Search Result
Results for "
proliferation arrest
" in MedChemExpress (MCE) Product Catalog:
1
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-130588A
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GSAO TFA
|
Mitochondrial Metabolism
|
Cancer
|
Glutathione arsenoxide (GSAO) TFA is a potential anticancer agent and a tumour metabolism inhibitor. Glutathione arsenoxide TFA targets Mitochondrial endomycin nucleotide transferase (ANT). Glutathione arsenoxide TFA causes cell proliferation arrest and cell death. Glutathione arsenoxide TFA can be used to identify cell-surface proteins, such as Protein disulphide isomerase .
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-
-
- HY-146999
-
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Histone Methyltransferase
Epigenetic Reader Domain
Apoptosis
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Cancer
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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 .
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-
-
- HY-101029
-
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NEKs
Apoptosis
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Cancer
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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-N0623R
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Tryptophan (standard); Tryptophane (standard)
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Others
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Metabolic Disease
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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 .
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-
-
- HY-101030
-
|
NEKs
Apoptosis
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Cancer
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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 .
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-
-
- HY-115888
-
|
Macrophage migration inhibitory factor (MIF)
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Cancer
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MIF2-IN-1 (compound 5d) is a potent inhibitor of MIF2 tautomerase with an IC50 of 1.0 μM. MIF2-IN-1 suppresses the proliferation of non-small cell lung cancer cells by the induction of cell cycle arrest via deactivation of the MAPK pathway. MIF2-IN-1 has the potential for the research of cancer diseases .
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-
-
- HY-101030A
-
|
NEKs
Apoptosis
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Cancer
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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 .
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-
-
- HY-168556
-
|
CDK
PROTACs
DNA/RNA Synthesis
|
Cancer
|
YJ9069 is a selective CDK12/CDK13 PROTAC degrader with an IC50 of 22.22 nM for in VCaP cells. CDK12/13 degradation rapidly triggers gene-length-dependent transcriptional elongation defects, leading to DNA damage and cell-cycle arrest. YJ9069 effectively inhibits proliferation in subsets of prostate cancer cells and significantly suppresses prostate tumor growth. (Pink: CDK12/CDK13 degradation agent (HY-168658); Black: Linker (HY-W015967); Blue: ligand for E3 ligase (HY-103596)) .
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-
-
- HY-N10268
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NSC 299113
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Apoptosis
|
Cancer
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3-Hydroxyterphenyllin is a metabolite of Aspergillus candidus.3-Hydroxyterphenyllin suppresses proliferation and causes cytotoxicity against A2780/CP70 and OVCAR-3 cells. 3-Hydroxyterphenyllin induces S phase arrest and apoptosis. 3-Hydroxyterphenyllin has the potential for the research of ovarian cancer .
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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-14521
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DDATHF
|
Antifolate
Apoptosis
Caspase
Bcl-2 Family
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Cancer
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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
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DDATHF hydrate
|
Antifolate
Apoptosis
Caspase
Bcl-2 Family
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Cancer
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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-14521A
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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 .
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-
-
- HY-N0863
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NSC-698790; Smilax saponin B
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Apoptosis
|
Cancer
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Methyl protodioscin(NSC-698790) is a furostanol bisglycoside with antitumor properties; shows to reduce proliferation, cause cell cycle arrest.
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-
-
- HY-159147
-
|
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) .
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-
-
- HY-149343
-
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Apoptosis
Autophagy
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Cancer
|
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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-
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- HY-N1516
-
|
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-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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-
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- HY-118902
-
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CDK
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Others
|
Aloisine B (compound 9) is a cyclin-dependent kinase (CDK) inhibitor. Aloisine B inhibits cell proliferation by arresting cells in both G1 and G2 via competing with ATP-binding pocket .
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-
-
- HY-N1925
-
|
Apoptosis
Autophagy
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Neurological Disease
Inflammation/Immunology
Cancer
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Tea polyphenol is the floorboard of phenolic compounds in tea. Tea polyphenol exhibits biological activity including antioxidant and anti-cancer activities, inhibition of cell proliferation, induction of apoptosis, cell cycle arrest and modulation of carcinogen metabolism .
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-
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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-155459
-
|
Microtubule/Tubulin
|
Cancer
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Tubulin polymerization-IN-57 (compound 5a) is a tubulin inhibitor and is an α-naphthoxy-substituted carbendazim (HY-13582) derivative. Tubulin polymerization-IN-57 induces mitotic arrest and inhibits cancer cell proliferation .
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-
-
- HY-N1255
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(-)-Scoulerine; Discretamine
|
Microtubule/Tubulin
Beta-secretase
Apoptosis
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Cancer
|
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-150571
-
|
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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-
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- HY-N7045
-
|
Androgen Receptor
Apoptosis
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Cancer
|
Isosilybin B, a flavonolignan isolated from Silybum marianum, has anti-prostate cancer (PCA) activity via inhibiting proliferation and inducing G1 phase arrest and apoptosis. Isosilybin B causes androgen receptor (AR) degradation .
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-
-
- HY-156266
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Rhiz
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Others
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Cancer
|
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-N0211
-
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EGFR
Apoptosis
|
Cancer
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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 .
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-
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- HY-18626
-
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Topoisomerase
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Cancer
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NK 314 is an inhibitor for topoisomerase IIα, which generates the break of DNA double-strand. NK 314 arrests the cell cycle at G2 phase in human acute myeloid leukemia cells, inhibits the proliferation of CEM with IC90 of 55 nM .
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-
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- HY-159515
-
|
Apoptosis
DNA/RNA Synthesis
Reactive Oxygen Species
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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 .
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-
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- HY-N1196
-
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NF-κB
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Inflammation/Immunology
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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 .
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-
-
- HY-B1029
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Danazol
4 Publications Verification
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PKC
Apoptosis
Tyrosinase
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Endocrinology
Cancer
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Danazol inhibits the proliferation of cancer cell MDA-MB-231 and MCF-7 with IC50 of 65 µg/mL and 31 µg/mL. Danazol arrests the cell cycle at G1 phase, induces apoptosis in MDA-MB-231 through PKCα signaling pathway .
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-
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- HY-151939
-
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DNA/RNA Synthesis
Apoptosis
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Cancer
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BLM-IN-2 is a Bloom's Syndrome Protein (BLM) inhibitor with an IC50 value of 0.8 μM. BLM-IN-2 effectively suppresses the proliferation, invasion, cell cycle arrest and apoptosis of CRC cells. BLM-IN-2 can be used for the reserarch of colorectal cancer (CRC) .
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-
-
- HY-N1338
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NSC 122417
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mTOR
Akt
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Cancer
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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 .
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-
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- 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 .
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-
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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 .
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-
-
- HY-134333
-
|
Apoptosis
|
Cancer
|
ICCB280 is a potent inducer of C/EBPα. ICCB280 exhibits anti-leukemic properties including terminal differentiation, proliferation arrest, and apoptosis through activation of C/EBPα and affecting its downstream targets (such as C/EBPε, G-CSFR and c-Myc) .
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-
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- HY-N10447
-
|
Apoptosis
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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 .
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-
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- HY-B1029R
-
|
Tyrosinase
PKC
Apoptosis
|
Endocrinology
Cancer
|
Danazol standard inhibits the proliferation of cancer cell MDA-MB-231 and MCF-7 with IC50 of 65 µg/mL and 31 µg/mL. Danazol arrests the cell cycle at G1 phase, induces apoptosis in MDA-MB-231 through PKCα signaling pathway .
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-
-
- HY-18969
-
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CDK
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Cancer
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LDC3140 is a selective CDK7 inhibitor (IC50<5 nM). By inhibiting the activity of CDK7, LDC3140 affects the regulation of the cell cycle, leading to cell cycle arrest and thus inhibiting the proliferation of tumor cells. LDC3140 can be used in the research of cancer treatment .
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-
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- HY-162763
-
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Apoptosis
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Cancer
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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 .
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-
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- HY-172110
-
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EGFR
Akt
p38 MAPK
ERK
Apoptosis
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Cancer
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Apoptosis inducer 35 (Compound 6) is a multi-targeted inhibitor, that reduces the expressions of EGFR, AKT, ERK and P38-MAPKα. Apoptosis inducer 35 inhibits the proliferation of cancer cell A549 and Jurkat, arrests the cell cycle at S phase, and induces apoptosis .
