Search Result
Results for "
G0/G1 phase cell cycle arrest
" in MedChemExpress (MCE) Product Catalog:
1
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-N0837
-
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NSC17821; NSC23880
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PI3K
Akt
mTOR
Autophagy
Apoptosis
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Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
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Veratramine (NSC17821; NSC23880) is an orally active inhibitor of the PI3K/Akt/mTOR signaling pathway and a SIGMAR1 modulator. Veratramine induces autophagic apoptosis of tumor cells, arrests the cell cycle at the G0/G1 phase, and inhibits epithelial-mesenchymal transition (EMT)-related proteins to reduce tumor migration. Veratramine reduces spinal cord and sciatic nerve pathological damage in a neuropathy model by inhibiting SIGMAR1 binding to NMDAR and phosphorylation of NMDAR Ser896. Veratramine has anti-tumor proliferation, apoptosis induction, anti-inflammatory and neuroprotective activities, and can be used in the study of cancers such as liver cancer and osteosarcoma, as well as diabetic peripheral neuropathy .
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-
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- HY-13768
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Topotecan
Maximum Cited Publications
38 Publications Verification
SKF 104864A; NSC 609669
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Topoisomerase
Autophagy
Apoptosis
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Cancer
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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 .
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-
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- HY-15221
-
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Apoptosis
Histone Demethylase
MDM-2/p53
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Cardiovascular Disease
Cancer
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Methylstat is a potent histone demethylases inhibitor. Methylstat shows anti-proliferative activity with low cytotoxicity. Methylstat induces apoptosis and cell cycle arrest at G0/G1 phase. Methylstat increases the expression of p53 and p21 protein levels. Methylstat inhibits angiogenesis induced by various cytokines. Methylstat can be used as a chemical probe for addressing its role in angiogenesis .
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-
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- HY-B1165
-
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p38 MAPK
Checkpoint Kinase (Chk)
Histamine Receptor
5-HT Receptor
CDK
PARP
Apoptosis
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Cancer
|
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Cyproheptadine hydrochloride sesquihydrate acts as a p38 MAP kinase activator, CHK2 activator, histamine H1 receptor inhibitor and serotonin receptor inhibitor. Cyproheptadine hydrochloride sesquihydrate mediates cell cycle arrest via G1 phase arrest, G1/S transition arrest, G0/G1 phase arrest, reduced expression of cyclins D1/D2/D3, upregulated expression of HBP1, p16, p21, p27, and decreased phosphorylation of retinoblastoma protein. Cyproheptadine hydrochloride sesquihydrate induces Apoptosis by increasing PARP and cleaved PARP, as well as activating the mitochondrial caspase pathway. Cyproheptadine hydrochloride sesquihydrate inhibits tumor growth with extremely low toxicity to normal cells. Cyproheptadine hydrochloride sesquihydrate can be used in research related to hepatocellular carcinoma, multiple myeloma and acute myeloid leukemia .
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- HY-131906
-
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JAK
FLT3
Apoptosis
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Cancer
|
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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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-
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- HY-17026E
-
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dFdCTP trisodium
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Drug Metabolite
DNA/RNA Synthesis
Apoptosis
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Cancer
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Gemcitabine triphosphate (dFdCTP) trisodium is the active metabolite of Gemcitabine (HY-17026). The mechanism of Gemcitabine triphosphate trisodium cell-killing is its competition with cytidine triphosphate during DNA replication, which results in the inhibition of chain elongation. Gemcitabine triphosphate trisodium shows a Ki of 11.2 μM against DNA polymerase α and 14.4 μM against DNA polymerase ε. Gemcitabine triphosphate trisodium partially inhibits dCMP deaminase and acts as a substrate for DNA synthesis to incorporate into cellular DNA and RNA. Gemcitabine triphosphate trisodium disrupts DNA and RNA synthesis, arrests cell cycle in G0/G1 and S phases, triggers apoptosis, reduces tumor cell proliferation. Gemcitabine triphosphate trisodium can be used for the research of pancreatic cancer and non-small cell lung cancer .
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-
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- HY-N7844
-
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Benzyladenosine
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Apoptosis
Adenosine Receptor
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Inflammation/Immunology
Cancer
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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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-
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- HY-15485
-
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Phosphodiesterase (PDE)
Apoptosis
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Inflammation/Immunology
Cancer
|
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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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-
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- HY-N0440
-
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Influenza Virus
NF-κB
5 alpha Reductase
Keap1-Nrf2
Lactate Dehydrogenase
Apoptosis
|
Infection
Neurological Disease
Inflammation/Immunology
Endocrinology
Cancer
|
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Germacrone is a sesquiterpene compound with multiple biological activities. Germacrone inhibits the H1N1 and H3N2 influenza A virus and the influenza B virus. Germacrone blocks the progressionof arthritis by regulating Th1/Th2 balance and inhibiting NF-κB signaling. Germacrone can arrest the cell cycle at G0/G1 and G2/M phases and induce apoptosis in breast cancer cells. Germacrone inhibits 5α-reductase and has anti-androgenic effect. Germacrone has neuroprotective functions and can be used for the study of traumatic brain injury (TBI). Germacrone also has antioxidant activity .
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-
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- HY-17026A
-
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dFdCTP
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Drug Metabolite
DNA/RNA Synthesis
Apoptosis
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Cancer
|
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Gemcitabine triphosphate (dFdCTP) is the active metabolite of Gemcitabine (HY-17026). The mechanism of Gemcitabine triphosphate cell-killing is its competition with cytidine triphosphate during DNA replication, which results in the inhibition of chain elongation. Gemcitabine triphosphate shows a Ki of 11.2 μM against DNA polymerase α and 14.4 μM against DNA polymerase ε. Gemcitabine triphosphate partially inhibits dCMP deaminase and acts as a substrate for DNA synthesis to incorporate into cellular DNA and RNA. Gemcitabine triphosphate disrupts DNA and RNA synthesis, arrests cell cycle in G0/G1 and S phases, triggers apoptosis, reduces tumor cell proliferation. Gemcitabine triphosphate can be used for the research of pancreatic cancer and non-small cell lung cancer .
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- HY-114414
-
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HDAC
mTOR
Apoptosis
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Cancer
|
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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-124211
-
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Environmental Pollutants
MDM-2/p53
Aryl Hydrocarbon Receptor
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Cancer
|
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Dibenzo (a,i) pyrene is a polycyclic aromatic hydrocarbon and also a carcinogenic ligand of the TCDD (Ah) receptor. Dibenzo (a,i) pyrene binds to the TCDD (Ah) receptor in rat liver. Dibenzo (a,i) pyrene induces DNA adduct formation and upregulates the protein levels of p53 and p21 WAF1 in diploid lung fibroblasts. Dibenzo (a,i) pyrene alters the cell cycle distribution of diploid lung fibroblasts, increasing the proportion of cells in the S phase, decreasing the proportions of cells in the G0/G1 and G2/M phases, and causing S phase delay/arrest. Dibenzo (a,i) pyrene is applicable for cancer research .
