Search Result
Results for "
suppressed tumor cell proliferation
" in MedChemExpress (MCE) Product Catalog:
7
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-16938
-
|
5'-(Methylthio)-5'-deoxyadenosine; 5'-Deoxy-5'-(methylthio)adenosine; 5'-S-Methyl-5'-thioadenosine
|
Endogenous Metabolite
Apoptosis
Parasite
|
Metabolic Disease
Cancer
|
|
5'-Methylthioadenosine (5'-(Methylthio)-5'-deoxyadenosine) is a nucleoside generated from S-adenosylmethionine (SAM) during polyamine synthesis . 5'-Methylthioadenosine suppresses tumors by inhibiting tumor cell proliferation, invasion, and the induction of apoptosis while controlling the inflammatory micro-environments of tumor tissue. 5'-Methylthioadenosine and its associated materials have striking regulatory effects on tumorigenesis .
|
-
-
- HY-18768
-
NCT-501
5 Publications Verification
|
Aldehyde Dehydrogenase (ALDH)
Akt
β-catenin
Necroptosis
|
Cancer
|
|
NCT-501 is a reversible, non-competitive, selective, blood-brain barrier-permeable ALDH1A1 inhibitor with an IC50 of 40 nM. NCT-501 inhibits the AKT-β-catenin signaling pathway, induces necroptosis in nasopharyngeal carcinoma cells, suppresses their proliferation and inhibits stem cell spheroid formation. NCT-501 can be used in research related to nasopharyngeal carcinoma, esophageal squamous cell carcinoma and malignant tumors .
|
-
-
- HY-173629
-
|
|
Ras
Apoptosis
|
Cancer
|
|
RMC-5127 is a small molecule inhibitor that binds to GTP-targeted KRAS G12V, with oral bioavailability and blood-brain barrier permeability. RMC-5127 inhibits the activities of the RAS and MAPK pathways, suppresses the proliferation of KRAS G12V-mutant cancer cells and induces their apoptosis. RMC-5127 can be used for the research of KRAS G12V-mutant non-small cell lung cancer, pancreatic ductal adenocarcinoma, colorectal cancer and intracranial KRAS G12V tumors .
|
-
-
- HY-148807
-
|
QC8222 free base; TACH 101 free base
|
Histone Demethylase
Apoptosis
|
Cancer
|
|
Zavondemstat (QC8222 free base; TACH 101 free base) is an orally active pan-KDM4 inhibitor, with a IC50 ≤ 0.08 μM against human KDM4A-D and a Kᵢ of 0.52 μM against human KDM4C. Zavondemstat induces cell apoptosis, causes S-phase cell cycle arrest, reduces the population of tumor-initiating cells and inhibits cancer cell proliferation. Zavondemstat suppresses tumor growth and induces tumor regression in mouse xenograft models. Zavondemstat can be used for the research of various cancers including colorectal cancer, esophageal squamous cell carcinoma and triple-negative breast cancer .
|
-
-
- 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-142870
-
|
|
Pyruvate Carboxylase (PC)
Apoptosis
β-catenin
ERK
Wnt
|
Cancer
|
|
ZY-444 is an anti-cancer agent, targeting pyruvate carboxylase (PC). ZY-444 suppresses the Wnt/β-catenin/Snail signaling pathway by blocking nuclear translocation of β-catenin. ZY-444 selectively inhibits proliferation, migration, and invasion and induces apoptosis in cancer cells. ZY-444 exhibits potent anti-tumor in cancer mouse models. ZY-444 can be used for the study of breast cancer, lung cancer (NSCLC), prostate cancer and iodine-refractory thyroid cancer .
|
-
-
- 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-N0448
-
|
|
AMPK
Reactive Oxygen Species (ROS)
Akt
PI3K
Interleukin Related
TNF Receptor
Apoptosis
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
10-Gingerol is an AMPK agonist, which is found in the ginger oleoresin from fresh rhizome with anti-inflammatory, antioxidant and anti-proliferative activities. 10-Gingerol suppresses neointimal hyperplasia and inhibits vascular smooth muscle cell proliferation. 10-Gingerol exhibits substantial scavenging activities with an IC50 value of 10.47 μM against DPPH radical, an IC50 value of 1.68 μM against superoxide radical and an IC50 value of 1.35 μM against hydroxyl radical. 10-Gingerol inhibits the proliferation of MDA-MB-231 tumor cell line with an IC50 of 12.1 μM. 10-Gingerol suppresses the proliferation, migration, invasion, and induced apoptosis through targeting the PI3K/Akt signaling pathway in MDA-MB-231/IR cells. 10-Gingerol can be used in research on various common cancers such as ovarian cancer and colon cancer, as well as colitis and neurodegenerative diseases .
|
-
-
- HY-176523
-
|
|
Ras
|
Cancer
|
|
KRAS G12D inhibitor 29 (Compound Formula (I)) is an orally active and selective KRAS G12D mutant inhibitor. KRAS G12D inhibitor 29 blocks downstream signaling pathways mediated by KRAS G12D, suppressing tumor cell proliferation. KRAS G12D inhibitor 29 is promising for research of KRAS G12D mutation-related cancers (such as pancreatic cancer, lung cancer, colorectal cancer) .
|
-
-
- HY-121802
-
|
|
Hedgehog
|
Cancer
|
|
Dynarrestin is a aminothiazole inhibitor of cytoplasmic dyneins 1 and 2. Dynarrestin rapidly and reversibly inhibits dynein 1-driven microtubule gliding in vitro plus a range of dynein 1- and 2-dependent processes in cells without affecting ATP hydrolysis and interfering with ciliogenesis. Dynarrestin suppresses hedgehog (Hh)-dependent proliferation of neuronal precursors and tumor cells .
|
-
-
- HY-N6950
-
|
|
PI3K
Akt
mTOR
Parasite
Apoptosis
|
Infection
Cancer
|
|
Hederacolchiside A1, isolated from Pulsatilla chinensis, suppresses proliferation of tumor cells by inducing apoptosis through modulating PI3K/Akt/mTOR signaling pathway . Hederacolchiside A1 has antischistosomal activity, affecting parasite viability both in vivo and in vitro .
|
-
-
- HY-P99364
-
|
Anti-VEGFR1/FLT1 Reference Antibody; IMC-18F1
|
VEGFR
Apoptosis
p38 MAPK
Akt
|
Endocrinology
Cancer
|
|
Icrucumab (Anti-VEGFR1/FLT1 Reference Antibody; IMC-18F1) is an IgG1 antibody inhibitor targeting VEGFR-1/FLT1 with anti-tumor activity. By blocking ligand-dependent phosphorylation and downstream signal transduction, Icrucumab reduces the activities of MAPK and Akt in breast cancer xenograft models, inhibits the proliferation and invasion of VEGFR-1-positive tumor cells, and reverses the conversion of M1 macrophages to the pro-tumor M2-like phenotype. Icrucumab also inhibits tumor cell proliferation, promotes apoptosis, and effectively suppresses tumor growth through direct targeting of tumors and host support mechanisms. In addition, Icrucumab exhibits a synergistic effect when combined with chemotherapeutic agents, and it is used in research related to various cancers including advanced solid malignancies, thyroid cancer, melanoma, and lung cancer .
|
-
-
- HY-N0743
-
|
|
α-synuclein
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Senkyunolide A is a phthalide, anti-tumor cell proliferation agent with anticancer activity. Senkyunolide A protects neurons from corticosterone (HY-B1618)-induced apoptosis by decreasing protein phosphatase PP2A and α-synuclein phosphorylation and protein level. Senkyunolide A also inhibits osteoarthritis through the NLRP3 signaling pathway and suppresses the expression of CD137, a diagnostic biomarker for atherosclerosis .
|
-
-
- HY-134463
-
|
|
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
|
NHWD-870 is a potent, orally active and selective BET family bromodomain inhibitor and only binds bromodomains of BRD2, BRD3, BRD4 (IC50=2.7 nM), and BRDT. NHWD-870 has potent tumor suppressive efficacies and suppresses cancer cell-macrophage interaction. NHWD-870 increases tumor apoptosis and inhibits tumor proliferation .
|
-
-
- HY-13464
-
|
Brigatinib analog
|
Anaplastic lymphoma kinase (ALK)
EGFR
|
Cancer
|
|
ALK-IN-1 is an orally active, blood-brain barrier-permeable ALK and EGFR inhibitor. ALK-IN-1 binds to and inhibits ALK kinase, ALK fusion proteins, and wild-type and mutant EGFR variants, thereby disrupting their corresponding signaling pathways. ALK-IN-1 can suppress the growth and proliferation of tumor cells and exhibits potential inhibitory activity against mutant EGFR. ALK-IN-1 can be used in the research of non-small-cell lung cancer .
|
-
-
- HY-123981
-
5MPN
3 Publications Verification
|
Phosphatase
|
Cancer
|
|
5MPN is a first-in-class, potent, orally active and selective 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase 4 (PFKFB4) inhibitor. 5MPN appears to be a competitive inhibitor of the F6P binding site (Ki=8.6 μM). 5MPN does not inhibit PFK-1 or PFKFB3. 5MPN targets the sugar metabolism of tumors and suppresses proliferation of multiple human cancer cell lines .
|
-
-
- HY-124676A
-
|
|
Apoptosis
|
Cancer
|
|
DB2115 tetrahydrochloride is a highly selective PU.1 inhibitor that suppresses the binding of PU.1 to DNA (IC50: 2.3 nM). DB2115 tetrahydrochloride can inhibit tumor cell proliferation and induce apoptosis. DB2115 tetrahydrochloride can be used in the research of tumors such as leukemia .
