis
Mitophagy
|
Cancer
|
|
NSCLC-IN-1 (Compound A10-2) induces mitophagy and ferroptosis through targeting transmembrane BAX inhibitor motif containing 6 (TMBIM6). NSCLC-IN-1 induces mitochondrial Ca 2+ imbalance, leading to mitochondrial damage. NSCLC-IN-1 reduces intracellular glutathione (GSH), increases the accumulation of lipid peroxides (LPO) and malondialdehyde (MDA) content. NSCLC-IN-1 is a potent anti-NSCLC agent .
|
-
- HY-N0203
-
|
ICodonolactone; 8β-Hydroxyasterolide
|
Apoptosis
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Atractylenolide III (ICodonolactone) is the main component of Atractylodes rhizome and has the activity of inducing apoptosis in lung cancer cells. Atractylenolide III is an orally active gastroprotective agent .
|
-
- HY-106035
-
|
YSV
|
P-glycoprotein
|
Cancer
|
|
Tyroservatide (YSV) is an active, low-molecular-weight polypeptide that has been shown to have antitumor effects on hepatocellular carcinoma and lung cancer cell .
|
-
- HY-N15227
-
|
|
Others
|
Cancer
|
|
(+)-N-Methylhernovine is an aporphine alkaloid that can be isolated from Hernandia nymphaeifolia. (+)-N-Methylhernovine exhibits slight cytotoxicity in cancer cells .
|
-
- HY-P10403
-
|
|
IGF-1R
|
Inflammation/Immunology
Cancer
|
|
IGFBP-3 peptide is a 18-amino acid insulin-like growth factor binding protein-3. IGFBP-3 peptide binds Humanin (HY-P1928) and Hyaluronan (HY-B0633A), blocks the interaction of CD44 and hyaluronan .
|
-
- HY-143458
-
|
|
FAK
PROTACs
|
Cancer
|
|
FAK PROTAC B5 (Compound B5) is a FAK PROTAC degrader with an IC50 value of 14.9 nM. FAK PROTAC B5 presents strong FAK degradation activity, antiproliferative activity, outstanding plasma stability and moderate membrane permeability. FAK PROTAC B5 inhibits cell migration and invasion .
|
-
- HY-103464
-
|
5'-FIO
|
FLT3
|
Cancer
|
|
5'-Fluoroindirubinoxime (5’-FIO, compound 13), an Indirubin (HY-N0117) derivative, is a potent FLT3 inhibitor, with an IC50 of 15 nM .
|
-
- HY-144760
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
EGFR-IN-3 (Compound 4c) is a potent EGFR inhibitor with an IC50 of 0.32 µM against EGFRwt-TK. EGFR-IN-3 shows cytotoxic activity against cancer cell lines and induces apoptosis .
|
-
- HY-125097
-
|
|
Bacterial
|
Cancer
|
|
5'-Hydroxy-staurosporine is an indolocarbazole alkaloid that can be isolated from marine Micromonospora sp. (strain L-31-CLCO-002). 5'-Hydroxy-staurosporine can be used in tumor related research .
|
-
- HY-157960
-
|
|
VEGFR
|
Cancer
|
|
VEGFR-2-IN-42 (compound 8c) is a potent VEGFR-2 inhibitor. VEGFR-2-IN-42 shows anti-proliferative effect against MCF7 cells with the IC50 of 25 µM .
|
-
- HY-146539
-
|
|
HDAC
VEGFR
|
Cancer
|
|
HDAC-IN-35 (Compound 14) is a potent, selective HDAC and VEGFR-2 inhibitor, with IC50 values of 0.166 and 13.2 µM for HDAC6 and VEGFR-2, respectively .
|
-
- HY-120786
-
|
6-(3′,4′,5′-Trimethoxybenzoyl)quinoline
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
MPT0B014 is a tubulin polymerization inhibitor. MPT0B014 induces cancer cell apoptosis. MPT0B014 can be used for the research of cancer .
|
-
- HY-150694
-
|
|
HDAC
|
Cancer
|
|
HDAC6-IN-11 (Compound 9) is a selective HDAC6 inhibitor with the IC50 value of 20.7 nM. HDAC6-IN-11 has more than 300-fold selectivity over HDAC other isoforms. HDAC6-IN-11 shows anti-proliferative activities against cancer cells .
|
-
- HY-121893
-
|
|
MDM-2/p53
NF-κB
|
Cancer
|
|
p53-MDM2-IN-3 (Compound 5s) is an orally active p53-MDM2 inhibitor with a Ki value of 0.25 μM. p53-MDM2-IN-3 exerts antitumor activity by inhibiting NF-κB pathway .
|
-
- HY-N3222
-
|
|
HIV
|
Infection
Cancer
|
|
Myriceric acid B is a potent HIV-1 entry inhibitor targeting gp41. Myriceric acid B is an antitumor agent .
|
-
- HY-161419
-
|
|
Histone Methyltransferase
|
Cancer
|
|
EZH2-IN-18 (compound 9e) is a potent inhibitor of enhancer of zeste homologue 2 (EZH2 WT) , with the IC50 of 1.01 nM. EZH2-IN-18 shows inhibition in proliferation and induction in apoptosis in tumor cells .
|
-
- HY-N12004
-
|
|
Others
|
Cancer
|
|
19-Hydroxy-10-deacetylbaccatin III (compound 13) is a taxane with potential antitumor activity. 19-Hydroxy-10-deacetylbaccatin III has weak cytotoxicity against A498 and NCI-H226 cell lines. The study found that the inhibition rates of 30 μg/mL 19-Hydroxy-10-deacetylbaccatin III on A498, NCI-H226 and PC-3 were 16.6% and 32% respectively .
|
-
- HY-110245
-
|
VU364849
|
Apoptosis
|
Cancer
|
|
DMH2 is a potent BMP receptor antagonist. DMH2 downregulates the expression of Id1 and Id3 proteins, and inhibits the proliferation and induces cell death of lung cancer cell lines .
|
-
- HY-168502
-
|
|
Apoptosis
HDAC
|
Cancer
|
|
HDAC-IN-81 (Compound 11g) is an HDAC inhibitor that can effectively inhibit HDAC1 (IC50 = 4.5 nM). HDAC-IN-81 possesses anti-cancer cell proliferation activity and can induce cell apoptosis .
|
-
- HY-100683
-
|
|
Phosphatase
|
Cancer
|
|
A12B4C3 is a potent human polynucleotide kinase/phosphatase (hPNKP) inhibitor with an IC50 value of 0.06 μM. A12B4C3 has antiproliferative activity against cancer cells. A12B4C3 can also enhance the radiosensitivity of certain cancer cells .
|
-
- HY-168926
-
|
|
Reactive Oxygen Species
Apoptosis
|
Cancer
|
|
NQO2-IN-1 (Compound 20b) is the inhibitor for quinone oxidoreductase (NQO) that inhibits NQO2 with an IC50 of 95 nM. NQO2-IN-1 overcomes the resistance of NSCLC cells to tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) by induction of ROS and apoptosis .
|
-
- HY-172179
-
|
|
EGFR
VEGFR
|
Cancer
|
|
EGFR/VEGFR2-IN-5 (Compound 14) is an orally active dual inhibitor of EGFR and VEGFR2 with an IC50 value of 1.15 µM for VEGFR2 and an IC50 value of 0.28 μM for EGFR T790M. EGFR/VEGFR2-IN-5 has significant anticancer activity .
|
-
- HY-146200
-
|
|
PI3K
mTOR
|
Cancer
|
|
PI3K/mTOR Inhibitor-8 (Compound 18b) is a PI3K and mTOR dual inhibitor with IC50 values of 0.46 nM and 12 nM against PI3Kα and mTOR, respectively. PI3K/mTOR Inhibitor-8 induces HCT-116 cells apoptosis and arrests cell cycle at the G1/S phase .
|
-
- HY-149092
-
|
|
TAM Receptor
|
Cancer
|
|
Anticancer agent 109 (compound 6-15) is an inhibitor of the Gas6-Axl axis with anti-cancer activity. Anticancer agent 109 inhibits the expression of Gas6 and Axl, and the expression p-PI3K and p-AKT in cancer cells, leads to G1 phase arrest and promotes cancer cells apoptosis, and inhibits tumor growth significantly in nude mouse tumor bearing models .
|
-
- HY-149260
-
-
- HY-118319
-
-
- HY-170607
-
|
|
Apoptosis
|
Cancer
|
|
HPCR exhibits anti-proliferative activity against multi cancer cells. HPCR is involved in cell apoptosis .
|
-
- HY-158331
-
|
|
PROTACs
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
|
Gal-ARV-771, PROTAC prodrug, is a gal modified ARV-771 (HY-100972). Gal-ARV-771 can be activated in SA-β-Gal-expressed cancer senescent cells to release ARV-771. Gal-ARV-771 induces selective degradation of BRD4 protein by the ubiquitin-proteasome pathway in senescent cells. Gal-ARV-771 promotes apoptosis of senescent cancer cells .
|
-
- HY-129125
-
|
|
STAT
|
Cancer
|
|
YMU1 is a selective inhibitor of human thymidylate kinase (hTMPK) with an IC50 of 610 nM. YMU1 inhibits tumor proliferation .
|
-
- HY-149578
-
|
|
Microtubule/Tubulin
HDAC
|
Cancer
|
|
Tubulin/HDAC-IN-3 (compound 12a) is a potent tubulin/HDAC dual inhibitor. Tubulin/HDAC-IN-3 effectively disrupts tubulin polymerization (IC50: 5.4 μM). Tubulin/HDAC-IN-3 exhibits potent HDAC1/8 inhibitory activities, with IC50 values of 0.155 and 0.177 μM, respectively. Tubulin/HDAC-IN-3 works through blocking cellular cycle, inducing apoptosis and inhibiting colony formation .
|
-
- HY-136431
-
|
|
Aminoacyl-tRNA Synthetase
|
Cancer
|
|
BC-DXI-843 is a potent and specific AIMP2-DX2 inhibitor with an IC50 of 0.92 μM, more than 100-fold selectivity over AIMP2 (IC50 >100 μM) in a luciferase assay. BC-DXI-843 acts as a promising lead targeting AIMP2-DX2 in lung cancer .
|
-
- HY-170909
-
|
|
PIKfyve
|
Others
|
|
PIKfyve-IN-4 (Compound 40) is an orally active and selective inhibitor of phosphatidylinositol-3-phosphate 5-kinase (PIKfyve), with an IC50 of 0.60 nM. PIKfyve-IN-4 exhibits good systemic tolerance .
|
-
- HY-143460
-
|
|
Carbonic Anhydrase
|
Cancer
|
|
CAXII-IN-1 (Compound 17) is a selective CA XII inhibitor with Ki values of 3.8 nM and 56.0 nM against hCA XII and hCA IX, respectively. CAXII-IN-1 shows antitumor activity .
|
-
- HY-116052
-
|
|
MDM-2/p53
NF-κB
|
Cancer
|
|
p53-MDM2-IN-2 (Compound 5q) is an orally active p53-MDM2 inhibitor with a Ki value of 0.25 μM. p53-MDM2-IN-2 exerts antitumor activity by inhibiting NF-κB pathway .
|
-
- HY-161402
-
|
|
DNA Methyltransferase
|
Cancer
|
|
METTL16-IN-1 is a potent METTL16 inhibitor with an IC50 value of 1.7 μM and a Kd value of 1.35 μM. Mettl16-in-1 inhibits the binding interaction of U6 snRNA deletion and METTL16 MTD with an IC50 value of 2.5 μM. METTL16-IN-1 has antitumor activity .
|
-
- HY-152077
-
|
|
Apoptosis
|
Cancer
|
|
Telomerase-IN-5 is a potent telomerase inhibitor. Telomerase-IN-5 has antiproliferative activity and induces apoptosis .
|
-
- HY-169483
-
-
- HY-121254
-
|
|
Acyltransferase
|
Cancer
|
|
GERI-BP002-A is an inhibitor of acyl-CoA:cholesterol acyltransferase (ACAT) produced by Aspergillus fumigatus F93, which can be used in cancer research .
|
-
- HY-163872
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
PROTAC SMARCA2/4-degrader-10 (compound I-399) is a potent SMARCA2 degrader with an DC50 value of ＜100 nM. PROTAC SMARCA2/4-degrader-10 has the potential for the research of cancer (Blue:SMARCA2/4 ligand, (HY-159542); Black: linker (HY-W088435); Pink:VHL ligand (HY-125845)) .
|
-
- HY-161338
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulin polymerization-IN-61 (Compound 9a) is a tubulin polymerization inhibitor. Tubulin polymerization-IN-61 destroys the microtubule skeleton, blocks the cell cycle in G2/M phase, induces Apoptosis, and inhibits cancer cell migration and colony formation. Tubulin polymerization-IN-61 shows antitumor activity in vivo against 4T1 xenograft model .
|
-
- HY-163807
-
|
|
PROTACs
FKBP
|
Cancer
|
|
22-SLF is a PROTAC degrader, that degrades FK506-binding protein 12 (FKBP12) with a DC50 of 0.5 µM in a FBXO22 dependent manner. 22-SLF degrades other endogenous proteins, such as BRD4 and EML4-ALK fusion protein.(Pink: Ligand for target protein SLF (HY-114872); Black: Linker (HY-163821); Blue: Ligand for E3 ligase (HY-163826)) .
|
-
- HY-168529
-
|
|
Myosin
|
Cancer
|
|
NU074381b (compound 5b) is a potent S100A4 inhibitor. NU074381b inhibits S100A4-NMII complex formation with an IC50 value of 0.48 µM. NU074381b inhibits cell proliferation and migration .
|
-
- HY-147731
-
|
|
HDAC
|
Cancer
|
|
HDAC6-IN-9 (compound 12c) is a potent and selective HDAC6 inhibitor with IC50 values of 11.8, 15.2, 4.2, 139.6, 21.3 nM for HDAC1,HDAC3, HDAC6, HDAC8, HDAC10, respectively. HDAC6-IN-9 shows anti-proliferative activities .
|
-
- HY-N6727
-
|
Aspergillin
|
Apoptosis
PKA
NF-κB
Bacterial
Fungal
Antibiotic
|
Infection
Inflammation/Immunology
Cancer
|
|
Gliotoxin is a secondary metabolite, the most abundant mycotoxin secreted by A. fumigatus, inhibits the phagocytosis of macrophages and the immune functions of other immune cells . Gliotoxin inhibits inducible NF-κB activity by preventing IκB degradation, which consequently induces host-cell apoptosis . Gliotoxin activates PKA and increases intracellular cAMP concentration; modulates actin cytoskeleton rearrangement to facilitate A. fumigatus internalization into lung epithelial cells . Gliotoxin is a potent NOTCH2 transactivation inhibitor, can effectively induce apoptosis of chronic lymphocytic leukemia (CLL) cells .
|
-
- HY-163270
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
PM534, tubulin targeting agent, inhibits tubulin assembly with IC50 values of 0.8-3.2 nM. PM534 binds to the colchicine site of tubulin, which has high antitumor activity .
|
-
- HY-147801
-
|
|
Topoisomerase
Apoptosis
|
Cancer
|
|
Topoisomerase IIα-IN-3 (Compound 12c) is a DNA intercalative topoisomerase-IIα inhibitor. Topoisomerase IIα-IN-3 arrests cell cycle at the G0/G1 phase and induces apoptosis .
|
-
- HY-163661
-
|
|
Apoptosis
Autophagy
MDM-2/p53
|
Cancer
|
|
p53-MDM2-IN-5 (compound 5a) is a potent p53-MDM2 inhibitor. p53-MDM2-IN-5 induces apoptosis, autophagy and DNA damage. p53-MDM2-IN-5 induces cell cycle arrest at S and G2/M phases. p53-MDM2-IN-5 shows anti-tumor activity .
|
-
- HY-N11082
-
-
- HY-125158A
-
|
|
Aurora Kinase
|
Cancer
|
|
(E/Z)-HOI-07 is a potent and selective Aurora B inhibitor. HOI-07 has antitumor activity .
|
-
- HY-B1041
-
|
Pimagedine hydrochloride; GER-11; Aminoguanidinium chloride
|
NO Synthase
Apoptosis
|
Endocrinology
|
|
Aminoguanidine hydrochloride (Pimagedine hydrochloride) is an inhibitor of diamine oxidase and nitric oxide synthase. Aminoguanidine hydrochloride has a dose-dependent inhibitory effect on apoptosis induced by Doxorubicin (HY-15142). Aminoguanidine hydrochloride has antioxidant properties. Aminoguanidine hydrochloride can be used in diabetic nephropathy research .
|
-
- HY-170590
-
|
|
VEGFR
Apoptosis
Reactive Oxygen Species
|
Cancer
|
|
VEGFR-2-IN-61 (Compound 7b) is an inhibitor for VEGFR-2 with an IC50 of 2.83 µM. VEGFR-2-IN-61 inhibits the proliferation of multi cancer cells (IC50 for MCF-7 is 2.12 μM). VEGFR-2-IN-61 inhibits the cell migration, induces oxidative stress and apoptosis in MCF-7 .
|
-
- HY-145859
-
-
- HY-162102
-
|
|
Discoidin Domain Receptor
|
Cancer
|
|
DDR1-IN-8 (compound 7s) is a potent inhibitor of DDR1/2, with the IC50 values of 0.045 μM and 0.126 μM, respectively. DDR1-IN-8 has anti-tumor activity .
|
-
- HY-157872
-
|
|
Aldehyde Dehydrogenase (ALDH)
|
Cancer
|
|
ALDH1A1-IN-4 (compound A1) is a potent inhibitor of aldehyde dehydrogenase (ALDH) A1, with IC50 value of 0.32 μM. ALDH1A1-IN-4 plays an important role in cancer research .
|
-
- HY-162344
-
|
|
Apoptosis
Autophagy
|
Cancer
|
|
Ir-CA is an antitumor agent. Ir-CA can accumulate in mitochondria and induces mitochondria dysfunction. Ir-CA induces apoptosis and autophagy. Ir-CA initiates mitophagy and cell cycle arrest to kill Cisplatin (HY-17394)-resistant A549R cells. Ir-CA can effectively inhibit metastasis by inhibiting MMP-2/MMP-9 .
|
-
- HY-170640
-
|
|
FLT3
Reactive Oxygen Species
Apoptosis
|
Cancer
|
|
FLT3-IN-29 (Compound MY-10) is a FLT3 inhibitor (IC50s: 6.5 and 10.3 nM for FLT3-ITD and FLT3-D835Y mutants). FLT3-IN-29 arrests cell cycle at the G0/G1 phase and efficiently induces Apoptosis. FLT3-IN-29 also reduces reactive oxygen species (ROS) production and mitochondrial membrane potential (MMP). FLT3-IN-29 displays antileukemic activity .
|
-
- HY-162482
-
|
|
EGFR
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
EGFR kinase inhibitor 5 (Compound 4c) is an orally active inhibitor for epidermal growth factor receptor (EGFR) kinase, with IC50 of 18.35 μM. EGFR kinase inhibitor 5 induces apoptosis. EGFR kinase inhibitor 5 exhibits anticancer and anti-inflammatory activity with low toxicity (LD50 range: 500-2000 mg/kg) .
|
-
- HY-144650
-
|
|
Apoptosis
HSP
|
Cancer
|
|
Hsp90-Cdc37-IN-3 (Compound 9) is a novel celastrol−imidazole derivative with anticancer activity. Hsp90-Cdc37-IN-3 inhibits Hsp90−Cdc37 by covalent-binding, and induces apoptosis .
|
-
- HY-B1041A
-
|
Pimagedine; GER-11(free base) ; Aminoguanidinium
|
NO Synthase
Apoptosis
|
Endocrinology
|
|
Aminoguanidine (Pimagedine hydrochloride) is an inhibitor of diamine oxidase and nitric oxide synthase. Aminoguanidine has a dose-dependent inhibitory effect on apoptosis induced by Doxorubicin (HY-15142). Aminoguanidine has antioxidant properties. Aminoguanidine can be used in diabetic nephropathy research .
|
-
- HY-149846
-
|
|
EGFR
|
Cancer
|
|
SIQ17 is an EGFR inhibitor that inhibits its activity by occupying the ATP-binding site, with IC50 of 0.62 nM. SIQ17 shows more effective EGFR-TK inhibitory activity compared to the known inhibitor Erlotinib (HY-50896) (IC50 of ∼20 nM). SIQ17 can be used for cancer research
|
-
- HY-163199
-
|
|
ASCT
mTOR
Apoptosis
Autophagy
|
Cancer
|
|
ASCT2-IN-2 (compound 25e) is an ASCT2 inhibitor with IC50 of 5.14 μM. ASCT2-IN-2 regulates amino acid metabolism as well as mTOR signaling and thereby induces cell apoptosis. ASCT2-IN-2 inhibits tumor growth .
|
-
- HY-163371
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
EGFR WT/T790M-IN-1 (Compound 16h) is a dual EGFR WT and EGFR T790 inhibitor. EGFR WT/T790M-IN-1 can arrest the cell cycle in G2/M phase and induce apoptosis. EGFR WT/T790M-IN-1 has anti-cancer activity .
|
-
- HY-162483
-
|
|
EGFR
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
EGFR kinase inhibitor 6 (Compound 4b) is an orally active inhibitor for epidermal growth factor receptor (EGFR) kinase, with IC50 of 24.34 μM. EGFR kinase inhibitor 6 induces apoptosis. EGFR kinase inhibitor 6 exhibits anticancer and anti-inflammatory activity with low toxicity (LD50 range: 500-2000 mg/kg) .
|
-
- HY-P10850
-
|
|
TNF Receptor
NF-κB
Apoptosis
|
Inflammation/Immunology
|
|
PIYLGGVFQ is a peptide inhibitor for TNF-α. PIYLGGVFQ inhibits TNF-α-mediated apoptosis, NF-κB nuclear translocation and activation. PIYLGGVFQ exhibits anti-arthritic activity in the CIA mouse model .
|
-
- HY-146223
-
|
|
Ras
|
Cancer
|
|
AZD4625 (Compound 21) is a highly potent, selective, covalent and allosteric inhibitor of the mutant GTPase KRAS G12C. AZD4625 has high oral bioavailability .
|
-
- HY-146409
-
|
|
Apoptosis
|
Cancer
|
|
Antitumor agent-59 (Compound 13b) is a potent antitumor agent. Antitumor agent-59 effectively inhibits the proliferation and migration of HCT116 cells. Antitumor agent-59 induces HCT116 cell apoptosis and arrests the cell cycle at the G2/M phase .
|
-
- HY-161656
-
|
|
PROTAC Linkers
|
Cancer
|
|
PIP-C-3-Azaspiro[5.5]undecane-boc is the linker for PROTAC. PIP-C-3-Azaspiro[5.5]undecane-boc is utilized for synthesis of PROTAC SOS1 degrader-10 (HY-161654) .
|
-
![PIP-C-3-Azaspiro[5.5]undecane-boc](//file.medchemexpress.eu/product_pic/hy-161656.gif)
- HY-163724
-
|
|
TrxR
Apoptosis
|
Cancer
|
|
LW-216 is a TrxR1 inhibitor that induces Apoptosis. LW-216 has anti-tumor activity .
|
-
- HY-N0883
-
|
Gamabufagin
|
VEGFR
|
Cancer
|
|
Gamabufotalin (Gamabufagin), a main active compound isolated from Chinese medicine Chansu, has been shown to strongly inhibit cancer cell growth and inflammatory response. Gamabufotalin could inhibite angiogenesis by inhibiting the activation of VEGFR-2 signaling pathways.
|
-
- HY-172395
-
|
|
Microtubule/Tubulin
Topoisomerase
Apoptosis
Reactive Oxygen Species
|
Cancer
|
|
TopoII/tubulin-IN-1 (Compound 1B8) is a TopoII/tubulin inhibitor. TopoII/tubulin-IN-1 can inhibit the proliferation and the level of ROS of tumor cells, induce apoptosis and cell cycle arrest of tumor cells, but has no significant cytotoxicity to normal cells. TopoII/tubulin-IN-1 has antitumor activity .
|
-
- HY-147795
-
|
|
NAMPT
Apoptosis
Reactive Oxygen Species
|
Cancer
|
|
Nampt-IN-8 (Compound 10d) is an NAMPT inhibitor with an IC50 of 0.183 μM. Nampt-IN-8 is also a relatively good NQO1 substrate. Nampt-IN-8 induces cell apoptosis and ROS .