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- HY-10815
-
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Sigma Receptor
Apoptosis
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Neurological Disease
Cancer
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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 .
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- HY-173557
-
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Histone Methyltransferase
Apoptosis
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Cancer
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PRMT7-IN-2 (A33) is a selective PRMT7 inhibitor with an IC50 of 0.50 μM. PRMT7-IN-2 arrests cell cycle at G0/G1 phase, induces cell apoptosis, and inhibits cell growth in vivo and in vitro. PRMT7-IN-2 decreases the monomethylarginine level of PRMT7, increases expression of epithelial marker (E-cadherin, and reduces expression of mesenchymal markers such as N-cadherin, Vimentin, and ZEB2 .
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- HY-174371
-
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Molecular Glues
Casein Kinase
MDM-2/p53
MALT1
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Neurological Disease
Cancer
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INNO-220 is an orally active, CRBN-dependent molecular glue degrader targeting CK1α. INNO-220 induces cell cycle arrest at G0/G1 phase and triggers apoptosis by degrading CK1α. INNO-220 disrupts the assembly and function of the CARD11/BCL10/MALT1 complex, thereby inhibiting NF-κB signaling in stimulated T cells and lymphoma cells that harbor an activating mutation in CARD11. INNO-220 provides a new direction for lymphoma research.
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- HY-N1930
-
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Hinesol
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Apoptosis
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Cancer
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(-)-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 .
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- HY-149891
-
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HSP
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Cancer
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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 .
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-
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- HY-149132
-
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DDA
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LXR
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Cancer
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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 .
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- HY-164384
-
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PI3K
Akt
mTOR
Apoptosis
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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-174129
-
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Btk
Apoptosis
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Cancer
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TM471-1 is an orally active and covalent Bruton's tyrosine kinase (BTK) inhibitor with IC50 values of 1.3 nM (BTK WT), >40,000 nM (BTK C481S), 7.9 nM (TEC) and 12.4 nM (TXK). TM471-1 inhibits cell growth in vivo and in vitro, arrests cell cycle at G0/G1 phase and induces cell apoptosis .
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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-N16567
-
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Apoptosis
Caspase
PARP
Survivin
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Cancer
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Acrofolione A is an acetophenone dimer isolated from Acronychia pendunculata with anticancer effects. Acrofolione A induces G0/G1 phase cell cycle arrest and apoptosis in human NALM-6 pre-B cell leukaemia cells. Acrofolione A can be used for leukaemia research .
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- HY-144733
-
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Estrogen Receptor/ERR
Apoptosis
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Cancer
|
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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 .
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- HY-10638
-
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c-Kit
Apoptosis
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Cancer
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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 .
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- HY-129592
-
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Apoptosis
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Cancer
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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 .
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- HY-N12044
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Apoptosis
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Cancer
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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 .
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- HY-122359A
-
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rel-L-Centchroman; Ormeloxifene
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Estrogen Receptor/ERR
Apoptosis
Reactive Oxygen Species (ROS)
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Cancer
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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 .
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- HY-163535
-
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HDAC
DNA Methyltransferase
Apoptosis
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Inflammation/Immunology
Cancer
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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) .
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- HY-168205
-
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HSP
Apoptosis
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Cancer
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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 .
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- HY-115906
-
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FLT3
MNK
Apoptosis
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Cancer
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K783-0308 is a potent and selective dual inhibitor of FLT3 and MNK2 with IC50 values of 680 and 406 nM, respectively. K783-0308 inhibits the growth of MOLM-13 (IC50=10.5 µM) and MV-4-11 (IC50=10.4 µM) cells. K783-0308 promotes acute myeloid leukemia (AML) cell apoptosis and cell cycle arrests in the G0/G1 phase .
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- HY-179124
-
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Apoptosis
Caspase
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Cancer
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Apoptosis inducer 52 is a derivative of flutamide that induces apoptosis in prostate cancer cells. Apoptosis inducer 52 promotes apoptosis by activating both intrinsic and extrinsic apoptotic pathways, without generating reactive oxygen species (ROS). Apoptosis inducer 52 triggers caspase 3/7 activity and the externalization of phosphatidylserine, leading to cell cycle arrest at the G0/G1 phase. Apoptosis inducer 52 can be used for the research of androgen receptor (AR)-dependent and -independent prostate cancers and leukemia .
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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-178350
-
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CDK
HDAC
Apoptosis
Histamine Receptor
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Cancer
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MFDCH016 is a potent HDAC1/6 (IC50 = 38/59 nM) and CDK4/6 (IC50 = 680/720 nM) inhibitor. MFDCH016 induces apoptosis and cell cycle arrest in G2/M and G0/G1 phases in MCF-7 cells. MFDCH016 can modulate the HDAC-p21-CDK signaling pathway, increasing the levels of acetylated H3 and p21. MFDCH016 can be used for the study of breast cancer .
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- HY-178941
-
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Dihydroorotate Dehydrogenase
Apoptosis
Caspase
Reactive Oxygen Species (ROS)
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Cancer
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DHODH-IN-32 (Compound A1) is a DHODH inhibitor. DHODH-IN-32 shows significant cytotoxicity against NCI-60 cell lines, especially being sensitive to breast cancer, prostate cancer and leukemia cell lines. DHODH-IN-32 can induce cell apoptosis by activating the Caspase pathway. DHODH-IN-32 causes G0/G1 phase cell cycle arrest and inhibits cellular metabolism by ROS. DHODH-IN-32 exhibits significant anti-tumor properties in mouse breast cancer models. DHODH-IN-32 can be used for the study of breast cancer .
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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-159897
-
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PAK
LIM Kinase (LIMK)
Apoptosis
Reactive Oxygen Species (ROS)
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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-13768C
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SKF 104864A hydrochloride hydrate; NSC 609669 hydrochloride hydrate
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Topoisomerase
Apoptosis
Autophagy
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Cancer
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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 .
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- HY-162416
-
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CDK
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Cancer
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CDK7-IN-27 (Compound 37) is a selective inhibitor for cyclin-dependent kinase 7 (CDK7), with Ki of 3 nM. CDK7-IN-27 arrests the cell cycle at G0/G1 phase .
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- HY-145762
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Apoptosis
Histone Methyltransferase
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Cancer
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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 .
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- HY-149063
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Apoptosis
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Cancer
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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 .
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- HY-155544
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c-Met/HGFR
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Cancer
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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 .
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- HY-147801
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Topoisomerase
Apoptosis
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Cancer
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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 .
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- HY-155503
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Apoptosis
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Cancer
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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 .