|
-
-
- HY-141807
-
|
|
PROTACs
Akt
|
Cancer
|
|
MS21 is an effective AKT PROTAC degrader. MS21 can inhibit mutations in the PI3K/PTEN pathway, suppress the proliferation and induce cell cycle arrest of tumor cells. MS21 has anti-tumor activity. (Pink: AKT ligand-2 (HY-48682); Black: Linker (HY-W014125); Blue: (S,R,S)-AHPC (HY-125845)) .
|
-
-
- HY-16938S1
-
|
5'-(Methylthio)-5'-deoxyadenosine-d3; 5'-Deoxy-5'-(methylthio)adenosine-d3; 5'-S-Methyl-5'-thioadenosine-d3
|
Apoptosis
Parasite
Endogenous Metabolite
|
Inflammation/Immunology
|
|
5'-Methylthioadenosine-d3 is the deuterium labeled 5'-Methylthioadenosine . 5'-Methylthioadenosine (5'-(Methylthio)-5'-deoxyadenosine) is a nucleoside generated from S-adenosylmethionine (SAM) during polyamine synthesis. 5'-Methylthioadenosine suppresses tumors by inhibiting tumor cell proliferation, invasion, and the induction of apoptosis while controlling the inflammatory micro-environments of tumor tissue. 5'-Methylthioadenosine and its associated materials have striking regulatory effects on tumorigenesis .
|
-
-
- HY-W040055
-
|
D-(+)-Neopterin; D-erythro-Neopterin
|
NF-κB
PPAR
ERK
Raf
Src
|
Cardiovascular Disease
Inflammation/Immunology
|
|
Neopterin is an immune system activator metabolized by GTP and can be produced by activated macrophages. Neopterin has the potential to resist vascular inflammation and atherosclerosis. Neopterin inhibits the phosphorylation of NF-κB and promotes the expression of PPAR-γ, thereby suppressing the inflammatory response of vascular endothelial cells, reducing the formation of macrophage foam cells, and regulating the migration and proliferation of vascular smooth muscle cells. Neopterin can be used in research fields such as cardiovascular diseases (such as atherosclerosis), inflammation-related diseases and tumor immunomonitoring .
|
-
-
- HY-148105
-
|
|
MNK
Eukaryotic Initiation Factor (eIF)
Apoptosis
FLT3
DYRK
|
Cancer
|
|
DS12881479 is a selective non-ATP-competitive MNK1 inhibitor with an IC50 value of 387 nM. DS12881479 stabilizes MNK1 in its autoinhibited DFD-out conformation, blocks eIF4E phosphorylation, suppresses tumor cell proliferation and induces weak apoptosis. DS12881479 also inhibits FLT3 and DYRK1a kinase activity at high concentrations. DS12881479 can be used for the research of cancer, such as leukemia .
|
-
-
- HY-161781
-
-
-
- HY-178836
-
|
|
Drug-Linker Conjugates for ADC
Ras
|
Cancer
|
|
Z56-L23 is a conjugate of RAS-targeting ADC cytotoxic payload-linker with anti-tumor activity. Z56-L23 can be conjugated with HER3 antibody, EGFR antibody or EGFRxHER3 bispecific antibody to form intact antibody-drug conjugates (ADCs). ADC molecules related to Z56-L23 effectively inhibit the proliferation of tumor cells and also significantly suppress tumor growth in xenograft mouse models. Z56-L23 can be used in the research of pancreatic cancer .
|
-
-
- HY-155994
-
|
|
PROTACs
PIKfyve
Autophagy
|
Cancer
|
|
PIK5-12d is a PROTAC PIKfyve degrader (DC50 = 1.48 nM). PIK5-12d induces massive cytoplasmic vacuolization and blocks autophagic flux in multiple prostate cancer cells. PIK5-12d inhibits prostate cancer cell proliferation. PIK5-12d significantly suppresses tumor proliferation in mice bearing LTL-331R human prostate cancer PDX tumors. PIK5-12d can be used for the study of prostate cancer. (Pink: PIKfyve ligand (HY-175631), Blue: VHL Ligand (HY-125845), Black: Linker, PIKfyve ligand-linker conjugate (HY-175632)) .
|
-
-
- HY-120868
-
TP-004
1 Publications Verification
|
MetAP
|
Metabolic Disease
Cancer
|
|
TP-004 is a potent and reversible inhibitor of methionine aminopeptidase 2 (MetAP2), with an IC50 of 6 nM against MetAP2. TP-004 is a chemical probe. TP-004 suppresses MetAP2 enzymatic activity, blocks N-terminal methionine cleavage, impairs protein maturation and stability, and thereby inhibits cell proliferation and angiogenesis. TP-004 can be used for the study of tumors and diseases associated with excessive angiogenesis .
|
-
-
- HY-N0475
-
|
Hypolide; (+)-Triptophenolide
|
Androgen Receptor
Pyroptosis
Caspase
Bcl-2 Family
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Triptophenolide (Hypolide) is a colorless crystal isolated from the ethyl acetate extract of Tripterygium wilfordii. Triptophenolide is an orally active pan‑antagonist of the androgen receptor (AR) with an IC50 of 467 nM against human wild‑type AR. Triptophenolide reduces AR expression, inhibits AR nuclear translocation, downregulates prostate‑specific antigen mRNA levels, and suppresses the growth of AR‑positive prostate cancer cells. Triptophenolide shows anti-tumor effects against breast cancer by inhibiting cell proliferation and migration, inducing G1-phase arrest and apoptosis, repressing xenograft tumor growth. Triptophenolide inhibits pyroptosis, alleviates tissue inflammation, and ameliorates synovial injury. Triptophenolide can be used for the study of prostate cancer, rheumatoid arthritis and breast cancer .
|
-
-
- HY-174346
-
|
|
E1/E2/E3 Enzyme
Apoptosis
DNA/RNA Synthesis
|
Cancer
|
|
Skp2-IN-4 is an Skp2 inhibitor with a IC50 of 0.38 μM for Skp2-Cks1 binding. Skp2-IN-4 improves anti-tumor activity, inhibits the proliferation and induces S phase arrest by targeting Skp2. Skp2-IN-4 significantly enhances Cisplatin (HY-17394) chemosensitivity by suppressing the tumor cell stemness in NCl-H1299 xenograft mice model, promising for lung cancer and esophageal cancer research .
|
-
-
- HY-W654139
-
|
|
Isotope-Labeled Compounds
Endogenous Metabolite
Parasite
Apoptosis
|
Metabolic Disease
|
|
5'-Deoxy-5'-(methylthio)adenosine-d3 is deuterium labeled 5'-Methylthioadenosine. 5'-Methylthioadenosine (5'-(Methylthio)-5'-deoxyadenosine) is a nucleoside generated from S-adenosylmethionine (SAM) during polyamine synthesis . 5'-Methylthioadenosine suppresses tumors by inhibiting tumor cell proliferation, invasion, and the induction of apoptosis while controlling the inflammatory micro-environments of tumor tissue. 5'-Methylthioadenosine and its associated materials have striking regulatory effects on tumorigenesis.
|
-
-
- HY-159884
-
|
|
Tim3
TNF Receptor
IFNAR
|
Cancer
|
|
MG-T-19 is an effective TIM-3 inhibitor that can suppress the interaction of TIM-3 with PtdSer, CEACAM1, and Gal-9. MG-T-19 can increase the production of tumor necrosis factor-α (TNF-α) and interferon-γ (IFN-γ) in peripheral blood mononuclear cells (PBMCs) from healthy donors, and enhance the ability of PBMCs to inhibit the proliferation of Kasumi-1 cells (an acute myelogenous leukemia cell line) .
|
-
-
- HY-P991358
-
|
LFA-102; X213
|
Estrogen Receptor/ERR
STAT
Akt
|
Cancer
|
|
XOMA-213 (LFA-102; X213) is a human monoclonal antibody (mAb) targeting the prolactin receptor (PRLR), with a Kd value of 2 nM against the human target. XOMA-213 blocks PRL-induced cell proliferation and inhibits the activation of multiple PRLR ligands, including PRL and human growth hormone (hGH). XOMA-213 suppresses PRL-induced phosphorylation of Stat5, Akt and ERK1/2 in cells. XOMA-213 induces tumor regression, delays disease progression, and inhibits PRLR signaling as well as tumor growth. XOMA-213 can be used in research related to breast cancer .
|
-
-
- HY-172609
-
|
|
Phosphatase
Apoptosis
MDM-2/p53
Caspase
|
Metabolic Disease
Cancer
|
|
SL-176 is a PPM1D (Wip1) inhibitor. SL-176 inhibits lipid droplet formation, downregulates the mRNA and protein expression of PPARγ and C/EBPα, and blocks adipocyte differentiation. SL-176 induces G2/M cell cycle arrest, apoptosis and inhibits cell proliferation in breast cancer cells overexpressing PPM1D, and activates components of the p53 pathway. SL-176 suppresses tumor growth in a zebrafish model of neuroblastoma. SL-176 is applicable to research related to obesity, breast cancer and neuroblastoma .
|
-
-
- HY-116269
-
|
|
Ras
Apoptosis
PAK
ERK
|
Cancer
|
|
AZA197 is a selective small molecule inhibitor of Cdc42.AZA197 suppresses colon cancer cell proliferation, cell migration, invasion and increases apoptosis by down-regulating the PAK1 and ERK signaling pathways in vitro. AZA197 reduces tumor growth and significantly increases mouse survival in SW620 tumor xenografts. AZA197 can be used for the study of colon cancer .