|
-
- HY-159454
-
|
|
PROTACs
|
Cancer
|
|
SMARCA2/4-degrader-3 (compound I-433) is a PROTAC SMARCA2/4-degrader based on VH032-NH2, with a degradation potency (DC50) <100 nM in MV4-11 cells .
|
-
- HY-133219
-
|
|
Topoisomerase
|
Cancer
|
|
Guajadial C is a Top1 catalytic inhibitor that delays Top1 poison-mediated DNA damage. Guajadial C shows cytotoxicity against cancer cells .
|
-
- HY-161655
-
-
- HY-158073
-
|
|
SARS-CoV
|
Infection
|
|
ML2006a4 is an orally active inhibitor for SARS-CoV-2 main protease (M pro) with IC50 in picomolare value. ML2006a4 is cell permeable and antiviral active, that inhibits replication in SARS-CoV-2 in cells Huh7.5.1-ACE2-TMPRSS2 (Huh7.5.1++) in picomolare level
|
-
- HY-N0211
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
Cyasterone, a natural EGFR inhibitor, mainly isolated from Ajuga decumbens Thunb (Labiatae). Cyasterone manifests anti-proliferation effect by induced apoptosis and cell cycle arrests. Cyasterone may serves as a therapeutic anti-tumor agent against human tumors .
|
-
- HY-146223A
-
|
|
Ras
|
Cancer
|
|
(3R,10R,14aS)-AZD4625 is the isomer of AZD4625 (HY-146223), and can be used as an experimental control. AZD4625 (Compound 21) is a highly potent, selective, covalent and allosteric inhibitor of the mutant GTPase KRAS G12C. AZD4625 has high oral bioavailability .
|
-
- HY-148839
-
|
|
c-Myc
|
Cancer
|
|
c-Myc inhibitor 9 (compound 332) is a c-Myc inhibitor with an logEC50 of ≥6. c-Myc inhibitor 9 inhibits tumor growth in nude mouse models. c-Myc inhibitor 9 can be used for cancer research .
|
-
- HY-138956
-
|
|
NF-κB
RSV
|
Infection
|
|
MAY0132 is a potent and selective EPAC2 inhibitor with an IC50 of 0.4 μM. MAY0132 significantly inhibits replication of HMPV, AdV and RSV, reduces viral infection-induced cytokine/chemokine production, and inhibits NF-κB activation. MAY0132 has antiviral activity and can be used in the study of respiratory virus infection .
|
-
- HY-N0211R
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
Cyasterone (Standard) is the analytical standard of Cyasterone. This product is intended for research and analytical applications. Cyasterone, a natural EGFR inhibitor, mainly isolated from Ajuga decumbens Thunb (Labiatae). Cyasterone manifests anti-proliferation effect by induced apoptosis and cell cycle arrests. Cyasterone may serves as a therapeutic anti-tumor agent against human tumors .
|
-
- HY-122944
-
|
|
Others
|
Cancer
|
|
20-Deoxocarnosol (compound 7) is a potent anti-cancer agent that can be found in the roots of Salvia deserta. 20-Deoxocarnosol shows cytotoxicity in cancer cells .
|
-
- HY-144053
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-36 is a potent EGFR inhibitor with IC50s of 19.09 nM, 120.01 nM, 2.35 nM for EGFR (WT), HER2 (WT), HER2 (A775_G776insYVMA), respectively. EGFR-IN-36 has potential for wild and/or mutant EGFR and/or HER2 kinase mediated tumors research .
|
-
- HY-157891
-
|
|
Apoptosis
|
Cancer
|
|
JBC117 is a novel anticancer lead compound targeting Pygo2 PHD. JBC117 can effectively antagonize the cell effect of β-catenin-dependent activity and inhibit the migration and invasion of cancer cells. JBC117 can induce apoptosis .
|
-
- HY-169509
-
|
|
PARP
Necroptosis
Topoisomerase
RIP kinase
Mixed Lineage Kinase
|
Cancer
|
|
Topoisomerase I/II Inhibitor 8 (Compound Ru7) is a dual catalytic inhibitor of Topoisomerase I/II, capable of inducing DNA damage and PARP-1 activation, which subsequently leads to the activation of RIPK1, RIPK3, and MLKL, ultimately triggering necroptosis. Topoisomerase I/II Inhibitor 8 demonstrates remarkable anticancer activity by effectively targeting the nuclei of cancer cells and inducing cell death through necroptosis, showing great clinical potential in circumventing drug resistance in cancer treatment .
|
-
- HY-172214
-
|
|
SARS-CoV
Virus Protease
|
Infection
|
|
AB-343 is a selective covalent inhibitor of SARS-CoV-2 M pro, with an IC50 of 8 nM and a Ki of 2.8 nM. AB-343 can effectively inhibit the main proteases of SARS-CoV-2 and many other coronaviruses, and is also active against some resistant variants. AB-343 can be used in the research of treating coronavirus infection-related diseases .
|
-
- HY-17037A
-
|
LS 519 free base; Pirenzepin; Gastrozepin
|
mAChR
|
Metabolic Disease
Cancer
|
|
Pirenzepine (LS 519 free base) is a selective M1 mAChR (muscarinic acetylcholine receptor) antagonist. Pirenzepine reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine shows anti-proliferative activity to cancer cells .
|
-
- HY-17037S1
-
|
LS 519-d8 dihydrochloride; Pirenzepin-d8 dihydrochloride; Gastrozepin-d8 dihydrochloride
|
Isotope-Labeled Compounds
mAChR
|
Cancer
|
|
Pirenzepine-d8 (LS 519-d8; Pirenzepin-d8) dihydrochloride is a deuterium labeled Pirenzepine (dihydrochloride) (HY-17037). Pirenzepine (LS 519) dihydrochloride is a selective M1 mAChR (muscarinic acetylcholine receptor) antagonist. Pirenzepine dihydrochloride reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine dihydrochloride shows anti-proliferative activity to cancer cells .
|
-
- HY-13283
-
MF63
1 Publications Verification
|
PGE synthase
|
Inflammation/Immunology
|
|
MF63 is a selective and orally active inhibitor of mPGES-1. MF63 reduces the accumulation of PGE2, relieves pyresis, hyperalgesia, and inflammatory pain by inhibiting mPGES-1 .
|
-
- HY-172096
-
|
|
Bcr-Abl
Src
|
Cancer
|
|
cSRC/BCR-ABL-IN-1 (compound 21b) is a potent Bcr-Abl and C-Src inhibitor with IC50 values of 56.2, 101 nM for Bcr-Abl, C-Src, respectively. cSRC/BCR-ABL-IN-1 shows cytotoxicity activity .
|
-
- HY-163524
-
|
|
Apoptosis
|
Cancer
|
|
NAE-IN-2 (compound III-26) is N2–(1-benzylpiperidin-4-yl)quinazoline-2,4-diamine derivative, and inhibits Cullin1 and Cullin3. NAE-IN-2 inhibits migration and induces cell apoptosis of gastric cancer cells .
|
-
- HY-101996
-
|
|
Bcl-2 Family
|
Cancer
|
|
SMBA1 is a potent Bax agonist with a Ki value of 43.3 nM. SMBA1 enhances the Bax expression. SMBA1 shows anti-tumor activity. SMBA1 has the potential for the research of lung cancer .
|
-
- HY-147971
-
|
|
Parasite
Topoisomerase
|
Infection
Cancer
|
|
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 .
|
-
- HY-N4058R
-
|
|
Apoptosis
|
Cancer
|
|
Helichrysetin (Standard) is the analytical standard of Helichrysetin. This product is intended for research and analytical applications. Helichrysetin is isolated from the flower Helichrysum odoratissimum. Helichrysetin is an ID2 (DNA binding inhibitor 2) inhibitor. Helichrysetin induces apoptosis. Helichrysetin has anti-tumor and antioxidant activity .
|
-
- HY-119283
-
-
- HY-150218
-
|
ODN 2006 sodium; ODN 7909 sodium; PF-3512676 sodium; CpG 7909 sodium
|
Toll-like Receptor (TLR)
|
Cancer
|
|
Agatolimod sodium (ODN 2006) is a class B CpG ODN and is a TLR9 agonist. Agatolimod sodium can be used as vaccine adjuvant. Agatolimod sodium can be used for the research of cancer. Sequence: 5’-TCGTCGTTTTGTCGTTTTGTCGTT-3’ .
|
-
- HY-N1820
-
-
- HY-164895
-
|
|
PIN1
|
Cancer
|
|
PIN1 degrader-1 (Compound 158H9) is the inhibitor for proline cis trans isomerase (Pin1) with an IC50 of 21.5 nM. PIN1 degrader-1 forms covalent bond with Cys113 of Pin1, induces conformational changes in Pin1, reduces its stability, and leads to a proteasome-dependently degradation. PIN1 degrader-1 inhibits the cell viability of multi cancer cells, and can be used in cancer research .
|
-
- HY-146114
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Antitumor agent-67 (compound 3) is a potent antitumor agent. Antitumor agent-67 has highly selective toxicity to cancer cells and lower damage to normal cells. Antitumor agent-67 can be activated by NQO1 and effectively liberate podophyllotoxin and kill tumor cells. Antitumor agent-67 significantly suppresses cancer growth in HepG2 xenograft models without obvious toxicity .
|
-
- HY-17037
-
|
LS 519; Pirenzepin dihydrochloride; Gastrozepin dihydrochloride
|
mAChR
|
Metabolic Disease
Cancer
|
|
Pirenzepine (LS 519) dihydrochloride is a selective M1 mAChR (muscarinic acetylcholine receptor) antagonist. Pirenzepine dihydrochloride reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine dihydrochloride shows anti-proliferative activity to cancer cells .
|
-
- HY-146463
-
|
|
DNA/RNA Synthesis
Bacterial
|
Infection
|
|
NusB-IN-1 (Compound 22r) is a potent, orally active bacterial rRNA synthesis inhibitor. NusB-IN-1 shows antimicrobial activity against MRSA and VRSA . NusB-IN-1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-161750
-
|
|
PROTACs
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
|
PROTAC ALK degrader-2 (B1-PEG) is an ALK degrader based on PROTACs, with the DC50 of 45 nM in H3122 EML4-ALK DC50 (GSH+). PROTAC ALK degrader-2, through PEGylation, is engineered to self-organize into micelles in water and releases its active form in response to the tumor-specific high GSH environment .
|
-
- HY-146367
-
|
|
VEGFR
Apoptosis
Reactive Oxygen Species
|
Cancer
|
|
VEGFR-2-IN-19 (Compound 15b) is a potent VEGFR2 inhibitor. VEGFR-2-IN-19 induces cell apoptosis and increases intracellular reactive oxygen species level. VEGFR-2-IN-19 can be used as an anticancer agent .
|
-
- HY-147698
-
|
|
CDK
Topoisomerase
Apoptosis
|
Cancer
|
|
ZLHQ-5f is a dual CDK2 and Topo I inhibitor with an IC50 of 0.145 μM against CDK2/CycA2. ZLHQ-5f arrests the cell cycle in S-phase, triggers apoptosis in HCT116 cells, and has a good safety profile .
|
-
- HY-172088
-
|
|
Microtubule/Tubulin
MMP
NF-κB
Apoptosis
|
Cancer
|
|
Tubulin/MMP-IN-3 (Compound 15j) is the dual inhibitor for tubulin polymerization and MMP, and inhibits MMP-2 and MMP-9 with IC50 of 21.13 μM and 19.24 μM. Tubulin/MMP-IN-3 inhibits NF-κB signaling pathway, causes mitochondrial dysfunction and the apoptosis through a mitochondrial-dependent pathway. Tubulin/MMP-IN-3 exhibits antiproliferative activity in a variety of cancer cells, arrests the cell cycle at G2/M phase, and exhibits antitumor efficacy in mouse models .
|
-
- HY-W451275
-
|
|
Apoptosis
|
Cancer
|
|
HG106 is an effective SLC7A11 inhibitor. HG106 mediates apoptosis by increasing oxidative stress and endoplasmic reticulum stress, and it has antitumor activity .
|
-
- HY-P10218A
-
|
|
MARCKS
PKC
|
Inflammation/Immunology
Cancer
|
|
MANS peptide TFA is the TFA salt form of MANS peptide (HY-P10218). MANS peptide TFA is an inhibitor for myristoylated alanine-rich C kinase substrate (MARCKS), which competes with MARCKS in cells for membrane binding, and thus inhibits the stimulation of mucin secretion and tumor metastasis .
|
-
- HY-132296
-
|
|
FAK
PROTACs
|
Cancer
|
|
GSK215 is a potent and selective PROTAC focal adhesion kinase (FAK) degrader with a pDC50 of 8.4. GSK215 is designed by a binder for the VHL E3 ligase and the FAK inhibitor VS-4718. GSK215 induces rapid and prolonged FAK degradation, giving a long-lasting effect on FAK levels and a marked pharmacokinetic/pharmacodynamics (PK/PD) disconnect .
|
-
- HY-149000
-
|
|
PI3K
Apoptosis
|
Cancer
|
|
PI3Kα-IN-7 (Compound A12) is a potent PI3Kα inhibitor. PI3Kα-IN-7 also inhibits PI3Kβ. PI3Kα-IN-7 decreases cancer cells mitochondrial membrane potential and induces apoptosis .
|
-
- HY-P10218
-
|
|
MARCKS
PKC
|
Inflammation/Immunology
Cancer
|
|
MANS peptide is an inhibitor for myristoylated alanine-rich C kinase substrate (MARCKS), which competes with MARCKS in cells for membrane binding, and thus inhibits the stimulation of mucin secretion and tumor metastasis .
|
-
- HY-161749
-
|
|
PROTACs
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
|
PROTAC ALK degrader-1 (compound B1) is an ALK degrader based on PROTACs, with the DC50 of 26 nM in H3122 EML4-ALK. PROTAC ALK degrader-1 can be used to synthesis PROTAC ALK degrader-2 (HY-161750) with superior bioavailability .
|
-
- HY-143463
-
|
|
c-Met/HGFR
|
Cancer
|
|
AC-386 is a highly potent c-Met inhibitor with IC50 value of 7.42 nM. AC-386 has antiproliferative activities against certain cancer cell lines. AC-386 can be used for researching anti-cancer resistance .
|
-
- HY-161360
-
|
|
SHP2
Apoptosis
|
Cancer
|
|
LXQ-217 is an oral active SHP2 inhibitor with the IC50 of 2.01 μM. LXQ-217 induces apoptosis and inhibits cell growth in vivo and in vitro .
|
-
- HY-N7158
-
|
|
Others
|
Cancer
|
|
Elasticamide is a natural compound isolated from Ficus elastica Roxb. Elasticamide inhibits the cell growth in the U373n, with the IC50 of 88 μM .
|
-
- HY-146136
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
EGFR-IN-56 (Compound 13a) is a potent EGFR inhibitor with IC50 values of 541.7 nM and 132.1 nM against EGFR T790M and EGFR T790M/L858R, respectively. EGFR-IN-56 blocks cancer cells in G2/M phase and induce into late apoptosis .
|
-
- HY-142160
-
|
|
Raf
|
Cancer
|
|
GNE-9815 (compound 7) is a highly selective, pan-RAF inhibitor with good oral bioavailability. GNE-9815 exhibits Ki values of 0.062 and 0.19 nM for CRAF and BRAF, respectively. GNE-9815 combines with MEK inhibitor Cobimetinib (HY-13064) shows synergistic modulation of MAPK pathway. GNE-9815 can be used in studies of KRAS mutant cancers .
|
-
- HY-149033
-
|
|
Others
|
Cancer
|
|
Kobusine derivative-2, a kobusine derivative, has antiproliferative activity against cancer cells. Kobusine derivative-2 can induce the arrest of MDA-MB-231 cells in the sub-G1 phase. Anticancer activity .
|
-
- HY-16942
-
|
|
Apoptosis
|
Cancer
|
|
Damulin B is a dammarane-type saponin found in Gynostemma pentaphyllum.Damulin B can induce cell apoptosis and has anti-cancer activities in vitro .
|
-
- HY-146048
-
|
|
Apoptosis
Reactive Oxygen Species
|
Cancer
|
|
Antitumor agent-57 (Compound 3o) is an NQO1-directed antitumor agent. Antitumor agent-57 inhibits tumor cell growth, triggers ROS generation and induces cell apoptosis .
|
-
- HY-163542
-
|
|
Bacterial
|
Inflammation/Immunology
|
Pneumolysin-IN-1 (compound PB-3) is a targeted small molecule inhibitor of Pneumolysin (PLY) (IC50=3.1 µM). Pneumolysin-IN-1 is a pore blocking agent and an anti-virulence factor. Pneumolysin-IN-1 can be used to study the infection caused by Streptococcus pneumoniae .
|
-
- HY-156278
-
|
|
Apoptosis
Autophagy
|
Cancer
|
|
FB49 is a highly selective inhibitor of Bcl-2-associated athanogene 3 (BAG3), with the Ki of 45 μM. FB49 inhibits the cell growth in human tumoral cells, but has no toxicity in human peripheral mononuclear cells. FB49 block cell cycle in G1 phase and to induce apoptosis as well as autophagy in medulloblastoma HD-MB03 treated cells .
|
-
- HY-124722
-
|
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
OHM1 is an analog of HIF1α CTAD that inhibits its binding with p300/CBP. OHM1 targets CH1 domain with an affinity of 0.53 μM .
|
-
- HY-P10386
-
|
|
Bcl-2 Family
|
Cancer
|
|
155H1 (Compound 11) is a stapled peptide, that covalently binds hMcl1 (172-323) with IC50 of 18 nM .
|
-
- HY-N4058
-
|
|
Apoptosis
|
Cancer
|
|
Helichrysetin is isolated from the flower Helichrysum odoratissimum. Helichrysetin is an ID2 (DNA binding inhibitor 2) inhibitor. Helichrysetin induces apoptosis. Helichrysetin has anti-tumor and antioxidant activity .
|
-
- HY-N6998
-
|
|
Apoptosis
|
Cancer
|
|
Paederosidic acid is isolated from P.?scandens with anticancer and anti‐inflammation activities. Paederosidic acid inhibits lung caner cells via inducing mitochondria-mediated apoptosis .
|
-
- HY-169350
-
|
|
Glutathione S-transferase
|
Cancer
|
|
EA-B2L is a potent degrader of glutathione S-transferase (GSTP), with the DC50 of 48 μM. EA-B2L is a kind of Boc2Lys-linked Ethacrynic acid (HY-B1640). EA-B2L plays an important role in cancer research .
|
-
- HY-143462
-
|
|
HDAC
c-Met/HGFR
Apoptosis
|
Cancer
|
|
c-Met/HDAC-IN-2 is a highly potent c-Met and HDAC dual inhibitor with IC50s of 18.49 nM and 5.40 nM for HDAC1 and c-Met, respectively. c-Met/HDAC-IN-2 has antiproliferative activities against certain cancer cell lines. c-Met/HDAC-IN-2 can cause G2/M-phase arrest and induce apoptosis in HCT-116. c-Met/HDAC-IN-2 can be used for researching anti-cancer resistance .
|
-
- HY-152076
-
|
|
Apoptosis
|
Cancer
|
|
Telomerase-IN-4 is a potent telomerase inhibitor. Telomerase-IN-4 has antiproliferative activity and induces apoptosis .
|
-
- HY-170429
-
|
|
PIN1
|
Cancer
|
|
BJP-07-017-3 is the inhibitor for proline cis trans isomerase (Pin1) with an IC50 of 9 nM. BJP-07-017-3 forms covalent bond with Cys113 of Pin1, induces conformational changes in Pin1, reduces its stability, and leads to a proteasome-dependently degradation .
|
-
- HY-75564R
-
-
- HY-34595
-
|
|
RET
|
Cancer
|
|
Pyrazoloadenine is a potent RET (REarranged during Transfection) lung cancer oncoprotein inhibitor. Pyrazoloadenine shows anticancer activity .
|
-
- HY-170967
-
|
|
Apoptosis
Caspase
PARP
Reactive Oxygen Species
|
Cancer
|
|
IPH10 is an anti-cancer agent that exhibits a strong anti-tumor effect in vivo without hepatic and renal toxicity. IPH10 can significantly increase the content of ROS, decrease the mitochondrial membrane potential, and induce apoptosis in tumor cells .
|
-
- HY-161697
-
|
|
Carbonic Anhydrase
|
Cancer
|
|
hCAIX-IN-20 (compound APBS-5m) is a potent inhibitor of carbonic anhydrase IX (hCA IX), with the Ki of 2.7 nM. hCAIX-IN-20 plays an important role in cancer research .
|
-
- HY-149222
-
|
|
Apoptosis
|
Cancer
|
|
Apoptosis inducer 12 (Compound 3z) is an apoptosis inducer that induces apoptosis through the mitochondrial pathway. Apoptosis inducer 12 can be used for the research of cancer .
|
-
- HY-17037R
-
|
|
mAChR
|
Metabolic Disease
Cancer
|
|
Pirenzepine (dihydrochloride) (Standard) is the analytical standard of Pirenzepine (dihydrochloride). This product is intended for research and analytical applications. Pirenzepine (LS 519) dihydrochloride is a selective M1 mAChR (muscarinic acetylcholine receptor) antagonist. Pirenzepine dihydrochloride reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine dihydrochloride shows anti-proliferative activity to cancer cells .
|
-
- HY-B0914
-
|
Undecylenic acid
|
Fungal
Amyloid-β
Reactive Oxygen Species
Proteasome
Bacterial
|
Infection
Neurological Disease
Endocrinology
Cancer
|
|
10-Undecenoic acid (Undecylenic acid) is an antifungal agent. 10-Undecenoic acid inhibits Aβ oligomerization, scavenges ROS and inhibits μ-calpain activity. 10-Undecenoic acid has neuroprotective effects. 10-Undecenoic acid has anticancer effects on a variety of tumors. 10-Undecenoic acid inhibits C. albicans biofilm formation and MRSA infection. 10-Undecenoic acid inhibits quorum sensing signals of Bacillus subtilis and Pseudomonas aeruginosa .
|
-
- HY-W042191
-
|
|
Fungal
Apoptosis
Caspase
Bcl-2 Family
MDM-2/p53
PARP
|
Infection
Cancer
|
|
Oxychloroaphine could be isolated from the bacterium Pantoea agglomerans naturally present in soil. Oxychloroaphine has broad-spectrum antifungal activity. Oxychloroaphine has cytotoxicity in a dose-dependent manner and induces apoptosis. Oxychloroaphine can be used in research of cancer .
|
-
- HY-146693
-
|
|
TGF-β Receptor
|
Cancer
|
|
CJJ300 is a transforming growth factor-β (TGF-β) inhibitor with an IC50 of 5.3 µM. CJJ300 inhibits TGF-β signaling by disrupting the formation of the TGF-β-TβR-I-TβR-II signaling complex .
|
-
- HY-118988
-
|
|
PPAR
Apoptosis
|
Cancer
|
|
CAY10506 is a PPARγ ligand that can induce cell death and ROS production in a PPARγ-dependent manner in vitro. CAY10506 exhibits radiosensitizing effects, enhancing γ-radiations-induced apoptosis and caspase-3-mediated poly (ADP-ribose) polymerase (PARP) cleavage. CAY10506 can be used in cancer research .
|
-
- HY-144259
-
|
|
Beta-lactamase
Bacterial
|
Infection
|
|
Metallo-β-lactamase-IN-4 (compound 40) is a potent metallo-β-lactamases (MBL) inhibitor, with IC50 values of 0.1 μM (VIM-1), 1.3 μM (NDM-1), and 5.0 μM (IMP-7), respectively .
|
-
- HY-18572A
-
|
Sodium 2,4-dichlorophenoxyacetate; 2,4-Dichlorophenoxyacetic acid sodium salt
|
DNA/RNA Synthesis
Apoptosis
|
Others
|
|
2,4-D sodium salt (Sodium 2,4-dichlorophenoxyacetate) is a selective herbicide that can be orally active for the control of broad-leaved weeds. 2,4-D sodium salt can induce < b>apoptosis. 2,4-D sodium salt inhibits DNA and protein synthesis, thereby preventing normal plant growth and development .
|
-
- HY-151623
-
ACBI2
1 Publications Verification
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
ACBI2 is a highly potent and orally active VHL PROTAC SMARCA2 degrader (EC50: 7 nM), which selectively degrades SMARCA2 with a DC50 value of 1 nM in RKO cells. ACBI2 can be used in the research of lung cancer .
|
-
- HY-101961
-
|
AG 1288
|
c-Kit
|
Inflammation/Immunology
|
|
Tyrphostin AG 1288 is a potent Tyrosine Kinase inhibitor. Tyrphostin AG 1288 inhibits ICAM1 expression and TNFα-mediated cytotoxicity in vitro .