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-
-
- HY-131724
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p-DDAP; p-Dodecylaminophenol
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Apoptosis
|
Cancer
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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 .
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-
-
- HY-130588
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GSAO
|
Mitochondrial Metabolism
|
Cancer
|
Glutathione arsenoxide (GSAO) is a potential anticancer agent and a tumour metabolism inhibitor. Glutathione arsenoxide targets Mitochondrial endomycin nucleotide transferase (ANT). Glutathione arsenoxide causes cell proliferation arrest and cell death. Glutathione arsenoxide can be used to identify cell-surface proteins, such as Protein disulphide isomerase .
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-
-
- HY-161141
-
|
c-Met/HGFR
|
Cancer
|
EGFR/ C-Met-in-2 (Compound H-22) is a dual inhibitor of EGFR/c-Met. EGFR/c-Met-IN-2 inhibits cell proliferation by arresting G2/M phase. EGFR/c-Met-IN-2 has antitumor activity .
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-
-
- 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 .
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-
-
- 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 .
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-
-
- HY-159096
-
|
Apoptosis
|
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-168263
-
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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 .
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-
-
- HY-N7043
-
|
Apoptosis
|
Cancer
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Isosilybin A, a flavonolignan isolated from silymarin, has anti-prostate cancer (PCA) activity. Isosilybin A inhibits proliferation and induces G1 phase arrest and apoptosis in cancer cells, which activates apoptotic machinery in PCA cells via targeting Akt-NF-κB-androgen receptor (AR) axis .
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-
-
- HY-N0636
-
|
Apoptosis
|
Cancer
|
Eriocitrin is a flavonoid isolated from lemons that is a powerful antioxidant. Eriocitrin inhibits the proliferation of liver cancer cells by arresting the cell cycle in the S phase by upregulating p53, cyclin A, cyclin D3 and CDK6. Eriocitrin triggers apoptosis by activating intrinsic signaling pathways involving mitochondria .
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-
- HY-144766
-
|
Apoptosis
|
Cancer
|
ATX inhibitor 13 (10c) is an orally active and potent ATX inhibitor, with an IC50 of 3.4 nM. ATX inhibitor 13 inhibits proliferation and migration, and induces apoptosis and G2 phase arrest in RAW264.7 cells. ATX inhibitor 13 suppresses tumor cell colony formation .
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- HY-120027
-
|
Microtubule/Tubulin
Apoptosis
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Cancer
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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 .
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- HY-N1516A
-
|
Apoptosis
|
Cancer
|
(Z)-Ganoderenic acid D is the z-isomer of Ganoderenic acid D (HY-N1516). (Z)-Ganoderenic acid D is the triterpene that can be isolated from Ganoderma, and contributes to the bitter taste of the basidiocarps and extracts of Ganoderma species. Ganoderenic acid D inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis .
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-
- HY-N2058
-
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Bacterial
Apoptosis
|
Infection
Cancer
|
Neogambogic acid, an active ingredient in garcinia, induces apoptosis and has anticancer effect. Neogambogic acid has significant inhibitory activity toward methicillin-resistant Staphylococcus aureus (MRSA) .
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-
- HY-18643
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TZ9
2 Publications Verification
|
E1/E2/E3 Enzyme
Apoptosis
|
Cancer
|
TZ9 is a selective Rad6 inhibitor. TZ9 inhibits Rad6B-induced histone H2A ubiquitination, downregulates intracellular β-catenin, induces G2-M arrest and apoptosis, and inhibits the proliferation and migration of metastatic human breast cancer cells .
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-
- 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 .
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-
- HY-146390
-
|
Autophagy
Reactive Oxygen Species
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Cancer
|
Antiproliferative agent-5 (compound 4o) can significantly and irreversibly inhibit proliferation of gastric cancer cells. Antiproliferative agent-5 causes the G2/M phase arrest, and induces ROS accumulation and activation of autophagy. Antiproliferative agent-5 can be used for researching anticancer .
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-
- HY-157148
-
|
c-Met/HGFR
Trk Receptor
|
Cancer
|
1D228 is a c-Met/TRK inhibitor with antitumor activity. 1D228 inhibits cyclin D1 to induce G0/G1 arrest and inhibit cancer cell proliferation and migration. 1D228 can be used in the study of gastric, liver and vascular tumors .
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-
- HY-139054
-
|
Apoptosis
|
Cancer
|
4'-Methoxyflavone is a flavonoid with antioxidant properties and anti-proliferative activity against cancer cells. 4'-Methoxyflavone can inhibit cycle-dependent kinases leading to cell cycle arrest and regulate cell signaling pathways to influence cell proliferation and apoptosis. 4'-Methoxyflavone can be used in cancer chemoprevention research .
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- HY-P10421
-
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ERK
|
Cancer
|
PKCδ substrate acts as a nuclear transporter of ERK2 and is involved in ERK2 mediated gene activation. PKCδ is involved in the regulation of cell growth, proliferation, cell cycle arrest, and apoptosis by phosphorylating hBVR and other proteins. PKCδ substrate can be used to study the development of diseases, especially cancer biology .
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- HY-114545
-
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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 .
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- HY-10638
-
|
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-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 .
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-
- HY-101990
-
|
VEGFR
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Others
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IMS2186 is an anti-choroidal neovascularization (CNV) agent that inhibits angiogenesis upstream of VEGF. IMS2186 can arrest cancer cell cycle in G2/M phase, thus exerting anti-proliferation and anti-angiogenesis effects. IMS2186 has no intraocular toxicity and reduces the amount of eye leakage and diseased cells .
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-
- HY-163160
-
|
Apoptosis
Epigenetic Reader Domain
|
Cancer
|
Bet-in-23 (Compound 23) is a BD2-selective BET inhibitor with an IC50 of 2.9 nM. BET-IN-23 has anticancer activity and can significantly inhibit the proliferation of acute myeloid leukemia (AML) cell lines by inducing G0/G1 arrest and apoptosis in vitro .
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-
- HY-161268
-
-
- HY-158233
-
|
Apoptosis
VEGFR
|
Cancer
|
Apoptotic agent-4 (Compound 9) is a apoptosis inducer. Apoptotic agent-4 inhibits VEGFR-2 with an IC50 of 0.5717 μM. Apoptotic agent-4 inhibits cancer cell proliferation and arrests the cell at both the G2/M and Pre-G1 phases .
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-
- 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-149451
-
|
RET
VEGFR
c-Myc
|
Cancer
|
SYHA1815 is an orally active RET inhibitor (IC50=0.9 nmol/L) with antitumor activity. SYHA1815 is more selective for RET than KDR (IC50=15.9 nmol/L). SYHA1815 arrests the G1 cell cycle and inhibits RET-driven cell proliferation by downregulating c-Myc .
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-
- 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 .
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-
- HY-N7045R
-
|
Androgen Receptor
Apoptosis
|
Cancer
|
Isosilybin B (Standard) is the analytical standard of Isosilybin B. This product is intended for research and analytical applications. Isosilybin B, a flavonolignan isolated from Silybum marianum, has anti-prostate cancer (PCA) activity via inhibiting proliferation and inducing G1 phase arrest and apoptosis. Isosilybin B causes androgen receptor (AR) degradation .
|
-
- HY-170323
-
|
Apoptosis
|
Cancer
|
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 .
|
-
- HY-N1401
-
|
MMP
Apoptosis
HSV
|
Infection
Inflammation/Immunology
Cancer
|
20(R)-Ginsenoside Rh2, a matrix metalloproteinase (MMP) inhibitor, acts as a cell antiproliferator. It has anticancer effects via blocking cell proliferation and causing G1 phase arrest. 20(R)-Ginsenoside Rh2 induces apoptosis, and has anti-inflammatory and antioxidative activity . 20(R)-Ginsenoside Rh2 inhibits the replication and proliferation of mouse and human gammaherpesvirus 68 (MHV-68) with an IC50 of 2.77 μM for murine MHV-68 .
|
-
- HY-145670
-
|
Akt
MDM-2/p53
|
Cancer
|
cis,trans-Germacrone is a isomer of Germacrone (HY-N0440). Germacrone exhibits a wide range of antitumor, antioxidant and anti-inflammatory effects. Germacrone inhibits lung cancer cell proliferation and alters the Akt/MDM2/p53. Germacrone also arrests cell cycle at G1/S phase .