|
-
-
- HY-177332
-
|
|
TAM Receptor
SARS-CoV
Akt
|
Infection
Cancer
|
|
SLC-391 is an orally active AXL kinase inhibitor with an IC50 of 9.6 nM against AXL kinase. SLC-391 inhibits Gas6-induced AXL-dependent phosphorylation of Akt. SLC-391 inhibits SARS-CoV-2 infection, entry and replication in cells. SLC-391 suppresses cancer cell proliferation. SLC-391 inhibits tumor growth in mouse solid tumor xenograft models. SLC-391 can be used for the research of COVID-19, influenza virus infection, triple-negative breast cancer, chronic myeloid leukemia and non-small cell lung cancer .
|
-
-
- 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)) .
|
-
-
- HY-16938S
-
|
5'-(Methylthio)-5'-deoxyadenosine-13C6; 5'-Deoxy-5'-(methylthio)adenosine-13C6; 5'-S-Methyl-5'-thioadenosine-13C6
|
Endogenous Metabolite
Apoptosis
|
Metabolic Disease
Cancer
|
|
5'-Methylthioadenosine- 13C6 is the 13C-labeled 5'-Methylthioadenosine. 5'-Methylthioadenosine (5'-(Methylthio)-5'-deoxyadenosine) is a nucleoside generated from S-adenosylmethionine (SAM) during polyamine synthesis . 5'-Methylthioadenosine suppresses tumors by inhibiting tumor cell proliferation, invasion, and the induction of apoptosis while controlling the inflammatory micro-environments of tumor tissue. 5'-Methylthioadenosine and its associated materials have striking regulatory effects on tumorigenesis .
|
-
-
- HY-175243
-
|
|
Adenosine Deaminase
Apoptosis
|
Cancer
|
|
ADAR1-IN-1 is a potent ADAR1 inhibitor. ADAR1-IN-1 significantly suppressed DU-145 cell proliferation (IC50 = 1.11 μM), clonogenicity, migration, and invasion, arrests cell cycle, and induces apoptosis. ADAR1-IN-1 safely and effectively inhibits tumor growth. ADAR1-IN-1 can be used for the study of prostate cancer (PCa) .
|
-
-
- HY-137062
-
|
|
CDK
|
Cancer
|
|
CGP-79807 is a purine-based CDK inhibitor. CGP-79807 can block the cell cycle by inhibiting CDK activity to suppress the proliferation of tumor cells. CGP-79807 can be used in the study of cancer .
|
-
-
- HY-177134
-
|
|
VEGFR
c-Met/HGFR
|
Cancer
|
|
Taligantinib (Compound Example 70) is an orally active and selective dual inhibitor targeting vascular endothelial growth factor receptor 2 (VEGFR-2) and hepatocyte growth factor receptor (c-Met). Taligantinib suppresses tumor angiogenesis and cell proliferation. Taligantinib is promising for research of solid tumors such as non-small cell lung cancer and hepatocellular carcinoma .
|
-
-
- HY-120412
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
SKLB188 is an orally active and potent epidermal growth factor receptor (EGFR) inhibitor (IC50=5 nM). SKLB188 suppresses MEK/Erk and Akt/mTOR signaling pathways to inhibit head and neck squamous cell carcinoma (HNSCC) proliferation and induce caspase-dependent apoptosis. SKLB188 is promising for research of EGFR-overexpressing solid tumors .
|
-
-
- HY-148807A
-
|
QC8222; TACH 101
|
Apoptosis
Histone Demethylase
|
Cancer
|
|
Zavondemstat (QC8222; TACH 101) L-lysine is an orally active pan-KDM4 inhibitor, with a IC50 ≤ 0.08 μM against human KDM4A-D and a Kᵢ of 0.52 μM against human KDM4C. Zavondemstat L-lysine induces cell apoptosis, causes S-phase cell cycle arrest, reduces the population of tumor-initiating cells and inhibits cancer cell proliferation. Zavondemstat L-lysine suppresses tumor growth and induces tumor regression in mouse xenograft models. Zavondemstat L-lysine can be used for the research of various cancers including colorectal cancer, esophageal squamous cell carcinoma and triple-negative breast cancer .
|
-
-
- HY-16938R
-
|
5'-(Methylthio)-5'-deoxyadenosine (Standard); 5'-Deoxy-5'-(methylthio)adenosine (Standard); 5'-S-Methyl-5'-thioadenosine (Standard)
|
Reference Standards
Endogenous Metabolite
Apoptosis
Parasite
|
Metabolic Disease
Cancer
|
|
5'-Methylthioadenosine (Standard) is the analytical standard of 5'-Methylthioadenosine. This product is intended for research and analytical applications. 5'-Methylthioadenosine (5'-(Methylthio)-5'-deoxyadenosine) is a nucleoside generated from S-adenosylmethionine (SAM) during polyamine synthesis[1]. 5'-Methylthioadenosine suppresses tumors by inhibiting tumor cell proliferation, invasion, and the induction of apoptosis while controlling the inflammatory micro-environments of tumor tissue. 5'-Methylthioadenosine and its associated materials have striking regulatory effects on tumorigenesis[2].
|
-
-
- HY-A0020R
-
|
ED-71 (Standard); 2-(3-hydroxypropoxy)-1,25-dihydroxyvitamin D3 (Standard)
|
Reference Standards
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-W753201
-
|
5'-(Methylthio)-5'-deoxyadenosine-13C; 5'-Deoxy-5'-(methylthio)adenosine-13C; 5'-S-Methyl-5'-thioadenosine-13C
|
Isotope-Labeled Compounds
Apoptosis
Parasite
Endogenous Metabolite
|
Cancer
|
|
5'-Methylthioadenosine- 13C (5'-(Methylthio)-5'-deoxyadenosine- 13C) is the 13C-labeled 5'-Methylthioadenosine (HY-16938). 5'-Methylthioadenosine (5'-(Methylthio)-5'-deoxyadenosine) is a nucleoside generated from S-adenosylmethionine (SAM) during polyamine synthesis . 5'-Methylthioadenosine suppresses tumors by inhibiting tumor cell proliferation, invasion, and the induction of apoptosis while controlling the inflammatory micro-environments of tumor tissue. 5'-Methylthioadenosine and its associated materials have striking regulatory effects on tumorigenesis .
|
-
-
- HY-177796
-
|
|
Apoptosis
CDK
Caspase
PARP
|
Cancer
|
|
TMLB-C16 is a potent and orally active B3GAT3 inhibitor with a KD of 3.962 μM. TMLB-C16 suppresses proliferation and migration, and induces cell cycle arrest and apoptosis in MHCC-97H (IC50 = 6.53 μM) and HCCLM3 cells (IC50 = 6.22 μM). TMLB-C16 inhibits tumor growth in both MHCC-97H and HCCLM3 xenograft tumor mouse models without causing obvious toxicity. TMLB-C16 can be used for hepatocellular carcinoma research .
|
-
-
- HY-N6950R
-
|
|
Reference Standards
PI3K
Akt
mTOR
Parasite
Apoptosis
|
Infection
Cancer
|
|
Hederacolchiside A1 (Standard) is the analytical standard of Hederacolchiside A1. This product is intended for research and analytical applications. Hederacolchiside A1, isolated from Pulsatilla chinensis, suppresses proliferation of tumor cells by inducing apoptosis through modulating PI3K/Akt/mTOR signaling pathway . Hederacolchiside A1 has antischistosomal activity, affecting parasite viability both in vivo and in vitro .
|
-
-
- HY-N0448R
-
|
|
Reference Standards
Others
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
10-Gingerol (Standard) is the analytical standard of 10-Gingerol (HY-N0448). This product is intended for research and analytical applications. 10-Gingerol is an AMPK agonist, which is found in the ginger oleoresin from fresh rhizome with anti-inflammatory, antioxidant and anti-proliferative activities. 10-Gingerol suppresses neointimal hyperplasia and inhibits vascular smooth muscle cell proliferation. 10-Gingerol exhibits substantial scavenging activities with an IC50 value of 10.47 μM against DPPH radical, an IC50 value of 1.68 μM against superoxide radical and an IC50 value of 1.35 μM against hydroxyl radical. 10-Gingerol inhibits the proliferation of MDA-MB-231 tumor cell line with an IC50 of 12.1 μM. 10-Gingerol suppresses the proliferation, migration, invasion, and induced apoptosis through targeting the PI3K/Akt signaling pathway in MDA-MB-231/IR cells. 10-Gingerol is promising for research of ulcerative colitis .
|
-
-
- HY-175010
-
|
|
STAT
Apoptosis
Bcl-2 Family
Caspase
|
Cancer
|
|
STAT3-IN-44 is a potent STAT3 inhibitor with IC50s of 1.84 (C6 cells) and 4.81 μM (A549 cells). STAT3-IN-44 inhibits STAT3 phosphorylation, downregulates Bcl-2, and upregulates Caspase-3 to promote late-stage apoptosis. STAT3-IN-44 significantly suppresses tumor cell proliferation and migration. STAT3-IN-44 can be used for the study of cancers such as glioma and lung cancer .
|
-
-
- HY-175733
-
|
|
RIO Kinase
Apoptosis
|
Cancer
|
|
CQ3196 is an orally active RIOK2 inhibitor with a Kd of 14 nM. CQ3196 effectively inhibits the ATPase activity of RIOK2, with an IC50 value of 72 nM. CQ3196 inhibits cell proliferation and colony formation in gastric cancer cell lines. CQ3196 induces cell apoptosis in HGC-27 and AGS cells. CQ3196 suppresses downstream signal pathway of RIOK2. CQ3196 reduces phosphorylation of mTOR and AKT. CQ3196 modulates ribosome function and protein synthesis. CQ3196 inhibits tumor growth and can be used for gastric cancer invtro and invivo research .