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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-163722
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EGFR
Dihydrofolate reductase (DHFR)
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Cancer
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EGFR/DHFR-IN-1 (Compound 10e) is a dual inhibitor of EGFR and DHFR with IC50s of 0.151 and 0.541 µM, respectively. EGFR/DHFR-IN-1 arrests the cell cycle at both G0-G1 and S phases .
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- HY-165064
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L-Erythro cer(d18:1/2:0); N-Acetyl-L-erythro-sphingosine; Acetyl-L-erythro-sphingosine
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Apoptosis
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Cancer
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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 .
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- HY-170323
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Apoptosis
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Cancer
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4-TM.P binds to the minor groove of DNA, inhibits proliferation of cancer cell K562 with an IC50 of 25 µM, arrests the cell cycle at G0/G1 phase, and induces apoptosis in cell K562. 4-TM.P can be used in anti-leukemia research .
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- HY-146040
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Apoptosis
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Cancer
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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 .
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- HY-146063
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Apoptosis
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Cancer
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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 .
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- HY-P11173
-
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DNA Alkylator/Crosslinker
Apoptosis
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Cancer
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Cr-ACP1 is an anti-cancerous peptide. Cr-ACP1 binds to DNA, inducing cell cycle arrest in the G0-G1 phase, leading to the initiation of Apoptosis mechanisms. Cr-ACP1 exhibits anticancer effects against colon cancer and epidermoid carcinoma .
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- HY-170558
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FLT3
Apoptosis
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Cancer
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FW-1 is a type I inhibitor for FLT3 with IC50 of ca. 1 μM. FW-1 exhibits cytotoxicity in FLT3 mutated AML cell. FW-1 arrests the cell cycle at G0/G1 phase, and induces apoptosis in cell MV4-11 and MOLM-13 .
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- HY-159101
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EGFR
PD-1/PD-L1
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Cancer
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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 .
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- HY-168559
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EGFR
Apoptosis
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Cancer
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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 .
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- HY-174151
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Topoisomerase
Apoptosis
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Cancer
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XSJ110 is a potent irreversible topoisomerase I (Topo I) inhibitor with an IC50 value of 0.133 μM. XSJ110 blocks DNA topoisomerization, induces DNA double-strand breaks, and triggers cell cycle arrest at G0/G1 phase, inducing tumor cell apoptosis. XSJ110 is promising for research of ampullary carcinoma (AC) .
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- HY-162755
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SHP2
Apoptosis
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Cancer
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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 .
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- HY-157814
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Apoptosis
Epigenetic Reader Domain
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Cancer
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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 .
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- HY-110293
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FLT3
Apoptosis
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Cancer
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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-149735
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Epigenetic Reader Domain
Apoptosis
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Cancer
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BET-IN-20 (compound 10) is an inhibitor of BRD4 BD1 (IC50=1.9 nM) with anticancer activity. BET-IN-20 can promote acute myeloid leukemia (AML) cell apoptosis and arrest the cell cycle in the G0/G1 phase. BET-IN-20 also inhibits c-Myc and CDK6 and enhances PARP cleavage .
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- HY-162868
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c-Met/HGFR
HDAC
Apoptosis
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Cancer
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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-168605
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MMP
Apoptosis
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Cancer
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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 .
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- HY-N3764
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Akt
Dihydrofolate reductase (DHFR)
Endogenous Metabolite
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Others
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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-170792
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Histone Methyltransferase
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Cancer
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PRMT5-IN-48 (compound D3) is an orally effective PRMT5 inhibitor (IC50=20.7 nM) with anticancer activity. PRMT5-IN-48 can inhibit the growth of various cancer cells, induce apoptosis (apoptosis), and arrest the cell cycle at the G0/G1 phase. PRMT5-IN-48 can be used for non-Hodgkin lymphoma (NHL) research .
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- HY-170382
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Estrogen Receptor/ERR
Apoptosis
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Cancer
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ER covalent antagonist-1 (Compound 39D) is the antagonist for estrogen receptor α (ERα). ER covalent antagonist-1 inhibits the proliferation of ERα-positive cell MCF-7 with an IC50 of 0.98 μM, arrests the cell cycle at G0/G1 phase, and induces apoptosis. ER covalent antagonist-1 exhibits antitumor efficacy in mouse model .
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- HY-163894
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Apoptosis
HDAC
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Cancer
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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-159149
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Reactive Oxygen Species (ROS)
Apoptosis
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Cancer
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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-123486
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Apoptosis
Bcr-Abl
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Cancer
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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-151630
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Carbonic Anhydrase
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Cancer
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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 .
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- HY-176066A
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c-Myc
Apoptosis
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Cancer
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c-Myc inhibitor 16 iodide (Compound W11) is a selective c-Myc G-quadruplex (c-Myc G4) inhibitor. c-Myc inhibitor 16 iodide inhibits the transcription and translation of the c-Myc gene, disrupts the tumor cell cycle, arrests cell growth in the G0/G1 phase and activates the mitochondrial apoptosis pathway to induce early apoptosis of cancer cells. c-Myc inhibitor 16 iodide is promising for research of breast cancer .
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-
- HY-168072
-
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Interleukin Related
Apoptosis
Autophagy
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Cancer
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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 .
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-
- HY-162936
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FLT3
Apoptosis
|
Cancer
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|
SILA-123 is a FLT3 inhibitor (FLT3-WT: IC50=2.1 nM; FLT3-ITD: IC50=1.0 nM). SILA-123 inhibits FLT3 phosphorylation and downstream signaling pathways, leading to apoptosis by arresting cell cycle progression at the G0/G1 phase. SILA-123 can be used in the study of acute myeloid leukemia .
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-
- HY-169408
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Cytochrome P450
EGFR
Apoptosis
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Cancer
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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-146442
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Raf
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Cancer
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BRAF V600E/CRAF-IN-1 (Compound 8b) is a potent inhibitor of BRAF V600E/CRAF. BRAF V600E/CRAF-IN-1 triggers apoptosis and cell cycle arrest at G0/G1 phase in HCT-116 colon cancer cell. BRAF V600E/CRAF-IN-1 has the potential for the research of cancer diseases .
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- HY-172092
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Apoptosis
Ferroptosis
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Cancer
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BG11 induces the accumulation of Fe 2+ and intracellular lipid peroxides, induces ferroptosis. BG11 regulates the expression of Bax and Bcl-2 proteins, and induces apoptosis in MDA-MB-231 cell. BG11 arrests the cell cycle at G0/G1 and S phase, inhibits the proliferation of TNBC cancer cell (IC50 for MDA-MB-231 and BT549 is 0.49 μM and 0.52 μM), and inhibits the cell migration and invasion. BG11 exhibits antitumor efficacy in mouse models .
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- HY-162456
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Apoptosis
Reactive Oxygen Species (ROS)
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Cancer
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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 .
