Search Result
Results for "
induces cell cycle arrest
" in MedChemExpress (MCE) Product Catalog:
3
Biochemical Assay Reagents
13
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-118034
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p38 MAPK
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Cancer
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MTBT is an anticancer agent and p38 activator with antiproliferative and apoptosis-inducing (apoptosis) activities. MTBT increases the phosphorylation of histone H3 serine in cancer cells, thereby arresting the cell cycle in the M phase. SB203580 (HY-10256), a specific inhibitor of p38 MAPK, abolished MTBT-induced cell cycle arrest .
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- HY-N5074
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Apoptosis
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Cancer
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Terrestrosin D, a steroidal saponin from Tribulus terrestris L., induces cell cycle arrest and cancer cells apoptosis. Terrestrosin D has antiangiogenic activities .
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- HY-136489
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PARP
Apoptosis
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Cancer
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KU-0058948 is a specific and potent PARP1 inhibitor with an IC50 of 3.4 nM. KU-0058948 induces cell cycle arrest and apoptosis of primary myeloid leukemic cells and myeloid leukemic cell lines .
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- HY-163451
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Apoptosis
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Cancer
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Apoptosis inducer 17 is a Curcumin-Piperlongumine hybrid molecule that increases cell cycle arrest and apoptosis through activating JNK signaling pathway in lung cancer cells .
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- HY-158407
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Apoptosis
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Cancer
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Anticancer agent 220 is a chromanone derivative with anticancer effects. Anticancer agent 220 shows highly potent activity in the colon cancer cell lines. Anticancer agent 220 induces apoptosis and cell cycle arrest in cells .
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- HY-W154265
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Glutathione S-transferase
Apoptosis
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Cancer
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2,2′-Dihydroxychalcone, a flavonoid, is a glutathione S-transferase (GST) inhibitor with an IC50 of 28.9 μM in human colon cancer cells. 2,2′-Dihydroxychalcone induces cell cycle arrest and apoptosis in prostate cancer cells. 2,2′-Dihydroxychalcone has anticancer and anti-inflammatory properties .
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- HY-N1342
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Apoptosis
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Cancer
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Rocaglaol induces apoptosis and cell cycle arrest in LNCaP cells .
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- HY-N12717
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Apoptosis
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Cancer
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Casuarinin is an active product that can be isolated from the bark of Terminalia arjuna. Casuarinin induces apoptosis and cell cycle arrest .
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- HY-163444
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Apoptosis
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Cancer
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Apoptosis inducer 15 (Compound 3) induces cell apoptosis and cell cycle arrest at G2/M phase. Apoptosis inducer 15 is cytotoxicitic without causing DNA fragmentation .
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- HY-N7707
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Apoptosis
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Cancer
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Sandacanol is a specific agonist of olfactory receptor (OR10H1). Sandacanol induces cell cycle arrest and some apoptosis in bladder cancer cells .
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- HY-N1983
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Apoptosis
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Cancer
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Caudatin is a steroidal cmpound found in Cynanchum auriculatum, causes cell cycle arrest and induces apoptosis, with anti-cancer and antiangiogenic properties .
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- HY-18952A
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FLT3
Apoptosis
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Cancer
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(Z)-SU5614 is a potent FLT3 inhibitor and selectively induces growth arrest, apoptosis, and cell cycle arrest in Ba/F3 and AML cell lines expressing a constitutively activated FLT3 .
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- HY-19331
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GLUT
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Cancer
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WZB117 is a glucose transporter 1 (Glut1) inhibitor, which downregulates glycolysis, induces cell-cycle arrest, and inhibits cancer cell growth in vitro and in vivo.
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- HY-N10188
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Others
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Cancer
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Nidurufin is a potent cell cycle inhibitor with antitumor activity.Nidurufin induces in vitro cell cycle arrest at G2/M transition in the K562 cell line in a concentration and time dependent manner(IC50=12.6 μM) .
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- HY-149343
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Apoptosis
Autophagy
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Cancer
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Anticancer agent 132 (compound Rh1) is an inducer of apoptosis and autophagy with antitumor and antimetastasis activity. Anticancer agent 132 arrests cell cycle and inhibits cell proliferation .
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- HY-124261
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Apoptosis
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Cancer
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Sampangine is an alkaloid that induces apoptosis by inducing cell cycle arrest in the G0/G1 phase. Sampangine can inhibit the biosynthesis of heme .
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- HY-N9534
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Reactive Oxygen Species
Apoptosis
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Cancer
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Xylopine is an aporphine alkaloid with cytotoxic activity on cancer cells. Xylopine induces oxidative stress, causes G2/M cell cycle arrest and apoptosis in cancer cells .
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- HY-100508
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HDAC
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Cancer
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ITSA-1 is an activator of histone deacetylase (HDAC), and counteract trichostatin A (TSA)-induced cell cycle arrest, histone acetylation, and transcriptional activation .
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- HY-169101
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Apoptosis
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Cancer
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KSRP-IN-1 (compound 8) is a KSRP inhibitor that induces Apoptosis and cell cycle arrest. KSRP-IN-1 has antitumor activity .
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- HY-150571
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Topoisomerase
c-Myc
Apoptosis
ROS Kinase
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Cancer
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Anticancer agent 76 (Compound CT2-3) is an anticancer agent. Anticancer agent 76 significantly inhibits the proliferation of human NSCLC cells, induces cell cycle arrest, causes ROS generation and induces cell apoptosis .
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- HY-N1516
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Apoptosis
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Cancer
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Ganoderenic acid D is a triterpene identified from the effective compounds of Ganoderma lucidum extract (GLE). Ganoderenic acid D inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis .
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- HY-139828
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Apoptosis
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Cancer
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Anticancer agent 14 is a lead compound (IC50: 0.20 to 0.65 μM) that induces apoptosis, cell cycle arrest, and loss of mitochondrial membrane potential in breast cancer cells.
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- HY-N1039A
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Others
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Cancer
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Manool is a diterpene from Salvia officinalis. Manool induces selective cytotoxicity in cancer cells. Manool arrests the cancer cells at the G(2)/M phase of the cell cycle .
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- HY-111244
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Others
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Others
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DCB-3503 is a small molecule inhibitor of cell cycle progression, which has the activity of inducing G?/G? phase arrest and apoptosis in human hepatoma cells. DCB-3503 can inhibit the proliferation of human hepatoma cells, induce cell cycle arrest and apoptosis, and its mechanism is related to downregulating cyclin-dependent kinase (CDK) 2, CDK4 and CDK6, while activating PARP, caspase-3, caspase-9 and Bax, and downregulating Bcl-2.
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- HY-116204
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Others
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Others
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SKLB70326 is a small molecule inhibitor of cell cycle progression, which has the activity of inducing G?/G? phase arrest and apoptosis in human hepatoma cells. SKLB70326 can inhibit the proliferation of human hepatoma cells, induce cell cycle arrest and apoptosis, and its mechanism is related to downregulating cyclin-dependent kinase (CDK) 2, CDK4 and CDK6, while activating PARP, caspase-3, caspase-9 and Bax, and downregulating Bcl-2.
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- HY-13216
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HDAC
Apoptosis
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Cancer
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Pyroxamide is a potent inhibitor of histone deacetylase 1 (HDAC1) with an ID50 of 100 nM. Pyroxamide can induce apoptosis and cell cycle arrest in leukemia .
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- HY-N6744
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Apoptosis
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Infection
Cancer
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Chaetoglobosin A, the active principle within the extract of Penicillium aquamarinium, is a member of the cytochalasan family. Chaetoglobosin A preferentially induces apoptosis. Chaetoglobosin A targets filamentous actin in CLL cells and thereby induces cell-cycle arrest and inhibits membrane ruffling and cell migration .
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- HY-112314
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Src
Bcr-Abl
Apoptosis
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Cancer
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AZD0424 is an orally active, and dual selective Src/Abl kinase inhibitor with potential antineoplastic activity . AZD0424 induces apoptosis and cell cycle arrest in lymphoma cells .
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- HY-N0726
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Dracohodin perochlorate
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Apoptosis
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Cancer
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Dracorhodin perchlorate (Dracohodin perochlorate) is a natural product extracted from a natural medicine Dragon's blood. Dracorhodin perchlorate inhibits cell proliferation and induces cell cycle arrest and apoptosis .
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- HY-N6038
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Autophagy
Fungal
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Cancer
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Gartanin is a natural xanthone of mangosteen, with antioxidant, anti-inflammatory, antifungal, neuroprotective and antineoplastic properties. Gartanin induces cell cycle arrest and autophagy and suppresses migration in human glioma cells .
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- HY-N0048
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Apoptosis
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Cancer
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Polyphyllin II is one of the most significant saponins in Rhizoma Paridis and has toxic effects on kinds of cancer cells. Polyphyllin II induces apoptosis through caspases activation and cell-cycle arrest .
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- HY-B1787
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mTOR
Drug Metabolite
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Cancer
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Sulindac sulfone is an mTORC1 pathway inhibitor and a metabolite of Sulindac. Sulindac sulfone inhibits colon cancer cell growth and induces cell cycle arrest. Sulindac sulfone is used in cancer research .
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- HY-117465
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Others
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Cancer
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HAC-Y6 has anticancer activity via cell cycle arrest. HAC-Y6 induces apoptosis in COLO 205 cells with an IC50 of 0.52 µM .
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- HY-152245
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Epigenetic Reader Domain
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Cancer
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Physachenolide C is a potent and selective BET inhibitor that induces apoptosis and arrests the cell cycle in the G0-G1 phase, with antitumor activity .
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- HY-127067
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Akt
EGFR
mTOR
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Inflammation/Immunology
Cancer
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Yuanhuadin, extracted from Genkwa Flos Daphne genkwa, has antitumor activity through inhibiting Akt/mTOR and EGFR pathways, induce cell-cycle arrest and abortion .
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- HY-161763
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Microtubule/Tubulin
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Cancer
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Tubulin polymerization-IN-65 is a tubulin polymerisation inhibitor with a broad spectrum cytotoxic. Tubulin polymerization-IN-65 induces G2 + M cell cycle arrest .
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- HY-122249
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Microtubule/Tubulin
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Cancer
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MT-7 is a potent mitotic inhibitor. MT-7 shows antiproliferative activity. MT-7 induces cell cycle arrest at G2/M phase. MT-7 induces specific, reversible mitotic arrest and inhibits the polymerization of cellular microtubules .
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- HY-N10670
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Methylpluviatolide
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Apoptosis
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Cancer
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Bursehernin (Methylpluviatolide) is an antitumor agent. Bursehernin induces Apoptosis and cell cycle arrest at G2/M phase. Bursehernin shows anti-proliferative activity .
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- HY-136489A
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PARP
Apoptosis
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Cancer
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KU-0058948 hydrochloride is a specific and potent PARP1 inhibitor with an IC50 of 3.4 nM. KU-0058948 hydrochloride induces cell cycle arrest and apoptosis of primary myeloid leukemic cells and myeloid leukemic cell lines .
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- HY-18621
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OTS514
3 Publications Verification
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TOPK
Apoptosis
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Cancer
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OTS514 is a highly potent TOPK inhibitor with an IC50 of 2.6 nM. OTS514 strongly suppresses the growth of TOPK-positive cancer cells . OTS514 induces cell cycle arrest and apoptosis .
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- HY-N0800
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(-)-Protosappanin B
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Apoptosis
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Cancer
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Protosappanin B is a phenolic compound extracted from Caesalpinia sappan. Anti-cancer activity . Protosappanin B induces apoptosis and causes G1 cell cycle arrest in human bladder cancer cells .
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- HY-N4171
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Apoptosis
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Inflammation/Immunology
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Dihydrocucurbitacin B, a triterpene isolated from Cayaponia tayuya roots, inhibits nuclear factor of activated T cells (NFAT), induces cell cycle arrested in the G0 phase, and inhibits delayed type hypersensitivity .
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- HY-N12603
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Apoptosis
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Cancer
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Typhatifolin B (Compd 2), an anti-cancer agent, could remarkably induce cell apoptosis and G0/G1 cycle arrest, as well as block cell migration and invasion .
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- HY-121512
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HDAC
Apoptosis
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Cancer
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SK-7041 is a HDAC inhibitor with the IC50 of 172 nM. SK-7041 induces the hyperacetylation of histones H3 and H4 .SK-7041 inhibits tumor cell growth in vivo and in vitro, induces cell apoptosis, and arrests cell cycle at the G1 phase .
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- HY-N11050
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Apoptosis
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Cancer
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Xerophilusin B, an anticancer agent isolated from Isodon xerophilus, exhibits antiproliferative effects on esophageal squamous cell carcinoma (ESCC) cell lines, induces G2/M cell cycle arrest, and mediates apoptosis .
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- HY-N11645
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GA-Mf
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Apoptosis
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Cancer
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Ganoderic acid Mf is an antitumor triterpenoid. Ganoderic acid Mf causes cell cycle arrest in the G1 phase. Ganoderic acid Mf shows high selectivity between normal and cancer cells and induces cell apoptosis via mitochondria mediated pathway .
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- HY-133838
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BM41440
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Parasite
PKC
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Infection
Cancer
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Ilmofosine (BM41440) is a potent and selective protein kinase C inhibitor. Ilmofosine induces cell cycle arrest at the G2 phase. Ilmofosine also is an anti-leishmanial agent .
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- HY-120836
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DNA/RNA Synthesis
Apoptosis
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Cancer
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AOH1160 is a potent oral small molecule proliferating cell nuclear antigen (PCNA) inhibitor that interferes with DNA replication, blocks homologous recombination-mediated DNA repair, leads to cell cycle arrest and induces apoptosis .
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- HY-120140
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- HY-13566
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CKD-602 free base
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Topoisomerase
Apoptosis
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Cancer
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Belotecan (CKD-602 free base) is a DNA topoisomerase I inhibitor. Belotecan induces cell apoptosis and cell-cycle arrest. Belotecan is a camptothecin analogue with anti-tumor effects, it can be used for the research of cancer .
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- HY-152099
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Apoptosis
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Cancer
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Antiproliferative agent-19 (compound 4a) is an anti-cancer agent that exerts anti-proliferative effects on lung cancer cells by inducing apoptosis. antiproliferative agent-19 also induces cell cycle arrest in the G2/M phase .
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- HY-126324
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Apoptosis
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Cancer
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IV-23 (Compound 20) is a potent Noxa mediated apoptosis inducer, and it is a promising anticancer agent with potential. IV-23 inhibits cell growths in vitro and in vivo, reduces colony formation, arrests cell cycle at M phase, and induces esophageal squamous cell carcinoma (ESCC) .
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- HY-10222
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BMS-247550; Aza-epothilone B
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Microtubule/Tubulin
Apoptosis
Bacterial
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Cancer
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Ixabepilone (BMS-247550) is an orally bioavailable?microtubule?inhibitor, which binds to tubulin and promotes tubulin polymerization and microtubule stabilization, thereby arrests cells in the G2-M phase of the cell cycle and induces tumor cell apoptosis.
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- HY-150655
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HSP
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Cancer
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Hsp90-IN-15 is an Hsp90 inhibitor with anticancer activity. Hsp90-IN-15 induces cell apoptosis, arrests the cell cycle at S phase and decreases the expression level of Hsp90 in Hela cell .
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- HY-159096
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Apoptosis
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Cancer
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Apoptosis inducer 21 (Compound 5h) inhibits the proliferation of lung cancer cell H69AR with an IC50 of 1.58 μM. Apoptosis inducer 21 arrests the cell cycle at G0/G1 phase, induces apoptosis in H69AR .
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- HY-151905
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c-Met/HGFR
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Cancer
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D6808 is a highly selective and potent c‑Met inhibitor with an IC50 value of 2.9 nM. D6808 induces cell apoptosis and cell cycle arrest. D6808 can be used for the research of NSCLC and gastric cancers .
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- HY-126412
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Apoptosis
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Cancer
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Neochamaejasmine A is a biflavonoid that can be isolated from the roots of Stellera chamaejasme L.. Neochamaejasmine A inhibits proliferation, induces cell cycle arrest and apoptosis in tumor cells. Neochamaejasmine A can be used in the research of cancers such as prostate cancer, hepatoma cancer .
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- HY-168620
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CDK
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Cancer
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CDK6-IN-1 (compound 4i) is a CDK6 inhibitor. CDK6-IN-1 inhibits cell growth and induces cell cycle arrest at G1-phase .
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- HY-N11774
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Apoptosis
Caspase
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Cancer
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Euphornin is a anticaner agent, that can be isolated from E. helioscopia. Euphornin induces apoptosis via caspase-mediated pathways. Euphornin induces cell cycle arrest by increasing the level of the phospho-CDK1 (Tyr15) protein .
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- HY-143302
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Apoptosis
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Cancer
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Anticancer agent 31 is a 1,3-diphenylurea quinoxaline derivative, and a anticancer agent. Anticancer agent 31 exhibits antitumor acitvity by arresting cell cycle at S phase and inducing apoptosis .
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- HY-N2602
-
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MDM-2/p53
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Cancer
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Sanggenol L induces caspase-dependent and caspase-independent apoptosis in melanoma skin cancer cells . Sanggenol L induces of apoptosis via suppression of PI3K/Akt/mTOR signaling and cell cycle arrest via activation of p53 in p
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- HY-135217
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Apoptosis
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Cancer
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Apiole is an anti-tumor agent that induces apoptosis and inhibits human colon cancer cells by inducing G0/G1 cell cycle arrest. Apiole also significantly inhibited colon tumor development in an in vivo mouse xenograft model .
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- HY-161814
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Apoptosis
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Metabolic Disease
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Apoptosis inducer 20 (12) causes G2/M cell cycle arrest and induction of apoptosis via caspase 3/7 activation, which occurred during M arrest. Apoptosis inducer 20 is a novel indolic benzenesulfonamide with anti-proliferative effect against a broad panel of cancer cell lines, which is proming for research of new anti-mitotic agents .
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- HY-N2374
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Apoptosis
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Cancer
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Eupatorin, a naturally occurring flavone, arrests cells at the G2-M phase of the cell cycle and induces apoptotic cell death involving activation of multiple caspases, mitochondrial release of cytochrome c and poly(ADP-ribose) polymerase cleavage .
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- HY-13563
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T138067
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Microtubule/Tubulin
Apoptosis
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Cancer
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Batabulin (T138067) is an antitumor agent, which binds covalently and selectively to a subset of the β-tubulin isotypes, thereby disrupting microtubule polymerization. Batabulin affects cell morphology and leads to cell-cycle arrest ultimately induces apoptotic cell death .
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- HY-13563A
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T138067 sodium
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Microtubule/Tubulin
Apoptosis
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Cancer
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Batabulin sodium (T138067 sodium) is an antitumor agent, which binds covalently and selectively to a subset of the β-tubulin isotypes, thereby disrupting microtubule polymerization. Batabulin sodium affects cell morphology and leads to cell-cycle arrest ultimately induces apoptotic cell death .
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- HY-125612
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5'-Hydroxymorusin
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Apoptosis
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Cancer
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Artonin E (5'-Hydroxymorusin) is a known prenylated flavonoid that induces apoptosis and arrests the cell cycle in S phase. Artonin E can induce anti-proliferative effects through mitochondrial pathway dysregulation and can be used in cancer research .
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- HY-N1255
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(-)-Scoulerine; Discretamine
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Microtubule/Tubulin
Beta-secretase
Apoptosis
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Cancer
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Scoulerine ((-)-Scoulerine), an isoquinoline alkaloid, is a potent antimitotic compound. Scoulerine is also an inhibitor of BACE1 (?-site amyloid precursor protein cleaving enzyme 1). Scoulerine inhibits proliferation, arrests cell cycle, and induces apoptosis in cancer cells .
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- HY-N10798
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(-)-Kusunokinin
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Apoptosis
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Cancer
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Kusunokinin ((-)-Kusunokinin) is a nature product that could be isolated form P. nigrum. Kusunokinin has anticancer activity. Kusunokinin arrests cell cycle at G2/M phase and induce apoptosis .
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- HY-163924
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Apoptosis
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Cancer
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Apoptosis inducer 25 (Compound 4H) inhibits the proliferation of cell BGC-823 with IC50 of 0.37 μM. Apoptosis inducer 25 arrests cell cycle at G2/M phase, induces apoptosis in cell BGC-823, and causes mitochondrial dysfunction. Apoptosis inducer 25 exhibits good pharmacokinetic properties in rats .
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- HY-N11600
-
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Apoptosis
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Cancer
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β-Apopicropodophyllin is a nature product that could be isolated from Hyptis wticillata.β-Apopicropodophyllin induces apoptosis by inducing microtubule disruption, DNA damage, cell cycle arrest and ER stress. β-Apopicropodophyllin can be used in research of cancer .
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- HY-162311
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Ferroptosis
Autophagy
Reactive Oxygen Species
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Cancer
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Anticancer agent 194 (compound 10p) is a ferroptosis and autophagy inducer. Anticancer agent 194 arrests colon cancer cell cycle at G2/M phase, but can't induce cell apoptosis. Anticancer agent 194 independently triggeres cell ferroptosis and autophagy through the massive accumulation of ROS .
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- HY-N13123
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Apoptosis
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Cancer
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Tenacissoside C is an anti-cancer compound that inhibits angiogenesis. Tenacissoside C induces apoptosis in cancer cells by down-regulating the expression of anti-apoptotic factors and activating caspase-9 and caspase-3. Tenacissoside C also causes cell cycle arrest in cancer cells and induces apoptosis through the mitochondrial pathway.
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- HY-116664
-
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Apoptosis
Ras
Raf
Caspase
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Cancer
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DPQZ is an anti-tubulin agent that inhibits cell separation and induces cell cycle arrest at the G2/M phase. In addition, DPQZ induces caspase-dependent apoptosis of HSC-3 cells by inhibiting Ras/Raf and activating MAP kinase. DPQZ can be used in the study of oral cancer .
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- HY-N6016
-
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Apoptosis
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Cancer
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Bacopaside II, an extract from the medicinal herb Bacopa monnieri, blocks the Aquaporin-1 (AQP1) water channel and impairs migration of cells that express AQP1. Bacopaside II induces cell cycle arrest and apoptosis .
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- HY-156266
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Rhiz
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Others
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Cancer
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Rhizochalinin (Rhiz) is a cytotoxic sphingolipid. Rhizochalinin (Rhiz) counteracts glioblastoma cell proliferation by inducing apoptosis, G2/M-phase cell cycle arrest, and inhibition of autophagy. Rhizochalinin (Rhiz) can be used for human glioblastoma research .
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- HY-118748
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SRF
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Microtubule/Tubulin
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Cancer
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Suprafenacine is a cell permeable, tubulin-destabilizing molecule which bind microtubules at the colchicine-binding site and inhibit polymerization. Suprafenacine can induce G2/M cell cycle arrest and apoptosis, and can be used for cancer research .
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- HY-161339
-
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Apoptosis
Sirtuin
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Cancer
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SIRT2-IN-13 (compound 7c) is an inhibitor of SIRT2 and induces apoptosis. SIRT2-IN-13 selectively inhibits colon cancer and leukemia cells and arrests the cell cycle in the G2 phase .
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- HY-N6012
-
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Apoptosis
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Inflammation/Immunology
Cancer
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(-)-Alkannin, found in Alkanna tinctoria, is used as a food coloring. (-)-Alkannin shows anticancer activity, arrests cell cycle, and induces apoptosis. (-)-Alkannin improves hepatic inflammation in a Rho-kinase pathway .
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- HY-147848
-
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Microtubule/Tubulin
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Cancer
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Tubulin polymerization-IN-27 (compound 5j) is a tubulin polymerization inhibitor. Tubulin polymerization-IN-27 can arrest cell cycle at G2/M phase and induce apoptosis .
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- HY-147824
-
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Microtubule/Tubulin
Apoptosis
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Cancer
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Tubulin polymerization-IN-22 is a tubulin polymerization inhibitor with an IC50 of 8.1 μM. Tubulin polymerization-IN-22 arrests cell cycle at G2/M phase and induces apoptosis .
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- HY-146163
-
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Topoisomerase
Apoptosis
|
Cancer
|
|
Topoisomerase II inhibitor 7 (compound 3a) is a potent inhibitor of topoisomerase II alpha subtype, with an IC50 of 3.19 μM. Topoisomerase II inhibitor 7 can induce cell cycle arrest and apoptosis .
|
-
- HY-113471
-
|
|
Apoptosis
HSV
|
Infection
Inflammation/Immunology
Cancer
|
|
Perillic acid is the metabolite of Perillyl alcohol (HY-N7000). Perillic acid induces lung cancer cell cycle arrest and apoptosis. Perillic acid shows anti-HSV-1 and immunomodulatory activities .
|
-
- HY-126423
-
|
Isorhamnetin 3-O-glucuronide
|
Apoptosis
|
Cancer
|
|
Isorhamnetin 3-glucuronide is a potent anticancer agent. Isorhamnetin 3-glucuronide shows anti-proliferative activity. Isorhamnetin 3-glucuronide induces Apoptosis and cell cycle arrest at S-phase .
|
-
- HY-162625
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulin inhibitor 47 (compound C11) is a potent tubulin inhibitor. Tubulin inhibitor 47 induces apoptosis and cell cycle arrest at the M phase. Tubulin inhibitor 47 shows anti-tumor activity .
|
-
- HY-N1983R
-
|
|
Apoptosis
|
Cancer
|
|
Caudatin (Standard) is the analytical standard of Caudatin. This product is intended for research and analytical applications. Caudatin is a steroidal cmpound found in Cynanchum auriculatum, causes cell cycle arrest and induces apoptosis, with anti-cancer and antiangiogenic properties .
|
-
- HY-N1338
-
|
NSC 122417
|
mTOR
Akt
|
Cancer
|
|
Royleanone, a diterpenoid isolated from plants, inhibits the proliferation of cancer cells by inducing cell cycle arrest and mitochondria-mediated apoptosis, also inhibits cell migration potential, inhibits mTOR/PI3/AKT signaling pathway in LNCaP prostate cancer cells .
|
-
- HY-N0036
-
|
(+)-Costunolide; Costus lactone
|
Apoptosis
Endogenous Metabolite
|
Cancer
|
|
Costunolide ((+)-Costunolide) is a naturally occurring sesquiterpene lactone, with antioxidative, anti-inflammatory, antiallergic, bone remodeling, neuroprotective, hair growth promoting, anticancer, and antidiabetic properties. Costunolide can induce cell cycle arrest and apoptosis on breast cancer cells .
|
-
- HY-P2698
-
|
|
HDAC
Apoptosis
|
Cancer
|
|
1-Alaninechlamydocin, a cyclic tetrapeptide, is a potent HDAC inhibitor (IC50=6.4 nM). 1-Alaninechlamydocin induces G2/M cell cycle arrest and apoptosis in MIA PaCa-2 cells .
|
-
- HY-146754
-
|
|
MMP
Apoptosis
|
Cancer
|
|
MMP2-IN-1 is a moderate potenet MMP2 inhibitor with IC50 of 6.8 µM. MMP2-IN-1 exhibits remarkable antiproliferative activity in certain cancer cells by arresting the cell cycle and inducing apoptosis .
|
-
- HY-108164
-
|
|
Apoptosis
Bcl-2 Family
Caspase
|
Cancer
|
|
Aspidin BB is a phloroglucinol derivative, which can be isolated from the aerial part of Dryopteris championii. Aspidin BB has anticancer activity. Aspidin BB induces cell cycle arrest and apoptosis in human ovarian HO-8910 cells .
|
-
- HY-156298
-
|
|
PARP
Apoptosis
|
Cancer
|
|
PARP1-IN-16 (compound 12a) is a potent PARP1 inhibitor, with an IC50 of 1.89 nM. PARP1-IN-16 can arrest the cell cycle in S phase and induce apoptosis in HCT-116 cells .
|
-
- HY-13629
-
-
- HY-13768C
-
|
SKF 104864A hydrochloride hydrate; NSC 609669 hydrochloride hydrate
|
Topoisomerase
Apoptosis
Autophagy
|
Cancer
|
|
Topotecan hydrochloride hydrate is an orally active and potent Topoisomerase I inhibitor. Topotecan hydrochloride hydrate induces cell cycle arrest in G0/G1 and S phases and promotes apoptosis. Topotecan hydrochloride hydrate shows anticancer activity .
|
-
- HY-122151
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
MPT0B002 is a potent microtubule inhibitor with anticancer activities. MPT0B002 disrupts tubulin polymerization, induces apoptosis, and arrests cell cycle at the G2/M phase .
|
-
- HY-N7223
-
|
|
YAP
Apoptosis
|
Cancer
|
|
Lappaol F, a lignin, is an anticancer agent. Lappaol F inhibits YAP<、b> mRNA and protein level. Lappaol F inhibits tumor cell growth by inducing cell cycle arrest. Lappaol F induces cancer cell apoptosis, and inhibits tumor growth. Lappaol F can be isolated from Arctium lappa Linne (Asteraceae) .
|
-
- HY-W303895
-
|
|
Others
|
Others
Cancer
|
|
Luteolin (monohydrate) is the monohydrate of Luteolin. Luteolin (Luteoline), a flavonoid, is also a potent Nrf2 inhibitor. Luteolin has anti-inflammatory and anticancer properties, induces apoptosis and cell cycle arrest in multiple human cancer cell lines, including non-small lung cancer cells, and inhibits cell metastasis and angiogenesis .
|
-
- HY-101030
-
|
|
NEKs
Apoptosis
|
Cancer
|
|
MBM-17 is a potent NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 3 nM. It effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis. MBM-55 shows antitumor activities, and no obvious toxicity to mice .
|
-
- HY-N7496
-
|
|
Apoptosis
|
Cancer
|
|
Odoroside A is an active ingredient extracted from the leaves of Nerium oleander Linn. Odoroside A has anti-cancer activity. Odoroside A could induce apoptosis and cell cycle arrest through ROS/p53 signaling pathway, leading to the tumor cell death .
|
-
- HY-111524
-
|
|
HSP
Apoptosis
|
Cancer
|
|
CPUY201112 is a potent heat shock protein Hsp90 inhibitor with Kd of 27 nM. CPUY201112 induces p53-mediated apoptosis in MCF-7 cells, resulting in cell cycle arrest, which can be used in cancer research .
|
-
- HY-149849
-
|
|
Thymidylate Synthase
|
Cancer
|
|
TS-IN-2 (compound 17) is a thymidylate synthase (TS) inhibitor with an IC50 of 0.81 μM. TS-IN-2 induces cancer cell apoptosis and cell cycle arrest in S phase, and also inhibit DNA synthesis, resulting in DNA damage .
|
-
- HY-15611
-
|
|
CRM1
|
Cancer
|
|
KPT-185 is an orally bioavailable and selective inhibitor of CRM1 and displays potent antiproliferative properties at submicromolar concentrations (IC50=100-500 nM), induces apoptosis, cell-cycle arrest, and myeloid differentiation in AML cell lines and patient blasts .
|
-
- HY-162453
-
|
|
Apoptosis
MMP
|
Cancer
|
|
Anticancer agent 204 (Compound 6), a cinnamide fluorinated derivative, possesses anticancer activity. Anticancer agent 204 can arrest the cell cycle of HepG2 cells in the G1 phase and induce apoptosis by reducing the level of mitochondrial membrane polarization (MMP) .
|
-
- HY-124632
-
WJ460
2 Publications Verification
|
Ferroptosis
Autophagy
|
Cancer
|
|
WJ460 is a potent inhibitor of myoferlin (MYOF) that interacts directly with MYOF. WJ460 inhibits the migration and growth, induces cell cycle arrest, mitochondrial autophagy, lipid peroxidation and ferroptosis in tumor cells. WJ460 has anti-tumor activity .
|
-
- 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-129592
-
|
|
Apoptosis
|
Cancer
|
|
p-Tolylmaleimide (compound 9) is a naphthalimide derivative that has cytotoxic effects on cancer cells. p-Tolylmaleimide can arrest the cell cycle of human acute myeloid leukemia cells K562 in the sub-G0/G1 phase and induce apoptosis .
|
-
- HY-126566
-
|
|
Fungal
HDAC
Apoptosis
|
Infection
Cancer
|
|
Trichostatin C is an inhibitor for histone deacetylase (HDAC), induces apoptosis and arrests cell cycle at G2/M phase, and exhibits anticancer activity against lung cancer and urothelial bladder cancer . Trichostatin C induces differentation of Friend leukemic cells . Trichostatin C exhibits antifungal activity .
|
-
- HY-17548
-
|
|
Caspase
Apoptosis
|
Cancer
|
|
VMY-1-103 is an inhibitor for cyclin/Cdk complex, that arrests the cell cycle at G1 phase. VMY-1-103 reduces mitochondrial membrane potential, induces p53 phosphorylation and and PARP cleavage, activates caspase-3, and thus induces apoptosis in prostate cancer cell LNCaP .
|
-
- HY-113638
-
|
GS-456332
|
Stearoyl-CoA Desaturase (SCD)
Apoptosis
|
Cancer
|
|
CVT-11127 is a potent SCD inhibitor. CVT-11127 induces apoposis and arrests the cell cycle at the G1/S phase. CVT-11127 has the potential for the research of lung cancer .
|
-
- HY-147868
-
|
|
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
|
DC-CPin711 is a potent and selective inhibitor of CREB-binding protein (CBP) bromodomain with an IC50 of 0.0626 μM. DC-CPin711 arrests cell cycle at G1 phase and induces apoptosis .
|
-
- HY-163808
-
|
|
Apoptosis
|
Cancer
|
|
Anticancer agent 237 (compound 13) is a potent anticancer agent. Anticancer agent 237 shows cytotoxicity. Anticancer agent 237 induces apoptosis and cell cycle arrest at the S and G2/M phases .
|
-
- HY-N6031
-
-
- HY-155314
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin polymerization-IN-50 (compound 7n) is a inhibitor of tubulin polymerization, with the IC50 of 5.05 μM in SK-Mel-28 cells. Tubulin polymerization-IN-50 induces the cell cycle arrest in the G2/M phase .
|
-
- HY-N6038R
-
|
|
Autophagy
Fungal
|
Cancer
|
|
Gartanin (Standard) is the analytical standard of Gartanin. This product is intended for research and analytical applications. Gartanin is a natural xanthone of mangosteen, with antioxidant, anti-inflammatory, antifungal, neuroprotective and antineoplastic properties. Gartanin induces cell cycle arrest and autophagy and suppresses migration in human glioma cells .
|
-
- HY-N7695
-
|
|
Apoptosis
Autophagy
|
Cancer
|
|
Physalin B, one of the major active steroidal constituents of Cape gooseberry, induces cell cycle arrest and triggers apoptosis in breast cancer cells through modulating p53-dependent apoptotic pathway. Physalin B inhibits the ubiquitin-proteasome pathway and induces incomplete autophagic response in human colon cancer cells in vitro .
|
-
- HY-144361
-
|
|
Apoptosis
|
Cancer
|
|
Antitumor agent-44 (Compound 5n) disrupts the mitochondrial homeostasis, induces cell cycle arrest and apoptosis in human adenocarcinoma cells. Antitumor agent-44 (Compound 5n) possesses good anti-tumor activity in a lung-cancer-cell xenograft mice model .
|
-
- HY-146999
-
|
|
Histone Methyltransferase
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
|
YM458 is a potent EZH2 and BRD4 dual inhibitor with IC50s of 490 nM and 34 nM, respectively. YM458 inhibits cell proliferation and colony formation and induces cell cycle arrest and apoptosis in solid cancer cells. YM458 can be used for researching anticancer .
|
-
- HY-163923
-
|
|
Apoptosis
|
Cancer
|
|
Apoptosis inducer 24 (Compound 4) inhibits the proliferation of gastric cancer cells with IC50 of 1.2-4.8 μM. Apoptosis inducer 24 arrests cell cycle at G2/M phase, induces apoptosis in cell BGC-823, and causes mitochondrial dysfunction. Apoptosis inducer 24 exhibits antitumor efficacy in mice, without significant toxicity (LD50 is 91.2 mg/kg) .
|
-
- HY-N6576
-
|
|
Apoptosis
|
Cancer
|
|
Hellebrigenin, one of bufadienolides belonging to cardioactive steroids, is isolated from traditional Chinese medicine Venenum Bufonis. Hellebrigenin induces DNA damage and cell cycle G2/M arrest. Hellebrigenin triggers mitochondria-mediated apoptosis.
|
-
- HY-158775
-
|
|
Ferroptosis
Apoptosis
Autophagy
|
Cancer
|
|
Ferroptocide is a cell death inducer that triggers ferroptosis and has anti-tumor activity. Ferroptocide can induce oxidative stress, leading to G2/M cell cycle arrest and apoptosis activation in LNCaP cells, while also effectively inhibiting the cell viability of both LNCaP and TRAMP-C1 cells. Ferroptocide can be used to study its capability to induce mitochondrial autophagy and to trigger immunogenic cell death (ICD) in prostate cancer cells .
|
-
- HY-108474
-
|
AG 337
|
Thymidylate Synthase
|
Cancer
|
|
Nolatrexed dihydrochloride (AG 337) is a non-competitive lipophilic inhibitor of thymidylate synthase, interacts at the folate cofactor binding site of the enzyme, with a Ki of 11 nM for human thymidylate synthase . Nolatrexed dihydrochloride (AG 337) induces cell cycle arrest in S phase of cancer cells. Anti-cancer activity .
|
-
- HY-19826
-
|
|
DNA Methyltransferase
ADC Cytotoxin
Autophagy
Apoptosis
|
Cancer
|
|
Isofistularin-3 is a direct, DNA-competitive DNMT1 inhibitor, with an IC50 of 13.5 μM. Isofistularin-3, as a DNA demethylating agent, induces cell cycle arrest and sensitization to TRAIL in cancer cells. Isofistularin-3 can be used as an ADC cytotoxin .
|
-
- HY-139535
-
|
CG-806
|
FLT3
Btk
Apoptosis
|
Cancer
|
|
Luxeptinib (CG-806) is an orally active, reversible, first-in-class, non-covalent and potent pan-FLT3/pan-BTK inhibitor. Luxeptinib induces cell cycle arrest, apoptosis or autophagy in acute myeloid leukemia cells .
|
-
- HY-145762
-
|
|
Apoptosis
Histone Methyltransferase
|
Cancer
|
|
YM281 is a potent EZH2 inhibitor. YM281 induces cell apoptosis and cell cycle arrest at the G0/G1 phase. YM281 shows antitumor effects in vivo. YM281 has the potential for the research of lymphoma .
|
-
- HY-149348
-
|
|
Topoisomerase
PARP
Apoptosis
|
Cancer
|
|
DiPT-4 is a dual TOP1/PARP1 inhibitor that induces massive DNA double-strand breaks (DSBs), cell cycle arrest, and apoptosis in cancer cells. DiPT-4 has the potential to overcome cancer drug resistance .
|
-
- HY-163299
-
|
|
Ras
Apoptosis
|
Cancer
|
|
pan-KRAS-IN-5 (compound 15a) is a pan-KRAS translation inhibitor by targeting 5′-UTR RNA G-quadruplexes (rG4s). pan-KRAS-IN-5 induces cell cycle arrest and promptes apoptosis in KRAS-driven cancer cells .
|
-
- HY-162276
-
|
|
Reactive Oxygen Species
DNA/RNA Synthesis
|
Cancer
|
|
Anticancer agent 188 (compound D43) inhibits DNA synthesis in TNBC cells, leading to cell cycle arrest at the G2/M phase. Anticancer agent 188 has anti-cancer viability by inducing ROS-mediated apoptosis and DNA damage .
|
-
- HY-162291
-
|
|
Src
Apoptosis
|
Cancer
|
|
Lck-IN-3 (compound 7m) is an LCK inhibitor targeting acute lymphoblastic leukemia (ALL) that inhibits LCK phosphorylation. Lck-IN-3 can induce cell cycle arrest in the G2/M phase, leading to apoptosis in ALL cells .
|
-
- HY-117884
-
|
|
Apoptosis
|
Cancer
|
|
(Rac)-CCT 250863 (compound rac-21) is a selective and reversible NEK 2 inhibitor with an IC50 of 0.073 µM. (Rac)-CCT 250863 shows good effects of inducing cell cycle arrest and also can antiproliferative in cells (Pomalidomide sensitive/resistant). (Rac)-CCT 250863 induces apoptosis when combines with Pomalidomide .