|
-
- 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-170313
-
|
GLUT
Apoptosis
Reactive Oxygen Species
|
Cancer
|
GLUT-1-IN-4 (Compound 13) is the p53 protein-dependent inhibitor for GLUT-1 glucose transporter. GLUT-1-IN-4 inhibits the proliferation of multiple cancer cells with IC50 in submicromolar levels. GLUT-1-IN-4 arrests the cell cycle, stimulates oxidative stress, and induces apoptosis .
|
-
- 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-149086
-
|
RAR/RXR
Apoptosis
PARP
Bcl-2 Family
|
Cancer
|
BPA-B9 is a RXRα ligand and antagonist targeting the pRXRα-PLK1 interaction. BPA-B9 has excellent RXRα-binding affinity (KD=39.29 ± 1.12 nM). BPA-B9 inhibits the proliferation of cancer cells by inducing mitotic arrest and cell apoptosis .
|
-
- HY-153751
-
|
Epigenetic Reader Domain
|
Cancer
|
BRD4-IN-4 (Compound 1) is a BRD4 inhibitor (IC50=6.83 μM). BRD4-IN-4 selectively inhibits MV4-11 cell line proliferation and arrests cell at G1 phase. BRD4-IN-4 can be used for research of MLL leukemia .
|
-
- 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-163924
-
|
Apoptosis
|
Cancer
|
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 .
|
-
- HY-105414
-
|
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 .
|
-
- HY-170843
-
|
Apoptosis
|
Cancer
|
Antitumor agent-198 (Compound A3) exhibits cytotoxicity in head and neck squamous cell carcinoma (HNSCC) cells, that inhibits the proliferation of CAL27, HN6, HN30, SCC9 and SCC25 with IC50 of 4 nM-77 nM. Antitumor agent-198 inhibits the HNSCC cell migration, arrests the cell cycle, and induces apoptosis .
|
-
- HY-170954
-
|
Apoptosis
c-Met/HGFR
TAM Receptor
|
Cancer
|
C-Met/Axl-IN-1 (Compound 22a) is an orally active and selective type II c-Met/Axl inhibitor with IC50 values of 1 nM and 10 nM, respectively. C-Met/Axl-IN-1 can inhibit proliferation, induce cell cycle arrest and apoptosis of tumor cells. C-Met/Axl-IN-1 has strong anti-tumor activity .
|
-
- HY-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-161409
-
|
Androgen Receptor
Apoptosis
|
Cancer
|
SC912 is an AR-V7 inhibitor (IC50 = 0.36 μM). SC912 possesses safety, potency and selectivity. SC912 binds directly to AR-FL and AR-V7 proteins, inhibites nuclear localization and chromatin binding capabilities. SC912 exerts anticancer activity through inhibition of proliferation, induction of cell cycle arrest and apoptosis .
|
-
- HY-N0636R
-
|
Apoptosis
|
Cancer
|
Eriocitrin (Standard) is the analytical standard of Eriocitrin. This product is intended for research and analytical applications. Eriocitrin is a flavonoid isolated from lemons that is a powerful antioxidant. Eriocitrin inhibits the proliferation of liver cancer cells by arresting the cell cycle in the S phase by upregulating p53, cyclin A, cyclin D3 and CDK6. Eriocitrin triggers apoptosis by activating intrinsic signaling pathways involving mitochondria .
|
-
- HY-N7043R
-
|
Apoptosis
|
Cancer
|
Isosilybin A (Standard) is the analytical standard of Isosilybin A. This product is intended for research and analytical applications. Isosilybin A, a flavonolignan isolated from silymarin, has anti-prostate cancer (PCA) activity. Isosilybin A inhibits proliferation and induces G1 phase arrest and apoptosis in cancer cells, which activates apoptotic machinery in PCA cells via targeting Akt-NF-κB-androgen receptor (AR) axis .
|
-
- HY-N12563
-
|
c-Myc
Apoptosis
|
Cancer
|
γ-Sitosterol is an inhibitor for c-Myc. γ-Sitosterol inhibits the proliferation of cancer cell MCF-7 and A549 with IC50 of 240.73 μg/mL and 696.6 μg/mL, arrests the cell cycle at G2/M phase, and induces apoptosis. γ-Sitosterol upregulates the expression of cell cycle regulators cyclin B/E .
|
-
- HY-171183
-
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
AB8939 is an effective small moleculeMicrotubule/Tubulin polymerization inhibitor with anti-tumor activity (it inhibits tumor cell proliferation with an IC50 of less than 10 nM). AB8939 can effectively evade resistance mechanisms mediated by things like P-glycoprotein and myeloperoxidase. AB8939 can induce G2/M phase cell cycle arrest and apoptosis in cells .
|
-
- HY-168927
-
|
Apoptosis
Pyroptosis
|
Cancer
|
Apoptosis inducer 36 (Compound 42) exhibits anti-leukemic activity through reduction of leukemia stem cells (LSCs) and induction of differentiation. Apoptosis inducer 36 inhibits the proliferation of AML cells, arrests cell cycle at G1 phase, and induces PANoptosis including apoptosis, pyroptosis and necrosis. Prodrug of apoptosis inducer 36 exhibits orally active antitumor efficacy in mouse model .
|
-
- 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-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-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-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-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-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 .
|
-
- HY-164489
-
|
EGFR
Akt
ERK
Apoptosis
|
Cancer
|
KU004 is a potent dual EGFR/HER2 inhibitor with anticancer effects. KU004 inhibits the proliferation of human breast cancer SKBR3 cells by inducing G1 phase arrest. KU004 blocks the activation of HER2, EGFR and downstream Akt and Erk pathways and induces cell Apoptosis mainly via the extrinsic pathway. KU004 is a quinazoline derivative .
|
-
- HY-117511
-
|
STAT
Apoptosis
Interleukin Related
TGF-beta/Smad
|
Others
|
HJC0123 is a STAT3 inhibitor. HJC0123 inhibits the proliferation of hepatic stellate cells and induces cell cycle arrest and apoptosis. HJC0123 reduces the phosphorylation, nuclear translocation and transcriptional activities of STAT3, increases the production of IL-6, inhibits the phosphorylation of Smad2/3 and down-regulates SOCS3. HJC0123 can be used in the study of liver fibrosis .
|
-
- 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-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-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-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-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-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-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-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-30272
-
|
Apoptosis
DNA/RNA Synthesis
|
Cancer
|
Monobenzone is a potent skin depigmenting agent. Monobenzone induces depigmentation and exhibits good potential for vitiligo research. Monobenzone is a potent inhibitor of RNR (Ribonucleotide reductase) enzyme activity by targeting RRM2 (a regulatory small subunit M2 of RNR) protein, and thus has significant anti-leukemia efficacy in vitro and in vivo. Monobenzone inhibits acute myeloid leukemia (AML) cells proliferation and DNA synthesis, induces cell cycle arrest, and 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-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-147861
-
|
Topoisomerase
Apoptosis
|
Cancer
|
Topoisomerase II inhibitor 11 (compound 3d) is a potent Topoisomerase II inhibitor, with an IC50 of 2.89 μM. Topoisomerase II inhibitor 11 shows 92.46% inhibition on renal cancer cell line A498 with an IC50 of 3.5 μM. Topoisomerase II inhibitor 11 causes cell cycle arrest at the G2/M phase leading to cell proliferation inhibition and pro-apoptotic activity .
|
-
- 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-162868
-
|
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 .
|
-
- 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 .
|
-
- 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-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 .
|
-
- 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 .
|
-
- 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-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-120625
-
|
HSP
|
Cancer
|
PU3 is a small molecule inhibitor of Hsp90 that competes with geldanamycin for Hsp90. PU3 induces degradation of proteins, including Her2, similar to geldanamycin. PU3 inhibits the growth of breast cancer cells, causing retinoblastoma protein hypophosphorylation, G1 arrest, and differentiation. PU3 represents a novel class of synthetic compounds that bind to Hsp90 and inhibit the proliferation of cancer cells. PU3 could provide a new strategy for the treatment of cancers .
|
-
- 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 .
|
-
- 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 .
|
-
- 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 .
|
-
- 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 .
|
-
- 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 .