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- HY-N7844S
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Benzyladenosine-d5
|
Isotope-Labeled Compounds
Apoptosis
Adenosine Receptor
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Inflammation/Immunology
Cancer
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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-143246
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EGFR
Apoptosis
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Cancer
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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-146443
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Raf
|
Cancer
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|
BRAF V600E/CRAF-IN-2 (Compound 9c) is a potent inhibitor of BRAF V600E/CRAF with IC50s of 0.888 and 0.229 μM, respectively. BRAF V600E/CRAF-IN-2 triggers apoptosis and cell cycle arrest at G0/G1 phase in HCT-116 colon cancer cell. BRAF V600E/CRAF-IN-2 has the potential for the research of cancer diseases .
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-
- HY-158138
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PARP
Topoisomerase
Apoptosis
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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-161966
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Apoptosis
Reactive Oxygen Species (ROS)
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-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-168858
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Trk Receptor
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Cancer
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|
TRK-IN-30 (Compound C11) is the inhibitor for tropomyosin receptor kinase (TRK) that inhibits TRKA, TRKB and TRKC and drug resistant mutant TRKA G595R with an IC50 of 1.8, 0.98, 3.8, and 54 nM, respectively. TRK-IN-30 inhibits the activation of the downstream PI3K/AKT and MEK/ERK signaling pathways. TRK-IN-30 inhibits the colony formation and cell migration of Km-12, arrests the cell cycle at G0/G1 phase, and induces apoptosis in Km-12 .
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- HY-173558
-
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PD-1/PD-L1
HDAC
Apoptosis
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Cancer
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|
PD-L1/HDAC3-IN-1 (PH3) is a dual PD-L1/HDAC3 Inhibitor with IC50 values of 89.4 nM and 107 nM for PD-1/PD-L1 and HDAC3, respectively. PD-L1/HDAC3-IN-1 induces cell apoptosis and arrests cell cycle at G0/G1 phase. PD-L1/HDAC3-IN-1 shows anticancer activity both in vivo and in vitro .
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-
- HY-170640
-
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FLT3
Reactive Oxygen Species (ROS)
Apoptosis
|
Cancer
|
|
FLT3-IN-29 (Compound MY-10) is a FLT3 inhibitor (IC50s: 6.5 and 10.3 nM for FLT3-ITD and FLT3-D835Y mutants). FLT3-IN-29 arrests cell cycle at the G0/G1 phase and efficiently induces Apoptosis. FLT3-IN-29 also reduces reactive oxygen species (ROS) production and mitochondrial membrane potential (MMP). FLT3-IN-29 displays antileukemic activity .
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-
- HY-130624
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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-161694
-
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DNA Methyltransferase
|
Cancer
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|
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 .
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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-159519
-
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|
Apoptosis
EGFR
|
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-169170
-
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|
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-105414
-
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Drug Derivative
|
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 .
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-
- HY-N18190
-
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NF-κB
Apoptosis
|
Cancer
|
|
N-Desmethyldauricine is a NF-κB p65 inhibitor and apoptosis inducer. N-Desmethyldauricine reduces the protein expression level of p65, induces apoptosis, arrests the cell cycle at the G0/G1 phase, attenuates intercellular adhesion, and inhibits the growth of 3D spheroids of triple-negative breast cancer. N-Desmethyldauricine can be used in studies related to triple-negative breast cancer .
|
-
- HY-115797
-
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MDM-2/p53
Caspase
c-Myc
Apoptosis
NF-κB
|
Cancer
|
|
LQFM030 is a novel small molecule MDM2 inhibitor. LQFM030 exhibits concentration dependent cytotoxicity in K562 cells (IC50 = 0.28 mM). LQFM030 induces cell apoptosis through G0/G1 phase cell cycle arrest and increased Caspase activity. LQFM030 downregulates the mRNA expression of MDM2, MDMX, p73, MYC, and NF-κB. LQFM030 is commonly used in research on cancers such as leukemia .
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-
- HY-183262
-
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Parasite
Reactive Oxygen Species (ROS)
|
Infection
|
|
Antileishmanial agent-40 is an orally active and selective antileishmanial agent. Antileishmanial agent-40 elevates intracellular reactive oxygen species (ROS) levels in Leishmania donovani promastigotes. Antileishmanial agent-40 induces cell cycle arrest at the sub-G0/G1 phase in Leishmania donovani promastigotes, indicative of programmed-like parasite death. Antileishmanial agent-40 can be used for the research of leishmaniasis .
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-
- HY-173118
-
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|
EGFR
Apoptosis
|
Cancer
|
|
EGFR-IN-152 (compound D4) is a potent EGFR tyrosine kinase inhibitor, exhibiting potent EGFR L858R/T790M/C797S inhibition activity (IC50 = 40 nM). EGFR-IN-152 induces G0/G1 phase cell cycle arrest and apoptosis, thereby inhibiting colony formation and cell proliferation of non-small cell lung cancer (NSCLC) cells. EGFR-IN-152 can be used for NSCLC research .
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-
- HY-N7844R
-
|
Benzyladenosine (Standard)
|
Apoptosis
Adenosine Receptor
Phytohormone
Reference Standards
|
Inflammation/Immunology
Cancer
|
|
N6-Benzyladenosine (Standard) (Benzyladenosine (Standard)) is the analytical standard of N6-Benzyladenosine (HY-N7844). This product is intended for research and analytical applications. 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-180782
-
|
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DNA/RNA Synthesis
Reactive Oxygen Species (ROS)
Caspase
Apoptosis
|
Cancer
|
|
Triphenyltin(IV) diisopropyl dithiocarbamate (Compound OC2) is an anti-leukemia agent. Triphenyltin(IV) diisopropyl dithiocarbamate exhibits extremely strong cytotoxicity towards Jurkat cells, with an IC₅₀ value of 0.1 μM. Triphenyltin(IV) diisopropyl dithiocarbamate causes DNA damage, which subsequently leads to mitochondrial dysfunction, a large amount of ROS production, and ultimately results in the activation of the mitochondrial apoptosis pathway (involving the activation of Caspase-9/-3) and the G0/G1 phase cell cycle arrest, all of which jointly lead to the death of leukemia cells .
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-
- HY-183364
-
-
- HY-183297
-
|
|
CDK
|
Cancer
|
|
CDK4-IN-5 is a potent, orally active and selective CDK4 inhibitor. CDK4-IN-5 suppresses CDK4 expression and downregulates the CDK4/CyclinD1 complex. CDK4-IN-5 induces G0/G1 phase cell cycle arrest in bladder cancer cells via CyclinD1 expression suppression. CDK4-IN-5 selectively exerts activity against bladder cancer cells. CDK4-IN-5 can be used for the research of bladder cancer .