|
-
- HY-125010
-
|
|
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
Dicycloplatin is a DNA damage inducer. Dicycloplatin induces DNA damage by activating biphosphorylated checkpoint kinase 2 (CHK2), breast cancer 1 (BRCA1) and triphosphorylated p53. Dicycloplatin can induce cell cycle arrest, inhibit proliferation and lead to apoptosis in prostate cancer PC3 cells and lung cancer NCI/H446 cells. Dicycloplatin can be used in cancer researchr .
|
-
- HY-107780
-
|
c-di-GMP; cyclic diguanylate; 5GP-5GP
|
STING
Endogenous Metabolite
|
Cancer
|
|
Cyclic-di-GMP is a STING agonist and a bacterial second messenger that coordinates different aspects of bacterial growth and behavior, including motility, virulence, biofilm formation, and cell cycle progression. Cyclic-di-GMP has anti-cancer cell proliferation activity and also induces elevated CD4 receptor expression and cell cycle arrest. Cyclic-di-GMP can be used in cancer research .
|
-
- HY-13721
-
|
Idronoxil; Dehydroequol; Haginin E
|
Caspase
Apoptosis
Topoisomerase
|
Cancer
|
|
Phenoxodiol (Idronoxil), a synthetic analog of Genestein, activates the mitochondrial caspase system, inhibits XIAP (an apoptosis inhibitor), and sensitizes the cancer cells to Fas-mediated apoptosis. Phenoxodiol also inhibits DNA topoisomerase II by stabilizing the cleavable complex. Phenoxodiol induces cell cycle arrest in the G1/S phase of the cell cycle and upregulates p21 WAF1 via a p53 independent manner .
|
-
- HY-107780A
-
|
c-di-GMP sodium; cyclic diguanylate sodium; 5GP-5GP sodium
|
STING
Endogenous Metabolite
|
Cancer
|
|
Cyclic-di-GMP sodium is a STING agonist and a bacterial second messenger that coordinates different aspects of bacterial growth and behavior, including motility, virulence, biofilm formation, and cell cycle progression. Cyclic-di-GMP sodium has anti-cancer cell proliferation activity and also induces elevated CD4 receptor expression and cell cycle arrest. Cyclic-di-GMP sodium can be used in cancer research .
|
-
- HY-101266
-
|
DS-3032
|
MDM-2/p53
E1/E2/E3 Enzyme
Apoptosis
|
Cancer
|
|
Milademetan (DS-3032) is a specific and orally active MDM2 inhibitor for the research of acute myeloid leukemia (AML) or solid tumors. Milademetan (DS-3032) induces G1 cell cycle arrest, senescence and apoptosis .
|
-
- HY-N6722
-
|
Tridolgosir
|
Apoptosis
Antibiotic
|
Infection
Cancer
|
|
Swainsonine (Tridolgosir) is an natural indolizidine alkaloid, a potent and reversible α-mannosidase inhibitor. Swainsonine induces apoptosis and cell cycle arrest at G2/M phase. Swainsonine shows anti-tumor activity .
|
-
- HY-101266B
-
|
DS-3032b; DS-3032 tosylate hydrate
|
MDM-2/p53
E1/E2/E3 Enzyme
Apoptosis
|
Cancer
|
|
Milademetan (DS-3032) tosylate hydrate is a specific and orally active MDM2 inhibitor for the research of acute myeloid leukemia (AML) or solid tumors. Milademetan (DS-3032) tosylate hydrate induces G1 cell cycle arrest, senescence and apoptosis .
|
-
- HY-18621A
-
|
|
TOPK
Apoptosis
|
Cancer
|
|
OTS514 hydrochloride is a highly potent TOPK inhibitor, which inhibits TOPK kinase activity with a median inhibitory concentration (IC50) value of 2.6 nM. OTS514 hydrochloride strongly suppresses the growth of TOPK-positive cancer cells . OTS514 hydrochloride induces cell cycle arrest and apoptosis .
|
-
- HY-143266
-
|
|
Topoisomerase
Apoptosis
|
Cancer
|
|
Topoisomerase I inhibitor 3 (Compound ZML-14) is a topoisomerase I inhibitor and can interact with topoisomerase I-DNA complex. Topoisomerase I inhibitor 3 induces HepG2 cell apoptosis and arrests cell cycle at G2/M phase .
|
-
- HY-149063
-
|
|
Apoptosis
|
Cancer
|
|
Antitumor agent-92, an Icaritin (HY-N0678) derivative, causes arrest at the G0/G1 phase in the cell cycle and induces cell apoptosis. Antitumor agent-92 has the potential for hepatocellular carcinoma (HCC) research .
|
-
- HY-N0726R
-
|
|
Apoptosis
|
Cancer
|
|
Dracorhodin perchlorate (Standard) is the analytical standard of Dracorhodin perchlorate. This product is intended for research and analytical applications. Dracorhodin perchlorate (Dracohodin perochlorate) is a natural product extracted from a natural medicine Dragon's blood. Dracorhodin perchlorate inhibits cell proliferation and induces cell cycle arrest and apoptosis .
|
-
- HY-116473
-
|
|
Others
|
Cancer
|
|
CFM-1 is a small molecule antagonist of CARP-1/APC-2 binding with an EC50 value of 4.1 μM. CFM-1 induces G2M cell cycle arrest and suppresses viabilities of human breast cancer cells .
|
-
- HY-168128
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin polymerization-IN-69 (compund 6c) significantly inhibits microtubule/tubulin polymerization in vitro (78.3% inhibition) with an IC50 value of 6.53 μM, and rapidly induces apoptotic cell death and G2/M cell cycle arrest in MCF-7 cells .
|
-
- HY-126856
-
|
|
HDAC
Apoptosis
|
Cancer
|
|
HC-Toxin, a cyclic tetrapeptide, is a potent HDAC inhibitor with an IC50 of 30 nM . HC-Toxin induces tumor cell apoptosis and has anticancer effects .
|
-
- HY-13768
-
|
SKF 104864A; NSC 609669
|
Topoisomerase
Autophagy
Apoptosis
|
Cancer
|
|
Topotecan (SKF 104864A; NSC 609669) is an orally active and potent Topoisomerase I inhibitor. Topotecan induces cell cycle arrest in G0/G1 and S phases and promotes apoptosis. Topotecan shows anticancer activity .
|
-
- HY-N0211
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
Cyasterone, a natural EGFR inhibitor, mainly isolated from Ajuga decumbens Thunb (Labiatae). Cyasterone manifests anti-proliferation effect by induced apoptosis and cell cycle arrests. Cyasterone may serves as a therapeutic anti-tumor agent against human tumors .
|
-
- HY-N7083
-
-
- HY-13630
-
|
BMY-40481
|
Topoisomerase
Bacterial
Autophagy
Apoptosis
|
Infection
Neurological Disease
Cancer
|
|
Etoposide phosphate (BMY-40481) is a potent anti-cancer chemotherapy agent and a selective topoisomerase II inhibitor to prevent re-ligation of DNA strands. Etoposide phosphate is the phosphate ester proagent of etoposide and is considered as active equivalent to Etoposide. Etoposide phosphate induces cell cycle arrest, apoptosis, and autophagy.
|
-
- HY-149530
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
EGFR-IN-86 (compound 4i) is an EGFR inhibitor (IC50: 1.5 nM) with high activity against glioblastoma. EGFR-IN-86 induces apoptosis and arrests the U87 cell cycle in the G2/M phase .
|
-
- HY-168504
-
|
|
Histone Demethylase
Apoptosis
|
Cancer
|
|
LSD1-IN-36 is a potent LSD1 inhibitor with an IC50 value of 0.8 nM. LSD1-IN-36 induces apoptosis and arrests the cell cycle. LSD1-IN-36 shows antitumor activity .
|
-
- HY-135217R
-
|
|
Apoptosis
|
Cancer
|
|
Apiole (Standard) is the analytical standard of Apiole. This product is intended for research and analytical applications. Apiole is an anti-tumor agent that induces apoptosis and inhibits human colon cancer cells by inducing G0/G1 cell cycle arrest. Apiole also significantly inhibited colon tumor development in an in vivo mouse xenograft model .
|
-
- HY-100507
-
-
- HY-P1126
-
|
DLS 15
|
Microtubule/Tubulin
ADC Cytotoxin
Apoptosis
|
Cancer
|
|
Dolastatin 15 (DLS 15), a depsipeptide derived from Dolabella auricularia, is a potent antimitotic agent structurally related to the antitubulin agent Dolastatin 10. Dolastatin 15 induces cell cycle arrest and apoptosis in multiple myeloma cells. Dolastatin 15 can be used as an ADC cytotoxin .
|
-
- HY-144340
-
|
|
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
Antitumor agent-43 (Compound 4B) is a potent antitumor agent, with an IC50of 0.5 µM for (T-24 cell). Antitumor agent-43 (Compound 4B) induces cell cycle arrest at G2/M phase .
|
-
- HY-113471A
-
|
|
Apoptosis
Bacterial
|
Infection
Cancer
|
|
(S)-(-)-Perillic acid is a terpenoid plant extract with antimicrobial and anticancer activities. (S)-(-)-Perillic acid induces cell apoptosis and cell cycle arrest, and increases the levell of Bax, Bcl2, p21 and caspase-3 proteins. (S)-(-)-Perillic acid can be used for cancer and infection research .
|
-
- HY-155232
-
|
|
PI3K
Apoptosis
|
Cancer
|
|
PI3Kδ-IN-16 is a potent and selective inhibitor of PI3Kδ. PI3Kδ-IN-16 has a strong anti-proliferative effect on cells, causing cell cycle arrest and inducing apoptosis .
|
-
- HY-161358
-
|
|
FAK
Apoptosis
|
Cancer
|
|
FAK-IN-20 (Compound 7b) is an inhibitor of FAK with an IC50 value of 0.27 nM. FAK-IN-20 exhibits anticancer activity. FAK-IN-20 can arrest the cell cycle in the G2/M phase and induce cell apoptosis by generating ROS .
|
-
- HY-18621B
-
|
|
Apoptosis
|
Others
|
|
(S)-OTS514 is the S enantiomer of OTS514 (HY-18621). OTS514 is a highly potent TOPK inhibitor with an IC50 of 2.6 nM. OTS514 strongly suppresses the growth of TOPK-positive cancer cells . OTS514 induces cell cycle arrest and apoptosis .
|
-
- HY-162763
-
|
|
Apoptosis
|
Cancer
|
|
FLQY2 is a camptothecin analog that exhibits outstanding antitumor efficacy against various solid tumors. FLQY2 possesses both in vitro and in vivo anti-pancreatic cancer activity, inhibiting cell proliferation, colony formation, inducing apoptosis, and causing cell cycle arrest at nanomolar concentrations .
|
-
- HY-10222R
-
|
|
Microtubule/Tubulin
Apoptosis
Bacterial
|
Cancer
|
|
Ixabepilone (Standard) is the analytical standard of Ixabepilone. This product is intended for research and analytical applications. Ixabepilone (BMS-247550) is an orally bioavailable microtubule inhibitor, which binds to tubulin and promotes tubulin polymerization and microtubule stabilization, thereby arrests cells in the G2-M phase of the cell cycle and induces tumor cell apoptosis.
|
-
- HY-145438
-
|
|
Others
|
Cancer
|
|
Antitumor agent-38 is a potent antitumor agents. Antitumor agent-38 shows antiproliferative activity for cancer cells. Antitumor agent-38 induces cell cycle arrest at the late S and G2/M phase without interfering with microtubule formation or cell morphology[1].
|
-
- HY-146409
-
|
|
Apoptosis
|
Cancer
|
|
Antitumor agent-59 (Compound 13b) is a potent antitumor agent. Antitumor agent-59 effectively inhibits the proliferation and migration of HCT116 cells. Antitumor agent-59 induces HCT116 cell apoptosis and arrests the cell cycle at the G2/M phase .
|
-
- HY-114545
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
5HPP-33 is an inhibitor for tubulin polymerization with IC50 of 8.1 μM. 5HPP-33 inhibits the proliferation of leukemia cell and multiple myeloma cells with IC50 of 1-10 μM, arrests the cell cycle at G2/M phase, and induces apoptosis .
|
-
- HY-10638
-
|
|
c-Kit
Apoptosis
|
Cancer
|
|
AP23464 is an ATP-based inhibitor for Kit, that inhibits the phosphorylation of Kit wildtype and mutants, with IC50 of 5-85 nM. AP23464 inhibits the proliferation of Kit mutated cells (IC50 is 3-20 nM), arrests the cell cycle at G0/G1 phase, and induces apoptosis in Kit mutated cells .
|
-
- HY-N13164
-
|
|
PI3K
Akt
Apoptosis
|
Cancer
|
Polygalacin D3 is a triterpenoid saponin compound that can be extracted from the roots of the balloon flower. Polygalacin D3 can inhibit the proliferation of non-small cell lung cancer (NSCLC) cell lines by blocking the PI3K/Akt pathway, and it induces cell cycle arrest and cell apoptosis .
|
-
- HY-107780B
-
|
c-di-GMP diammonium; cyclic diguanylate diammonium; 5GP-5GP diammonium
|
STING
Endogenous Metabolite
|
Cancer
|
|
Cyclic-di-GMP diammonium is a STING agonist and a bacterial second messenger that coordinates different aspects of bacterial growth and behavior, including motility, virulence, biofilm formation, and cell cycle progression. Cyclic-di-GMP diammonium has anti-cancer cell proliferation activity and also induces elevated CD4 receptor expression and cell cycle arrest. Cyclic-di-GMP diammonium can be used in cancer research .
|
-
- HY-110382
-
|
c-di-GMP disodium; cyclic diguanylate disodium; 5GP-5GP disodium
|
STING
Endogenous Metabolite
|
Cancer
|
|
Cyclic-di-GMP disodium is a STING agonist and a bacterial second messenger that coordinates different aspects of bacterial growth and behavior, including motility, virulence, biofilm formation, and cell cycle progression. Cyclic-di-GMP disodium has anti-cancer cell proliferation activity and also induces elevated CD4 receptor expression and cell cycle arrest. Cyclic-di-GMP disodium can be used in cancer research .
|
-
- HY-W127705
-
|
|
Fluorescent Dye
|
Others
|
|
Quinacrine mustard dihydrochloride is a fluorochrome. Quinacrine mustard dihydrochloride as a polycyclic aromatic agent can be used as mutagenic agent induces the mutants of bacteria. Quinacrine mustard dihydrochloride induces cell cycle arrest at G2/M-phase. Quinacrine mustard dihydrochloride has the potential for the research of plant, animal, or human chromosomes .
|
-
- HY-14661
-
|
|
Kinesin
|
Cancer
|
|
SB-743921 free base is a potent selective inhibitor of the mitotic kinesin KSP (Eg5), with a Ki of 0.1 nM. SB-743921 free base can induce mitotic arrest, block cell cycle progression, induce apoptosis, and can be used in the research of myeloma, leukemia and other diseases .
|
-
- HY-148870
-
|
|
ADC Cytotoxin
|
Cancer
|
|
Maytansinoid B is a kind of ADC Cytotoxin. Maytansinoid B can be used to conjugates with antibodies to form antibody-drug conjugates (ADCs). Maytansinoids are known as antimitotic agents, binding to tubulin and inhibiting microtubule assembly. Maytansinoids induces G2/M arrest in the cell cycle to induce apoptosis .
|
-
- HY-144733
-
|
|
Estrogen Receptor/ERR
Apoptosis
|
Cancer
|
|
ERα antagonist 1 (Compound 19d) is a potent, selective, covalent estrogen receptor α (ERα) antagonist. ERα antagonist 1 induces apoptosis and cell cycle G0/G1 phase arrest in MCF-7 cells .
|
-
- HY-131724
-
|
p-DDAP; p-Dodecylaminophenol
|
Apoptosis
|
Cancer
|
|
4-(Dodecylamino)phenol (p-DDAP) is an anticancer agent. 4-(Dodecylamino)phenol has anti-tumor activity and can suppress proliferation, arrest the cell cycle and induce apoptotic cell death. 4-(Dodecylamino)phenol can be used for the research of cancer, such as prostate cancer .
|
-
- HY-151978
-
|
|
Indoleamine 2,3-Dioxygenase (IDO)
Apoptosis
|
Cancer
|
|
ZC0109 is a dual inhibitor of IDO1 and thioredoxin reductase 1 (TrxR1) with IC50s of 50 nM and 3.0 μM, respectively. ZC0109 induces ROS accumulation and cell cycle arrest at G1/S phase, thus leads to cancer cells apoptosis .
|
-
- HY-146806
-
|
|
MDM-2/p53
|
Cancer
|
|
YL93 is a dual inhibitors of MDM2/4 with Ki values of 0.64 μM and 1.1 nM for MDM4 and MDM2, respectively. YL93 induces cell-cycle arrest and apoptosis. YL93 shows p53-dependent cell growth inhibition .
|
-
- HY-162352
-
|
|
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
|
SDU-071 is a potent and orally active inhibitor of BRD4-p53 inhibitor. SDU-071 inhibits MDA-MB-231 cells proliferation with an IC50 of 10.5 μM. SDU-071 induces cell cycle arrest and apoptosis .
|
-
- HY-163622
-
|
|
Apoptosis
|
Cancer
|
|
USP10-IN-3 (compound D1) is a potent USP10 inhibitor with an IC50 value of 7.2 µM. USP10-IN-3 inhibits cell proliferation. USP10-IN-3 induces apoptosis and cell cycle arrest at S-phase .
|
-
- HY-168263
-
|
|
Histone Methyltransferase
Apoptosis
|
Cancer
|
|
PRMT5-IN-45 (compound 36) is a potent and selective PRMT5 inhibitor with an IC50 of 3 nM. PRMT5-IN-45 potently reduces the level of symmetric dimethylarginines (sDMA) and inhibits the proliferation of MOLM-13 cell lines by inducing apoptosis and cell cycle arrest .
|
-
- HY-126067
-
|
|
Glycosidase
Apoptosis
|
Inflammation/Immunology
|
|
(-)-Pinoresinol is a plant-derived tetrahydrofuran lignan that inhibits α-glucosidase and acts as a hypoglycemic agent. (-)-Pinoresinol has some anti-inflammatory effects and acts as a chemopreventive agent, inducing increased apoptosis and cell cycle G2/M arrest .
|
-
- HY-155339
-
|
|
Apoptosis
DNA/RNA Synthesis
|
Cancer
|
|
Anticancer agent 168 (compound d16) is a inhibitor of DNA2. Anticancer agent 168 induces apoptosis and cell-cycle arrest mainly at S-phase, and exhibits anticancer activities and overcomes chemotherapy resistance in mutp53-bearing cancers .
|
-
- HY-169106
-
|
|
Topoisomerase
Apoptosis
|
Cancer
|
|
Topoisomerase inhibitor 4 (compound 45) is a potent Topoisomerase1/2 inhibitor. Topoisomerase inhibitor 4 causes cell cycle arrest in the G2/M phase by inducing Apoptosis. Topoisomerase inhibitor 4 has antitumor activity .
|
-
- HY-169124
-
|
|
Apoptosis
Reactive Oxygen Species
Protease Activated Receptor (PAR)
Bcl-2 Family
|
Cancer
|
|
Apoptosis Inducer 28 (Compound X1) is an apoptosis-inducing agent with anticancer activity in vitro. Apoptosis Inducer 28 can arrest the cell cycle at the G1 phase, promote cell death, and induce apoptosis by disrupting mitochondrial membrane potential. Apoptosis inducer 28 can also decrease the production of reactive oxygen species, downregulate the gene expression of BAX, Bcl-xL, and Bcl-2, while upregulating the gene expression of PAR-4 .
|
-
- HY-150231
-
SU056
1 Publications Verification
|
YB-1
|
Cancer
|
|
SU056 is a YB-1 inhibitor. SU056 induces cell-cycle arrest, apoptosis, and inhibits cell migration in ovarian cancer cells. SU056 interacts with YB-1 and inhibits and its associated downstream proteins and pathways. SU056 can enhance the cytotoxic effects of Paclitaxel (HY-B0015) .
|
-
- HY-N2374R
-
|
|
Apoptosis
|
Cancer
|
|
Eupatorin (Standard) is the analytical standard of Eupatorin. This product is intended for research and analytical applications. Eupatorin, a naturally occurring flavone, arrests cells at the G2-M phase of the cell cycle and induces apoptotic cell death involving activation of multiple caspases, mitochondrial release of cytochrome c and poly(ADP-ribose) polymerase cleavage .
|
-
- HY-165064
-
|
L-Erythro cer(d18:1/2:0); N-Acetyl-L-erythro-sphingosine; Acetyl-L-erythro-sphingosine
|
Others
|
Cancer
|
|
C2 L-Erythro ceramide (d18:1/2:0) is a cell-permeable sphingolipid. C2 L-Erythro ceramide (d18:1/2:0) induces cell cycle arrest in the G0/G1 phase and inhibits cell growth .
|
-
- HY-148923
-
|
|
STAT
|
Cancer
|
|
MC0704 is a STAT3 inhibitor with an IC50 value of 2.13 μM. MC0704 induces cell apoptosis and cell cycle arrest. MC0704 shows antitumor activity in mouse breast cancer models. MC0704 can be used for the research of metastatic triple-negative breast cancer (mTNBC) .
|
-
- HY-120027
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Kribb3 is an inhibitor for microtubule. KRIBB3 inhibits the proliferation of cancer cells with GI50 of 0.2-2.5 μM, arrests cell cycle at G2/M phase, and induces apoptosis in HCT-116. Kribb3 exhibits antitumor activity in mouse models .
|
-
- HY-N0800R
-
|
|
Apoptosis
|
Cancer
|
|
Protosappanin B (Standard) is the analytical standard of Protosappanin B. This product is intended for research and analytical applications. Protosappanin B is a phenolic compound extracted from Caesalpinia sappan. Anti-cancer activity . Protosappanin B induces apoptosis and causes G1 cell cycle arrest in human bladder cancer cells .
|
-
- HY-42484
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
ER-076349 is an inhibitor of tubulin polymerization, induces G2-M cell cycle arrest, and disrupts mitotic spindles. ER-076349 inhibits cancer cell growth, and inhibits tumor growth in several human tumor xenografts. ER-076349 is an analog of Halichondrin B .
|
-
- HY-N11722
-
|
|
PPAR
Apoptosis
Bacterial
|
Infection
Inflammation/Immunology
Cancer
|
|
Panduratin A, a natural chalcone compound, is a PPAR-α/δ activator. Panduratin A induces apoptosis, and promotes cell cycle arrest at G0/G1 phase in multiple hematologic malignant cell lines. Panduratin A has anticancer, antioxidant, anti-inflammatory, antibacterial, and antibiofilm activities .
|
-
- HY-155609
-
|
|
VEGFR
|
Cancer
|
|
VEGFR-2-IN-31 (compound 3i) is a potent VEGFR-2 inhibitor (IC50=8.93 nM), and an anti-prostate cancer agent. VEGFR-2-IN-31 arrests cell cycle at the S-phase and induces apoptosis.
|
-
- HY-N6623
-
|
|
Apoptosis
Endogenous Metabolite
Reactive Oxygen Species
|
Cancer
|
|
Malvidin-3-galactoside chloride, an anthocyanin monomer, induces hepatocellular carcinoma (HCC) cells cycle arrest and apoptosis. Malvidin-3-galactoside chloride inhibits the production and accumulation of ROS. Malvidin-3-galactoside chloride has anti-tumor function .
|
-
- HY-B0294S
-
|
|
Parasite
Microtubule/Tubulin
Apoptosis
|
Infection
Cancer
|
|
Flubendazole-d3 is the deuterium labeled Flubendazole. Flubendazole is a safe and efficacious anthelmintic agent, which is widely used for anthelmintic to human, rodents and ruminants. Flubendazole exerts anticancer activities by mechanisms including inhibition of microtubule function. Flubendazole induces p53-mediated apoptosis and arrests G2/M cell cycle[1][2].
|
-
- HY-158049
-
|
|
Apoptosis
Ferroptosis
|
Cancer
|
|
Anticancer agent 199 (Compound G-4) induces apoptosis in triple negative breast cancer (TNBC) cells via the mitochondrial pathway through inhibiting EGFR, AKT and MAPK pathways. Anticancer agent 199 also induces Ferroptosis by down-regulating LCN2. Anticancer agent 199 inhibits TNBC cell viability and migration, and induces S phase cell cycle arrest. Anticancer agent 199 is a derivate of cyclin-dependent kinase inhibitor Rocovitine .
|
-
- HY-N0416
-
-
- HY-N0421
-
|
Cinobufagine
|
Apoptosis
|
Neurological Disease
Cancer
|
|
Cinobufagin is an anticancer agent that can be secreted by the Asiatic toad Bufo gargarizans. Cinobufagin induces the cell cycle arrests in the G1 phase or G2/M phase, leading to apoptosis in cancer cells. Cinobufagin inhibits tumor growth in melanoma and glioblastoma multiforme xenograft mouse models .
|
-
- HY-N1428
-
-
- HY-N1986
-
|
|
HSP
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Cucurbitacin D is the active ingredient in Trichosanthes kirilowii and can disrupt the interaction between Hsp90 and two co-chaperones, Cdc37 and p23. Cucurbitacin D is an inflammasome activator. Cucurbitacin D induces cell cycle arrest and cell apoptosis, exhibiting anti-tumor and anti-inflammatory effects .
|
-
- HY-107632
-
-
- HY-147771
-
|
|
CDK
Apoptosis
|
Cancer
|
|
ZLWT-37 is a potent, orally active CDKs inhibitor with IC50 values of 0.002 μM and 0.054 μM against CDK9 and CDK2, respectively. ZLWT-37 induces apoptosis and arrests the cell cycle in the G2/M phase in HCT116 cells .
|
-
- HY-149075
-
|
|
Salt-inducible Kinase (SIK)
|
Cancer
|
|
MR22 is a potent pan-SIK (salt-inducible kinase) inhibitor. MR22 no longer exhibits activity on STE group kinases and displays excellent selectivity in a representative kinase panel. MR22-dependent SIK inhibition led to centrosome dissociation and subsequent cell-cycle arrest in ovarian cancer cells .
|
-
- HY-149344
-
|
|
Apoptosis
Autophagy
EGFR
|
Cancer
|
|
Anticancer agent 133 (compound Rh2) is an anti-cancer agent with cytotoxic and antimetastatic activities. Anticancer agent 133 induces cell cycle arrest, apoptosis, and autophagy. Anticancer agent 133 also inhibits cell metastasis via suppression of EGFR expression mediated by FAK-regulated integrin β1 .
|
-
- HY-108716
-
|
CBS9106; SL-801
|
CRM1
Apoptosis
|
Cancer
|
|
CBS9106 (SL-801) is a reversible oral CRM1 inhibitor with CRM1 degrading and antitumor activities. CBS9106, inhibits CRM1-dependent nuclear export, causing arrest of the cell cycle and inducing apoptosis in a time- and dose-dependent manner for a broad spectrum of cancer cells .
|
-
- HY-114699
-
|
|
Endogenous Metabolite
|
Cancer
|
|
DC_YM21 is an inhibitor of menin-MLL interaction with potent and selective proliferation blocking activity. DC_YM21 can induce cell cycle arrest and differentiation of leukemia cells carrying MLL translocation. DC_YM21 shows potential application value in inhibiting MLL leukemia .
|
-
- HY-N13174
-
|
|
Reactive Oxygen Species
Apoptosis
|
Inflammation/Immunology
|
Peanut procyanidin A is a type of A-type procyanidin that can be extracted from peanut skins. Peanut procyanidin A can protect prostate DU145 cells from H2O2-induced oxidative stress damage through the MAPKs signaling pathway, alleviate cell cycle arrest, and reduce cell apoptosis. Peanut procyanidin A can also regulate gut microbiota and metabolism in mice with DSS (HY-116282)-induced ulcerative colitis .
|
-
- HY-152173
-
|
|
HDAC
Apoptosis
Bcl-2 Family
CDK
|
Cancer
|
|
HDAC-IN-51 is a potent histone deacetylase (HDAC) inhibitor with IC50 values of 0.32, 0.353, 0.431, 0.515, and 85.4 μM for HDAC10, HDAC1, HDAC2, HDAC3 and HDAC11, respectively. HDAC-IN-51 induces cell cycle arrest and apoptosis, modulating cell cycle-/apoptosis-related miRNAs expression. HDAC-IN-51 can be used in research of cancer .
|
-
- HY-155544
-
|
|
c-Met/HGFR
|
Cancer
|
|
Antitumor agent-111 (compound 46) is an c-Met kinase inhibitor (IC50=46 nM) with antitumor and antiproliferative activity. Antitumor agent-111 arrests cell cycle at G0/G1 phase, and induces apoptosis .
|
-
- HY-N1196
-
|
|
NF-κB
|
Inflammation/Immunology
|
|
Suberosin, isolated from Plumbago zeylanica, exhibits anti-inflammatory and anticoagulant activity. Suberosin suppresses PHA-induced PBMC proliferation and arrested cell cycle progression from the G1 transition to the S phase through the modulation of the transcription factors NF-AT and NF-κB .
|
-
- HY-144754
-
|
|
VEGFR
Apoptosis
|
Cancer
|
|
VEGFR-2-IN-13 (Compound 19a) is a potent VEGFR-2 inhibitor with an IC50 of 3.4 nM. VEGFR-2-IN-13 disrupts the HepG2 cell cycle by arresting the G2/M phase and induces apoptosis .
|
-
- HY-147801
-
|
|
Topoisomerase
Apoptosis
|
Cancer
|
|
Topoisomerase IIα-IN-3 (Compound 12c) is a DNA intercalative topoisomerase-IIα inhibitor. Topoisomerase IIα-IN-3 arrests cell cycle at the G0/G1 phase and induces apoptosis .
|
-
- HY-147895
-
|
|
Histone Acetyltransferase
Apoptosis
|
Cancer
|
|
PCAF-IN-2 (compound 17) is a potent PCAF inhibitor with an IC50 value of 5.31 µM. PCAF-IN-2 shows anti-tumour activity. CAF-IN-2 induces apoptosis and arrest the cell cycle at the G2/M phase .
|
-
- HY-155503
-
|
|
Apoptosis
|
Cancer
|
|
Antitumor agent-103 (compound 24l) is an apoptosis inducer with antiproliferative and anti-clony formation activities. Antitumor agent-103 arrests cell cycle at G0/G1 phase, enhances NO production, and exhibits anti-tumor activity .
|
-
- HY-114413
-
|
|
HSP
Apoptosis
|
Cancer
|
|
YZ129 is an inhibitor of the HSP90-calcineurin-NFAT pathway against glioblastoma, directly binding to heat shock protein 90 (HSP90) with an IC50 of 820 nM on NFAT nuclear translocation. YZ129-induced GBM cell-cycle arrest at the G2/M phase promotes apoptosis and inhibited tumor cell proliferation and migration .
|
-
- HY-122359A
-
|
rel-L-Centchroman; Ormeloxifene
|
Estrogen Receptor/ERR
Apoptosis
Reactive Oxygen Species
|
Cancer
|
|
rel-Levormeloxifene (rel-L-Centchroman) is the relative configuration of Levormeloxifene (HY-122359). rel-Levormeloxifene is a selective estrogen receptor modulator (SERM). rel-Levormeloxifene inhibits proliferation of leukemia cells with IC50 about 7 μM, arrests cell cycle at G0/G1 phase, and induces apoptosis. rel-Levormeloxifene induces differentation of myelogenesis leukemia, and enhances ROS production in K562 cells .
|
-
- HY-163740
-
|
|
Apoptosis
Necroptosis
VEGFR
|
Cancer
|
|
VEGFR-2-IN-46 (compound 4d) is a potent VEGFR-2 inhibitor with an EC50 value of 67.0 nM. VEGFR-2-IN-46 shows cytotoxicity and induces cell cycle arrest at the G2/M phase. VEGFR-2-IN-46 induces necrosis and apoptosis .
|
-
- HY-N2369
-
|
|
Apoptosis
Influenza Virus
|
Infection
Cancer
|
|
Chelidonine, an isoquinoline alkaloid, can be isolated from Chelidonium majus L.. Chelidonine causes G2/M arrest and induces caspase-dependent and caspase-independent apoptosis, and prevents cell cycle progression of stem cells in Dugesia japonica. Chelidonine has cytotoxic activity against melanoma cell lines. with anticancer and antiviral activity .
|
-
- HY-146718
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulin polymerization-IN-9 is a potent tubulin inhibitor with IC50 of 1.82 μM. Tubulin polymerization-IN-9 causes cell cycle arrest at G2/M phase, and induces cell apoptosis and depolarized mitochondria of K562 cells. Tubulin polymerization-IN-9 has potent anti-vascular and antitumor activities .
|
-
- HY-152774
-
|
|
Akt
PI3K
|
Cancer
|
|
Antitumor agent-86 (compound 5a) inhibits MCF-7 breast cancer cells with an IC50 value of 2.62 µM. Antitumor agent-86 induces cell apoptosis and cell cycle arrest, and shows antineoplastic activity by targeting RAS/PI3K/Akt/JNK signaling cascades .
|
-
- HY-157324
-
|
|
EGFR
Apoptosis
VEGFR
|
Cancer
|
|
EGFR-IN-94 (compound 5a) is a EGFR inhibitor with IC50 of 0.086?μM, and also has IC50 of 0.107μM and 2.52 μM for VEGFR-2 and Topo II, respectively. EGFR-IN-94 induces cell apoptosis and arrests cell cycle at the S phase in HepG-2 cells .
|
-
- HY-164462
-
|
|
PKC
NF-κB
Apoptosis
|
Cancer
|
|
BHA536 is an orally active selective inhibitor for PKCα/β and NF-kB signaling pathway. BHA536 inhibits the proliferation of CD79-mutated ABC DLBCL cell, arrests cell cycle at G1 phase, and induces apoptosis in TMD8 cell. BHA536 exhibits antitumor efficacy in mice .
|
-
- HY-144637
-
|
|
Apoptosis
Autophagy
|
Cancer
|
|
Autophagy inducer 2 (Compound 11i) is a potent autophagy inducer. Autophagy inducer 2 exhibits apparent antiproliferative activity against the MCF-7 cell line with an IC50 value of 1.31 μM and remarkably inhibits the colony formation of the MCF-7 cells. Autophagy inducer 2 arrests the MCF-7 cells in the G2/M phase by regulating the cell-cycle-related proteins Cdk-1 and Cyclin B1. Autophagy inducer 2 has the potential for the research of breast cancer .
|
-
- HY-13630A
-
|
BMY-40481 disodium
|
Topoisomerase
Autophagy
Apoptosis
|
Neurological Disease
Cancer
|
|
Etoposide phosphate disodium (BMY-40481 disodium) is a potent anti-cancer chemotherapy agent and a selective topoisomerase II inhibitor to prevent re-ligation of DNA strands. Etoposide phosphate disodium is the phosphate ester proagent of etoposide and is considered as active equivalent to Etoposide. Etoposide phosphate disodium induces cell cycle arrest, apoptosis, and autophagy.
|
-
- HY-146407
-
|
|
Apoptosis
|
Cancer
|
|
Anticancer agent 53 is a potent anticancer agent. Anticancer agent 53 shows in vitro cytotoxicity. Anticancer agent 53 induces apoptosis and cell cycle arrest in S/G2/M phases. Anticancer agent 53 shows antitumor activity with no apparent toxicity .
|
-
- HY-146227
-
|
|
Topoisomerase
Apoptosis
|
Cancer
|
|
DNA topoisomerase II inhibitor 1 (compound 8ed) is a potent DNA topoisomerase II inhibitor. DNA topoisomerase II inhibitor 1 shows anti-proliferative activity. DNA topoisomerase II inhibitor 1 induces apoptosis and cell cycle arrest at sub G1 phase .
|
-
- HY-W278582
-
|
|
Topoisomerase
Apoptosis
|
Cancer
|
|
Topoisomerase II inhibitor 14 (compound 2f) is a potent inhibtor of Topoisomerase II, with anticancer activity. Topoisomerase II inhibitor 14 induces apoptosis, and arrests cell cycle at S phase. Topoisomerase II inhibitor 14 exhibits antioxidant effect and decreases the level of GSH, MDA, and NO .
|
-
- HY-161146
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
EGFR-IN-100 (compound 3f) is a EGFR inhibitor with IC50 range of 0.137-0.507 μM. EGFR-IN-100 has antiproliferative activity and induces the apoptosis pathway. EGFR-IN-100 arrests the MCF-7 cell cycle at the S phase .
|
-
- HY-101030A
-
|
|
NEKs
Apoptosis
|
Cancer
|
|
MBM-17S is a potent NIMA-related kinase 2 (Nek2) inhibitor, with an IC50 of 3 nM. MBM-17S effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis. MBM-17S shows antitumor activities, and no obvious toxicity to mice .
|
-
- HY-N8441
-
|
17β-Neriifolin
|
Atg8/LC3
Na+/K+ ATPase
Apoptosis
Beclin1
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Neriifolin, a CNS-penetrating cardiac glycoside, is an inhibitor of the Na +, K +-ATPase. Neriifolin can target beclin 1, inhibits the formation of LC3-associated phagosomes and ameliorates experimental autoimmune encephalomyelitis (EAE) development. Neriifolin induces cell cycle arrest and apoptosis in human hepatocellular carcinoma HepG2 cells [2.
|
-
- HY-151624
-
|
|
PARP
Apoptosis
|
Cancer
|
|
PARP-2-IN-2 (compound 27) is a PARP‑2 inhibitor with an IC50 value of 0.057 µM. PARP-2-IN-2 induces cell cycle arrest and apoptosis of MCF-7 breast cancer cells. PARP-2-IN-2 can be used for the research of cancer .
|
-
- HY-163090
-
|
|
HDAC
Reactive Oxygen Species
Apoptosis
|
Cancer
|
|
HR488B is an efficient HDAC1 inhibitor. HR488B specifically suppressed the growth of CRC cells by inducing cell cycle G0/G1 arrest and apoptosis. HR488B causes mitochondrial dysfunction, reactive oxygen species (ROS) generation, and DNA damage accumulation .
|
-
- HY-161268
-
-
- HY-N0036R
-
|
|
Apoptosis
Endogenous Metabolite
|
Cancer
|
|
Costunolide (Standard) is the analytical standard of Costunolide. This product is intended for research and analytical applications. Costunolide ((+)-Costunolide) is a naturally occurring sesquiterpene lactone, with antioxidative, anti-inflammatory, antiallergic, bone remodeling, neuroprotective, hair growth promoting, anticancer, and antidiabetic properties. Costunolide can induce cell cycle arrest and apoptosis on breast cancer cells .
|
-
- HY-N6016R
-
|
|
Apoptosis
|
Cancer
|
|
Bacopaside II (Standard) is the analytical standard of Bacopaside II. This product is intended for research and analytical applications. Bacopaside II, an extract from the medicinal herb Bacopa monnieri, blocks the Aquaporin-1 (AQP1) water channel and impairs migration of cells that express AQP1. Bacopaside II induces cell cycle arrest and apoptosis .
|
-
- HY-N0816
-
|
|
Apoptosis
Pyroptosis
|
Cancer
|
|
Polyphyllin VI, an active saponin, possess anti-cancer activities. Polyphyllin VI induces G2/M cell cycle arrest and triggers apoptosis. Polyphyllin VI induces caspase-1-mediated pyroptosis via the induction of ROS/NF-κB/NLRP3/GSDMD signal axis in non-small cell lung cancer .
|
-
- HY-146743
-
|
|
Apoptosis
|
Cancer
|
|
Antitumor agent-53 is a potent antitumor agent. Antitumor agent-53 induces cell cycle arrest at the G2/M phase. Antitumor agent-53 inhibits the PI3K/AKT pathway to induce the apoptosis of HGC-27 cells. Antitumor agent-53 has the potential for the research of gastrointestinal tumors .
|
-
- HY-150765
-
|
|
PARP
Apoptosis
|
Cancer
|
|
PARP1-IN-12 is a potent PARP1 inhibitor with an IC50 of 2.99 nM. PARP1-IN-12 exhibits antiproliferative activity, can induce cell apoptosis and cause cycle arrest at G2/M phase. PARP1-IN-12 also can induce DNA double strand breaks (DSBs) in BRCA-deficient cells .