|
-
- HY-143250
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 12 (Hit 9) is a novel tubulin inhibitor (IC50=25.3 μM). Tubulin inhibitor 12 shows anti-tumor activity and anti-proliferative activity .
|
-
- HY-108633
-
|
|
PARP
|
Cancer
|
|
AR-C66096 (FPL 66096) tetrasodium is a selective platelet P2YT receptor antagonist. AR-C66096 tetrasodium effectively blocks ADP-induced platelet aggregation. AR-C66096 tetrasodium can be used in the research of thromboembolism .
|
-
- HY-P10930A
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
wrwycr-NH2 (TFA) is a peptide. wrwycr-NH2 (TFA) is cytotoxic to multiple cancer cells, can induce DNA damage and cell cycle arrest, but does not induce endoplasmic reticulum stress. wrwycr-NH2 (TFA) has anti-tumor activity, and it shows better efficacy when used in combination with DNA-damaging agents .
|
-
- HY-W042191R
-
-
- HY-144261
-
|
|
Beta-lactamase
Bacterial
|
Infection
|
|
Metallo-β-lactamase-IN-3 (compound 35) is a potent metallo-β-lactamases (MBL) inhibitor. Metallo-β-lactamase-IN-3 shows high activity against VIM-1 and NDM-1, with IC50 of 0.6 and 1.0 μM, respectively. Metallo-β-lactamase-IN-3 does not show inhibition of IMP-7 .
|
-
- HY-N10472
-
|
|
STAT
|
Cancer
|
|
STAT3-IN-14 (Compound 1) is a STAT3 inhibitor and has STAT3 phosphorylation inhibitory activity. STAT3-IN-14 (Compound 1) can directly bind to the hinge region of STAT3 .
|
-
- HY-169278
-
|
|
Epigenetic Reader Domain
PROTACs
|
Cancer
|
|
PROTAC SMARCA2 degrader-26 (compound 45) is a potent SMARCA2 PROTAC degrader. PROTAC SMARCA2 degrader-26 induces SMARCA2 and SMARCA4 degradation in VCaP cells with the percent degradation of 94% and 57% for SMARCA2 and SMARCA4, respectively. PROTAC SMARCA2 degrader-26 shows antiproliferative activity .
|
-
- HY-18572
-
|
2,4-Dichlorophenoxyacetic acid
|
DNA/RNA Synthesis
Apoptosis
|
Others
|
|
2,4-D (2, 4-dichlorophenoxyacetic acid) is a selective herbicide that can be orally active for the control of broad-leaved weeds. 2,4-D can induce apoptosis. 2,4-D inhibits DNA and protein synthesis, thereby preventing normal plant growth and development .
|
-
- HY-161358
-
|
|
FAK
Apoptosis
|
Cancer
|
|
FAK-IN-20 (Compound 7b) is an inhibitor of FAK with an IC50 value of 0.27 nM. FAK-IN-20 exhibits anticancer activity. FAK-IN-20 can arrest the cell cycle in the G2/M phase and induce cell apoptosis by generating ROS .
|
-
- HY-121323R
-
|
|
Apoptosis
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Acarbose (Standard) is the analytical standard of Acarbose. This product is intended for research and analytical applications. Acarbose (BAY g 5421), antihyperglycemic agent, is an orally active alpha-glucosidase inhibitor (IC50=11 nM). Acarbose can potentiate the hypoglycemic effects of sulfonylureas or insulin .
|
-
- HY-152237
-
|
|
IKK
|
Cancer
|
|
TBK1-IN-1 is a potent and selective TANK binding kinase 1 (TBK1) inhibitor with an IC50 value of 22.4 nM. TBK1-IN-1 inhibits TBK1 downstream target genes cxcl10 and ifnβ expression. TBK1-IN-1 has anticancer activity .
|
-
- HY-145119AS
-
|
VV116; GS-621763-d1 hydrobromide
|
SARS-CoV
RSV
Influenza Virus
|
Infection
|
|
Mindeudesivir (JT001; VV116; GS-621763-d1) hydrobromide is a deuterated version of Remdesivir (HY-104077), a highly orally active nucleoside antiviral against SARS-CoV-2 and respiratory syncytial virus (RSV). Mindeudesivir hydrobromide retains the antiviral activity of Remdesivir against COVID-19, and is the first domestically produced deuterium targeting the COVID-19 .
|
-
- HY-149900
-
|
|
Biochemical Assay Reagents
|
Infection
|
|
Antiviral agent 33 (compound 1c) is a double-stranded DNA (dsDNA) virus inhibitor with IC50 values of 0.0790 and 0.1572 µM for VACV and AdV5, respectively. Antiviral agent 33 also has potential for oral administration .
|
-
- HY-151563
-
|
|
Deubiquitinase
|
Cancer
|
|
OTUB1/USP8-IN-1 is a potent dual OTUB1/USP8 inhibitor with IC50 values of 0.17 and 0.28 nM for OTUB1 and USP8, respectively. OTUB1/USP8-IN-1 can be used in research of cancer .
|
-
- HY-148900
-
|
|
E1/E2/E3 Enzyme
|
Cancer
|
|
SCFSkp2-IN-2 (Compound AAA-237) is a Skp2 inhibitor with a KD of 28.77 μM. AAA-237 induces apoptosis of NSCLC cells and shows antitumor activities .
|
-
- HY-163134
-
|
|
DNA-PK
|
Cancer
|
|
DNA-PK-IN-12 (compound 31t) is an oral active DNA-PK inhibitor with the IC50 of 0.1 nM. DNA-PK-IN-12 inhibits cell growth and Hct116 cell colony formation with the IC50 of 33.28 μM, and shows antitumor activity in vivo .
|
-
- HY-162481
-
|
|
Apoptosis
|
Cancer
|
|
Anticancer agent 210 (Compound 7a) is a Gefitinib (HY-50895) derivative. Anticancer agent 210 inhibits proliferation, migration and colony formation of cancer cells. Anticancer agent 210 induces apoptosis in cells H1299 .
|
-
- HY-170793
-
|
|
PD-1/PD-L1
VISTA
|
Cancer
|
|
PD-L1/VISTA-IN-1 (Compound P17) is an orally active dual-target inhibitor of PD-L1 and VISTA. PD-L1/VISTA-IN-1 can block the PD-1/PD-L1 interaction (IC50: 0.1492 μM) and the VISTA pathway (KD: 0.2723 μM), thereby reactivating T cells. PD-L1/VISTA-IN-1 has anti-tumor activity .
|
-
- HY-144262
-
|
|
Beta-lactamase
Bacterial
|
Infection
|
|
Metallo-β-lactamase-IN-4 (compound 40) is a potent metallo-β-lactamases (MBL) inhibitor, with IC50 values of 0.5 μM (VIM-1), 2.1 μM (NDM-1), and 3.3 μM (IMP-7), respectively .
|
-
- HY-152173
-
|
|
HDAC
Apoptosis
Bcl-2 Family
CDK
|
Cancer
|
|
HDAC-IN-51 is a potent histone deacetylase (HDAC) inhibitor with IC50 values of 0.32, 0.353, 0.431, 0.515, and 85.4 μM for HDAC10, HDAC1, HDAC2, HDAC3 and HDAC11, respectively. HDAC-IN-51 induces cell cycle arrest and apoptosis, modulating cell cycle-/apoptosis-related miRNAs expression. HDAC-IN-51 can be used in research of cancer .
|
-
- HY-18572AR
-
-
- HY-104068
-
|
|
Histone Acetyltransferase
Epigenetic Reader Domain
|
Cancer
|
|
Naphthol AS-E is a potent and cell-permeable inhibitor of KIX-KID interaction. Naphthol AS-E directly binds to the KIX domain of CBP (Kd:8.6 μM), blocks the interaction between the KIX domain and the KID domain of CREB with IC50 of 2.26 μM. Naphthol AS-E can be used for cancer research.
|
-
- HY-158006
-
|
|
MetAP
|
Cancer
|
|
SDX-7539 is a selective inhibitor for Methionine aminopeptidase type 2 (MetAP2). SDX-7539 inhibits proliferarion of HUVECs with an IC50 of 120 μM. SDX-7539 exhibits antitumor activity in NSCLC xenograft athymic nude mice .
|
-
- HY-172201
-
|
|
NF-κB
Reactive Oxygen Species
Autophagy
Apoptosis
HIF/HIF Prolyl-Hydroxylase
Akt
STAT
PI3K
|
Inflammation/Immunology
Cancer
|
|
NF-κB-IN-19 (Compound 8) is an NF-κB inhibitor. NF-κB-IN-19 effectively induces DNA damage, promotes the generation of ROS, and induces autophagy and apoptosis through the NF-κB signaling pathway in tumor cells. In addition, NF-κB-IN-19 can inhibit the levels of VEGF and HIF-1α, and exert antiproliferative activity in tumor cells through the PI3K/AKT and STAT-3 pathways. NF-κB-IN-19 can effectively overcome cisplatin resistance and has anti-tumor activity .
|
-
- HY-121323
-
-
- HY-151504
-
|
ALM301
|
Akt
|
Cancer
|
|
Engasertib is an orally active highly specific AKT inhibitor with IC50 values of 0.13 µM, 0.09 µM and 2.75 µM for AKT1, AKT2 and AKT3, respectively. Engasertib inhibits AKT phosphorylation and modulates downstream signalling in vitro. Engasertib can inhibit cancer cell proliferation and tumor growth .
|
-
- HY-159518
-
|
|
Reactive Oxygen Species
Mitochondrial Metabolism
Apoptosis
|
Cancer
|
|
ROS inducer 4 (compound TE3) is a mitochondrial inhibitor. ROS inducer 4 causes a series of mitochondria-related physiological changes in tumors, such as mitochondrial fragmentation, explosive generation and accumulation of ROS, decreased mitochondrial membrane potential, decreased ATP content, and activation of ROS-mediated apoptotic signaling in mitochondria .
|
-
- HY-171047
-
|
|
Apoptosis
Autophagy
DNA/RNA Synthesis
Akt
mTOR
|
Cancer
|
|
Autophagy inducer 7 (Compound SSA) is an Autophagy and Apoptosis inducer. Autophagy inducer 7 activates autophagy by inhibiting Akt/mTOR signaling and the expression of downstream proteins. Autophagy inducer 7 suppresses DNA synthesis and causes a G0-G1 cell-cycle arrest. Autophagy inducer 7 inhibits tumor cell growth .
|
-
- HY-18572R
-
|
|
DNA/RNA Synthesis
Apoptosis
|
Others
|
|
2,4-D (Standard) is the analytical standard of 2,4-D. This product is intended for research and analytical applications. 2,4-D (2, 4-dichlorophenoxyacetic acid) is a selective herbicide that can be orally active for the control of broad-leaved weeds. 2,4-D can induce apoptosis. 2,4-D inhibits DNA and protein synthesis, thereby preventing normal plant growth and development .
|
-
- HY-A0032A
-
|
|
CMV
|
Infection
Inflammation/Immunology
Cancer
|
|
Valganciclovir hydrochloride is an orally active antiviral agent. Valganciclovir hydrochloride can inhibit the growth of adenoviruses and have a protective effect on immunosuppressed hamsters. Valganciclovir hydrochloride can be used for the research of Cytomegalovirus .
|
-
- HY-138962
-
|
K-Carrageenan Karra Type
|
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
κ-Carrageenan is a natural polymer which predominantly available in red seaweeds. κ-Carrageenan is an effective agent carrier to deliver curcumin in cancer cells and to induce apoptosis. κ-carrageenan serves as a potential inflammatory agent that magnifies existing intestinal inflammation .
|
-
- HY-B0914B
-
|
Undecylenic acid (copper)
|
Fungal
Bacterial
Amyloid-β
Reactive Oxygen Species
Proteasome
|
Infection
Neurological Disease
Endocrinology
Cancer
|
|
10-Undecenoic acid copper (Undecylenic acid copper) is an antifungal agent. 10-Undecenoic acid copper inhibits Aβ oligomerization, scavenges ROS and inhibits μ-calpain activity. 10-Undecenoic acid copper has neuroprotective effects. 10-Undecenoic acid copper has anticancer effects on a variety of tumors. 10-Undecenoic acid copper inhibits C. albicans biofilm formation and MRSA infection. 10-Undecenoic acid copper inhibits quorum sensing signals of Bacillus subtilis and Pseudomonas aeruginosa .
|
-
- 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-18329
-
|
|
MDM-2/p53
STAT
Apoptosis
|
Cancer
|
|
TDP-665759 is an inhibitor for HDm2:p53 complex, and thus activates p53, inhibits STAT3 signaling pathway (EC50 of 5.90 μM) and the cell viability of p53 expressing A549R (IC50 of 7.02 μM). TDP-665759 induces apoptosis in HepG2. TDP-665759 exhibits antitumor efficacy in mouse models .
|
-
- HY-147767
-
|
|
PI3K
Apoptosis
Reactive Oxygen Species
|
Cancer
|
|
PI3Kα-IN-6 (Compound 5b) is a PI3Kα inhibitor. PI3Kα-IN-6 exhibits anticancer potential and no toxicity in normal cells. PI3Kα-IN-6 increases generation of ROS, reduces mitochondrial membrane potential (MMP) and induces apoptosis .
|
-
- HY-N2359
-
|
|
Beta-lactamase
PKC
Bcl-2 Family
Apoptosis
Autophagy
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Chelerythrine is a natural alkaloid, acts as a potent and selective Ca 2+/phospholopid-dependent PKC antagonist, with an IC50 of 0.7 μM . Chelerythrine has antitumor, antidiabetic and anti-inflammatory activity . Chelerythrine inhibits the BclXL-Bak BH3 peptide binding with IC50 of 1.5 μM and displaces Bax from BclXL. Chelerythrine triggers apoptosis and autophagy .
|
-
- HY-148266
-
|
|
E1/E2/E3 Enzyme
|
Cancer
|
|
UBA5-IN-1 (compound 8.5) is a selective UBA5 inhibitor with an IC50 value of 4.0 μM. UBA5-IN-1 inhibits cell proliferation of Sk-Luci6 cancer cells with high expression levels of UBA5 .
|
-
- HY-169797
-
|
|
STAT
Survivin
Apoptosis
|
Cancer
|
|
STAT3-IN-38 (Compound 4m) is an inhibitor of STAT3 (KD of rhSTAT3: 45.33 µM). STAT3-IN-38 binds to the SH2 domain of STAT3 protein and suppresses the STAT3’s phosphorylation at site pTyr705 as well as its downstream genes (Survivin and Mcl-1). STAT3-IN-38 could block cell-cycle and induce Apoptosis in colorectal cancer cells .
|
-
- HY-W105318
-
|
PBP
|
TGF-beta/Smad
Apoptosis
|
Cancer
|
|
Pentabromophenol (PBP) is a brominated flame retardant (BFR) widely used in various consumer products to reduce the flammability of materials used in different utility items. Pentabromophenol can accelerate the degradation of transforming growth factor-β (TGF-β) receptors by promoting clathrin-mediated endocytosis, thereby inhibiting the TGF-β signaling pathway. Additionally, Pentabromophenol can also induce apoptosis in peripheral blood mononuclear cells (PBMCs) .
|
-
- HY-107430R
-
-
- HY-163767
-
|
|
β-catenin
|
Inflammation/Immunology
Cancer
|
|
Antitumor agent-171 (Compound 35) is an inhibitor for β-catenin/BCL9 interaction with IC50 of 1.61 μM. Antitumor agent-171 exhibits high affinity to β-catenin with Kd of 0.63 μM. Antitumor agent-171 inhibits the gene expression of axin2 with IC50 of 0.84 μM. Antitumor agent-171 inhibits cell viability of HCT116 with IC50 of 4.39 μM. Antitumor agent-171 activates T cells, promotes antigen presentation, and exhibits antitumor efficacy and good pharmacokinetic characteristics in mouse models .
|
-
- HY-151132
-
|
IsoQC-IN-1
|
CD47
|
Cancer
|
|
Glutaminyl cyclases-IN-1 (IsoQC-IN-1) is a potent glutaminyl cyclases (QC) inhibitor with IC50 values of 12 nM and 73 nM for human QC and isoQC, respectively. Glutaminyl cyclases-IN-1 can selectively interfere with the interaction of CD47/SIRPα through isoQC inhibition, and enhances the increased phagocytic activity of both THP-1 and U937 macrophages .
|
-
- HY-149085
-
|
|
RAR/RXR
|
Cancer
|
|
XS-060 is a potent anticancer agent and RXRα antagonist. XS-060 significantly induces RXRα-dependent mitotic arrest by inhibiting pRXRα-PLK1 interaction. XS-060 inhibits p-RXRα interaction with PLK1 but has no effect on RXRα heterodimerization with RARγ. XS-060 inhibits the in situ interaction between p-RXRα and PLK1 at the centrosome .
|
-
- HY-19365
-
AB-MECA
1 Publications Verification
|
Adenosine Receptor
|
Neurological Disease
|
|
AB-MECA is a high affinity A3 adenosine receptor agonist with a binding Ki of 430.5 nM for human A3 receptors in CHO cells. AB-MECA can enhance plasma histamine level .
|
-
- HY-154994
-
|
|
JAK
|
Inflammation/Immunology
|
|
JAK-IN-30 (compound 31) is a water-soluble JAK inhibitor with IC50 values of 2, 15, 18 and 2 nM for JAK2, JAK1, JAK3 and TYK2, respectively. JAK-IN-30 has research potential for dry eye disease (DED) .
|
-
- HY-141701
-
|
|
mTOR
HDAC
|
Cancer
|
|
mTOR/HDAC-IN-1 (Compound 50) is a selective mTOR and HDAC dual inhibitor with IC50 values of 0.49 and 0.91 nM against mTOR and HDAC1, respectively. mTOR/HDAC-IN-1 can be studied as an anti-cancer agent .
|
-
- HY-161366
-
|
|
PI3K
|
Cancer
|
|
OMS14 is exhibits inhibitory activity for phosphoinositide 3-kinase γ (PI3Kγ) and PIK3CD/PIK3R1, which inhibits 19% PI3Kγ and 65% PIK3CD/PIK3R1 activity at 100 μM. OMS14 exhibits anticancer efficacy in various cancer cells .
|
-
- HY-14151
-
|
|
5-HT Receptor
Apoptosis
Autophagy
|
Neurological Disease
Cancer
|
|
Prucalopride is an orally active, selective and specific 5-HT 4 receptor agonist (high affinity), with pKis of 8.6 and 8.1 for human 5-HT4a/4b receptors, respectively. Prucalopride improves intestinal motility by promoting regeneration of the intestinal nervous system in rats. Prucalopride also shows anticancer activity by blocking of the PI3K/AKT/mTor signaling pathway. Prucalopride can be used in studies of chronic constipation, pseudo-intestinal obstruction and cancer .
|
-
- HY-10211
-
Tanespimycin
Maximum Cited Publications
47 Publications Verification
17-AAG; NSC 330507; CP 127374
|
HSP
Autophagy
Mitophagy
Bacterial
Apoptosis
Antibiotic
|
Infection
Cancer
|
|
Tanespimycin (17-AAG) is a potent HSP90 inhibitor with an IC50 of 5 nM, having a 100-fold higher binding affinity for tumour cell derived HSP90 than normal cell derived HSP90 . Tanespimycin depletes cellular STK38/NDR1 and reduces STK38 kinase activity. Tanespimycin also downregulates the stk38 gene expression .
|
-
- HY-107430B
-
|
Hydroxythiamine chloride
|
Apoptosis
|
Cancer
|
|
Oxythiamine (Hydroxythiamine) chloride, an analogue of anti-metabolite, can suppress the non-oxidative synthesis of ribose and induce cell apoptosis. Oxythiamine is a thiamine antagonist and inhibits transketolase (TK). Oxythiamine chloride inhibits cancer cell apoptosis and inhibits cell proliferation .
|
-
- HY-159006
-
|
|
Cytochrome P450
|
Cancer
|
|
CYP1B1 ligand 3 (Compound A1) is a selective inhibitor for cytochrome P450 enzyme CYP1B1 with an IC50 of 11.9 nM. CYP1B1 ligand 3 can be utilized for the synthesis of PROTAC CYP1B1 degrader-2 (HY-158429) .
|
-
- HY-14151R
-
|
|
5-HT Receptor
Apoptosis
Autophagy
|
Neurological Disease
Cancer
|
|
Prucalopride (Standard) is the analytical standard of Prucalopride. This product is intended for research and analytical applications. Prucalopride is an orally active, selective and specific 5-HT 4 receptor agonist (high affinity), with pKis of 8.6 and 8.1 for human 5-HT4a/4b receptors, respectively. Prucalopride improves intestinal motility by promoting regeneration of the intestinal nervous system in rats. Prucalopride also shows anticancer activity by blocking of the PI3K/AKT/mTor signaling pathway. Prucalopride can be used in studies of chronic constipation, pseudo-intestinal obstruction and cancer .
|
-
- HY-B0736AR
-
|
|
Fungal
Autophagy
Apoptosis
p38 MAPK
Microtubule/Tubulin
|
Infection
|
|
Sertaconazole (nitrate) (Standard) is the analytical standard of Sertaconazole (nitrate). This product is intended for research and analytical applications. Sertaconazole nitrate (FI7056) is a broad-spectrum topical antifungal agent, exhibits anti-inflammatory activity via activation of a p38-COX-2-PGE2 pathway. Sertaconazole nitrate is also a microtubule inhibitor, shows antiproliferative effect, induces apoptosis and autophagy, and can also inhibit the migration of cells .
|
-
- HY-141877
-
MS4322
1 Publications Verification
YS43-22
|
PROTACs
Histone Methyltransferase
|
Cancer
|
MS4322 (YS43-22) is a specific PRMT5 PROTAC degrader. MS4322 reduces the PRMT5 protein level with a DC50 of 1.1 μM in MCF-7 cells. MS4322 inhibits the methyltransferase activity of PRMT5 with an IC50 of 18 nM. MS4322 promotes ubiquitination and degradation of PRMT5. MS4322 can be used for the research of breast cancer, lung cancer, and hepatocellular cancer. (Pink: PRMT5 ligand (HY-173092); Blue: E3 ligase ligand HY-112078); Black: linker (HY-124780); E3+linker (HY-173093 )) .
|
-
- HY-153181
-
|
|
MEK
|
Cancer
|
|
Trametiglue, a derivative of Trametinib (HY-10999), targets both KSR-MEK and RAF-MEK with unprecedented potency and selectivity via unique interfacial binding interactions .
|
-
- HY-107430
-
|
Hydroxythiamin
|
Apoptosis
Endogenous Metabolite
|
Cancer
|
|
Oxythiamine (Hydroxythiamin), an analogue of anti-metabolite, can suppress the non-oxidative synthesis of ribose and induce cell apoptosis. Oxythiamine is a thiamine antagonist and inhibits transketolase (TK). Oxythiamine inhibits cancer cell apoptosis and inhibits cell proliferation .
|
-
- HY-155069
-
|
|
Apoptosis
|
Cancer
|
|
Antiproliferative agent-27 (compound 11) is an antiproliferative agent that significantly reduces the number of tumor cell colonies and induces apoptosis. Antiproliferative agent-27 has the potential to be used in the study of cancer .
|
-
- HY-107430A
-
|
Hydroxythiamine chloride hydrochloride
|
Apoptosis
Endogenous Metabolite
|
Cancer
|
|
Oxythiamine (Hydroxythiamine) chloride hydrochloride, an analogue of anti-metabolite, can suppress the non-oxidative synthesis of ribose and induce cell apoptosis. Oxythiamine chloride hydrochloride is a thiamine antagonist and inhibits transketolase (TK). Oxythiamine chloride hydrochloride inhibits cancer cell apoptosis and inhibits cell proliferation .
|
-
- HY-151968
-
|
|
Ras
|
Cancer
|
|
KRAS G12C inhibitor 57 (Compound 50) is a potent, selective, covalent and orally active KRAS G12C inhibitor with an IC50 of 0.21 μM in KRAS G12C/SOS1 binding assay. KRAS G12C inhibitor 57 induces cancer cell apoptosis .
|
-
- HY-B0736
-
-
- HY-111207
-
|
|
CDK
Apoptosis
|
Cancer
|
|
CA224 (Compound 1) is a selective and orally active Cdk4–cyclin D1 inhibitor with an IC50 of 6.2 µM. CA224 induces cell apoptosis and shows antitumor activity .
