Search Result
Results for "
A549,
" in MedChemExpress (MCE) Product Catalog:
2
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- 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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-
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- HY-172116
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-
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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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-
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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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-
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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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-
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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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-
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- HY-P1935
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-
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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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-
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- HY-139425
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-
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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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-
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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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-
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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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-
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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-168247
-
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PROTACs
Epigenetic Reader Domain
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Cancer
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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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-
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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-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-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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-
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- HY-169370
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-
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- HY-170653
-
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DNA/RNA Synthesis
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Cancer
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Anticancer agent 262 (compound 3h) is a DNA intercalating anticancer agent, with an IC50 of 5.7 µM against A549 cancer cells .
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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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-
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- HY-103662
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-
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- HY-159820
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Others
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Cancer
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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 .
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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-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-N9003
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Others
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Cancer
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Dihydroprehelminthosporol (Compound 1) from the
fungusVeronaea sp.of the separated. Dihydroprehelminthosporol on
human cancer cell line A549 and SK-0A-3 has cytotoxicity .
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- HY-N12364
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Others
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Cancer
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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 .
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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-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-N10852
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Others
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Cancer
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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 .
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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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-
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- HY-W471938
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Others
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Cancer
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Antiproliferative agent-35 (Compound 4) inhibits the proliferation of B16 and A549 cells, with IC50s of 13.2 and 9.2 μM resspectively .
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-
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- HY-163860
-
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EGFR
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Cancer
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EGFR-TK-IN-3 (3) is an EGFR TK inhibitor, with an IC50 of 2.33 μM against Erlotinib (HY-50896)-resistant 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-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-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-120581
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PGE synthase
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Cancer
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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 .
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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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-
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- HY-162341
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Topoisomerase
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Cancer
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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 .
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-
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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-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-N6969A
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Adrenergic Receptor
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Cancer
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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 .
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- HY-N6955
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Others
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Cancer
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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 .
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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-162108
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Apoptosis
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Cancer
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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 .
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- HY-N0753
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Others
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Cancer
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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 .
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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-116038
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Others
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Cancer
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Kulinone has cytotoxic effects against A549, H460 and HGC27 with IC50 values of 6.2 ± 0.1, 7.8 ± 1.2, 5.6 ± 0.2 μg/ml 。
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- HY-149841
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Akt
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Cancer
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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 .
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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-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-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-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-N1056
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Zerumbetol
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Others
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Cancer
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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 .
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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-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-111320
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Bacterial
Antibiotic
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Cancer
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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.
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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-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-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-165114
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Endogenous Metabolite
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Cancer
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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 .
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- HY-148572
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Indoleamine 2,3-Dioxygenase (IDO)
NAMPT
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Cancer
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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 .
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- HY-N10898
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Lipoxygenase
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Inflammation/Immunology
Cancer
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(-)-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) .
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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-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-N6252
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Others
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Cancer
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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 .
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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-N11662
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Others
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Cancer
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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 .
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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-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-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-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-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-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-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-115983
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CD47
Apoptosis
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Cancer
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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-147348
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Biochemical Assay Reagents
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Cancer
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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 .
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- HY-N10904
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Others
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Cancer
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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) .
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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-156450
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ERK
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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-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-158019
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
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 .
|
-
- HY-N4048
-
|
|
Others
|
Cancer
|
|
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 .
|
-
- 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-158020
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
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 .
|
-
- 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-161891
-
|
|
EGFR
Akt
|
Cancer
|
|
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 .
|
-
- HY-170549
-
|
|
VEGFR
|
Cancer
|
|
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 .
|
-
- HY-130624
-
|
|
HSP
Apoptosis
|
Cancer
|
|
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 .
|
-
- 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-152147
-
|
|
PROTACs
HDAC
Apoptosis
DNA/RNA Synthesis
|
Cancer
|
|
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 .
|
-
- 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-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-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-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-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-N8025
-
|
|
Others
|
Cancer
|
|
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 .
|
-
- 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-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-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-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-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-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-115960
-
|
|
Others
|
Cancer
|
|
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 .
|
-
- HY-145861
-
|
|
Histone Demethylase
Apoptosis
|
Cancer
|
|
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 .
|
-
- HY-146319
-
-
- 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-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-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-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-169272
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
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 .
|
-
- 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-147030
-
|
|
PARP
|
Cancer
|
|
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 .
|
-
- 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-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-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-163713
-
|
|
SARS-CoV
|
Infection
|
|
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 .
|
-
- HY-168607
-
|
|
TGF-beta/Smad
|
Cancer
|
|
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 .
|
-
- HY-170559
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
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 .
|
-
- HY-172110
-
|
|
EGFR
Akt
p38 MAPK
ERK
Apoptosis
|
Cancer
|
|
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 .
|
-
- HY-147862
-
|
|
EGFR
Apoptosis
|
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 .
|
-
- HY-156110
-
|
|
Insulin Receptor
|
Cancer
|
|
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 .