|
-
- HY-N12044
-
|
|
Apoptosis
|
Cancer
|
|
Asparanin A is an apoptosis inducer with anticancer activity. Asparanin A induces cell cycle arrest in the G0/G1 phase through mitochondria and PI3K/AKT signaling pathways, inhibiting cancer cell growth. Asparanin A also demonstrated in vivo efficacy in a mouse xenograft model of Ishikawa endometrial carcinoma, significantly inhibiting tumor growth .
|
-
- HY-162344
-
|
|
Apoptosis
Autophagy
|
Cancer
|
|
Ir-CA is an antitumor agent. Ir-CA can accumulate in mitochondria and induces mitochondria dysfunction. Ir-CA induces apoptosis and autophagy. Ir-CA initiates mitophagy and cell cycle arrest to kill Cisplatin (HY-17394)-resistant A549R cells. Ir-CA can effectively inhibit metastasis by inhibiting MMP-2/MMP-9 .
|
-
- HY-163535
-
|
|
HDAC
DNA Methyltransferase
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
J208 is a dual inhibitor for histone deacetylase (HDAC) and DNA methyltransferase (DNMT). J208 inhibits proliferation of cancer cells, as well as the migration/invasion of triple-negative breast cancer (TNBC) cells. J208 induces apoptosis, arrests the cell cycle at G0/G1 phase. J2008 activates the innate immune signalling pathway in TNBC, by inducing the expression of endogenous retroviruses (ERVs) .
|
-
- HY-117113
-
|
|
Notch
|
Cancer
|
|
JI051 is a stabilizer for the Hes1-PHB2 interaction. JI051 interacts with a cancer-associated protein chaperone prohibitin 2 (PHB2), induces cell-cycle arrest by inhibiting the Notch downstream effector gene Hes1. Anti-cancer activity .
|
-
- HY-146711
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 24 is a potent tubulin inhibitor. Tubulin inhibitor 24 inhibits tubulin polymerization. Tubulin inhibitor 24 induces cell cycle arrest at the G2/M phase in a concentration-dependent manner. Tubulin inhibitor 24 shows antitumor activity with no obvious toxicity .
|
-
- HY-N10447
-
|
|
Apoptosis
|
Cancer
|
|
Kurzipene D (compound 4) is a potent anticancer agent. Kurzipene D induces the apoptosis and arrested the HepG2 cell cycle at S stage. Kurzipene D shows anti-tumor effects using in vivo zebrafish model. Kurzipene D has the property of inhibiting tumor proliferation and migration .
|
-
- HY-N9968
-
|
|
Akt
Apoptosis
|
Cancer
|
|
Cucurbitacin C is a triterpenoid calabinoid that can be isolated from Cucurbitaceae plants. Cucurbitacin C has anti-cancer activity in vivo and in vitro. Cucurbitacin C can induce cell cycle arrest in G1 or G2/M phase and apoptosis by inhibiting Akt signaling .
|
-
- HY-121777
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
SFOM-0046 arrests cell cycle in S-phase and causes DNA replication stress leading to the phosphorylation of H2AX into γ-H2AX. SFOM-0046 induces DNA damages. SFOM-0046 is a potent anticancer agent .
|
-
- HY-168560
-
|
|
MMP
|
Cancer
|
|
MMP Inhibitor 4 (compound 4 B) is a potent MMP inhibitor. MMP Inhibitor 4 shows antiproliferative activity. MMP Inhibitor 4 induces cell cycle arrest at subG1 phase. MMP Inhibitor 4 decreases the mRNA expression of MMP2, MMP9 and VEGFA .
|
-
- HY-12678
-
|
NMS-E628; RXDX-101
|
ROS Kinase
Trk Receptor
Anaplastic lymphoma kinase (ALK)
Autophagy
|
Cancer
|
|
Entrectinib (NMS-E628) is an orally active, BBB-penetrated and centrally active inhibitor of TrkA/B/C, ROS1 and ALK, with IC50 values of 1, 3, 5, 12 and 7 nM, respectively. Entrectinib induces apoptosis and cycle arrest in cancer cells, has antitumor activity, and attenuates bleomycin-induced lung fibrosis in mice .
|
-
- HY-147906
-
|
|
Apoptosis
PARP
|
Cancer
|
|
Anticancer agent 71 (Compound 4b) is a potent anticancer agent and induces apoptosis. Anticancer agent 71 arrests cell cycle at G2/M phase and induces apoptosis through upregulating Bax, Ikb-α and cleaved PARP and downregulating Bcl-2 expression levels. Anticancer agent 71 shows antiproliferative activity .
|
-
- HY-151985
-
|
|
Apoptosis
|
Cancer
|
|
TACC3 inhibitor 1 is a potent and cross the blood-brain barrier TACC3 inhibitor. TACC3 inhibitor 1 induces Apoptosis and cell cycle arrest at G2/M phase. TACC3 inhibitor 1 induces the generation of intracellular ROS. TACC3 inhibitor 1 shows antiproliferative and anti-tumor activity .
|
-
- HY-N11576
-
|
|
Apoptosis
GSK-3
c-Myc
β-catenin
|
Cancer
|
|
Secalonic acid D is a toxic compound against tumor cells. Secalonic acid D can be isolated from the metabolites of Aspergillus aculeatus. Secalonic acid D activates GSK3-β, and degrades β-catenin. Thus, Secalonic acid D down-regulates c-Myc expression, arrests cell cycle at G1 phase, induces cell apoptosis .
|
-
- HY-161151
-
|
|
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
Frangulin B (Compd 11g), a potent anticancer agent, is a potential pan RecQ helicase inhibitor . Frangulin B (Compd 11g) induces apoptosis in both HCT-116 and MDA-MB-231 cell lines, but also causes an G2/M phase cell cycle arrest in HCT-116 cells .
|
-
- HY-162227
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Antitumor agent-138 (compound 5b) is an inhibitor against tubulin polymerization at tubulin colchicine-binding sites, with IC50 of 1.87 μM. Antitumor agent-138 arrests the cell cycle at G2/M phase and induces an apoptosis in MCF-7 cells. Antitumor agent-138 inhibits cells migration and angiogenesis .
|
-
- HY-137135
-
|
|
Phosphatase
Apoptosis
ERK
p38 MAPK
JNK
|
Cancer
|
|
Cantharidic acid is a selective inhibitor for protein phosphatase 2 (PP2A) and protein phosphatase 1 (PP1). Cantharidic acid inhibits cell viability and arrest cell cycle at sub G1 phase, induces apoptosis in cells NPC-39 and HONE-1 through the upregulation of ERK1/2, p38, and JNK1/2 pathway .
|
-
- HY-125677
-
|
|
Caspase
Reactive Oxygen Species
Apoptosis
|
Cancer
|
|
SHetA2 is a derivative of heteroarotinoid, that exhibits cytotoxicity in cancer cells with IC50 of 0.37–4.6 μM. SHetA2 regulates cancer cells differentiation, induces apoptosis through the intrinsic mitochondrial pathway, and arrest cell cycle at G2 phase. SHetA2 exhibits good pharmacokinetic characteristics and antitumor efficacy in mice. SHetA2 is orally active .
|
-
- HY-12286
-
|
|
Proteasome
Apoptosis
Autophagy
Caspase
Bcl-2 Family
NF-κB
PARP
|
Cancer
|
|
PI-1840 is a potent and selective chymotrypsin-like (CT-L) inhibitor for with an IC50 value of 27 nM. PI-1840 inhibits cell proliferation and arrest cell cycle at G2/M phase. PI-1840 induces apoptosis and induces autophagy. PI-1840 induces the accumulation of proteasome substrates p27, Bax, and IκB-α .
|
-
- HY-149132
-
|
DDA
|
LXR
|
Cancer
|
|
Dendrogenin A (DDA) is a ligand for liver X receptor (LXR), that induces the expression of sodium/iodine symporter, and increases iodine uptake. Dendrogenin A induces cell differentiation of MCF-7, and reactivates the function of lactating cells. Dendrogenin A induces the expressions of the TSH receptor, thyroid peroxidase, and thyroglobulin, and affects thyroid hormone generation. Dendrogenin A exhibits cytotoxicity in cancer cell B-CPAP and 8505c with IC50 of 4.1 and 6.2 µM. Dendrogenin A arrests the cell cycle at G0/G1 phase .
|
-
- HY-13629R
-
|
|
Topoisomerase
Autophagy
Mitophagy
Bacterial
Apoptosis
Antibiotic
|
Infection
Cancer
|
|
Etoposide (Standard) is the analytical standard of Etoposide. This product is intended for research and analytical applications. Etoposide (VP-16; VP-16-213) is an anti-cancer chemotherapy agent. Etoposide inhibits topoisomerase II, thus stopping DNA replication. Etoposide induces cell cycle arrest, apoptosis and autophagy .
|
-
- HY-N1428A
-
|
|
Endogenous Metabolite
Apoptosis
Antibiotic
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Citric acid monohydrate is a natural preservative and food tartness enhancer. Citric acid monohydrate induces apoptosis and cell cycle arrest at G2/M phase and S phase. Citric acid monohydrate cause oxidative damage of the liver by means of the decrease of antioxidative enzyme activities. Citric acid monohydrate causes renal toxicity in mice .
|
-
- HY-150048
-
|
|
CD73
Apoptosis
|
Cancer
|
|
BK50164 is a potent CD73 inhibitor with an IC50 value of 13.089 µM. BK50164 binds to CD99 with a KD value of 1.5 µM. BK50164 shows antiproliferative activity. BK50164 induced Apoptosis and cell cycle arrest at Sub-G1 phase .
|
-
- HY-163697
-
|
|
Wee1
Apoptosis
|
Cancer
|
|
WEE1-IN-7 (compound 12h) is a potent and orally activeWEE1 inhibitor with an IC50 value of 2.1 nM. WEE1-IN-7 induces apoptosis and cell cycle arrest at the S phase. WEE1-IN-7 shows antitumor activity .
|
-
- HY-118921
-
|
|
Apoptosis
|
Infection
Inflammation/Immunology
Cancer
|
|
Ovatodiolide is a compound that can be isolated from Anisomeles indica. Ovatodiolide has anti-bacterial and anti-inflammatory properties. Ovatodiolide also has anti-cancer activity that induces cell cycle G2/M arrest and apoptosis via a ROS-dependent ATM/ATR signaling pathways .
|
-
- HY-N2342
-
|
PCC1
|
Apoptosis
|
Cancer
|
|
Procyanidin C1 (PCC1), a natural polyphenol with oral activity, causes DNA damage, cell cycle arrest and induces apoptosis. Procyanidin C1 decreases the level of Bcl-2, but enhances BAX, caspase 3 and 9 expression in cancer cells. Procyanidin C1 shows senotherapeutic activity and increases lifespan in mice .
|
-
- HY-N10018
-
|
25-Anhydrocimigenol xyloside
|
Caspase
|
Cancer
|
|
Cimiside E (25-Anhydrocimigenol xyloside) is a triterpene xyloside, Cimiside E possesses apoptotic action on gastric cancer cells, with an IC50 value of 14.58 μM. Cimiside E induces cell cycle arrest at G2/M phase, and mediates apoptosis through the induction of the caspase cascade for both the extrinsic and intrinsic pathways .
|
-
- HY-155441
-
|
|
CDK
|
Cancer
|
CDK2-IN-20 (compound 3b) is an inhibitor of CDK2. CDK2-IN-20 has cytotoxicity on tumor cells presenting an IC50 range of 5.52-17.09 µM. CDK2-IN-20 arrests the MCF-7 cell cycle at the S phase and induces apoptosis .
|
-
- HY-100507A
-
|
CC 122 hydrochloride
|
E1/E2/E3 Enzyme
Apoptosis
Molecular Glues
NF-κB
|
Inflammation/Immunology
Cancer
|
|
Avadomide hydrochloride (CC 122 hydrochloride) is the hydrochloride form of Avadomide (HY-100507). Avadomide hydrochloride is an orally active cereblon modulator. Avadomide hydrochloride modulates cereblon E3 ligase activity, inhibits NF-κB pathway, arrests the cell cycle at G1 phase, and thus induces apoptosis in cancer cell PDAC. Avadomide hydrochloride exhibits potent antitumor and immunomodulatory activities .
|
-
- HY-101266A
-
|
DS-3032 tosylate
|
MDM-2/p53
|
Cancer
|
|
Milademetan tosylate is the tosylate salt form of Milademetan (HY-101266). Milademetan tosylate is an orally active inhibitor for MDM2. Milademetan tosylate arrests the cell cycle at G1 pahse, induces the apoptosis Milademetan tosylate restores the p53 activity by targeting the p53-MDM2 interaction, and exhibits anticancer activity against Merkel cell carcinoma (MCC) .
|
-
- HY-N0623R
-
|
Tryptophan (standard); Tryptophane (standard)
|
Others
|
Metabolic Disease
|
|
L-Tryptophan (standard) is the analytical standard of L-Tryptophan. L-Tryptophan (Tryptophan) is an orally active and essential amino acid that is the precursor of serotonin, melatonin, and vitamin B3. L-Tryptophan can promote an increase in stemness and osteogenic ability of BMSCs in vitro and in vivo. L-Tryptophan inhibits cell proliferation and induced cell cycle arrest with high levels .
|
-
- HY-169293
-
|
|
Apoptosis
|
Cancer
|
|
Antiproliferative agent-63 (compound 4d), a ring-annulated analogue of Cannabidiol, is an anticancer agent. Antiproliferative agent-63 demonstrates a promising activity against breast and colorectal cancer. Antiproliferative agent-63 arrests the G1 phase of the cell cycle and induces apoptosis via the mitochondrial pathway in breast cancer cell lines .
|
-
- HY-12300A
-
|
CFI-400945 hydrochloride
|
Polo-like Kinase (PLK)
Apoptosis
|
Cancer
|
|
Ocifisertib hydrochloride (CFI-400945 hydrochloride) is the hydrochloride salt form of Ocifisertib (HY-12300). Ocifisertib hydrochloride is an orally active PLK4 inhibitor with a Ki and an IC50 of 0.26 nM and 2.8 nM. Ocifisertib hydrochloride inhibits growth of various cancer cells, arrests cell cycles at G2/M phase, and induces apoptosis. Ocifisertib hydrochloride exhibits antitumor efficacy in mouse model .
|
-
- HY-N12960
-
|
|
Apoptosis
Bcl-2 Family
Caspase
COX
MMP
STAT
|
Cancer
|
|
Artobiloxanthone (Compound AA3) exhibits antitumor activity, particularly against oral squamous cell carcinoma (OSCC). Artobiloxanthone inhibits Akt/mTOR pathway and STAT3 pathway, inhibits proliferation of SAS and T.Tn (with IC50 of 11 and 22 μM), and inhibits the cancer cell migration. Artobiloxanthone arrests cell cycle at S phase, and induces apoptosis in OSCC cells through activation of caspase 3/9 .
|
-
- HY-W338764
-
|
|
Apoptosis
Aryl Hydrocarbon Receptor
|
Cancer
|
|
AHR agonist 3 is an aryl hydrocarbon receptor (AhR) agonist, that can induces cell cycle arrest or apoptosis via activation of tumor-suppressive transcriptional programs. AHR agonist 3 inhibits triple-negative breast cancer (TNBC) stem cell growth via AhR while exhibits minimal cytotoxicity against normal human primary cells and can be used for cancer research .
|
-
- HY-10815
-
|
|
Sigma Receptor
Apoptosis
|
Neurological Disease
Cancer
|
|
σ1 Receptor antagonist-1 is a highly potent and selective sigma 1 receptor antagonist (pKi=10.28). σ1 Receptor antagonist-1 inhibits cell growth, arrests cell cycle at G0/G1 phase and induces apoptosis of MCF-7/ADR cells .
|
-
- HY-10521
-
|
SB-480848
|
Phospholipase
Apoptosis
|
Cardiovascular Disease
Cancer
|
|
Darapladib (SB-480848) is an orally active, selective and reversible Lp-PLA2 inhibitor (IC50=0.25 nM). Darapladib can trigger irreversible actions on glioma cell apoptosis and induce cycle arrest. Darapladib can be used in the study of atherosclerosis and cancer .
|
-
- HY-150538
-
|
|
STAT
Apoptosis
|
Cancer
|
|
STAT3-IN-12 is a potent STAT3 signal inhibitor that can inhibit IL-6 induced JAK/STAT3 signalling pathway activation. STAT3-IN-12 inhibits cancer cell growth, migration, and induce cell apoptosis as well as cycle arrest. STAT3-IN-12 can be used in cancer-related research, such as hepatocellular carcinoma (HCC) and oesophageal carcinoma .
|
-
- HY-162332
-
|
|
Apoptosis
EGFR
JNK
|
Cancer
|
|
EGFR-PK/JNK-2-IN-1 (Compound 6c) is a dual inhibitor of EGFR-PK and JNK-2 with IC50s of 2.7 and 3.0 μM, respectively. EGFR-PK/JNK-2-IN-1 can induce apoptosis and induce cell cycle arrest at different cell phases. EGFR-PK/JNK-2-IN-1 can be used for the research of cancer .
|
-
- HY-157814
-
|
|
Apoptosis
Epigenetic Reader Domain
|
Cancer
|
|
Menin-MLL inhibitor-25 (compound A6) is a potent Menin-MLL interaction inhibitor with an IC50 value of 0.38 µM. Menin-MLL inhibitor-25 shows anti-proliferative activity. Menin-MLL inhibitor-25 induces apoptosis and cell cycle arrest at G0/G1 phase. Menin-MLL inhibitor-25 reverses the differentiation arrest .
|
-
- HY-50767
-
Palbociclib
Maximum Cited Publications
165 Publications Verification
PD 0332991
|
CDK
|
Cancer
|
|
Palbociclib (PD 0332991) is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib has potent anti-proliferative activity and induces cell cycle arrest in cancer cells, which can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma .
|
-
- HY-17583
-
-
- HY-144132
-
|
|
Apoptosis
Microtubule/Tubulin
|
Cancer
|
|
αβ-Tubulin-IN-1 is a potent and orally active αβ-Tubulin inhibitor. αβ-Tubulin-IN-1 induces cell cycle arrest at G2/M and efficient apoptosis. αβ-Tubulin-IN-1 inhibits tumor cell migration and Metastasis. αβ-Tubulin-IN-1 shows significant antitumor efficacy in a dose dependent manner .
|
-
- HY-144797
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 22 (compound 4c) is a potent inhibitor of tubulin with anti-angiogenesis and anti-cancer properties. Tubulin inhibitor 22 arrests MGC-803 cell cycle at G2/M phase. Tubulin inhibitor 22 dose-dependently causes Caspase-induced apoptosis of MGC-803 cells through mitochondrial dysfunction .
|
-
- HY-101989
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulin polymerization-IN-24 (compound HMBA) is a potent tubulin polymerization inhibitor. Tubulin polymerization-IN-24 inhibits MCF-7 cells proliferation. Tubulin polymerization-IN-24 induces apoptosis and cell cycle arrest at G2/M phase. Tubulin polymerization-IN-24 increase the GTP hydrolysis rate and inhibits microtubule assembly .
|
-
- HY-146189
-
|
|
Topoisomerase
Apoptosis
|
Cancer
|
|
Topoisomerase II inhibitor 9 (Compound 19b) is a Topo II inhibitor with an IC50 of 0.97 μM. Topoisomerase II inhibitor 9 is also a classical DNA-intercalator with an IC50 of 43.51 μM. Topoisomerase II inhibitor 9 arrests the cell cycle at the G2/M phase and induces apoptosis in Hep G‐2 cells .
|
-
- HY-13691
-
|
Ro-31-7453
|
Akt
mTOR
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
MKC-1 (Ro-31-7453) is an orally active and potent cell cycle inhibitor with broad antitumor activity. MKC-1 inhibits the Akt/mTOR pathway. MKC-1 arrests cellular mitosis and induces cell apoptosis by binding to a number of different cellular proteins including tubulin and members of the importin β family .
|
-
- HY-147219
-
|
|
PROTACs
Anaplastic lymphoma kinase (ALK)
EGFR
Apoptosis
|
Cancer
|
|
SIAIS164018 is a PROTAC-based ALK and EGFR degrader, with IC50 value of 2.5 nM and 6.6 nM for ALK and ALK G1202R, respectively. SIAIS164018 strongly inhibits cancer cells migration and invasion, causes G1 cell cycle arrest and induces apoptosis. SIAIS164018 exhibits better property than Brigatinib (HY-12857) .
|
-
- HY-150791
-
|
|
Reactive Oxygen Species
DNA/RNA Synthesis
|
Cancer
|
|
FLDP-5 is a blood-brain barrier (BBB) penetrant curcuminoid analogues. FLDP-5 can induce production of ROS (Reactive Oxygen Species), DNA damage and cell cycle S phase arrest. FLDP-5 exhibits highly potent tumour-suppressive effects with anti-proliferative and anti-migratory activities on LN-18 cells .
|
-
- HY-50767B
-
|
PD-0332991 dihydrochloride
|
CDK
|
Cancer
|
|
Palbociclib (PD 0332991) dihydrochloride is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib dihydrochloride has potent anti-proliferative activity and induces cell cycle arrest in cancer cells, which can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma .
|
-
- HY-N7844
-
|
Benzyladenosine
|
Apoptosis
Adenosine Receptor
|
Inflammation/Immunology
Cancer
|
|
N6-Benzyladenosine is an adenosine receptor agonist, has a cytoactive activity. N6-Benzyladenosine arrests cell cycle at G0/G1 phase and induces cell apoptosis. N6-Benzyladenosine also exerts inhibitory effect on T. gondii adenosine kinase and glioma - .
|
-
- HY-N1930
-
|
Hinesol
|
Apoptosis
|
Cancer
|
|
(-)-Hinesol (Hinesol) is a potent anticancer agent. (-)-Hinesol induces apoptosis and cell cycle arrest at G0/G1 phase. (-)-Hinesol downregulates MEK/ERK pathway and NF-κB pathway and mediates theexpression of cyclin D1, Bax and Bcl-2. (-)-Hinesol has the potential for the research of non–small cell lung cancer .
|
-
- HY-50767C
-
|
PD-0332991 hydrochloride
|
CDK
|
Cancer
|
|
Palbociclib (PD 0332991) hydrochloride is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib hydrochloride has potent anti-proliferative activity and induces cell cycle arrest in cancer cells. Palbociclib hydrochloride can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma .
|
-
- HY-117652
-
|
|
Apoptosis
Bcl-2 Family
MDM-2/p53
|
Infection
Inflammation/Immunology
Cancer
|
|
Lobetyol is a natural compound that can be isolated from Lobelia chinensis. Lobetyol induces apoptosis and cell cycle arrest in MKN45 cells. Lobetyol shows anti-virus, anti-inflammation and anti-tumor activity . Lobetyol is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-147219A
-
|
|
PROTACs
Anaplastic lymphoma kinase (ALK)
EGFR
Apoptosis
|
Cancer
|
|
SIAIS164018 hydrochloride is a PROTAC-based ALK and EGFR degrader, with IC50 value of 2.5 nM and 6.6 nM for ALK and ALK G1202R, respectively. SIAIS164018 hydrochloride strongly inhibits cancer cells migration and invasion, causes G1 cell cycle arrest and induces apoptosis. SIAIS164018 hydrochloride exhibits better property than Brigatinib (HY-12857) .
|
-
- HY-Q04764
-
|
|
Thyroid Hormone Receptor
Apoptosis
|
Cancer
|
|
TI17 is an inhibitor of the thyroid hormone receptor-interacting protein Trip13 and has anticancer activity. TI17 effectively inhibits multiple myeloma (MM) cell proliferation and induces cell cycle arrest and apoptosis. Trip13 is an AAA-ATPase that mediates double-strand break (DSB) repair; TI17 inhibits Trip13 function and increases DNA damage .
|
-
- HY-121917
-
|
|
c-Myc
Apoptosis
|
Inflammation/Immunology
|
|
APTO-253 (LOR-253) hydrochloride is a small molecule that inhibits c-Myc expression, stabilizes G-quadruplex DNA, and induces cell cycle arrest and apoptosis in acute myeloid leukemia cells. APTO-253 hydrochloride mediates anticancer activity via induction of Kruppel-like factor 4 (KLF4) tumor suppressor. APTO-253 hydrochloride exhibits antiarthritic activity.
|
-
- HY-105414
-
|
|
Others
|
Cancer
|
|
Esterbut-3 is a potent anticancer agent. Esterbut-3 inhibits cell proliferation. Esterbut-3 decreases the antigen expression of 115D8, 140C1 and increases the antigen expression of 123C3. Esterbut-3 induces cell cycle arrest at G0/G1 phase .
|
-
- HY-15228
-
RX-3117
1 Publications Verification
TV-1360; Fluorocyclopentenylcytosine
|
Nucleoside Antimetabolite/Analog
Apoptosis
|
Cancer
|
|
RX-3117 (TV-1360) is a potent and orally active anticancer and antimetaboliteagent. RX-3117 inhibits DNA methyltransferase 1 (DNMT1). RX-3117 shows antiproliferative and anti-tumour activity. RX-3117 induces cell cycle arrest at S phase and apoptosis .
|
-
- HY-N0662
-
-
- HY-101518
-
|
APG-115; AA-115
|
MDM-2/p53
E1/E2/E3 Enzyme
Apoptosis
|
Cancer
|
|
Alrizomadlin (APG-115) is an orally active MDM2 protein inhibitor binding to MDM2 protein with IC50 and Ki values of 3.8 nM and 1 nM, respectively . Alrizomadlin blocks the interaction of MDM2 and p53 and induces cell-cycle arrest and apoptosis in a p53-dependent manner .
|
-
- HY-105930
-
|
D-19466
|
Apoptosis
Caspase
Bcl-2 Family
|
Cancer
|
|
Lobaplatin (D-19466) is a diastereometric mixture of platinum(II) complexe. Lobaplatin arrests cell cycle at G1 and G2/M phase. Lobaplatin induces apoptosis by increasing expressions of caspase and Bax, decreasing expression of Bcl-2. Lobaplatin can be used for research of cancer .
|
-
- HY-145584
-
|
JPI-547/OCN-201
|
PARP
Apoptosis
Wnt
β-catenin
|
Cardiovascular Disease
Neurological Disease
Cancer
|
|
Nesuparib (JPI-547) is an orally active PARP 1/2 and Tankyrase 1/2 inhibitor involved in the Wnt/β-catenin pathway. Nesuparib can induce cell cycle arrest and apoptosis and has anti-tumor activity. Nesuparib can be used to study cancer, neurological diseases and cardiovascular diseases .
|
-
- HY-143412
-
|
|
HDAC
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
MIR002 is a potent and orally active DNA polymerase α (POLA1) and HDAC 11 dual inhibitor. MIR002 induces acetylation of p53, activation of p21, G1/S cell cycle arrest, and apoptosis. MIR002 shows significant antitumor activity in vivo .
|
-
- HY-13629S1
-
-
- HY-146063
-
|
|
Apoptosis
|
Cancer
|
|
Anticancer agent 54 is a potent anticancer agent. Anticancer agent 54 shows antiproliferative activity. Anticancer agent 54 induces apoptosis and cell cycle arrest at G0/G1 phases. Anticancer agent 54 shows anticancer activity depends on DNA intercalation and ROS generation .
|
-
- HY-146040
-
|
|
Apoptosis
|
Cancer
|
|
Anticancer agent 47 (compound 4j) is a potent anticancer agent. Anticancer agent 47 shows antiproliferative activities. Anticancer agent 47 induces apoptosis and cell cycle arrest at G0/G1 phase. Anticancer agent 47 shows shows antitumor activities in vivo .
|
-
- HY-149024
-
|
|
VEGFR
Apoptosis
MDM-2/p53
|
Cancer
|
|
VEGFR-2-IN-23 (compound 11b) is a potent and selective VEGFR-2 inhibitor with an IC50 value of 0.34 nM. VEGFR-2-IN-23 shows antitumor activity. VEGFR-2-IN-23 induces apoptosis and cell cycle arrest at G1 phase .
|
-
- HY-149252
-
|
|
Apoptosis
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 32 is a potent and orally active tubulin inhibitor. Tubulin inhibitor 32 shows anti-proliferative activity and inhibits microtubule polymerization. Tubulin inhibitor 32 induces Apoptosis and cell cycle arrest at G2/M phase. Tubulin inhibitor 32 shows anti-tumor activity .
|
-
- HY-162001
-
INX-315
1 Publications Verification
|
CDK
|
Cancer
|
|
INX-315 is an orally active and selective CDK2 inhibitor that induces cell cycle arrest in the G1 phase. INX-315 reduces CDK2 substrate phosphorylation and inhibits tumor growth in a dose-dependent manner in xenograft mouse models. INX-315 may be used in cancer research .
|
-
- HY-157396
-
|
|
Aurora Kinase
Apoptosis
|
Cancer
|
|
JAB-2485 is a potent and selective Aurora kinase A (AURKA) inhibitor, with an IC50 of 0.33 nM. JAB-2485 exhibits around 1700-fold selectivity for AURKA over AURKB. JAB-2485 induces cell cycle arrest and apoptosis. JAB-2485 can be used for the research of cancer .
|
-
- HY-158438
-
|
|
MNK
|
Cancer
|
|
MNK1/2-IN-8 (compound 15b) is a MNK1/2 inhibitor with the IC50 values of 0.8 and 1.5 nM against Mnk1 and Mnk2. MNK1/2-IN-8 shows anti-proliferative activity and induces cell cycle arrest .
|
-
- HY-13629S
-
-
- HY-161617
-
|
|
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
LASSBio-2052 is a derivative of N-acylhydrazone with antitumor activity against hepatocellular carcinoma (HCC). LASSBio-2052 inhibits HCC cells HepG2 and Hep3B, with IC50 of 18 and 41 μM. LASSBio-2052 arrests the cell cycle at G2/M phase, through downregulation of FOXM1. LASSBio-2052 induces apoptosis in HCC cells .
|
-
- HY-147973
-
|
|
c-Myc
Apoptosis
|
Cancer
|
|
IZTZ-1, an imidazole-benzothiazole conjugate, is a c-MYC G4 ligand. IZTZ-1 is able to downregulate the c-MYC expression by stabilizing c-MYC G4. IZTZ-1 induces cell cycle arrest, apoptosis, thereby inhibiting cell proliferation in B16 cells. IZTZ-1 shows antitumor activity, and can be used for melanoma research .
|
-
- HY-146812
-
|
|
G-quadruplex
|
Cancer
|
|
DIZ-3 is a selective multimeric G4 ligand based on a G4-ligand-dimerizing strategy. DIZ-3 intercalates into the G4-G4 interface, stabilizing the higher-order structure. DIZ-3 induces cell cycle arrest and apoptosis, and thus inhibits cell proliferation in alternative lengthening of telomere (ALT) cancer cells .
|
-
- HY-12037A
-
|
ON-01910
|
Polo-like Kinase (PLK)
PI3K
Apoptosis
|
Cancer
|
|
Rigosertib (ON-01910) is a multi-kinase inhibitor and a selective anti-cancer agent, which induces apoptosis by inhibition the PI3 kinase/Akt pathway, promots the phosphorylation of histone H2AX and induces G2/M arrest in cell cycle . Rigosertib is a selective and non-ATP-competitive inhibitor of PLK1 with an IC50 of 9 nM .
|
-
- HY-16594
-
|
|
Proteasome
Apoptosis
ROS Kinase
|
Infection
Cardiovascular Disease
Neurological Disease
Cancer
|
|
Lactacystin is a potent, orally active, irreversible, cell-permeable, selective 20S proteasome inhibitor (IC50 = 4.8 μM). Lactacystin also inhibits the lysosomal enzyme cathepsin A. Lactacystin inhibits cell growth and induces apoptosisand cell cycle arrest, and has antiviral and antioxidative activity. Lactacystin induces neurite outgrowth and hypertension. Lactacystin has the potential for the research of cancer, Neurological Disease, hypertension and Malaria, and so on [1] [2] [3] [4] [5] [6] [7] [8] [9] [10] .
|
-
- HY-N11439
-
|
|
CDK
Akt
ERK
Apoptosis
Bacterial
|
Infection
Neurological Disease
Cancer
|
|
Albanol B is an arylbenzofuran derivative which can be isolated from mulberries. Albanol B exhibits anti-Alzheimer's disease, anti-bacterial and antioxidant activities. Albanol B inhibits cancer cells proliferation, down-regulates CDK1 expression. Albanol B also induces cell cycle arrest at G2/M and apoptosis. And Albanol B induces mitochondrial ROS production and increases the phosphorylation levels of AKT and ERK1/2 .
|
-
- HY-50767A
-
|
PD 0332991 monohydrochloride
|
CDK
|
Cancer
|
|
Palbociclib (PD 0332991) monohydrochloride is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib monohydrochloride has potent anti-proliferative activity and induces cell cycle arrest in cancer cells, which can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma .
|
-
- HY-A0065
-
|
PD 0332991 isethionate
|
CDK
|
Cancer
|
|
Palbociclib (PD 0332991) isethionate is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib isethionate has potent anti-proliferative activity and induces cell cycle arrest in cancer cells, which can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma .
|
-
- HY-144786
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulin polymerization-IN-4 is a potent tubulin polymerization inhibitor with IC50 value of 4.6 μM. Tubulin polymerization-IN-4 can disrupt tubulin polymerization and vasculature, arrest the cell cycle at the G2/M phase, induce apoptosis, and suppress clonogenesis and migration in HeLa cells. Tubulin polymerization-IN-4 can be used for researching cervical cancer .
|
-
- HY-147854
-
|
|
Raf
Apoptosis
|
Cancer
|
|
B-Raf IN 9 (compound 8b) is a potent B-Raf inhibitor, with an IC50 of 24.79 nM. B-Raf IN 9 induces apoptosis and shows cell cycle arrest at G2/M phase. B-Raf IN 9 exhibits potent antitumor activity against human prostate cancer PC-3 cell line, with an IC50 of 7.83 µM .
|
-
- HY-50767D
-
|
PD 0332991 orotate
|
CDK
|
Cancer
|
|
Palbociclib (PD 0332991) orotate is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib orotate has potent anti-proliferative activity and induces cell cycle arrest in cancer cells. Palbociclib orotate can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma .
|
-
- HY-162755
-
|
|
SHP2
Apoptosis
|
Cancer
|
|
SHP2-IN-30 (compound 14i) is an allosteric SHP2 inhibitor with an IC50 of 104 nM. SHP2-IN-30 shows low inhibitory effect on SHP2-PTP. SHP2-IN-30 induces cell apoptosis and arrests the cell cycle at the G0/G1 phase .
|
-
- HY-115932
-
|
|
Aurora Kinase
Apoptosis
|
Cancer
|
|
Aurora kinase-IN-1 (Compound 9) is a potent inhibitor of aurora kinase. Aurora kinase-IN-1 upregulates the expression of G1 cell cycle inhibitory proteins including p21 and p27, and G1 progressive cyclin D1, and downregulates G1-to-S progressive cyclins, resulting in cell cycle arrest at the G1/S boundary. Aurora kinase-IN-1 also induces apoptosis. Aurora kinase-IN-1 is a lead compound for chemotherapeutic agents .
|
-
- HY-144712
-
|
|
G-quadruplex
Apoptosis
|
Cancer
|
|
L5-DA is a G-quadruplex (G4) ligand and selectively stabilized for G4s over ds26. L5-DA exhibits significant cytotoxicity against HeLa cells (IC50=4.3 μM). L5-DA stabilizes G4s in HeLa cells, induces apoptosis, and cell cycle arrest .
|
-
- HY-146311
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin polymerization-IN-16 (compound 5g) is a potent inhibitor of tubulin polymerization. Tubulin polymerization-IN-16 shows most potent against cancer cells, with IC50 values of 0.084-0.221 μM. Tubulin polymerization-IN-16 potently disrupts microtubule/tubulin dynamics, induces cell cycle arrest at G2/M phase in SGC-7901 cells .
|
-
- HY-138071
-
|
8αTGH
|
STAT
Pyroptosis
Apoptosis
Reactive Oxygen Species
c-Myc
Bcl-2 Family
TrxR
|
Cancer
|
|
8α-Tigloyloxyhirsutinolide 13-O-acetate (8αTGH) is a potent and orally active STAT3 inhibitor. 8α-Tigloyloxyhirsutinolide 13-O-acetate induces early oxidative stress and pyroptosis, and late DNA damage, cell cycle arrest, apoptosis in the TNBC cells. 8α-Tigloyloxyhirsutinolide 13-O-acetate suppresses tumor cell growth in vitro and tumor growth in vivo .
|
-
- HY-N2369A
-
|
|
Apoptosis
Influenza Virus
|
Infection
Cancer
|
|
Chelidonine (hydrochloride) is the hydrochloride form of Chelidonine (HY-N2369).Chelidonine, an isoquinoline alkaloid, can be isolated from Chelidonium majus L. Chelidonine causes G2/M arrest and induces caspase-dependent and caspase-independent apoptosis, and prevents cell cycle progression of stem cells in Dugesia japonica. Chelidonine has cytotoxic activity against melanoma cell lines. with anticancer and antiviral activity .
|
-
- HY-163707
-
|
|
Apoptosis
|
Cancer
|
|
UR778Br targets the GTPase-activating protein-related domain (GRD domain) of IQGAP1 proteins. UR778Br inhibits the proliferation of human acute myeloid leukemia (AML), arrests the cell cycle at the G2/M phase, and induces apoptosis. UR778Br inhibits colony formation of primary and AML cells, without significant impacts on normal bone marrow cells .
|
-
- HY-159515
-
|
|
Apoptosis
DNA/RNA Synthesis
Reactive Oxygen Species
|
Cancer
|
|
PBE-AMF is a prodrug that activates H2O2 with anticancer activity. PBE-AMF impedes tumor proliferation by inhibiting DNA synthesis, reducing ATP levels, inducing apoptosis, and arresting the cell cycle. PBE-AMF potently and selectively inhibits the proliferation of MDA-MB-231 cells (IC50=6.4 μM) while sparing non-cancerous MCF-10A cells .
|
-
- HY-117047
-
|
|
Apoptosis
Caspase
|
Cancer
|
|
ALC67 is a cytotoxic thiazolidine compound with an IC50 of approximately 5 μM against liver, breast cancer, colon cancer, and endometrial cancer cell lines. ALC67 induces apoptosis in cancer cells by activating caspase-9 and causing cell cycle arrest at the SubG1/G1 phase, via a pathway that is independent of death receptors. ALC67 can be used in cancer research .
|
-
- HY-163523
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
PYRIB-SO 2 is a potent antimitotic agent. PYRIB-SO 2 shows antiproliferative activity and induces cell cycle arrest at G2/M phase. PYRIB-SO 2 reduces and disruptes microtubule structures. PYRIB-SO 2 binds to the colchicine-binding site (C-BS) of α, β-tubulin .
|
-
- HY-N6939
-
|
|
HBV
Fungal
Apoptosis
Autophagy
Ferroptosis
|
Infection
Inflammation/Immunology
Cancer
|
|
Pseudolaric Acid B is a diterpene isolated from the root of Pseudolarix kaempferi (pinaceae), has anti-cancer, antifungal, and antifertile activities, and shows immunosuppressive activity on T lymphocytes . Pseudolaric Acid B inhibits hepatitis B virus (HBV) secretion through apoptosis and cell cycle arrest. Pseudolaric Acid B induces autophagy .
|
-
- HY-N7225
-
|
Gnidilatidin
|
DNA/RNA Synthesis
|
Cancer
|
|
Yuanhuacine (Gnidilatidin), a diterpene from Daphne genkwa, is an effective and highly selective inhibitor of the basal-like 2 (BL2) subtype of TNBC. Yuanhuacine can induce G2/M cell cycle arrest and has broad anti-tumor activity. Yuanhuacine is an orally active DNA damaging agent .
|
-
- HY-150004
-
|
|
c-Met/HGFR
HDAC
Apoptosis
|
Cancer
|
|
c-Met/HDAC-IN-3 (Compound 15f) is a dual c-Met and HDAC inhibitor with IC50 values of 12.50 nM and 26.97 nM against c-Met and HDAC1, respectively. c-Met/HDAC-IN-3 induces apoptosis and cause cell cycle arrest in G2/M phase .
|
-
- HY-143272
-
|
|
FGFR
|
Cancer
|
|
FGFR1 inhibitor-6 is a potent FGFR1 inhibitor with an IC50 value of 16.31 nM. FGFR1 inhibitor-6 shows cytotoxic activities. FGFR1 inhibitor-6 induces apoptosis and cell cycle arrest at pre-G1 and G2/M phase .