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-
- HY-182447
-
|
DL111-IT
|
CDK
Apoptosis
|
Endocrinology
Cancer
|
|
Contragestazol (DL111-IT) is a non-hormonal antifertility agent. Contragestazol reduces the expression of Cyclin D1 and CDK4, increases the expression of total retinoblastoma protein (pRb), and decreases the level of hyperphosphorylated pRb. Contragestazol induces G0/G1 phase cell cycle arrest. Contragestazol inhibits embryonic development by inducing luteal cell apoptosis and reducing intrauterine polyamine levels. Contragestazol exhibits antitumor activity against prostate cancer, S180 tumor and H22 tumor. Contragestazol shows extremely potent activity in terminating early pregnancy in animals .
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-
- HY-186045
-
|
|
Histone Methyltransferase
Apoptosis
DNA/RNA Synthesis
ATP-binding cassette (ABC) transporters
|
Cancer
|
|
SKLB06489 is a selective and orally active inhibitor of type I PRMT enzymes, with IC50 values of 64.55 nM (PRMT1), 4.21 nM (PRMT6), and 51.27 nM (PRMT8). SKLB06489 inhibits cell proliferation, colony formation, DNA replication, and DNA damage repair in cancer cells. SKLB06489 induces G0/G1-phase cell cycle arrest and apoptosis in cancer cells. SKLB06489 enhances intracellular cholesterol efflux via ABCA1 and ABCG1 upregulation, disrupts cholesterol metabolic homeostasis, and suppresses tumor growth in subcutaneous xenograft models. SKLB06489 can be used for the research of triple-negative breast cancer (TNBC) .
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-
- HY-181954
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
ZW-49 is an orally active pan-EGFR inhibitor with IC50 values at 0.03-1.5 nM. ZW-49 inhibits all subgroups of EGFR mutations with selectivity over wild-type EGFR and other target families. ZW-49 blocks the ATP-binding pocket, occupies a conserved hydrophobic subpocket, avoids steric conflicts with PACC mutation P loops. ZW-49 inhibits cancer cells proliferation, induces G0/G1 phase cell-cycle arrest and apoptosis, and demonstrates anti-proliferative activity in xenograft mice models. ZW-49 can be used for the research of cancer, such as non-small cell lung cancer .
|
-
- HY-123450
-
|
|
Bcr-Abl
Apoptosis
PDGFR
|
Cancer
|
|
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-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-152263
-
|
|
Hsp-targeting Chimeras
CDK
Apoptosis
|
Cancer
|
|
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.
|
-
- HY-179151
-
|
|
CDK
Reactive Oxygen Species (ROS)
SOD
|
Cancer
|
|
CDK4/6-IN-26 is a carbamate derivative that targets CDK4/CDK6. CDK4/6-IN-26 reduces CDK4/CDK6 levels, resulting in cell cycle arrest in the G0/G1 phase and in the S phase. CDK4/6-IN-26 exhibits high potency against SW480 cells (IC50 = 6.3 μM). CDK4/6-IN-26 affects ROS levels by increasing the expression of SOD2/MnSOD. CDK4/6-IN-26 establishes several interactions with the amino acids of the CDK6 active site. CDK4/6-IN-26 can be used for the research of colorectal cancer .
|
-
- HY-170978
-
|
|
PROTACs
CDK
|
Cancer
|
|
PROTAC CDK9 degrader-11 (Compound C3) is an orally active PROTAC degrader for CDK9 with DC50 of 1.09 nM. PROTAC CDK9 degrader-11 exhibits cytotoxicity in multi small cell lung cancer cell with IC50 of nanomolar levels. PROTAC CDK9 degrader-11 arrests cell cycle at G0/G1 phase, inhibits the cell invasion in DMS114 and DMS53 cell. PROTAC CDK9 degrader-11 exhibits antitumor efficacy in NCI-H446 xenograft mouse models .(Pink: ligand for target protein CDK9 ligand 3 (HY-170979); Black: linker; Blue: ligand for E3 ligase Cereblon E3 ligase Ligand 56 (HY-W247437))
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-
- HY-Y0106
-
|
|
mTOR
Xanthine Oxidase
Apoptosis
|
Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
|
|
2,6-Dihydroxyacetophenone, a polyphenolic derivative of Acetophenone (HY-Y0989), is an orally active mTOR inhibitor. 2,6-Dihydroxyacetophenone shows antioxidant activity. 2,6-Dihydroxyacetophenone inhibits cell growth and proliferation in CRC cells. 2,6-Dihydroxyacetophenone arrests at G0/G1 phase of cell cycle, induces apoptosis and suppresses cell migration in CRC cells. 2,6-Dihydroxyacetophenone inhibits xanthine oxidase (XOD) with an IC50 of 1.24 mM. 2,6-dihydroxyacetophenone improves uric acid metabolism in hyperuricemia mice, reduces plasma cholesterol in hypercholesterolemic rats, and inhibits lipid accumulation in HFD-induced obese mice. 2,6-Dihydroxyacetophenone can be used for the study of colorectal cancer (CRC), hyperuricemia and hypercholesterolemia .
|
-
- HY-175849
-
|
|
HyT
Anaplastic lymphoma kinase (ALK)
Apoptosis
STAT
|
Cancer
|
|
ALK degrader 1 is a potent, hydrophobic tag (HyT)-based degrader that induces ubiquitin-proteasome system (UPS)-dependent EML4-ALK degradation (DC50 = 0.13 μM). ALK degrader 1 demonstrates potent ALK degradation and antiproliferative effects in ALK-dependent cell lines, while showing minimal cytotoxicity in ALK fusion-negative cells. ALK degrader 1 triggers cell cycle arrest at the G0/G1 phase and stimulates apoptosis. ALK degrader 1 not only facilitates efficient degradation of the ALK protein but also disrupts key downstream effectors, including the STAT3 signaling axis. ALK degrader 1 mediates robust EML4-ALK degradation in vivo. ALK degrader 1 can be used for ALK-related diseases research .
|
-
- HY-124273
-
|
L-threo Cer(d18:1/2:0); L-threo Ceramide (d18:1/2:0); N-acetyl-L-threo-Sphingosine
|
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.
|
-
- HY-175542
-
|
|
STAT
Apoptosis
Reactive Oxygen Species (ROS)
PARP
|
Cancer
|
KB-15 is a STAT3 inhibitor. KB-15 exhibits potent anti-proliferative activity against AGS gastric cancer cells (IC50 = 0.29 μM) and BGC-823 gastric cancer cells (IC50 = 0.65 μM). KB-15 exerts anti-tumor effects by inhibiting STAT3 phosphorylation, downregulating HO-1 expression, and promoting intracellular ROS accumulation. KB-15 induces G0/G1 phase cell cycle arrest and apoptosis, as well as suppresses colony formation and migration of gastric cancer cells. KB-15 demonstrates excellent anti-tumor efficacy in BGC-823 subcutaneous xenograft model. KB-15 can be used for the study of gastric cancer .