|
-
-
- HY-178349
-
|
|
P-glycoprotein
Apoptosis
Autophagy
|
Cancer
|
|
P-gp inhibitor 30 is a potent P-gp inhibitor that reverses multidrug resistance in breast cancer by sensitizing resistant cells to Doxorubicin (ADM) (HY-15142). P-gp inhibitor 30 promotes apoptosis, induces autophagy, and suppresses proliferation, migration, and invasion of drug-resistant breast cancer cells when combined with ADM. P-gp inhibitor 30 inhibits breast tumor growth both in vitro and in vivo. P-gp inhibitor 30 can be used for drug-resistant breast cancer research .
|
-
-
- HY-173273
-
|
|
CDK
Apoptosis
DNA/RNA Synthesis
Akt
|
Cancer
|
|
YJZ5118 is a selective CDK12/CDK13 inhibitor with IC50 values of 39.5 nM and 26.4 nM. YJZ5118 suppresses transcription of DNA damage response genes and induces DNA damage in tumor cells. YJZ5118 inhibits proliferation and triggers apoptosis. YJZ5118 inhibits RNA polymerase II Ser2 phosphorylation and increases Akt pathway activity. YJZ5118 exhibits synergistic effects with Akt inhibitors. YJZ5118 can be used for the research of cancer, such as prostate cancer .
|
-
- HY-178343
-
|
|
Aurora Kinase
Apoptosis
|
Cancer
|
|
Aurora A-IN-5 is a potent and highly selective Aurora A inhibitor (IC50 = 0.02 μM), showing 362-fold selectivity for over Aurora B. Aurora A-IN-5 shows its selectivity through unique C−H/π interactions, enhanced hydrophobic contacts, an open binding pocket, and tighter protein packing. Aurora A-IN-5 suppresses Aurora A autophosphorylation, thereby inhibiting cancer cell proliferation by inducing G2/M phase arrest, triggering apoptosis, and suppressing colony formation. Aurora A-IN-5 inhibits tumor growth in MDA-MB-231 xenograft mouse models. Aurora A-IN-5 can be used for breast, cervical, prostate, and lymphoma cancer research .
|
-
- HY-131724
-
|
p-DDAP; p-Dodecylaminophenol
|
Apoptosis
|
Cancer
|
|
4-(Dodecylamino)phenol (p-DDAP) is an anticancer agent. 4-(Dodecylamino)phenol has anti-tumor activity and can suppress proliferation, arrest the cell cycle and induce apoptotic cell death. 4-(Dodecylamino)phenol can be used for the research of cancer, such as prostate cancer .
|
-
- HY-14716
-
|
|
DNA/RNA Synthesis
Raf
|
Cancer
|
|
CCT239065 is an orally available, effective inhibitor of the mutant protein kinase V600EBRAF (RAF) with anti-tumor activity. CCT239065 inhibits downstream signaling of V600EBRAF in cancer cells, blocking DNA synthesis and suppressing proliferation .
|
-
- 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 .
|
-
- HY-174321
-
|
|
p38 MAPK
PI3K
Akt
NF-κB
|
Cancer
|
|
A2073 is a flavagline derivative that potently inhibits the proliferation of erythroleukemia cells by causing cell cycle arrest and suppressing the MAPK, NF-κB, and PI3K signaling pathways. A2073 formes stable interactions with cell cycle-related proteins (CDK1, CCNA2, PRIM1). A2073 exhibits significant anti-proliferative activity against tumor cells while maintaining a favorable toxicity profile in a zebrafish xenograft tumor model. A2073 can be used for the study of acute erythroleukemia.
|
-
- HY-148807C
-
|
QC8222 sodium; TACH 101 sodium
|
Apoptosis
Histone Demethylase
|
Cancer
|
|
Zavondemstat (QC8222; TACH 101) sodium is an orally active pan-KDM4 inhibitor, with a IC50 ≤ 0.08 μM against human KDM4A-D and a Kᵢ of 0.52 μM against human KDM4C. Zavondemstat sodium induces cell apoptosis, causes S-phase cell cycle arrest, reduces the population of tumor-initiating cells and inhibits cancer cell proliferation. Zavondemstat sodium suppresses tumor growth and induces tumor regression in mouse xenograft models. Zavondemstat sodium can be used for the research of various cancers including colorectal cancer, esophageal squamous cell carcinoma and triple-negative breast cancer .
|
-
- HY-12965B
-
|
|
TAM Receptor
|
Cancer
|
|
(Z)-S49076 hydrochloride is an orally active inhibitor of MET and AXL that blocks the downstream signaling of these receptors both in vitro and in vivo, inhibiting the proliferation and migration of tumor cells and suppressing tumor growth in xenograft models. (Z)-S49076 hydrochloride is capable of overcoming the resistance to epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs) due to MET amplification in Erlotinib (HY-50896)-resistant cell lines both in vitro and in vivo. (Z)-S49076 hydrochloride can be used for research in non-small cell lung cancer (NSCLC) .
|
-
- HY-178921
-
|
|
Drug Derivative
Apoptosis
|
Cancer
|
HJ-4 is a Piperine (HY-N0144) derivative. HJ-4 potently inhibits the proliferation of CRC cells by dose-dependently reducing colony formation and DNA synthesis. HJ-4 markedly suppresses the adhesion, migration, invasion and induces apoptosis of CRC cells. HJ-4 demonstrates anti-tumor efficacy in chicken embryo chorioallantoic membrane (CAM) model implanted with HCT116/SW480 tumor spheroids. HJ-4 can be used for the study of colorectal cancer (CRC) .
|
-
- HY-173065
-
|
|
CDK
Apoptosis
|
Cancer
|
|
CDK9-IN-36 (Compound T7) is a potent, selective and metabolically stable CDK9 inhibitor with an IC50 value of 1.2 nM. CDK9-IN-36 effectively suppresses cell proliferation, reduces colony formation, and induces apoptosis in Osimertinib (HY-15772)-resistant NSCLC cells by downregulating Mcl-1. CDK9-IN-36 also demonstrates antitumor efficacy in a tumor xenograft model .
|
-
- HY-175820
-
|
|
VEGFR
ERK
Apoptosis
EGFR
|
Cancer
|
|
AGW-11 is a potent dual inhibitor of EGFR (IC50 = 556 nM) and VEGFR2 (IC50 = 289.7 nM). AGW-11 induces apoptosis and suppresses phosphorylation of EGFR, VEGFR2, and ERK1/2 in HUVECs. AGW-11 effectively inhibits cancer cell growth, reduces HUVEC proliferation, tube formation, and invasion, thereby blocking angiogenesis. AGW-11 significantly suppresses tumor growth and decreases lung metastasis in a 4T1 xenograft mouse model. AGW-11 can be used for the study of breast cancer .
|
-
- HY-16938S2
-
|
5'-(Methylthio)-5'-deoxyadenosine-13C5; 5'-Deoxy-5'-(methylthio)adenosine-13C5; 5'-S-Methyl-5'-thioadenosine-13C5
|
Isotope-Labeled Compounds
Endogenous Metabolite
Apoptosis
Parasite
|
Metabolic Disease
Cancer
|
|
5'-Methylthioadenosine- 13C5 (5'-(Methylthio)-5'-deoxyadenosine- 13C5) is the 13C--labeled 5'-Methylthioadenosine (HY-16938). 5'-Methylthioadenosine (5'-(Methylthio)-5'-deoxyadenosine) is a nucleoside generated from S-adenosylmethionine (SAM) during polyamine synthesis . 5'-Methylthioadenosine suppresses tumors by inhibiting tumor cell proliferation, invasion, and the induction of apoptosis while controlling the inflammatory micro-environments of tumor tissue. 5'-Methylthioadenosine and its associated materials have striking regulatory effects on tumorigenesis .
|
-
- HY-164551
-
|
|
VEGFR
STAT
ERK
Apoptosis
|
Cancer
|
YLL545 is a type of vascular endothelial growth factor receptor 2 (VEGFR2) inhibitor. YLL545 can inhibit VEGF-induced phosphorylation of VEGFR2 and the activation of downstream signaling factors (like phosphorylated STAT3 and phosphorylated ERK1/2) in human umbilical vein endothelial cells (HUVEC). YLL545 can suppress the proliferation, migration, invasion, and angiogenesis of HUVEC. YLL545 can induce apoptosis in breast cancer mice and inhibit tumor growth .
|
-
- HY-13464R
-
|
Brigatinib analog (Standard)
|
Reference Standards
Anaplastic lymphoma kinase (ALK)
EGFR
|
Cancer
|
|
ALK-IN-1 (Standard) is the analytical standard of ALK-IN-1 (Brigatinib analog) (HY-13464). This product is intended for research and analytical applications. ALK-IN-1 is an ALK and EGFR inhibitor. ALK-IN-1 binds to and inhibits ALK kinase, ALK fusion proteins, and wild-type and mutant EGFR variants, thereby disrupting their corresponding signaling pathways. ALK-IN-1 can suppress the growth and proliferation of tumor cells and exhibits potential inhibitory activity against mutant EGFR. ALK-IN-1 can be used in the research of non-small-cell lung cancer .