|
-
- HY-170382
-
|
Estrogen Receptor/ERR
Apoptosis
|
Cancer
|
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 .
|
-
- HY-168924
-
|
Wnt
β-catenin
|
Metabolic Disease
|
Wnt/β-catenin activator 1 (Compound 5m) is the orally active activator for Wnt/β-catenin signaling pathway, that arrests cell cycle at G1 phase, inhibits early proliferation of adipocytes, and inhibits adipogenesis in cell 3T3-L1 with an IC50 of 330 nM. Wnt/β-catenin activator 1 exhibits anti-adipogenic and anti-dyslipidemic activities in high-fat diet fed Syrian golden hamster model .
|
-
- HY-N1401R
-
|
MMP
Apoptosis
HSV
|
Infection
Inflammation/Immunology
Cancer
|
20(R)-Ginsenoside Rh2 (Standard) is the analytical standard of 20(R)-Ginsenoside Rh2. This product is intended for research and analytical applications. 20(R)-Ginsenoside Rh2, a matrix metalloproteinase (MMP) inhibitor, acts as a cell antiproliferator. It has anticancer effects via blocking cell proliferation and causing G1 phase arrest. 20(R)-Ginsenoside Rh2 induces apoptosis, and has anti-inflammatory and antioxidative activity . 20(R)-Ginsenoside Rh2 inhibits the replication and proliferation of mouse and human gammaherpesvirus 68 (MHV-68) with an IC50 of 2.77 μM for murine MHV-68 .
|
-
- HY-N4075R
-
|
Endogenous Metabolite
|
Metabolic Disease
Cancer
|
20(R)-Ginsenoside Rh2 (Standard) is the analytical standard of 20(R)-Ginsenoside Rh2. This product is intended for research and analytical applications. 20(R)-Ginsenoside Rh2, a matrix metalloproteinase (MMP) inhibitor, acts as a cell antiproliferator. It has anticancer effects via blocking cell proliferation and causing G1 phase arrest. 20(R)-Ginsenoside Rh2 induces apoptosis, and has anti-inflammatory and antioxidative activity . 20(R)-Ginsenoside Rh2 inhibits the replication and proliferation of mouse and human gammaherpesvirus 68 (MHV-68) with an IC50 of 2.77 μM for murine MHV-68 .
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- HY-146660
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c-Myc
Epigenetic Reader Domain
Apoptosis
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Cancer
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BRD4 Inhibitor-18 is a highly potent BRD4 inhibitor with an IC50 value of 110 nM. BRD4 Inhibitor-18 has a hydrophobic acetylcyclopentanyl side chain. BRD4 Inhibitor-18 can significantly suppress the proliferation of MV-4-11 cells with high BRD4 level. BRD4 Inhibitor-18 has apoptosis-promoting and G0/G1 cycle-arresting activity .
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- HY-146261
-
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Microtubule/Tubulin
Indoleamine 2,3-Dioxygenase (IDO)
Apoptosis
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Cancer
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HI5 is a potent tublin and IDO inhibitor, with an IC50 value of 70 nM in HeLa cells. HI5 inhibit IDO expression and decrease kynurenine production, leading to stimulating T cells activation and proliferation. HI5 can inhibit tubulin polymerization and cell migration, cause G2/M phase arrest, and induce apoptosis via the mitochondrial dependent apoptosis pathway and cause reactive oxidative stress generation in HeLa cells. HI5 can be used for researching anticancer .
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- HY-N2983
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Tyrosinase
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Others
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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-P99284
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MK-0646; h7C10
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IGF-1R
Apoptosis
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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-155227A
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Anaplastic lymphoma kinase (ALK)
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Cancer
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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 .
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- HY-163705
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PROTACs
FGFR
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Cancer
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BR-cpd7 is a PROTAC degrader for fibroblast growth factor receptor FGFR1/2 with DC50 of 10 nM. BR-cpd7 arrests cell cycle, inhibits proliferations of FGFR1/2 aberrant activated tumor cells. (Pink: ligand for target protein FGFR-IN-12 (HY-160013); Black: linker; Blue: ligand for E3 ligase Thalidomide-NH-CH2-COOH (HY-131717))
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- HY-N13063
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Apoptosis
Reactive Oxygen Species
PI3K
Akt
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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 .
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-
- HY-124122
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VEGFR
Checkpoint Kinase (Chk)
Apoptosis
Caspase
Bcl-2 Family
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Cancer
|
BPTQ is a potent inhibitor against VEGFR1 and CHK2 with IC50 values of 0.54 and 1.70 µmol/L, respectively. BPTQ is also an intercalator of DNA with anticancer activities. BPTQ inhibits the proliferation of HL-60 cells by arresting cells at S and G2/M phase with an IC50 value of 12 µmol/L. BPTQ also activates the mitochondria-mediated Apoptosis pathway by a decrease in mitochondrial membrane potential, increase in the Bax:Bcl-2 ratio and activation of caspases .
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- HY-169413
-
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Akt
|
Cancer
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AKT-IN-25 (Compound 14a) is an inhibitor for Akt, that inhibits the phosphorylation of Akt, and thereby inhibits the PI3K/Akt/mTOR signaling pathway. AKT-IN-25 arrests the cell cycle at G1 phase, inhibits the cell migration of PANC-1, and inhibits the proliferation of cancer cells PANC-1, PATU-T, and SUIT-2 with IC50s of 3.05, 1.32, and 3.85 μM, respectively .
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-
- HY-170591
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MDM-2/p53
Apoptosis
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Cancer
|
p53 Activator 14 (Compound 7A) is a derivative of Neratinib (HY-32721), that induces DNA damage, activates p53, and inhibits the proliferation of multi cancer cells (IC50=7.21 μM for HCT116 cell). p53 Activator 14 inhibits the adhesion, migration and invasion of HCT116, arrests the cell cycle, and induces apoptosis. p53 Activator 14 inhibits angiogenesis and exhibits antitumor efficacy in chick chorioallantoic membrane (CAM) model .
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-
- HY-170568
-
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Microtubule/Tubulin
Apoptosis
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Cancer
|
Tubulin polymerization-IN-73 (Compound 37) is an inhibitor for microtubule polymerization with an IC50 of 1.8 μM. Tubulin polymerization-IN-73 arrests the cell cycle at G2/M phase, induces apoptosis in A549 cell, inhibits the proliferation of A549 WT and A549/T resistant cell with IC50 of 0.023 μM and 0.057 μM. Tubulin polymerization-IN-73 exhibits antitumor efficacy in mouse model .
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-
- HY-158106
-
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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.
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-
- HY-163692
-
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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 .
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-
- HY-162808
-
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DNA/RNA Synthesis
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Cancer
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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 .
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-
- HY-18981R
-
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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
-
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Cytochrome P450
EGFR
Apoptosis
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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-169403
-
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STAT
Apoptosis
Reactive Oxygen Species
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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 .
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-
- HY-170402
-
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Sirtuin
Apoptosis
|
Cancer
|
SIRT6-IN-4 (Compound 10d) is a selective inhibitor for SIRT6 with an IC50 of 5.68 μM. SIRT6-IN-4 inhibits the proliferation of MCF-7 with an IC50 of 8.30 μM. SIRT6-IN-4 arrests the cell cycle at G2/M phase, inhibits thecell migration and invasion of MCF-7, and induces apoptosis. SIRT6-IN-4 exhibits antitumor efficacy in mouse models .
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- HY-N0440
-
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Influenza Virus
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Infection
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Germacrone is isolated from turmeric and has anti-influenza virus, anti-cancer, and neuroprotective activity. Germacrone inhibits the proliferation of human hepatoma cell lines by downregulating CDK1 and Bcl-2/Bcl-xl and upregulating p21 and Bax, leading to cell cycle arrest in the G2/M phase and apoptosis. Germacrone targets H1N1 and H3N2 influenza A viruses as well as influenza B viruses, significantly reducing viral titers in the lungs in animal models .
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-
- HY-137497
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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 .
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-
- HY-155226
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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%) .
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-
- HY-161644
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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 .