|
-
- HY-D2208
-
|
|
Fluorescent Dye
|
Others
|
|
SYTM Green is a permeable DNA dye that fluoresces green by binding to dsDNA (Ex/Em=503/530 nm). SYTM Green can also be used to stain bacteria, including Gram-positive and Gram-negative bacteria. Note: SYTM Green cannot penetrate living cells, and this product is equivalent to SYTOX Green .
|
-
- HY-168273
-
|
|
Amyloid-β
|
Neurological Disease
Cancer
|
|
Glutaminyl cyclases-IN-2 (compound 27) is a potent inhibitor of glutaminyl cyclase, with the IC50 of 0.08 μM. Glutaminyl cyclases-IN-2 plays an important role in cancer research .
|
-
- HY-163563
-
|
|
Ligands for Target Protein for PROTAC
|
Neurological Disease
|
|
JYQ-173 is a selective inhibitor for human Parkinson disease protein 7 (PARK7), with an IC50 of 19 nM. JYQ-173 exhibits good cell permeability. JYQ-173 is the ligand for target protein PARK7, which can be utilized for synthesis of PROTAC Degrader JYQ-194 (HY-163564) .
|
-
- HY-151497
-
-
- HY-146210
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-50 (Compound 9h) is a potent EGFR inhibitor against L858R resistance mutation (TEL-EGFR-L858R-BaF3: GI50=8 nM, TEL-EGFR-T790M-L858R-BaF3: GI50=6.03 μM). EGFR-IN-50 shows anti-proliferative activity to cancer cells .
|
-
- HY-151501
-
-
- HY-161285
-
|
|
MMP
|
Cancer
|
|
MMP-9/10-IN-2 (compound 6e) is a potent inhibitor of MMP10 and MMP9, with IC50 of 0.076 μM for MMP10, and 93.18% inhibition at 0.5 μM for MMP9. MMP-9/10-IN-2 plays an important role in anti-tumor .
|
-
- HY-149877
-
|
|
DNA/RNA Synthesis
Dihydroorotate Dehydrogenase
|
Cancer
|
|
hDHODH-IN-12 is a potent DHODH inhibitor with an IC50 value of 0.421 μM. DHODH is the rate-limiting enzyme in the de novo synthesis of pyrimidine which is essential in DNA/RNA Synthesis. hDHODH-IN-12 is present in the inner membrane of human mitochondria.hDHODH-IN-12 can be used for the research of lung cancer .
|
-
- HY-B0736A
-
|
FI7056
|
Fungal
Autophagy
Apoptosis
p38 MAPK
Microtubule/Tubulin
|
Infection
Cancer
|
|
Sertaconazole nitrate (FI7056) is a broad-spectrum topical antifungal agent, exhibits anti-inflammatory activity via activation of a p38-COX-2-PGE2 pathway. Sertaconazole nitrate is also a microtubule inhibitor, shows antiproliferative effect, induces apoptosis and autophagy, and can also inhibit the migration of cells .
|
-
- HY-N10391
-
|
Cleistenolide
|
Bacterial
|
Infection
Cancer
|
|
(-)-Cleistenolide is a α,β-unsaturated δ-lactone isolated from Cleistochlamys kirkii Oliver. (-)-Cleistenolide has antibacterial and antitumor activity .
|
-
- HY-P99345
-
|
TSR-042
|
PD-1/PD-L1
|
Cancer
|
|
Dostarlimab (TSR-042) is a humanized anti-PD-1 monoclonal antibody. Dostarlimab binds with high affinity to human PD-1 and competitively inhibits its interaction with its ligands, PD-L1 and PD-L2, with IC50s of 1.8 and 1.5 nM, respectively .
|
-
- HY-10211R
-
-
- HY-172251
-
|
|
FGFR
Apoptosis
|
Cancer
|
|
FGFR-IN-17 (Compound 12l) is an orally active irreversible inhibitor of FGFR, which has a strong inhibitory effect on FGFR and its mutants. FGFR-IN-17 can inhibit the proliferation and migration, and induce apoptosis of non-small cell lung cancer cells. FGFR-IN-17 has anti-tumor activity .
|
-
- HY-149032
-
|
|
Others
|
Cancer
|
|
Kobusine derivative-1 is a Kobusine derivative. Kobusine derivative-1 shows antiproliferative activities against cancer cells .
|
-
- HY-147816
-
|
|
Mitochondrial Metabolism
|
Cancer
|
|
Anticancer agent 70 (Compound 21), an anticancer agent, exhibits remarkable cytotoxic activity against numerous human cancer cell lines. Anticancer agent 70 results in the G0/G1-cell cycle arrest with a concomitant increase in p53 and p21 protein levels. Anticancer agent 70 leads to ATP depletion and disruption of the mitochondrial membrane potential .
|
-
- HY-129325
-
|
|
Antibiotic
Bacterial
Apoptosis
Bcl-2 Family
Caspase
|
Infection
Cancer
|
|
Cytochalasin H is a nature product that could be isolated from fungus Phomopsis sp. Cytochalasin H inhibits cell growth and induces apoptosis. Cytochalasin H has anti-angiogenic activity. Cytochalasin H is an antibiotic and has antibacterial activity .
|
-
- HY-16967
-
|
|
G-quadruplex
|
Cancer
|
|
MM41 is a potent stabilizer of human telomeric and gene promoter DNA quadruplexes. MM41 is potently against the MIA PaCa-2 pancreatic cancer cell line with IC50 value of <10 nM .
|
-
- HY-156275
-
|
|
Others
|
Cancer
|
|
OSBP-IN-1(compound 12) is a Schweinfurthins analogues targeted of oxysterol-binding protein (OSBP). OSBP-IN-1 has antitumor activity .
|
-
- HY-N1710
-
|
|
Apoptosis
Caspase
|
Cancer
|
|
28-Deoxonimbolide is a nimbin (HY-N3187) type limonoid, that can be isolated from Azadirachta indica seed extracts. 28-Deoxonimbolide shows anticancer activity. 28-Deoxonimbolide induces apoptotic cell death in HL60 cells via both the mitochondrial- and the death receptor-mediated pathways .
|
-
- HY-136540
-
|
RvD3
|
AMPK
Autophagy
|
Inflammation/Immunology
|
|
Resolvin D3 (RvD3) is a docosahexaenoic acid (DHA) derived mediator. Resolvin D3 is dysregulated in arthritis and reduces arthritic inflammation .
|
-
- HY-151502
-
-
- HY-161153
-
|
|
Apoptosis
|
Cancer
|
|
Microtubule inhibitor 9 (Compound O-7) is a 2-Aryl-1H-benzo [d] imidazole derivative with in vitro anticancer activity. Microtubule inhibitor 9 can induce cell cycle arrest at the G2/M phase and early apoptosis. Microtubule inhibitor 9 inhibits cancer cell migration by inhibiting wound healing and colony formation .
|
-
- HY-163768
-
|
|
β-catenin
|
Inflammation/Immunology
Cancer
|
|
Antitumor agent-172 (Compound 28) is an inhibitor for β-catenin/BCL9 interaction with IC50 of 3.92 μM. Antitumor agent-172 exhibits high affinity to β-catenin with Kd of 82 nM. Antitumor agent-172 activates T cells, promotes antigen presentation, and exhibits antitumor efficacy and good pharmacokinetic characteristics in mouse models .
|
-
- HY-158138
-
|
|
PARP
Topoisomerase
Apoptosis
|
Cancer
|
|
TOPOI/PARP-1-IN-1 (Compound B6) is an orally active, low cytotoxic TOPOI/PARP dual inhibitor with an IC50 value of 0.09 μM for PARP1. TOPOI/PARP-1-IN-1 can effectively inhibit the proliferation and migration of cancer cells. TOPOI/PARP-1-IN-1 also causes cell cycle arrest in the G0/G1 phase and induces apoptosis. The tumor growth inhibition rate (TGI) of TOPOI/PARP-1-IN-1 in mice is 75.4% .
|
-
- HY-161076
-
-
- HY-19747
-
HPOB
3 Publications Verification
|
HDAC
Apoptosis
|
Cancer
|
|
HPOB is a highly potent and selective inhibitor of HDAC6 with an IC50 of 56 nM. HPOB displays >30 fold less potent against other HDACs. HPOB enhances the effectiveness of DNA-damaging anticancer agents in transformed cells but not normal cells. HPOB does not block the ubiquitin-binding activity of HDAC6 .
|
-
- HY-W773183
-
|
Betulonic acid methyl ester; Methyl 3-oxolup-20(29)-en-28-oate
|
Others
|
Cancer
|
|
Methyl betulonate (Betulonic acid methyl ester) is a triterpenoid. Methyl betulonate inhibits cell growth of eight tumor (including resistant) and two normal fibroblast cell lines with the IC50s >50.0 μM .
|
-
- HY-163522
-
|
|
Influenza Virus
|
Infection
|
|
Neuraminidase-IN-20 (Compound 5i) is a potent inhibitor of mutant neuraminidase (NA) (H5N1-H274Y) (IC50= 0.44 μM).Neuraminidase-IN-20 binds to the 430 cavity site of NA and disrupts the enzymatic activity of NA .
|
-
- HY-170665
-
|
|
EGFR
|
Cancer
|
|
EGFR T790M/L858R-IN-9 (Compound 8) is an EGFR-L858R/T790M inhibitor that demonstrates potent inhibitory phosphorylation effects against the EGFR-L858R/T790M mutant kinase, with an IC50 value of 0.0064µM. EGFR T790M/L858R-IN-9 also inhibits the proliferation of non-small cell lung cancer (NSCLC) cells and can be utilized in cancer research .
|
-
- HY-D1719
-
|
|
Fluorescent Dye
|
Others
|
|
Cypate, a cyanine dye, is a near infrared (NIR) fluorescent probe for in vivo tumor imaging .
|
-
- HY-144793
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Deac-SS-Biotin is a potent antitumor agent with improved tumor targeting effects and reduced off-target toxicities. Deac-SS-Biotin uptakes into the cells through biotin-mediated internalization. Deac-SS-Biotin combined with DTT (Glutathione mimetic) can effectively inhibit microtubule assembly and displays greater antitumor activity .
|
-
- HY-164413
-
|
|
VEGFR
EGFR
RET
Apoptosis
|
Cancer
|
|
CLM3, a pyrazolopyrimidine derivative, is a multiple tyrosine kinase inhibitor. CLM3 shows antiproliferative and proapoptotic activity on endothelial and cancer cells, synergistically enhanced by SN38 (HY-13704). These effects are mainly due to its inhibition of phosphorylation of VEGFR-2, EGFR and RET tyrosine kinases and their related signaling pathways .
|
-
- HY-N2454
-
-
- HY-144686
-
|
|
ATM/ATR
PI3K
mTOR
|
Cancer
|
|
ATM Inhibitor-3 (compound 34) is a potent and selective ATM inhibitor, with an IC50 of 0.71 nM. ATM Inhibitor-3 shows inhibition of PI3K kinases family. ATM Inhibitor-3 exhibits favorable metabolic stability .
|
-
- HY-173000
-
|
|
Apoptosis
Ferroptosis
STAT
|
Cancer
|
|
STAT3-IN-40 (Compound 8b) is an anti-cancer agent. STAT3-IN-40 can trigger the immune responses of CD4+ and CD8+ T lymphocytes and induce ferroptosis and apoptosis of tumor cells by inhibiting the expression and phosphorylation of STAT3. STAT3-IN-40 can be used in the research of chemoimmunotherapeutic agents for cancer .
|
-
- HY-144687
-
|
|
ATM/ATR
PI3K
mTOR
|
Cancer
|
|
ATM Inhibitor-4 (compound 39) is a potent and selective ATM inhibitor, with an IC50 of 0.32 nM. ATM Inhibitor-4 shows stronger inhibition of PI3K kinases family. ATM Inhibitor-4 shows a full inhibition of mTOR at 1 μM. ATM Inhibitor-4 exhibits favorable metabolic stability .
|
-
- HY-155040
-
|
|
Biochemical Assay Reagents
|
Cancer
|
|
Antitumor agent-106 (compound 42) is an anticancer agent that exhibits good inhibitory activity (IC50=4.2-6.6 µM) against both lung cancer and colon cancer cell lines .
|
-
- HY-139056
-
-
- HY-119152
-
|
|
Insulin Receptor
Tyrosinase
Akt
|
Others
|
|
CMX-2043 is a novel analogue of α-Lipoic Acid (HY-N0492). CMX-2043 is effective in antioxidant effect, activation of insulin receptor kinase, soluble tyrosine kinase, and Akt phosphorylation. CMX-2043 shows protection against ischemia-reperfusion injury (IRI) in rat model .
|
-
- HY-149508
-
|
|
Keap1-Nrf2
Reactive Oxygen Species
|
Cancer
|
|
Nrf2-IN-3 (Compound R16) is a small-molecule NRF2 inhibitor and increases reactive oxygen species (ROS) production. Nrf2-IN-3 selectively binds KEAP1 mutants and restores their NRF2-inhibitory function by repairing the disrupted KEAP1/NRF2 interactions, leading to proteasome-dependent NRF2 degradation in cells. Nrf2-IN-3 sensitizes KEAP1-mutated tumor cells to Cisplatin (HY-17394), Gefitinib (HY-50895), and KEAP1 G333C-mutated xenograft to Cisplatin .
|
-
- HY-156694
-
|
|
Apoptosis
|
Cancer
|
|
Hydroxy-PP-Me is a potent and specific CBR1 inhibitor with an IC50 of 759 nM. Hydroxy-PP-Me inhibits serum-withdrawal-induced apoptosis. Hydroxy-PP-Me increases As2O3-induced apoptotic cell death compared with As2O3 alone .
|
-
- HY-123502
-
|
AZD-6738 formate
|
ATM/ATR
|
Cancer
|
|
Ceralasertib formate is a potent, selective and orally active ATR inhibitor with an IC50 value of 1 nM. Ceralasertib formate inhibits cell viability and induces DNA damage. Ceralasertib formate induces cell senescence. Ceralasertib formate shows antitumor activity .
|
-
- HY-125265
-
|
|
Glucocorticoid Receptor
|
Metabolic Disease
|
|
JTP-117968, a novel selective glucocorticoid receptor modulator (a non-steroidal SGRM, IC50 of 6.8 nM), exhibits improved transrepression/transactivation dissociation .
|
-
- HY-N2454R
-
-
- HY-170992
-
|
|
Autophagy
CDK
Atg8/LC3
PINK1/Parkin
|
Cancer
|
|
Autophagy agonist-1 (compound 22) is an Autophagy agonist. Autophagy agonist-1 exhibits significant anticancer activity against HepG2 cells and normal cells with IC50s of 8.8 μM and > 50 μM. Autophagy agonist-1 induces G1/S phase cell cycle arrest and inhibits CDK4 and CyclinD1 expression while upregulating P21. Autophagy agonist-1 promotes the accumulation of autophagosomes and the proteins LC3 and PINK1, enhancing autophagy and mitophagy in HepG2 cells .
|
-
- HY-161860
-
|
|
Bacterial
|
Cancer
|
|
Antibacterial agent 233 (Compound 7c) exhibits inhibitory efficacy against Helicobacter pylori with MIC of 0.4-1.6 μg/mL. Antibacterial agent 233 inhibits jack bean urease (IC50 is 0.27 μg/mL), changes the permeability of H. pylori cell membrane, causes the leakage of cellular contents. Antibacterial agent 233 exhibits metabolic stability in whole blood and artificial gastric fluid. Antibacterial agent 233 exhibits antitumor efficacy against U2OS in mice .
|
-
- HY-150597
-
|
|
HDAC
Apoptosis
|
Cancer
|
|
HDAC-IN-46 (compound 12c) is a potent HDAC inhibitor with an IC50 value of 0.21 μM and 0.021 μM for HDAC1 and HDAC6, respectively. HDAC-IN-46 upregulates p-p38, and downregulates Bcl-xL and cyclin D1 in MDA-MB-231 cells. HDAC-IN-46 induces significant G2 phase arrest and apoptosis. HDAC-IN-46 can be used for researching triple-negative breast cancer (TNBC) .
|
-
- HY-144685
-
|
|
ATM/ATR
|
Cancer
|
|
ATM Inhibitor-2 (compound 7) is a potent and selective ATM inhibitor, with an IC50 of <1 nM .
|
-
- HY-148117
-
-
- HY-151434
-
|
|
Glutaminase
Apoptosis
|
Cancer
|
|
GLS1 Inhibitor-6 (Compound 24y) is an orally active, potent and selective glutaminase 1 (GLS1) inhibitor (IC50=68 nM), shows 220-fold selectivity for GLS2. GLS1 Inhibitor-6 shows good anti-tumor activity, antitumor cell proliferation activity and induces apoptosis .
|
-
- HY-150571
-
|
|
Topoisomerase
c-Myc
Apoptosis
ROS Kinase
|
Cancer
|
|
Anticancer agent 76 (Compound CT2-3) is an anticancer agent. Anticancer agent 76 significantly inhibits the proliferation of human NSCLC cells, induces cell cycle arrest, causes ROS generation and induces cell apoptosis .
|
-
- HY-157137
-
|
|
PARP
Caspase
Apoptosis
|
Cancer
|
|
PARP1-IN-17 is a PARP-1 inhibitor (IC50 = 19.24 nM for PARP-1 and = 32.58 nM for PARP-2) and induce apoptosis. PARP1-IN-17 shows excellent anti-proliferative activity .
|
-
- HY-170655
-
|
|
PDI
Integrin
|
Cardiovascular Disease
|
|
PDI-IN-4 (Compound 14d) is an inhibitor of protein disulfide isomerase, with an IC50 value of 0.48 μM. PDI-IN-4 suppresses platelet aggregation and thrombus formation by attenuating GPIIb/IIIa activation without significantly causing cytotoxicity. PDI-IN-4 can be used in research on thrombosis .
|
-
- HY-15866
-
|
|
Others
|
Cancer
|
|
FR901465 is a potent anti-cancer and anti-tumor agent. FR901465 can be used for cancer research .
|
-
- HY-150596
-
|
|
Apoptosis
Bcl-2 Family
JNK
|
Cancer
|
|
CT1-3 is a potent anticancer agent. CT1-3 induces mitochondria-mediated apoptosis by regulating JNK/Bcl-2/Bax/XIAP pathway. CT1-3 suppresses the epithelial mesenchymal transition (EMT) potential of human cancer cells (HCCs) via regulating the E-cadherin/Snail axis, thus inhibits tumorigenesis. CT1-3 has a strong antitumor effect in mice model and exhibits no significant hepatic and renal toxicity .
|
-
- HY-163195
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
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 .
|
-
- HY-W010155
-
-
- HY-N7205
-
|
|
Others
|
Cancer
|
|
Glaucocalyxin D is a ent-kauranoid-type diterpenoid that can be isolated from Rabdosia japonica. Glaucocalyxin D shows cytotoxicity against various human tumor cell lines. Glaucocalyxin D can be used for cancer research .
|
-
- HY-172225
-
|
|
Apoptosis
Autophagy
Ferroptosis
|
Cancer
|
|
[Ru(phen)2(HMPIP)](PF6)2 (Compound 6A) is an anti-tumor agent. [Ru(phen)2(HMPIP)](PF6)2 can inhibit the proliferation and migration of HepG2 liver cancer cells, and induce apoptosis, autophagy, cell cycle arrest and ferroptosis of HepG2 liver cancer cells. [Ru(phen)2(HMPIP)](PF6)2 exerts its anti-tumor activity by stimulating immune response to increase CD8+ T cells .
|
-
2](//file.medchemexpress.eu/product_pic/hy-172225.gif)
- HY-N12603
-
|
|
Apoptosis
|
Cancer
|
|
Typhatifolin B (Compd 2), an anti-cancer agent, could remarkably induce cell apoptosis and G0/G1 cycle arrest, as well as block cell migration and invasion .
|
-
- HY-N3376
-
|
Spermatheridine; VLT045
|
Apoptosis
|
Cancer
|
|
Liriodenine (Spermatheridine; VLT045) is an aporphine alkaloid isolated from the plant?Mitrephora sirikitiae?and has anti-cancer activities . Liriodenine induces cell apoptosis, activates the intrinsic pathway by induction of caspase-3 and caspase-9 .
|
-
- HY-N0638
-
-
- HY-19825
-
|
|
Topoisomerase
ADC Cytotoxin
Antibiotic
|
Cancer
|
|
Rebeccamycin, an antitumor antibiotic, inhibits DNA topoisomerase I. Rebeccamycin appears to exert its primary antineoplastic effect by poisoning topoisomerase I and has negligible effect on protein kinase C and topoisomerase II .
|
-
- HY-50683
-
|
|
c-Met/HGFR
|
Metabolic Disease
Cancer
|
|
JNJ-38877605 is an orally active ATP-competitive inhibitor of c-Met with an IC50 of 4 nM, 600-fold selective for c-Met than 200 other tyrosine and serine-threonine kinases . JNJ-38877605 inhibits c-Met phosphorylation and regulates lipid accumulation. JNJ-38877605 can be used for tumor and metabolic disease reseach .
|
-
- HY-146889
-
|
|
Phosphodiesterase (PDE)
|
Cancer
|
|
ATX inhibitor 16 is a potent ATX inhibitor with an IC50 of 0.0021 μM. ATX inhibitor 16 shows excellent anti-proliferative activities in breast cancer cells .
|
-
- HY-14928A
-
|
|
PPAR
ERK
JNK
TGF-beta/Smad
NO Synthase
COX
NF-κB
Interleukin Related
|
Metabolic Disease
|
|
Lobeglitazone sulfate is a new type of thiazolidinedione. Lobeglitazone sulfate is the orally active agonist for PPAR with EC50 of 137.4 nM and 546.3 nM for PPARγ and PPARα. Lobeglitazone sulfate is the inhibitor for ERK/JNK/Smad/NF-κB signaling pathway. Lobeglitazone sulfate exhibits anti-inflammatory, anti-diabetic, anti-fibrotic and anti-atherosclerotic properties .
|
-
- HY-162071
-
|
|
Pyruvate Kinase
|
Cancer
|
|
PKM2-IN-5 (Compound G1) is an inhibitor for pyruvate kinase M2 (PKM2), with IC50 >70 μM .
|
-
- HY-172393
-
|
|
β-catenin
Apoptosis
Caspase
MDM-2/p53
Bcl-2 Family
Cytochrome P450
|
Cancer
|
|
TCF4/β-catenin-IN-1 (Compound 8b) is an inhibitor of TCF4/β-catenin, and induces apoptosis. TCF4/β-catenin-IN-1 up-regulates p53, caspase-3, caspase-8, caspase-9 levels and Bax protein expression as well as down-regulates Bcl-2 protein expression. TCF4/β-catenin-IN-1 can inhibit CYP3A4, CYP1A2, CYP2C19, and shows promising cytotoxic activity in cancer cells .
|
-
- HY-139606
-
|
|
p97
|
Cancer
|
|
VCP/p97 inhibitor-1 is a potent inhibitor of VCP/p97 (also called Cdc48, CDC-. 48, or Ter94) with an IC50 of 54.7 nM. VCP/p97 inhibitor-1 causes the dysregulation of protein homeostasis and disturbs the degradation of misfolded polypeptides by the ubiquitin-proteasome system (UPS) .
|
-
- HY-163760
-
|
|
HuR
MMP
|
Cancer
|
|
ZM-32 is an inhibitor for human antigen R (HuR), that downregulates the expression of VEGF-A and MMP9, and thus inhibits breast cancer tumor angiogenesis. ZM-32 exhibits broad-spectrum anti-proliferative effects in a variety of cancer cell lines, and exhibits antitumor efficacy against MDA-MB-231 in mouse models .
|
-
- HY-125085
-
|
|
Aldehyde Dehydrogenase (ALDH)
|
Cancer
|
|
ALDH3A1-IN-3 (CB29) is a selective inhibitor of ALDH3A1, with a Ki value of 4.7 μM and an IC50 value of 16 μM. ALDH3A1-IN-3 has no inhibitory potential on the in vitro activity of ALDH1A1, ALDH1A2, ALDH1A3, ALDH1B1, or ALDH2. ALDH3A1-IN-3 can be used in cellular oxidation and cancer research .
|
-
- HY-B0486R
-
|
|
Hexokinase
Mitochondrial Metabolism
Apoptosis
Parasite
|
Inflammation/Immunology
Cancer
|
|
Lonidamine (Standard) is the analytical standard of Lonidamine. This product is intended for research and analytical applications. Lonidamine (AF-1890) is a hexokinase and mitochondrial pyruvate carrier inhibitor (Ki: 2.5 μM). Lonidamine also inhibits aerobic glycolysis in cancer cells. Lonidamine can be used in the research of mitochondrial metabolism and inflammation, such as pulmonary fibrosis .