|
-
- HY-179049
-
|
|
EGFR
Microtubule/Tubulin
Akt
ERK
Autophagy
Atg8/LC3
p62
Ferroptosis
Reactive Oxygen Species (ROS)
|
Cancer
|
|
EGFR/tubulin-IN-1 (Compound 26) is a dual-target inhibitor of EGFR and tubulin. EGFR/tubulin-IN-1 significantly reduces the levels of p-EGFR, p-AKT, and p-ERK in cells, disrupting the microtubule structure of the cells. EGFR/tubulin-IN-1 significantly inhibits the proliferation of H1975 cells and significantly blocks the cells in the G2/M phase. EGFR/tubulin-IN-1 induces the expression of autophagy markers LC3B-II and Beclin-1, while down-regulating the expression of p62. EGFR/tubulin-IN-1 induces ferroptosis, with increased ROS content and depletion of glutathione (GSH). EGFR/tubulin-IN-1 inhibits epithelial-mesenchymal transition (EMT) and tumor metastasis. EGFR/tubulin-IN-1 has a significant tumor-suppressing effect in the H1975 transplanted tumor nude mouse model. EGFR/tubulin-IN-1 can be used for the study of non-small cell lung cancer .
|
-
- HY-162772
-
|
|
Isocitrate Dehydrogenase (IDH)
Apoptosis
|
Cancer
|
|
IDH1/2-IN-1 (Compound 6b) serves as a dual inhibitor of IDH1(R132H)/IDH2(R140Q) with IC50 values of 0.22 μM and 1.6 μM, respectively. IDH1/2-IN-1 effectively inhibits tumor growth by suppressing tumor cell proliferation and enhancing host defense through the activation of antioxidant enzymes. Additionally, IDH1/2-IN-1 reduces inflammation and promotes apoptosis, demonstrating robust antitumor activity. IDH1/2-IN-1 holds potential for research in leukemia .
|
-
- HY-183186
-
|
|
METTL3
Cytochrome P450
|
Cancer
|
|
EP102 is an orally active, selective inhibitor of the METTL3/METTL14 complex with an IC50 of 2 nM. EP102 reduces intracellular N6-methyladenosine levels, inhibits cancer cell proliferation, and thereby suppresses tumor growth in mouse models. EP102 is applicable for the research of acute myeloid leukemia, ovarian solid tumors and advanced solid tumors .
|
-
- HY-182082
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
XYD270 is an orally active BRD9 PROTAC degrader. XYD270 inhibits the proliferation of cancer cells. XYD270 suppresses tumor growth in a mouse model of acute myeloid leukemia. XYD270 can be used in research related to synovial sarcoma and acute myeloid leukemia .
|
-
- HY-183098
-
|
|
PROTACs
IKK
Apoptosis
|
Cancer
|
|
UNC8209 is a selective PROTAC-based TANK-binding kinase 1 (TBK1) degrader. UNC8209 recruits cereblon (CRBN) to mediate ubiquitin-proteasome pathway-dependent TBK1 degradation and reduces AAK1, GAK, and AURKA abundance. UNC8209 suppresses tumor cell proliferation, impairs in vivo tumor growth, inhibits colony and clonogenic growth and enhances tumor cell sensitivity to TNFα or IFN-γ. UNC8209 modulates cell cycle and induces mild apoptosis. UNC8209 can be used for the research of clear cell renal cell carcinoma, non-small cell lung cancer, pancreatic ductal adenocarcinoma .
|
-
- HY-183758
-
|
|
Nuclear Hormone Receptor 4A/NR4A
Apoptosis
|
Cancer
|
|
Nur77 modulator 6 is a Nur77 modulator with a Kd of 0.40 μM. Nur77 modulator 6 functionally modulates Nur77 to induce mitotic arrest and apoptosis in colorectal tumor cells. Nur77 modulator 6 suppresses colorectal cancer cell proliferation via Nur77-dependent mitotic arrest induction. Nur77 modulator 6 exhibits anti-proliferative activity against colorectal tumor cells. Nur77 modulator 6 can be used for the research of colorectal cancer .
|
-
- HY-183937A
-
|
|
PROTACs
Phosphatase
STAT
|
Cancer
|
|
PD-305 is a selective PTPN2 PROTAC degrader, with DC50 values of 0.25 nM and 5.11 nM against PTPN2 and PTPN1, respectively. PD-305 enhances IFN-γ-induced STAT1 phosphorylation, inhibits the proliferation of IFN-γ-stimulated colorectal cancer cells, promotes CD8 + T cell activation, enhances the tumor-killing activity of T cells, and suppresses tumor growth in mouse models. PD-305 can be used for the research of colorectal cancer .
|
-
- HY-181427
-
|
|
Androgen Receptor
|
Cancer
|
|
UT-143 is an orally active, selective irreversible covalent antagonist of androgen receptor (AR). UT-143 inhibits the proliferation of AR-positive prostate cancer cells, reduces the weight of androgen target tissues in rats, and suppresses the growth of AR-positive xenograft tumors. UT-143 can be used for the research of prostate cancer .
|
-
- HY-177957
-
|
|
CDK
|
Cancer
|
|
CDK2-IN-52 (Compound Cpb No 39) is a selective cyclin-dependent kinase 2 (CDK2) inhibitor with a DC50 value of 1-10 nM. CDK2-IN-52 induces cell cycle arrest and suppresses tumor cell proliferation. CDK2-IN-52 is promising for research of CDK2-overexpressing malignancies such as breast and ovarian cancers .
|
-
- HY-N19830
-
|
|
Reactive Oxygen Species (ROS)
Apoptosis
|
Cancer
|
|
Guavenoic acid is a triterpenoid compound that can be isolated from fresh leaves of Psidium guajava. Guavenoic acid protects cells in cellular oxidative damage models, inhibits intracellular ROS production, and suppresses cell apoptosis. Guavenoic acid significantly enhances cellular proliferation, promotes insulin synthesis and secretion, and upregulates the messenger RNA expression of insulin gene, PDX-1 and MafA. Guavenoic acid can be used in the research of diseases such as pancreatic islet β-cell tumors .
|
-
- HY-181970
-
|
|
Orphan Nuclear Receptor
Androgen Receptor
c-Myc
|
Cancer
|
|
XY25026 is an orally active LRH-1 inhibitor with an IC50 of 0.28 μM. XY25026 inhibits the proliferation of androgen receptor (AR)-positive prostate cancer cells, suppresses the expression of AR target genes KLK2 and KLK3, and inhibits tumor growth in xenograft models. XY25026 is applicable to the research of castration-resistant prostate cancer .
|
-
- HY-P991530
-
|
|
Biochemical Assay Reagents
|
Inflammation/Immunology
Cancer
|
|
YH004 is an anti-CD137 agonistic monoclonal antibody, with immunostimulating and antineoplastic activities. YH004 activates CD137 expressed on a variety of leukocyte subsets including activated T lymphocytes and natural killer cells. YH004 enhances CD137-mediated signaling and induces cytotoxic T-lymphocyte (CTL) proliferation, cytokine production and promotes anti-tumor response mediated by CTL. YH004 induces NK-mediated tumor cell killing and suppresses the immunosuppressive activity of regulatory T cells. YH004 can be studied in anticancer research .
|
-
- HY-153503
-
|
|
Anaplastic lymphoma kinase (ALK)
Insulin Receptor
|
Cancer
|
|
ALK-IN-24 is an orally active ALK inhibitor with an IC50 value of 1.7 nM. ALK-IN-24 also inhibits insulin receptor kinase with an IC50 value of 6 nM. ALK-IN-24 suppresses the proliferation of lung adenocarcinoma cells. ALK-IN-24 inhibits ALK-driven tumor growth in xenograft mouse models. ALK-IN-24 can be used in research related to non-small cell lung cancer .
|
-
- HY-181250
-
|
|
SHP2
|
Cancer
|
|
SHP2-IN-46 is an orally active SHP2 inhibitor (IC50 = 11.76 μM). SHP2-IN-46 inhibits SHP2 enzymatic activity and mediates anti-tumor activity. SHP2-IN-46 suppresses cell proliferation in various cancer cells. SHP2-IN-46 can be used in research related to lung adenocarcinoma, pancreatic cancer and hepatoblastoma .
|
-
- HY-181675
-
|
|
Microtubule/Tubulin
Apoptosis
Bcl-2 Family
Caspase
|
Cancer
|
|
CHNQD-01522 is a microtubule inhibitor targeting the colchicine binding site on β-tubulin. CHNQD-01522 binds to the colchicine binding site on β-tubulin, inhibits microtubule polymerization, and evades P-glycoprotein transport in cancer cells. CHNQD-01522 inhibits proliferation, suppresses tumor cell colony formation, arrests cell cycle in G2/M phases, and induces apoptosis in cancer cells. CHNQD-01522 upregulates of Bax and activation of caspase-9 and caspase-3. CHNQD-01522 shows anti-tumor efficacy in subcutaneous and orthotopic hepatocellular carcinoma xenograft tumor models. CHNQD-01522 can be used for the research of hepatocellular carcinoma .
|
-
- HY-180995
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
VARS1-IN-1 is a valyl-tRNA synthetase (VARS1) inhibitor with a Kd of 0.213 μM. VARS1-IN-1 suppresses VARS1’s tRNA aminoacylation activity, reduces charged levels of valine tRNAs and redues total protein synthesis rate. VARS1-IN-1 suppresses aggressive tumor growth and cell proliferation in PC3 prostate cancer xenograft models. VARS1-IN-1 can be used for the research of prostate cancer .
|
-
- HY-181694
-
|
|
Topoisomerase
HDAC
Apoptosis
Kinesin
RAD51
|
Cancer
|
|
SeSA-HCPT is an orally active dual-target inhibitor integrating Topo I and HDAC inhibition. SeSA-HCPT induces potent DNA damage, apoptosis, S-phase arrest in prostate cancer cells. SeSA-HCPT inhibits cancer cells proliferation and migration. SeSA-HCPT impairs homologous recombination by suppressing KIF4A-RAD51 signaling. SeSA-HCPT markedly inhibits CRPC tumor growth with minimal systemic toxicity .