|
-
- 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-161863
-
|
|
Microtubule/Tubulin
Reactive Oxygen Species
Apoptosis
|
Cancer
|
|
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
|
-
- 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-155359
-
|
|
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 .
|
-
- HY-156355
-
|
|
Others
|
Cancer
|
|
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) .
|
-
- HY-157402
-
|
|
Topoisomerase
EGFR
|
Cancer
|
|
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 .
|
-
- HY-N12607
-
|
|
Others
|
Cancer
|
|
Garcilatelic acid (Compound 5) is a compound that can be isolated from Garcinia lateriflora. Garcilatelic acid has antiproliferative activity against tumor cell lines (A549, MDA-MB-231, MCF-7, KB and KB-VIN), with IC50 values of 0.5-1.3 μM .
|
-
- 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-N10965
-
|
|
Others
|
Cancer
|
|
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 .
|
-
- 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-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-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-162891
-
|
|
EGFR
|
Cancer
|
|
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 .
|
-
- HY-169270
-
|
|
Epigenetic Reader Domain
PROTACs
|
Cancer
|
|
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 .
|
-
- 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-144394
-
|
|
Apoptosis
c-Met/HGFR
|
Cancer
|
|
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 .
|
-
- HY-N10853
-
|
|
Others
|
Cancer
|
|
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 .
|
-
- HY-124429
-
|
|
ERK
|
Cancer
|
|
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 .
|
-
- 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-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-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-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-129334
-
|
|
Telomerase
|
Cancer
|
|
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 .
|
-
- HY-162956
-
|
|
SARS-CoV
|
Infection
|
|
SARS-CoV-2-IN-97 (Compound CO-01) is an inhibitor for SARS-CoV-2 Nsp15 endoribonuclease with an IC50 of 53.5 μM. SARS-CoV-2-IN-97 exhibits low cytotoxicity in A549-AT cell with IC50 of 134 μM .
|
-
- HY-W159754
-
|
p-Hydroxyallylbenzene
|
Cholinesterase (ChE)
|
Cancer
|
|
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 .
|
-
- HY-138537
-
|
|
IKK
|
Cancer
|
|
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 .
|
-
- 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-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-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-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-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-157413
-
|
|
EGFR
|
Cancer
|
|
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 .
|
-
- 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-163198
-
|
|
ASCT
mTOR
Apoptosis
Autophagy
|
Cancer
|
|
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 .
|
-
- HY-158436
-
|
|
Microtubule/Tubulin
Autophagy
Apoptosis
|
Cancer
|
|
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 .
|
-
- HY-126841
-
|
|
Photosensitizer
|
Cancer
|
|
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-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-164389
-
|
|
Ras
|
Cancer
|
|
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 .
|
-
- 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-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-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-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-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-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-142945
-
|
|
Ras
|
Cancer
|
|
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 .
|
-
- 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 .
|
-
- HY-155039
-
|
|
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-157564
-
|
|
Apoptosis
|
Cancer
|
|
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) .
|
-
- 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-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-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-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-159576
-
|
O-Me B1939; O-Me E7389; O-Me ER-086526
|
ADC Cytotoxin
|
Cancer
|
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 .
|
-
- 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-168236
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
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))
|
-
- HY-161654
-
|
|
PROTACs
Ras
|
Cancer
|
|
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))
|
-
- 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-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) .
|
-
- 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-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-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-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-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-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-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-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-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-162342
-
|
|
Topoisomerase
|
Cancer
|
|
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 .
|
-
- HY-161403
-
|
|
Cytochrome P450
|
Cancer
|
|
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 .
|
-
- 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 .
|
-
- HY-139272
-
|
|
Others
|
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-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-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-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-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-161284
-
|
|
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) .
|
-
- HY-159176
-
|
|
Cytochrome P450
|
Cancer
|
|
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-163880
-
|
|
EGFR
Ras
p38 MAPK
Reactive Oxygen Species
|
Cancer
|
|
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 .
|
-
- HY-N12563
-
|
|
c-Myc
Apoptosis
|
Cancer
|
|
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 .
|
-
- 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-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-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-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-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 .
|
-
- 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-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-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-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-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-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-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-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-N0985
-
|
|
Others
|
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 渭g/ml, respectively .
|
-
- 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-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-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-161450
-
|
|
PROTACs
Ras
|
Cancer
|
|
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)) .
|
-
- 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-172112
-
|
|
VEGFR
Apoptosis
|
Cancer
|
|
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 .
|
-
- 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 .
|
-
- 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-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-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-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-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-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-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-149302
-
|
|
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-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-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 .
|
-
- HY-168606A
-
|
|
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 .
|
-
- 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 .
|
-
- 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-118528A
-
|
|
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-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-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-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 .
|
-
- 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-159123
-
|
|
MAP4K
|
Cancer
|
|
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 .
|
-
- 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-168113
-
|
|
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-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-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-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-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 .
|
-
- 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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-161668
-
|
|
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-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-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-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-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) .