|
-
- HY-113471
-
|
|
Apoptosis
HSV
|
Infection
Inflammation/Immunology
Cancer
|
|
Perillic acid is the metabolite of Perillyl alcohol (HY-N7000). Perillic acid induces lung cancer cell cycle arrest and apoptosis. Perillic acid shows anti-HSV-1 and immunomodulatory activities .
|
-
- HY-131059
-
|
|
Influenza Virus
|
Infection
|
|
CBS1117 is a virus entry inhibitor with an IC50 of 70 nM for influenza A virus, A/Puerto Rico/8/34 (H1N1). CBS1117 interferes with the hemagglutinin (HA)-mediated fusion process .
|
-
- HY-B0486
-
-
- HY-161773
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
HL389-NHC2-PEG3-C2NH inhibits proliferation of cancer cells MDA-MB-231 and MCF-7, with IC50 of 11.39 μM and 9.66 μM. HL389-NHC2-PEG3-C2NH can be utilized as a conjugate of an E3 ligase ligand and a linker, for the synthesis of PROTAC degrader HL435 (HY-161769) .
|
-
- HY-161501
-
|
|
GLUT
Topoisomerase
Apoptosis
|
Cancer
|
|
3-Fluoro-evodiamine glucose (Compound 8) is an evodiamine-glucose conjugate. 3-Fluoro-evodiamine glucose activates the expression of glucose transporter 1 (GLUT1), and inhibits topoisomerase I/II. 3-Fluoro-evodiamine glucose induces apoptosis and arrests the cell cycle at G2/M phase. 3-Fluoro-evodiamine glucose exhibits antitumor efficacy in vivo and in vitro, without significant toxicity .
|
-
- 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-161350
-
-
- HY-148413
-
|
ISIS 3521 sodium
|
PKC
|
Cancer
|
|
Aprinocarsen (ISIS 3521) sodium, a specific antisense oligonucleotide inhibitor of protein kinase C-alpha (PKC-α). Aprinocarsen sodium is a 20-mer oligonucleotide, it regulates cell differentiation and proliferation. Aprinocarsen sodium inhibits the growth of human tumor cell lines in nude mice. Aprinocarsen sodium shows the value as a chemotherapeutic compound of human cancers .
|
-
- HY-107591A
-
|
|
IKK
|
Inflammation/Immunology
|
|
(Rac)-PF-184 hydrate is a potent inhibitory factor-κB kinase 2 (IKK-2) inhibitor with an IC50 of 37 nM. (Rac)-PF-184 hydrate has anti-inflammatory effects .
|
-
- HY-N10558
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
PM050489 is an effective polyketone inhibitor of Microtubule/Tubulin that can be isolated from Madagascan sponge Lithoplocamia lithistoides. PM050489 inhibits mitosis with an IC50 value of 26.4 nM. PM050489 has antitumor activity and can be used in cancer research .
|
-
- HY-161770
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
HL389 inhibits proliferation of cancer cells MDA-MB-231 and MCF-7, with IC50 of 11.39 μM and 9.66 μM. HL389 can be utilized as the ligand for E3 ligase for the synthesis of PROTAC degrader HL435 (HY-161769) .
|
-
- HY-14928
-
-
- HY-151445
-
|
|
DNA Methyltransferase
Virus Protease
Flavivirus
|
Infection
|
|
ZIKV-IN-2 (compound 3a) is a potent ZIKV NS5 methyl transferase (MTase) inhibitor with an IC50 value of 38.86 μM. ZIKV-IN-2 inhibits ZIKV replication and infection. ZIKV-IN-2 can be used in research of Zika virus (ZIKV) .
|
-
- HY-144807
-
|
|
Carbonic Anhydrase
|
Cancer
|
|
Carbonic anhydrase inhibitor 9 is a potent carbonic anhydrase (CA) inhibitor with Kis of 56.4 and 56.9 nM for hCA II and IX, respectively. Antiproliferative activity .
|
-
- HY-150719
-
-
- HY-P2282
-
|
|
STAT
|
Cancer
|
|
APTSTAT3-9R, a specific STAT3-binding peptide, inhibits STAT3 activation and downstream signaling by specifically blocking STAT3 phosphorylation. APTSTAT3-9R exerts antiproliferative effects and antitumor activity .
|
-
- HY-122919
-
|
|
Endogenous Metabolite
|
Cancer
|
|
Momordicoside L is a Cucurbitane Triterpenoid, that can be isolated from the leaves of Momordica charantia. Momordicoside L shows anticancer activity .
|
-
- HY-107591
-
|
|
IKK
|
Inflammation/Immunology
|
|
(Rac)-PF-184 is a potent inhibitory factor-κB kinase 2 (IKK-2) inhibitor with an IC50 of 37 nM. (Rac)-PF-184 has anti-inflammatory effects .
|
-
- HY-170558
-
|
|
FLT3
Apoptosis
|
Cancer
|
|
FW-1 is a type I inhibitor for FLT3 with IC50 of ca. 1 μM. FW-1 exhibits cytotoxicity in FLT3 mutated AML cell. FW-1 arrests the cell cycle at G0/G1 phase, and induces apoptosis in cell MV4-11 and MOLM-13 .
|
-
- HY-144395
-
|
|
HDAC
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
HDAC6-IN-4 (C10) is a potent, orally active and highly selective HDAC6 inhibitor with an IC50 value of 23 nM. HDAC6-IN-4 induces cancer cells apoptosis and shows significant antitumor efficacy, without obvious toxicity .
|
-
- HY-N8915
-
|
|
Others
|
Others
|
|
Deoxyflindissone (Compound 13) is a triterpenoid
compound. Deoxyflindissone is isolated from natural Cornus walteri
.Deoxyflindissone has significant cytotoxic activity
.
|
-
- HY-151563A
-
|
|
Deubiquitinase
|
Cancer
|
|
OTUB1/USP8-IN-1 TFA is the TFA salt form of OTUB1/USP8-IN-1 (HY-151563). OTUB1/USP8-IN-1 TFA is a dual inhibitor for OTUB1/USP8, IC50 for OTUB1 and USP8 is 0.17 and 0.28 nM, respectively. OTUB1/USP8-IN-1 TFA inhibits proliferation of NSCLC cells. OTUB1/USP8-IN-1 TFA exhibits good pharmacokinetic characters in ICR mouse, and exhibits antitumor activity in H1975 xenograft mouse model .
|
-
- HY-146890
-
|
|
Phosphodiesterase (PDE)
|
Cancer
|
|
ATX inhibitor 17 is a potent ATX inhibitor with an IC50 of 0.019 μM. ATX inhibitor 17 shows excellent anti-proliferative activities in breast cancer cells .
|
-
- HY-150648
-
|
|
Aldose Reductase
|
Cancer
|
|
S07-2008 is a selective aldo-keto reductase family 1 member C3 (AKR1C3) inhibitor with an IC50 of 0.16 μM. S07-2008 shows anticancer activities .
|
-
- HY-170318
-
|
|
Myosin
|
Cancer
|
|
Adhibin is an allosteric inhibitor for RhoGAP class IX myosin, that inhibits Myo9 ATPase in mammalian and invertebrate with IC50 of 2.5 µM and 2.6 µM. Adhibin binds to the ATPase of myosin, interfers with its motor function, blocks the RhoGTPase related signaling pathway, and affects the cell migration, adhesion and cell division. Adhibin can be used in research about cancer metastasis .
|
-
- HY-151443
-
|
|
HDAC
|
Cancer
|
|
HDAC-IN-47 is an orally active inhibitor of histone deacetylase (HDAC), with IC50s of 19.75 nM (HDAC1), 5.63 nM (HDAC2), 40.27 nM (HDAC3), 57.8 nM (HDAC2), 302.73 nM (HDAC8), respectively. HDAC-IN-47 inhibits autophagy and induces apoptosis via the Bax/Bcl-2 and caspase-3 pathways. HDAC-IN-47 arrests cell cycle at G2/M phase, and shows anti-tumor efficacy in vivo .
|
-
- HY-149410
-
|
|
Topoisomerase
|
Cancer
|
|
MSN8C, an analog of mansonone E, is a novel catalytic inhibitor of human DNA topoisomerase II. MSN8C induces cancer cell apoptosis. MSN8C shows significant anti-tumor cell proliferation activity in vitro .
|
-
- HY-124451
-
|
|
Apoptosis
Autophagy
|
Cancer
|
|
2-Chloronaphthalene, serving as an intermediate in organic synthesis, is classified as a persistent organic pollutant. 2-Chloronaphthalene can induce apoptosis and autophagy, while inhibiting cell proliferation. 2-Chloronaphthalene leads to cell death through the interplay between autophagy and apoptosis .
|
-
- HY-161385
-
|
|
Topoisomerase
|
Cancer
|
|
Topoisomerase I inhibitor 21 (Compound 3e) is an inhibitor for Topoisomerase I through stabilization of enzyme-DNA complex. Topoisomerase I inhibitor 21 exhibits antiproliferative activity in 39 human cancer cells (JFCR39) with mean GI50 39 nM .
|
-
- HY-136265
-
|
|
Aminoacyl-tRNA Synthetase
|
Cancer
|
|
BC-LI-0186 is a potent and selective inhibitor of Leucyl-tRNA synthetase (LRS; LeuRS) and Ras-related GTP-binding protein D (RagD) interaction (IC50=46.11 nM). BC-LI-0186 competitively binds to the RagD interacting site of LRS (Kd=42.1 nM) and has on effects on LRS-Vps34, LRS-EPRS, RagB-RagD association, mTORC1 complex formation or the activities of 12 kinases. BC-LI-0186 can effectively suppress the activity of cancer-associated?MTOR?mutants and the growth of rapamycin-resistant cancer cells.?BC-LI-0186 is a promising agent for lung cancer research .
|
-
- HY-162227
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Antitumor agent-138 (compound 5b) is an inhibitor against tubulin polymerization at tubulin colchicine-binding sites, with IC50 of 1.87 μM. Antitumor agent-138 arrests the cell cycle at G2/M phase and induces an apoptosis in MCF-7 cells. Antitumor agent-138 inhibits cells migration and angiogenesis .
|
-
- HY-146407
-
|
|
Apoptosis
|
Cancer
|
|
Anticancer agent 53 is a potent anticancer agent. Anticancer agent 53 shows in vitro cytotoxicity. Anticancer agent 53 induces apoptosis and cell cycle arrest in S/G2/M phases. Anticancer agent 53 shows antitumor activity with no apparent toxicity .
|
-
- HY-124056
-
|
|
CXCR
|
Cancer
|
|
AZ10397767 is an orally active, selective CXCR2 receptor antagonist with an IC50 of 1 nM. AZ10397767 attenuates the Oxaliplatin (HY-17371)-induced NF-κB transcriptional activity and potentiates Oxaliplatin-induced apoptosis in androgen-independent prostate cancer (AIPC) cells. AZ10397767 significantly inhibits neutrophil recruitment into tumors which then adversely affects tumor growth in vitro and in vivo .
|
-
- HY-126566
-
|
|
Fungal
HDAC
Apoptosis
|
Infection
Cancer
|
|
Trichostatin C is an inhibitor for histone deacetylase (HDAC), induces apoptosis and arrests cell cycle at G2/M phase, and exhibits anticancer activity against lung cancer and urothelial bladder cancer . Trichostatin C induces differentation of Friend leukemic cells . Trichostatin C exhibits antifungal activity .
|
-
- HY-151155
-
|
|
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
|
ALK-IN-23 is a potent ALK inhibitor with IC50 values of 1.6 nM, 0.71 nM and 1.3 nM for ALK WT, ALK L1196M and ALK G1202R. ALK-IN-23 can block cell cycle in G2 phase and induce apoptosis. ALK-IN-23 inhibits cancer cell migration and colony formation in vitro. ALK-IN-23 exhibits antitumor activity in H2228 xenograft nude mice model with hypotoxicity .
|
-
- HY-151799
-
|
|
p62
E1/E2/E3 Enzyme
Apoptosis
|
Cancer
|
|
P62-RNF168 agonist-1 (compound 5a) is a low cytotoxicity P62-RNF168 agonist that enhances the interaction between P62 and RNF168. P62-RNF168 agonist-1 induces a reduction in H2A ubiquitination mediated by RNF168 and impairs homologous recombination-mediated DNA repair. P62-RNF168 agonist-1 also inhibits the growth of xenograft tumors in mice in a dose-dependent manner .
|
-
- HY-163381
-
|
|
Others
|
Cancer
|
|
Antiproliferative agent-48 (compound PC-A1) shows selective antiproliferative activity against triple-negative breast cancer (TNBC) cells .
|
-
- HY-15856B
-
|
Flupenthixol dihydrochloride
|
Dopamine Receptor
PI3K
Apoptosis
|
Neurological Disease
Cancer
|
|
Flupentixol is an orally active D1/D2 dopamine receptor antagonist and new PI3K inhibitor (PI3Kα IC50=127 nM). Flupentixol shows anti-proliferative activity to cancer cells and induces apoptosis. Flupentixol can also be used in schizophrenia, anxiolytic and depressive research .
|
-
- HY-B1357R
-
|
|
Bcl-2 Family
Caspase
Apoptosis
HSV
Na+/K+ ATPase
Calcium Channel
|
Cardiovascular Disease
Cancer
|
|
Digitoxin (Standard) is the analytical standard of Digitoxin. This product is intended for research and analytical applications. Digitoxin is an anti-cancer agent. Digitoxin induces apoptosis, inhibits influenza cytokine storm, causes DNA double-stranded breaks (DSBs) and blocks the cell cycle at the G2/M phase. Digitoxin induces calcium uptake into cells by forming transmembrane calcium channels and can be used for research of heart failure .
|
-
- HY-N0867
-
|
|
HIV
ULK
Bcl-2 Family
|
Infection
Cancer
|
|
13-Oxyingenol-dodecanoate (13OD) is a tumor suppressor agent. 13-Oxyingenol-dodecanoate has anti-HIV-1 activity with EC50 value of 33.7 nM .13-Oxyingenol-dodecanoate can induce the expression of ULK1 to effect mitochondrial dysfunction and cellular autophagy. 13-Oxyingenol-dodecanoate also increases the expression of BAX and suppresses the expression of BCL-2 to effect apoptosis .
|
-
- HY-120027
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Kribb3 is an inhibitor for microtubule. KRIBB3 inhibits the proliferation of cancer cells with GI50 of 0.2-2.5 μM, arrests cell cycle at G2/M phase, and induces apoptosis in HCT-116. Kribb3 exhibits antitumor activity in mouse models .
|
-
- HY-12486
-
|
10,11-(Methylenedioxy)-20(S)-camptothecin
|
Survivin
Apoptosis
IAP
|
Cancer
|
|
FL118 (10,11-(Methylenedioxy)-20(S)-camptothecin), a Camptothecin (HY-16560) analogue, is a potent and orally active survivin inhibitor. FL118 binds to oncoprotein DDX5 (p68) to dephosphorylates and degrades DDX5. FL118 can be used for the research of cancer .
|
-
- HY-B1513
-
|
|
Microtubule/Tubulin
SARS-CoV
|
Infection
Metabolic Disease
Cancer
|
|
α-Cyclodextrin (α-CD) is a soluble fiber derived from corn. α-Cyclodextrin can deplete sphingolipids and phospholipids from cell membranes. α-Cyclodextrin interacts with tubulin. α-Cyclodextrin improves defenses against SARS-CoV-2 infection. α-Cyclodextrin enhances the anticancer efficacy of Crcumin (HY-N0005) against breast, lung and cervical cancer. α-Cyclodextrin has beneficial effects on body weight and blood lipids .
|
-
- HY-149968
-
|
|
Histone Demethylase
Apoptosis
|
Cancer
|
|
LSD1-IN-25 (Compound 9j) is a potent, selective and orally active LSD1 inhibitor with an IC50 of 46 nM (Ki = 30.3 nM). LSD1-IN-25 induces cancer cell apoptosis .
|
-
- HY-152099
-
|
|
Apoptosis
|
Cancer
|
|
Antiproliferative agent-19 (compound 4a) is an anti-cancer agent that exerts anti-proliferative effects on lung cancer cells by inducing apoptosis. antiproliferative agent-19 also induces cell cycle arrest in the G2/M phase .
|
-
- HY-15856A
-
|
Flupenthixol
|
Dopamine Receptor
PI3K
Apoptosis
|
Neurological Disease
|
|
Flupentixol is an orally active D1/D2 dopamine receptor antagonist and new PI3K inhibitor (PI3Kα IC50=127 nM). Flupentixol shows anti-proliferative activity to cancer cells and induces apoptosis. Flupentixol can also be used in schizophrenia, anxiolytic and depressive research .
|
-
- HY-172170
-
|
|
Histone Demethylase
|
Cancer
|
|
LSD1-IN-39 (Compound 14) is a reversible inhibitor for LSD1 with an IC50 of 0.18 μM. LSD1-IN-39 exhibits broad-spectrum anti-proliferative activity against cancer cells, inhibits the cell migration of HepG2 and inhibits the epithelial-mesenchymal transition. LSD1-IN-39 exhibits antitumor activity in mouse models .
|
-
- HY-145828
-
|
|
Microtubule/Tubulin
Ferroptosis
|
Cancer
|
|
Microtubule inhibitor 2 is a potent and selective, orally active microtubule inhibitor. Microtubule inhibitor 2 triggers cell death through ferroptosis . Microtubule inhibitor 2 shows antitumor activity .
|
-
- HY-165245
-
|
|
Transmembrane Glycoprotein
|
Cancer
|
|
SBI-183 is an orally active inhibitor of QSOX1 (Kd: 20 μM). SBI-183 suppresses the proliferative and invasive phenotype of renal cancer cell lines, including triple negative breast cancer cell line, lung adenocarcinoma cell line and pancreatic ductal adenocarcinoma. SBI-183 inhibits tumor growth in two human xenograft mouse models of renal cell carcinoma in vivo .
|
-
- HY-151606
-
|
|
Akt
|
Cancer
|
|
Akt3 degrader 1 (compound 12l) is a selective Akt3 degrader that overcomes Osimertinib (HY-15772)-induced resistance in H1975OR NSCLC cells. Akt3 degrader 1 also has anti-proliferative activity and significantly inhibits tumour growth in mice. Akt3 degrader 1 can be used in the study of drug-resistant non-small cell lung cancer .
|
-
- HY-161966
-
|
|
Apoptosis
Reactive Oxygen Species
VEGFR
|
Cancer
|
|
VEGFR-2-IN-52 (compound 14d) is a potent VEGFR-2 inhibitor with an IC50 value of 191.1 nM. VEGFR-2-IN-52 decreases the protein expression of p-VEGFR-2, MMP9, p-ERK1/2 and p-MEK1. VEGFR-2-IN-52 shows cytotoxicity. VEGFR-2-IN-52 induces apoptosis and cell cycle arrest at G0/G1 phase. VEGFR-2-IN-52 increases the levels of ROS .
|
-
- HY-B1357
-
-
- HY-143241
-
|
|
HDAC
MDM-2/p53
Apoptosis
|
Cancer
|
|
HDAC-IN-34 (compound 27) is a potent HDAC inhibitor, with IC50 values of 0.022 and 0.45 μM for HDAC1 and HDAC6, respectively. HDAC-IN-34 can bind to DNA and cause DNA damage. HDAC-IN-34 causes cells apoptosis through p53 signaling pathway. HDAC-IN-34 exhibits significant anti-proliferation effect against HCT-116 cells, with an IC50 of 1.41 μM .
|
-
- HY-122181A
-
|
|
Histone Methyltransferase
|
Cancer
|
|
OTS186935 trihydrochloride is a protein methyltransferase SUV39H2 inhibitor with an IC50 of 6.49 nM. OTS186935 trihydrochloride shows significant inhibition of tumor growth in mouse xenograft models without any detectable toxicity. OTS186935 trihydrochloride regulates the production of γ-H2AX in cancer cells .
|
-
- HY-N1930
-
|
Hinesol
|
Apoptosis
|
Cancer
|
|
(-)-Hinesol (Hinesol) is a potent anticancer agent. (-)-Hinesol induces apoptosis and cell cycle arrest at G0/G1 phase. (-)-Hinesol downregulates MEK/ERK pathway and NF-κB pathway and mediates theexpression of cyclin D1, Bax and Bcl-2. (-)-Hinesol has the potential for the research of non–small cell lung cancer .
|
-
- HY-122181B
-
|
|
Histone Methyltransferase
|
Cancer
|
|
OTS186935 hydrochloride is a potent protein methyltransferase SUV39H2 inhibitor with an IC50 of 6.49 nM. OTS186935 hydrochloride shows significant inhibition of tumor growth in mouse xenograft models without any detectable toxicity. OTS193320 hydrochloride regulates the production of γ-H2AX in cancer cells .
|
-
- HY-B0712A
-
|
Ro 13-9904 sodium hydrate
|
Bacterial
Antibiotic
GSK-3
Aurora Kinase
|
Infection
Cancer
|
|
Ceftriaxone sodium hydrate (Ro 13-9904 sodium hydrate) is a broad spectrum β-lactam third-generation cephalosporin antibiotic, which has good antibacterial activity against a variety of gram-negative and positive bacteria. Ceftriaxone sodium hydrate is a covalent inhibitor of GSK3β with IC50 value of 0.78 μM. Ceftriaxone sodium hydrate is an inhibitor of Aurora B. Ceftriaxone sodium hydrate has anti-inflammatory, antitumor and antioxidant activities. Ceftriaxone sodium hydrate can be used in the study of bacterial infections and meningitis .
|
-
- HY-168477
-
|
|
HDAC
Autophagy
|
Cancer
|
|
HDAC1-IN-8 (compound 5c) is a potent and selective HDAC1 inhibitor with IC50 values of 11.94, 22.95, >500 µM for HDAC1, HDAC6, HDAC8, respectively. HDAC1-IN-8 shows antiproliferative activity. HDAC1-IN-8 induces cell cycle arrest at G1 and G2/M. HDAC1-IN-8 induces autophagy. HDAC1-IN-8 shows anticancer activity and has the potential for the research of lung cancer .
|
-
- HY-N2278
-
|
Leachianone E
|
Tyrosinase
Glycosidase
|
Cancer
|
|
Kushenol A (Leachianone E) is isolated from the root of Sophora flavescent. Kushenol A is a non-competitive tyrosinase inhibitor to block the conversion of L-tyrosine to L-DOPA, shows IC50 and Kivalues of 1.1 μM and 0.4 μM, respectively . Kushenol A is a flavonoid antioxidant, has inhibitory effects on alpha-glucosidase (IC50: 45 μM; Ki: 6.8 μM) and β-amylase . Kushenol A is confirmed as potential inhibitors of enzymes targeted by cosmetics for skin whitening and aging .
|
-
- HY-151429
-
|
|
Apoptosis
Ferroptosis
Bcl-2 Family
COX
|
Cancer
|
|
Antitumor agent-77 is an antitumor agent, inhibits cancer cells growth and migration. Antitumor agent-77 triggers ferroptosis by inhibiting GPx-4 and elevating COX2. Antitumor agent-77 also activates intrinsic apoptotic pathway (Bax-Bcl-2-caspase-3) and hinders Epithelial-mesenchymal transition (EMT) process of cancer cells .
|
-
- HY-116749
-
|
BBSKE
|
TrxR
|
Cancer
|
|
Ethaselen (BBSKE) is an orally active, selective thioredoxin reductase (TrxR) inhibitor with IC50s of 0.5 and 0.35 μM for the wild-type human TrxR1 and rat TrxR1, respectively. Ethaselen specifically binds to the unique selenocysteine-cysteine redox pair in the C-terminal active site of mammalian TrxR1. Ethaselen, an organoselenium compound, is a potent antitumor candidate that exerts potent inhibition on non-small cell lung cancer (NSCLC) by targeting TrxR .
|
-
- HY-N2802
-
|
9-Oxo-10,11-dehydroageraphorone
|
Apoptosis
Caspase
Parasite
|
Infection
Cancer
|
|
Euptox A (9-Oxo-10, 11-dehydroageraphorone), a cadenine sesquiterpene, is the main toxin that can be isolated from Eupatorium adenophorum. Euptox A induces apoptosis by improving the gene expression level of apoptotic proteases such as caspase-10 in HeLa cells .