|
-
- HY-B2201
-
|
Sodium citrate; Trisodium citrate anhydrous
|
Apoptosis
Endogenous Metabolite
|
Metabolic Disease
Cancer
|
|
Citric acid trisodium is a natural preservative and food tartness enhancer. Citric acid trisodium induces apoptosis and cell cycle arrest at G2/M phase and S phase. Citric acid trisodium cause oxidative damage of the liver by means of the decrease of antioxidative enzyme activities. Citric acid trisodium causes renal toxicity in mice .
|
-
- HY-118798
-
|
NSC663285
|
Phosphatase
|
Cancer
|
|
DA 3003-2 is a potent and selectively Cdc25 inhibitor. DA 3003-2 shows antiproliferative activity. DA 3003-2 induces cell cycle arrest at the G2/M phase and increases the expression of P-tyr 15 Cdc2. DA 3003-2 has the potential for the research of prostate cancer .
|
-
- HY-155285
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
YS-363 is a potent, selective, and orally active EGFR inhibitor, with IC50s of 0.96 nM and 0.67 nM for wild-type and L858R mutant forms of EGFR, respectively. YS-363 can induce G0/G1 cell cycle arrest and apoptosis .
|
-
- HY-N7083R
-
|
|
Apoptosis
Aldehyde Dehydrogenase (ALDH)
|
Inflammation/Immunology
Cancer
|
|
Citral (Standard) is the analytical standard of Citral. This product is intended for research and analytical applications. Citral is an orally active monoterpene compound in lemon grass essential oil and a natural ALDH1A inhibitor, which can induce apoptosis and cycle arrest in breast cancer cell lines, and has analgesic, anti-injurious and anti-inflammatory effects .
|
-
- HY-N0211R
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
Cyasterone (Standard) is the analytical standard of Cyasterone. This product is intended for research and analytical applications. Cyasterone, a natural EGFR inhibitor, mainly isolated from Ajuga decumbens Thunb (Labiatae). Cyasterone manifests anti-proliferation effect by induced apoptosis and cell cycle arrests. Cyasterone may serves as a therapeutic anti-tumor agent against human tumors .
|
-
- HY-13630R
-
|
|
Topoisomerase
Bacterial
Autophagy
Apoptosis
|
Infection
Neurological Disease
Cancer
|
|
Etoposide phosphate (Standard) is the analytical standard of Etoposide phosphate. This product is intended for research and analytical applications. Etoposide phosphate (BMY-40481) is a potent anti-cancer chemotherapy agent and a selective topoisomerase II inhibitor to prevent re-ligation of DNA strands. Etoposide phosphate is the phosphate ester proagent of etoposide and is considered as active equivalent to Etoposide. Etoposide phosphate induces cell cycle arrest, apoptosis, and autophagy.
|
-
- HY-168071
-
|
|
Pim
|
Cancer
|
|
Pim-1 kinase inhibitor 11 (10f) is a PIM-1 inhibitor, with an IC50 of 0.18 μM. Pim-1 kinase inhibitor 11 (10f) exhibits anticancer activity. Pim-1 kinase inhibitor 11 (10f) induces apoptosis and arrests cell cycle progression .
|
-
- HY-117102
-
|
|
Aryl Hydrocarbon Receptor
Checkpoint Kinase (Chk)
|
Cancer
|
|
ANI-7 is an activator of aryl hydrocarbon receptor (AhR) pathway. ANI-7 inhibits the growth of multiple cancer cells, and potently and selectively inhibits the growth of MCF-7 breast cancer cells with a GI50 of 0.56 μM. ANI-7 induces CYP1-metabolizing mono-oxygenases by activating AhR pathway, and also induces DNA damage, checkpoint Kinase 2 (Chk2) activation, S-phase cell cycle arrest, and cell death in sensitive breast cancer cell lines .
|
-
- HY-126596
-
|
|
Apoptosis
|
Cancer
|
|
Angelylalkannin is a naphthoquinone compound isolated from the root of Alkanna tinctoria. Angelylalkannin showed significant inhibitory effects in the antiproliferative effect test on human colon cancer cells HCT-116 and SW-480. The median inhibitory concentration (IC50) of Angelylalkannin was 4.76 mM for HCT-116 cells and 7.03 mM for SW-480 cells. Like alkannin, Angelylalkannin can arrest the cell cycle in the G1 phase and induce apoptosis at a concentration of 1-10 mM.
|
-
- HY-116904
-
|
|
Apoptosis
Akt
|
Cancer
|
|
Anticancer agent 253 (Compound 26) has anti-cancer activity against breast cancer cells, with IC50s of 6 μM (MCF-7), 10 μM (MDA-MB-231) and 6.4 μM (4T1 cells). Anticancer agent 253 arrests cell cycle and induces mitochondria-mediated apoptosis in cancer cells. Anticancer agent 253 inhibits Akt phosphorylation in human breast and prostate cancer .
|
-
- HY-121222
-
|
|
PI3K
Apoptosis
|
Cancer
|
|
alpha-Bisabolol, an orally active sesquiterpene alcohol, induces cell cycle arrest, mitochondrial apoptosis and inhibition of PI3K/Akt signalling pathways. alpha-Bisabolol exerts a protective action against Cisplatin (HY-17394)-induced nephrotoxicity by mitigating inflammation and oxidative stress through the inhibition of NFκB activation. alpha-Bisabolol exhibits anti-inflammatory, analgesic, antibiotic and anticancer activities .
|
-
- HY-125542
-
|
|
Apoptosis
PI3K
Akt
|
Cancer
|
|
DCZ3301 is a potent aryl-guanidino inhibitor. DCZ3301 inhibits cell proliferation, induces G2/M cell cycle arrest and apoptosis. DCZ3301 inhibits the activation of the PI3K/AKT pathway by downregulating the protein expression of PI3K and phosphorylation of AKT. DCZ3301 can be used in research of cancer .
|
-
- HY-16291
-
|
LOR-253; LT-253
|
c-Myc
KLF
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
APTO-253 (LOR-253) is a small molecule that inhibits c-Myc expression, stabilizes G-quadruplex DNA, and induces cell cycle arrest and apoptosis in acute myeloid leukemia cells. APTO-253 mediates anticancer activity through induction of the Krüppel-like factor 4 (KLF4) tumor suppressor . APTO-253 has antiarthritic activity .
|
-
- HY-77813
-
|
|
Bacterial
Apoptosis
Antibiotic
Parasite
Autophagy
Reactive Oxygen Species
|
Infection
Endocrinology
Cancer
|
|
Benzyl isothiocyanate is an orally available isothiocyanate with bactericidal, anticancer, antiangiogenic and anthelmintic activities. Benzyl isothiocyanate exerts anticancer functions by regulating multiple signaling pathways, including apoptosis, cell proliferation, cell cycle arrest, metastasis, angiogenesis, and autophagy. In addition, Benzyl isothiocyanate can enhance muscle insulin sensitivity to improve obesity-induced hyperglycemia .
|
-
- HY-144774
-
|
|
Topoisomerase
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
Topoisomerase I inhibitor 5 is an effective topoisomerase inhibitor with IC50 value of. Topoisomerase I inhibitor 5 can interfere with DNA and significantly inhibit the activity of Topoisomerase I. Topoisomerase I inhibitor 5 can arrest cell cycle at the G1 phase and induce MCF-7 cells apoptosis. Topoisomerase I inhibitor 5 has potency in reversing P-gp-mediated resistance to Adriamycin .
|
-
- HY-150636
-
|
|
Autophagy
Apoptosis
|
Cancer
|
|
Autophagy-IN-1 is a potent autophagy/mitophagy inhibitor, acts by selectively increasing the autophagic flux while blocking the autophagosome-lysosome fusion in cancer cells. Autophagy-IN-1 can induce apoptosis and cell cycle arrest. Autophagy-IN-1 significantly inhibits tumor growth in an HCT116 xenograft mouse model and with low toxicity. Autophagy-IN-1 can be used for researching colorectal cancer .
|
-
- HY-149891
-
|
|
HSP
|
Cancer
|
|
HSP90-IN-23 (Comp 12-1) is an inhibitor of heat shock protein 90(HSP90) with an IC50 of 9 nM. HSP90-IN-23 induces apoptosis of tumor cells and arrests the tumor cell cycle in G0/G1 phase. HSP90-IN-23 can be used for cancer research .
|
-
- HY-161153
-
|
|
Apoptosis
|
Cancer
|
|
Microtubule inhibitor 9 (Compound O-7) is a 2-Aryl-1H-benzo [d] imidazole derivative with in vitro anticancer activity. Microtubule inhibitor 9 can induce cell cycle arrest at the G2/M phase and early apoptosis. Microtubule inhibitor 9 inhibits cancer cell migration by inhibiting wound healing and colony formation .
|
-
- HY-N1428S6
-
|
|
Isotope-Labeled Compounds
Endogenous Metabolite
Apoptosis
Antibiotic
|
Cancer
|
|
Citric acid-d4-1 is deuterated labeled Citric acid (HY-N1428) Citric acid is a natural preservative and food tartness enhancer. Citric acid induces apoptosis and cell cycle arrest at G2/M phase and S phase in HaCaT cells. Citric acid cause oxidative damage of the liver by means of the decrease of antioxidative enzyme activities. Citric acid causes renal toxicity in mice.
|
-
- HY-161957
-
|
|
Topoisomerase
|
Cancer
|
|
Top1/2-IN-1 (compound 23) is an orally available dual inhibitor of Top1/2 with antiproliferative activity. Top1/2-IN-1 damages DNA with increased levels of reactive oxygen species, inducing apoptosis and cell cycle arrest in cancer cells. Top1/2-IN-1 exhibits in vivo antitumor activity in xenograft models .
|
-
- HY-N1428R
-
-
- HY-N0421R
-
|
|
Apoptosis
|
Neurological Disease
Cancer
|
|
Cinobufagin (Standard) is the analytical standard of Cinobufagin. This product is intended for research and analytical applications. Cinobufagin is an anticancer agent that can be secreted by the Asiatic toad Bufo gargarizans. Cinobufagin induces the cell cycle arrests in the G1 phase or G2/M phase, leading to apoptosis in cancer cells. Cinobufagin inhibits tumor growth in melanoma and glioblastoma multiforme xenograft mouse models .
|
-
- HY-121607
-
|
|
AP-1
Apoptosis
|
Cancer
|
|
INI-43 is an inhibitor of Kpnβ1, interfering with the nuclear localization of Kpnβ1 and known Kpnβ1 cargo proteins, NFAT, NFκB, AP-1, and NFY. INI-43 can inhibit the proliferation of cancer cells, cause G2-M cell cycle arrest in cancer cells, and induce the intrinsic apoptosis pathway .
|
-
- HY-N2369R
-
|
|
Apoptosis
Influenza Virus
|
Infection
Cancer
|
|
Chelidonine (Standard) is the analytical standard of Chelidonine. This product is intended for research and analytical applications. Chelidonine, an isoquinoline alkaloid, can be isolated from Chelidonium majus L.. Chelidonine causes G2/M arrest and induces caspase-dependent and caspase-independent apoptosis, and prevents cell cycle progression of stem cells in Dugesia japonica. Chelidonine has cytotoxic activity against melanoma cell lines. with anticancer and antiviral activity .
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-
- HY-162868
-
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c-Met/HGFR
HDAC
Apoptosis
|
Cancer
|
c-Met/HDAC-IN-4 is a dual inhibitor of c-Met/HDAC. The IC50 value of c-Met/HDAC-IN-4 for c-Met is 28.92 nM. c-Met/HDAC-IN-4 can induce G0/G1 phase cell cycle arrest and apoptosis in MDA-MB-231 breast cancer cells, and it inhibits the proliferation and invasion of breast cancer cell lines .
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-
- HY-12037
-
|
ON-01910 sodium
|
Polo-like Kinase (PLK)
PI3K
Apoptosis
|
Cancer
|
|
Rigosertib sodium (ON-01910 sodium) is a multi-kinase inhibitor and a selective anti-cancer agent, which induces apoptosis by inhibition the PI3K/Akt pathway, promotes the phosphorylation of histone H2AX and induces G2/M arrest in cell cycle . Rigosertib sodium is a selective and non-ATP-competitive inhibitor of PLK1 with an IC50 of 9 nM .
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-
- HY-15221
-
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Apoptosis
Histone Demethylase
MDM-2/p53
|
Cardiovascular Disease
Cancer
|
|
Methylstat is a potent histone demethylases inhibitor. Methylstat shows anti-proliferative activity with low cytotoxicity. Methylstat induces apoptosis and cell cycle arrest at G0/G1 phase. Methylstat increases the expression of p53 and p21 protein levels. Methylstat inhibits angiogenesis induced by various cytokines. Methylstat can be used as a chemical probe for addressing its role in angiogenesis .
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-
- HY-143411
-
|
|
HDAC
Apoptosis
DNA/RNA Synthesis
|
Cancer
|
|
GEM144 is a potent and orally active DNA polymerase α (POLA1) and HDAC 11 dual inhibitor. GEM144 induces acetylation of p53, activation of p21, G1/S cell cycle arrest, and apoptosis. GEM144 has significant antitumor activity in human orthotopic malignant pleural mesothelioma xenografts .
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-
- HY-147892
-
|
|
HDAC
Apoptosis
|
Cancer
|
|
HDAC-IN-42 (compound 14f) is a potent and selective HDAC inhibitor with IC50 values of 0.19 and 4.98 μM for HDAC1 and HDAC6, respectively. HDAC-IN-42 shows anticancer and anti-proliferative activity. HDAC-IN-42 induces apoptosis and cell cycle arrest at G2/M phase .
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-
- HY-150615
-
|
|
SphK
Apoptosis
|
Cancer
|
|
SphK1-IN-2 is a potent, selective SphK1 inhibitor with IC50 values of 19.81 nM and ＞10 μM for SphK1 and SphK2, respectively. SphK1-IN-2 exhibits anti-proliferative activities and induces cell cycle arrest and apoptosis. SphK1-IN-2 can be used for cancer research .
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-
- HY-146666
-
|
|
Apoptosis
STAT
|
Cancer
|
|
STAT3-IN-9 is a potent STAT3 inhibitor. STAT3-IN-9 inhibits the activation of STAT3 (Tyr705) without influencing the phosphorylation of STAT1 (Tyr701). STAT3-IN-9 induces apoptosis and cell cycle arrest at the G2/M phase .
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-
- HY-151207
-
|
|
Apoptosis
ADC Cytotoxin
|
Cancer
|
|
Anticancer agent 81 (Compound 37b3) is an anticancer agent and can induce tumor cell cycle arrest and apoptosis. Anticancer agent 81 can be used as a payload to conjugate with Trastuzumab (HY-P9907) to obtain the antibody–agent conjugate (ADC) T-PBA. T-PBA maintained its mode of target and internalization ability of Trastuzumab .
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-
- HY-149889
-
|
|
Apoptosis
EGFR
|
Cancer
|
|
EGFR-IN-78 (compound A5)，a 2-aminopyrimidine derivative，is a reversible inhibitor of EGFR C797S-TK，and also an inducer of apoptosis. EGFR-IN-78 shows anti-proliferative activity，inhibits EGFR phosphorylation and arrests cell cycle at G2/M phase .
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-
- HY-156279
-
|
|
Apoptosis
HDAC
|
Cancer
|
|
HDAC6-IN-22 (compound 30) is a inhibitor of HDAC6, with the IC50 of 4.63 nM. HDAC6-IN-22 has antiproliferative effects in vitro and in vivo towards multiple myeloma. HDAC6-IN-22
induces cell cycle arrest in the G2 phase and promotes apoptosis through the mitochondrial pathway .
|
-
- HY-W013053
-
|
DBA; 1,2,5,6-Dibenzanthracene; Benzo[k]tetraphene
|
DNA/RNA Synthesis
Apoptosis
MDM-2/p53
|
Cancer
|
|
Dibenz[a,h]anthracene (DBA) is a polycyclic aromatic hydrocarbon (PAH) of considerable tumorigenicity. Dibenz[a,h]anthracene results in DNA adduct formation leading to the activation of a DNA damage response. Dibenz[a,h]anthracene induces cell cycle arrest and apoptosis via both Tp53-dependent and Tp53-independent mechanisms .
|
-
![Dibenz[a,h]anthracene](//file.medchemexpress.eu/product_pic/hy-w013053.gif)
- HY-164117
-
|
|
Biochemical Assay Reagents
|
Cancer
|
|
BNN6 is a thermoresponsive NO donor. BNN6 can be used to synthesize a multifunctional bio-transducer BNN6-BiTiS3-iRGD. BNN6-BiTiS3-iRGD can produce NO, arrest the cell cycle and induce apoptosis, and synergize with photothermal therapy (PTT) to ameliorate cancer .
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-
- HY-103688
-
|
|
ADC Cytotoxin
|
Cancer
|
|
AcBut-N-Ac-γ-Calicheamicin is an ADC cytotoxic payload that induces cell cycle arrest and apoptosis by causing DNA double-strand breaks. AcBut-N-Ac-γ-Calicheamicin is primarily used in the synthesis of antibody-drug conjugates (ADC) and holds promise for research in the field of cancer, including acute lymphoblastic leukemia (ALL) and other hematological malignancies .
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-
- HY-N0816R
-
|
|
Apoptosis
Pyroptosis
|
Cancer
|
|
Polyphyllin VI (Standard) is the analytical standard of Polyphyllin VI. This product is intended for research and analytical applications. Polyphyllin VI, an active saponin, possess anti-cancer activities. Polyphyllin VI induces G2/M cell cycle arrest and triggers apoptosis. Polyphyllin VI induces caspase-1-mediated pyroptosis via the induction of ROS/NF-κB/NLRP3/GSDMD signal axis in non-small cell lung cancer .
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-
- HY-A0098
-
|
|
Bacterial
Fungal
Influenza Virus
Antibiotic
|
Infection
Inflammation/Immunology
Cancer
|
|
Tunicamycin is a mixture of homologous nucleoside antibiotic that inhibits N-linked glycosylation and blocks GlcNAc phosphotransferase (GPT). Tunicamycin causes accumulation of unfolded proteins in cell endoplasmic reticulum (ER) and induces ER stress, and causes blocking of DNA synthesis and cell cycle arrest in G1 phase. Tunicamycin inhibits gram-positive bacteria, yeasts, fungi, and viruses and has anti-cancer activity .Tunicamycin increases exosome release in cervical cancer cells .
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-
- HY-144763
-
|
|
Apoptosis
|
Cancer
|
|
XPO1-IN-1 (compound D4) is an orally active and potent XPO1 inhibitor, with an IC50 of 24 nM in MM.1S cell. XPO1-IN-1 can efficiently induce cell apoptosis and cell cycle arrest. XPO1-IN-1 displays favorable metabolic stability and pharmacokinetic properties. XPO1-IN-1 can be used for multiple myeloma (MM) research .
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-
- HY-147839
-
|
|
Topoisomerase
Apoptosis
|
Cancer
|
|
Topoisomerase II inhibitor 10 (compound 32a) is a potent topoisomerase II inhibitor with an IC50 value of 7.45 μM. Topoisomerase II inhibitor 10 causes cell cycle arrest at G2-M phase and induces apoptosis of HepG-2 cells. Topoisomerase II inhibitor 10 has excellent anti-proliferative activities against HepG-2, MCF-7, and HCT-116 cells .
|
-
- HY-150540
-
|
|
Bcl-2 Family
Apoptosis
|
Cancer
|
|
Bcl-2-IN-10 is an active Bcl-2 inhibitor that can release up to four nitric oxide (NO) molecules. Bcl-2-IN-10 has cytotoxic activities against cancer cells, such as human leukemia, breast cancer and lung cancer. Bcl-2-IN-10 induces cell apopotosis and arrest cell cycle of G2/M phase, and can be used in cancer-related research .
|
-
- HY-149912
-
|
|
Polo-like Kinase (PLK)
Trk Receptor
Apoptosis
|
Cancer
|
|
CZS-241 is an orally active and selective inhibitor of Polo-like Kinase (PLK) 4 (IC50=2.6 nM). CZS-241 inhibits TRKA with an IC50 value of 2.74 μM. CZS-241 induces apoptosis and arrests cell cycle at S/G2 phase. CZS-241 shows highly potent antiproliferative activity against leukemia cell lines, and exhibits safety against normal cell lines .
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-
- HY-149474
-
|
|
FLT3
HDAC
Apoptosis
|
Cancer
|
|
HDAC-IN-63 (Compound 63) is a dual FLT3/HDAC inhibitor (IC50: 0.844 and 30.0 nM for FLT3 and HDAC1 respectively). HDAC-IN-63 inhibits MV4-11 cell proliferation (IC50: 92 nM. HDAC-IN-63 induces apoptosis and arrests cell cycle in MV4-11 cells. HDAC-IN-63 can be used for research of acute myeloid leukemia (AML) .
|
-
- HY-N3764
-
|
|
Akt
Dihydrofolate reductase (DHFR)
Endogenous Metabolite
|
Others
|
|
Diosbulbin C is a diterpene lactone component, which can be extracted from traditional Chinese medicine Dioscorea bulbifera L.. Diosbulbin C possesses high anticancer activity in non-small cell lung cancer (NSCLC). Diosbulbin C could induce cell cycle arrest at G0/G1 phase in NSCLC. Diosbulbin C also inhibits the proliferation of NSCLC cells, possibly by downregulating the expression/activation of AKT, DHFR, and TYMS .
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-
- HY-159560
-
|
|
Apoptosis
DNA/RNA Synthesis
|
Cancer
|
|
PBA-AMF can be activated by H2O2 to release Amonafide (AMF) (HY-10982). PBA-AMF selectively inhibited the proliferation of breast cancer cells, while sparing non-cancerous cells. PBA-AMF inhibits tumor proliferation by inhibiting DNA synthesis, reducing ATP levels, inducing apoptosis, and arresting the cell cycle. PBA-AMF can be used for research of tumors and other diseases associated with increased H2O2 levels .
|
-
- HY-158968
-
|
|
MDM-2/p53
|
Cancer
|
|
MMs02943764 is a 1,2,4-triazole derivative with anticancer activity. MMs02943764 has significant antiproliferative effects on multiple cancer cell lines. PAC, a structural analog of MMs02943764, has significant cytotoxicity against the leukemia cell line K562 (IC50=35.264 μM), reduces the degradation of p53 by inhibiting Mdm2 and Pirh2, and induces K562 cell cycle arrest .
|
-
- HY-168605
-
|
|
MMP
Apoptosis
|
Cancer
|
|
DH-18 is a matrix metalloproteinase-2 (MMP-2) inhibitor with the IC50 values of 139.45 nM, 518.11 nM and 833.34 nM for MMP-2, MMP-9 and MMP-8, respectively. DH-18 induces cell apoptosis and arrests cell cycle in the G0/G1 phase. DH-18 inhibits cell growth and can be used for study of chronic myeloid leukemia .
|
-
- HY-13442C
-
|
B1939 (mesylate) (purity>99%, single impurity ≤ 0.15%); E7389 (mesylate) (purity>99%, single impurity ≤ 0.15%); ER-086526 (mesylate) (purity>99%, single impurity ≤ 0.15%)
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Eribulin mesylate (purity>99%, single impurity ≤ 0.15%) is an inhibitor for microtubule. Eribulin mesylate (purity>99%, single impurity ≤ 0.15%) inhibits the proliferation of cancer cell LM8 and Dunn, inhibits the cell migration of LM8, arrests the cell cycle at G2/M phase, and induces apoptosis in LM8. Eribulin mesylate (purity>99%, single impurity ≤ 0.15%) exhibits antitumor efficacy in mouse model .
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-
- HY-N0202
-
|
Asterolide
|
ERK
Apoptosis
p38 MAPK
Akt
Src
STAT
|
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Atractylenolide II (Asterolide) is a sesquiterpenoid compound. Atractylenolide II can induce G1 phase cell cycle arrest and apoptosis in B16 melanoma cells. Atractylenolide II is an orally effective anticancer agent that can exert anti-melanoma effects by inhibiting the STAT3 signaling pathway. In addition, Atractylenolide II has been shown to ameliorate myocardial fibrosis, oxidative stress, and neuroprotective activity .
|
-
- HY-N0451
-
|
5,7-Dihydroxy-4'-methoxyflavone
|
Apoptosis
Autophagy
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Acacetin (5,7-Dihydroxy-4'-methoxyflavone) is an orally active flavonoid derived from Dendranthema morifolium. Acacetin docks in the ATP binding pocket of PI3Kγ. Acacetin causes cell cycle arrest and induces apoptosis and autophagy in cancer cells. Acacetin has potent anti-cancer and anti-inflammatory activity and has the potential for pain-related diseases research .
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-
- HY-103255
-
|
|
Apoptosis
|
Cancer
|
|
CFM-4 is a potent small molecular antagonist of CARP-1/APC-2 binding. CFM-4 prevents CARP-1 binding with APC-2, causes G2M cell cycle arrest, and induces apoptosis with an IC50 range of 10-15 μM. CFM-4 also suppresses growth of drug-resistant human breast cancer cells .
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-
- HY-146006
-
|
|
Microtubule/Tubulin
MMP
|
Cancer
|
|
Tubulin/MMP-IN-1 (compound 15g) is a potent inhibitor of tubulin and MMP. Tubulin/MMP-IN-1 has the potential for the research of cancer diseases. Tubulin/MMP-IN-1 suppresses tubulin polymerization, induces cell cycle arrest at the G2/M phase, leads to reactive oxidative stress (ROS) generation of HepG2 cells, and results in apoptosis by the mitochondrial-dependent apoptotic pathway .
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-
- HY-N1428S3
-
|
|
Apoptosis
Endogenous Metabolite
Antibiotic
|
Cancer
|
|
Citric acid- 13C3 is the 13C labeled Citric acid[1]. Citric acid is a natural preservative and food tartness enhancer. Citric acid induces apoptosis and cell cycle arrest at G2/M phase and S phase in HaCaT cells. Citric acid cause oxidative damage of the liver by means of the decrease of antioxidative enzyme activities. Citric acid causes renal toxicity in mice[2][3][4].
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-
- HY-115567
-
|
1-(β-D-2-Deoxyribofuranosyl)-5-nitroindole
|
Apoptosis
|
Cancer
|
|
5-NIdR (1-(β-D-2-Deoxyribofuranosyl)-5-nitroindole), an artificial nucleoside, exhibits the ability to inhibit the replication of DNA lesions generated by Temozolomide (HY-17364). 5-NIdR induces cancer cells apoptosis and arrests cell cycle at G0 phase. 5-NIdR enhances Temozolomide anti-tumor efficacy in murine glioblastoma model .
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-
- HY-149376
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 38 (compound 14) is a tetrazole-based Tubulin inhibitor with antiproliferative potencies. Tubulin inhibitor 38 (100 nM，24 h) mediates mitotic arrest，blocks cell cycle at G2/M phase and induces apoptosis. Tubulin inhibitor 38 exhibits high cytotoxicity with high selectivity index among HeLa，MCF7，and U87 MG cells .
|
-
- HY-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-116447
-
|
|
Mitochondrial Metabolism
Apoptosis
|
Cancer
|
|
Antitumor agent-159 (Compound 13b) targets the mitochondria and downregulates cardiolipin levels. Antitumor agent-159 inhibits the proliferation of cancer cell MDA-MB-231, arrests the cell cycle at sub-G1 phase, and induces apoptosis in MDA-MB-231. Antitumor agent-159 exhibits antitumor efficacy in MDA-MB-231 xenograft mouse models .
|
-
- HY-N0416R
-
-
- HY-W654305
-
|
PD 0332991-d4
|
Isotope-Labeled Compounds
CDK
|
Cancer
|
|
Palbociclib-d4 is deuterium labeled Palbociclib. Palbociclib (PD 0332991) is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib has potent anti-proliferative activity and induces cell cycle arrest in cancer cells, which can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma .
|
-
- HY-N1986R
-
|
|
HSP
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Cucurbitacin D (Standard) is the analytical standard of Cucurbitacin D. This product is intended for research and analytical applications. Cucurbitacin D is the active ingredient in Trichosanthes kirilowii and can disrupt the interaction between Hsp90 and two co-chaperones, Cdc37 and p23. Cucurbitacin D is an inflammasome activator. Cucurbitacin D induces cell cycle arrest and cell apoptosis, exhibiting anti-tumor and anti-inflammatory effects .
|
-
- HY-169418
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulin polymerization-IN-71 (Compound 4k) is an inhibitor for tubulin polymerization with an IC50 of 3.06 μM. Tubulin polymerization-IN-71 inhibits the proliferation of cancer cell MG-63 and U2OS with IC50 of 0.08-0.14 μM. Tubulin polymerization-IN-71 arrests the cell cycle at G2/M phase, and induces apoptosis in MG-63 .
|
-
- HY-12678R
-
|
|
ROS Kinase
Trk Receptor
Anaplastic lymphoma kinase (ALK)
Autophagy
|
Cancer
|
|
Entrectinib (Standard) is the analytical standard of Entrectinib. This product is intended for research and analytical applications. Entrectinib (NMS-E628) is an orally active, BBB-penetrated and centrally active inhibitor of TrkA/B/C, ROS1 and ALK, with IC50 values of 1, 3, 5, 12 and 7 nM, respectively. Entrectinib induces apoptosis and cycle arrest in cancer cells, has antitumor activity, and attenuates bleomycin-induced lung fibrosis in mice .
|
-
- HY-151980
-
|
|
Mps1
Apoptosis
|
Cancer
|
|
Mps1-IN-5 is a potent and orally active Mps1 inhibitor with an IC50 value of 29 nM. Mps1-IN-5 induces Apoptosis and cell cycle arrests at G2/M phase. Mps1-IN-5 shows antiproliferative activity and anti-tumor activity. Mps1-IN-5 inhibits phosphorylation of Mps1 and induces DNA damage .
|
-
- HY-149371
-
|
|
HDAC
Apoptosis
|
Cancer
|
|
HDAC6-IN-16 (compound 5c) is a histone deacetylase 6 (HDAC6) inhibitor, based on Quinazolin-4(3H)-One. HDAC6-IN-16 exhibits anticancer effect, inhibits colony-forming. And HDAC6-IN-16 arrests cell cycle at G2 phase and induces apoptosis .
|
-
- HY-115452
-
|
|
JAK
Apoptosis
|
Cancer
|
|
G5-7, an orally active and allosteric JAK2 inhibitor, selectively inhibits JAK2 mediated phosphorylation and activation of EGFR (Tyr 1068) and STAT3 by binding to JAK2. G5-7 induces cell cycle arrest, apoptosis and possesses antiangiogenic effect. G5-7 has the potential for glioma study .
|
-
- HY-161138
-
|
|
BCL6
Apoptosis
|
Cancer
|
|
WK369 is a novel BCL6 small molecule inhibitor, which exhibits excellent anti-ovarian cancer bioactivity, induces cell cycle arrest and causes apoptosis. WK369 can directly bind to the BCL6-BTB domain and block the interaction between BCL6 and SMRT, leading to the reactivation of p53, ATR and CDKN1A .
|
-
- HY-159101
-
|
|
EGFR
PD-1/PD-L1
|
Cancer
|
|
EP26 is a potent and orally active EGFR and PD-L1 inhibitor with IC50 values of 48.6 nM, 1.77 µM, respectively. EP26 decreased the protein expression of p-EGFR. EP26 induces cell cycle arrest at G0/G1 phase. EP26 has the potential for the research of glioblastoma .
|
-
- HY-161970
-
|
|
Topoisomerase
Apoptosis
|
Cancer
|
|
XSJ05 is a camptothecin (CPT) derivative that can inhibit topoisomerase I (Topo I) to exert anti-cancer activity. XSJ05 can trigger DNA double-strand breaks, leading to DNA damage. XSJ05 can inhibit the growth of colorectal cancer (CRC), arrest the cell cycle in G2/M phase, and induce apoptosis .
|
-
- HY-168559
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
EGFR-IN-131 (compound 3a) is a potent and cross the blood-brain barrier EGFR inhibitor with an IC50 value of 272.9 nM. EGFR-IN-131 shows antiproliferative activity. EGFR-IN-131 induces apoptosis and cell cycle arrest at G0/G1 phase. EGFR-IN-131 decreases the protein expression of p-EGFR .
|
-
- HY-W011762
-
|
|
Others
|
Cancer
|
|
VK3-OCH3 is a potent antitumor agent. VK3-OCH3 shows cytotoxicity for neuroblastoma cell lines and low cytotoxicity for normal cell lines. VK3-OCH3 induces apoptosis and cell cycle arrest at G2/M phase in IMR-32 cells. VK3-OCH3 shows antitumor activity .
|
-
- HY-155227A
-
|
|
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
|
ALK/EGFR-IN-2 is a potent dual inhibitor of ALK and EGFR. ALK/EGFR-IN-2 induces apoptosis and G0/G1 cell cycle arrest in cancer cells. ALK/EGFR-IN-2 significantly inhibits the cell proliferation of H1975, PC9, and Baf3-EML4-ALK cancer cell lines with IC50s of 0.0034, 0.0065, and 0.0018 μM, respectively .
|
-
- 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-146980
-
|
|
Apoptosis
GLUT
|
Cancer
|
|
GLUT4-IN-2 is a potent and selective GLUT4 inhibitor with IC50s of 11.4 µM and 6.8 µM for GLUT1 and GLUT4, respectively. GLUT4-IN-2 induces cell apoptosis and cell cycle arrest at G0/G1phase. GLUT4-IN-2 shows potent antitumor activity .
|
-
- 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-161470
-
|
|
Histone Demethylase
E1/E2/E3 Enzyme
DNA/RNA Synthesis
Caspase
Apoptosis
|
Cancer
|
|
WS-384 is a dual LSD1 and DCN1-UBC12 protein-protein interaction inhibitor with oral activity, with IC50 values of 338.79 nM and 14.81 nM, respectively. WS-384 possesses anticancer activity and can cause cell cycle arrest, DNA damage, and induce apoptosis. WS-384 can be used in the research of non-small cell lung cancer (NSCLC) .
|
-
- HY-16291A
-
|
LOR-253 hydrochloride; LT-253 hydrochloride
|
c-Myc
|
Inflammation/Immunology
|
|
APTO-253?(LOR-253) hydrochloride is a small molecule that inhibits c-Myc expression, stabilizes G-quadruplex DNA and induces cell cycle arrest and apoptosis in acute myeloid leukemia cells. APTO-253?hydrochloride mediates anticancer activity via induction of Kruppel-like factor 4?(KLF4)?tumor suppressor. APTO-253?hydrochloride exhibits antiarthritic activity .
|
-
- HY-162803
-
|
|
Apoptosis
c-Met/HGFR
STAT
|
Cancer
|
|
c-Met-IN-24 (compound 3g) is a dual-target inhibitor of STAT-3 ( =4.7 μM) and c-MET ( =12.67 μM) with anticancer activity. c-Met-IN-24 arrests the G2/M cell cycle and induces apoptosis in SNB-75 cells. c-Met-IN-24 can be used in the study of central nervous system cancers .
|
-
- HY-159613
-
|
|
Apoptosis
|
Cancer
|
|
PELP1-IN-1 is a PELP1 inhibitor. SMIP34 reduces cell viability and colony formation. PELP1-IN-1 induces apoptosis and cell cycle arrest at S phase. PELP1-IN-1 decreases the expression of PELP1. PELP1-IN-1 shows antitumor activity. SMIP34 has the potential for the research of triple-negative breast cancer (TNBC) .
|
-
- HY-168085
-
|
|
YAP
Apoptosis
|
Cancer
|
|
CV-4-26 (Compound 22) is a covalent inhibitor of TEAD. CV-4-26 inhibits YAP/TEAD-based transcription, leading to the reduction of CTGF and CYR61 expression. CV-4-26 inhibits Huh7 and HepG2 cell colony formation, induces cell cycle arrest, and apoptosis. CV-4-26 shows antitumor activity against hepatocellular carcinoma (HCC) and hepatoblastoma (HB) .
|
-
- 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-N12124
-
|
Monascinol
|
Akt
mTOR
AMPK
Androgen Receptor
Apoptosis
Autophagy
|
Cancer
|
|
Monascuspiloin (Monascinol) exhibits anti-androgenic activity with an IC50 of 7 μM. Monascuspiloin inhibits viability of PC-3 and LNCaP with IC50 of 45 and 47 μM. Monascuspiloin induces apoptosis in LNCaP through inhibition of Akt/mTOR signaling pathway, induces autophagy through activation AMPK signaling pathway and arrest cell cycle at G2/M phase in PC-3. Monascuspiloin exhibits antitumor efficacy in mice .
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-
- HY-N13201
-
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Apoptosis
CDK
|
Inflammation/Immunology
Cancer
|
|
12-Deoxyphorbol 13-palmitate is a traditional Chinese medicine monomer with antitumor activity that can be isolated from the root of Euphorbia fischeriana. 12-Deoxyphorbol 13-palmitate induces gastric cancer cell cycle arrest and apoptosis by regulating key cell cycle regulators such as cyclin B、cyclin A and CDC2. In addition, 12-Deoxyphorbol 13-palmitate can significantly weaken APOL2–SERCA2–PERK–HES1 signaling and slow liver fibrosis by targeting APOL2 .
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-
- HY-N9942
-
|
|
Apoptosis
Autophagy
NF-κB
p38 MAPK
PI3K
Akt
mTOR
STAT
JAK
|
Inflammation/Immunology
Cancer
|
|
Physalin A is a biologically active withanolide. Physalin A shows anti-inflammatory, antifibrotic and ameliorative effects on autophagy in models of disc degeneration. Physalin A has antitumor activity and can induce apoptosis, ROS production and G2/M phase cell cycle arrest. Besides. Physalin A can significantly increase the activity of quinone reductase and increase the expression of detoxifying enzymesc .
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-
- HY-144811
-
|
|
CDK
Apoptosis
|
Cancer
|
|
CDK2-IN-9 is a potent CDK2 inhibitor with an IC50 of 0.63 µM. CDK2-IN-9 shows antiproliferative activity. CDK2-IN-9 induces apoptosis and cell cycle arrest at S and G2/M phase. CDK2-IN-9 has the potential for the research of melanoma .
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-
- HY-155570
-
|
|
PI3K
Apoptosis
Caspase
PARP
|
Cancer
|
|
Anticancer agent 137 (8q) is a potent PI3k inhibitor. Anticancer agent 137 has broad-spectrum anticancer activity. Anticancer agent 137 induces G2/M cell cycle arrest and apoptosis. Anticancer agent 137 increases cleaved PARP, caspase 3, and 7. Anticancer agent 137 can be used in research of cancer .
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-
- HY-162631
-
|
|
Apoptosis
Isocitrate Dehydrogenase (IDH)
|
Cancer
|
|
IDH1 Inhibitor 9 (compound 11S) is a potent IDH1 inhibitor with IC50 values of 124.4, 95.7 nM for IDH1 R132H, IDH1 R132C, respectively. IDH1 Inhibitor 9 induces apoptosis and cell cycle arrest at the S phase. IDH1 Inhibitor 9 shows anti-tumor activity .
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-
- HY-N1428AR
-
|
|
Endogenous Metabolite
Apoptosis
Antibiotic
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Citric acid (monohydrate) (Standard) is the analytical standard of Citric acid (monohydrate). This product is intended for research and analytical applications. Citric acid monohydrate is a natural preservative and food tartness enhancer. Citric acid monohydrate induces apoptosis and cell cycle arrest at G2/M phase and S phase. Citric acid monohydrate cause oxidative damage of the liver by means of the decrease of antioxidative enzyme activities. Citric acid monohydrate causes renal toxicity in mice .
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-
- HY-146302
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|
|
Apoptosis
|
Cancer
|
|
14-3-3η Protein inhibitor 1 (Compound C11) is a 14-3-3η protein inhibitor with a KD of 35 µM. 14-3-3η Protein inhibitor 1 shows inhibitory activities against several typical human liver cancer cell lines. 14-3-3η Protein inhibitor 1 induces cell apoptosis and G1-S cell cycle arrest with good metabolic stability .
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-
- HY-146452
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|
|
Apoptosis
|
Cancer
|
|
Anticancer agent 57 (compound 14) potently inhibits MDA-MB-231, MDA-MB-468, and MCF-7 cell lines, with IC50s of 6.43 ~ 8.00 μM. Anticancer agent 57 induces cell cycle arrest and significantly promotes apoptosis. Anticancer agent 57 inhibits tumor growth in nude mice xenografted with MADMB-231 cells. Anticancer agent 57 can be used for researching triple negative breast cancer (TNBC) .