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-
- HY-126876
-
|
Apoptosis
AMPK
Reactive Oxygen Species
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Cancer
|
GL-V9 inhibits proliferation of HepG2 cell (IC50 is 35.2 μM) through induction of apoptosis and cell cycle arrest at G2/M phase. GL-V9 regulates mitochondrial membrane potential and increases the production of intracellular reactive oxygen species. GL-V9 inhibits the pentose phosphate pathway (PPP), enhances fatty acid oxidation (FAO) through activation of AMPK, and thus inhibits the metastasis of cancer cells. GL-V9 exhibits antitumor efficacy in mouse model .
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-
- HY-163786
-
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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-169019
-
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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 .
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-
- HY-127057
-
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Androgen Receptor
CDK
MDM-2/p53
Apoptosis
Caspase
PARP
Bcl-2 Family
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Cancer
|
Lambertianic acid is a bioactive diterpene with anti-allergic, antibacterial and anticancer activities. Lambertianic acid decreases androgen receptor protein levels, cellular and secretory levels of prostate-specific antigen. Lambertianic acid also suppresses cell proliferation by inducing G1 arrest, downregulating CDK4/6 and cyclin D1, activating p53, p21 and p27. Lambertianic acid induces Apoptosis and the expression of related proteins, including cleaved caspase-3/9, c-PARP and BAX, and inhibited BCl-2. Lambertianic acid is promising for research of prostate cancer .
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-
- HY-172092
-
|
Apoptosis
Ferroptosis
|
Cancer
|
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-132231
-
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PI3K
Apoptosis
|
Cancer
|
FD223 is a potent and selective phosphoinositide 3-kinase delta (PI3Kδ) inhibitor. FD223 displays high potency (IC50=1 nM) and good selectivity over other isoforms (IC50s of 51 nM, 29 nM and 37 nM, respectively for α, β and γ). FD223 exhibits efficient inhibition of the proliferation of acute myeloid leukemia (AML) cell lines by suppressing p-AKT Ser473 thus causing G1 phase arrest during the cell cycle. FD223 has potential for the research of leukemia such as AML .
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-
- HY-158138
-
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PARP
Topoisomerase
Apoptosis
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Cancer
|
TOPOI/PARP-1-IN-1 (Compound B6) is an orally active, low cytotoxic TOPOI/PARP dual inhibitor with an IC50 value of 0.09 μM for PARP1. TOPOI/PARP-1-IN-1 can effectively inhibit the proliferation and migration of cancer cells. TOPOI/PARP-1-IN-1 also causes cell cycle arrest in the G0/G1 phase and induces apoptosis. The tumor growth inhibition rate (TGI) of TOPOI/PARP-1-IN-1 in mice is 75.4% .
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-
- HY-161694
-
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DNA Methyltransferase
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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 .
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-
- HY-161858
-
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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-168718
-
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FAK
JAK
Aurora Kinase
PI3K
Akt
Apoptosis
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Cancer
|
FAK-IN-22 (Compound 26) is an inhibitor of FAK, JAK3, and Aurora B, with IC50 values of 50.94 nM, 9.99 nM, and 0.49 nM, respectively, effectively inhibiting tumor occurrence and metastasis in pancreatic ductal adenocarcinoma (PDAC). FAK-IN-22 effectively inhibits the proliferation of PANC-1 cells, with an IC50 value of 0.15 μM. FAK-IN-22 induces apoptosis and G2/M phase arrest in PANC-1 cells by inhibiting the FAK/PI3K/Akt signaling pathway .
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-
- HY-170451
-
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PROTACs
MDM-2/p53
Apoptosis
|
Cancer
|
KT-253 is a p53 stabilizer and a PROTAC degrader for MDM2 (DC50=0.4 nM). KT-253 inhibits the proliferation of cancer cell RS4;11 with an IC50 of 0.3 nM, arrests the cell cycle at G2/M phase, and induces apoptosis. KT-253 exhibits antitumor efficacy in mouse models . (Pink: ligand for target protein MDM2 ligand 4 (HY-170452); Black: linker (HY-W001478); Blue: ligand for E3 ligase cereblon (HY-163927))
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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) .
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-
- HY-161641
-
|
Microtubule/Tubulin
|
Cancer
|
Tubulin polymerization-IN-62 (Compound 14b) is an inhibitor for microtubule polymerization (IC50 is 7.5 μM) and a degrader for α- and β-tubulin. Tubulin polymerization-IN-62 inhibits proliferation of cancer cells MCF-7, A549 and HCT-116, with IC50 of 32, 60 and 29 nM, respectively. Tubulin polymerization-IN-62 arrests the cell cycle at G2/M phase, inhibits the migration of MCF-7. Tubulin polymerization-IN-62 exhibits antitumor efficacy with a tumor growth inhibition rate (TGI) of 74.27% in 4T1 homograft mouse model .
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-
- HY-164384
-
|
PI3K
Akt
mTOR
Apoptosis
|
Cancer
|
DFX117 is a selective, orally active inhibitor for PI3Kα and c-Met tyrosine kinase. DFX117 inhibits PI3K/Akt/mTOR pathway, inhibits the proliferation of NCI-H1975, NCI-H1993, and HCC827 with IC50s 0.02-0.08 µM. DFX117 arrests cell cycle at G0/G1 phase, induces apoptosis in A549 and NCI-H1975. DFX117 exhibits antitumor efficacy in mice .
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-
- HY-164374
-
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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-N0440R
-
|
Influenza Virus
|
Infection
|
Germacrone (Standard) is the analytical standard of Germacrone. This product is intended for research and analytical applications. Germacrone is isolated from turmeric and has anti-influenza virus, anti-cancer, and neuroprotective activity. Germacrone inhibits the proliferation of human hepatoma cell lines by downregulating CDK1 and Bcl-2/Bcl-xl and upregulating p21 and Bax, leading to cell cycle arrest in the G2/M phase and apoptosis. Germacrone targets H1N1 and H3N2 influenza A viruses as well as influenza B viruses, significantly reducing viral titers in the lungs in animal models .
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-
- HY-161934
-
|
PARP
Reactive Oxygen Species
Apoptosis
|
Cancer
|
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-147858A
-
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PROTACs
|
Cancer
|
PROTAC EGFR degrader 7 (compound 13b) is a potent and selective CRBN-recruiting PROTAC EGFRL858R/T790M degrader, with a DC50 of 13 .2 nM.PROTAC EGFR degrader 7 inhibits NCI-H1975 cells proliferation, with an IC50 of 46 .82 nM.PROTAC EGFR degrader 7 significantly induces apoptosis and G2/M phase arrest in NCI-H1975 cell.PROTAC EGFR degrader 7 shows antitumor activity, and can be used for non-small cell lung cancer (NSCLC) research .
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-
- HY-161769
-
|
PROTACs
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
HL435 is a heterobifunctional molecule that degrades BRD4 by linking to JQ1, with DC50 of 11.9 nM and 21.9 nM, in MDA-MB-231 and MCF-7 cells, respectively. HL435 inhibits the proliferation of MDA-MB-231, MCF-7, 22Rv1 and A549, arrests the cell cycle and induces apoptosis. HL435 exhibits antitumor activity in mouse model. (Pink: ligand for target protein JQ-1 (HY-78695); Black: linker (HY-W004640); blue: ligand for E3 ligase HL389 (HY-161770))
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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-164411
-
|
c-Met/HGFR
|
Cancer
|
KRC-00715 is an effective oral c-Met inhibitor with an IC50 of 9.0 nM, demonstrating high selectivity in gastric cancer cells. KRC-00715 specifically inhibits the growth of c-Met-highly expressed cell lines by inducing G1/S phase arrest, leading to a reduction in downstream signaling pathways, including Akt and Erk, as well as c-Met activity. KRC-00715, in the gastric cancer cell line Hs746, is characterized by an IC50 of 39 nM, and it selectively inhibits the proliferation of c-Met-highly expressed cell lines. KRC-00715 reduces tumor size in Hs746T xenograft mouse models .
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-
- HY-159897
-
|
PAK
LIM Kinase (LIMK)
Apoptosis
Reactive Oxygen Species
|
Cancer
|
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-168725
-
|
PROTACs
Kinesin
Apoptosis
|
Cancer
|
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-115925
-
|
SHP2
Phosphatase
|
Cancer
|
SHP2-IN-9 is a specific SHP2 inhibitor (IC50 =1.174 μM) with enhanced blood–brain barrier penetration. SHP2-IN-9 shows 85-fold more selective for SHP2 than SHP1. SHP2-IN-9 inhibits SHP2-mediated cell signal transduction and cancer cell proliferation, and inhibits the growth of cervix cancer tumors and glioblastoma growth in vivo .