|
-
- 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-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-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-170368
-
|
|
SF3B1
|
Cancer
|
|
3’-Me Meayamycin D is a splicing modulator on SF3B1 and PHF5A, that affects the pre-mRNA splicing process, and downregulates the MCL-1 expression. 3’-Me Meayamycin D inhibits the proliferation of cancer cell HCT116, SW48, A549, DMS53 and DMS114 with GI50 of 4.6-7.2 nM. 3’-Me Meayamycin D exhibits good plasma stability in mice with a halt-life of 16 h .
|
-
- 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-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-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-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-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-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-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-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-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-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-119631
-
|
|
Others
|
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-159449
-
|
|
PROTACs
Epigenetic Reader Domain
|
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))
|
-
- 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-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-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-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-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-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-163871
-
|
|
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-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))
|
-
- 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))
|
-
- 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-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-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-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-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-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-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-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-163877
-
|
|
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
-
|
|
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-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)) .
|
-
- 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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-121255
-
|
(R)-Cryptopleurine; NSC 19912
|
Others
|
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-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-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-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-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-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-107298
-
|
|
p38 MAPK
Apoptosis
|
Cancer
|
|
1-Cinnamoyltrichilinin can inhibit the viability of HL-60 human leukemia cells, induceapoptosis of HL-60 cells, and increase nuclear fragmentation and fractional DNA content by activating the p38 MAPK pathway. The anti-cancer properties of 1-Cinnamoyltrichilinin are only effective against HL-60 cells, not in other human cancer cell lines, such as epidermoid
carcinoma (A431), lung epithelial carcinoma (A549), and mammary gland adenocarcinoma (MCF7),
at a 20 µM concentration, which is otherwise not toxic to a normal cell line (RAW 264.7). 1-Cinnamoyltrichilinin can be used in the research of leukemia .
|
-
- 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-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-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-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-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-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-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-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-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-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-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-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-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-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 .
|
-
- 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.
|
-
| 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-P1935
-
-
- HY-139425
-
-
- 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-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 .
|
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
- 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-N10208
-
-
- HY-N3179
-
-
- HY-N8954
-
-
- HY-N0781R
-
-
- HY-149436
-
-
- HY-N12563
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- HY-N0074
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- HY-135453
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- HY-W778562
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- HY-N1614
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- HY-N3210
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- HY-N10113
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- HY-N0985
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- HY-N12349
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- HY-N0084
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- HY-N12606
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- HY-N13139
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- HY-B0239
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- HY-108016
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- HY-N12079
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- HY-N8508
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Structural Classification
Natural Products
Microorganisms
Source classification
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Apoptosis
Cytochrome P450
PARP
JNK
Bcl-2 Family
Caspase
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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 .
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- HY-N9101
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Structural Classification
Caprifoliaceae
Source classification
Lignans
Phenylpropanoids
Viburnum cylindricum Buch.-Ham. ex D. Don
Plants
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Others
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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 .
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- HY-N12078
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- HY-B0239R
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- HY-115407
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Structural Classification
Natural Products
Microorganisms
Source classification
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Bacterial
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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) .
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- HY-N12589
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- HY-N13176
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- HY-N15267
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Structural Classification
Natural Products
Millettia peguensis Ali
Leguminosae
Source classification
Plants
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FAK
Akt
mTOR
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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) .
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- HY-107298
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Structural Classification
Natural Products
Source classification
Melia azedarach L.
Plants
Meliaceae
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p38 MAPK
Apoptosis
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1-Cinnamoyltrichilinin can inhibit the viability of HL-60 human leukemia cells, induceapoptosis of HL-60 cells, and increase nuclear fragmentation and fractional DNA content by activating the p38 MAPK pathway. The anti-cancer properties of 1-Cinnamoyltrichilinin are only effective against HL-60 cells, not in other human cancer cell lines, such as epidermoid
carcinoma (A431), lung epithelial carcinoma (A549), and mammary gland adenocarcinoma (MCF7),
at a 20 µM concentration, which is otherwise not toxic to a normal cell line (RAW 264.7). 1-Cinnamoyltrichilinin can be used in the research of leukemia .
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- HY-N0538
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- HY-N12135
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Structural Classification
Terpenoids
Labiatae
Source classification
Diterpenoids
Plants
Cyrtocymura cincta var. cincta
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Others
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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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| Cat. No. |
Product Name |
Chemical Structure |
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- HY-159176
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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-B0239S2
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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].
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| Cat. No. |
Product Name |
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Classification |
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- HY-159450
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Azide
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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 .
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- HY-159462
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Azide
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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 .
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- HY-159458
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Azide
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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 .
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- HY-159459
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Azide
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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 .
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- HY-159452
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Azide
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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 .
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- HY-159453
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Azide
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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 .
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- HY-159449
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Azide
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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-159461
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Azide
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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))
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- HY-159460
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Azide
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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))
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- HY-159455
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Azide
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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))
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- HY-159456
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Azide
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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))
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| Cat. No. |
Product Name |
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Classification |
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- HY-N0538
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Xylite
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Fillers
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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 .
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