|
-
- HY-175298
-
|
|
STAT
Src
Apoptosis
|
Cancer
|
|
STAT-3/c-Src-IN-1 (Compound 12d) is a dual STAT-3 (IC50=0.844 μM) and c-Src (IC50=0.268 μM) inhibitor. STAT-3/c-Src-IN-1 blocks tumor cell proliferation, migration, and angiogenesis signaling pathways. STAT-3/c-Src-IN-1 exhibits potent anti-proliferative activity against melanoma (SK-MEL-2) and CNS cancer (SNB-75) cell lines (GI50=-5.75 μM and -5.63 μM), inducing tumor cell apoptosis via G0/G1 and G2/M phase cell cycle arrest. STAT-3/c-Src-IN-1 is promising for research of melanoma and glioblastoma .
|
-
- HY-168962
-
|
|
HDAC
Apoptosis
Autophagy
Reactive Oxygen Species (ROS)
Mitochondrial Metabolism
Parasite
|
Infection
Cancer
|
|
HDAC-IN-88 (Compound HJ-9) is the inhibitor for HDAC that inhibits HDAC6, HDAC1, HDAC2, HDAC8 and HDAC3 with IC50s of 0.226, 1.103, 2.308, 3.255 and 3.864 μM, respectively. HDAC-IN-88 inhibits the proliferation of cancer cell HepG2, HCT116 and MV4-11 with IC50 of 5.47, 9.78 and 0.38 μM, inhibits the migration of HCT116, arrests the cell cycle at G0/G1 phase, and induces apoptosis and autophagy in MV4-11. HDAC-IN-88 reduces ROS level and mitochondrial membrane potential. HDAC-IN-88 exhibits antimalarial activity that inhibits P. falciparum 3D7 with EC50 of 165 nM. HDAC-IN-88 also exhibits anti-angiogenic activity .
|
-
- HY-N0837R
-
|
NSC17821 (Standard); NSC23880 (Standard)
|
Reference Standards
PI3K
Akt
mTOR
Autophagy
Apoptosis
|
Neurological Disease
Metabolic Disease
Cancer
|
|
Veratramine (NSC17821; NSC23880) (Standard) is the analytical standard of Veratramine (HY-N0837). This product is intended for research and analytical applications. Veratramine (NSC17821; NSC23880) is an orally active inhibitor of the PI3K/Akt/mTOR signaling pathway and a SIGMAR1 modulator. Veratramine induces autophagic apoptosis of tumor cells, arrests the cell cycle at the G0/G1 phase, and inhibits epithelial-mesenchymal transition (EMT)-related proteins to reduce tumor migration. Veratramine reduces spinal cord and sciatic nerve pathological damage in a neuropathy model by inhibiting SIGMAR1 binding to NMDAR and phosphorylation of NMDAR Ser896. Veratramine has anti-tumor proliferation, apoptosis induction, anti-inflammatory and neuroprotective activities, and can be used in the study of cancers such as liver cancer and osteosarcoma, as well as diabetic peripheral neuropathy .
|
-
- HY-N0440R
-
|
|
Reference Standards
Influenza Virus
NF-κB
5 alpha Reductase
Keap1-Nrf2
Lactate Dehydrogenase
Apoptosis
|
Infection
Neurological Disease
Inflammation/Immunology
Endocrinology
Cancer
|
|
Germacrone (Standard) is an analytical standard of Gemmacrone (HY-N0440). This product is intended for research and analytical applications. Germacrone (Standard) is a sesquiterpene compound with multiple biological activities. Germacrone (Standard) inhibits the H1N1 and H3N2 influenza A viruses and the influenza B virus. Germacrone (Standard) blocks the progressionof arthritis by regulating Th1/Th2 balance and inhibiting NF-κB signaling. Germacrone (Standard) can arrest the cell cycle at G0/G1 and G2/M phases and induce apoptosis in breast cancer cells. Germacrone (Standard) inhibits 5α-reductase and has anti-androgenic effect. Germacrone (Standard) has neuroprotective functions and can be used for the study of traumatic brain injury (TBI). Germacrone (Standard) also has antioxidant activity .
|
-
- HY-174396
-
|
|
PI3K
HDAC
Bcl-2 Family
Caspase
Reactive Oxygen Species (ROS)
Apoptosis
Histone Methyltransferase
Microtubule/Tubulin
|
Cancer
|
|
PI3Kδ/HDAC6-IN-1 (Compound 22E) is an orally active and dual inhibitor of PI3Kδ and HDAC6 with IC50 values of 2.4 nM and 6.2 nM, respectively. PI3Kδ/HDAC6-IN-1 exhibits potent antiproliferative effects on non-Hodgkin lymphoma (NHL) cells and possesses in vivo antitumor activity without significant toxicity. PI3Kδ/HDAC6-IN-1 arrests the cell cycle at the G0/G1 phase and induces apoptosis. PI3Kδ/HDAC6-IN-1 blocks the PI3K/AKT/mTOR signaling pathway and increases the acetylation levels of α-tubulin and histone H3 .
|
-
- 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 .
|
-
- HY-Y0106R
-
|
|
Reference Standards
mTOR
Xanthine Oxidase
Apoptosis
|
Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
|
|
2,6-Dihydroxyacetophenone (Standard) is the analytical standard of 2,6-Dihydroxyacetophenone (HY-Y0106). This product is intended for research and analytical applications. 2,6-Dihydroxyacetophenone, a polyphenolic derivative of Acetophenone (HY-Y0989), is an orally active mTOR inhibitor. 2,6-Dihydroxyacetophenone shows antioxidant activity. 2,6-Dihydroxyacetophenone inhibits cell growth and proliferation in CRC cells. 2,6-Dihydroxyacetophenone arrests at G0/G1 phase of cell cycle, induces apoptosis and suppresses cell migration in CRC cells. 2,6-Dihydroxyacetophenone inhibits xanthine oxidase (XOD) with an IC50 of 1.24 mM. 2,6-dihydroxyacetophenone improves uric acid metabolism in hyperuricemia mice, reduces plasma cholesterol in hypercholesterolemic rats, and inhibits lipid accumulation in HFD-induced obese mice. 2,6-Dihydroxyacetophenone can be used for the study of colorectal cancer (CRC), hyperuricemia and hypercholesterolemia .