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-
- HY-142696
-
|
CDK
Pim
Apoptosis
|
Cancer
|
CDK6/PIM1-IN-1 is a potent and balanced dual CDK6/PIM1 inhibitor with IC50 values of 39 and 88 nM, respectively. CDK6/PIM1-IN-1 inhibits CDK4 (IC50=3.6 nM). CDK6/PIM1-IN-1 significantly inhibits acute myeloid leukemia (AML) cell proliferation, arrest cell cycle at the G1 phase, and promote cell apoptosis. CDK6/PIM1-IN-1 exhibits potent anti-AML activity .
|
-
- HY-19542
-
C6-Cer; N-Hexanoylsphingosine
|
Apoptosis
|
Cancer
|
C6 Ceramide (C6-Cer) is a short-chain, cell-permeable ceramide pathway activator with anticancer activity. C6 Ceramide-mediated miR-29b expression participates in the progression of multiple myeloma through suppressing the proliferation, migration and angiogenesis of endothelial cells by targeting Akt signal pathway. C6 Ceramide exhibits multiple anti-cancer properties including cell cycle arrest, Apoptosis, inhibition of tumor growth and enhances the effects of chemotherapy in drug-resistant cancer cells. C6-ceramide can be used as an adjuvant for chemotherapeutic agents, to enhance anti-tumor effects .
|
-
- HY-150609
-
|
SHP2
Phosphatase
CDK
|
Cancer
|
SHP2/CDK4-IN-1 (compound 10) is an orally active and potent SHP2 and CDK4 dual inhibitor, with IC50 values of 4.3 and 18.2 nM, respectively. SHP2/CDK4-IN-1 effectively induces G0/G1 arrest to prevent the proliferation of TNBC cell lines. SHP2/CDK4-IN-1 shows significant antitumor efficacy in the EMT6 syngeneic mouse model. SHP2/CDK4-IN-1 can be used for triple-negative breast cancer (TNBC) research .
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-
- HY-161826
-
|
β-catenin
HSP
CDK
c-Myc
|
Cancer
|
Antitumor agent-174 (Compound 10) directly engages the N-terminal site of Hsp90 and promotes the degradation of β-catenin, thereby suppressing the Wnt/β-catenin signaling. Antitumor agent-174 effectively inhibits proliferation, induce S and G2/M phases arrest and block the clonogenic ability in CRC cells. Antitumor agent-174 down-regulates CDK1, Cyclin D1, c-Myc, Cyclin B1, and Cyclin A2, and upregulaties P21 proteins. Antitumor agent-174 has significant anti-tumor efficacy against colorectal cancer (CRC) with excellent pharmacokinetics and low toxicity .
|
-
- HY-116504
-
|
EGFR
Akt
ERK
Apoptosis
|
Cancer
|
WB-308 is a novel small molecule that was identified as an inhibitor of EGFR by an in vitro EGFR kinase activity system. WB-308 was able to reduce the proliferation and clonogenicity of NSCLC cells, causing G2/M phase arrest and apoptosis. In addition, WB-308 inhibited tumor growth in two in vivo animal models (lung orthotopic transplantation model and patient-derived clonal mouse model). WB-308 impaired the phosphorylation of EGFR, AKT, and ERK1/2 proteins. Compared with Gefitinib, WB-308 had lower cytotoxicity. This study showed that WB-308 is a new EGFR-TKI that may be considered as an alternative to Gefitinib in the clinical treatment of NSCLC.
|
-
- HY-168714
-
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
Microtubule inhibitor 12 (Compound 2k) is an inhibitor for microtubule polymerization with an IC50 of 22.23 μM. Microtubule inhibitor 12 arrests the cell cycle of B16-F10 at G2/M phase, induces apoptosis in B16-F10, and inhibits cell migration. Microtubule inhibitor 12 inhibits the proliferation of cancer cells B16-f10, A549, HepG2 and MCF-7, with IC50s of 0.098, 0.135, 0.109, and 0.259 μM, respectively. Microtubule inhibitor 12 exhibits antitumor efficacy in mouse model .
|
-
- HY-161863
-
|
Microtubule/Tubulin
Reactive Oxygen Species
Apoptosis
|
Cancer
|
Tubulin polymerization-IN-67 (Compound 5h) is an inhibitor for tubulin polymerization on colchicine binding site with an IC50 of 2.92 μM. Tubulin polymerization-IN-67 inhibits the proliferation of cancer cells HT29, A549, U2OS, MG-63 and HeLa with IC50s of 0.12-4.13 μM. Tubulin polymerization-IN-67 arrests the cell cycle at G2/M phase, induces apoptosis in cell U2OS, inhibits the cell migration of A549. Tubulin polymerization-IN-67 reduces the mitochondrial membrane potential (MMP) and increase intracellular ROS, inhibits the angiogenesis in HUVECs. Tubulin polymerization-IN-67 exhibits antitumor efficacy in mice
|
-
- HY-134061
-
|
Apoptosis
|
Cancer
|
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 .
|
-
- HY-13559
-
Azaspirane
|
Apoptosis
|
Cancer
|
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 .
|
-
- HY-168135
-
|
PROTACs
c-Met/HGFR
|
Cancer
|
PROTAC c-Met degrader-1 (Compound Met-DD4) is an orally active PROTAC degrader for c-Met with a DC50 of 6.21 nM. PROTAC c-Met degrader-1 inhibits the proliferation of c-Met-addicted cell MKN-45 with an IC50 of 4.37 nM, and arrests the cell cycle at G0/G1 phase. PROTAC c-Met degrader-1 exhibits antitumor efficacy in MKN-45 xenograft mouse models . (Pink: Ligand for target protein (HY-13404); Blue: Ligand for E3 ligase (HY-W087383); Black: Linker (HY-W074901))
|
-
- HY-168574
-
|
PROTACs
Sirtuin
Apoptosis
|
Cancer
|
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)
|
-
- 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-P10819
-
|
Histone Demethylase
Apoptosis
|
Cancer
|
S9-CMC1 TFA is a covalent peptide lysine-specific demethylase 1 (LSD1) inhibitor with an IC50 value of 2.53 μM. S9-CMC1 TFA specifically recognizes Cys360 in the enzyme-active region. S9-CMC1 TFA inhibits LSD1 activity, increasing H3K4me1 and H3K4me2 levels, leading to G1 cell cycle arrest and apoptosis and inhibiting cell proliferation. S9-CMC1 TFA significantly inhibits tumor growth in A549 xenograft animal models .
|
-
- HY-168895
-
|
AP-1
|
Cancer
|
c-Fos-IN-1 (Compound P16) is a c-Jun inhibitor, and decreases mRNA levels and protein levels of c-Fos. c-Fos-IN-1 also inhibits the phosphorylation activity of ERK and the transcriptional activity of AP-1. c-Fos-IN-1 shows anticancer activity by inhibiting ERK/c-Fos/Jun pathway. c-Fos-IN-1 inhibits the proliferation and migration of gastric cancer cells (IC50: 2.31 μM for MGC-803 cell). c-Fos-IN-1 arrests cell cycle at G2/M phase and induces cancer cell apoptosis. c-Fos-IN-1 inhibits gastric cancer tumor growth .
|
-
- HY-170927
-
|
JAK
STAT
Apoptosis
|
Cancer
|
JAK-IN-40 (Compound 46) is the inhibitor for JAK that inhibits JAK1, JAK2 and JAK3 with IC50s of 0.022, 0.759 and 1.601 μM, respectively. JAK-IN-40 inhibits the phosphorylation of STAT3. JAK-IN-40 inhibits the proliferation of cancer cell Ba/F3 and JAK1-TEL Ba/F3 with GI50 of 0.614 μM and 0.193 μM. JAK-IN-40 arrests cell cycle of H1975 and H2087 at G2/M phase, induces apoptosis. JAK-IN-40 exhibits a synergistic antitumor effect with Osimertinib (HY-15772) .