|
-
- HY-181834
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
PROTAC MLLT1 Degrader-1 is a PROTAC degrader targeting MLLT1. PROTAC MLLT1 Degrader-1 inhibits AML cell proliferation and viability, suppresses tumor growth in human AML xenograft models, and can block the oncogene transcriptional program. PROTAC MLLT1 Degrader-1 can be used for the research of MLL-rearranged acute myeloid leukemia (AML) .
|
-
- HY-P991999
-
|
|
FGFR
IFNAR
Interleukin Related
|
Cancer
|
|
OM-RCA-01 is an anti-FGFR1 monoclonal antibody with a Kd of 1.59 nM for human FGFR1. OM-RCA-01 inhibits the phosphorylation of FGFR1, blocks FGF-mediated signaling pathways, and suppresses the proliferation of downstream tumor cells. OM-RCA-01 delays tumor growth in lung cancer and renal cancer xenograft models expressing FGFR1. When combined with Nivolumab, OM-RCA-01 enhances the release of IFN-γ and IL-2. OM-RCA-01 is applicable for the research of lung cancer and renal cell carcinoma .
|
-
- HY-182064
-
|
|
EGFR
NO Synthase
COX
NF-κB
Interleukin Related
Apoptosis
|
Cancer
|
|
EGFR-IN-206 is an orally active EGFR inhibitor. EGFR-IN-206 inhibits the phosphorylation of the key tumor growth protein EGFR, and suppresses the proliferation, migration and invasion of EGFR triple-mutant tumor cell lines. EGFR-IN-206 downregulates the expression of inflammation-related proteins iNOS, COX-2 and NF-κB (p65). EGFR-IN-206 promotes the secretion of NO. EGFR-IN-206 reduces the secretion of IL-6. EGFR-IN-206 induces apoptosis (apoptosis) of EGFR triple-mutant tumor cells. EGFR-IN-206 exerts antitumor activity in EGFR triple-mutant mice. EGFR-IN-206 is applicable to the research of non-small cell lung cancer .
|
-
- HY-181541
-
|
|
HDAC
Apoptosis
Wnt
β-catenin
MDM-2/p53
c-Myc
|
Cancer
|
|
HIT211504993 is a selective histone deacetylase 6 (HDAC6) inhibitor with an IC50 of 0.070 μM. HIT211504993 suppresses cancer cell proliferation, cause G1 phase cell cycle arrest and induces apoptosis. HIT211504993 inhibits Myc-driven tumorigenesis via nucleocytoplasmic acetylation, p53 modulation, and Wnt/β-catenin signaling modulation. HIT211504993 inhibits tumor growth in a colon cancer xenograft mouse model. HIT211504993 can be used for the research of colon cancer .
|
-
- HY-180260
-
|
|
Reactive Oxygen Species (ROS)
|
Cancer
|
|
Anticancer agent 289 is a H2O2-responsive anticancer prodrug. Anticancer agent 289 exhibits H2O2-inducible DNA-alkylating activity, selectively inhibits the proliferation of high ROS-expressing cancer cells over nonmalignant cells, markedly suppresses tumor growth without observable toxicity in vivo. Anticancer agent 289 can be used for triple-negative breast cancer (TNBC) research .
|
-
- HY-182744
-
|
|
MDM-2/p53
|
Cancer
|
|
LLQ-45 is a covalent p53 Y220C mutant protein agonist with an EC50 of 24.97 μM. LLQ-45 activates the anti-tumor function of p53 Y220C through covalent modification, restores its DNA-binding ability and enhances its thermal stability. LLQ-45 selectively inhibits the proliferation of p53 Y220C mutant tumor cells, suppresses cell growth and upregulates the expression of CDKN1A. LLQ-45 can be used in studies related to p53 Y220C mutant cancers .
|
-
- HY-118273
-
|
|
Integrin
|
Inflammation/Immunology
Cancer
|
|
IPS-05002 is an α5β1 antagonist. IPS-05002 can inhibit VEGF-stimulated human umbilical vein endothelial cell (HUVEC) proliferation, adhesion, and migration, and also suppresses tubular network formation. IPS-05002 can upregulate IKB-β, XRCC4, and downregulate Cdc6 in VEGF-induced HUVECs. IPS-05002 can be used for the study of tumor angiogenesis .
|
-
- HY-181669
-
|
|
Histone Acetyltransferase
c-Myc
|
Cancer
|
|
P300-IN-6 is an orally active histone acetyltransferase p300 HAT domain inhibitor with human IC50 values of 7 nM. P300-IN-6 suppresses c-Myc expression, decreases H3K18ac and H3K27ac levels, and inhibits cancer cell proliferation.P300-IN-6 suppresses tumor growth in xenograft mouse models.P300-IN-6 can be used for the research of multiple myeloma .
|
-
- HY-181723
-
|
|
PARP
Bcl-2 Family
Apoptosis
|
Cancer
|
|
Anticancer agent 304 is an anticancer agent. Anticancer agent 304 binds to CDC45 with a Kd value of 83.0 μM. Anticancer agent 304 arrests the cell cycle of liver cancer cells at the G2/M phase, induces Apoptosis by upregulating C-PARP-1 and downregulating PARP-1 and BCL-2, and inhibits the migration, invasion and proliferation of liver cancer cells. Anticancer agent 304 suppresses tumor growth in animal models of hepatocellular carcinoma. Anticancer agent 304 is applicable to research related to liver cancer .
|
-
- HY-181147
-
|
|
PROTACs
HSP
|
Cancer
|
|
PROTAC HSP70 Degrader-1 (compound C4) is a cytosolic HSP70 PROTAC degrader that can engage CRBN to form a ternary complex. PROTAC HSP70 Degrader-1 mediates ubiquitination and proteasomal degradation of cytosolic HSP70. PROTAC HSP70 Degrader-1 exhibits cytotoxic activity against cancer cells, suppressing tumor cell proliferation and inducing apoptosis in combination with DTHIB. PROTAC HSP70 Degrader-1 can be used for the research of colon cancer and leukemia .
|
-
- HY-183682
-
|
|
EGFR
p38 MAPK
ERK
Akt
|
Cancer
|
|
AZ14289671 is an orally active, blood-brain barrier-penetrant tyrosine kinase (tyrosine kinase) inhibitor (TKI) that specifically targets non-small cell lung cancer (NSCLC) harboring EGFR exon 20 insertion mutations (EGFR Exon20Ins), while largely sparing wild-type EGFR to reduce off-target toxicities such as rash and diarrhea. AZ14289671 inhibits the downstream MAPK/ERK/AKT pathway, suppressing tumor cell proliferation, survival and migration. AZ14289671 can be used for NSCLC research .
|
-
- HY-180200
-
|
|
Ras
ERK
|
Cancer
|
|
RNK08954 is an orally active KRASG12D inhibitor with a Kd of 0.0395 nM. RNK08954 selectively binds the inactive GDP-bound KRASG12D form, suppresses downstream KRAS-mediated signaling pathways p-ERK1/2 experssion. RNK08954 inhibits KRASG12D-mutant cell proliferation, induces G0-G1 cell cycle arrest, and inhibits tumor growth in mouse xenograft models. RNK08954 can be used for the research of non-small cell lung cancer, pancreatic ductal adenocarcinoma .
|
-
- HY-180281
-
|
|
Zinc Finger Protein
Apoptosis
PI3K
Akt
|
Cancer
|
|
PLAGL2-IN-1 is a inhibitor of pleiomorphic adenoma-like protein 2 (PLAGL2) with a Kd of 2.23 µM. PLAGL2-IN-1 suppresses PLAGL2 transcriptional activity, induces G0/G1 cell cycle arrest, and apoptosis, thereby inhibiting hepatocellular carcinoma (HCC) cell proliferation. PLAGL2-IN-1 disrupts extracellular matrix organization and suppresses the PI3K-AKT pathway by reducing AKT phosphorylation. PLAGL2-IN-1 inhibits tumor growth in an HCCLM3 xenograft mouse model. PLAGL2-IN-1 can be used for the research of HCC .
|
-
- HY-181869
-
|
|
PROTACs
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
PROTAC BET Degrader-17 is a potent BET protein PROTAC degrader. By recruiting the VHL E3 ligase, PROTAC BET Degrader-17 specifically degrades BRD2, BRD3 (DC50=0.09 nM) and BRD4 (IC50=4.3 nM). PROTAC BET Degrader-17 exhibits strong anti-tumor activity in acute myeloid leukemia (AML) studies; it not only inhibits cancer cell proliferation, induces cell cycle arrest and apoptosis, but also effectively suppresses tumor growth in xenograft mouse models. PROTAC BET Degrader-17 can be used to explore targeted therapies for acute myeloid leukemia .
|
-
- HY-P992401
-
|
|
EGFR
CD3
PI3K
Akt
p38 MAPK
Caspase
Apoptosis
IFNAR
TNF Receptor
Interleukin Related
|
Cancer
|
|
M802 is an anti-HER2/CD3 bispecific antibody, with a Kd of 0.578 nM for human HER2 and a Kd of 71.2 nM for human CD3. M802 inhibits the PI3K/AKT and MAPK signaling pathways, suppresses tumor cell proliferation, activates caspase-3, and promotes tumor cell apoptosis (apoptosis). M802 recruits and activates CD3-positive immune cells, mediates cytotoxicity against HER2-positive tumor cells, and induces immune cells to secrete IFN-γ, TNF-α, IL-2 and IL-6. M802 exhibits anti-tumor efficacy in mice with gastric cancer xenografts. M802 can be used in research related to HER2-positive breast cancer, HER2-positive gastric cancer and other cancers. The recommended isotype control is human IgG1 kappa (HY-P99001) .