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-
- HY-145851
-
|
|
HDAC
Topoisomerase
Apoptosis
|
Cancer
|
|
Top/HDAC-IN-1 (Compound 29b) is a topoisomerase/HDAC dual inhibitor with IC50s of 18, 230, 790, 87, and 5250 nM for HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8, respectively. Top/HDAC-IN-1 exhibits potent antitumor activities against the HCT116 cell line with the IC50 of 180 nM. Top/HDAC-IN-1 efficiently induces apoptosis with G2 cell cycle arrest in HCT116 cells .
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-
- HY-156114
-
|
|
EGFR
CDK
|
Cancer
|
|
EGFR/CDK2-IN-2 (compound 6a) is a dual inhibitor of EGFR and CDK-2 with IC50s of 19.6 and 87.9 nM, respectively. EGFR/CDK2-IN-2 induces apoptosis in MCF-7 cells and arrests the cell cycle in the S phase. EGFR/CDK2-IN-2 has significant anti-cancer cell toxicity and inhibits MCF-7 with an IC50 of 0.39 μM .
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-
- HY-156115
-
|
|
EGFR
CDK
|
Cancer
|
|
EGFR/CDK2-IN-3 (compound 4b) is a dual inhibitor of EGFR and CDK-2 with IC50s of 71.7 and 113.7 nM, respectively. EGFR/CDK2-IN-3 induces apoptosis in MCF-7 cells and arrests the cell cycle in the S phase. EGFR/CDK2-IN-3 has significant anti-cancer cell toxicity and inhibits MCF-7 with an IC50 of 3.16 μM .
|
-
- HY-156116
-
|
|
EGFR
CDK
|
Cancer
|
|
EGFR/CDK2-IN-4 (compound 4c) is a dual inhibitor of EGFR and CDK-2 with IC50s of 89.6 and 165.4 nM, respectively. EGFR/CDK2-IN-4 induces apoptosis in MCF-7 cells and arrests the cell cycle in the S phase. EGFR/CDK2-IN-4 has significant anti-cancer cell toxicity and inhibits MCF-7 with an IC50 of 2.74 μM .
|
-
- HY-161372
-
|
|
PARP
c-Met/HGFR
Apoptosis
|
Cancer
|
|
PARP1/c-Met-IN-1 (Compound 16) is a selective dual inhibitor for PARP1 and c-Met, with IC50s of 3.3 and 32.2 nM, respectively. PARP1/c-Met-IN-1 induces cell apoptosis and cell cycle arrest in G2/M phase in MDA-MB-231 cells. PARP1/c-Met-IN-1 exhibits antitumor activity in mice .
|
-
- HY-119948
-
|
|
Cyclin G-associated Kinase (GAK)
MDM-2/p53
|
Cancer
|
AKCI is a type of AURKC-IκBα interaction inhibitor, with an IC50 value of 24.9 μM. In MDA-MB-231 cells, AKCI can induce G2/M cell cycle arrest by regulating the p53/p21/CDC2/cyclin B1 pathway, inhibit cell migration and invasion, and reduce colony formation and tumor growth. AKCI can be used for research on breast cancer .
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-
- HY-107632G
-
-
- HY-50767R
-
|
|
CDK
|
Cancer
|
|
Palbociclib (Standard) is the analytical standard of Palbociclib. This product is intended for research and analytical applications. Palbociclib (PD 0332991) is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib has potent anti-proliferative activity and induces cell cycle arrest in cancer cells, which can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma .
|
-
- HY-B0413
-
|
|
Parasite
HIF/HIF Prolyl-Hydroxylase
Microtubule/Tubulin
Antibiotic
|
Infection
Cancer
|
|
Fenbendazole is an orally active benzimidazole anthelmintic agent, with a broad antiparasitic range. Fenbendazole is a microtubule destabilizing agent and acts on helminthes primarily by binding to tubulin and disrupting the tubulin microtubule equilibrium. Fenbendazole stabilizes the transcriptional activator HIF-1α. Fenbendazole possesses an efficient anti-proliferative activity and induces apoptosis. Fenbendazole causes cell-cycle arrest and mitotic cell death, and has antitumor activity in mice xenografted with wild-type p53 .
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-
- HY-18981
-
|
(+)-Decursin
|
PKC
Apoptosis
CXCR
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Decursin ((+)-Decursin) is a potent anti-tumor agent. Decursin also is a cytotoxic agent and a potent protein kinase C activator. Decursin induces apoptosis and cell cycle arrest at G1 phase. Decursin decreases the expression of CDK2, CDK4, CDK6, cyclin D1 protein at 48 h. Decursin inhibits cell proliferation and migration. Decursin shows anti-tumor, anti-inflammatory and analgesic activities .
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-
- HY-114414
-
|
|
HDAC
mTOR
Apoptosis
|
Cancer
|
|
HDACs/mTOR Inhibitor 1 is a dual HDACs and mTOR inhibitor, with IC50s of 0.19 nM, 1.8 nM, 1.2 nM for HDAC1, HDAC6, mTOR, respectively. HDACs/mTOR Inhibitor 1 stimulates cell cycle arrest in G0/G1 phase and induces tumor cell apoptosis with low toxicity in vivo. HDACs/mTOR Inhibitor 1 can be used in the research of hematologic malignancies .
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-
- HY-14521
-
|
DDATHF
|
Antifolate
Apoptosis
Caspase
Bcl-2 Family
|
Cancer
|
|
Lometrexol (DDATHF), an antipurine antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) but do not induce detectable levels of DNA strand breaks. Lometrexol can further inhibit de novo purine synthesis, causing abnormal cell proliferation and apoptosis, even cell cycle arrest. Lometrexol has anticancer activity. Lometrexol also is a potent human Serine hydroxymethyltransferase1/2 (hSHMT1/2) inhibitor .
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-
- HY-14521B
-
|
DDATHF hydrate
|
Antifolate
Apoptosis
Caspase
Bcl-2 Family
|
Cancer
|
|
Lometrexol (DDATHF) hydrate, an antipurine antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) but do not induce detectable levels of DNA strand breaks. Lometrexol hydrate can further inhibit de novo purine synthesis, causing abnormal cell proliferation and apoptosis, even cell cycle arrest. Lometrexol hydrate has anticancer activity. Lometrexol hydrate also is a potent human Serine hydroxymethyltransferase1/2 (hSHMT1/2) inhibitor .
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-
- HY-147670
-
|
|
Hedgehog
Smo
Gli
Apoptosis
|
Cancer
|
|
TPB15 is an orally active and potent Hh (Hedgehog) signaling inhibitor. TPB15 markedly induces cell cycle arrest and apoptosis in MDA-MB-468 cells. TPB15 blocks Smo (Smoothened) translocation into the cilia and reduced Smo protein and mRNA expression. TPB15 inhibits the expression of the downstream regulatory factor glioma-associated oncogene 1 (Gli1). TPB15 shows good anti-tumor activity with low toxicity .
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-
- HY-161868
-
|
|
PARP
HDAC
Apoptosis
|
Cancer
|
|
DLC-50 is a dual inhibitor for PARP-1 and HDAC-1 with IC50 of 1.2 nM and 31 nM. DLC-50 inhibits the proliferation of cancer cells MDA-MB-436, MDA-MB-231, and MCF-7 with IC50 of 0.3, 2.7 and 2.41 μM. DLC-50 induces apoptosis in MDA-MB-231, arrests the cell cycle at G2 phase .
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-
- HY-N2342R
-
|
|
Apoptosis
|
Cancer
|
|
Procyanidin C1 (Standard) is the analytical standard of Procyanidin C1. This product is intended for research and analytical applications. Procyanidin C1 (PCC1), a natural polyphenol with oral activity, causes DNA damage, cell cycle arrest and induces apoptosis. Procyanidin C1 decreases the level of Bcl-2, but enhances BAX, caspase 3 and 9 expression in cancer cells. Procyanidin C1 shows senotherapeutic activity and increases lifespan in mice .
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-
- HY-13270
-
|
E7010
|
Microtubule/Tubulin
Autophagy
Apoptosis
|
Cancer
|
|
ABT-751 (E7010) is a novel, highly orally bioavailable sulfonamides antimitotic compound and tubulin binder. It prevents tubulin aggregation by binding to the colchicine site on β-tubulin, leading to cell cycle arrest in G2/M phase and inducing apoptosis, thus effectively preventing cell division. ABT-751 induces autophagy by inhibiting the AKT/MTOR signaling pathway. ABT-751 showed significant inhibition against various types of cancer cells, including lung, gastric, colon, and breast cancer .
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-
- HY-110293
-
|
|
FLT3
Apoptosis
|
Cancer
|
|
CHMFL-FLT3-122 is a potent, selective and orally active FLT3 kinase with an IC50 of 40 nM. CHMFL-FLT3-122 shows selectivity for FLT3 over BTK (IC50 of 421 nM) and c-KIT (IC50 of 559 nM) kinases. CHMFL-FLT3-122 induces apoptosis by arresting the cell cycle into the G0/G1 phase .
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-
- HY-130616
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
EGFR-IN-11 is a fourth-generation EGFR-tyrosine kinase inhibitor (EGFR-TKI) with an IC50 of 18 nM for triple mutant EGFR L858R/T790M/C797S. EGFR-IN-11 significantly suppresses the EGFR phosphorylation, induce the apoptosis, and arrest cell cycle at G0/G1 .
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-
- HY-19554
-
|
|
Histone Methyltransferase
Apoptosis
|
Cancer
|
|
MM-401 is a MLL1 H3K4 methyltransferase inhibitor. MM-401 inhibits MLL1 activity (IC50 = 0.32 μM) by blocking MLL1-WDR5 interaction. MM-401 can induce cell cycle arrest, apoptosis and differentiation. MM-401 can be used for the research of MLL leukemia .
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-
- HY-147513
-
|
|
Akt
Apoptosis
|
Cancer
|
|
AKT-IN-12 (compound 3e) is a potent Akt kinase inhibitor with an IC50 value of 0.55 μM. AKT-IN-12 induces G0/G1 cell cycle arrest and apoptosis. AKT-IN-12 also inhibits p-AKT, p-ERK, and activates p-JNK, JNK. AKT-IN-12 can be used for researching leukemia .
|
-
- HY-19554A
-
|
|
Histone Methyltransferase
Apoptosis
|
Cancer
|
|
MM-401 (TFA) is a MLL1 H3K4 methyltransferase inhibitor. MM-401 inhibits MLL1 activity (IC50 = 0.32 μM) by blocking MLL1-WDR5 interaction. MM-401 can induce cell cycle arrest, apoptosis and differentiation. MM-401 can be used for the research of MLL leukemia .
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-
- HY-148592
-
|
|
Cytochrome P450
|
Cancer
|
|
Antitumor agent-87 is a potent antitumor agent. Antitumor agent-87 shows a high affinity for CYP1A1 with a Ki value of 0.23 µM. Antitumor agent-87 shows antiproliferative activity. Antitumor agent-87 induces cell cycle arrest at the G2/M phase. Antitumor agent-87 show antitumoral activity .
|
-
- HY-149291
-
|
|
ATM/ATR
Apoptosis
|
Cancer
|
|
ATM Inhibitor-7 is a potent and selective ataxia-telangiectasia mutated (ATM) inhibitor with an IC50 value of 1.0 nM. ATM Inhibitor-7 induces Apoptosis and cell cycle arrest at G2/M phase when combinanted with CPT-11 (HY-16562). ATM Inhibitor-7 combines with CPT-11 shows antitumor activity .
|
-
- HY-149800
-
|
|
PARP
Apoptosis
Caspase
|
Cancer
|
|
PARP-1-IN-3, a benzamide derivative, is a potent PARP-1 inhibitor with IC50 values of 0.25 nM and 2.34 nM for PARP-1 and PARP-2, respectively. PARP-1-IN-3 induces apoptosis and arrest cell cycle at G2/M phase. PARP-1-IN-3 can be used in research of cancer .
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-
- HY-160853
-
|
|
Apoptosis
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 42 (Compound 14b) dose-dependently inhibited the activity of β-microtubulin (IC50 = 3.5 µM).Tubulin inhibitor 42 interferes with microtubule dynamic homeostasis, resulting in the arrest of the cancer cell cycle in the G2/M phase and inducing apoptosis. Tubulin inhibitor 42 significantly inhibits the angiogenic process in vitro and in vivo, preventing vascularization and tumor growth .
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-
- HY-120490
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
NMK-TD-100 is a modulator for microtubule. NMK-TD-100 binds to tubulin, inhibits the tubulin polymerization with an IC50 of 17.5 µM, inhibits mitosis, and decreases mitochondrial membrane potential (MMP). NMK-TD-100 inhibits the proliferation of HeLa with an IC50 of 1.42 µM, arrests cell cycle at G2/M phase, induces apoptosis in HeLa .
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-
- HY-N0662R
-
-
- HY-121605
-
|
|
Others
|
Cancer
|
|
RL71 is a curcuminoid anticancer agent that exhibits potent cytotoxicity against a variety of ER-negative breast cancer cells. RL71 (1 μM) induces cell cycle arrest in the G2/M phase and induces apoptosis in SKBr3 cells. RL7 also decreases HER2/neu phosphorylation and increases p27. RL71 also significantly reduced the phosphorylation of Akt and transiently increased the stress kinases JNK1/2 and p38 MAPK. Furthermore, RL71 exhibited anti-angiogenic potential in vitro, inhibiting the migration of HUVEC cells and the ability of these cells to form tubular networks .
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-
- HY-100574A
-
|
|
Protein Arginine Deiminase
Apoptosis
MicroRNA
|
Inflammation/Immunology
Cancer
|
|
Cl-amidine hydrochloride is an orally active peptidylarginine deminase (PAD) inhibitor, with IC50 values of 0.8 μM, 6.2 μM and 5.9 μM for PAD1, PAD3, and PAD4, respectively. Cl-amidine hydrochloride induces apoptosis in cancer cells. Cl-amidine hydrochloride induces microRNA (miR)-16 (miRNA-16, microRNA-16) expression and causes cell cycle arrest. Cl-Amidine hydrochloride prevents histone 3 citrullination and neutrophil extracellular trap formation, and improves survival in a murine sepsis model .
|
-
- HY-100574
-
|
|
Protein Arginine Deiminase
Apoptosis
MicroRNA
|
Inflammation/Immunology
Cancer
|
|
Cl-amidine is an orally active peptidylarginine deminase (PAD) inhibitor, with IC50 values of 0.8 μM, 6.2 μM and 5.9 μM for PAD1, PAD3, and PAD4, respectively. Cl-amidine induces apoptosis in cancer cells. Cl-amidine induces microRNA (miR)-16 (miRNA-16, microRNA-16) expression and causes cell cycle arrest. Cl-Amidine prevents histone 3 citrullination and neutrophil extracellular trap formation, and improves survival in a murine sepsis model .
|
-
- HY-146138
-
|
|
EGFR
VEGFR
Casein Kinase
Topoisomerase
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
EGFR-IN-57 (Compound 25a) is a potent, orally active EGFR-TK inhibitor with an IC50 of 0.054 µM. EGFR-IN-57 also inhibits VEGFR-2, CK2α, topoisomerase IIβ and tubulin polymerization with IC50 values of 0.087, 0.171, 0.13 and 3.61 µM, respectively. EGFR-IN-57 induces cell cycle arrest at G2/M and pre-G1 phases. EGFR-IN-57 induces cancer cell apoptosis .
|
-
- HY-19471
-
|
|
Others
|
Cancer
|
|
(rac)-ZK-304709 is an isomer of ZK-304709. It is a first-in-class oral multi-target tumor growth inhibitor that inhibits multiple cell cycle-dependent kinases (Cdks), vascular endothelial growth factor receptor kinases (VEGF-RTKs), and platelet-derived growth factor receptor kinase β (PDGF-RTKβ). (rac)-ZK-304709 can dose-dependently inhibit the proliferation and colony formation of neuroendocrine tumor (NET) cells. It directly acts on NET cells by inducing G2 cell cycle arrest and apoptosis, while reducing the expression of MCL1, survivin, and HIF1α. In an orthotopic BON tumor model, (rac)-ZK-304709 reduced primary tumor growth by 80% and reduced tumor microvascular density. These results suggest that (rac)-ZK-304709 can effectively control tumor growth by inducing apoptosis and inhibiting tumor-induced angiogenesis, and may be a potential agent for the treatment of NET.
|
-
- HY-158106
-
|
|
CDK
|
Cancer
|
|
AZD8421 is a selective CDK2 inhibitor (IC50: 9 nM) with selectivity for CDK1, CDK4 and CDK6. AZD8421 inhibits cancer cell proliferation by inhibiting pRB phosphorylation, inducing cell cycle arrest and senescence. AZD8421 demonstrated promising single efficacy and synergy with CDK4/6 inhibitors such as Palbociclib (HY-50767) in in vivo breast and ovarian models. AZD8421 also has potent single-agent inhibitory activity against drug-resistant breast cancer cells.
|
-
- HY-169075
-
|
|
HDAC
CDK
Apoptosis
|
Cancer
|
|
CDK/HDAC-IN-4 is a high selective dual cyclin-dependent kinase (CDK)/histone deacetylase (HDAC) inhibitor with IC50 values of 88.4 and 168.9 nM, respectively. CDK/HDAC-IN-4 exhibits antiproliferative capacities against hematological and solid tumor cells. CDK/HDAC-IN-4 also induces MV-4-11 cell Apoptosis and S cell cycle arrests. CDK/HDAC-IN-4 possesses a significant antitumor potency in the MV-4-11 xenograft model .
|
-
- HY-120914
-
|
GO-Y015
|
TrxR
Apoptosis
|
Cancer
|
|
TrxR1-IN-B19 (GO-Y015) (Compound B19) is a Curcumin (HY-N0005) derivative and colvalent TrxR1 inhibitor. TrxR1-IN-B19 inhibits TrxR1 enzyme activity to elevate oxidative stress, and then induce ROS-mediated ER Stress and mitochondrial dysfunction, subsequently resulting in cell cycle arrest and apoptosis .
|
-
- HY-11107
-
|
|
c-Met/HGFR
Autophagy
Apoptosis
|
Cancer
|
|
PHA-665752 is a selective, ATP-competitive, and active-site inhibitor of the catalytic activity of c-Met kinase (Ki=4 nM; IC50=9 nM). PHA-665752 exhibits >50-fold selectivity for c-Met compared with a panel of diverse tyrosine and serine-threonine kinases. PHA-665752 induces apoptosis and cell cycle arrest, and exhibits cytoreductive antitumor activity .
|
-
- HY-100900
-
|
|
Deubiquitinase
|
Cancer
|
|
ML364 is a selective ubiquitin specific peptidase 2 (USP2) inhibitor (IC50=1.1 μM) with anti-proliferative activity, which direct binds to USP2 (Kd=5.2 μM), induces an increase in cellular cyclin D1 degradation and causes cell cycle arrest. ML364 increases the levels of mitochondrial ROS and decreases in the intracellular content of ATP .
|
-
- HY-124421
-
|
NSC-703786
|
Aryl Hydrocarbon Receptor
|
Others
|
|
5F-203 (NSC-703786) is a cytotoxic molecule that forms DNA adducts and cell cycle arrest. 5F-203 induces aryl hydrocarbon receptor (AhR) signaling and elevates expression of CYP1A1. 5F-203 also increases the levels of reactive oxygen species as well as activates JNK, ERK, and p38 .
|
-
- HY-115909
-
|
|
CDK
|
Cancer
|
|
ZDLD20, a β-carboline, is orally active and selective CDK4/CycD3 inhibitor with an IC50 value of 6.51 μM. ZDLD20 exhibits potent anti-HCT116 activity including inhibition of colony formation, inhibition of invasion and migration, inducing of apoptosis, and arresting of G1 phase in cell cycle. ZDLD20 exhibits potent anticancer activity .
|
-
- HY-146492
-
|
|
VEGFR
Raf
Apoptosis
|
Cancer
|
|
VEGFR-2/BRAF-IN-2 (Compound 4a) is a dual VEGFR-2 and BRAF kinases inhibitor with IC50 values of 0.111, 0.089 and 0.071 µM against VEGFR-2, BRAF V600E and BRAF WT, respectively. VEGFR-2/BRAF-IN-2 induces apoptosis and arrests the cell cycle mainly in the G1 phase .
|
-
- HY-150511
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
3-(3-Phenoxybenzyl)amino-β-carboline is a potent tubulin inhibitor. 3-(3-Phenoxybenzyl)amino-β-carboline promotes selective degradation of αβ-tubulin heterodimers. 3-(3-Phenoxybenzyl)amino-β-carboline induces G2/M phase cell cycle arrest and apoptosis. 3-(3-Phenoxybenzyl)amino-β-carboline exhibits anticancer activity .
|
-
- HY-143278
-
|
|
Topoisomerase
FLT3
Apoptosis
|
Cancer
|
|
FLT3-IN-13 (compound 20) is a potent and effective antileukemic topoisomerase II and FLT3 dual inhibitor with IC50 values of 2.26 μM and 2.26 μM, respectively. FLT3-IN-13 arrests cell cycle at G2/M phase and induce apoptosis. FLT3-IN-13 has anticytotoxic activity, particularly against leukemia .
|
-
- HY-148522
-
|
|
FLT3
|
Cancer
|
|
FLT3-IN-18 is a potent and selective FLT3 inhibitor with an IC50 value of 0.003 μM. FLT3-IN-18 induces apoptosis and cell cycle arrest at G1 phase. FLT3-IN-18 inhibits FLT3 and STAT5 phosphorylation. FLT3-IN-18 has the potential for the research of acute myeloid leukemia (AML) .
|
-
- HY-115589
-
|
|
Polo-like Kinase (PLK)
Apoptosis
|
Cancer
|
|
YLT-11 is a potent, selective and orally active PLK4 inhibitor with Kd values of >10000, 653, >10000, 5.2 nM for PLK1, PLK2, PLK3, PLK4, respectively. YLT-11 shows antiproliferative activity. YLT-11 induces Apoptosis and cell cycle arrest at G2/M phase. YLT-11 show anticancer activity .
|
-
- HY-156737
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin polymerization-IN-49 (compound 12d) is a potent tubulin polymerization inhibitor. Tubulin polymerization-IN-49 bound to colchicine site on tubulin and inhibited tubulin polymerization. Tubulin polymerization-IN-49 induces cell cycle arrest at G2/M phase and apoptosis. Tubulin polymerization-IN-49 has anticancer active and prevents tumor generation, inhibits tumor proliferation and angiogenesis .
|
-
- HY-157320
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulin/PARP-IN-2 (compound 14) is a dual PARP-Tubulin inhibitor. Tubulin/PARP-IN-2 inhibits PARP1, PARP2, and tubulin activity with IC50 values of 74 nM, 109 nM, and 1.4 µM, respectively. Tubulin/PARP-IN-2 induces apoptosis as well as autophagy. Tubulin/PARP-IN-2 causes cell cycle arrest at the G2/M phase .
|
-
- HY-N6623R
-
|
|
Apoptosis
Endogenous Metabolite
Reactive Oxygen Species
|
Cancer
|
|
Malvidin-3-galactoside (chloride) (Standard) is the analytical standard of Malvidin-3-galactoside (chloride). This product is intended for research and analytical applications. Malvidin-3-galactoside chloride, an anthocyanin monomer, induces hepatocellular carcinoma (HCC) cells cycle arrest and apoptosis. Malvidin-3-galactoside chloride inhibits the production and accumulation of ROS. Malvidin-3-galactoside chloride has anti-tumor function .
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-
- HY-132260
-
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IMGN529; Debio 1562
|
Antibody-Drug Conjugates (ADCs)
Apoptosis
|
Cancer
|
|
Naratuximab emtansine (IMGN529) is a CD37-targeted ADC consisting of a humanized IgG1 mAb coupled to the microtubule disruptor DM1. Naratuximab emtansine has high affinity and specificity for CD37, allowing ADC internalization, processing and intracellular release of DM1. Due to its ability to disrupt microtubule assembly, DM1 can subsequently induce cell cycle arrest and apoptosis .
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-
- HY-169067
-
|
Mtx-C
|
p38 MAPK
|
Cancer
|
|
0-Methoxy-canthin-6-one (Mtx-C) is a DNA damage inducer. 0-Methoxy-canthin-6-one promotes cell cycle arrest at the G2/M phase by intercalating into DNA, thereby inducing myeloid differentiation of acute myeloid leukemia (AML) cells and leukemic stem cells (LSCs). The myeloid differentiation in AML and LSC cells is characterized by increased expression of myeloperoxidase, CD15, CD11b, and CD14, as well as activation of p38 MAPK. 0-Methoxy-canthin-6-one can be used in leukemia research .
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-
- HY-101029
-
|
|
NEKs
Apoptosis
|
Cancer
|
|
MBM-55 is a potent NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 1 nM. MBM-55 shows a 20-fold or greater selectivity in most kinases with the exception of RSK1 (IC50=5.4 nM) and DYRK1a (IC50=6.5 nM). MBM-55 effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis. MBM-55 shows antitumor activities, and no obvious toxicity to mice .
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-
- HY-N2071
-
-
- HY-100001
-
|
|
TRP Channel
CRAC Channel
Potassium Channel
Autophagy
Apoptosis
|
Cardiovascular Disease
Cancer
|
|
SKF-96365 hydrochloride is a potent TRP channel blocker and a store-operated Ca 2+ entry (SOCE) inhibitor. SKF-96365 hydrochloride significantly inhibits hERG, hKCNQ1/hKCNE1, hKir2.1 and hKv4.3 current, and significantly prolongs the QTc interval in isolated guinea pig hearts. SKF-96365 hydrochloride exhibits potent anti-neoplastic activity by inducing cell-cycle arrest and apoptosis in colorectal cancer cells .
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-
- HY-N7175
-
|
9,11-Dehydroergosterol peroxide; 9(11)-DHEP
|
Apoptosis
Endogenous Metabolite
|
Cancer
|
|
5,8-Epidioxyergosta-6,9(11),22-trien-3-ol (9,11-Dehydroergosterol peroxide), an important steroid from medicinal mushroom, exerts antitumor activity in several tumor types. 5,8-Epidioxyergosta-6,9(11),22-trien-3-ol inhibits HT29 cell growth by inducing CDKN1A expression, thus causing cell cycle arrest and apoptosis .
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-
- HY-144654
-
|
|
HDAC
Topoisomerase
|
Cancer
|
|
HDAC/Top-IN-1 is an orally active and pan HDAC/Top dual inhibitor with IC50s of 0.036 μM, 0.14 μM, 0.059 μM, 0.089 μM and 9.8 μM for HDAC1, HDAC2, HDAC3, HDAC6 and HDAC8. HDAC/Top-IN-1 efficiently induces apoptosis with S cell-cycle arrest in HEL cells. HDAC/Top-IN-1 has exhibits excellent in vivo antitumor efficacy .
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-
- HY-144293
-
|
|
Apoptosis
HDAC
|
Cancer
|
|
HDAC-IN-31 is a potent, selective and orally active HDAC inhibitor with IC50s of 84.90, 168.0, 442.7, >10000 nM for HDAC1, HDAC2, HDAC3, HDAC8, respectively. HDAC-IN-31 induces apoptosis and cell cycle arrests at G2/M phase. HDAC-IN-31 shows good antitumor efficacy. HDAC-IN-31 has the potential for the research of diffuse large B-cell lymphoma .
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-
- HY-146392
-
|
|
HDAC
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
HDAC-IN-39 (compound 16c) is a potent HDAC inhibitor, with IC50 values of 1.07 μM (HDAC1), 1.47 μM (HDAC2), and 2.27 μM (HDAC3), respectively. HDAC-IN-39 also significantly inhibits microtubule polymerization. HDAC-IN-39 induces cell cycle arrest at the G2/M phase. HDAC-IN-39 displays promising anticancer activity against resistant cancer cells .
|
-
- HY-146444
-
|
|
Apoptosis
Bcl-2 Family
Caspase
Reactive Oxygen Species
|
Cancer
|
|
Anticancer agent 56 (compound 4d) is a potent anti-cancer agent with agent-likeness properties, possessing anticancer activity against several cancer cell lines (IC50<3 μM). Anticancer agent 56 induces cell cycle arrest at G2/M phase and triggers mitochondrial apoptosis pathway. Anticancer agent 56 acts by accumulation of ROS, up regulation of BAX, down regulation of Bcl-2 and activation of caspases 3, 7, 9 .
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-
- HY-146200
-
|
|
PI3K
mTOR
|
Cancer
|
|
PI3K/mTOR Inhibitor-8 (Compound 18b) is a PI3K and mTOR dual inhibitor with IC50 values of 0.46 nM and 12 nM against PI3Kα and mTOR, respectively. PI3K/mTOR Inhibitor-8 induces HCT-116 cells apoptosis and arrests cell cycle at the G1/S phase .
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-
- HY-146228
-
|
|
HSP
Apoptosis
Topoisomerase
EGFR
VEGFR
|
Cancer
|
|
HSP90-IN-13 (compound 5k) is a highly potent HSP90 pan inhibitor with an IC50 value of 25.07 nM. HSP90-IN-13 has multi-target activity against EGFR, VEGFR-2 and Topoisomerase-2. HSP90-IN-13 causes cell cycle arrest at G2/M phase and induces apoptosis of MCF-7 cells through mitochondrial-mediated pathway .
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-
- HY-N2983
-
|
|
Tyrosinase
|
Others
|
|
Cajanin is a potent and orally active anti-melanogenic agent. Cajanin shows antiproliferative activity in MNT1 Cells. Cajanin efficiently decreases the melanin content. Cajanin down-regulates the mRNA and protein expression levels of MITF, tyrosinase, TRP-1 and Dct (TRP-2). Cajanin induces cell cycle arrest at G2/M and S phase. Cajanin stimulates osteoblast proliferation. Cajanin has the potential for the research of human hyperpigmented disorders and menopausal osteoporosis .
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-
- HY-149029
-
|
|
HDAC
Apoptosis
Reactive Oxygen Species
|
Cancer
|
|
TH-6 is a potent HDAC inhibitor with IC50s of 0.115, 0.135, 0.242, 0.138, 2.120 µM for HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, respectively. TH-6 inhibits cell migration and invasion. TH-6 induces apoptosis and cell cycle arrest at G2/M phase. TH-6 shows anti-tumor activity .
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-
- HY-14521A
-
|
DDATHF disodium
|
Antifolate
Apoptosis
Caspase
Bcl-2 Family
|
Cancer
|
|
Lometrexol (DDATHF) disodium, an antipurine antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) but do not induce detectable levels of DNA strand breaks. Lometrexol disodium can further inhibit de novo purine synthesis, causing abnormal cell proliferation and apoptosis, even cell cycle arrest. Lometrexol disodium has anticancer activity. Lometrexol disodium also is a potent human Serine hydroxymethyltransferase1/2 (hSHMT1/2) inhibitor .
|
-
- HY-148333
-
MS177
2 Publications Verification
|
PROTACs
Histone Methyltransferase
Apoptosis
|
Cancer
|
|
MS177 is an effective and fast-acting EZH2 degrader. MS177 is a PROTAC that consists of a CRBN ligand, linker, and a potent enzymatic EZH2 inhibitor C24 (C24 IC50): 12?nM). MS177 effectively depletes both canonical EZH2–PRC2 and noncanonical EZH2–cMyc complexes. MS177 induces leukaemia cell growth inhibition, apoptosis and cell cycle progression arrest .
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-
- HY-149630
-
|
|
VEGFR
HDAC
Apoptosis
|
Cancer
|
|
VEGFR2/HDAC1-IN-1 (compound 13) is a potent VEGFR-2/HDAC dual inhibitor, with IC50s of 57.83 nM and 9.82 nM, respectively. VEGFR2/HDAC1-IN-1 arrests the cell cycle at the S and G2 phases, and induces apoptosis in HeLa cells. VEGFR2/HDAC1-IN-1 exhibits anti-angiogenic effect .
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-
- 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 .
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-
- HY-N0451R
-
|
5,7-Dihydroxy-4'-methoxyflavone (Standard)
|
Apoptosis
Autophagy
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Acacetin (Standard) is the analytical standard of Acacetin. This product is intended for research and analytical applications. Acacetin (5,7-Dihydroxy-4'-methoxyflavone) is an orally active flavonoid derived from Dendranthema morifolium. Acacetin docks in the ATP binding pocket of PI3Kγ. Acacetin causes cell cycle arrest and induces apoptosis and autophagy in cancer cells. Acacetin has potent anti-cancer and anti-inflammatory activity and has the potential for pain-related diseases research .
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-
- HY-162679
-
|
|
c-Met/HGFR
Apoptosis
|
Cancer
|
|
c-Met degrader-1 (Compound H11) is an orally active c-Met degrader (through the ubiquitin proteasome system). c-Met degrader-1 has anti-hepatocellular carcinoma activity (HCC) and inhibits tumor growth in MHCC97H xenografts. c-Met degrader-1 inhibits HCC cell growth, arrests cell cycle, and induces apoptosis. c-Met degrader-1 may overcome resistance to type Ib inhibitors .
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-
- HY-N13063
-
|
|
Apoptosis
Reactive Oxygen Species
PI3K
Akt
|
Cancer
|
|
Anticancer agent 235 (Compound 49) is a modulator for PI3K/AKT/mTOR pathway, that promotes the generation of ROS, reduces the mitochondrial membrane potential, and thereby inhibits the proliferation of cancer cells HCT116, Caco-2, AGS and SMMC-772 with IC50 of 0.35-26.9 μM. Anticancer agent 235 arrests the cell cycle at G2/M phase, and induces apoptosis in HCT116 .
|
-
- HY-168072
-
|
|
Interleukin Related
Apoptosis
Autophagy
|
Cancer
|
|
GP130-IN-1 (compound 49) is a potent GP130 inhibitor with significant in vitro antitumor activity and higher selectivity than Bazedoxifene (HY-A0031). GP130-IN-1 induces ultrastructural changes in cells, causing cell cycle arrest in the G0/G1 phase in a time-dependent manner and triggering apoptosis and autophagy. GP130-IN-1 can be used in the study of triple-negative breast cancer .
|
-
- HY-117688
-
|
|
HDAC
Topoisomerase
Apoptosis
|
Cancer
|
|
WJ35435 is a dual-targeted anticancer hybrid that induces anti-HDAC (in particular HDAC1 and HDAC6) and anti-topoisomerase I activities that causes DNA damage associated with a low DNA repair capability and induces cell cycle arrest at G1- and G2-phase to apoptosis. WJ35435 induces histone H3 acetylation and phosphorylation, α-tubulin acetylation and γ-H2AX formation to achieve anti-HDAC effect. WJ35435 is promising for research of cancer .
|
-
- HY-100574B
-
|
|
Protein Arginine Deiminase
Apoptosis
MicroRNA
|
Inflammation/Immunology
Cancer
|
|
Cl-amidine TFA is an orally active peptidylarginine deminase (PAD) inhibitor, with IC50 values of 0.8 μM, 6.2 μM and 5.9 μM for PAD1, PAD3, and PAD4, respectively. Cl-amidine TFA induces apoptosis in cancer cells. Cl-amidine TFA induces microRNA (miR)-16 (miRNA-16, microRNA-16) expression and causes cell cycle arrest. Cl-Amidine TFA prevents histone 3 citrullination and neutrophil extracellular trap formation, and improves survival in a murine sepsis model .
|
-
- HY-110382S
-
|
13C20,15N10-c-di-GMP, 13C20,15N10-Cyclic diguaylate, 13C20,15N10-3’,5’-Cyclic diguaylic Acid
|
Isotope-Labeled Compounds
Endogenous Metabolite
STING
|
Cancer
|
|
13C20, 15N10-Cyclic di-GMP ( 13C20, 15N10-c-di-GMP) is 13C and 15N labeled Cyclic-di-GMP (disodium). Cyclic-di-GMP disodium is a STING agonist and a bacterial second messenger that coordinates different aspects of bacterial growth and behavior, including motility, virulence, biofilm formation, and cell cycle progression. Cyclic-di-GMP disodium has anti-cancer cell proliferation activity and also induces elevated CD4 receptor expression and cell cycle arrest. Cyclic-di-GMP disodium can be used in cancer research .
|
-
- HY-146683
-
|
|
Aldehyde Dehydrogenase (ALDH)
Apoptosis
|
Cancer
|
|
KS106 is a potent ALDH inhibitor with IC50s of 334, 2137, 360 nM for ALDH1A1, ALDH2, and ALDH3A1, respectively. KS106 shows antiproliferative and anticancer effects with low low toxic.KS106 significantly increases ROS activity, lipid peroxidation and toxic aldehyde accumulation. KS106 induces apoptosis and cell cycle arrest at the G2/M phase .
|
-
- HY-146682
-
|
|
Aldehyde Dehydrogenase (ALDH)
Apoptosis
|
Cancer
|
|
KS100 is a potent ALDH inhibitor with IC50s of 230, 1542, 193 nM for ALDH1A1, ALDH2, and ALDH3A1, respectively. KS100 shows antiproliferative and anticancer effects with low low toxic. KS100 significantly increases ROS activity, lipid peroxidation and toxic aldehyde accumulation. KS10600 induces apoptosis and cell cycle arrest at the G2/M phase .
|
-
- HY-157165
-
|
|
Microtubule/Tubulin
PARP
|
Cancer
|
|
Tubulin/PARP-IN-1 (compound 14) is a dual PARP-tubulin inhibitor with activity against endometrial cancer. Tubulin/PARP-IN-1 inhibits PARP and tubulin with IC50s of 74 nM (PARP1), 109 nM (PARP2), and 1.4 μM (Microtubule/Tubulin), respectively. Tubulin/PARP-IN-1 can induce apoptosis and autophagy and cause cell cycle arrest in the G2/M phase .
|
-
- HY-155489
-
|
|
Anaplastic lymphoma kinase (ALK)
Apoptosis
|
Cancer
|
|
DDO-2728 (compound 19) is a selective AlkB homologue 5 (ALKBH5) inhibitor with an IC50 of 2.97 μM. DDO-2728 increases the abundance of N 6 methyladenosine (m 6A) modifications, inducing cell apoptosis and cycle arrest. DDO-2728 suppresses tumor growth in the MV4−11 xenograft model with favorable safety profile, shows the potential of targeting ALKBH5 in cancer research .
|
-
- HY-163371
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
EGFR WT/T790M-IN-1 (Compound 16h) is a dual EGFR WT and EGFR T790 inhibitor. EGFR WT/T790M-IN-1 can arrest the cell cycle in G2/M phase and induce apoptosis. EGFR WT/T790M-IN-1 has anti-cancer activity .
|
-
- HY-N6939R
-
|
|
HBV
Fungal
Apoptosis
Autophagy
Ferroptosis
|
Infection
Inflammation/Immunology
Cancer
|
|
Pseudolaric Acid B (Standard) is the analytical standard of Pseudolaric Acid B. This product is intended for research and analytical applications. Pseudolaric Acid B is a diterpene isolated from the root of Pseudolarix kaempferi (pinaceae), has anti-cancer, antifungal, and antifertile activities, and shows immunosuppressive activity on T lymphocytes . Pseudolaric Acid B inhibits hepatitis B virus (HBV) secretion through apoptosis and cell cycle arrest. Pseudolaric Acid B induces autophagy .
|
-
- HY-162456
-
|
|
Apoptosis
Reactive Oxygen Species
|
Cancer
|
|
Anticancer agent 205 (compound 9) is a potent anticancer agent. Anticancer agent 205 binds to G4-mtDNA target and inhibits the replication, transcription, and translation of mtDNA (mitochondrial genome). Anticancer agent 205 causes mitochondrial dysfunction, increases ROS production, induces DNA damage and cellular senescence. Anticancer agent 205 induces apoptosis and cell cycle arrests at G0/G1 phase. Anticancer agent 205 has the potential for the research of colorectal cancer .