|
-
- HY-181078
-
|
|
c-Myc
Apoptosis
Bcl-2 Family
|
Cancer
|
|
Cephalotaxine-ester-(R)-1-ethoxy-3-mercaptopropan-2-ol-Ph (3,4OMe) is an anti-leukemic agent with potent ribosome-targeting protein synthesis inhibition. Cephalotaxine-ester-(R)-1-ethoxy-3-mercaptopropan-2-ol-Ph (3,4OMe) downregulates short-lived oncoproteins, including c-Myc and Mcl-1, by inhibiting protein synthesis. Cephalotaxine-ester-(R)-1-ethoxy-3-mercaptopropan-2-ol-Ph (3,4OMe) induces cell cycle arrest at the G0/G1 phase and triggers mitochondrial pathway-mediated apoptosis in acute myeloid leukemia (AML) cells. Cephalotaxine-ester-(R)-1-ethoxy-3-mercaptopropan-2-ol-Ph (3,4OMe) is applicable for research on leukemia .
|
-
- HY-N2392
-
|
|
Parasite
Lipoxygenase
Opioid Receptor
Apoptosis
Autophagy
Reactive Oxygen Species (ROS)
Interleukin Related
TNF Receptor
PGE synthase
COX
|
Infection
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Kukoamine A, a spermine alkaloid, is an orally active and brain-penetrant component found in the root barks of Lycium chinense (L. chinense) Miller. Kukoamine A inhibits purified Crithidia fasciculata trypanothione reductase and soybean lipoxygenase, activates μ-opioid receptor. Kukoamine A can inhibt cancer cell proliferation, migration and invasion, cause G0/G1 phase cell cycle arrest and induce apoptosis. Kukoamine A exerts neuroprotective effect and can induce autophagy . Kukoamine A inhibits LPS (HY-D1056)-induced NO, ROS, PGE2, TNF-α, IL-1β, IL-6 production and COX-2 activity. Kukoamine A reverses palmitic acid-induced insulin resistance, lipid accumulation, and oxidative stress via downregulation of Srebp-1c. Kukoamine A can be used for the research of cancer, infection, inflammation, metabolic and neurological disease, such as glioblastoma and Parkinson's disease .
|
-
- HY-181727
-
|
|
Androgen Receptor
HSP
CDK
|
Cancer
|
|
AR/AR-V7 degrader-1 is an orally active AR and AR-V7 degrader. AR/AR-V7 degrader-1 disrupts the interaction between AR/AR-V7 and HSP90, leading to their ubiquitination and degradation in castration-resistant prostate cancer cells. AR/AR-V7 degrader-1 regulates the expression of cell cycle-related proteins in prostate cancer cells (downregulates CDK4, CDK6, Cyclin D1, Cyclin E1; upregulates P21) and induces G0/G1 phase arrest. AR/AR-V7 degrader-1 inhibits the proliferation and migration of prostate cancer cells. AR/AR-V7 degrader-1 suppresses the growth of castration-resistant prostate cancer tumors in nude mice and induces the degradation of AR and AR-V7 in tumor tissues. AR/AR-V7 degrader-1 is applicable to the research of castration-resistant prostate cancer .
|
-
- HY-W131302
-
|
N,N-Ethylenediglycine
|
Endogenous Metabolite
|
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 .
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-
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P11173
-
|
|
DNA Alkylator/Crosslinker
Apoptosis
|
Cancer
|
|
Cr-ACP1 is an anti-cancerous peptide. Cr-ACP1 binds to DNA, inducing cell cycle arrest in the G0-G1 phase, leading to the initiation of Apoptosis mechanisms. Cr-ACP1 exhibits anticancer effects against colon cancer and epidermoid carcinoma .
|
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-N0837
-
|
NSC17821; NSC23880
|
Alkaloids
Piperidine Alkaloids
Structural Classification
other families
Classification of Application Fields
Plants
Disease Research Fields
Source Classification
Cancer
|
PI3K
Akt
mTOR
Autophagy
Apoptosis
|
|
Veratramine (NSC17821; NSC23880) is an orally active inhibitor of the PI3K/Akt/mTOR signaling pathway and a SIGMAR1 modulator. Veratramine induces autophagic apoptosis of tumor cells, arrests the cell cycle at the G0/G1 phase, and inhibits epithelial-mesenchymal transition (EMT)-related proteins to reduce tumor migration. Veratramine reduces spinal cord and sciatic nerve pathological damage in a neuropathy model by inhibiting SIGMAR1 binding to NMDAR and phosphorylation of NMDAR Ser896. Veratramine has anti-tumor proliferation, apoptosis induction, anti-inflammatory and neuroprotective activities, and can be used in the study of cancers such as liver cancer and osteosarcoma, as well as diabetic peripheral neuropathy .
|
-
-
- HY-17026E
-
|
dFdCTP trisodium
|
Structural Classification
Natural Products
Classification of Application Fields
Endogenous metabolite
Disease Research Fields
Source Classification
Cancer
|
Drug Metabolite
DNA/RNA Synthesis
Apoptosis
|
|
Gemcitabine triphosphate (dFdCTP) trisodium is the active metabolite of Gemcitabine (HY-17026). The mechanism of Gemcitabine triphosphate trisodium cell-killing is its competition with cytidine triphosphate during DNA replication, which results in the inhibition of chain elongation. Gemcitabine triphosphate trisodium shows a Ki of 11.2 μM against DNA polymerase α and 14.4 μM against DNA polymerase ε. Gemcitabine triphosphate trisodium partially inhibits dCMP deaminase and acts as a substrate for DNA synthesis to incorporate into cellular DNA and RNA. Gemcitabine triphosphate trisodium disrupts DNA and RNA synthesis, arrests cell cycle in G0/G1 and S phases, triggers apoptosis, reduces tumor cell proliferation. Gemcitabine triphosphate trisodium can be used for the research of pancreatic cancer and non-small cell lung cancer .
|
-
-
- HY-N2392
-
|
|
Cardiovascular Disease
Alkaloids
Structural Classification
other families
Classification of Application Fields
Other Alkaloids
Phenols
Polyphenols
Plants
Disease Research Fields
Source Classification
|
Parasite
Lipoxygenase
Opioid Receptor
Apoptosis
Autophagy
Reactive Oxygen Species (ROS)
Interleukin Related
TNF Receptor
PGE synthase
COX
|
|
Kukoamine A, a spermine alkaloid, is an orally active and brain-penetrant component found in the root barks of Lycium chinense (L. chinense) Miller. Kukoamine A inhibits purified Crithidia fasciculata trypanothione reductase and soybean lipoxygenase, activates μ-opioid receptor. Kukoamine A can inhibt cancer cell proliferation, migration and invasion, cause G0/G1 phase cell cycle arrest and induce apoptosis. Kukoamine A exerts neuroprotective effect and can induce autophagy . Kukoamine A inhibits LPS (HY-D1056)-induced NO, ROS, PGE2, TNF-α, IL-1β, IL-6 production and COX-2 activity. Kukoamine A reverses palmitic acid-induced insulin resistance, lipid accumulation, and oxidative stress via downregulation of Srebp-1c. Kukoamine A can be used for the research of cancer, infection, inflammation, metabolic and neurological disease, such as glioblastoma and Parkinson's disease .