|
-
- HY-N0447
-
|
TRP Channel
Bacterial
Apoptosis
Autophagy
STAT
PERK
EGFR
PI3K
Akt
mTOR
Caspase
MMP
|
Infection
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
8-Gingerol can be found in the rhizome of ginger (Z. officinale) and has oral bioactivity. It activates TRPV1, with an EC50 value of 5.0 µM. 8-Gingerol inhibits COX-2 and also suppresses the growth of H. pylori in vitro. Additionally, 8-Gingerol exhibits anticancer, antioxidant, and anti-inflammatory properties by inhibiting the epidermal growth factor receptor (EGFR) and modulating its downstream STAT3/ERK pathway to suppress the proliferation, migration, and invasion of colorectal cancer cells. 8-Gingerol also exerts immunosuppressive effects by inhibiting oxidative stress, inducing cell cycle arrest, promoting apoptosis, and regulating autophagy. Furthermore, 8-Gingerol has cardioprotective effects. 8-Gingerol is promising for research in the fields of cancer, infection, immunosuppression, and cardiovascular diseases.
|
-
- HY-146095
-
|
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 .
|
-
- HY-147858
-
|
PROTACs
EGFR
Apoptosis
|
Cancer
|
PROTAC EGFR degrader 7 (compound 13b) is a potent and selective CRBN-recruiting PROTAC EGFR L858R/T790M degrader, with a DC50 of 13.2 nM. PROTAC EGFR degrader 7 inhibits NCI–H1975 cells proliferation, with an IC50 of 46.82 nM. PROTAC EGFR degrader 7 significantly induces apoptosis and G2/M phase arrest in NCI–H1975 cell. PROTAC EGFR degrader 7 shows antitumor activity, and can be used for non-small cell lung cancer (NSCLC) research . PROTAC EGFR degrader 7 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-161923
-
|
EGFR
Apoptosis
Akt
ERK
|
Cancer
|
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 .
|
-
- HY-169938
-
|
HDAC
Histone Demethylase
Apoptosis
|
Cancer
|
LSD1/HDAC-IN-2 (Compound 20c) is the inhibitor for LSD and HDAC, that inhibits LSD1, HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8, with IC50s of 39.0, 1.4, 1.0, 1.3, 2.9 and 16.0 nM, respectively. LSD1/HDAC-IN-2 inhibits the proliferation of cancer cells, especially the colorectal cancer cells. LSD1/HDAC-IN-2 arrests the cell cycle at G2/M phase, inhibits cell migration, and induces apoptosis in HCT-116 and HT-29 cells. LSD1/HDAC-IN-2 exhibits antitumor efficacy in mouse model without significant toxicity .
|
-
- HY-159122
-
|
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 .
|
-
- HY-12708
-
Chlorpromazine
Maximum Cited Publications
66 Publications Verification
|
Dopamine Receptor
Cytochrome P450
Autophagy
5-HT Receptor
|
Cardiovascular Disease
Neurological Disease
Cancer
|
Chlorpromazine is an orally active, blood-brain barrier-transparent antipsychotic agent that effectively antagonises D2 dopamine receptors and 5-HT2A, which is widely used in schizophrenia and other psychiatric disorders. Chlorpromazine exerts anti-cancer activity through a variety of pathways, including anti-proliferation, induction of autophagy and cycle arrest (G2-M phase), inhibition of cytochrome c oxidase (CcO), inhibition of tumour growth and metastasis, and inhibition of tumour immune escape. Chlorpromazine also blocks hNav1.7 channels (IC50=25.9 μM; concentration-dependent) and HERG potassium channels (IC50=21.6 μM), which has potential for analgesic and cardiac arrhythmic studies. Chlorpromazine also can inhibit clathrin-mediated endocytosis .
|
-
- HY-B0407A
-
|
Dopamine Receptor
Autophagy
Cytochrome P450
5-HT Receptor
|
Cardiovascular Disease
Neurological Disease
Cancer
|
Chlorpromazine hydrochloride is an orally active, blood-brain barrier-transparent antipsychotic agent that effectively antagonises D2 dopamine receptors and 5-HT2A, which is widely used in schizophrenia and other psychiatric disorders. Chlorpromazine hydrochloride exerts anti-cancer activity through a variety of pathways, including anti-proliferation, induction of autophagy and cycle arrest (G2-M phase), inhibition of cytochrome c oxidase (CcO), inhibition of tumour growth and metastasis, and inhibition of tumour immune escape. Chlorpromazine hydrochloride also blocks hNav1.7 channels (IC50=25.9 μM; concentration-dependent) and HERG potassium channels (IC50=21.6 μM), which has potential for analgesic and cardiac arrhythmic studies. Chlorpromazine hydrochloride also can inhibit clathrin-mediated endocytosis .
|
-
- HY-157213
-
|
Apoptosis
PROTACs
FLT3
|
Cancer
|
LWY713 is a PROTAC-class FLT3 degrader (DC50=0.64 nM), which selectively induces FLT3 degradation via cereblon and proteasome-dependent pathways. LWY713 inhibits cell proliferation and induces G0/G1 phase arrest and apoptosis in MV4-11 cells. LWY713 shows effective in vivo antitumor activity in MV4-11 xenograft models . LWY713 consists of a target protein ligand (red part) Gilteritinib (HY-12432), an E3 ubiquitin ligase ligand (blue part) Lenalidomide-F (HY-W039233), and a PROTAC linker (black part) Glycolic acid (HY-W015967). E3 ubiquitin ligase and linker can form Lenalidomide-Glycolic acid (HY-169373); the active control for the target protein ligand is Naproxen Gilteritinib (HY-169374).
|
-
- 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-B0407AR
-
|
Dopamine Receptor
Autophagy
Cytochrome P450
5-HT Receptor
|
Cardiovascular Disease
Neurological Disease
Cancer
|
Chlorpromazine (hydrochloride) (Standard) is the analytical standard of Chlorpromazine (hydrochloride). This product is intended for research and analytical applications. Chlorpromazine hydrochloride is an orally active, blood-brain barrier-transparent antipsychotic agent that effectively antagonises D2 dopamine receptors and 5-HT2A, which is widely used in schizophrenia and other psychiatric disorders. Chlorpromazine hydrochloride exerts anti-cancer activity through a variety of pathways, including anti-proliferation, induction of autophagy and cycle arrest (G2-M phase), inhibition of cytochrome c oxidase (CcO), inhibition of tumour growth and metastasis, and inhibition of tumour immune escape. Chlorpromazine hydrochloride also blocks hNav1.7 channels (IC50=25.9 μM; concentration-dependent) and HERG potassium channels (IC50=21.6 μM), which has potential for analgesic and cardiac arrhythmic studies. Chlorpromazine hydrochloride also can inhibit clathrin-mediated endocytosis .
|
-
- HY-W041470R
-
|
Endogenous Metabolite
|
Metabolic Disease
|
Chlorpromazine (hydrochloride) (Standard) is the analytical standard of Chlorpromazine (hydrochloride). This product is intended for research and analytical applications. Chlorpromazine hydrochloride is an orally active, blood-brain barrier-transparent antipsychotic agent that effectively antagonises D2 dopamine receptors and 5-HT2A, which is widely used in schizophrenia and other psychiatric disorders. Chlorpromazine hydrochloride exerts anti-cancer activity through a variety of pathways, including anti-proliferation, induction of autophagy and cycle arrest (G2-M phase), inhibition of cytochrome c oxidase (CcO), inhibition of tumour growth and metastasis, and inhibition of tumour immune escape. Chlorpromazine hydrochloride also blocks hNav1.7 channels (IC50=25.9 μM; concentration-dependent) and HERG potassium channels (IC50=21.6 μM), which has potential for analgesic and cardiac arrhythmic studies. Chlorpromazine hydrochloride also can inhibit clathrin-mediated endocytosis .
|
-
- HY-170329
-
|
PROTACs
Androgen Receptor
Apoptosis
|
Cancer
|
PROTAC AR Degrader-8 (Compound NP18) is the PROTAC degrader for androgen receptor (AR), that degrades AR-FL with DC50 of 0.018 μM and 0.14 μM in 22Rv1 cell and LNCaP cell, degrades AR-V7 with DC50 of 0.026 μM in 22Rv1 cell. PROTAC AR Degrader-8 inhibits the proliferation of cancer cell 22Rv1 and LNCaP with IC50 of 0.038 μM and 1.11 μM. PROTAC AR Degrader-8 arrests cell cycle at G2/M phase, induces apoptosis in 22Rv1 cell. PROTAC AR Degrader-8 exhibits anticancer efficacy in mouse and zebrafish model . (Pink: ligand for target protein AR ligand-33 (HY-170330); Black: linker (HY-W007731); Blue: ligand for E3 ligase Cereblon (HY-14658))
|
-
- HY-A0020
-
ED-71; 2-(3-hydroxypropoxy)-1,25-dihydroxyvitamin D3
|
VD/VDR
Apoptosis
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
Eldecalcitol (ED-71) is an orally active vitamin D3 analogue, inhibits bone resorption and increases bone mineral density. Eldecalcitol (ED-71) displays anti-tumor effect and inhibits cell proliferation, migration and induces apoptosis by suppressing GPx-1 .