|
-
- HY-12678S
-
|
NMS-E628-d4; RXDX-101-d4
|
ROS Kinase
Trk Receptor
Anaplastic lymphoma kinase (ALK)
Autophagy
Isotope-Labeled Compounds
|
Cancer
|
|
Entrectinib-d4 (NMS-E628-d4; RXDX-101-d4) is the deuterium labeled Entrectinib (HY-12678). Entrectinib is an orally active, BBB-penetrated and centrally active inhibitor of TrkA/B/C, ROS1 and ALK, with IC50 values of 1, 3, 5, 12 and 7 nM, respectively. Entrectinib induces apoptosis and cycle arrest in cancer cells, has antitumor activity, and attenuates bleomycin-induced lung fibrosis in mice .
|
-
- HY-137497
-
|
|
Ras
Apoptosis
|
Cancer
|
|
KRAS inhibitor-9, a potent KRAS inhibitor (Kd=92 μM), blocks the formation of GTP-KRAS and downstream activation of KRAS. KRAS inhibitor-9 binds to KRAS G12D, KRAS G12C and KRAS Q61H protein with a moderate binding affinity. KRAS inhibitor-9 causes G2/M cell cycle arrest and induces apoptosis. KRAS inhibitor-9 selectively inhibits the proliferation of NSCLC cells with KRAS mutation but not normal lung cells .
|
-
- HY-150772
-
|
|
Microtubule/Tubulin
HDAC
Apoptosis
Mitochondrial Metabolism
|
Cancer
|
|
Tubulin/HDAC-IN-1 is a dual tubulin and HDAC-IN-1 inhibitor through CH/π interaction with tubulin and hydrogen bond interaction with HDAC8. Tubulin/HDAC-IN-1 inhibits tubulin polymerization and selectively inhibits HDAC8 (IC50: 150 nM). Tubulin/HDAC-IN-1 has cytotoxicity against various human cancer cells, also arrests cell cycle in the G2/M phase and induces cell apoptosis. Tubulin/HDAC-IN-1 can be used in the research of hematologic and solid tumors such as neuroblastoma, leukemia .
|
-
- HY-151154
-
|
|
EGFR
|
Cancer
|
|
EGFR/HER2/DHFR-IN-1 is a potent anticancer agent with high selectivity against MCF-7 breast cancer cells. EGFR/HER2/DHFR-IN-1 is a multiple inhibitor of EGFR/HER2 kinase and DHFR, with IC50s of 0.153 μM, 0.108 μM, 0.291 μM, respectively. EGFR/HER2/DHFR-IN-1 arrests cell cycle at G1/S and induces cells apoptosis .
|
-
- HY-162308
-
|
|
Histone Methyltransferase
Apoptosis
|
Cancer
|
|
NSD-IN-3 (compound 3) is a potent nuclear receptor binding SET domain (NSD) inhibitor. NSD-IN-3 inhibits NSD2-SET and NSD3-SET with IC50 values of 0.81 μM and 0.84 μM, respectively. NSD-IN-3 inhibits histone H3K36 dimethylation and decreases the expression of NSDs-targeted genes in non-small cell lung cancer cells. NSD-IN-3 induces s-phase cell cycle arrest and apoptosis .
|
-
- HY-161644
-
|
|
STAT
Apoptosis
|
Cancer
|
|
STAT3-IN-27 (Compound 41) is an orally active inhibitor for phosphorylation of STAT3 (KD is 4.4 μM) and STAT3 transcription (IC50 is 22.57 nM). STAT3-IN-27 inhibits proliferation of various cancer cells with IC50 of 10-500 nM. STAT3-IN-27 arrests the cell cycle at G2/M phase, induces mitochondrial dysfunction and apoptosis in HCT116, inhibits cell migration of HCT116. STAT3-IN-27 exhibits antitumor efficacy in mouse model .
|
-
- HY-169019
-
|
|
PI3K
Apoptosis
|
Cancer
|
XJTU-L453 is a PI3Kα inhibitor with an IC50 value of 0.4 nM. XJTU-L453 can inhibit the proliferation of breast cancer cell lines T47D and MCF7, with IC50 values of 0.2 μM and 0.5 μM, respectively. XJTU-L453 can inhibit the PI3K pathway, induce cell cycle arrest, and trigger cell apoptosis (apoptosis). XJTU-L453 also has antitumor activity in MCF7 xenograft mice .
|
-
- HY-13270A
-
|
E7010 hydrochloride
|
Microtubule/Tubulin
Autophagy
Apoptosis
|
Cancer
|
|
ABT-751 (E7010) hydrochloride is a novel, highly orally bioavailable sulfonamides antimitotic compound and tubulin binder. It prevents tubulin aggregation by binding to the colchicine site on β-tubulin, leading to cell cycle arrest in G2/M phase and inducing apoptosis, thus effectively preventing cell division. ABT-751 (E7010) hydrochloride induces autophagy by inhibiting the AKT/MTOR signaling pathway. ABT-751 (E7010) hydrochloride showed significant inhibition against various types of cancer cells, including lung, gastric, colon, and breast cancer .
|
-
- HY-161694
-
|
|
DNA Methyltransferase
|
Cancer
|
|
DNMT1-IN-3 (compound 7t-S) is an effective DNA methyltransferase 1 (DNMT1) inhibitor with an IC50 value of 0.777 μM and a KD value of 0.183 μM. DNMT1-IN-3 can bind to the methyl donor S-adenosyl-l-methionine (SAM) site in DNMT1. DNMT1-IN-3 can inhibit cell proliferation in K562 cells by inducing cells apoptosis and arresting cell cycle at G0 / G1 phase, which has the potential to be used for the research of hematologic tumor .
|
-
- HY-121222R
-
|
|
PI3K
Apoptosis
|
Cancer
|
|
alpha-Bisabolol (Standard) is the analytical standard of alpha-Bisabolol. This product is intended for research and analytical applications. alpha-Bisabolol, an orally active sesquiterpene alcohol, induces cell cycle arrest, mitochondrial apoptosis and inhibition of PI3K/Akt signalling pathways. alpha-Bisabolol exerts a protective action against Cisplatin (HY-17394)-induced nephrotoxicity by mitigating inflammation and oxidative stress through the inhibition of NFκB activation. alpha-Bisabolol exhibits anti-inflammatory, analgesic, antibiotic and anticancer activities .
|
-
- HY-B0413R
-
|
|
Parasite
HIF/HIF Prolyl-Hydroxylase
Microtubule/Tubulin
Antibiotic
|
Infection
|
|
Fenbendazole (Standard) is the analytical standard of Fenbendazole. This product is intended for research and analytical applications. Fenbendazole is an orally active benzimidazole anthelmintic agent, with a broad antiparasitic range. Fenbendazole is a microtubule destabilizing agent and acts on helminthes primarily by binding to tubulin and disrupting the tubulin microtubule equilibrium. Fenbendazole stabilizes the transcriptional activator HIF-1α. Fenbendazole possesses an efficient anti-proliferative activity and induces apoptosis. Fenbendazole causes cell-cycle arrest and mitotic cell death, and has antitumor activity in mice xenografted with wild-type p53 .
|
-
- HY-144725
-
|
|
HDAC
Apoptosis
|
Cancer
|
|
HDAC1/6-IN-1 (compound D7) is a potent multitarget inhibitor of GLP, HDAC6 and HDAC1, with IC50 values of 1.3, 13, and 89 nM, respectively. HDAC1/6-IN-1 can inhibit the methylation and deacetylation of H3K9 on protein level. HDAC1/6-IN-1 induces cancer cell apoptosis, G0/G1 cell cycle arrest, and blocks migration and invasion .
|
-
- HY-148712
-
|
|
Apoptosis
Sirtuin
|
Cancer
|
|
SIRT6 activator 12q is potent, selective and orally active SIRT6 activator with IC50 values of 171.20, >200, >200, >200, 0.58 μM for SIRT1, SIRT2, SIRT3, SIRT5, SIRT6, respectively. SIRT6 activator 12q inhibits cell growth and migration. SIRT6 activator 12q induces Apoptosis and cell cycle arrest at G2 phase. SIRT6 activator 12q shows anticancer activity .
|
-
- HY-148833
-
|
|
MDM-2/p53
|
Cancer
|
|
MDM2-p53-IN-16 is a MDM2-p53 complex inhibitor with an IC50 value of 4.3 nM to dissociate human p53/MDM2 complex. MDM2-p53-IN-16 reactivates p53, and induces Glioblastoma Multiforme (GBM) cell apoptosis and cell-cycle arrest. MDM2-p53-IN-16 can be used for the cancer research .
|
-
- HY-149979
-
|
|
Apoptosis
|
Cancer
|
|
SLC7A11-IN-1 is a potent solute carrier family 7 member 11 (SLC7A11, xCT) inhibitor. SLC7A11-IN-1 shows antiproliferative activity. SLC7A11-IN-1 inhibits cell invasion and metastasis. SLC7A11-IN-1 induces Apoptosis and cell cycle arrest at S-phase. SLC7A11-IN-1 shows anti-tumor activity .
|
-
- HY-13265
-
AR-42
2 Publications Verification
HDAC-42; OSU-HDAC42
|
HDAC
Autophagy
Apoptosis
|
Cancer
|
|
AR-42 (HDAC-42; OSU-HDAC42) is a potent, orally bioavailable pan-HDAC inhibitor (IC50=16 nM). AR-42 induces growth inhibition, cell-cycle arrest, apoptosis, and activation of caspases-3/7. AR-42 promotes hyperacetylation of H3, H4, and alpha-tubulin, and up-regulation of p21. AR-42 shows cytotoxicity against various human cancer cell lines .
|
-
- HY-155177
-
|
|
CDK
|
Cancer
|
|
CDK9-IN-27 (Compound 6a) is a CDK9 inhibitor (IC50s: 0.424 μM). CDK9-IN-27 induces apoptosis and cell cycle arrest at S stage. CDK9-IN-27 has cytotoxic action against HepG2, HCT-116 and MCF-7 cell lines, with IC50s of 10.31-40.34 μM. CDK9-IN-27 can be used for cancer research .
|
-
- HY-149633
-
|
|
EGFR
Dihydrofolate reductase (DHFR)
Apoptosis
|
Cancer
|
|
EGFR/HER2/DHFR-IN-3 (compound 4c) is a potent dual inhibitor of EGFR/HER2, with IC50s of 0.138 and 0.092 μM, respectively. EGFR/HER2/DHFR-IN-3 also inhibits DHFR, with an IC50 of 0.193 M. EGFR/HER2/DHFR-IN-3 causes arrest at the S phase of the cell cycle and induces apoptosis in MCF7 breast cancer cells .
|
-
- HY-163692
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
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 .
|
-
- HY-163747
-
|
|
VEGFR
|
Cancer
|
|
VEGFR-2-IN-47 (compound 7g) is a potent VEGFR-2 inhibitor with an IC50 value of 0.072 µM. VEGFR-2-IN-47 can induce G2 / M phase cell cycle arrest, promote apoptosis, and boost immunomodulation by downregulating TNF-α expression and upregulating IL-2 levels in MCF-7 cells. VEGFR-2-IN-47 has the potential to be used for the research of cancer such as breast cancer and liver carcinoma .
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-
- HY-N2071R
-
|
|
Cytochrome P450
Fungal
Apoptosis
Caspase
|
Infection
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Cedrol (Standard) is the analytical standard of Cedrol. This product is intended for research and analytical applications. Cedrol is a potent competitive inhibitor of cytochrome P-450(CYP) enzyme. Cedrol plays an anticancer role by inducing cell cycle arrest and Caspase-dependent apoptosis. Cedrol acts as a neutrophil agonist that can desensitize cells to subsequent stimulation of N-formyl peptides. Cedrol prevents neuropathic pain caused by chronic contractile injury by inhibiting oxidative stress and inflammation. In addition, Cedrol has antibacterial, hair loss prevention and anti-anxiety properties.
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-
- HY-N0202R
-
|
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ERK
Apoptosis
p38 MAPK
Src
Akt
STAT
|
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Atractylenolide II (Standard) is the analytical standard of Atractylenolide II. This product is intended for research and analytical applications. Atractylenolide II (Asterolide) is a sesquiterpenoid compound. Atractylenolide II can induce G1 phase cell cycle arrest and apoptosis in B16 melanoma cells. Atractylenolide II is an orally effective anticancer agent that can exert anti-melanoma effects by inhibiting the STAT3 signaling pathway. In addition, Atractylenolide II has been shown to ameliorate myocardial fibrosis, oxidative stress, and neuroprotective activity .
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-
- HY-18981R
-
|
|
PKC
Apoptosis
CXCR
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Decursin (Standard) is the analytical standard of Decursin. This product is intended for research and analytical applications. Decursin ((+)-Decursin) is a potent anti-tumor agent. Decursin also is a cytotoxic agent and a potent protein kinase C activator. Decursin induces apoptosis and cell cycle arrest at G1 phase. Decursin decreases the expression of CDK2, CDK4, CDK6, cyclin D1 protein at 48 h. Decursin inhibits cell proliferation and migration. Decursin shows anti-tumor, anti-inflammatory and analgesic activities [4].
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-
- HY-169408
-
|
|
Cytochrome P450
EGFR
Apoptosis
|
Cancer
|
|
EGFR-IN-137 (Compound 4c) is an inhibitor for aromatase and EGFR with IC50s of 1.67 μg/mL and 0.08 μg/mL. EGFR-IN-137 inhibits the proliferation of cancer cell MCF-7 and MDA-MB-231 with IC50s of 1.62 µM and 4.14 µM. EGFR-IN-137 arrests the cell cycle at G0/G1 phase in MDA-MB-231, and induces apoptosis through caspase-dependent pathway .
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-
- HY-161501
-
|
|
GLUT
Topoisomerase
Apoptosis
|
Cancer
|
|
3-Fluoro-evodiamine glucose (Compound 8) is an evodiamine-glucose conjugate. 3-Fluoro-evodiamine glucose activates the expression of glucose transporter 1 (GLUT1), and inhibits topoisomerase I/II. 3-Fluoro-evodiamine glucose induces apoptosis and arrests the cell cycle at G2/M phase. 3-Fluoro-evodiamine glucose exhibits antitumor efficacy in vivo and in vitro, without significant toxicity .
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-
- HY-15485
-
|
|
Phosphodiesterase (PDE)
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Zardaverine is an orally active and selective PDE3/4 inhibitor (IC50)=0.58 uM/0.17 uM) with potent bronchodilator activity. Zardaverine also selectively inhibits the proliferation of HCC cells and induces apoptosis and cycle arrest (G0/G1 phase). Zardaverine has good antitumor potential and is effective in both bronchial relaxation and reduction of inflammation in asthma .
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-
- HY-N6714
-
|
|
Topoisomerase
Androgen Receptor
Estrogen Receptor/ERR
Apoptosis
|
Infection
Cancer
|
|
Alternariol is an orally ingested mycotoxin produced by Alternaria, capable of inhibiting the activity of topoisomerase I and II (topoisomerase I, topoisomerase II). Alternariol has weak estrogenic (Estrogen Receptor/ERR) and androgen/antiandrogen (Androgen Receptor) effects. Alternariol can induce apoptosis, trigger cell cycle arrest, suppress innate immune responses, and exhibit anti-tumor activity. Alternariol has genotoxic, mutagenic, and endocrine-disrupting effects .
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-
- HY-115908
-
|
|
CDK
Apoptosis
|
Cancer
|
|
ZDLD13, a β-carboline, is an orally active and selective CDK4/CycD3 inhibitor with an IC50 value of 0.38 μM. ZDLD13 exhibits potent anti-HCT116 activity including inhibition of colony formation, inhibition of invasion and migration, inducing of apoptosis, and arresting of G1 phase in cell cycle. ZDLD13 shows significant tumor growth inhibition in HCT116 tumor xenograft model .
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-
- HY-146491
-
|
|
VEGFR
Raf
Apoptosis
|
Cancer
|
|
VEGFR-2/BRAF-IN-1 (Compound 4b) is a dual VEGFR-2 and BRAF kinases inhibitor with IC50 values of 0.049, 0.063 and 0.005 µM against VEGFR-2, BRAF V600E and BRAF WT, respectively. VEGFR-2/BRAF-IN-1 induces apoptosis and arrests the cell cycle mainly in the G1/S phase .
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-
- HY-151630
-
|
|
Carbonic Anhydrase
|
Cancer
|
|
hCAIX-IN-16 (Compound 12d) is hCA IX inhibitor, with Ki values of 190.0 and 187.9 nM for hCA IX and hCA XII, respectively. hCAIX-IN-16 can arrest the cell cycle of breast cancer MDA-MB-468 in G0-G1 and S phase and induce apoptosis. hCAIX-IN-16 shows good broad-spectrum anticancer activity and can be used for cancer research .
|
-
- HY-124727
-
|
|
JAK
Apoptosis
|
Cancer
|
|
ZT55 is an orally active and highly-selective JAK2 inhibitor with an IC50 value of 0.031 μM. ZT55 inhibits the proliferation of JAK2 V617F-expressing HEL cell lines and induces apoptosis and cycle arrest. ZT-55 also effectively inhibits the growth of HEL xenograft tumours in a mice model. ZT-55 can be used in studies of myeloproliferative neoplasms, polycythemia vera and primary thrombocythemia .
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-
- HY-118529
-
|
|
Phosphatase
|
Cancer
|
|
JUN-1111 is an irreversible and selective Cdc25 phosphatase inhibitor with IC50 values of 0.38, 1.8, 0.66, 28, 37 µM for Cdc25A, Cdc25B, Cdc25C, VHR, PTP1B, respectively. JUN-1111 induces cell cycle arrest at G1 and G2/M phases. JUN-1111 decreases the expression of phosphoCdk1 .
|
-
- HY-146817
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulin polymerization-IN-11 is a potent tubulin polymerization inhibitor with an IC50 value of 3.4 µM. Tubulin polymerization-IN-11 shows antiproliferative activity. Tubulin polymerization-IN-11 induces Apoptosis and cell cycle arrest at G2/M phase. Tubulin polymerization-IN-11 decreases the expression of cyclin B1, p-cdc2, and Bcl-2 protein levels and increases the expression of cleaved PARP .
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-
- HY-128912
-
|
|
Histone Demethylase
|
Cancer
|
|
Arborinine is a potent and orally activeLSD1 inhibitor. Arborinine increases the expression of H3K4me1/2, H3K9me1/2, E-cad protein and decreases the expression of UBE2O protein level. Arborinine induces cell cycle arrest at S phase. Arborinine shows antitumor activity .
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-
- HY-157913
-
|
|
Pyruvate Kinase
Apoptosis
|
Cancer
|
|
PKM2-IN-6 (compound 7d) is a potent and orally active PKM2 inhibitor with an IC50 value of 23 nM. PKM2-IN-6 induces apoptosis and cell cycle arrest at G2 phase. PKM2-IN-6 reduces the level of PKM1 and PKM2 at the mRNA level. PKM2-IN-6 shows anticancer activity and has the potential for the research of triple-negative breast cancer .
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-
- HY-107592
-
|
|
IKK
STAT
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
ACHP (compound 4j) is a selective and orally active IκB kinase inhibitor with IC50 values of 8.5 nM and 250 nM for IKKβ and IKKα, respectively. ACHP can effectively inhibit the STAT3 signaling pathway and induce cancer cell cycle arrest and apoptosis. ACHP shows anti-inflammatory activity in a mouse ear edema model. ACHP can be used in anti-inflammatory and anti-cancer (such as multiple myeloma and leukemia) studies .
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-
- HY-120667
-
|
|
MDM-2/p53
Apoptosis
|
Cancer
|
|
DS-5272 is an orally acitve inhibitor for p53-MDM2 with an IC50 of 20 nM. DS-5272 inhibits the proliferation of SJSA-1 (wildtype p53, IC50=0.17 μM) and DLD-1 (mutant p53). DS-5272 arrest the cell cycle, and induces apoptosis in SJSA-1. DS-5272 exhibits antitumor efficacy in mice .
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-
- HY-159149
-
|
|
Reactive Oxygen Species
Apoptosis
|
Cancer
|
|
Antitumor agent-182 (Compound 12a) decreases mitochondrial membrane potential (MMP) and enhances ROS levels. Antitumor agent-182 arrests the cell cycle at G0/G1 phase, induces apoptosis in HeLa. Antitumor agent-182 inhibits the proliferation of HeLa, PC-3 and HCT-15 with IC50s of 8.83, 10.07 and 7.84 μM, respectively .
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-
- HY-163894
-
|
|
Apoptosis
HDAC
|
Cancer
|
|
HDAC6-IN-48 (compound 5i) is a potent and selective HDAC6 inhibitor with IC50 values of 5.16, 396.72, 638.08 nM for HDAC6, HDAC3, HDAC1, respectively. HDAC6-IN-48 induces apoptosis and cell cycle arrest at G0/G1 phase. HDAC6-IN-48 increases the protein expression of acetylated α-tubulin .
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-
- HY-123486
-
|
|
Apoptosis
Bcr-Abl
|
Cancer
|
|
HS-438 is a potent and selective BCR-ABL inhibitor. HS-438 shows antiproliferative activity. HS-438 decreases the expression of phosphorylation of BCR-ABL (Tyr177). HS-438 induces apoptosis and cell cycle arrest at G0/G1 phase. HS-438 shows antitumor activity. HS-438 has the potential for the research of chronic myeloid leukemia (CML) .
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-
- HY-W013053R
-
|
|
DNA/RNA Synthesis
Apoptosis
MDM-2/p53
|
Cancer
|
|
Dibenz[a,h]anthracene (Standard) is the analytical standard of Dibenz[a,h]anthracene. This product is intended for research and analytical applications. Dibenz[a,h]anthracene (DBA) is a polycyclic aromatic hydrocarbon (PAH) of considerable tumorigenicity. Dibenz[a,h]anthracene results in DNA adduct formation leading to the activation of a DNA damage response. Dibenz[a,h]anthracene induces cell cycle arrest and apoptosis via both Tp53-dependent and Tp53-independent mechanisms .
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-
![Dibenz[a,h]anthracene (Standard)](//file.medchemexpress.eu/product_pic/hy-w013053r.gif)
- HY-168205
-
|
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HSP
Apoptosis
|
Cancer
|
|
HSP90-IN-33 (compound 24e) is a potent Hsp90 inhibitor with Kd values of ≥200, 7.3 µM for Hsp90α, Hsp90β, respectively. HSP90-IN-33 induces apoptosis and cell cycle arrest at G0/G1 phase. HSP90-IN-33 decreases the protein expression of ERα, CDK4 and Akt .
|
-
- HY-168655
-
|
|
Apoptosis
EGFR
VEGFR
|
Cancer
|
|
EGFR/VEGFR2-IN-3 (compound 9) is a potent EGFR and VEGFR-2 inhibitor with IC50 values of 0.129, 0.142, 3.428 µM for EGFR, VEGFR-2, COX-2, respectively. EGFR/VEGFR2-IN-3 shows cytotoxicity. EGFR/VEGFR2-IN-3 induces apoptosis and cell cycle arrest at G2/M phase .
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-
- 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 .
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-
- HY-159175
-
|
|
PROTACs
Deubiquitinase
Apoptosis
MDM-2/p53
|
Cancer
|
|
XM-U-14 is a selective PROTAC USP7 Degrader (DC50: 0.74 nM in inducing USP7 degradation in RS4;11 cell line). XM-U-14 upregulates the levels of p53 and p21. XM-U-14 also significantly inhibits acute lymphoblastic leukemia (ALL) cell growth (IC50: 0.5 nM and 8.3 nM for RS4;11 cells and Reh cells respectively). XM-U-14 induces apoptosis and cycle arrest. XM-U-14 inhibits tumor growth. (Blue: VHL ligand (HY-159465), Black: linker (HY-W539783); Pink: USP7 inhibitor (HY-159464)) .
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-
- HY-163661
-
|
|
Apoptosis
Autophagy
MDM-2/p53
|
Cancer
|
|
p53-MDM2-IN-5 (compound 5a) is a potent p53-MDM2 inhibitor. p53-MDM2-IN-5 induces apoptosis, autophagy and DNA damage. p53-MDM2-IN-5 induces cell cycle arrest at S and G2/M phases. p53-MDM2-IN-5 shows anti-tumor activity .
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-
- HY-168565
-
|
|
Apoptosis
Microtubule/Tubulin
Reactive Oxygen Species
|
Cancer
|
|
Tubulin polymerization-IN-70 (compound Q19) is a potent tubulin polymerization inhibitor. Tubulin polymerization-IN-70 shows antiproliferative activity. Tubulin polymerization-IN-70 target the colchicine binding site of tubulin and inhibited tubulin polymerization. Tubulin polymerization-IN-70 induces apoptosis and cell cycle arrest at G2/M phase. Tubulin polymerization-IN-70 induces mitochondrial membrane potential decrease and increases the levels of reactive oxygen species (ROS). Tubulin polymerization-IN-70 shows antiangiogenic and anticancer activity .
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-
- HY-155523
-
|
|
Microtubule/Tubulin
HDAC
Apoptosis
|
Cancer
|
|
Tubulin/HDAC-IN-2 (Compound II-19k) is a dual inhibitor of Tubulin and HDAC, with an IC50 of 0.403 μM, 0.591μM, 3.552μM, 0.459μM for HDAC1/2/3/6. Tubulin/HDAC-IN-2 blocks cell cycle arrest at G2 phase, induces cell apoptosis. Tubulin/HDAC-IN-2 inhibits the growth of hematoma and solid tumor cells, reduces tumor metastasis, and also inhibits tumor growth in a liver tumor allograft mouse model .
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-
- 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 .
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-
- HY-168102
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Antiproliferative agent-59 (Compound 14u) is an inhibitor for tubulin polymerization. Antiproliferative agent-59 exhibits antiproliferative activities against cancer cells Huh7, SGC-7901, and MCF-7 with IC50 of 0.03, 0.18, and 0.13μM. Antiproliferative agent-59 arrests the cell cycle at G2/M phase and induces apoptosis in Huh7 cell. Antiproliferative agent-59 exhibits antitumor efficacy against liver cancer in Huh7 xenograft mouse models, without significant toxicity .
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-
- HY-149522
-
|
|
Bcl-2 Family
Apoptosis
|
Cancer
|
|
BCL6-IN-10 (Compound WK499) is a BCL6 inhibitor. BCL6-IN-10 interrupts the binding of BCL6 to SMRT protein. BCL6-IN-10 induces cell apoptosis, cell cycle arrest and DNA damage. BCL6-IN-10 inhibits AML cell proliferation (IC50s: 0.91, 1.63, 1.026, 7.42, 0.87, 0.85μM for OCl-AML3, THP1, MOLM13, HL60, KG1, NB4 cell respectively) .
|
-
- HY-164374
-
|
|
PAK
|
Cancer
|
|
AK963/40708899 is a potent PAK1 inhibitor. AK963/40708899 suppresses the proliferation of human gastric cancer cells by downregulation of PAK1-NF-κB-cyclinB1 pathway. AK963/40708899 induces cell cycle arrest at G2 phase and reduces the migration and invasion. AK963/40708899 inhibits the formation of filopodia and promots cell adhesion which in turn inhibits invasive potential of gastric cells by negatively regulating PAK1-LIMKl-cofilin and PAK1-ERK-FAK pathways .
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-
- HY-101029A
-
|
|
NEKs
Ribosomal S6 Kinase (RSK)
DYRK
Apoptosis
|
Cancer
|
|
MBM-55S is a potent NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 1 nM. MBM-55S shows a 20-fold or greater selectivity in most kinases with the exception of RSK1 (IC50=5.4 nM) and DYRK1a (IC50=6.5 nM). MBM-55S effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis. MBM-55S shows antitumor activities, and no obvious toxicity to mice .
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-
- HY-131906
-
|
|
JAK
FLT3
Apoptosis
|
Cancer
|
|
JAK2-IN-7 is a selective JAK2 inhibitor with IC50s of 3, 11.7, and 41 nM for JAK2, SET-2, and Ba/F3 V617F cells, respectively. JAK2-IN-7 possesses >14-fold selectivity over JAK1, JAK3, FLT3. JAK2-IN-7 stimulates cell cycle arrest in the G0/G1 phase and induces tumor cellapoptosis. Antitumor activities .
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-
- HY-N6588
-
|
3,4,5-triCQA
|
Akt
NF-κB
|
Inflammation/Immunology
Cancer
|
|
3,4,5-Tricaffeoylquinic acid (3,4,5-triCQA) inhibits tumor necrosis factor-α-stimulated production of inflammatory mediators in keratinocytes via suppression of Akt- and NF-κB-pathways. 3,4,5-Tricaffeoylquinic acid induces cell cycle arrest at G0/G1, actin cytoskeleton organization, chromatin remodeling, neuronal differentiation, and bone morphogenetic protein signaling in human neural stem cells. 3,4,5-Tricaffeoylquinic acid has the potential for the research of aging-associated diseases .
|
-
- HY-124500
-
|
|
STAT
Apoptosis
|
Cancer
|
|
AC-4-130 is a potent STAT5 SH2 domain inhibitor. AC-4-130 directly binds to STAT5 and disrupts STAT5 activation, dimerization, nuclear translocation, and STAT5-dependent gene transcription. AC-4-130 induces cell cycle arrest and apoptosis in FLT3-ITD-driven leukemic cells. AC-4-130 has anti-cancer activity and can efficiently block pathological levels of STAT5 activity in acute myeloid leukemia (AML) .
|
-
- HY-146751
-
|
|
PI3K
Akt
mTOR
Apoptosis
|
Cancer
|
|
PI3K/Akt/mTOR-IN-2 is a PI3K/AKT/mTOR pathway inhibitor. PI3K/Akt/mTOR-IN-2 possess anti-cancer effects and selectivity against MDA-MB-231 cells with IC50 value of 2.29 μM. PI3K/Akt/mTOR-IN-2 can induce cancer cell cycle arrest and apoptosis .
|
-
- HY-155226
-
|
|
FLT3
Apoptosis
|
Cancer
|
|
FLT3-IN-21 (compound LC-3) is a potent FLT3 inhibitor (IC50: 8.4 nM) and induces apoptosis. FLT3-IN-21 can arrest the cell cycle in the G1 phase and inhibit the proliferation of FLT3-ITD-positive AML cells MV-4-11 (IC50: 5.3 nM). In mice, FLT3-IN-21 (10 mg/kg/d) inhibited tumor growth in the MV-4-11 xenograft model (TGI=92.16%) .
|
-
- HY-149636
-
|
|
EGFR
CDK
VEGFR
|
Cancer
|
|
Multi-target kinase inhibitor 2 (compound 5K) is a multi-targeted kinase inhibitor, and exhibits activity against EGFR, Her2, VEGFR2, and CDK2 enzymes, with IC50 values ranging from 40 to 204 nM. Multi-target kinase inhibitor 2 shows cytotoxic effects were observed against HepG2, HeLa , MDA-MB-231 and MCF-7, with IC50 of 41, 57, 51 and 59 μM. Multi-target kinase inhibitor 2 induces cell cycle arrest and apoptosis in HepG2 cells.
|
-
- HY-163786
-
|
|
PROTACs
CDK
Apoptosis
|
Cancer
|
|
PROTAC CDK4/6 degrader 1 (Compound 7f) is a dual degrader for CDK4 and CDK6 with DC50 of 10.5 and 2.5 nM. PROTAC CDK4/6 degrader 1 inhibits the proliferation of cell Jurkat (IC50 is 0.18 μM), arrests the cell cycle at G1 phase and induces apoptosis. (Pink: ligand for target protein YY173 (HY-163787); Black: linker (HY-163788); Blue: ligand for E3 ligase (HY-10984))
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-
- HY-120561
-
|
|
Trk Receptor
IRAK
Pim
Apoptosis
|
Cancer
|
|
PC-046 is a multi-target inhibitor for tyrosine receptor kinase B (TrkB), IRAK-4 and Pim-1, with IC50 of 13.4 μM, 15.4 μM and 19.1 μM, respectively. PC-046 exhibits cytotoxicity against pancreatic cancer cell BxPC3 with IC50 of 7.5-130 nM. PC-046 induces apoptosis and arrests cell cycle at G2/M phase in BxPC3. PC-046 exhibits antitumor efficacy and exhibits good pharmacokinetic characteristics in mice .
|
-
- HY-W131302
-
|
N,N-Ethylenediglycine
|
Others
|
Cancer
|
|
Ethylenediaminediacetic acid (N,N-Ethylenediglycine) is an important ligand that enhances the antiproliferative activity of metal complexes. The complexes formed by ethylenediacetic acid and metal ions exhibited significant antiproliferative properties in MCF-7 cancer cell line. The metal complexes of ethylenediacetic acid were able to interact with DNA and were studied by CD and EPR spectroscopy techniques. Ethylenediaminediacetic acid and its metal complexes were able to induce cell cycle arrest at the G(0)/G(1) phase. The crystal structure analysis of ethylenediacetic acid provided important structural information for understanding its biological activity .
|
-
- HY-N7844S
-
|
Benzyladenosine-d5
|
Isotope-Labeled Compounds
Apoptosis
Adenosine Receptor
|
Inflammation/Immunology
Cancer
|
|
N6-Benzyladenosine-d5 (Benzyladenosine-d5) is deuterium labeled N6-Benzyladenosine. N6-Benzyladenosine is an adenosine receptor agonist, has a cytoactive activity. N6-Benzyladenosine arrests cell cycle at G0/G1 phase and induces cell apoptosis. N6-Benzyladenosine also exerts inhibitory effect on T. gondii adenosine kinase and glioma .
|
-
- HY-N3387
-
|
|
Apoptosis
NF-κB
Akt
MMP
|
Inflammation/Immunology
Cancer
|
|
Licoricidin (LCD) is isolated from Glycyrrhiza uralensis Fisch, possesses anti-cancer activities. Licoricidin (LCD) inhibit SW480 cells (IC50=7.2 μM) by inducing cycle arrest, apoptosis and autophagy, and is a potential chemopreventive or chemotherapeutic agent against colorectal cancer . Licoricidin (LCD) inhibits Lung Metastasis by inhibition of tumor angiogenesis and lymphangiogenesis as well as changes in the local microenvironment of tumor tissues the anticarcinogenic effect . Licoricidin enhanced gemcitabine-induced cytotoxicity in Osteosarcoma (OS) cells by inactivation of the Akt and NF-κB pathways in vitro and in vivo . Licoricidin blocks UVA-induced photoaging via ROS scavenging, limits the activity of MMP-1, it can be considered as an active ingredient in new topically applied anti-ageing formulations .
|
-
- HY-16350
-
|
NKP-1339; IT-139; KP-1339
|
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
BOLD-100 (NKP-1339; IT-139) is the first-in-class ruthenium-based anticancer agent in development against solid cancer with limited side effects. BOLD-100 induces G2/M cell cycle arrest, blockage of DNA synthesis, and induction of apoptosis via the mitochondrial pathway. BOLD-100 has a high tumor targeting potential, strongly binds to serum proteins such as albumin and transferrin and activates in the reductive tumor milieu .
|
-
- HY-N0711
-
|
Cymophenol
|
Notch
Apoptosis
Fungal
Endogenous Metabolite
Bacterial
|
Infection
Inflammation/Immunology
Cancer
|
|
Carvacrol is an orally active monoterpenic phenol that can be extract from an abundant number of aromatic plants, including thyme and oregano, possessing antioxidant, antibacterial, antifungal, anticancer, anti-inflammatory, hepatoprotective, spasmolytic, and vasorelaxant properties. Carvacrol also causes cell cycle arrest in G0/G1, downregulates Notch-1, and Jagged-1, and induces apoptosis. Carvacrol is used in low concentrations as a food flavoring ingredient and preservative, as well as a fragrance ingredient in cosmetic formulations .
|
-
- HY-144777
-
|
|
FLT3
Apoptosis
|
Cancer
|
|
FLT3-IN-14 is a potent FLT3 inhibitor with IC50s of 5.6 nM and 1.4 nM for FLT3-WT and FLT3-ITD. FLT3-IN-14 reduces the phosphorylation of FLT3 (Y591), induces cell cycle arrest at G1 phase and apoptosis. FLT3-IN-14 significantly reduces the tumor growth in an MV4-11 xenograft mouse model .
|
-
- HY-147914
-
|
|
Apoptosis
|
Cancer
|
|
NSD2-IN-1 (compound 38) is a potent and high selective NSD2-PWWP1 (nuclear receptor-binding SET domain 2-PWWP1) inhibitor, with an IC50 of 0.11 μM. NSD2-IN-1 can bind to NSD2-PWWP1 and then affect the expression of genes regulated by NSD2. NSD2-IN-1 induces apoptosis and cell cycle arrest .
|
-
- HY-151984
-
|
|
CDK
|
Cancer
|
|
CDK9-IN-22 is a potent CDK9 inhibitor with IC50s of 10.4, 876.2 nM for CDK9, CDK, respectively. CDK9-IN-22 induces apoptosis and cell cycle arrests at G2/M phase. CDK9-IN-22 decreases the expression of p-RNAPII (S2) and CDK9 protein. CDK9-IN-22 shows antiproliferative and aiti-tumor activity .
|
-
- HY-P99284
-
|
MK-0646; h7C10
|
IGF-1R
Apoptosis
|
Cancer
|
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Dalotuzumab (MK-0646) is a recombinant humanized monoclonal antibody (IgG1 type) targeting IGF-1R. Dalotuzumab acts by inhibiting IGF-1- and IGF-2-mediated tumor cell proliferation, IGF-1R autophosphorylation, and Akt phosphorylation. Dalotuzumab also induces apoptosis and cycle arrest. Dalotuzumab in combination with other anticancer agents such as statins can enhance the antitumor activity of Dalotuzumab in vitro and in vivo .
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-
- HY-153202
-
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MDM-2/p53
Apoptosis
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Cancer
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SLMP53-2 is a mutant p53 reactivator. SLMP53-2 restores wild-type-like conformation and DNA-binding ability of mutp53-Y220C by enhancing its interaction with the Hsp70, leading to the reestablishment of p53 transcriptional activity. SLMP53-2 can induce cell cycle arrest, apoptosis and endoplasmic reticulum (ER) stress. SLMP53-2 exhibits antitumor activity .
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-
- HY-P5910
-
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MDM-2/p53
Apoptosis
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Cancer
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Azurin p28 peptide is a tumor-penetrated antitumor peptide. Azurin p28 peptide redues proteasomal degradation of p53 through formation of a p28: p53 complex. Azurin p28 peptide induces apoptosis or cell cycle arrest. Azurin p28 peptide inhibits p53-positive tumor growths. Azurin p28 peptide shows antiangiogenic effect by inhibiting phosphorylation of VEGFR-2, FAK and Akt .
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-
- HY-13559
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Azaspirane
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Apoptosis
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Cancer
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Atiprimod (Azaspirane) is an orally bioavailable small molecule with antitumor, anti-inflammatory, and anti-angiogenic activities. Atiprimod blocks the signaling pathways of interleukin-6 and vascular endothelial growth factor (VEGF) by inhibiting the phosphorylation of signal transducer and activator of transcription 3 (STAT3). Atiprimod also downregulates the anti-apoptotic proteins Bcl-2, Bcl-XL, and Mcl-1, thereby inhibiting cell proliferation, inducing cell cycle arrest, and inducing apoptosis. Atiprimod triggers persistent ER stress-mediated apoptosis in breast cancer cells by activating the PERK/eIF2α/ATF4/CHOP axis and inhibiting the nuclear translocation of STAT3/NF-κB transcription factors .
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-
- HY-147682
-
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NF-κB
Apoptosis
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Cancer
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NF-κB-IN-5 (compound 4d) is an orally active and potent NF-κB inhibitor by interacting directly with NF-κB. NF-κB-IN-5 shows antitumor activity against human cancer cell lines (HCT116, U87-MG, HepG2, BGC823, PC9), with IC50 values of 5.35, 2.81, 2.83, 2.02 and 3.90 μM, respectively. NF-κB-IN-5 induces apoptosis in U87-MG tumor cell and cell cycle arrest in G0/G1 phase .
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- HY-155073
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Microtubule/Tubulin
Apoptosis
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Cancer
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Tubulin inhibitor 35 (compound 6b) is a dual inhibitor of topoisomerase I (IC50=~50 μM) and tubulin polymerization (IC50=5.69 μM). Tubulin inhibitor 35 inhibits migration and invasion of MGC-803 and RKO cell lines，and induces apoptosis via arresting cell cycle at G2/M phase. Tubulin inhibitor 35 exhibis potent efficacy in gastrointestinal tumor inhibiton (inhibits MGC-803 (IC50=0.09 μM) and RKO (IC50=0.2 μM) cell lines) .