|
-
- HY-151428
-
|
|
Ferroptosis
Apoptosis
Bcl-2 Family
COX
|
Cancer
|
|
Antitumor agent-78 is an antitumor agent, inhibits cancer cells growth and migration. Antitumor agent-78 triggers ferroptosis by inhibiting GPx-4 and elevating COX2. Antitumor agent-78 also activates intrinsic apoptotic pathway (Bax-Bcl-2-caspase-3) and hinders Epithelial-mesenchymal transition (EMT) process of cancer cells .
|
-
- HY-143435
-
|
|
Apoptosis
|
Cancer
|
|
AG6033 is a potential novel CRBN modulator. AG6033 suppresses various tumor cells by modulating the interactions between CRBN and various antitumor target proteins. AG6033 can cause GSPT1 and IKZF1 degradation. AG6033 induces CRBN-dependent cytotoxic effect .
|
-
- HY-B0712AR
-
|
|
Bacterial
Antibiotic
GSK-3
Aurora Kinase
|
Infection
Cancer
|
|
Ceftriaxone (sodium hydrate) (Standard) is the analytical standard of Ceftriaxone (sodium hydrate). This product is intended for research and analytical applications. Ceftriaxone sodium hydrate (Ro 13-9904 sodium hydrate) is a broad spectrum β-lactam third-generation cephalosporin antibiotic, which has good antibacterial activity against a variety of gram-negative and positive bacteria. Ceftriaxone sodium hydrate is a covalent inhibitor of GSK3β with IC50 value of 0.78 μM. Ceftriaxone sodium hydrate is an inhibitor of Aurora B. Ceftriaxone sodium hydrate has anti-inflammatory, antitumor and antioxidant activities. Ceftriaxone sodium hydrate can be used in the study of bacterial infections and meningitis .
|
-
- HY-10824
-
|
PT523
|
Antifolate
Dihydrofolate reductase (DHFR)
|
Cancer
|
|
Talotrexin (PT523), an analog of Aminopterin (HY-14518), is a nonpolyglutamatable classic antifolate. Talotrexin is a RFC (reduced folate carrier) specific inhibitor and selectively inhibits RFC transport. Talotrexin shows antitumor activity by targeting DHFR to inhibit tumor growth .
|
-
- HY-12300A
-
|
CFI-400945 hydrochloride
|
Polo-like Kinase (PLK)
Apoptosis
|
Cancer
|
|
Ocifisertib hydrochloride (CFI-400945 hydrochloride) is the hydrochloride salt form of Ocifisertib (HY-12300). Ocifisertib hydrochloride is an orally active PLK4 inhibitor with a Ki and an IC50 of 0.26 nM and 2.8 nM. Ocifisertib hydrochloride inhibits growth of various cancer cells, arrests cell cycles at G2/M phase, and induces apoptosis. Ocifisertib hydrochloride exhibits antitumor efficacy in mouse model .
|
-
- HY-B0712
-
|
Ro 13-9904 free acid
|
Bacterial
Antibiotic
GSK-3
Aurora Kinase
|
Infection
Inflammation/Immunology
Cancer
|
|
Ceftriaxone (Ro 13-9904 free acid) is a broad spectrum β-lactam third-generation cephalosporin antibiotic, which has good antibacterial activity against a variety of gram-negative and positive bacteria. Ceftriaxone is a covalent inhibitor of GSK3β with IC50 value of 0.78 μM. Ceftriaxone is an inhibitor of Aurora B. Ceftriaxone has anti-inflammatory, antitumor and antioxidant activities. Ceftriaxone can be used in the study of bacterial infections and meningitis .
|
-
- HY-N3737
-
|
|
Aurora Kinase
PERK
Reactive Oxygen Species
|
Cancer
|
|
Derrone, a prenylated isoflavones, is an Aurora kinase inhibitor, with IC50 values of 6 and 22.3 μM against Aurora B and Aurora A, respectively. Derrone shows anti-tumor activity .
|
-
- HY-B0712S1
-
|
Ro 13-9904-13C2,d3 triethylammonium salt
|
Antibiotic
Aurora Kinase
GSK-3
Bacterial
Isotope-Labeled Compounds
|
Infection
Inflammation/Immunology
Cancer
|
|
Ceftriaxone- 13C2,d3 triethylammonium salt is 13C and deuterated labeled Ceftriaxone (HY-B0712). Ceftriaxone (Ro 13-9904 free acid) is a broad spectrum β-lactam third-generation cephalosporin antibiotic, which has good antibacterial activity against a variety of gram-negative and positive bacteria. Ceftriaxone is a covalent inhibitor of GSK3β with IC50 value of 0.78 mM. Ceftriaxone is an inhibitor of Aurora B. Ceftriaxone has anti-inflammatory, antitumor and antioxidant activities. Ceftriaxone can be used in the study of bacterial infections and meningitis .
|
-
- HY-149086
-
|
|
RAR/RXR
Apoptosis
PARP
Bcl-2 Family
|
Cancer
|
|
BPA-B9 is a RXRα ligand and antagonist targeting the pRXRα-PLK1 interaction. BPA-B9 has excellent RXRα-binding affinity (KD=39.29 ± 1.12 nM). BPA-B9 inhibits the proliferation of cancer cells by inducing mitotic arrest and cell apoptosis .
|
-
- HY-151446
-
|
|
DNA Methyltransferase
Virus Protease
Flavivirus
|
Infection
|
|
ZIKV-IN-3 (compound 5a), an andrographolide derivatives, is a potent ZIKV NS5 methyl transferase (MTase) inhibitor with an IC50 value of 18.34 μM. ZIKV-IN-3 inhibits ZIKV replication and infection. ZIKV-IN-3 can be used in research of Zika virus (ZIKV) .
|
-
- HY-173145
-
|
|
Aminopeptidase
|
Cancer
|
|
CD13-IN-1 (Compound 5f) is a CD13 inhibitor with an IC50 of 1.71 μM. CD13-IN-1 can inhibit the proliferation of multiple tumor cells and has anti-tumor activity .
|
-
- HY-146999
-
|
|
Histone Methyltransferase
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
|
YM458 is a potent EZH2 and BRD4 dual inhibitor with IC50s of 490 nM and 34 nM, respectively. YM458 inhibits cell proliferation and colony formation and induces cell cycle arrest and apoptosis in solid cancer cells. YM458 can be used for researching anticancer .
|
-
- HY-128222
-
|
Hydrazinecarboselenoamide
|
Bacterial
|
Infection
Cancer
|
|
Selenosemicarbazide (Hydrazinecarboselenoamide) exhibits antimicrobial activity, that inhibits B. subtilis, S. aureus, Klebsiella pneumoniae, Sarcina lutea and Mycobacterium tuberculosis. Selenosemicarbazide forms complex with metal ions, and exhibits antitumor efficacy against cancer cells
|
-
- HY-145857
-
|
|
HSP
Apoptosis
|
Cancer
|
|
GRP78-IN-1 exhibits several interactions with GRP78 residues with binding energy of -8.07 kcal/mol. GRP78-IN-1 shows the potent cytotoxic, anti-proliferative in cancer cells. GRP78-IN-1 exhibits promising apoptosis in breast cancer cells and wound healing properties .
|
-
- HY-168497
-
|
|
Histone Methyltransferase
|
Cancer
|
|
C-MS023 is a photo-activatable MS023 (HY-19615) prodrug, achieving spatiotemporal inhibition of Histone Arginine Asymmetric Dimethylation. C-MS023 inhibits PRMT6 mediated asymmetric dimethylation of H3 arginine 2 (H3R2me2a), with an estimate IC50 of 0.2224 μM. The photolysis of C-MS023 could be triggered by visible light irradiation at 420 nm, thereby liberating MS023 for effective downregulation of histone arginine asymmetric dimethylation and DNA replication-related transcriptomic activities .
|
-
- HY-151883
-
|
|
Apoptosis
MDM-2/p53
|
Cancer
|
|
APE1-IN-2 (compound AP1) is a Pt(IV) proagent, targeting a critical BER protein, apurinic/apyrimidinic endonuclease 1 (APE1). APE1-IN-2 shows anticancer activity. APE1-IN-2 induces intracellular accumulation of platinum and activates DNA damage response and apoptosis signals .
|
-
- HY-122181
-
|
|
Histone Methyltransferase
|
Cancer
|
|
OTS186935 is a potent protein methyltransferase SUV39H2 inhibitor with an IC50 of 6.49 nM. OTS186935 shows significant inhibition of tumor growth in mouse xenograft models without any detectable toxicity. OTS193320 regulates the production of γ-H2AX in cancer cells .
|
-
- HY-B0712R
-
-
- HY-10824A
-
|
PT523 monoammonium
|
Dihydrofolate reductase (DHFR)
Antifolate
|
Cancer
|
|
Talotrexin monoammonium is the monoammonium salt form of Talotrexin (HY-10824). Talotrexin monoammonium is an analog of Aminopterin (HY-14518), and is a nonpolyglutamatable classic antifolate. Talotrexin monoammonium is a reduced folate carrier (RFC) specific inhibitor and selectively inhibits RFC transport. Talotrexin monoammonium shows antitumor activity by targeting DHFR to inhibit tumor growth .
|
-
- HY-107909
-
|
1,3-Dimethylxanthine sodium glycinate; Theo-24 sodium glycinate
|
Adenosine Receptor
HDAC
Apoptosis
Interleukin Related
TNF Receptor
|
Cancer
|
|
Theophylline (1,3-Dimethylxanthine) sodium glycinate is a potent phosphodiesterase (PDE) inhibitor, adenosine receptor antagonist, and histone deacetylase (HDAC) activator. Theophylline sodium glycinate inhibits PDE3 activity to relax airway smooth muscle. Theophylline sodium glycinate has anti-inflammatory activity by increase IL-10 and inhibit NF-κB into the nucleus. Theophylline sodium glycinate induces apoptosis. Theophylline sodium glycinate can be used for asthma and chronic obstructive pulmonary disease (COPD) research .
|
-
- HY-B0809S1
-
|
1,3-Dimethylxanthine-d3; Theo-24-d3
|
Endogenous Metabolite
Adenosine Receptor
HDAC
TNF Receptor
Interleukin Related
Phosphodiesterase (PDE)
Apoptosis
Isotope-Labeled Compounds
|
Cancer
|
|
Theophylline-d3 is deuterated labeled Theophylline (HY-B0809). Theophylline (1,3-Dimethylxanthine) is a potent phosphodiesterase (PDE) inhibitor, adenosine receptor antagonist, and histone deacetylase (HDAC) activator. Theophylline (1,3-Dimethylxanthine) inhibits PDE3 activity to relax airway smooth muscle. Theophylline (1,3-Dimethylxanthine) has anti-inflammatory activity by increase IL-10 and inhibit NF-κB into the nucleus. Theophylline (1,3-Dimethylxanthine) induces apoptosis. Theophylline (1,3-Dimethylxanthine) can be used for asthma and chronic obstructive pulmonary disease (COPD) research .
|
-
- HY-149263
-
|
|
Influenza Virus
Virus Protease
|
Infection
|
|
HAA-09 is an orally active and potent anti-influenza agent, targeting the influenza PB2_cap binding domain. HAA-09 displays potent anti-influenza A virus activity, with an EC50 of 0.03 μM. HAA-09 shows polymerase inhibition, with an IC50 of 0.06±0.004 μM. HAA-09 blocks virus replication without causing obvious cytotoxicity .
|
-
- HY-169938
-
|
|
HDAC
Histone Demethylase
Apoptosis
|
Cancer
|
|
LSD1/HDAC-IN-2 (Compound 20c) is the inhibitor for LSD and HDAC, that inhibits LSD1, HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8, with IC50s of 39.0, 1.4, 1.0, 1.3, 2.9 and 16.0 nM, respectively. LSD1/HDAC-IN-2 inhibits the proliferation of cancer cells, especially the colorectal cancer cells. LSD1/HDAC-IN-2 arrests the cell cycle at G2/M phase, inhibits cell migration, and induces apoptosis in HCT-116 and HT-29 cells. LSD1/HDAC-IN-2 exhibits antitumor efficacy in mouse model without significant toxicity .
|
-
- HY-117235
-
-
- HY-161470
-
|
|
Histone Demethylase
E1/E2/E3 Enzyme
DNA/RNA Synthesis
Caspase
Apoptosis
|
Cancer
|
|
WS-384 is a dual LSD1 and DCN1-UBC12 protein-protein interaction inhibitor with oral activity, with IC50 values of 338.79 nM and 14.81 nM, respectively. WS-384 possesses anticancer activity and can cause cell cycle arrest, DNA damage, and induce apoptosis. WS-384 can be used in the research of non-small cell lung cancer (NSCLC) .
|
-
- HY-B0712B
-
|
Ro 13-9904
|
Antibiotic
GSK-3
Bacterial
Aurora Kinase
|
Infection
Inflammation/Immunology
Cancer
|
|
Ceftriaxone sodium salt (Ro 13-9904) is a broad spectrum β-lactam third-generation cephalosporin antibiotic, which has good antibacterial activity against a variety of gram-negative and positive bacteria. Ceftriaxone sodium salt is a covalent inhibitor of GSK3β with IC50 value of 0.78 μM. Ceftriaxone sodium salt is an inhibitor of Aurora B. Ceftriaxone sodium salt has anti-inflammatory, antitumor and antioxidant activities. Ceftriaxone sodium salt can be used in the study of bacterial infections and meningitis .
|
-
- HY-107801R
-
|
|
Interleukin Related
HSV
HIV
HPV
|
Infection
Inflammation/Immunology
|
|
Inosine pranobex (Standard) is the analytical standard of Inosine pranobex. This product is intended for research and analytical applications. Inosine pranobex is an orally active immunomodulator. Inosine pranobex has broad-spectrum antiviral activity. Inosine pranobex inhibits human immunodeficiency virus (HIV), herpes simplex virus (HSV), vaccinia virus (VACV), human tumor virus (HPV), Cytomegalovirus, influenza virus (INFV), parainfluenza virus (PIV), and Epstein-Barr virus .
|
-
- HY-B0809A
-
|
1,3-Dimethylxanthine monohydrate; Theo-24 monohydrate
|
Phosphodiesterase (PDE)
Adenosine Receptor
HDAC
Apoptosis
Interleukin Related
TNF Receptor
Endogenous Metabolite
|
Cancer
|
|
Theophylline (1,3-Dimethylxanthine) monohydrate is a potent phosphodiesterase (PDE) inhibitor, adenosine receptor antagonist, and histone deacetylase (HDAC) activator. Theophylline (1,3-Dimethylxanthine) monohydrate inhibits PDE3 activity to relax airway smooth muscle. Theophylline (1,3-Dimethylxanthine) monohydrate has anti-inflammatory activity by increase IL-10 and inhibit NF-κB into the nucleus. Theophylline (1,3-Dimethylxanthine) monohydrate induces apoptosis. Theophylline (1,3-Dimethylxanthine) monohydrate can be used for asthma and chronic obstructive pulmonary disease (COPD) research .
|
-
- HY-D1726
-
|
|
Deubiquitinase
|
Cancer
|
|
8RK59, a Bodipy probe, is a potent UCHL1 (ubiquitin C-terminal hydrolase L1) inhibitor, with an IC50 close to 1 μM. 8RK59 could penetrate and label living cells. BodipyFL-alkyne is coupled to the azide of 8RK64 (HY-148254) using copper(I)-mediated click chemistry, resulting in compound 8RK59 .
|
-
- HY-B0809
-
|
1,3-Dimethylxanthine; Theo-24
|
Phosphodiesterase (PDE)
Adenosine Receptor
HDAC
Apoptosis
Interleukin Related
TNF Receptor
Endogenous Metabolite
|
Cancer
|
|
Theophylline (1,3-Dimethylxanthine) is a potent phosphodiesterase (PDE) inhibitor, adenosine receptor antagonist, and histone deacetylase (HDAC) activator. Theophylline (1,3-Dimethylxanthine) inhibits PDE3 activity to relax airway smooth muscle. Theophylline (1,3-Dimethylxanthine) has anti-inflammatory activity by increase IL-10 and inhibit NF-κB into the nucleus. Theophylline (1,3-Dimethylxanthine) induces apoptosis. Theophylline (1,3-Dimethylxanthine) can be used for asthma and chronic obstructive pulmonary disease (COPD) research .
|
-
- HY-122882
-
|
|
E1/E2/E3 Enzyme
|
Inflammation/Immunology
|
|
HOIPIN-8 is a potent inhibitor of linear ubiquitin chain assembly complex (LUBAC) with an IC50 of 11 nM. HOIPIN-8 is a HOIPIN-1 derivative with enhanced the potency by 255-fold in the petit-LUBAC inhibition, and 10-fold and 4-fold in the LUBAC- and TNF-α-mediated NF-κB activation, respectively than HOIPIN-1. HOIPIN-1 is a promising tool to explore the cellular functions of LUBAC .
|
-
- HY-107801
-
|
Imunovir; Delimmun; Groprinosin
|
Interleukin Related
HSV
HIV
HPV
|
Infection
Inflammation/Immunology
|
|
Inosine pranobex is an orally active immunomodulator. Inosine pranobex has broad-spectrum antiviral activity. Inosine pranobex inhibits human immunodeficiency virus (HIV), herpes simplex virus (HSV), vaccinia virus (VACV), human tumor virus (HPV), Cytomegalovirus, influenza virus (INFV), parainfluenza virus (PIV), and Epstein-Barr virus
.
|
-
- HY-B0809B
-
|
1,3-Dimethylxanthine sodium acetate; Theo-24 sodium acetate
|
Endogenous Metabolite
Phosphodiesterase (PDE)
Adenosine Receptor
HDAC
Apoptosis
Interleukin Related
TNF Receptor
|
Cancer
|
|
Theophylline (1,3-Dimethylxanthine) sodium acetate is a potent phosphodiesterase (PDE) inhibitor, adenosine receptor antagonist, and histone deacetylase (HDAC) activator. Theophylline (1,3-Dimethylxanthine) sodium acetate inhibits PDE3 activity to relax airway smooth muscle. Theophylline (1,3-Dimethylxanthine) sodium acetate has anti-inflammatory activity by increase IL-10 and inhibit NF-κB into the nucleus. Theophylline (1,3-Dimethylxanthine) sodium acetate induces apoptosis. Theophylline (1,3-Dimethylxanthine) sodium acetate can be used for asthma and chronic obstructive pulmonary disease (COPD) research .
|
-
- HY-170430
-
|
|
Molecular Glues
E1/E2/E3 Enzyme
|
Cancer
|
|
HGC652 is the molecular glue, that targets E3 ubiquitin ligase TRIM21, promotes the formation of a ternary complex between TRIM21 and NUP98, induces degradation of NUP155 and nuclear pore complex proteins, thereby causing the cell death. HGC652 inhibits the proliferation of multi cancer cells, according to the expression level of TRIM21 .
|
-
- HY-117235R
-
-
- HY-173133
-
|
|
Autophagy
Atg7
|
Cancer
|
|
Antitumor agent-199 (Compound 4b) is an antitumor agent. Antitumor agent-199 exhibits significant antiproliferative activity against multiple tumor cell lines. Antitumor agent-199 can induce autophagy in cancer cells via the ATG5/ATG7 pathway and can be used in the study of cancer .
|
-
- HY-18976
-
-
- HY-N3980R
-
|
|
Autophagy
RAD51
|
Infection
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Guaiol (Standard) is the analytical standard of Guaiol. This product is intended for research and analytical applications. Guaiol is a sesquiterpenoid alcohol with oral activity found in various traditional Chinese medicines, exhibiting biological activities such as anti-proliferative, autophagy-promoting, insecticidal, anti-anxiety, anti-inflammatory, diuretic, and blood pressure-lowering effects. Guaiol induces apoptosis in non-small cell lung cancer cells by regulating the stability of RAD51 through autophagy modulation. Guaiol can also act directly on parasites, inhibiting their growth by affecting the kinetoplast, mitochondrial matrix and plasma membrane of the promastigotes. Guaiol kills amastigotes at an IC50 of 0.01 µg/mL. Guaiol can be used in research related to cancer, infections, cardiovascular diseases, and inflammatory conditions [4]
|
-
- HY-N8884
-
|
|
PTEN
Akt
NF-κB
Interleukin Related
TNF Receptor
|
Inflammation/Immunology
|
|
Coelonin is a dihydrophenanthrene with anti-inflammation activity. Coelonin inhibits LPS-induced PTEN phosphorylation. Coelonin inhibits NF-κB activation and p27Kip1 degradation by regulating the PI3K/AKT pathway negatively. Coelonin can inhibit IκBα phosphorylation and degradation and increases the expression of IκBα protein .
|
-
- HY-Y0152R
-
|
|
Apoptosis
Parasite
Autophagy
Caspase
Calcium Channel
|
Others
Inflammation/Immunology
Cancer
|
|
Cinchonine (Standard) is the analytical standard of Cinchonine. This product is intended for research and analytical applications. Cinchonine is a natural compound present in Cinchona bark with antimalarial, antitumor, anti-inflammatory, anti platelet-aggregation and anti-obesity properties. Cinchonine inhibits cells proliferation and autophagy and induces apoptosis through activation of Caspase-3. Cinchonine activates endoplasmic reticulum stress-induced apoptosis in human liver cancer cells .
|
-
- HY-N10447
-
|
|
Apoptosis
|
Cancer
|
|
Kurzipene D (compound 4) is a potent anticancer agent. Kurzipene D induces the apoptosis and arrested the HepG2 cell cycle at S stage. Kurzipene D shows anti-tumor effects using in vivo zebrafish model. Kurzipene D has the property of inhibiting tumor proliferation and migration .
|
-
- HY-N3980
-
|
Champacol; Guaiac alcohol
|
Autophagy
RAD51
|
Infection
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Guaiol is a sesquiterpenoid alcohol with oral activity found in various traditional Chinese medicines, exhibiting biological activities such as anti-proliferative, autophagy-promoting, insecticidal, anti-anxiety, anti-inflammatory, diuretic, and blood pressure-lowering effects. Guaiol induces apoptosis in non-small cell lung cancer cells by regulating the stability of RAD51 through autophagy modulation. Guaiol can also act directly on parasites, inhibiting their growth by affecting the kinetoplast, mitochondrial matrix and plasma membrane of the promastigotes. Guaiol kills amastigotes at an IC50 of 0.01 µg/mL. Guaiol can be used in research related to cancer, infections, cardiovascular diseases, and inflammatory conditions [4]
|
-
- HY-170954
-
|
|
Apoptosis
c-Met/HGFR
TAM Receptor
|
Cancer
|
|
C-Met/Axl-IN-1 (Compound 22a) is an orally active and selective type II c-Met/Axl inhibitor with IC50 values of 1 nM and 10 nM, respectively. C-Met/Axl-IN-1 can inhibit proliferation, induce cell cycle arrest and apoptosis of tumor cells. C-Met/Axl-IN-1 has strong anti-tumor activity .
|
-
- HY-N0451
-
|
5,7-Dihydroxy-4'-methoxyflavone
|
Apoptosis
Autophagy
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Acacetin (5,7-Dihydroxy-4'-methoxyflavone) is an orally active flavonoid derived from Dendranthema morifolium. Acacetin docks in the ATP binding pocket of PI3Kγ. Acacetin causes cell cycle arrest and induces apoptosis and autophagy in cancer cells. Acacetin has potent anti-cancer and anti-inflammatory activity and has the potential for pain-related diseases research .
|
-
- HY-146957
-
|
|
Virus Protease
Flavivirus
|
Cancer
|
|
ZIKV-IN-1 is a potent zika virus inhibitor with an EC50 of 2.8 μM and EC90 of 6.8 μM. ZIKV-IN-1 shows anti-ZIKV activity with low cytotoxicity. ZIKV-IN-1 shows a strong affinity to ZIKV RdRp domain . ZIKV-IN-1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-151971
-
|
|
Aurora Kinase
Polo-like Kinase (PLK)
|
Cancer
|
|
Aurora kinase-IN-3 (Compound 15a) is an orally active AURKB inhibitor that elicits an AURKB-suppressive activity by disrupting the mitotic localization of AURKB, rather than inhibiting its phosphorylation of H3 at Ser10 .
|
-
- HY-124284
-
-
- HY-168953
-
|
|
P-glycoprotein
Apoptosis
Bcl-2 Family
Reactive Oxygen Species
Caspase
|
Cancer
|
|
Lysosomal P-gp targeted agent 1 (Compound 14) is an anti-tumor agent targeting lysosomal P-glycoprotein (Pgp). Lysosomal P-gp targeted agent 1 is selectively transported into lysosomes by overexpressed Pgp, release nitric oxide (NO) to generate reactive oxygen species (ROS), resulting in lysosomal membrane permeabilization (LMP) and inducing apoptosis. Lysosomal P-gp targeted agent 1 can overcome P-glycoprotein-mediated drug resistance and lead to cell cycle arrest, but relatively low toxicity to normal cells. Lysosomal P-gp targeted agent 1 has antitumor activity, significantly inhibits tumor volume .