|
-
- HY-171824
-
|
|
PROTACs
c-Met/HGFR
Apoptosis
|
Cancer
|
|
PROTAC c-Met Degrader-4 (compound D15) is a potent orally active PROTAC c-MET degrader. PROTAC c-Met Degrader-4 demonstrates excellent intracellular degradation potency with a DC50 < 0.5 nM. PROTAC c-Met Degrader-4 induces cell cycle arrest and apoptosis, inhibits cell invasion and migration, thereby suppressing cell proliferation. PROTAC c-Met Degrader-4 inhibits the growth of Hs746T xenograft tumors in nude mice. PROTAC c-Met Degrader-4 can be used for cancer research, such as non-small cell lung cancer and gastric cancer .
|
-
- HY-185075
-
|
LY4050784
|
SWI/SNF Complex
|
Cancer
|
|
FHD-909 (LY4050784) is an orally active and selective SMARCA2 (BRM) ATPase inhibitor. FHD-909 potently inhibits purified BRM ATPase with an IC50 of 0.0025 μM and exhibits 35.69-fold selectivity for BRM over purified SMARCA4 (BRG1) ATPase. FHD-909 induces synthetic lethality, suppresses cell proliferation, modulates target gene expression, and achieves remarkable tumor growth inhibition and regression in SMARCA4-mutant cancer cells and xenograft models. FHD-909 can be used for the research of SMARCA4/BRG1-mutant cancers, advanced solid tumors, and BAF complex-related disorders .
|
-
- HY-P992200
-
|
|
Transmembrane Glycoprotein
PI3K
Akt
p38 MAPK
NF-κB
MMP
Apoptosis
Caspase
Bcl-2 Family
|
Cardiovascular Disease
Cancer
|
|
Anti-CD146 Antibody (AA98) is an antibody targeting CD146 and an angiogenesis inhibitor. Anti-CD146 Antibody (AA98) blocks the dimerization of CD146 as well as its downstream PI3K/AKT, p38 MAPK and NF-κB signaling pathways; it inhibits the expression of MMP9 and ICAM1, epithelial-mesenchymal transition (EMT), and the proliferation, migration and tube formation of endothelial cells. Anti-CD146 Antibody (AA98) enhances radiation-induced cancer cell apoptosis and survival inhibition, reduces tumor microvessel density, and suppresses tumor growth, invasion and vasculogenic mimicry. Anti-CD146 Antibody (AA98) can be used in research related to cervical cancer, liver cancer, malignant phyllodes tumor of the breast, uveal melanoma, leiomyosarcoma, pancreatic cancer, other tumors and angiogenesis .
|
-
- HY-180885S
-
|
|
Ras
ERK
|
Cancer
|
|
KRAS G12D-IN-35 (example 7) is a potent and orally active KRAS G12D inhibitor. KRAS G12D-IN-35 suppresses p-ERK in AGS cells and potently inhibits the proliferation of various KRAS G12D-mutant cancer cell lines. KRAS G12D-IN-35 inhibits tumor growth in HPAC and GP2D mouse models. KRAS G12D-IN-35 can be used for cancer research, such as pancreatic and colorectal cancer .
|
-
- HY-186045
-
|
|
Histone Methyltransferase
Apoptosis
DNA/RNA Synthesis
ATP-binding cassette (ABC) transporters
|
Cancer
|
|
SKLB06489 is a selective and orally active inhibitor of type I PRMT enzymes, with IC50 values of 64.55 nM (PRMT1), 4.21 nM (PRMT6), and 51.27 nM (PRMT8). SKLB06489 inhibits cell proliferation, colony formation, DNA replication, and DNA damage repair in cancer cells. SKLB06489 induces G0/G1-phase cell cycle arrest and apoptosis in cancer cells. SKLB06489 enhances intracellular cholesterol efflux via ABCA1 and ABCG1 upregulation, disrupts cholesterol metabolic homeostasis, and suppresses tumor growth in subcutaneous xenograft models. SKLB06489 can be used for the research of triple-negative breast cancer (TNBC) .
|
-
- HY-105369
-
|
|
Anaplastic lymphoma kinase (ALK)
Apoptosis
|
Cancer
|
|
KF-20444 is an orally active ALK inhibitor with blood-brain barrier penetration. KF-20444 exhibits strong inhibitory activity against ALK fusion proteins (EML4-ALK) and ALK resistance mutations (including L1196M, G1202R, and F1174L). KF-20444 effectively suppresses the phosphorylation of ALK in ALK-driven cancer cell lines, thereby inhibiting cancer cell proliferation and inducing apoptosis. KF-20444 demonstrates anti-tumor efficacy in mouse models bearing ALK-positive non-small cell lung cancer (NSCLC) or neuroblastoma. KF-20444 can be used for the study of ALK-driven malignancies .
|
-
- HY-182331
-
|
|
PROTACs
RAR/RXR
Androgen Receptor
Apoptosis
Caspase
MDM-2/p53
|
Cancer
|
|
WCF-598 is a RXRγ (Kd: 234.2 nM) PROTAC degrader. WCF-598 induces RXRγ degradation via the ubiquitin-proteasome pathway and binds directly to RXRγ. WCF-598 indirectly induces AR-V7 degradation, impairs the stability of the RXRγ-AR-V7 complex, downregulates AR-V7 levels, and inhibits the transcription of downstream target genes of AR-V7. WCF-598 induces tumor cell apoptosis, inhibits cell proliferation, activates the p53 signaling pathway, and suppresses cell cycle progression. WCF-598 can be used for the research of prostate cancer .
|
-
- HY-12929
-
|
SU093
|
Pim
Apoptosis
|
Cancer
|
|
NSC756093 (SU093) is a GBP1:PIM1 interaction inhibitor. NSC756093 binds to GBP1-PIM1 with a Kd of 38 nM. NSC756093 suppresses proliferation, reduces migration, induces G1 phase cell-cycle arrest, and increases apoptotic cell death in ovarian cancer cells. NSC756093 reduces cellular proteasomal activity, induces accumulation of ubiquitinated proteins, and restrains tumor progression and lung metastasis in murine ovarian cancer xenograft models. NSC756093 increases sensitivity of prostate cancer cells to Docetaxel (HY-B0011) and sensitizes GBP1-overexpressing ovarian cancer cells to Paclitaxel (HY-B0015). NSC756093 can be used for the research of prostate cancer and ovarian cancer .
|
-
- HY-178373
-
|
|
Topoisomerase
DNA/RNA Synthesis
Reactive Oxygen Species (ROS)
MDM-2/p53
Caspase
|
Cancer
|
|
Topoisomerase I-IN-18, a derivative of Thiosemicarbazide (HY-Y0032), is a Topoisomerase I inhibitor. Topoisomerase I-IN-18 can disrupt DNA synthesis and transcription. Topoisomerase I-IN-18 inhibits tumor cell proliferation by inducing S-phase cell cycle arrest. Topoisomerase I-IN-18 can enhance mitochondria-mediated apoptosis, suppress cell migration, and increase intracellular Reactive Oxygen Species (ROS) levels. Topoisomerase I-IN-18 can increase p53 protein expression, γH2AX phosphorylation, upregulate Bax expression, downregulate Bcl-2 expression, and activate the caspase cascade. Topoisomerase I-IN-18 can be used for the study of lung cancer .
|
-
- HY-176128
-
|
|
PROTACs
Androgen Receptor
Apoptosis
PARP
Caspase
|
Cancer
|
|
BWA-6047 is an oral active PROTAC degrader targeting AR/AR-V7 and GSPT1 with DC50 values of 3.7, 3.0 and 1.2 nM in 22Rv1 cells. BWA-6047 suppresses the expression of AR downstream target genes and and transcriptional activity. BWA-6047 inhibits cancer cells proliferation, causes G1 phase cell cycle arrest and induces apoptosis. BWA-6047 increases cleaved-PARP-1 and cleaved-caspase-3 levels. BWA-6047 reduces growth of LNCaP xenograft tumors in mice models without obvious toxicity. BWA-6047 can be used for the research of prostate cancer .
|
-
- HY-156794
-
|
DSP-5336
|
Epigenetic Reader Domain
FLT3
|
Cancer
|
Enzomenib (DSP-5336) is an orally active Menin inhibitor (IC50=1.4 nM, Kd=6.0 nM). Enzomenib disrupts the interaction between Menin and KMT2A/MLL fusion proteins, specifically inhibits the expression of leukemia driver genes such as HOX/MEIS1, and upregulates ITGAM. Enzomenib effectively induces cell differentiation, inhibits tumor cell proliferation, and suppresses primitive cell colony formation. Enzomenib reduces disease burden and prolongs survival, but causes adverse reactions including differentiation syndrome and QTc interval prolongation. Enzomenib is used for research on relapsed/refractory acute myeloid leukemia, acute lymphoblastic leukemia, and other hematologic malignancies with mixed lineage leukemia (MLL) rearrangements or NPM1 mutations .
|
-
- HY-183728
-
|
|
YAP
|
Cancer
|
|
LC-TEAD01 is a potent covalent transcription enhancer-associated domain (TEAD) inhibitor with an IC50 of 116 nM and a Ki of 0.132 μM. LC-TEAD01 disrupts the TEAD-YAP interaction and inhibits TEAD-dependent transcriptional activity. LC-TEAD01 suppresses the proliferation of NF2-deficient cancer cells. LC-TEAD01 inhibits tumor growth in NF2-deficient xenograft models. LC-TEAD01 can be used in studies related to NF2-deficient malignant pleural mesothelioma .