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- HY-161934
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PARP
Reactive Oxygen Species
Apoptosis
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Cancer
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PARP1-IN-27 (Compound 9B) is the inhibitor for PARP1 and PARP2, with IC50 of 2.53 nM and 6.45 nM in cell SUM149PT. PARP1-IN-27 inhibits the proliferation of BRCA-mutated cancer cells SUM149PT, HCC1937 and Capan-1, with IC50 of 0.62, 1.91 and 4.26 μM respectively. PARP1-IN-27 aggravates DNA double-strand breaks, increases ROS generation, arrests cell cycle at G2/M phase, and induces apoptosis in SUM149PT .
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-
- HY-169096
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Microtubule/Tubulin
Apoptosis
|
Cancer
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DPP-21 is an inhibitor of tubulin polymerization (IC50: 2.4 μM). DPP-21 shows anti-proliferative activity against cancer cell lines, with IC50s of 0.38 nM (HCT116), 11.69 nM (B16), 5.37 nM (HeLa), 9.53 nM (MCF7), 8.94 nM (H23) and 9.37 nM (HepG2) respectively. DPP-21 arrests the cell cycle in the G2/M phase of mitosis, subsequently inducing tumor cell apoptosis (decreases Bcl-2 but upregulates the pro-apoptotic protein Bax) .
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-
- HY-159966
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Topoisomerase
HDAC
Reactive Oxygen Species
Apoptosis
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Cancer
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Top/HDAC-IN-3 (Compound 31) is an orally active dual inhibitor of Topoisomerase and HDAC. Top/HDAC-IN-3 increases reactive oxygen species (ROS) levels, leading to DNA damage, thereby inhibiting cancer cell colony formation and migration, inducing cancer cell Apoptosis, and causing cell cycle arrest. In the NSCLC model, Top/HDAC-IN-3 exhibited significant antitumor effects, with a tumor growth inhibition (TGI) of 77.5% at 100 mg/kg, surpassing the efficacy of the HDAC inhibitor SAHA (HY-10221) and the combination of SAHA (HY-10221) with the topoisomerase inhibitor Irinotecan (HY-16562) .
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- HY-155816
-
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PROTACs
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Cancer
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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.
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-
- HY-169006
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Apoptosis
PKC
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Cancer
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Evo312 is a dose-dependent inhibitor of protein kinase CβⅠ (PKCβⅠ) (IC50 is 117.34 nM). Evo312 induces PANC-GR (acquired gemcitabine-resistant PC cells) cell cycle arrest and apoptosis by inhibiting PKCβ1 protein expression. Evo312 has antiproliferative effects in pancreatic cancer cells PANC-1 and PANC-GR cells with IC50 of 0.08 μM and 0.07 μM, and in human normal pancreatic ductal epithelial cells HPDE6-c7 with IC50 of 2.95 μM. Evo312 exhibits antitumor activity in a PANC-GR cell transplantation mouse model .
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-
- HY-134061
-
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Apoptosis
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Cancer
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Arecaidine propargyl ester hydrobromide is an agonist of M2 muscarinic acetylcholine receptors and has the activity of inhibiting tumor cell proliferation. The application of arecaidine propargyl ester hydrobromide has shown that it can reduce the number of ovarian cancer cells in vitro and induce apoptosis and the production of reactive oxygen species (ROS) at specific concentrations. Arecaidine propargyl ester hydrobromide can also arrest cells at the G2/M phase of the cell cycle and increase the percentage of abnormal mitosis. Arecaidine propargyl ester hydrobromide is more sensitizing to ovarian surface epithelial cells with higher M2 receptor levels than to cancer cells. Arecaidine propargyl ester hydrobromide exhibits the effect of lowering arterial blood pressure when interacting with the cardiovascular system in a natural physiological state, indicating its potential pharmacological application .
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- HY-15815
-
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Epigenetic Reader Domain
Apoptosis
CDK
HIV
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Cancer
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Bromosporine is a potent BET inhibitor with an IC50 value of 2.1 μM for PCAF. Bromosporine can arrest cell cycle and induce apoptosis in cancer cells. Bromosporine exhibits excellent antitumor activity in xenograft mice model when combined with 5-FU (HY-90006). Bromosporine can increase CDK9 T-loop phosphorylation in HIV-1 latency models, resulting the protection of reactivate HIV-1 replication from latency. Bromosporine can be used to research colorectal cancer, acute myeloid leukemia (AML) and AIDS .
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-
- HY-155982
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STAT
|
Cancer
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STAT3-IN-20 (Compound 40) is a selective STAT3 inhibitor (IC50: 0.65 μM). STAT3-IN-20 binds the SH2 domain to inhibit STAT3 phosphorylation, translocation, and downstream gene transcription. STAT3-IN-20 exhibits antiproliferative activities against STAT3-overactivated DU145 and MDA-MB-231 cancer cells (IC50: 2.97 μM and 3.26 μM respectively). STAT3-IN-20 induces cell cycle arrest and apoptosis .
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-
- HY-158138
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PARP
Topoisomerase
Apoptosis
|
Cancer
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|
TOPOI/PARP-1-IN-1 (Compound B6) is an orally active, low cytotoxic TOPOI/PARP dual inhibitor with an IC50 value of 0.09 μM for PARP1. TOPOI/PARP-1-IN-1 can effectively inhibit the proliferation and migration of cancer cells. TOPOI/PARP-1-IN-1 also causes cell cycle arrest in the G0/G1 phase and induces apoptosis. The tumor growth inhibition rate (TGI) of TOPOI/PARP-1-IN-1 in mice is 75.4% .
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-
- HY-123237
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c-Met/HGFR
FLT3
Trk Receptor
Apoptosis
Autophagy
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Cancer
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KRC-108, an aminopyridine, is an orally active multiple kinase inhibitor with IC50s of 80 nM, 23 nM, 3 nM, 70 nM, 30 nM, 39 nM for c-Met, c-Met M1250T, c-Met Y1230D, Ron, Flt3 and TrkA, respectively. KRC-108 induces cell cycle arrest, apoptotic cell death, and autophagy. KRC-108 exhibits anti-tumor activity in vivo in HT29 colorectal cancer, NCI-H441 lung cancer xenograft models in athymic BALB/c nu/nu mice .
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- HY-N4327
-
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NF-κB
Apoptosis
Akt
Bcl-2 Family
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Infection
Inflammation/Immunology
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Eurycomalactone is an active quassinoid could be isolated from Eurycoma longifolia Jack. Eurycomalactone is a potent NF-κB inhibitor with an IC50 value of 0.5 μM. Eurycomalactone inhibits protein synthesis and depletes cyclin D1. Eurycomalactone enhances radiosensitivity through arrest cell cycle at G2/M phase and delayed DNA double-strand break repair. Eurycomalactone inhibits the activation of AKT/NF-κB signaling, induces apoptosis and enhances chemosensitivity to Cisplatin (HY-17394) .
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- HY-13260A
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Akt
Autophagy
Apoptosis
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Cancer
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CCT128930 hydrochloride is a potent and selective inhibitor of AKT (IC50=6 nM). CCT128930 hydrochloride has 28-fold selectivity over the closely related PKA kinase (IC50=168 nM) through the targeting of Met282 of AKT (Met173 of PKA-AKT chimera), as well as 20-fold selectivity over p70S6K (IC50=120 nM). CCT128930 hydrochloride induces cell cycle arrest, DNA damage, and autophagy. Antitumor activity .
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-
- HY-150688
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JNK
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Cancer
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JAK3-IN-13 (compound 12n) is a potent, selective and orally active JAK3 inhibitor with IC50 values of 4728, 2039, 8, 365 nM for NK1, JNK2, JNK3, Tyk2, respectively. JAK3-IN-13 shows antiproliferative activity. JAK3-IN-13 induces cell cycle arrest at G0/G1 phase. JAK3-IN-13 shows antitumor activity .
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-
- HY-151443
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HDAC
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Cancer
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HDAC-IN-47 is an orally active inhibitor of histone deacetylase (HDAC), with IC50s of 19.75 nM (HDAC1), 5.63 nM (HDAC2), 40.27 nM (HDAC3), 57.8 nM (HDAC2), 302.73 nM (HDAC8), respectively. HDAC-IN-47 inhibits autophagy and induces apoptosis via the Bax/Bcl-2 and caspase-3 pathways. HDAC-IN-47 arrests cell cycle at G2/M phase, and shows anti-tumor efficacy in vivo .
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- HY-161302
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Apoptosis
DNA/RNA Synthesis
PARP
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Cancer
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Polθ/PARP-IN-1 (compound 25d) is a potent dual DNA polymerase theta (Polθ) and PARP inhibitor with IC50 values of 45.6, 5.4 nM, respectively. Polθ/PARP-IN-1 shows antiproliferative activity. Polθ/PARP-IN-1 induces apoptosis and cell cycle arrest at G2/M phase, causes DNA damage. Polθ/PARP-IN-1 shows anti-tumor activity .
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- HY-P5910A
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MDM-2/p53
Apoptosis
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Cancer
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Azurin p28 peptide TFA is a tumor-penetrated antitumor peptide. Azurin p28 peptide TFA redues proteasomal degradation of p53 through formation of a p28: p53 complex. Azurin p28 peptide TFA induces apoptosis or cell cycle arrest. Azurin p28 peptide TFA inhibits p53-positive tumor growths. Azurin p28 peptide TFA shows antiangiogenic effect by inhibiting phosphorylation of VEGFR-2, FAK and Akt .
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- HY-W653896
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Isotope-Labeled Compounds
Androgen Receptor
Apoptosis
Topoisomerase
Estrogen Receptor/ERR
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Infection
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Alternariol-d2 is deuterium labeled Alternariol. Alternariol is an orally ingested mycotoxin produced by Alternaria, capable of inhibiting the activity of topoisomerase I and II (topoisomerase I, topoisomerase II). Alternariol has weak estrogenic (Estrogen Receptor/ERR) and androgen/antiandrogen (Androgen Receptor) effects. Alternariol can induce apoptosis, trigger cell cycle arrest, suppress innate immune responses, and exhibit anti-tumor activity. Alternariol has genotoxic, mutagenic, and endocrine-disrupting effects .
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- HY-N6714R
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Topoisomerase
Androgen Receptor
Estrogen Receptor/ERR
Apoptosis
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Infection
Cancer
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Alternariol (Standard) is the analytical standard of Alternariol. This product is intended for research and analytical applications. Alternariol is an orally ingested mycotoxin produced by Alternaria, capable of inhibiting the activity of topoisomerase I and II (topoisomerase I, topoisomerase II). Alternariol has weak estrogenic (Estrogen Receptor/ERR) and androgen/antiandrogen (Androgen Receptor) effects. Alternariol can induce apoptosis, trigger cell cycle arrest, suppress innate immune responses, and exhibit anti-tumor activity. Alternariol has genotoxic, mutagenic, and endocrine-disrupting effects .
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- HY-144792
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Bcl-2 Family
MDM-2/p53
Caspase
Apoptosis
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Cancer
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|
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 .
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-
- HY-144791
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Bcl-2 Family
MDM-2/p53
Caspase
Apoptosis
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Cancer
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|
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 .
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-
- HY-162319
-
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Apoptosis
HDAC
Microtubule/Tubulin
Reactive Oxygen Species
|
Cancer
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|
Tubulin/HDAC-IN-4 (compound 9n) is a dual Tubulin and HDAC inhibitor with IC50 values of 0.73, 0.43, 0.62, 2.34 µM for HDAC1, HDAC2, HDAC6, HDAC7, respectively. Tubulin/HDAC-IN-4 inhibits the tubulin polymerization by targeting the colchicine binding site. Tubulin/HDAC-IN-4 induces apoptosis and cell cycle arrest at G2/M phase. Tubulin/HDAC-IN-4 induces a significant elevation of intracellular ROS levels. Tubulin/HDAC-IN-4 shows anti-angiogenesis activity and anticancer activity .
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-
- HY-12678S1
-
|
NMS-E628-d8; RXDX-101-d8
|
Isotope-Labeled Compounds
Autophagy
Anaplastic lymphoma kinase (ALK)
Trk Receptor
ROS Kinase
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Cancer
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Entrectinib-d8 (NMS-E628-d8; RXDX-101-d8) is a deuterated version of Entrectinib (HY-12678). Entrectinib (NMS-E628) is an orally available, blood-brain barrier permeable, central nervous system active TrkA/B/C, ROS1 and ALK inhibitor with IC50 values of 1, 3, 5, 12 and 12, respectively. 7 nM. Entrectinib induces apoptosis and cycle arrest in cancer cells, has anti-tumor activity, and also alleviates bleomycin-induced pulmonary fibrosis in mice .
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-
- HY-13224A
-
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Endogenous Metabolite
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Cancer
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AZD4877 hydrochloride is a synthetic dynein inhibitor with potential anti-tumor activity. AZD4877 selectively inhibits the microtubule dynein KSP (also known as kinesin-5 or Eg5), which may lead to inhibition of mitotic spindle assembly. The action of AZD4877 may activate the spindle assembly checkpoint, leading to cell cycle arrest at the mitotic stage. AZD4877 may induce cell death in actively dividing tumor cells. AZD4877 may be less likely to cause peripheral neuropathy associated with microtubule-targeted compounds as it is not involved in post-mitotic processes. AZD4877 is essential for the formation of bipolar spindles and the proper segregation of sister chromosomes .
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-
- HY-168739
-
|
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Topoisomerase
Reactive Oxygen Species
Apoptosis
Survivin
Bcl-2 Family
IAP
DNA/RNA Synthesis
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Cancer
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Topoisomerase I inhibitor 17 (Compound 7h) is a Topoisomerase I (Top1) inhibitor. Topoisomerase I inhibitor 17 reduces DDX5 and reverses the locking of Top1 activity by DDX5. Topoisomerase I inhibitor 17 induces Top1-mediated DNA damage and promotes reactive oxygen species (ROS) production. Topoisomerase I inhibitor 17 induces Apoptosis (reduces antiapoptotic proteins XIAP, Bcl-2, Survivin and up-regulates pro-apoptotic proteins Bax, γH2AX). Topoisomerase I inhibitor 17 also blocks the progression of the G2/M checkpoint and induces cell cycle arrest. Topoisomerase I inhibitor 17 significantly inhibits colony formation and cell migration in colorectal cancer cells. Topoisomerase I inhibitor 17 effectively reduces tumors in human PDX tumor mice .
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-
- HY-126251
-
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CDK
Apoptosis
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Cancer
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CDK9-IN-7 (compound 21e) is a selective, highly potent, and orally active CDK9/cyclin T inhibitor (IC50=11 nM), which exhibits more potent over other CDKs (CDK4/cyclinD=148 nM; CDK6/cyclinD=145 nM). CDK9-IN-7 shows antitumor activity without obvious toxicity. CDK9-IN-7 induces NSCLC cell apoptosis, arrests the cell cycle in the G2 phase, and suppresses the stemness properties of NSCLC .
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-
- HY-143246
-
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EGFR
Apoptosis
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Cancer
|
|
EGFR kinase inhibitor 1 is a potent EGFR inhibitor with IC50s of 37, 1.7, >300 nM for WT, l885R/T790M, L858R/T790M/C797S, respectively. EGFR kinase inhibitor 1 induces apoptosis and cell cycle arrest at G0/G1-phase. EGFR kinase inhibitor 1 inhibits the cell motility. EGFR kinase inhibitor 1 shows antiproliferative and anti-tumor activity .
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-
- HY-18200A
-
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E5555 hydrochloride; ER-172594-00 hydrochloride
|
Protease Activated Receptor (PAR)
JAK
Apoptosis
|
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-149407
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VEGFR
CDK
EGFR
Necroptosis
Apoptosis
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Cancer
|
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Multi-kinase-IN-4 (compound 5d) is multi-targeted kinase inhibitor, including VEGFR2, EGFR, HER2, and CDK2, with IC50 values of 0.33, 0.22, 0.18 and 2.09 μM, respectively. Multi-kinase-IN-4 shows broad-spectrum anti-cancer activities against HepG2, MCF-7, MDA-231, and HeLa cell lines (IC50 = 1.94–7.1 µM), but exhibits lower toxicity in the WI-38 cells (IC50 = 40.85 µM). Multi-kinase-IN-4 induces apoptosis and arrests cell cycle at S phase in HepG2 cells. Multi-kinase-IN-4 has the potential for the research of cancer .
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-
- HY-161863
-
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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
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-
- HY-159519
-
|
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Apoptosis
EGFR
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Cancer
|
|
EGFR/HER2-IN-16 (compound 12K) is an effective dual-target inhibitor of EGFR (IC50=6.15 nM) and HER-2 (IC50=9.78 nM) with anti-tumor activity. EGFR/HER2-IN-16 can inhibit the migration of SK-BR-3 cells, arrest the cell cycle in the G0/G1 phase, and induce apoptosis. EGFR/HER2-IN-16 exhibits good anti-proliferative activity against tumor cell models and has little damage to healthy cells. EGFR/HER2-IN-16 can be used in breast cancer research .
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-
- HY-161521
-
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Polo-like Kinase (PLK)
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Cancer
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|
PLK1-IN-10 (Compound 4Bb) is an orally active PLK1 PBD (polo-box domain) inhibitor. PLK1-IN-10 blocks the interaction of PLK1 with the cell division regulator protein 1 (PRC1) and decreases the protein expression of the CDK1-Cyclin B1 complex. PLK1-IN-10 reacts with glutathione (GSH) to increase cellular oxidative stress, ultimately leading to cell death .
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-
- HY-147901
-
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Histone Demethylase
CDK
Apoptosis
Caspase
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Cancer
|
|
KDM1/CDK1-IN-1 (compound 4) is a potent KDM1 and CDK1 inhibitor, with IC50 values of 0.096 and 0.078 μM, respectively.KDM1/CDK1-IN-1 induces cell cycle arrest at G2/M phase and apoptosis in HOP-92 cells. KDM1/CDK1-IN-1 exhibits potent cytotoxic activity against the CCRF-CEM, HOP-92 and Hep-G2 cells, with IC50 values of 16.34, 3.45 and 7.79 μM, respectively .
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-
- HY-168714
-
|
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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 .
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-
- HY-163288
-
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Histone Methyltransferase
HSP
Apoptosis
|
Cancer
|
|
EZH2/HSP90-IN-29 is a dual inhibitor for EZH2 and HSP90, with IC50s of 6.29 nM and 60.1 nM, for EZH2 and HSP90, respectively. EZH2/HSP90-IN-29 increases apoptosis/necrosis-related gene expression, induces cell cycle arrest at M phase and inhibits reactive oxygen species (ROS) catabolism pathway. EZH2/HSP90-IN-29 is able to cross the blood-brain-barrier (BBB) .
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-
- HY-168623
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|
|
EGFR
Apoptosis
Necroptosis
Bcl-2 Family
Caspase
MDM-2/p53
|
Cancer
|
|
EGFR-IN-134 (compound 3f), a triazolo[3,4-a]isoquinoline derivative, is a potent EGFR inhibitor with an IC50 of 0.023 µM. EGFR-IN-134 induces apoptosis and necrosis. EGFR-IN-134 initiates cell cycle arrest at the G2/M and pre-G1 phases, downregulates anti-apoptotic protein Bcl2 and upregulates pro-apoptotic proteins: p53, Bax, and caspases 3, 8, and 9. EGFR-IN-134 shows antiproliferative and anticancer activity .
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-
- HY-139604
-
|
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MARK
Apoptosis
|
Cancer
|
|
PCC0208017 is a microtubule affinity regulating kinases (MARK3/MARK4) inhibitor with IC50s of 1.8 and 2.01 nM, respectively. PCC0208017 has much lower inhibitory activity against MARK1 and MARK2, with IC50s of 31.4 and 33.7 nM, respectively. PCC0208017 suppresses glioma progression in vitro and in vivo. PCC0208017 disrupts microtubule dynamics and induces G2/M phase cell cycle arrest and cell apoptosis. PCC0208017 demonstrates robust antitumor activity in vivo and displays good BBB permeability .
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-
- HY-143233
-
|
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Pim
HDAC
Apoptosis
|
Cancer
|
|
PIM-1/HDAC-IN-1 (compound 4d) is a PIM-1 inhibitor, with an IC50 of 343.87 nM. PIM-1/HDAC-IN-1 has strong inhibitory activity and selectivity against HDAC 1 and HDAC 6, with IC50 values of 63.65 and 62.39 nM, respectively. PIM-1/HDAC-IN-1 exhibits apoptosis inducing potential in MCF-7 cell lines. PIM-1/HDAC-IN-1 shows pre-G1 apoptosis and cell cycle arrest at G2/M phase .
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-
- HY-161769
-
|
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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))
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-
- 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 .
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- HY-162895
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Polo-like Kinase (PLK)
Akt
CDK
Caspase
Apoptosis
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Cancer
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NL13 is a Polo-like kinase 4 (PLK4) inhibitor with an IC50 value of 2.32 μM. NL13 can inhibit the viability of PC3 and DU145 prostate cancer cells, with IC50 values of 3.51 μM and 2.53 μM, respectively. NL13 can lead to the inactivation of the AKT signaling pathway by downregulating CCNB1/CDK1, inducing G2/M cell cycle arrest, and triggering apoptosis through the cleavage of caspase-9/caspase-3. In prostate cancer mice, NL13 can inhibit tumor growth .
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- HY-169093
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PROTACs
Epigenetic Reader Domain
Apoptosis
|
Cancer
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MS41 is a selective eleven-nineteen leukemia (ENL) PROTAC degrader, with DC50s of 3.50 nM (MV4;11), 2.84 nM (SEMK2), 3.03 nM (Jurkat), and 26.58 nM (KASUMI1), respectively. MS41 effectively inhibits the growth of ENL-dependent leukemia cells, induces G1 cell cycle arrest and increases apoptosis. MS41 reduces the chromatin occupancy of ENL-associated transcription elongation machinery, and suppresses oncogenic gene expression and leukemia progression. Red: ENL ligand (HY-169094). Black: linker (HY-W105744). Blue: VHL ligand (HY-112078) .
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- HY-159897
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PAK
LIM Kinase (LIMK)
Apoptosis
Reactive Oxygen Species
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Cancer
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PAK4-IN-5 (Compound 12i) is a PAK4 inhibitor (IC50: 7.68 nM for PAK4, 1872.01 nM for PAK1). PAK4-IN-5 binds to PAK4 stably via multiple interactions. PAK4-IN-5 inhibits the proliferation and the migratory potential of MDA-MB-231 cells by inhibiting the phosphorylation of PAK4 and LIMK1. PAK4-IN-5 arrests cell cycle in the G0/G1 phase, induces apoptosis and ROS production. LD50: >500 mg/kg for mice (p.o.) .
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- HY-169938
-
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HDAC
Histone Demethylase
Apoptosis
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Cancer
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LSD1/HDAC-IN-2 (Compound 20c) is the inhibitor for LSD and HDAC, that inhibits LSD1, HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8, with IC50s of 39.0, 1.4, 1.0, 1.3, 2.9 and 16.0 nM, respectively. LSD1/HDAC-IN-2 inhibits the proliferation of cancer cells, especially the colorectal cancer cells. LSD1/HDAC-IN-2 arrests the cell cycle at G2/M phase, inhibits cell migration, and induces apoptosis in HCT-116 and HT-29 cells. LSD1/HDAC-IN-2 exhibits antitumor efficacy in mouse model without significant toxicity .
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- HY-157125
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PI3K
Apoptosis
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Cancer
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PI3Kα-IN-14 (compound F8) is a selective PI3Kα inhibitor with an IC50 of 0.14 nM. PI3Kα-IN-14 induces a great decrease in mitochondrial membrane which caused cell cycle arrest at G1 phase and apoptosis in U87-MG cells. PI3Kα-IN-14 shows significant anti-proliferative activities against three tumor-derived cell lines (PC-3: IC50 of 0.28 μM; HCT-116: IC50 of 0.57 μM; and U87-MG: IC50 of 1.37 μM) .
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- HY-168574
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Sirtuin
Apoptosis
PROTACs
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Cancer
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SZU-B6 is a PROTAC degrader for SIRT6 with DC50 of 45 nM and 154 nM in cell SK-HEP-1 and Huh-7. SZU-B6 inhibits the proliferation of cell SK-HEP-1 with an IC50 of 1.51 μM, inhibits the colony formation of SK-HEP-1 and Huh-7, induces apoptosis and arrests the cell cycle at G2/M phase in SK-HEP-1. SZU-B6 exhibits antitumor efficacy in mouse model. (Pink: ligand for target protein (HY-16605); Black: linker (HY-W012935); BLue: ligand for E3 ligase (HY-W453548)
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- HY-152263
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PROTACs
CDK
Apoptosis
|
Cancer
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HEMTAC CDK4/6 degrader 1 is a PROTAC connected by ligands for HSP90 and CDK4/6 with a Kd value of 35.7 μM. HEMTAC CDK4/6 degrader 1 induces CDK4/6 degradation in B16F10 melanoma cells. HEMTAC CDK4/6 degrader 1 arrests cell cycle at G0/G1 phase and induces apoptosis. HEMTAC CDK4/6 degrader 1 can be used in research of cancer . HEMTAC CDK4/6 degrader 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-143471
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PLK1/BRD4-IN-1
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Polo-like Kinase (PLK)
Epigenetic Reader Domain
Apoptosis
Androgen Receptor
c-Myc
|
Cancer
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WNY0824 (PLK1/BRD4-IN-1) is an orally active dual inhibitor of PLK1 and BET protein families, with IC50 values of 22, 402.5, 150.7, 103.9, and 311.9 nmol/L for PLK1, BRD2, BRD3, BRD4, and BRDT, respectively. WNY0824 induces cell cycle arrest and apoptosis by inhibiting AR- and MYC-mediated transcriptional processes. In addition, WNY0824 also inhibits tumor growth in Enzalutamide (HY-70002) resistant CRPC xenograft tumor models .
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- HY-146276
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HDAC
CDK
Apoptosis
|
Cancer
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CDK/HDAC-IN-2 is a potent HDAC/CDK dual inhibitor with IC50 of 6.4, 0.25, 45, >1000, 8.63, 0.30, >1000 nM for HDAC1, HDAC2, HDAC3, HDAC6,8, CDK1, CDK2, CDK4,6,7, respectively. CDK/HDAC-IN-2 shows excellent antiproliferative activities. CDK/HDAC-IN-2 induces apoptosis and cell cycle arrest at G2/M phase. CDK/HDAC-IN-2 shows potent antitumor efficacy .
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- HY-151436
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CDK
Cholinesterase (ChE)
Apoptosis
|
Cancer
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|
ZLMT-12 (compound 35), tacrine derivatives, is a potent, orally active CDK2/9 inhibitor with IC50 values of 0.002 and 0.011 μM for CDK9 and CDK2, respectively. ZLMT-12 has a weak inhibitory effect on AChE (IC50=19.023 μM) and BChE (IC50=2.768 μM). ZLMT-12 has low toxicity and antiproliferative activity. ZLMT-12 induces apoptosis and arrests the cell cycle in the S phase and G2/M phase .
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- HY-154855
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HDAC
|
Cancer
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HDAC-IN-56 ((S)-17b) is an orally active class I histone deacetylase (HDAC) inhibitor with IC50 values of 56.0 ± 6.0, 90.0 ± 5.9, 422.2 ± 105.1, >10000 nM for HDAC1, HDAC2, HDAC3, and HDAC4-11, respectively. HDAC-IN-56 has potent inhibitory activity while strongly increasing intracellular levels of acetylhistone H3 and P21 and effectively inducing G1 cell cycle arrest and apoptosis.HDAC-IN-56 has antitumor activity .
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- HY-N0711R
-
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Notch
Apoptosis
Fungal
Endogenous Metabolite
Bacterial
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Infection
Inflammation/Immunology
Cancer
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Carvacrol (Standard) is the analytical standard of Carvacrol. This product is intended for research and analytical applications. Carvacrol is an orally active monoterpenic phenol that can be extract from an abundant number of aromatic plants, including thyme and oregano, possessing antioxidant, antibacterial, antifungal, anticancer, anti-inflammatory, hepatoprotective, spasmolytic, and vasorelaxant properties. Carvacrol also causes cell cycle arrest in G0/G1, downregulates Notch-1, and Jagged-1, and induces apoptosis. Carvacrol is used in low concentrations as a food flavoring ingredient and preservative, as well as a fragrance ingredient in cosmetic formulations .
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- HY-161966
-
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Apoptosis
Reactive Oxygen Species
VEGFR
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Cancer
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VEGFR-2-IN-52 (compound 14d) is a potent VEGFR-2 inhibitor with an IC50 value of 191.1 nM. VEGFR-2-IN-52 decreases the protein expression of p-VEGFR-2, MMP9, p-ERK1/2 and p-MEK1. VEGFR-2-IN-52 shows cytotoxicity. VEGFR-2-IN-52 induces apoptosis and cell cycle arrest at G0/G1 phase. VEGFR-2-IN-52 increases the levels of ROS .
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- HY-161923
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EGFR
Apoptosis
Akt
ERK
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Cancer
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EGFR-IN-120 (Compound 11eg) is an orally active EGFR inhibitor. EGFR-IN-120 inhibits EGFR L858R/T790M/C797S with an IC50 value of 0.053 μM, and has a relatively weak effect on EGFR WT (IC50: 1.05 μM). EGFR-IN-120 inhibits the phosphorylation of EGFR and main downstream effectors (STAT3, AKT, and Erk). EGFR-IN-120 induces cell cycle arrest and cell apoptosis in EGFR mutant cells. EGFR-IN-120 inhibits the proliferation of the NSCLC cells harboring EGFR L858R/T790M/C797S with an IC50 of 0.052 μM .
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- HY-149521
-
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PI3K
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Cancer
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PI3K-IN-47 (Compound 27) is a bivalent PI3K inhibitor (IC50: 0.44 nM for PI3Kα, 7.18 nM, 13.92 nM, 22.83 nM for PI3Kβ, PI3Kγ, PI3Kδ). PI3K-IN-47 induces cell cycle arrest in G1 phase, inhibits colony formation and cell migration. PI3K-IN-47 inhibits tumor growth in HGC-27 xenograft mice .
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- HY-101257
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CDK
|
Cancer
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YKL-5-124 is a potent, selective, irreversible and covalent CDK7 inhibitor with IC50s of 53.5 nM and 9.7 nM for CDK7 and CDK7/Mat1/CycH, respectively. YKL-5-124 is >100-fold greater selective for CDK7 than CDK9 and CDK2, and inactive against CDK12 and CDK13. YKL-5-124 induces a strong cell-cycle arrest, inhibits E2F-driven gene expression, and exhibits little effect on RNA polymerase II phosphorylation status .
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- HY-146253
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CDK
Apoptosis
Bcl-2 Family
Caspase
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Cancer
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CDK1/2/4-IN-1 (compound 3a) is a potent CDK inhibitor with IC50 values of 1.47, 0.78 and 0.87 μM for CDK1, CDK2 and CDK4, respectively. CDK1/2/4-IN-1 arrests cell cycle at G2/M phase and induces apoptosis. CDK1/2/4-IN-1 elevates Bax, caspase-3, P53 levels and decreases Bcl-2 level. CDK1/2/4-IN-1 can be used for cancer research .
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-
- HY-152146
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Apoptosis
FGFR
HDAC
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Cancer
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HDAC-IN-50 is a potent and orally active FGFR and HDAC dual inhibitor with IC50 values of 0.18, 1.2, 0.46, 1.4, 1.3, 1.6, 2.6, 13 nM for FGFR1, FGFR2, FGFR3, FGFR4, HDAC1, HDAC2, HDAC6, HDAC8, respectively. HDAC-IN-50 induces Apoptosis and cell cycle arrest at G0/G1 phase. HDAC-IN-50 decreases the expression of pFGFR1, pERK, pSTAT3. HDAC-IN-50 shows anti-tumor activity .
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- HY-W032013S3
-
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Octanol-d5
|
Calcium Channel
Endogenous Metabolite
Isotope-Labeled Compounds
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Others
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1-Octanol-d5 is deuterated labeled Carvacrol (HY-N0711). Carvacrol is an orally active monoterpenic phenol that can be extract from an abundant number of aromatic plants, including thyme and oregano, possessing antioxidant, antibacterial, antifungal, anticancer, anti-inflammatory, hepatoprotective, spasmolytic, and vasorelaxant properties. Carvacrol also causes cell cycle arrest in G0/G1, downregulates Notch-1, and Jagged-1, and induces apoptosis. Carvacrol is used in low concentrations as a food flavoring ingredient and preservative, as well as a fragrance ingredient in cosmetic formulations .
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- HY-163511
-
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Akt
Apoptosis
mTOR
PI3K
Microtubule/Tubulin
|
Cancer
|
|
PI3K/Akt/mTOR-IN-4 (compound 4r) is a potent PI3K/Akt/mTOR and tubulin polymerization inhibitor. PI3K/Akt/mTOR-IN-4 induce apoptosis and cell cycle arrest at G2/M phase. PI3K/Akt/mTOR-IN-4 decreases the expression of p-PI3K, p-Akt, and p-mTOR, β-tubulin .
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-
- HY-164384
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PI3K
Akt
mTOR
Apoptosis
|
Cancer
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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 .
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-
- HY-158310
-
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EGFR
Ras
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Cancer
|
|
SOS1/EGFR-IN-1 (compound SE-9) is a dual-target inhibitor for the prostate cancer. SOS1/EGFR-IN-1 inhibits effectively SOS1(IC50=42.13±1.55 nM) and EGFR(IC50=1.01±0.04 nM) by inhibiting their downstream effector molecules. SOS1/EGFR-IN-1 induces apoptosis and G1 phase cell cycle arrest, reducing angiogenesis and migration. SOS1/EGFR-IN-1 shows significant antitumor effects in prostate cancer cells PC-3 (IC50=0.45±0.03 μM) .
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-
- HY-168608
-
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TRP Channel
Apoptosis
PI3K
Akt
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Cancer
|
|
TRPM7-IN-1 (compound SUD), a benzoylurea derivative, is an effective TRPM7 inhibitor. TRPM7-IN-1 induces cell cycle arrest and apoptosis, decreases the migration of MCF-7 and BGC-823 cells. TRPM7-IN-1 decreases vimentin expression and increases E-cadherin expression. TRPM7-IN-1 potentially reduces the TRPM7-like current and decreases TRPM7 expression through the PI3K/Akt signaling pathway. TRPM7-IN-1 is a potential agent to suppress the metastasis of breast and gastric cancer by inhibiting TRPM7 expression and function .
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- HY-123450
-
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Bcr-Abl
Apoptosis
PDGFR
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Cancer
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|
S116836, a potent, orally active BCR-ABL tyrosine kinase inhibitor, blocks both wild-type as well as T315I Bcr-Abl. S116836 arrests the cells in the G0/G1 phase of cell cycle, induces apoptosis, increases ROS production, and decreases GSH production in BaF3/WT and BaF3/T315I cells. S116836 also inhibits SRC, LYN, HCK, LCK and BLK, and receptor tyrosine kinases such as FLT3, TIE2, KIT, PDGFR-β. Antitumor activies . S116836 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-101257B
-
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CDK
|
Cancer
|
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YKL-5-124 TFA is a potent, selective, irreversible and covalent CDK7 inhibitor with IC50s of 53.5 nM and 9.7 nM for CDK7 and CDK7/Mat1/CycH, respectively. YKL-5-124 TFA is >100-fold greater selective for CDK7 than CDK9 and CDK2, and inactive against CDK12 and CDK13. YKL-5-124 TFA induces a strong cell-cycle arrest, inhibits E2F-driven gene expression, and exhibits little effect on RNA polymerase II phosphorylation status .
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-
- HY-146749
-
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FLT3
Trk Receptor
Apoptosis
|
Cancer
|
|
FLT3/TrKA-IN-1 is a potent FLT3/TrKA dual kinase inhibitor with the IC50s of 43.8 nM, 97.2 nM, 92.5 nM and 23.6 nM for FLT3, FLT3-ITD, FLT3-TKD and TrKA, respectively. FLT3/TrKA-IN-1 induces cell cycle arrest at the G0/G1 phase as well as apoptosis and shows antiproliferative activity in vitro. FLT3/TrKA-IN-1 has the potential for the research of Acute myeloid leukemia (AML) .
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-
- HY-152226
-
|
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HDAC
Apoptosis
|
Cancer
|
|
MC2590 is a potent pyridine-containing histone deacetylase (HDAC) inhibitor. MC2590 is a inhibitor of HDAC1-3, -6, -8, and -10 (class I/IIb-selective inhibitor) with IC50s of 0.015 μM-0.156 μM. MC2590 also inhibits HDAC isoforms HDAC4, HDAC5, HDAC7, HDAC9, HDAC11 with IC50s of 1.35 μM-3.98 μM. MC2625 induces G2/M cell cycle arrest and modulates pro- and anti-apoptotic microRNAs towards apoptosis induction .
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- HY-168725
-
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PROTACs
Kinesin
Apoptosis
|
Cancer
|
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PROTAC KSP-IN-1 (Compound 21) is a PROTAC Degrader for kinesin spindle protein (KSP), that degrades KSP in HCT-116 with DC50 of 114.8 nM. PROTAC KSP-IN-1 inhibits the proliferation of HCT-116 with IC50 of 10 nM, arrests the cell cycle of HCT-116 at G2/M phase, and induces apoptosis in HCT-116. PROTAC KSP-IN-1 exhibits antitumor efficacy in mouse model . (Blue: Ligand for E3 Ligase Cereblon (HY-103596); Blank: Linker (HY-168726); Pink: Target Protein Ligand (HY-168727))
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- HY-124273
-
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L-threo Cer(d18:1/2:0); L-threo Ceramide (d18:1/2:0); N-acetyl-L-threo-Sphingosine
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Endogenous Metabolite
|
Cardiovascular Disease
|
|
C2 L-threo Ceramide (d18:1/2:0) (L-threo Cer(d18:1/2:0); L-threo Ceramide (d18:1/2:0)) is a bioactive sphingolipid and cell-permeable analog of naturally occurring ceramides. It stimulates cholesterol efflux in CHO cells expressing the human ABCA1 receptor when used at a concentration of 10 μM, however, this efflux is 50% less than that stimulated by C2 ceramide. C2 L-threo Ceramide inhibits IL-4 production by 17% in EL4 T cells stimulated with phorbol 12-myristate 13-acetate when used at a concentration of 10 μM. It also induces cell cycle arrest in the G0/G1 phase and a 7-fold increase in sphingosine accumulation as well as inhibits growth of HL-60 leukemia cells.
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-
- HY-159122
-
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Carbonic Anhydrase
Reactive Oxygen Species
Apoptosis
|
Cancer
|
|
CA IX-IN-2 (Compound 9o) is an inhibitor for carbonic anhydrase (CA), that inhibits CA IX, CA XII and CA II with an IC50 of 5.6, 7.4 and 430 nM, respectively. CA IX-IN-2 inhibits the proliferation of cancer cell HCT-116, SW480, MDA-MB 231 and MCF-7, with IC50s of 14.63-29.33 μM. CA IX-IN-2 intercalates DNA, arrests cell cycle at G1/S phase, and induces apoptosis in MDA-MB-231. CA IX-IN-2 affects the mitochondrial membrane potential (MMP), increases the intracellular ROS levels, causes mitochondrial damage, and inhibits the cell migration of MDA-MB-231. CA IX-IN-2 exhibits antitumor efficacy in mouse models .
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-
- HY-147898
-
|
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PI3K
Apoptosis
|
Cancer
|
|
PI3K-IN-33 (Compound 6e) is a highly selective PI3K inhibitor with IC50 values of 11.73, 6.09 and 11.18 μM for PI3K-α、PI3K-β and PI3K-δ , respectively. PI3K-IN-33 arrests cell cycle at G2/M phase and induces apoptosis. PI3K-IN-33 can be used in leukemia research .
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-
- HY-147900
-
|
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PI3K
Apoptosis
|
Cancer
|
|
PI3K-IN-35 (Compound 6l) is a highly selective PI3K inhibitor with IC50 values of 13.98, 7.22 and 10.94 μM for PI3K-α、PI3K-β and PI3K-δ, respectively. PI3K-IN-35 arrests cell cycle at G2/M phase and induces apoptosis. PI3K-IN-35 can be used in leukemia research .