|
-
- HY-A0020R
-
|
VD/VDR
Apoptosis
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
Eldecalcitol (Standard) is the analytical standard of Eldecalcitol. This product is intended for research and analytical applications. Eldecalcitol (ED-71) is an orally active vitamin D3 analogue, inhibits bone resorption and increases bone mineral density. Eldecalcitol (ED-71) displays anti-tumor effect and inhibits cell proliferation, migration and induces apoptosis by suppressing GPx-1 .
|
-
- HY-N6871
-
|
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 .
|
-
- 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 |
Target |
Research Area |
-
- HY-P10421
-
|
ERK
|
Cancer
|
PKCδ substrate acts as a nuclear transporter of ERK2 and is involved in ERK2 mediated gene activation. PKCδ is involved in the regulation of cell growth, proliferation, cell cycle arrest, and apoptosis by phosphorylating hBVR and other proteins. PKCδ substrate can be used to study the development of diseases, especially cancer biology .
|
-
- HY-P10819
-
|
Histone Demethylase
Apoptosis
|
Cancer
|
S9-CMC1 TFA is a covalent peptide lysine-specific demethylase 1 (LSD1) inhibitor with an IC50 value of 2.53 μM. S9-CMC1 TFA specifically recognizes Cys360 in the enzyme-active region. S9-CMC1 TFA inhibits LSD1 activity, increasing H3K4me1 and H3K4me2 levels, leading to G1 cell cycle arrest and apoptosis and inhibiting cell proliferation. S9-CMC1 TFA significantly inhibits tumor growth in A549 xenograft animal models .
|
Cat. No. |
Product Name |
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 .
|
Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-N0623
-
-
-
- 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-N0863
-
-
-
- HY-N1516
-
-
-
- HY-N0726
-
-
-
- HY-N1925
-
-
-
- HY-N1255
-
-
-
- HY-N7045
-
-
-
- HY-N10268
-
-
-
- HY-126412
-
|
Flavonoids
Thymelaeaceae
Stellera chamaejasme Linn.
Plants
Biflavones
|
Apoptosis
|
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 .
|
-
-
- HY-N0211
-
-
-
- HY-N1196
-
-
-
- HY-N1338
-
-
-
- HY-N0726R
-
-
-
- HY-N10447
-
-
-
- HY-N7043
-
-
-
- HY-N0636
-
-
-
- HY-N1516A
-
-
-
- HY-N2058
-
-
-
- HY-139054
-
-
-
- HY-N0211R
-
-
-
- HY-N13164
-
-
-
- HY-N7045R
-
-
-
- HY-N1401
-
-
-
- HY-N0636R
-
-
-
- HY-N7043R
-
-
-
- HY-N12563
-
-
-
- HY-77813
-
-
-
- HY-N12960
-
-
-
- HY-107780
-
-
-
- HY-107780A
-
-
-
- HY-107780B
-
-
-
- HY-110382
-
-
-
- HY-18981
-
-
-
- HY-N11439
-
-
-
- HY-N3764
-
-
-
- HY-N1401R
-
-
-
- HY-N4075R
-
-
-
- HY-N2983
-
-
-
- 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-N0440
-
-
-
- HY-127057
-
-
-
- HY-N0440R
-
|
Structural Classification
Terpenoids
Sesquiterpenes
Source classification
Plants
Curcuma longa
Zingiberaceae
|
Influenza Virus
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Germacrone (Standard) is the analytical standard of Germacrone. This product is intended for research and analytical applications. Germacrone is isolated from turmeric and has anti-influenza virus, anti-cancer, and neuroprotective activity. Germacrone inhibits the proliferation of human hepatoma cell lines by downregulating CDK1 and Bcl-2/Bcl-xl and upregulating p21 and Bax, leading to cell cycle arrest in the G2/M phase and apoptosis. Germacrone targets H1N1 and H3N2 influenza A viruses as well as influenza B viruses, significantly reducing viral titers in the lungs in animal models .
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- HY-N0447
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Zingiber officinale Roscoe
Structural Classification
Monophenols
Classification of Application Fields
Source classification
Phenols
Plants
Inflammation/Immunology
Disease Research Fields
Zingiberaceae
Cancer
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TRP Channel
Bacterial
Apoptosis
Autophagy
STAT
PERK
EGFR
PI3K
Akt
mTOR
Caspase
MMP
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8-Gingerol can be found in the rhizome of ginger (Z. officinale) and has oral bioactivity. It activates TRPV1, with an EC50 value of 5.0 µM. 8-Gingerol inhibits COX-2 and also suppresses the growth of H. pylori in vitro. Additionally, 8-Gingerol exhibits anticancer, antioxidant, and anti-inflammatory properties by inhibiting the epidermal growth factor receptor (EGFR) and modulating its downstream STAT3/ERK pathway to suppress the proliferation, migration, and invasion of colorectal cancer cells. 8-Gingerol also exerts immunosuppressive effects by inhibiting oxidative stress, inducing cell cycle arrest, promoting apoptosis, and regulating autophagy. Furthermore, 8-Gingerol has cardioprotective effects. 8-Gingerol is promising for research in the fields of cancer, infection, immunosuppression, and cardiovascular diseases.
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- HY-W041470R
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Structural Classification
Ketones, Aldehydes, Acids
Source classification
Endogenous metabolite
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Endogenous Metabolite
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Chlorpromazine (hydrochloride) (Standard) is the analytical standard of Chlorpromazine (hydrochloride). This product is intended for research and analytical applications. Chlorpromazine hydrochloride is an orally active, blood-brain barrier-transparent antipsychotic agent that effectively antagonises D2 dopamine receptors and 5-HT2A, which is widely used in schizophrenia and other psychiatric disorders. Chlorpromazine hydrochloride exerts anti-cancer activity through a variety of pathways, including anti-proliferation, induction of autophagy and cycle arrest (G2-M phase), inhibition of cytochrome c oxidase (CcO), inhibition of tumour growth and metastasis, and inhibition of tumour immune escape. Chlorpromazine hydrochloride also blocks hNav1.7 channels (IC50=25.9 μM; concentration-dependent) and HERG potassium channels (IC50=21.6 μM), which has potential for analgesic and cardiac arrhythmic studies. Chlorpromazine hydrochloride also can inhibit clathrin-mediated endocytosis .
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- HY-N6871
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Infection
Structural Classification
Colophony
Classification of Application Fields
Pinaceae
Ketones, Aldehydes, Acids
Metabolic Disease
Plants
Inflammation/Immunology
Disease Research Fields
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Bacterial
IKK
Ferroptosis
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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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Product Name |
Chemical Structure |
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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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Product Name |
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Classification |
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- HY-B1029
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Danazol
4 Publications Verification
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Alkynes
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Danazol inhibits the proliferation of cancer cell MDA-MB-231 and MCF-7 with IC50 of 65 µg/mL and 31 µg/mL. Danazol arrests the cell cycle at G1 phase, induces apoptosis in MDA-MB-231 through PKCα signaling pathway .
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- HY-147858
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Alkynes
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PROTAC EGFR degrader 7 (compound 13b) is a potent and selective CRBN-recruiting PROTAC EGFR L858R/T790M degrader, with a DC50 of 13.2 nM. PROTAC EGFR degrader 7 inhibits NCI–H1975 cells proliferation, with an IC50 of 46.82 nM. PROTAC EGFR degrader 7 significantly induces apoptosis and G2/M phase arrest in NCI–H1975 cell. PROTAC EGFR degrader 7 shows antitumor activity, and can be used for non-small cell lung cancer (NSCLC) research . PROTAC EGFR degrader 7 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-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-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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Product Name |
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Classification |
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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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