|
-
- HY-162360
-
|
|
Apoptosis
EGFR
Caspase
Bcl-2 Family
|
Cancer
|
|
EGFR-IN-109 (compound 4) is an EGFR inhibitor, with the IC50 values of 25.8 and 182.3 nM for EGFR WT and EGFR T790M, respectively. EGFR-IN-109 arrests the cancer cells’ growth at the G2/M phase and induces both early and late apoptosis. EGFR-IN-109 can be used in cancer research .
|
-
- HY-136057
-
|
|
Ferroptosis
|
Cancer
|
|
iFSP1 is a potent, selective and glutathione-independent inhibitor of ferroptosis suppressor protein 1 (FSP1) (AIFM2) with an EC50 of 103 nM. iFSP1 selectively induces ferroptosis in GPX4-knockout cells which overexpressed FSP1. iFSP1 is able to sensitize a variety of human cancer cell lines to the ferroptosis inducer, such as (1S,3R)-RSL3 (HY-100218A) .
|
-
- HY-Y0152
-
|
(8R,9S)-Cinchonine; LA40221
|
Apoptosis
Parasite
Autophagy
Caspase
Calcium Channel
|
Others
Inflammation/Immunology
Cancer
|
|
Cinchonine is a natural compound present in Cinchona bark with antimalarial, antitumor, anti-inflammatory, anti platelet-aggregation and anti-obesity properties. Cinchonine inhibits cells proliferation and autophagy and induces apoptosis through activation of Caspase-3. Cinchonine activates endoplasmic reticulum stress-induced apoptosis in human liver cancer cells .
|
-
- HY-168565
-
|
|
Apoptosis
Microtubule/Tubulin
Reactive Oxygen Species
|
Cancer
|
|
Tubulin polymerization-IN-70 (compound Q19) is a potent tubulin polymerization inhibitor. Tubulin polymerization-IN-70 shows antiproliferative activity. Tubulin polymerization-IN-70 target the colchicine binding site of tubulin and inhibited tubulin polymerization. Tubulin polymerization-IN-70 induces apoptosis and cell cycle arrest at G2/M phase. Tubulin polymerization-IN-70 induces mitochondrial membrane potential decrease and increases the levels of reactive oxygen species (ROS). Tubulin polymerization-IN-70 shows antiangiogenic and anticancer activity .
|
-
- HY-148098
-
|
|
Ras
|
Cancer
|
|
Pan KRas-IN-1 is a pan KRas inhibitor, can be used for agent resistance in cancer developed with KRas G12C inhibitors .
|
-
- HY-N2534R
-
|
|
AMPK
Apoptosis
Cytochrome P450
Phosphatase
NF-κB
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Endocrinology
Cancer
|
|
Karanjin (Standard) is the analytical standard of Karanjin. This product is intended for research and analytical applications. Karanjin is an orally active furanoflavonoid which can be isolated from several Leguminosae. Karanjin exhibits evident anti-diabetic, anti-cancer, anti-inflammatory, antioxidant, anticolitis, anti-ulcer, anti-Alzheimer properties and multiple insect repellent/insecticidal, acaricide properties, suggesting the potential of Karanjin to be applied to relevant research .
|
-
- HY-112764
-
|
|
Liposome
|
Metabolic Disease
|
|
DMG-PEG 2000 is used?for the preparation of liposome for siRNA delivery with improved transfection efficiency in vitro. DMG-PEG 2000 is also used for the?lipid nanoparticle for an oral plasmid DNA delivery approach in vivo through a facile surface modification to improve the mucus permeability and delivery efficiency of the nanoparticles .
|
-
- HY-113825
-
|
|
CDK
|
Cancer
|
|
CLK1/2-IN-2 is CLK1 and CLK2 inhibitor with IC50 values of 16 nM and 45 nM, respectively. CLK1/2-IN-2 exhibits potent anti-cancer activities [1] .
|
-
- HY-112764A
-
|
|
Liposome
|
Metabolic Disease
|
|
DMG-PEG Excipient is used?for the preparation of liposome for siRNA delivery with improved transfection efficiency in vitro. DMG-PEG Excipient is also used for the?lipid nanoparticle for an oral plasmid DNA delivery approach in vivo through a facile surface modification to improve the mucus permeability and delivery efficiency of the nanoparticles .
|
-
- HY-N0164R
-
|
|
PINK1/Parkin
Opioid Receptor
Autophagy
Mitophagy
Ferroptosis
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Matrine (Standard) is the analytical standard of Matrine. This product is intended for research and analytical applications. Matrine (Matridin-15-one) is an alkaloid found in plants from the Sophora genus that can act as a kappa opioid receptor and u-receptor agonist. Matrine has a variety of pharmacological effects, including anti-cancer, anti-oxidative stress, anti-inflammation and anti-apoptosis effects. Matrine is potential in the research of disease like human non-small cell lung cancer, hepatoma, papillary thyroid cancer and acute kidney injury (AKI) .
|
-
- HY-124896
-
|
6-Geranylnaringenin; Mimulone
|
Phosphatase
Apoptosis
Autophagy
|
Inflammation/Immunology
Cancer
|
|
Bonannione A (6-Geranylnaringenin; Mimulone), a prenylflavonoid, is an orally active and potent protein tyrosine phosphatase 1B (PTP1B) inhibitor with an IC50 of 14 µM. Bonannione A triggers caspase-dependent apoptosis. Bonannione A induces autophagy through p53-mediated AMPK/mTOR pathway. Bonannione A shows anti-inflammatory, antiradical and anti-cancer activity .
|
-
- HY-113670
-
|
|
CDK
|
Cancer
|
|
CLK1/2-IN-2 is CLK1 and CLK2 inhibitor with IC50 values of 1.1 nM and 2.4 nM, respectively. CLK1/2-IN-2 exhibits potent anti-cancer activities [1] .
|
-
- HY-N2534
-
-
- HY-147803
-
|
|
Reactive Oxygen Species
|
Cancer
|
|
TrxR-IN-5 (compound 4f) is a potent TrxR (thioredoxin reductase) inhibitor, with an IC50 of 0.16 μM. TrxR-IN-5 increases the levels of ROS, thus leading to potent antiproliferative effects. TrxR-IN-5 exhibits prominent anticacer and anti-metastasis effects .
|
-
- HY-N0164
-
|
Matridin-15-one; Vegard; α-Matrine
|
PINK1/Parkin
Opioid Receptor
Autophagy
Mitophagy
Ferroptosis
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Matrine (Matridin-15-one) is an alkaloid found in plants from the Sophora genus that can act as a kappa opioid receptor and u-receptor agonist. Matrine has a variety of pharmacological effects, including anti-cancer, anti-oxidative stress, anti-inflammation and anti-apoptosis effects. Matrine is potential in the research of disease like human non-small cell lung cancer, hepatoma, papillary thyroid cancer and acute kidney injury (AKI) .
|
-
- HY-123611
-
|
RX-5902
|
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
Supinoxin (RX-5902) is an orally active inhibitor of phosphorylated-p68 RNA helicase (P-p68) and a potent first-in-class anti-cancer agent. Supinoxin interacts with Y593 phosphorylated-p68 and attenuates the nuclear shuttling of β-catenin. Supinoxin induces cell apoptosis and inhibits growth of TNBC cancer cell lines with IC50s ranging from 10 nM to 20 nM .
|
-
- HY-161644
-
|
|
STAT
Apoptosis
|
Cancer
|
|
STAT3-IN-27 (Compound 41) is an orally active inhibitor for phosphorylation of STAT3 (KD is 4.4 μM) and STAT3 transcription (IC50 is 22.57 nM). STAT3-IN-27 inhibits proliferation of various cancer cells with IC50 of 10-500 nM. STAT3-IN-27 arrests the cell cycle at G2/M phase, induces mitochondrial dysfunction and apoptosis in HCT116, inhibits cell migration of HCT116. STAT3-IN-27 exhibits antitumor efficacy in mouse model .
|
-
- HY-161857
-
|
|
Akt
mTOR
Caspase
CDK
|
Cancer
|
|
Akt/mTOR-IN-1 (Compound 8r) is an AKT/mTOR signaling pathway inhibitor exhibiting an IC50 value of 0.8 µM with anticancer activity. Akt/mTOR-IN-1 can decrease the expression of Caspase 3 and increase the expression of the autophagic protein Cyclin B1, thereby inducing cell autophagy and apoptosis. Akt/mTOR-IN-1 can be used in research related to non-small cell lung cancer (NSCLC) .
|
-
- HY-122872
-
|
|
p38 MAPK
|
Cancer
|
|
MKK7-COV-9 is a potent and selective covalent inhibitor of MKK7 and targets a specific protein–protein interaction of MKK7. MKK7-COV-9 blocks primary B cell activation in response to LPS with an EC50 of 4.98 μM .
|
-
- HY-14454
-
TPh A
2 Publications Verification
Triphenyl Compound A
|
Others
|
Cancer
|
|
TPh A (Triphenyl Compound A) is a potent inhibitor of the nuclear protein pirin and binds specifically to pirin with a Ki of 0.6 uM. TPh A disrupts the formation of the bcl3–pirin complex. TPh A can be used as a novel small molecule tool to regulate pirin in cells .
|
-
- HY-172255
-
|
|
PI4K
Apoptosis
Autophagy
PI3K
Akt
|
Cancer
|
|
PI4KIII beta inhibitor 4 (Compound 16) is a selective PI4KIIIβ inhibitor with an IC50 of 0.005 μM. PI4KIIIβ inhibitor 4 induces tumor cell apoptosis, cell cycle arrest, and autophagy by inhibiting the PI3K/AKT pathway. PI4KIIIβ inhibitor 4 can be used in the study of cancer .
|
-
- HY-132302A
-
|
|
Akt
PKA
PKC
ROCK
Ribosomal S6 Kinase (RSK)
SGK
|
Cancer
|
|
Hu7691 free base is an orally active, selective Akt inhibitor with IC50s of 4.0 nM, 97.5 nM, 28 nM for Akt1, Akt2 and Akt3, respectively. Hu7691 free base inhibits tumor growth and enables decrease of cutaneous toxicity in mice .
|
-
- HY-132302
-
|
|
Akt
PKA
PKC
ROCK
Ribosomal S6 Kinase (RSK)
SGK
|
Cancer
|
|
Hu7691 is an orally active, selective Akt inhibitor with IC50s of 4.0 nM, 97.5 nM, 28 nM for Akt1, Akt2 and Akt3, respectively. Hu7691 inhibits tumor growth and enables decrease of cutaneous toxicity in mice .
|
-
- HY-158058
-
|
|
Toll-like Receptor (TLR)
Pyroptosis
|
Inflammation/Immunology
Cancer
|
|
WYJ-2 is a selective agonist for toll-like receptor 2/1 (TLR2/1) with EC50 of 18.57 nM in human TLR2 and TLR1 transient-cotransfected HEK 293T cells. WYJ-2 induces pyroptosis and exhibits anticancer activity against non-small cell lung cancer (NSCLC) .
|
-
- HY-150753
-
-
- HY-122094
-
-
- HY-136241
-
|
|
NAMPT
Caspase
|
Cancer
|
|
OT-82 is a potent, selective and orally active inhibitor of NAMPT. OT-82 is selectively toxic to cells of hematopoietic origin and?induces cell death in a NAD + dependent manner. OT-82 is a promising antineoplastic agent for the study of hematological malignancies .
|
-
- HY-149486
-
|
|
FGFR
|
Cancer
|
|
FGFR1 inhibitor 7 (compound 5) is an inhibitor of FGFR1 Tyrosine Kinase with IC50 value of 0.33 nM. FGFR1 inhibitor 7 shows broad-spectrum cytotoxicity agasinst human cancer cell lines, and inhibits MOLT3 cells with IC50 of 2.1 μM .
|
-
- HY-W005379
-
|
|
TGF-beta/Smad
|
Inflammation/Immunology
|
|
DGM is an inhibitor of the TGF-β1/Smad signaling pathway with significant antifibrotic effects. DGM inhibits the epithelial-mesenchymal transition (EMT) process in alveolar epithelial cells and slows the progression of pulmonary fibrosis in vivo by reducing lung inflammation, improving lung function, and decreasing extracellular matrix (ECM) remodeling. DGM can be used in research on idiopathic pulmonary fibrosis (IPF) and EMT-related diseases .
|
-
- HY-12325
-
|
|
Fatty Acid Synthase (FASN)
|
Cancer
|
|
GSK2194069 is a potent inhibitor of β-ketoyl reductase (KR) of fatty acid synthase (FASN), with an IC50 value of 7.7 nM. GSK2194069 shows specifically inhibitory effect on FAS expressing cancer cells, by acting potent efficacy on acetoacetyl-CoA, NADPH with IC50 or Ki values of 4.8 nM and 5.6 nM, respectively .
|
-
- HY-106381
-
|
|
PKC
|
Inflammation/Immunology
Cancer
|
|
Aurothiomalate sodium is a potent and selective oncogenic PKCι signaling inhibitor. Aurothiomalate sodium inhibits tumor cell proliferation and not cell apoptosis. Aurothiomalate sodium is a potent thioredoxin reductase (TrxR) inhibitor. Aurothiomalate sodium, an anti-rheumatoid agent, exhibits potent anti-tumor activity .
|
-
- HY-126255
-
|
|
NAMPT
|
Metabolic Disease
|
|
SBI-797812 is an orally active nicotinamide phosphoribosyltransferase (NAMPT) activator. SBI-797812 shifts NAMPT to NMN formation, increases NAMPT affinity for ATP, stabilizes phosphorylated NAMPT, promotes consumption of the pyrophosphate by-product, and blunts feedback inhibition by NAD +. SBI-797812 increases intracellular nicotinamide mononucleotide (NMN) and elevates liver NAD + in mice .
|
-
- HY-149283
-
|
|
JAK
HDAC
Apoptosis
|
Cancer
|
|
JAK/HDAC-IN-2 is a potent 2-amino-4-phenylaminopyrimidine JAK/HDAC dual-target inhibitor. JAK/HDAC-IN-2 potently inhibits HDAC3/6 and JAK1/2 at nanomolar levels. JAK/HDAC-IN-2 has proapoptotic activity and inhibits histone deacetylation and STAT3 phosphorylation. JAK/HDAC-IN-2 presents remarkable antiproliferative activity in both hematological malignancies and solid cancers .
|
-
- HY-N0214R
-
-
- HY-N0214A
-
-
- HY-N0214
-
-
- HY-161618
-
|
|
JAK
EGFR
PI3K
IGF-1R
GSK-3
|
Inflammation/Immunology
Endocrinology
|
|
MJ04 is a selective inhibitor for Janus Kinase 3 (JAK 3) with an IC50 of 2.03 nM. MJ04 inhibits T cell differentation and inhibits the proinfammatory cytokines in Lipopolysaccharides (HY-D1056)‑induced macrophages. MJ04 exhibits good pharmacokinetic characters in mice, promotes hair growth in DHT-induced androgenetic alopecia (AGA) in athymic mice model, without significant toxicity (LD50 >2 g/kg) .
|
-
- HY-W011303
-
-
- HY-W011303R
-
-
- HY-149003
-
|
|
PARP
Apoptosis
|
Cancer
|
|
PARP1-IN-10 (compound 12c) is a no-cytotoxicity and potent PARP1 inhibitor with an IC50 value of 50.62 nM in vitro. PARP1-IN-10 causes cell cycle arrest at G2/M phase and apoptosis, and enhances the cytotoxicity of temozolomide (TMZ) .
|
-
- HY-P10757
-
-
- HY-14543
-
-
| Cat. No. |
Product Name |
Type |
-
- HY-D2208
-
|
|
Fluorescent Dyes/Probes
|
|
SYTM Green is a permeable DNA dye that fluoresces green by binding to dsDNA (Ex/Em=503/530 nm). SYTM Green can also be used to stain bacteria, including Gram-positive and Gram-negative bacteria. Note: SYTM Green cannot penetrate living cells, and this product is equivalent to SYTOX Green .
|
-
- HY-D1726
-
|
|
Fluorescent Dyes/Probes
|
|
8RK59, a Bodipy probe, is a potent UCHL1 (ubiquitin C-terminal hydrolase L1) inhibitor, with an IC50 close to 1 μM. 8RK59 could penetrate and label living cells. BodipyFL-alkyne is coupled to the azide of 8RK64 (HY-148254) using copper(I)-mediated click chemistry, resulting in compound 8RK59 .
|
| Cat. No. |
Product Name |
Type |
-
- HY-112764
-
|
|
Drug Delivery
|
|
DMG-PEG 2000 is used?for the preparation of liposome for siRNA delivery with improved transfection efficiency in vitro. DMG-PEG 2000 is also used for the?lipid nanoparticle for an oral plasmid DNA delivery approach in vivo through a facile surface modification to improve the mucus permeability and delivery efficiency of the nanoparticles .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P3397A
-
|
|
GHSR
|
Cancer
|
|
JV-1-36 acetate is a growth hormone-releasing hormone (GHRH) antagonist. JV-1-36 acetate inhibits the production of reactive oxygen species in A549 lung cancer cells. JV-1-36 can be used to study the effect of GHRH antagonists in vitro .
|
-
- HY-P10087
-
|
Mouse TREM-1(213–221), GF9
|
Peptides
|
Cancer
|
|
Mouse TREM-1 SCHOOL peptide (Mouse TREM-1(213-221), GF9) targets interactions between TREM-1 and its signaling partner DAP-12, and inhibits TREM-1 signaling. Mouse TREM-1 SCHOOL peptide has antitumor effect .
|
-
- HY-P1935
-
-
- HY-P3397
-
|
|
GHSR
|
Cancer
|
|
JV-1-36 is a growth hormone-releasing hormone (GHRH) antagonist. JV-1-36 inhibits the production of reactive oxygen species in A549 lung cancer cells. JV-1-36 can be used to study the effect of GHRH antagonists in vitro .
|
-
- HY-P3116
-
|
|
Bacterial
|
Cancer
|
|
Thiocoraline is a depsipeptide that can be isolated by marine Micromonospora. Thiocoraline has antitumor activity with IC50s of 0.002, 0.002, 0.01 and 0.002 μg/mL in P388, A549, HT-29 and MEL-28 cells, respectively. Thiocoraline also a strong antimicrobial activity against Gram-positive microorganisms .
|
-
- HY-139425
-
-
- HY-P10711
-
|
|
Autophagy
|
Cancer
|
|
ALA-A2 is an anticancer peptide discovered in alpha-lactalbumin that selectively kills cancer cells by inducing Autophagy. ALA-A2 has cell-penetrating capabilities, allowing it to effectively enter cells without relying on membranolytic effects. In A549 lung cancer cells, ALA-A2 demonstrates significant dose-dependent anticancer activity. ALA-A2 holds promise for research in cancer therapy and autophagy regulation .
|
-
- HY-P10819
-
|
|
Histone Demethylase
Apoptosis
|
Cancer
|
|
S9-CMC1 TFA is a covalent peptide lysine-specific demethylase 1 (LSD1) inhibitor with an IC50 value of 2.53 μM. S9-CMC1 TFA specifically recognizes Cys360 in the enzyme-active region. S9-CMC1 TFA inhibits LSD1 activity, increasing H3K4me1 and H3K4me2 levels, leading to G1 cell cycle arrest and apoptosis and inhibiting cell proliferation. S9-CMC1 TFA significantly inhibits tumor growth in A549 xenograft animal models .
|
-
- HY-P10403
-
|
|
IGF-1R
|
Inflammation/Immunology
Cancer
|
|
IGFBP-3 peptide is a 18-amino acid insulin-like growth factor binding protein-3. IGFBP-3 peptide binds Humanin (HY-P1928) and Hyaluronan (HY-B0633A), blocks the interaction of CD44 and hyaluronan .
|
-
- HY-P10850
-
|
|
TNF Receptor
NF-κB
Apoptosis
|
Inflammation/Immunology
|
|
PIYLGGVFQ is a peptide inhibitor for TNF-α. PIYLGGVFQ inhibits TNF-α-mediated apoptosis, NF-κB nuclear translocation and activation. PIYLGGVFQ exhibits anti-arthritic activity in the CIA mouse model .
|
-
- HY-P10218A
-
|
|
MARCKS
PKC
|
Inflammation/Immunology
Cancer
|
|
MANS peptide TFA is the TFA salt form of MANS peptide (HY-P10218). MANS peptide TFA is an inhibitor for myristoylated alanine-rich C kinase substrate (MARCKS), which competes with MARCKS in cells for membrane binding, and thus inhibits the stimulation of mucin secretion and tumor metastasis .
|
-
- HY-P10218
-
|
|
MARCKS
PKC
|
Inflammation/Immunology
Cancer
|
|
MANS peptide is an inhibitor for myristoylated alanine-rich C kinase substrate (MARCKS), which competes with MARCKS in cells for membrane binding, and thus inhibits the stimulation of mucin secretion and tumor metastasis .
|
-
- HY-P10386
-
|
|
Bcl-2 Family
|
Cancer
|
|
155H1 (Compound 11) is a stapled peptide, that covalently binds hMcl1 (172-323) with IC50 of 18 nM .
|
-
- HY-P10930A
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
wrwycr-NH2 (TFA) is a peptide. wrwycr-NH2 (TFA) is cytotoxic to multiple cancer cells, can induce DNA damage and cell cycle arrest, but does not induce endoplasmic reticulum stress. wrwycr-NH2 (TFA) has anti-tumor activity, and it shows better efficacy when used in combination with DNA-damaging agents .
|
-
- HY-119152
-
|
|
Insulin Receptor
Tyrosinase
Akt
|
Others
|
|
CMX-2043 is a novel analogue of α-Lipoic Acid (HY-N0492). CMX-2043 is effective in antioxidant effect, activation of insulin receptor kinase, soluble tyrosine kinase, and Akt phosphorylation. CMX-2043 shows protection against ischemia-reperfusion injury (IRI) in rat model .
|
-
- HY-P2282
-
|
|
STAT
|
Cancer
|
|
APTSTAT3-9R, a specific STAT3-binding peptide, inhibits STAT3 activation and downstream signaling by specifically blocking STAT3 phosphorylation. APTSTAT3-9R exerts antiproliferative effects and antitumor activity .
|
-
- HY-P10757
-
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P99345
-
|
TSR-042
|
PD-1/PD-L1
|
Cancer
|
|
Dostarlimab (TSR-042) is a humanized anti-PD-1 monoclonal antibody. Dostarlimab binds with high affinity to human PD-1 and competitively inhibits its interaction with its ligands, PD-L1 and PD-L2, with IC50s of 1.8 and 1.5 nM, respectively .
|
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-126422
-
-
-
- HY-P1935
-
-
-
- HY-162614
-
-
-
- HY-N11470
-
-
-
- HY-N7585
-
-
-
- HY-N3687
-
-
-
- HY-N10201
-
-
-
- HY-N4029
-
-
-
- HY-N2199
-
-
-
- HY-N7589
-
-
-
- HY-N2429
-
-
-
- HY-N10082
-
-
-
- HY-N8025
-
-
-
- HY-75564
-
-
-
- HY-N11912
-
-
-
- HY-126841
-
|
|
Structural Classification
Microorganisms
Source classification
Phenols
|
Photosensitizer
|
|
5-Methoxysterigmatocystin is a mycotoxin with cytotoxic and genotoxic properties. 5-Methoxysterigmatocystin exhibits cytotoxicity against cancer cells A549 and HepG2 (IC50 of 5.5 and 0.7 μM), and induces DNA damage. 5-Methoxysterigmatocystin is a photosensitizer, which utilizes the visible to generate singlet oxygen ( 1O2) .