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-
- HY-147899
-
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PI3K
Apoptosis
|
Cancer
|
|
PI3K-IN-34 (Compound 6g) is a highly selective PI3K inhibitor with IC50 values of 11.73, 6.09 and 11.18 μM for PI3K-α、PI3K-β and PI3K-δ , respectively. PI3K-IN-34 arrests cell cycle at G2/M phase and induces apoptosis. PI3K-IN-34 can be used in leukemia research .
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- HY-161688
-
|
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Apoptosis
HDAC
|
Cancer
|
|
HDAC-IN-73 (compound P-503) is a histone deacetylase (HDAC) inhibitor. HDAC-IN-73 shows IC50s values of 0.17, 0.49 µM for HDAC1 and HDAC6, respectively. Notably, HDAC-IN-73's inhibitory potency against HDAC6 is heightened, exhibiting a 9-fold greater efficacy than PsA (HY-N2150) (IC50=3.9 μM). HDAC-IN-73 shows potent antiproliferative activity, induces apoptosis, and causes cell cycle arrest at G2 / M phase. HDAC-IN-73 has the potential to be used for the research of cancer such as colon cancer .
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-
- HY-146095
-
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MDM-2/p53
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
p53 Activator 2 (compound 10ah) intercalats into DNA and results in significant DNA double-strand break.p53 Activator 2 increases the expression of p53, p-p53, CDK4, p21 to cause cell cycle arrest at G2/M phase.p53 Activator 2 induce apoptosis and significantly down-regulates the anti-apoptosis proteins Bcl-2, Bcl-xL and the levels of cyclin B1.p53 Activator 2 has anti-proliferation activity against MGC-803 cells, with an IC50 of 1.73 µM. p53 Activator 2 displays potent anticancer efficiency against MGC-803 xenograft tumors models .
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- HY-162927
-
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MDM-2/p53
Apoptosis
|
Cancer
|
|
p53-MDM2-IN-6 (Compound 10a), a LSM-83177 hydrazone analog, is a potent p53-MDM2 inhibitor with an IC50 value of 11.08 µg/mL. p53-MDM2-IN-6 arrests the cell cycle in the S phase and induces early and late Apoptosis with antiproliferative activity against HT29 cell lines with an IC50 value of 10.44 µg/mL. p53-MDM2-IN-6 inhibits p53-MDM2 interaction with increment in p-53 level and decrease the expression of GST enzymes. p53-MDM2-IN-6 is promising for research of colorectal cancer .
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- HY-N6871
-
|
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Bacterial
IKK
Ferroptosis
|
Infection
Metabolic Disease
Inflammation/Immunology
Cancer
|
Abietic acid, an orally active diterpene isolated from Colophony, displays significant anti-proliferative, anti-inflammatory, anti-obesity effect, bacteriostatic, cell cycle arresting and pro-apoptotic activities. Abietic acid inhibits lipoxygenase activity for allergy. Abietic acid enhances cell migration and tube formation in HUVECs. Abietic acid induces significant angiogenic potential, which is associated with upregulation of extracellular signal-regulated kinase (ERK) and p38 expression. Abietic acid attenuates sepsis-induced lung injury by inhibiting nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) pathway to inhibit M1 macrophage polarization. Abietic acid exhibits a positive effect against liver injury by attenuating inflammation and ferroptosis. Abietic acid shows accelerated wound closure in a mouse model of cutaneous wounds. Abietic acid significantly reduces the proliferation and growth of NSCLC cells by IKKβ inhibition.Additionally, Abietic acid ameliorates psoriasis-like inflammation and modulates gut microbiota in mice. Abietic acid is promising for research in non-small-cell lung cancer (NSCLC), liver injury-related deseases and psoriasis .
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-
- HY-101034
-
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CHMFL-ABL-KIT-155
|
Bcr-Abl
c-Kit
Apoptosis
PDGFR
Discoidin Domain Receptor
|
Cancer
|
|
CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155; compound 34) is a highly potent and orally active type II ABL/c-KIT dual kinase inhibitor (IC50s of 46 nM and 75 nM, respectively), and it also presents significant inhibitory activities to BLK (IC50=81 nM), CSF1R (IC50=227 nM), DDR1 (IC50=116 nM), DDR2 (IC50=325 nM), LCK (IC50=12 nM) and PDGFRβ (IC50=80 nM) kinases. CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155) arrests cell cycle progression and induces apoptosis .
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- HY-145736A
-
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Drug-Linker Conjugates for ADC
Apoptosis
|
Cancer
|
|
β-Glucuronide-dPBD-PEG5-NH2 TFA is the β-glucuronide-linked pyrrolobenzodiazepine dimer, which binds to the prenylated antibody for synthesis of antibody-drug conjugate (ADC) cIRCR201-dPBD.β-glucuronide-linkage as a cleavable linker. β-Glucuronide-dPBD-PEG5-NH2 TFA, as a proagent of cIRCR201-dPBD, reduces side effects. β-Glucuronide-dPBD-PEG5-NH2 TFA can induce apoptosis and arrest cell cycle. β-Glucuronide-dPBD-PEG5-NH2 TFA has antitumor activity .
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-
- HY-145736
-
|
|
Drug-Linker Conjugates for ADC
Apoptosis
|
Cancer
|
|
β-Glucuronide-dPBD-PEG5-NH2 is the β-glucuronide-linked pyrrolobenzodiazepine dimer, which binds to the prenylated antibody for synthesis of antibody-drug conjugate (ADC) cIRCR201-dPBD. β-glucuronide-linkage as a cleavable linker. β-Glucuronide-dPBD-PEG5-NH2, as a proagent of cIRCR201-dPBD, reduces side effects. β-Glucuronide-dPBD-PEG5-NH2 can induce apoptosis and arrest cell cycle. β-Glucuronide-dPBD-PEG5-NH2 has antitumor activity .
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-
- HY-147825
-
|
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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-169170
-
|
|
Apoptosis
DNA/RNA Synthesis
Epigenetic Reader Domain
PARP
|
Cancer
|
|
PARP1/BRD4-IN-3 (compound HF4) is a potent BRD4 and PARP1 inhibitor with IC50 values of 1210, 2019 nM for BRD4, PARP1, respectively. PARP1/BRD4-IN-3 shows antiproliferative activities. PARP1/BRD4-IN-3 induces apoptosis and cell cycle arrest at G0/G1 phase. PARP1/BRD4-IN-3 causes DNA damage and reduces the protein expression of Rad51. PARP1/BRD4-IN-3 shows antitumor efficacy .
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-
- HY-159147
-
|
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PROTACs
ROS Kinase
Apoptosis
|
Cancer
|
|
SIAIS039 is an orally active c-ros oncogene 1 (ROS1)-specific PROTAC with DC50s of 154.46 nM, 126.47 nM, 143.69 nM for HCC78 cells, Ba/F3 expressing the CD74-ROS1 fusion and Ba/F3 expressing the SDC4-ROS1 fusion, respectively. SIAIS039 suppresses cell proliferation, induces cell cycle arrest and apoptosis, and inhibits clonogenicity against ROS1-positive cells. SIAIS039 demonstrates anti-tumour effects against ROS1-driven tumor growth vivo. SIAIS039 is composed of the ALK inhibitor Brigatinib (HY-12857), a linker EM-12 (HY-138793), and a VHL ligand E3 ubiquitin ligase 1-Butyne (Red: Brigatinib; Blue: VHL ligand; Black: linker) .
|
-
- HY-149824
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
EGFR T790M/L858R-IN-2 is a potent and selective EGFRT790M/L858R inhibitor with IC50 values of 3.5, 1290 nM for EGFRT790M/L858R, EGFR WT, respectively. EGFR T790M/L858R-IN-2 decreases the expression of p-EGFR, P-AKT, P-ERK1/2. EGFR T790M/L858R-IN-2 induces Apoptosis and cell cycle arrest in the G1 phase. EGFR T790M/L858R-IN-2 shows anti-cancer activity .
|
-
- HY-158117
-
|
|
Apoptosis
Autophagy
|
Cancer
|
|
[Cu2Cl2(4'-(4-Methoxy-1-naphthyl)-terpy)2](PF6)2 (Compound 3) is a copper complex, which inhibits cell viability of HCT116, HCT116DoxR, A2780 and fibroblasts, with IC50s of 0.13, 0.15, 0.66 and 6.24 μM, respectively. [Cu2Cl2(4'-(4-Methoxy-1-naphthyl)-terpy)2](PF6)2 induces apoptosis and autophagy, and arrests cell cycle at G0/G1 phase in HCT116DoxR. [Cu2Cl2(4'-(4-Methoxy-1-naphthyl)-terpy)2](PF6)2 exhibits antimetastatic efficacy .
|
-
2](//file.medchemexpress.eu/product_pic/hy-158117.gif)
- HY-163985
-
|
|
PROTACs
FGFR
Apoptosis
|
Cancer
|
|
PROTAC FGFR2 degrader 1 (compound N5) is a PROTAC that effectively targets FGFR2 with DC50 of 6.46 nM, the FGFR2 IC50 is 0.08 nM. PROTAC FGFR2 degrader 1 has anti-proliferative activity and highly selective, induces G0/G1 arrest of KATOIII and SNU16 cell cycle and inhibits apoptosis by reducing the activation of p-ERK and p-PLCγ, the downstream proteins of FGFR2.
PROTAC FGFR2 degrader 1 inhibits gastric cancer cells remained above 50% at a concentration of 0.17 nM.
PROTAC FGFR2 degrader 1 potently inhibits the growth of SNU16 xenograft tumors in mouse model (Structure Note: Pink, FGFR2 activator: HY-18708; Blue, E3 ligase ligand: HY--10984; Black, linker: HY-163989; E3 ligase ligand + linker：HY-163986) .
|
-
- HY-161989
-
|
|
PROTACs
BCL6
|
Cancer
|
|
DZ-837 (compound 3d) is a PROTAC targeting BCL6 with a DC50 of approximately 600 nM. DZ-837 can induce cell cycle arrest and exert synergistic anticancer effects with Ibrutinib (HY-10997). DZ-837 is composed of PROTAC target protein ligand BCL6 ligand-2 (HY-161990) (red part), E3 ubiquitin ligase ligand Thalidomide-4-OH (HY-103596) (blue part), and PROTAC Linker (HY-W245803) (black part), among which the conjugate of E3 ubiquitin ligase ligand + Linker is 2-(2,6-Dioxopiperidin-3-yl)-4-((2-(2-hydroxyethoxy)ethyl)amino)isoindoline-1,3-dione (HY-W924949) [1] .
|
-
- HY-163679
-
|
|
Estrogen Receptor/ERR
Cytochrome P450
PROTACs
Apoptosis
|
Cancer
|
|
PROTAC ERα Degrader-9 (Compound 18c) is a dual-targeting PROTAC degrader, which degrades estrogen receptor α (ERα) and aromatase (ARO). PROTAC ERα Degrader-9 binds to ERα with a Ki of 0.25 μM, inhibits ARO with an IC50 of 4.6 μM. PROTAC ERα Degrader-9 inhibits the proliferation of MCF-7 wildtype (IC50=0.54 μM) and ERα mutants MCF-7 EGFR (IC50=0.075 μM), MCF-7 D538G (IC50=0.31 μM), MCF-7 Y537S (IC50=2.3 μM), downregulates the expressions of ERS1 and MYC. PROTAC ERα Degrader-9 arrests the cell cycle at G2/M, induces apoptosis in MCF-7. PROTAC ERα Degrader-9 exhibits antitumor efficacy in mouse models. (Pink: ligand for target protein (HY-163680); Black: linker (HY-W007559); Blue: ligand for E3 ligase (HY-112078))
|
-
| Cat. No. |
Product Name |
Type |
-
- HY-W127705
-
|
|
Fluorescent Dyes/Probes
|
|
Quinacrine mustard dihydrochloride is a fluorochrome. Quinacrine mustard dihydrochloride as a polycyclic aromatic agent can be used as mutagenic agent induces the mutants of bacteria. Quinacrine mustard dihydrochloride induces cell cycle arrest at G2/M-phase. Quinacrine mustard dihydrochloride has the potential for the research of plant, animal, or human chromosomes .
|
| Cat. No. |
Product Name |
Type |
-
- HY-N1428A
-
|
|
Buffer Reagents
|
|
Citric acid monohydrate is a natural preservative and food tartness enhancer. Citric acid monohydrate induces apoptosis and cell cycle arrest at G2/M phase and S phase. Citric acid monohydrate cause oxidative damage of the liver by means of the decrease of antioxidative enzyme activities. Citric acid monohydrate causes renal toxicity in mice .
|
-
- HY-B2201
-
|
Sodium citrate; Trisodium citrate anhydrous
|
Buffer Reagents
|
|
Citric acid trisodium is a natural preservative and food tartness enhancer. Citric acid trisodium induces apoptosis and cell cycle arrest at G2/M phase and S phase. Citric acid trisodium cause oxidative damage of the liver by means of the decrease of antioxidative enzyme activities. Citric acid trisodium causes renal toxicity in mice .
|
-
- HY-N1428AR
-
|
|
Buffer Reagents
|
|
Citric acid (monohydrate) (Standard) is the analytical standard of Citric acid (monohydrate). This product is intended for research and analytical applications. Citric acid monohydrate is a natural preservative and food tartness enhancer. Citric acid monohydrate induces apoptosis and cell cycle arrest at G2/M phase and S phase. Citric acid monohydrate cause oxidative damage of the liver by means of the decrease of antioxidative enzyme activities. Citric acid monohydrate causes renal toxicity in mice .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-113638
-
|
GS-456332
|
Stearoyl-CoA Desaturase (SCD)
Apoptosis
|
Cancer
|
|
CVT-11127 is a potent SCD inhibitor. CVT-11127 induces apoposis and arrests the cell cycle at the G1/S phase. CVT-11127 has the potential for the research of lung cancer .
|
-
- HY-P2698
-
|
|
HDAC
Apoptosis
|
Cancer
|
|
1-Alaninechlamydocin, a cyclic tetrapeptide, is a potent HDAC inhibitor (IC50=6.4 nM). 1-Alaninechlamydocin induces G2/M cell cycle arrest and apoptosis in MIA PaCa-2 cells .
|
-
- HY-P1126
-
|
DLS 15
|
Microtubule/Tubulin
ADC Cytotoxin
Apoptosis
|
Cancer
|
|
Dolastatin 15 (DLS 15), a depsipeptide derived from Dolabella auricularia, is a potent antimitotic agent structurally related to the antitubulin agent Dolastatin 10. Dolastatin 15 induces cell cycle arrest and apoptosis in multiple myeloma cells. Dolastatin 15 can be used as an ADC cytotoxin .
|
-
- HY-P10324
-
|
p16INK4a peptide
|
Peptides
|
Cancer
|
|
TAT-p16 (p16INK4a peptide) is a peptide mimic of p16INK4a that can induce an early G phase cell cycle arrest in the absence of active cyclin E:Cdk2 complex .
|
-
- HY-19554
-
|
|
Histone Methyltransferase
Apoptosis
|
Cancer
|
|
MM-401 is a MLL1 H3K4 methyltransferase inhibitor. MM-401 inhibits MLL1 activity (IC50 = 0.32 μM) by blocking MLL1-WDR5 interaction. MM-401 can induce cell cycle arrest, apoptosis and differentiation. MM-401 can be used for the research of MLL leukemia .
|
-
- HY-P5910
-
|
|
MDM-2/p53
Apoptosis
|
Cancer
|
|
Azurin p28 peptide is a tumor-penetrated antitumor peptide. Azurin p28 peptide redues proteasomal degradation of p53 through formation of a p28: p53 complex. Azurin p28 peptide induces apoptosis or cell cycle arrest. Azurin p28 peptide inhibits p53-positive tumor growths. Azurin p28 peptide shows antiangiogenic effect by inhibiting phosphorylation of VEGFR-2, FAK and Akt .
|
-
- HY-P5910A
-
|
|
MDM-2/p53
Apoptosis
|
Cancer
|
|
Azurin p28 peptide TFA is a tumor-penetrated antitumor peptide. Azurin p28 peptide TFA redues proteasomal degradation of p53 through formation of a p28: p53 complex. Azurin p28 peptide TFA induces apoptosis or cell cycle arrest. Azurin p28 peptide TFA inhibits p53-positive tumor growths. Azurin p28 peptide TFA shows antiangiogenic effect by inhibiting phosphorylation of VEGFR-2, FAK and Akt .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P99284
-
|
MK-0646; h7C10
|
IGF-1R
Apoptosis
|
Cancer
|
|
Dalotuzumab (MK-0646) is a recombinant humanized monoclonal antibody (IgG1 type) targeting IGF-1R. Dalotuzumab acts by inhibiting IGF-1- and IGF-2-mediated tumor cell proliferation, IGF-1R autophosphorylation, and Akt phosphorylation. Dalotuzumab also induces apoptosis and cycle arrest. Dalotuzumab in combination with other anticancer agents such as statins can enhance the antitumor activity of Dalotuzumab in vitro and in vivo .
|
-
- HY-132260
-
|
IMGN529; Debio 1562
|
Antibody-Drug Conjugates (ADCs)
Apoptosis
|
Cancer
|
|
Naratuximab emtansine (IMGN529) is a CD37-targeted ADC consisting of a humanized IgG1 mAb coupled to the microtubule disruptor DM1. Naratuximab emtansine has high affinity and specificity for CD37, allowing ADC internalization, processing and intracellular release of DM1. Due to its ability to disrupt microtubule assembly, DM1 can subsequently induce cell cycle arrest and apoptosis .
|
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
- HY-N0726R
-
-
- HY-N0211
-
-
- HY-N7083
-
-
- HY-135217R
-
-
- HY-N13164
-
-
- HY-107780B
-
-
- HY-110382
-
-
- HY-N0623
-
-
- HY-126067
-
-
- HY-N2374R
-
-
- HY-N0800R
-
-
- HY-N11722
-
-
- HY-N6623
-
-
- HY-N0416
-
-
- HY-N0421
-
-
- HY-N1428
-
-
- HY-N1986
-
-
- HY-N13174
-
-
- HY-N1196
-
-
- HY-N2369
-
-
- HY-N8441
-
-
- HY-N0036R
-
-
- HY-N6016R
-
-
- HY-N0816
-
-
- HY-N12044
-
-
- HY-N10447
-
-
- HY-N9968
-
-
- HY-N11576
-
-
- HY-149132
-
|
DDA
|
Triterpenes
Structural Classification
Terpenoids
Source classification
Endogenous metabolite
|
LXR
|
|
Dendrogenin A (DDA) is a ligand for liver X receptor (LXR), that induces the expression of sodium/iodine symporter, and increases iodine uptake. Dendrogenin A induces cell differentiation of MCF-7, and reactivates the function of lactating cells. Dendrogenin A induces the expressions of the TSH receptor, thyroid peroxidase, and thyroglobulin, and affects thyroid hormone generation. Dendrogenin A exhibits cytotoxicity in cancer cell B-CPAP and 8505c with IC50 of 4.1 and 6.2 µM. Dendrogenin A arrests the cell cycle at G0/G1 phase .
|
-
- HY-13629R
-
-
- HY-118921
-
-
- HY-N2342
-
-
- HY-N10018
-
-
- HY-N0623R
-
|
Tryptophan (standard); Tryptophane (standard)
|
Structural Classification
Alkaloids
Ketones, Aldehydes, Acids
Source classification
Endogenous metabolite
|
Others
|
|
L-Tryptophan (standard) is the analytical standard of L-Tryptophan. L-Tryptophan (Tryptophan) is an orally active and essential amino acid that is the precursor of serotonin, melatonin, and vitamin B3. L-Tryptophan can promote an increase in stemness and osteogenic ability of BMSCs in vitro and in vivo. L-Tryptophan inhibits cell proliferation and induced cell cycle arrest with high levels .
|
-
- HY-N12960
-
-
- HY-17583
-
-
- HY-N7844
-
-
- HY-N1930
-
-
- HY-117652
-
-
- HY-N0662
-
-
- HY-16594
-
|
|
Structural Classification
Microorganisms
Antibiotics
Source classification
Other Antibiotics
|
Proteasome
Apoptosis
ROS Kinase
|
|
Lactacystin is a potent, orally active, irreversible, cell-permeable, selective 20S proteasome inhibitor (IC50 = 4.8 μM). Lactacystin also inhibits the lysosomal enzyme cathepsin A. Lactacystin inhibits cell growth and induces apoptosisand cell cycle arrest, and has antiviral and antioxidative activity. Lactacystin induces neurite outgrowth and hypertension. Lactacystin has the potential for the research of cancer, Neurological Disease, hypertension and Malaria, and so on [1] [2] [3] [4] [5] [6] [7] [8] [9] [10] .
|
-
- HY-N11439
-
-
- HY-138071
-
-
- HY-N6939
-
-
- HY-N7225
-
-
- HY-N7083R
-
-
- HY-N0211R
-
-
- HY-126596
-
-
- HY-121222
-
-
- HY-77813
-
-
- HY-N1428R
-
-
- HY-N0421R
-
|
|
Structural Classification
Animals
Source classification
Steroids
|
Apoptosis
|
|
Cinobufagin (Standard) is the analytical standard of Cinobufagin. This product is intended for research and analytical applications. Cinobufagin is an anticancer agent that can be secreted by the Asiatic toad Bufo gargarizans. Cinobufagin induces the cell cycle arrests in the G1 phase or G2/M phase, leading to apoptosis in cancer cells. Cinobufagin inhibits tumor growth in melanoma and glioblastoma multiforme xenograft mouse models .
|
-
- HY-N2369R
-
-
- HY-N0816R
-
|
|
Structural Classification
other families
Source classification
Plants
Steroids
|
Apoptosis
Pyroptosis
|
|
Polyphyllin VI (Standard) is the analytical standard of Polyphyllin VI. This product is intended for research and analytical applications. Polyphyllin VI, an active saponin, possess anti-cancer activities. Polyphyllin VI induces G2/M cell cycle arrest and triggers apoptosis. Polyphyllin VI induces caspase-1-mediated pyroptosis via the induction of ROS/NF-κB/NLRP3/GSDMD signal axis in non-small cell lung cancer .
|
-
- HY-A0098
-
-
- HY-N3764
-
-
- HY-N0202
-
-
- HY-N0451
-
-
- HY-N0416R
-
-
- HY-N1986R
-
-
- HY-N12124
-
-
- HY-N13201
-
-
- HY-N9942
-
-
- HY-18981
-
-
- HY-N2342R
-
-
- HY-N0662R
-
-
- HY-N6623R
-
-
- HY-N2071
-
-
- HY-N7175
-
|
9,11-Dehydroergosterol peroxide; 9(11)-DHEP
|
Structural Classification
Classification of Application Fields
Source classification
Solanum lyratum Thunberg
Solanaceae
Plants
Disease Research Fields
Steroids
Cancer
|
Apoptosis
Endogenous Metabolite
|
|
5,8-Epidioxyergosta-6,9(11),22-trien-3-ol (9,11-Dehydroergosterol peroxide), an important steroid from medicinal mushroom, exerts antitumor activity in several tumor types. 5,8-Epidioxyergosta-6,9(11),22-trien-3-ol inhibits HT29 cell growth by inducing CDKN1A expression, thus causing cell cycle arrest and apoptosis .
|
-
- HY-N2983
-
-
- HY-N0451R
-
-
- HY-N6939R
-
|
|
Structural Classification
Pinaceae
Terpenoids
Diterpenoids
Plants
|
HBV
Fungal
Apoptosis
Autophagy
Ferroptosis
|
|
Pseudolaric Acid B (Standard) is the analytical standard of Pseudolaric Acid B. This product is intended for research and analytical applications. Pseudolaric Acid B is a diterpene isolated from the root of Pseudolarix kaempferi (pinaceae), has anti-cancer, antifungal, and antifertile activities, and shows immunosuppressive activity on T lymphocytes . Pseudolaric Acid B inhibits hepatitis B virus (HBV) secretion through apoptosis and cell cycle arrest. Pseudolaric Acid B induces autophagy .
|
-
- HY-121222R
-
|
|
Structural Classification
other families
Terpenoids
Sesquiterpenes
Source classification
Plants
|
PI3K
Apoptosis
|
|
alpha-Bisabolol (Standard) is the analytical standard of alpha-Bisabolol. This product is intended for research and analytical applications. alpha-Bisabolol, an orally active sesquiterpene alcohol, induces cell cycle arrest, mitochondrial apoptosis and inhibition of PI3K/Akt signalling pathways. alpha-Bisabolol exerts a protective action against Cisplatin (HY-17394)-induced nephrotoxicity by mitigating inflammation and oxidative stress through the inhibition of NFκB activation. alpha-Bisabolol exhibits anti-inflammatory, analgesic, antibiotic and anticancer activities .
|
-
- HY-N2071R
-
|
|
Structural Classification
Cedrus deodara (Roxburgh) G. Don
Pinaceae
Terpenoids
Sesquiterpenes
Source classification
Plants
|
Cytochrome P450
Fungal
Apoptosis
Caspase
|
|
Cedrol (Standard) is the analytical standard of Cedrol. This product is intended for research and analytical applications. Cedrol is a potent competitive inhibitor of cytochrome P-450(CYP) enzyme. Cedrol plays an anticancer role by inducing cell cycle arrest and Caspase-dependent apoptosis. Cedrol acts as a neutrophil agonist that can desensitize cells to subsequent stimulation of N-formyl peptides. Cedrol prevents neuropathic pain caused by chronic contractile injury by inhibiting oxidative stress and inflammation. In addition, Cedrol has antibacterial, hair loss prevention and anti-anxiety properties.
|
-
- HY-N0202R
-
|
|
Structural Classification
Terpenoids
Sesquiterpenes
Source classification
Astragalus caprinus L.
Plants
Compositae
|
ERK
Apoptosis
p38 MAPK
Src
Akt
STAT
|
|
Atractylenolide II (Standard) is the analytical standard of Atractylenolide II. This product is intended for research and analytical applications. Atractylenolide II (Asterolide) is a sesquiterpenoid compound. Atractylenolide II can induce G1 phase cell cycle arrest and apoptosis in B16 melanoma cells. Atractylenolide II is an orally effective anticancer agent that can exert anti-melanoma effects by inhibiting the STAT3 signaling pathway. In addition, Atractylenolide II has been shown to ameliorate myocardial fibrosis, oxidative stress, and neuroprotective activity .
|
-
- HY-18981R
-
|
|
Structural Classification
Source classification
Coumarins
Phenylpropanoids
Umbelliferae
Plants
Echinacea angustifolia DC.
|
PKC
Apoptosis
CXCR
|
|
Decursin (Standard) is the analytical standard of Decursin. This product is intended for research and analytical applications. Decursin ((+)-Decursin) is a potent anti-tumor agent. Decursin also is a cytotoxic agent and a potent protein kinase C activator. Decursin induces apoptosis and cell cycle arrest at G1 phase. Decursin decreases the expression of CDK2, CDK4, CDK6, cyclin D1 protein at 48 h. Decursin inhibits cell proliferation and migration. Decursin shows anti-tumor, anti-inflammatory and analgesic activities [4].
|
-
- HY-N6714
-
-
- HY-128912
-
-
- HY-N6588
-
|
3,4,5-triCQA
|
Structural Classification
Classification of Application Fields
Simple Phenylpropanols
Source classification
Phenols
Polyphenols
Phenylpropanoids
Plants
Convolvulaceae
Inflammation/Immunology
Disease Research Fields
Ipomoea batatas (Linn.) Lamarck
|
Akt
NF-κB
|
|
3,4,5-Tricaffeoylquinic acid (3,4,5-triCQA) inhibits tumor necrosis factor-α-stimulated production of inflammatory mediators in keratinocytes via suppression of Akt- and NF-κB-pathways. 3,4,5-Tricaffeoylquinic acid induces cell cycle arrest at G0/G1, actin cytoskeleton organization, chromatin remodeling, neuronal differentiation, and bone morphogenetic protein signaling in human neural stem cells. 3,4,5-Tricaffeoylquinic acid has the potential for the research of aging-associated diseases .
|
-
- HY-N3387
-
-
- HY-N0711
-
|
Cymophenol
|
Structural Classification
Monophenols
Preservatives
Classification of Application Fields
Labiatae
Phenols
Plants
Inflammation/Immunology
Disease Research Fields
Food Research
|
Notch
Apoptosis
Fungal
Endogenous Metabolite
Bacterial
|
|
Carvacrol is an orally active monoterpenic phenol that can be extract from an abundant number of aromatic plants, including thyme and oregano, possessing antioxidant, antibacterial, antifungal, anticancer, anti-inflammatory, hepatoprotective, spasmolytic, and vasorelaxant properties. Carvacrol also causes cell cycle arrest in G0/G1, downregulates Notch-1, and Jagged-1, and induces apoptosis. Carvacrol is used in low concentrations as a food flavoring ingredient and preservative, as well as a fragrance ingredient in cosmetic formulations .
|
-
- HY-N4327
-
-
- HY-N6714R
-
|
|
Structural Classification
Microorganisms
Source classification
Phenols
Polyphenols
|
Topoisomerase
Androgen Receptor
Estrogen Receptor/ERR
Apoptosis
|
|
Alternariol (Standard) is the analytical standard of Alternariol. This product is intended for research and analytical applications. Alternariol is an orally ingested mycotoxin produced by Alternaria, capable of inhibiting the activity of topoisomerase I and II (topoisomerase I, topoisomerase II). Alternariol has weak estrogenic (Estrogen Receptor/ERR) and androgen/antiandrogen (Androgen Receptor) effects. Alternariol can induce apoptosis, trigger cell cycle arrest, suppress innate immune responses, and exhibit anti-tumor activity. Alternariol has genotoxic, mutagenic, and endocrine-disrupting effects .
|
-
- HY-N0711R
-
|
|
Structural Classification
Monophenols
Labiatae
Phenols
Plants
|
Notch
Apoptosis
Fungal
Endogenous Metabolite
Bacterial
|
|
Carvacrol (Standard) is the analytical standard of Carvacrol. This product is intended for research and analytical applications. Carvacrol is an orally active monoterpenic phenol that can be extract from an abundant number of aromatic plants, including thyme and oregano, possessing antioxidant, antibacterial, antifungal, anticancer, anti-inflammatory, hepatoprotective, spasmolytic, and vasorelaxant properties. Carvacrol also causes cell cycle arrest in G0/G1, downregulates Notch-1, and Jagged-1, and induces apoptosis. Carvacrol is used in low concentrations as a food flavoring ingredient and preservative, as well as a fragrance ingredient in cosmetic formulations .
|
-
- HY-N6871
-
|
|
Infection
Structural Classification
Colophony
Classification of Application Fields
Pinaceae
Ketones, Aldehydes, Acids
Metabolic Disease
Plants
Inflammation/Immunology
Disease Research Fields
|
Bacterial
IKK
Ferroptosis
|
Abietic acid, an orally active diterpene isolated from Colophony, displays significant anti-proliferative, anti-inflammatory, anti-obesity effect, bacteriostatic, cell cycle arresting and pro-apoptotic activities. Abietic acid inhibits lipoxygenase activity for allergy. Abietic acid enhances cell migration and tube formation in HUVECs. Abietic acid induces significant angiogenic potential, which is associated with upregulation of extracellular signal-regulated kinase (ERK) and p38 expression. Abietic acid attenuates sepsis-induced lung injury by inhibiting nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) pathway to inhibit M1 macrophage polarization. Abietic acid exhibits a positive effect against liver injury by attenuating inflammation and ferroptosis. Abietic acid shows accelerated wound closure in a mouse model of cutaneous wounds. Abietic acid significantly reduces the proliferation and growth of NSCLC cells by IKKβ inhibition.Additionally, Abietic acid ameliorates psoriasis-like inflammation and modulates gut microbiota in mice. Abietic acid is promising for research in non-small-cell lung cancer (NSCLC), liver injury-related deseases and psoriasis .
|
-
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-B0294S
-
|
|
|
Flubendazole-d3 is the deuterium labeled Flubendazole. Flubendazole is a safe and efficacious anthelmintic agent, which is widely used for anthelmintic to human, rodents and ruminants. Flubendazole exerts anticancer activities by mechanisms including inhibition of microtubule function. Flubendazole induces p53-mediated apoptosis and arrests G2/M cell cycle[1][2].
|
-
-
- HY-N1428S6
-
|
|
|
Citric acid-d4-1 is deuterated labeled Citric acid (HY-N1428) Citric acid is a natural preservative and food tartness enhancer. Citric acid induces apoptosis and cell cycle arrest at G2/M phase and S phase in HaCaT cells. Citric acid cause oxidative damage of the liver by means of the decrease of antioxidative enzyme activities. Citric acid causes renal toxicity in mice.
|
-
-
- HY-P10324
-
|
|
|
TAT-p16 (p16INK4a peptide) is a peptide mimic of p16INK4a that can induce an early G phase cell cycle arrest in the absence of active cyclin E:Cdk2 complex .
|
-
-
- HY-13629S1
-
|
|
|
Etoposide- 13C,d3 is the 13C- and deuterium labeled Etoposide. Etoposide (VP-16; VP-16-213) is an anti-cancer chemotherapy agent. Etoposide inhibits topoisomerase II, thus stopping DNA replication. Etoposide induces cell cycle arrest, apoptosis and autophagy[1].
|
-
-
- HY-13629S
-
|
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Etoposide-d3 (VP-16-d3) is the deuterium labeled Etoposide (HY-13629). Etoposide (VP-16) is an anti-cancer chemotherapy agent. Etoposide inhibits topoisomerase II, thus stopping DNA replication. Etoposide induces cell cycle arrest, apoptosis and autophagy .
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- HY-N1428S3
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Citric acid- 13C3 is the 13C labeled Citric acid[1]. Citric acid is a natural preservative and food tartness enhancer. Citric acid induces apoptosis and cell cycle arrest at G2/M phase and S phase in HaCaT cells. Citric acid cause oxidative damage of the liver by means of the decrease of antioxidative enzyme activities. Citric acid causes renal toxicity in mice[2][3][4].
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- HY-W654305
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Palbociclib-d4 is deuterium labeled Palbociclib. Palbociclib (PD 0332991) is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib has potent anti-proliferative activity and induces cell cycle arrest in cancer cells, which can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma .
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- HY-110382S
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13C20, 15N10-Cyclic di-GMP ( 13C20, 15N10-c-di-GMP) is 13C and 15N labeled Cyclic-di-GMP (disodium). Cyclic-di-GMP disodium is a STING agonist and a bacterial second messenger that coordinates different aspects of bacterial growth and behavior, including motility, virulence, biofilm formation, and cell cycle progression. Cyclic-di-GMP disodium has anti-cancer cell proliferation activity and also induces elevated CD4 receptor expression and cell cycle arrest. Cyclic-di-GMP disodium can be used in cancer research .
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- HY-12678S
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Entrectinib-d4 (NMS-E628-d4; RXDX-101-d4) is the deuterium labeled Entrectinib (HY-12678). Entrectinib is an orally active, BBB-penetrated and centrally active inhibitor of TrkA/B/C, ROS1 and ALK, with IC50 values of 1, 3, 5, 12 and 7 nM, respectively. Entrectinib induces apoptosis and cycle arrest in cancer cells, has antitumor activity, and attenuates bleomycin-induced lung fibrosis in mice .
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- HY-N7844S
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N6-Benzyladenosine-d5 (Benzyladenosine-d5) is deuterium labeled N6-Benzyladenosine. N6-Benzyladenosine is an adenosine receptor agonist, has a cytoactive activity. N6-Benzyladenosine arrests cell cycle at G0/G1 phase and induces cell apoptosis. N6-Benzyladenosine also exerts inhibitory effect on T. gondii adenosine kinase and glioma .
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- HY-W653896
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Alternariol-d2 is deuterium labeled Alternariol. Alternariol is an orally ingested mycotoxin produced by Alternaria, capable of inhibiting the activity of topoisomerase I and II (topoisomerase I, topoisomerase II). Alternariol has weak estrogenic (Estrogen Receptor/ERR) and androgen/antiandrogen (Androgen Receptor) effects. Alternariol can induce apoptosis, trigger cell cycle arrest, suppress innate immune responses, and exhibit anti-tumor activity. Alternariol has genotoxic, mutagenic, and endocrine-disrupting effects .
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- HY-12678S1
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Entrectinib-d8 (NMS-E628-d8; RXDX-101-d8) is a deuterated version of Entrectinib (HY-12678). Entrectinib (NMS-E628) is an orally available, blood-brain barrier permeable, central nervous system active TrkA/B/C, ROS1 and ALK inhibitor with IC50 values of 1, 3, 5, 12 and 12, respectively. 7 nM. Entrectinib induces apoptosis and cycle arrest in cancer cells, has anti-tumor activity, and also alleviates bleomycin-induced pulmonary fibrosis in mice .
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- HY-W032013S3
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1-Octanol-d5 is deuterated labeled Carvacrol (HY-N0711). Carvacrol is an orally active monoterpenic phenol that can be extract from an abundant number of aromatic plants, including thyme and oregano, possessing antioxidant, antibacterial, antifungal, anticancer, anti-inflammatory, hepatoprotective, spasmolytic, and vasorelaxant properties. Carvacrol also causes cell cycle arrest in G0/G1, downregulates Notch-1, and Jagged-1, and induces apoptosis. Carvacrol is used in low concentrations as a food flavoring ingredient and preservative, as well as a fragrance ingredient in cosmetic formulations .
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- HY-134061
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Alkynes
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Arecaidine propargyl ester hydrobromide is an agonist of M2 muscarinic acetylcholine receptors and has the activity of inhibiting tumor cell proliferation. The application of arecaidine propargyl ester hydrobromide has shown that it can reduce the number of ovarian cancer cells in vitro and induce apoptosis and the production of reactive oxygen species (ROS) at specific concentrations. Arecaidine propargyl ester hydrobromide can also arrest cells at the G2/M phase of the cell cycle and increase the percentage of abnormal mitosis. Arecaidine propargyl ester hydrobromide is more sensitizing to ovarian surface epithelial cells with higher M2 receptor levels than to cancer cells. Arecaidine propargyl ester hydrobromide exhibits the effect of lowering arterial blood pressure when interacting with the cardiovascular system in a natural physiological state, indicating its potential pharmacological application .
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- HY-159519
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Azide
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EGFR/HER2-IN-16 (compound 12K) is an effective dual-target inhibitor of EGFR (IC50=6.15 nM) and HER-2 (IC50=9.78 nM) with anti-tumor activity. EGFR/HER2-IN-16 can inhibit the migration of SK-BR-3 cells, arrest the cell cycle in the G0/G1 phase, and induce apoptosis. EGFR/HER2-IN-16 exhibits good anti-proliferative activity against tumor cell models and has little damage to healthy cells. EGFR/HER2-IN-16 can be used in breast cancer research .
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- HY-159147
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Azide
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SIAIS039 is an orally active c-ros oncogene 1 (ROS1)-specific PROTAC with DC50s of 154.46 nM, 126.47 nM, 143.69 nM for HCC78 cells, Ba/F3 expressing the CD74-ROS1 fusion and Ba/F3 expressing the SDC4-ROS1 fusion, respectively. SIAIS039 suppresses cell proliferation, induces cell cycle arrest and apoptosis, and inhibits clonogenicity against ROS1-positive cells. SIAIS039 demonstrates anti-tumour effects against ROS1-driven tumor growth vivo. SIAIS039 is composed of the ALK inhibitor Brigatinib (HY-12857), a linker EM-12 (HY-138793), and a VHL ligand E3 ubiquitin ligase 1-Butyne (Red: Brigatinib; Blue: VHL ligand; Black: linker) .
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- HY-N0623
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Tryptophan; Tryptophane
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Freeze-drying Protective Agents
Solubilizing Agents
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L-Tryptophan (Tryptophan) is an orally active and essential amino acid that is the precursor of serotonin, melatonin, and vitamin B3. L-Tryptophan can promote an increase in stemness and osteogenic ability of BMSCs in vitro and in vivo. L-Tryptophan inhibits cell proliferation and induced cell cycle arrest with high levels .
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- HY-115567
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1-(β-D-2-Deoxyribofuranosyl)-5-nitroindole
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Nucleosides and their Analogs
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5-NIdR (1-(β-D-2-Deoxyribofuranosyl)-5-nitroindole), an artificial nucleoside, exhibits the ability to inhibit the replication of DNA lesions generated by Temozolomide (HY-17364). 5-NIdR induces cancer cells apoptosis and arrests cell cycle at G0 phase. 5-NIdR enhances Temozolomide anti-tumor efficacy in murine glioblastoma model .
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