|
-
-
- HY-N7844
-
-
-
- HY-N0440
-
-
-
- HY-17026A
-
|
dFdCTP
|
Structural Classification
Natural Products
Classification of Application Fields
Endogenous metabolite
Disease Research Fields
Source Classification
Cancer
|
Drug Metabolite
DNA/RNA Synthesis
Apoptosis
|
|
Gemcitabine triphosphate (dFdCTP) is the active metabolite of Gemcitabine (HY-17026). The mechanism of Gemcitabine triphosphate cell-killing is its competition with cytidine triphosphate during DNA replication, which results in the inhibition of chain elongation. Gemcitabine triphosphate shows a Ki of 11.2 μM against DNA polymerase α and 14.4 μM against DNA polymerase ε. Gemcitabine triphosphate partially inhibits dCMP deaminase and acts as a substrate for DNA synthesis to incorporate into cellular DNA and RNA. Gemcitabine triphosphate disrupts DNA and RNA synthesis, arrests cell cycle in G0/G1 and S phases, triggers apoptosis, reduces tumor cell proliferation. Gemcitabine triphosphate can be used for the research of pancreatic cancer and non-small cell lung cancer .
|
-
-
- HY-N1930
-
-
-
- HY-149132
-
|
DDA
|
Triterpenes
Terpenoids
Endogenous metabolite
Source Classification
|
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-N0440R
-
|
|
Structural Classification
Terpenoids
Sesquiterpenes
Plants
Curcuma longa
Source Classification
Zingiberaceae
|
Reference Standards
Influenza Virus
NF-κB
5 alpha Reductase
Keap1-Nrf2
Lactate Dehydrogenase
Apoptosis
|
|
Germacrone (Standard) is an analytical standard of Gemmacrone (HY-N0440). This product is intended for research and analytical applications. Germacrone (Standard) is a sesquiterpene compound with multiple biological activities. Germacrone (Standard) inhibits the H1N1 and H3N2 influenza A viruses and the influenza B virus. Germacrone (Standard) blocks the progressionof arthritis by regulating Th1/Th2 balance and inhibiting NF-κB signaling. Germacrone (Standard) can arrest the cell cycle at G0/G1 and G2/M phases and induce apoptosis in breast cancer cells. Germacrone (Standard) inhibits 5α-reductase and has anti-androgenic effect. Germacrone (Standard) has neuroprotective functions and can be used for the study of traumatic brain injury (TBI). Germacrone (Standard) also has antioxidant activity .
|
-
-
- HY-Y0106
-
|
|
Classification of Application Fields
Ketones, Aldehydes, Acids
Phenols
Polyphenols
Metabolic Disease
Endogenous metabolite
Disease Research Fields
Source Classification
|
mTOR
Xanthine Oxidase
Apoptosis
|
|
2,6-Dihydroxyacetophenone, a polyphenolic derivative of Acetophenone (HY-Y0989), is an orally active mTOR inhibitor. 2,6-Dihydroxyacetophenone shows antioxidant activity. 2,6-Dihydroxyacetophenone inhibits cell growth and proliferation in CRC cells. 2,6-Dihydroxyacetophenone arrests at G0/G1 phase of cell cycle, induces apoptosis and suppresses cell migration in CRC cells. 2,6-Dihydroxyacetophenone inhibits xanthine oxidase (XOD) with an IC50 of 1.24 mM. 2,6-dihydroxyacetophenone improves uric acid metabolism in hyperuricemia mice, reduces plasma cholesterol in hypercholesterolemic rats, and inhibits lipid accumulation in HFD-induced obese mice. 2,6-Dihydroxyacetophenone can be used for the study of colorectal cancer (CRC), hyperuricemia and hypercholesterolemia .
|
-
-
- HY-N0837R
-
|
NSC17821 (Standard); NSC23880 (Standard)
|
Alkaloids
Piperidine Alkaloids
Structural Classification
other families
Plants
Source Classification
|
Reference Standards
PI3K
Akt
mTOR
Autophagy
Apoptosis
|
|
Veratramine (NSC17821; NSC23880) (Standard) is the analytical standard of Veratramine (HY-N0837). This product is intended for research and analytical applications. Veratramine (NSC17821; NSC23880) is an orally active inhibitor of the PI3K/Akt/mTOR signaling pathway and a SIGMAR1 modulator. Veratramine induces autophagic apoptosis of tumor cells, arrests the cell cycle at the G0/G1 phase, and inhibits epithelial-mesenchymal transition (EMT)-related proteins to reduce tumor migration. Veratramine reduces spinal cord and sciatic nerve pathological damage in a neuropathy model by inhibiting SIGMAR1 binding to NMDAR and phosphorylation of NMDAR Ser896. Veratramine has anti-tumor proliferation, apoptosis induction, anti-inflammatory and neuroprotective activities, and can be used in the study of cancers such as liver cancer and osteosarcoma, as well as diabetic peripheral neuropathy .
|
-
-
- HY-124261
-
-
-
- HY-N16567
-
-
-
- HY-N12044
-
-
-
- HY-N3764
-
-
-
- HY-Y0106R
-
|
|
Structural Classification
Ketones, Aldehydes, Acids
Phenols
Polyphenols
Endogenous metabolite
Source Classification
|
Reference Standards
mTOR
Xanthine Oxidase
Apoptosis
|
|
2,6-Dihydroxyacetophenone (Standard) is the analytical standard of 2,6-Dihydroxyacetophenone (HY-Y0106). This product is intended for research and analytical applications. 2,6-Dihydroxyacetophenone, a polyphenolic derivative of Acetophenone (HY-Y0989), is an orally active mTOR inhibitor. 2,6-Dihydroxyacetophenone shows antioxidant activity. 2,6-Dihydroxyacetophenone inhibits cell growth and proliferation in CRC cells. 2,6-Dihydroxyacetophenone arrests at G0/G1 phase of cell cycle, induces apoptosis and suppresses cell migration in CRC cells. 2,6-Dihydroxyacetophenone inhibits xanthine oxidase (XOD) with an IC50 of 1.24 mM. 2,6-dihydroxyacetophenone improves uric acid metabolism in hyperuricemia mice, reduces plasma cholesterol in hypercholesterolemic rats, and inhibits lipid accumulation in HFD-induced obese mice. 2,6-Dihydroxyacetophenone can be used for the study of colorectal cancer (CRC), hyperuricemia and hypercholesterolemia .
|
-
-
- HY-N18190
-
-
-
- HY-N7844R
-
-
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-N7844S
-
|
|
|
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 .
|
-
| Cat. No. |
Product Name |
|
Classification |
-
- HY-152263
-
|
|
|
PROTAC Synthesis
|
|
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.
|
-
- HY-159519
-
|
|
|
Azide
|
|
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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