|
-
-
- HY-N4048
-
-
-
- HY-N12563
-
-
-
- HY-N7980
-
-
-
- HY-129334
-
-
-
- HY-N10853
-
-
-
- HY-N10965
-
-
-
- HY-N0985
-
-
-
- HY-W778562
-
-
-
- HY-N10208
-
-
-
- HY-N8954
-
-
-
- HY-N13139
-
-
-
- HY-116038
-
-
-
- HY-N12079
-
-
-
- HY-135453
-
-
-
- HY-N12364
-
-
-
- HY-N9003
-
-
-
- HY-N10852
-
-
-
- HY-N12078
-
-
-
- HY-N6969A
-
|
|
Structural Classification
Alkaloids
Other Alkaloids
Source classification
Stephania epigaea Lo
Plants
Menispermaceae
|
Adrenergic Receptor
|
|
Dicentrine hydrochloride is a drug with anti-inflammatory and anti-cancer activity. Dicentrine hydrochloride exerts its effects by enhancing TNF-α-induced apoptosis in A549 lung adenocarcinoma cells. Dicentrine hydrochloride increases caspase-8, -9, -3 and poly(ADP-ribose) polymerase (PARP) activities. Dicentrine hydrochloride inhibits TNF-α-induced invasion and migration of A549 cells. Dicentrine hydrochloride significantly inhibited the TNF-α-activated TAK1, p38, JNK and Akt signaling pathways, and reduced the transcriptional activities of NF-κB and AP-1 .
|
-
-
- HY-N6955
-
-
-
- HY-N10113
-
-
-
- HY-N0753
-
-
-
- HY-N9101
-
|
|
Structural Classification
Caprifoliaceae
Source classification
Lignans
Phenylpropanoids
Viburnum cylindricum Buch.-Ham. ex D. Don
Plants
|
Others
|
|
4,4'-Dihydroxy-3,3',9-trimethoxy-9,9'-epoxylignan is a lignans that can be isolated from the Viburnum foetidum. 4,4'-Dihydroxy-3,3',9-trimethoxy-9,9'-epoxylignan has cytotoxicity against A549, SK-OV-3, SKMEL-2 and HCT15 cell line with IC50s of 67.14, 67.38, 64.11 and 76.31 μg/mL, respectively .
|
-
-
- HY-N1056
-
-
-
- HY-N10898
-
-
-
- HY-N12589
-
-
-
- HY-N11662
-
-
-
- HY-N6252
-
-
-
- HY-N10904
-
-
-
- HY-B0239
-
-
-
- HY-108016
-
-
-
- HY-N15267
-
|
|
Structural Classification
Natural Products
Millettia peguensis Ali
Leguminosae
Source classification
Plants
|
FAK
Akt
mTOR
|
|
Ovalitenone is a flavonoid compound that can be isolated from the plant Millettia peguensis. It shows no cytotoxic effects on lung cancer H460 and A549 cells, but it significantly inhibits anchorage-independent growth, CSC-like phenotypes, colony formation, and the migration and invasion capabilities of cancer cells. Ovalitenone can significantly reduce the levels of N-cadherin, snail, and slug, while increasing E-cadherin, thus inhibiting the EMT pathway. Additionally, Ovalitenone suppresses the signaling pathways regulated by focal adhesion kinase (FAK), ATP-dependent tyrosine kinase (AKT), mammalian target of rapamycin (mTOR), and cell division cycle 42 (Cdc42) .
|
-
-
- HY-113796
-
-
-
- HY-N4251
-
-
- HY-N7535
-
-
- HY-N8934
-
-
- HY-N13163
-
-
- HY-N1841
-
-
- HY-119767
-
-
- HY-N0781
-
-
- HY-N3615
-
-
- HY-N12617
-
-
- HY-N10351
-
-
- HY-B0239R
-
-
- HY-W667666
-
-
- HY-N6578
-
-
- HY-134008
-
-
- HY-123898
-
-
- HY-N13078
-
|
|
Structural Classification
Microorganisms
Source classification
Steroids
|
Others
|
|
3-epi-Resibufogenin (compound 2) is an anticancer agent that can be produced by biotransformation of Resibufogenin (HY-N0815) from Actinomucor elegans AS 3.2778. 3-epi-Resibufogenin exhibits cytotoxicity against cancer cells with IC50 values ??of 42.5 μM (A549) and 48.4 μM (H1299), respectively .
|
-
- HY-N13162
-
|
|
Triterpenes
Structural Classification
Terpenoids
Source classification
Cucurbitaceae
Plants
Hemsleya pengxianensis W. J. Chang
|
Others
|
|
Hemsleyadin D is a triterpenoid compound derived from Hemsleya penxianensis with antitumor activity. Its IC50 values against K562, MGC-803, U118, HepG2, A549, and MCF-7 cells are 93.9, 47.1, 25.9, 56.1, 66.3, and 67.6 μM, respectively .
|
-
- HY-163742
-
-
- HY-N0781R
-
-
- HY-N3179
-
-
- HY-149436
-
-
- HY-N1614
-
-
- HY-N0074
-
-
- HY-N3210
-
-
- HY-N0538
-
-
- HY-N12349
-
-
- HY-N12135
-
|
|
Structural Classification
Terpenoids
Labiatae
Source classification
Diterpenoids
Plants
Cyrtocymura cincta var. cincta
|
Others
|
|
15α-Hydroxy-20-oxo-6,7-seco-ent-kaur-16-en-1,7α(6,11α)-diolide (compound 2) is an enantio-kaurene diterpenoid (ent -kaurene diterpenoid), which can be isolated from Rubescens rubescens. 15α-Hydroxy-20-oxo-6,7-seco-ent-kaur-16-en-1,7α(6,11α)-diolide has cellular activity against EC-1, U87, A549, MCF-7 and HeLa cell lines Toxicity, IC50s are 37.69 μM, 79.362 μM, 80.07 μM, 197.35 μM, 462.13 μM, and 180.09 μM respectively .
|
-
- HY-N0084
-
-
- HY-N12606
-
-
- HY-N8508
-
|
|
Structural Classification
Natural Products
Microorganisms
Source classification
|
Apoptosis
Cytochrome P450
PARP
JNK
Bcl-2 Family
Caspase
|
|
Myrothecine A is a trichothecene mycotoxin found in M. roridum. Myrothecine A induces apoptosis, promotes the cytochrome c release, PARP-cleavage and phosphorylation of JNK, increases Bax and cleaved caspase-3, -5, and -8 levels. Myrothecine A has anticancer activities and promotes the maturation of DC cells in the microenvironment. Myrothecine A inhibits proliferation of A549, MCF-7, HepG2, and SMMC-7721 cancer cells with IC50s of 95, 70, 60, and 25 µM, respectively .
|
-
- HY-115407
-
|
|
Structural Classification
Natural Products
Microorganisms
Source classification
|
Bacterial
|
|
Cochliodone A is an active compound extracted from cultures of the deep-sea derived fungus Chaetomium sp. and has antibacterial and anticancer activity. Cochliodone A is toxic to a variety of bacteria, with MICs of 15.3 μg/mL (V. vulnificus), 32.7 μg/mL (V. rotiferianus), 15.9 μg/mL (S. aureus ATCC 43300), and 16.3 μg/mL (S . aureus CGMCC 1.12409). Cochliodone A also inhibits a variety of cancer cell lines, with IC50s of 28.1 μM (A549), 20.7 μM (HeLa), and 23.2 μM (Hep G2) .
|
-
- HY-N13176
-
-
- HY-N14995
-
-
- HY-16941
-
-
- HY-122942
-
-
- HY-N12996
-
-
- HY-N0203R
-
-
- HY-N0203
-
-
- HY-N15227
-
-
- HY-N3222
-
-
- HY-N12004
-
-
- HY-121254
-
-
- HY-N6727
-
-
- HY-N11082
-
-
- HY-N0883
-
-
- HY-133219
-
-
- HY-N0211
-
-
- HY-N0211R
-
-
- HY-122944
-
-
- HY-N4058R
-
-
- HY-N1820
-
-
- HY-N7158
-
-
- HY-16942
-
-
- HY-N4058
-
-
- HY-N6998
-
-
- HY-75564R
-
-
- HY-B0914
-
-
- HY-W042191
-
-
- HY-W042191R
-
-
- HY-N10472
-
-
- HY-18572
-
-
- HY-18572R
-
|
|
Ketones, Aldehydes, Acids
Source classification
Endogenous metabolite
|
DNA/RNA Synthesis
Apoptosis
|
|
2,4-D (Standard) is the analytical standard of 2,4-D. This product is intended for research and analytical applications. 2,4-D (2, 4-dichlorophenoxyacetic acid) is a selective herbicide that can be orally active for the control of broad-leaved weeds. 2,4-D can induce apoptosis. 2,4-D inhibits DNA and protein synthesis, thereby preventing normal plant growth and development .
|
-
- HY-138962
-
-
- HY-N2359
-
-
- HY-107430R
-
-
- HY-107430
-
-
- HY-107430A
-
-
- HY-N10391
-
-
- HY-129325
-
-
- HY-N1710
-
-
- HY-N2454
-
-
- HY-N2454R
-
-
- HY-W010155
-
-
- HY-N7205
-
-
- HY-N12603
-
-
- HY-N3376
-
-
- HY-N0638
-
-
- HY-19825
-
-
- HY-N6642
-
-
- HY-N10558
-
-
- HY-122919
-
-
- HY-N8915
-
-
- HY-126566
-
-
- HY-B1357R
-
-
- HY-N0867
-
-
- HY-B1513
-
-
- HY-B1357
-
-
- HY-N1930
-
-
- HY-N2278
-
-
- HY-N2802
-
-
- HY-N3737
-
-
- HY-117235
-
-
- HY-B0809A
-
-
- HY-B0809
-
-
- HY-B0809B
-
-
- HY-117235R
-
-
- HY-N3980R
-
|
|
Structural Classification
Natural Products
Source classification
Distemonanthus benthamianus Baill.
Plants
Compositae
|
Autophagy
RAD51
|
|
Guaiol (Standard) is the analytical standard of Guaiol. This product is intended for research and analytical applications. Guaiol is a sesquiterpenoid alcohol with oral activity found in various traditional Chinese medicines, exhibiting biological activities such as anti-proliferative, autophagy-promoting, insecticidal, anti-anxiety, anti-inflammatory, diuretic, and blood pressure-lowering effects. Guaiol induces apoptosis in non-small cell lung cancer cells by regulating the stability of RAD51 through autophagy modulation. Guaiol can also act directly on parasites, inhibiting their growth by affecting the kinetoplast, mitochondrial matrix and plasma membrane of the promastigotes. Guaiol kills amastigotes at an IC50 of 0.01 µg/mL. Guaiol can be used in research related to cancer, infections, cardiovascular diseases, and inflammatory conditions [4]
|
-
- HY-N8884
-
-
- HY-Y0152R
-
-
- HY-N10447
-
-
- HY-N3980
-
|
Champacol; Guaiac alcohol
|
Infection
Structural Classification
Natural Products
Classification of Application Fields
Source classification
Distemonanthus benthamianus Baill.
Plants
Compositae
Disease Research Fields
|
Autophagy
RAD51
|
|
Guaiol is a sesquiterpenoid alcohol with oral activity found in various traditional Chinese medicines, exhibiting biological activities such as anti-proliferative, autophagy-promoting, insecticidal, anti-anxiety, anti-inflammatory, diuretic, and blood pressure-lowering effects. Guaiol induces apoptosis in non-small cell lung cancer cells by regulating the stability of RAD51 through autophagy modulation. Guaiol can also act directly on parasites, inhibiting their growth by affecting the kinetoplast, mitochondrial matrix and plasma membrane of the promastigotes. Guaiol kills amastigotes at an IC50 of 0.01 µg/mL. Guaiol can be used in research related to cancer, infections, cardiovascular diseases, and inflammatory conditions [4]
|
-
- HY-N0451
-
-
- HY-Y0152
-
-
- HY-N2534R
-
-
- HY-N0164R
-
-
- HY-124896
-
|
6-Geranylnaringenin; Mimulone
|
Paulownia tomentosa (Thunb.) Steud.
Scrophulariaceae
Plants
|
Phosphatase
Apoptosis
Autophagy
|
|
Bonannione A (6-Geranylnaringenin; Mimulone), a prenylflavonoid, is an orally active and potent protein tyrosine phosphatase 1B (PTP1B) inhibitor with an IC50 of 14 µM. Bonannione A triggers caspase-dependent apoptosis. Bonannione A induces autophagy through p53-mediated AMPK/mTOR pathway. Bonannione A shows anti-inflammatory, antiradical and anti-cancer activity .
|
-
- HY-N2534
-
-
- HY-N0164
-
-
- HY-122094
-
-
- HY-N0214R
-
-
- HY-N0214A
-
-
- HY-N0214
-
-
- HY-W011303
-
-
- HY-W011303R
-
-
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-17037S1
-
|
|
|
Pirenzepine-d8 (LS 519-d8; Pirenzepin-d8) dihydrochloride is a deuterium labeled Pirenzepine (dihydrochloride) (HY-17037). Pirenzepine (LS 519) dihydrochloride is a selective M1 mAChR (muscarinic acetylcholine receptor) antagonist. Pirenzepine dihydrochloride reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine dihydrochloride shows anti-proliferative activity to cancer cells .
|
-
-
- HY-145119AS
-
|
|
|
Mindeudesivir (JT001; VV116; GS-621763-d1) hydrobromide is a deuterated version of Remdesivir (HY-104077), a highly orally active nucleoside antiviral against SARS-CoV-2 and respiratory syncytial virus (RSV). Mindeudesivir hydrobromide retains the antiviral activity of Remdesivir against COVID-19, and is the first domestically produced deuterium targeting the COVID-19 .
|
-
-
- HY-159176
-
|
|
|
Antitumor agent-183 (compound 3f) has antitumor activity with metabolic stability. Antitumor agent-183 inhibits cancer cell growth, with IC50s less than 5 nM for A549, HCT116, and HS578T cells. The albumin-bound nanoparticle formulation of Antitumor agent-183 has prolonged retention in the tumor tissues .
|
-
-
- HY-B0239S2
-
|
|
|
Threo-Chloramphenicol-d6 is the deuterium labeled Chloramphenicol[1]. Chloramphenicol is an orally active, potent and broad-spectrum antibiotic. Chloramphenicol shows antibacterial activity. Chloramphenicol represses the oxygen-labile transcription factor and hypoxia inducible factor-1 alpha (HIF-1α) in hypoxic A549 and H1299 cells. Chloramphenicol suppresses the mRNA levels of vascular endothelial growth factor (VEGF) and glucose transporter 1, eventually decreasing VEGF release. Chloramphenicol can be used for anaerobic infections and lung cancer research[2][3][4].
|
-
-
- HY-160220S
-
|
|
|
KRAS inhibitor-23 (Isomer 2 of compound i) is a potent inhibitor of KRAS that plays an important role in cancer research .
|
-
-
- HY-B0712S1
-
|
|
|
Ceftriaxone- 13C2,d3 triethylammonium salt is 13C and deuterated labeled Ceftriaxone (HY-B0712). Ceftriaxone (Ro 13-9904 free acid) is a broad spectrum β-lactam third-generation cephalosporin antibiotic, which has good antibacterial activity against a variety of gram-negative and positive bacteria. Ceftriaxone is a covalent inhibitor of GSK3β with IC50 value of 0.78 mM. Ceftriaxone is an inhibitor of Aurora B. Ceftriaxone has anti-inflammatory, antitumor and antioxidant activities. Ceftriaxone can be used in the study of bacterial infections and meningitis .
|
-
-
- HY-B0809S1
-
|
|
|
Theophylline-d3 is deuterated labeled Theophylline (HY-B0809). Theophylline (1,3-Dimethylxanthine) is a potent phosphodiesterase (PDE) inhibitor, adenosine receptor antagonist, and histone deacetylase (HDAC) activator. Theophylline (1,3-Dimethylxanthine) inhibits PDE3 activity to relax airway smooth muscle. Theophylline (1,3-Dimethylxanthine) has anti-inflammatory activity by increase IL-10 and inhibit NF-κB into the nucleus. Theophylline (1,3-Dimethylxanthine) induces apoptosis. Theophylline (1,3-Dimethylxanthine) can be used for asthma and chronic obstructive pulmonary disease (COPD) research .
|
-
| Cat. No. |
Product Name |
|
Classification |
-
- HY-159449
-
|
|
|
Azide
|
|
PROTAC SMARCA2 degrader-5 (Compound I-425) is a PROTAC degrader for catalytic subunit of the SWI/SNF complex SMARCA2. PROTAC SMARCA2 degrader-5 degrades SMARCA2 in MV411 and in A549 with DC50 <100 nM, degrades SMARCA4 with DC50 of 100-500 nM . (Pink: Ligand for target protein (HY-159531); Black: Linker (HY-159538); Blue: Ligand for E3 ligase (S,R,S)-AHPC (HY-125845))
|
-
- HY-159461
-
|
|
|
Azide
|
|
PROTAC SMARCA2/4-degrader-9 (Compound I-503) is a PROTAC degrader for catalytic subunit of the SWI/SNF complex SMARCA2 and SMARCA4. PROTAC SMARCA2 degrader-9 degrades SMARCA2 in MV411 and in A549 with DC50 <100 nM, degrades SMARCA4 in MV411 with DC50 <100 nM . (Pink: Ligand for target protein (HY-159545); Black: Linker (HY-W006635); Blue: Ligand for E3 ligase (S,R,S)-AHPC (HY-125845))
|
-
- HY-159455
-
|
|
|
Azide
|
|
PROTAC SMARCA2/4-degrader-4 (Compound I-434) is a PROTAC degrader for catalytic subunit of the SWI/SNF complex SMARCA2 and SMARCA4. PROTAC SMARCA2/4-degrader-4 degrades SMARCA2 in MV411 and in A549 with DC50 <100 nM, degrades SMARCA4 in MV411 with DC50 <100 nM. (Pink: Ligand for target protein (HY-159472); Black: Linker (HY-159478); Blue: Ligand for E3 ligase (S,R,S)-AHPC (HY-125845))
|
-
- HY-159456
-
|
|
|
Azide
|
|
PROTAC SMARCA2/4-degrader-5 (Compound I-437) is a PROTAC degrader for catalytic subunit of the SWI/SNF complex SMARCA2 and SMARCA4. PROTAC SMARCA2/4-degrader-5 degrades SMARCA2 in MV411 and in A549 with DC50 <100 nM, degrades SMARCA4 in MV411 with DC50 of 100-500 nM. (Pink: Ligand for target protein (HY-159545); Black: Linker (HY-159557); Blue: Ligand for E3 ligase (S,R,S)-AHPC (HY-125845))
|
-
- HY-159460
-
|
|
|
Azide
|
|
PROTAC SMARCA2/4-degrader-8 (Compound I-502) is a PROTAC degrader for catalytic subunit of the SWI/SNF complex SMARCA2. PROTAC SMARCA2/4-degrader-8 degrades SMARCA2 with DC50 <100 nM in A549 and in MV411, degrades SMARCA4 with DC50<100 nM in MV411(Pink: Ligand for target protein (HY-159545); Black: Linker (HY-W063924); Blue: Ligand for E3 ligase (S,R,S)-AHPC (HY-125845))
|
-
- HY-159462
-
|
|
|
Azide
|
|
PROTAC SMARCA2 degrader-10 (compound I-507) is a PROTAC degrader targeting SMARCA2; it degrades SMARCA2 proteins in A549 cells with an DC50 <100 nM, and a maximum degradation rate (Dmax%) >90 after 24 h of treatment .
|
-
- HY-159450
-
|
|
|
Azide
|
|
PROTAC SMARCA2 degrader-6 (compound I-427) is a PROTAC degrader targeting SMARCA2; it degrades SMARCA2 proteins in A549 cells with an DC50 <100 nM, and a maximum degradation rate (Dmax%) >90 after 24 h of treatment .
|
-
- HY-159459
-
|
|
|
Azide
|
|
PROTAC SMARCA2/4-degrader-32 (compound I-446) is a PROTAC degrader targeting SMARCA2 and SMARCA4; it degrades SMARCA2/4 proteins in A549 cells with the DC50s <100 nM, and the maximum degradation rate (Dmax%) >90 after 24 h of treatment .
|
-
- HY-159458
-
|
|
|
Azide
|
|
SMARCA2/4-degrader-7 (compound I-439) is a PROTAC degrader targeting SMARCA2 and SMARCA4; it degrades SMARCA2/4 proteins in A549 cells with the DC50s <100 nM, and the maximum degradation rate (Dmax%) >90 after 24 h of treatment .
|
-
- HY-159452
-
|
|
|
Azide
|
|
SMARCA2/4-degrader-1 (compound I-430) is a PROTAC degrader targeting SMARCA2 and SMARCA4; it degrades SMARCA2/4 proteins in A549 cells with the DC50s <100 nM, and the maximum degradation rate (Dmax%) >90 after 24 h of treatment .
|
-
- HY-159453
-
|
|
|
Azide
|
|
SMARCA2/4-degrader-2 (compound I-431) is a PROTAC degrader targeting SMARCA2 and SMARCA4; it degrades SMARCA2/4 proteins in A549 cells with the DC50s <100 nM, and the maximum degradation rate (Dmax%) >90 after 24 h of treatment .
|
-
- HY-159087
-
|
|
|
Azide
|
|
RGB110 (Compound 10d) is a PROTAC inhibitor for D-dopachrome tautomerase with an IC50 of 5.9 μM. RGB110 causes no degradation of D-DT. (Pink: ligand for target protein (HY-159164); Black: linker (HY-W125017); Blue: ligand for E3 ligase CRBN (HY-10984))
|
-
- HY-159454
-
|
|
|
Azide
|
|
SMARCA2/4-degrader-3 (compound I-433) is a PROTAC SMARCA2/4-degrader based on VH032-NH2, with a degradation potency (DC50) <100 nM in MV4-11 cells .
|
| Cat. No. |
Product Name |
|
Classification |
-
- HY-N0538
-
|
Xylite
|
|
Fillers
|
|
Xylitol can be classified as a polyol and sugar alcohol, exhibiting inhibitory activity on cancer cell proliferation. It induces autophagy (Autophagy) and cell death in A549 cells by activating the autophagy signaling pathway, as evidenced by the increased expression of LC3-II and Atg5-Atg12 upon Xylitol treatment. Additionally, Xylitol inhibits acetaldehyde production by Candida species, thereby reducing their carcinogenic potential. In vivo, Xylitol induces alterations in the gut microbiota of mice, which may enhance cholesterol accumulation and upregulate hepatic ChREBP, while also slowing tumor growth in the B16F10 melanoma C57BL/6 mouse model .
|
-
- HY-150218
-
|
ODN 2006 sodium; ODN 7909 sodium; PF-3512676 sodium; CpG 7909 sodium
|
|
CpG ODNs
|
|
Agatolimod sodium (ODN 2006) is a class B CpG ODN and is a TLR9 agonist. Agatolimod sodium can be used as vaccine adjuvant. Agatolimod sodium can be used for the research of cancer. Sequence: 5’-TCGTCGTTTTGTCGTTTTGTCGTT-3’ .
|
-
- HY-148413
-
|
ISIS 3521 sodium
|
|
Antisense Oligonucleotides
|
|
Aprinocarsen (ISIS 3521) sodium, a specific antisense oligonucleotide inhibitor of protein kinase C-alpha (PKC-α). Aprinocarsen sodium is a 20-mer oligonucleotide, it regulates cell differentiation and proliferation. Aprinocarsen sodium inhibits the growth of human tumor cell lines in nude mice. Aprinocarsen sodium shows the value as a chemotherapeutic compound of human cancers .
|
-
- HY-B1513
-
|
|
|
Others
|
|
α-Cyclodextrin (α-CD) is a soluble fiber derived from corn. α-Cyclodextrin can deplete sphingolipids and phospholipids from cell membranes. α-Cyclodextrin interacts with tubulin. α-Cyclodextrin improves defenses against SARS-CoV-2 infection. α-Cyclodextrin enhances the anticancer efficacy of Crcumin (HY-N0005) against breast, lung and cervical cancer. α-Cyclodextrin has beneficial effects on body weight and blood lipids .
|
-
- HY-112764
-
DMG-PEG 2000
Maximum Cited Publications
8 Publications Verification
|
|
Pegylated Lipids
|
|
DMG-PEG 2000 is used?for the preparation of liposome for siRNA delivery with improved transfection efficiency in vitro. DMG-PEG 2000 is also used for the?lipid nanoparticle for an oral plasmid DNA delivery approach in vivo through a facile surface modification to improve the mucus permeability and delivery efficiency of the nanoparticles .
|
-
- HY-112764A
-
|
|
|
Emulsifiers
Liposomal Film-forming Agents
|
|
DMG-PEG Excipient is used?for the preparation of liposome for siRNA delivery with improved transfection efficiency in vitro. DMG-PEG Excipient is also used for the?lipid nanoparticle for an oral plasmid DNA delivery approach in vivo through a facile surface modification to improve the mucus permeability and delivery efficiency of the nanoparticles .
|
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