|
-
- HY-N3005
-
|
|
Apoptosis
Autophagy
NOD-like Receptor (NLR)
Pyroptosis
|
Inflammation/Immunology
Cancer
|
|
Britannin is an NLRP3 inhibitor with an IC50 of 3.630 μM, exhibiting anti-inflammatory activity. Britannin inhibits the activation and assembly of the NLRP3 inflammasome by blocking the interaction between NLRP3 and NEK7. Additionally, Britannin demonstrates antitumor activity by inhibiting the proliferation of tumor cells through blocking the interaction between HIF-1α and Myc, thereby suppressing PD-L1 expression and enhancing cytotoxic T lymphocyte activity. Britannin can also induce apoptosis and autophagy in liver cancer cells by activating ROS-regulated AMPK. Britannin holds promise for research in the fields of anti-inflammatory and antitumor therapeutics .
|
-
- HY-181965
-
|
|
Ras
ERK
p38 MAPK
|
Cancer
|
|
KRAS G12C-IN-78 is a selective SWII-binding KRASG12C dual inhibitor targeting both inactive and active states. KRAS G12C-IN-78 rapidly inhibits ERK1/2 phosphorylation, induces covalent adduct formation with endogenous KRASG12C, suppresses MAPK pathway gene expression, and inhibits cellular proliferation in KRASG12C mutant cells. KRAS G12C-IN-78 can be used for the research of KRASG12C mutant solid tumors, including pancreatic ductal adenocarcinoma and non-small cell lung cancer .
|
-
- HY-182614
-
|
|
Src
Cathepsin
PI3K
Akt
Ras
Raf
ERK
MMP
|
Cancer
|
|
BJ-2302 is a Src kinase inhibitor with an IC50 of 3.23 μM, and inhibits cathepsin S (CTSS) activity .BJ-2302 binds to Src, suppresses PI3K/AKT and Ras/Raf/ERK pathways, and reduces CTSS and MMP-9 expression .BJ-2302 inhibits cancer cell invasion, metastasis, proliferation, and tumor growth .BJ-2302 does not induce cytotoxicity in normal breast epithelial cells .BJ-2302 can be used for the research of breast cancer and triple-negative breast cancer .
|
-
- HY-183643
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
RUVBL1/2-IN-1 is an orally active RUVBL1/2 complex inhibitor with an EC50 of 0.012 μM against human targets. RUVBL1/2-IN-1 impairs ATPase-related functions, thereby reducing nuclear MYC protein levels, impairing DNA damage response and inhibiting cancer cell proliferation. In a MYC-dependent Burkitt's lymphoma xenograft model, RUVBL1/2-IN-1 effectively inhibits tumor growth and suppresses the activity of RUVBL1 R117H mutant cells. RUVBL1/2-IN-1 has been applied in research related to MYC-dependent Burkitt's lymphoma .
|
-
- HY-N0475R
-
|
Hypolide (Standard); (+)-Triptophenolide (Standard)
|
Reference Standards
Androgen Receptor
Pyroptosis
Caspase
Bcl-2 Family
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Triptophenolide (Standard) (Hypolide) is the analytical standard of Triptophenolide (HY-N0475). This product is intended for research and analytical applications. Triptophenolide is a colorless crystal isolated from the ethyl acetate extract of Tripterygium wilfordii. Triptophenolide is an orally active pan‑antagonist of the androgen receptor (AR) with an IC50 of 467 nM against human wild‑type AR. Triptophenolide reduces AR expression, inhibits AR nuclear translocation, downregulates prostate‑specific antigen mRNA levels, and suppresses the growth of AR‑positive prostate cancer cells. Triptophenolide shows anti-tumor effects against breast cancer by inhibiting cell proliferation and migration, inducing G1-phase arrest and apoptosis, repressing xenograft tumor growth. Triptophenolide inhibits pyroptosis, alleviates tissue inflammation, and ameliorates synovial injury. Triptophenolide can be used for the study of prostate cancer, rheumatoid arthritis and breast cancer .
|
-
- HY-W766368
-
|
C6-Cer-13C2,d2; N-Hexanoylsphingosine-13C2,d2
|
Isotope-Labeled Compounds
Apoptosis
|
Cancer
|
|
C6 Ceramide- 13C2,d2 (C6-Cer- 13C2,d2) is the deuterium labeled and 13C-labeled C6 Ceramide (HY-19542). 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-13495
-
ML281
2 Publications Verification
|
STK33
PKA
Aurora Kinase
Bcl-2 Family
Apoptosis
|
Metabolic Disease
Cancer
|
|
ML281 is a highly selective inhibitor of serine/threonine kinase 33 (STK33) with an IC50 value of 14 nM. ML281 shows 700-fold selectivity over PKA and 550-fold over AurB. ML281 exerts core mechanism by inhibiting STK33: in small cell lung cancer, ML281 downregulates RPS6/BAD signaling phosphorylation, induces apoptosis, and suppresses proliferation, invasion . ML281 reduces STK33-mediated 4-hydroxyphenylpyruvate dioxygenase (HPD) phosphorylation in tyrosinemia . ML281 is suitable for research on STK33 function, KRAS mutation-related cancers (pancreatic cancer, colon cancer, lung adenocarcinoma, etc.), small cell lung cancer, and tyrosinemia-related damage
|
-
- HY-N6865
-
-
- HY-N4308
-
|
Hexa-O-methylquercetagetin; Quercetagetin hexamethyl ether; 3,5,6,7,3',4'-Hexamethoxyflavone
|
NF-κB
IKK
Bcl-2 Family
|
Cancer
|
|
Hexamethylquercetagetin (Hexa-O-methylquercetagetin; Quercetagetin hexamethyl ether; 3,5,6,7,3',4'-Hexamethoxyflavone) is an orally active NF-κB inhibitor. Hexamethylquercetagetin inhibits NF-κB-derived luciferase activity, reduces phosphorylated p65 and IκBα, Cyclin D1, Bcl-2 and blocks TNFα-induced NF-κB activation. Hexamethylquercetagetin inhibits survival and proliferation of cervical carcinoma cells. Hexamethylquercetagetin suppresses tumor volume and weight in BALB/c nude mouse xenograft models of cervical carcinoma. Hexamethylquercetagetin can be used for the research of cancer, such as cervical carcinoma .
|
-
- HY-P991977
-
|
5G9
|
EGFR
Apoptosis
PARP
Akt
ERK
|
Cancer
|
|
BSI-001 (5G9) is a HER2-targeting antibody. BSI-001 inhibits cell proliferation and migration, induces apoptosis and PARP cleavage, and suppresses HER2-mediated downstream signaling pathways (including the phosphorylation of EGFR, HER3, AKT and ERK) when combined with Trastuzumab (HY-P9907) in HER2-positive cancer cells. BSI-001 exhibits synergistic anti-tumor efficacy in animal models of gastric cancer and breast cancer when combined with Trastuzumab. BSI-001 can be used for the research of HER2-positive breast cancer and HER2-overexpressing gastric cancer .
|
-
- HY-156794A
-
|
DSP-5336 enantiomer
|
Drug Isomer
FLT3
Epigenetic Reader Domain
|
Cardiovascular Disease
Cancer
|
Enzomenib enantiomer (DSP-5336 enantiomer) is an enantiomer of Enzomenib (HY-156794). Enzomenib (DSP-5336) is an orally active Menin inhibitor (IC50=1.4 nM, Kd=6.0 nM). Enzomenib disrupts the interaction between Menin and KMT2A/MLL fusion proteins, specifically inhibits the expression of leukemia driver genes such as HOX/MEIS1, and upregulates ITGAM. Enzomenib effectively induces cell differentiation, inhibits tumor cell proliferation, and suppresses primitive cell colony formation. Enzomenib reduces disease burden and prolongs survival, but causes adverse reactions including differentiation syndrome and QTc interval prolongation. Enzomenib is used for research on relapsed/refractory acute myeloid leukemia, acute lymphoblastic leukemia, and other hematologic malignancies with mixed lineage leukemia (MLL) rearrangements or NPM1 mutations .
|
-
- HY-N1255A
-
|
(-)-Scoulerine hydrochloride; Discretamine hydrochloride
|
Apoptosis
PI3K
Akt
mTOR
Adrenergic Receptor
GABA Receptor
Beta-secretase
Bcl-2 Family
|
Cancer
|
|
Scoulerine ((-)-Scoulerine; Discretamine) hydrochloride is a multi-target inhibitor with anti-tumor and antioxidant activities. Scoulerine hydrochloride mainly targets the PI3K/Akt/mTOR signaling axis and α1D-adrenergic receptor, disrupts microtubule structure, and induces cell cycle arrest and apoptosis. Scoulerine hydrochloride effectively inhibits mitochondrial dehydrogenase activity, targets GABA receptors and BACE1, and suppresses the proliferation, migration, invasion, epithelial-mesenchymal transition and stem cell properties of cancer cells. Scoulerine hydrochloride also exhibits multiple pharmacological activities including anti-Plasmodium falciparum, antibacterial, antiemetic and antitussive effects, and regulates endoplasmic reticulum stress and mitochondrial function (modulates Bax, Bcl-2 and cytochrome c). Scoulerine hydrochloride is applicable to research related to leukemia, ovarian cancer, and colorectal cancer .
|
-
- HY-N1255
-
|
(-)-Scoulerine; Discretamine
|
Bcl-2 Family
Apoptosis
mTOR
GABA Receptor
PI3K
Adrenergic Receptor
Beta-secretase
Akt
|
Cancer
|
|
Scoulerine ((-)-Scoulerine; Discretamine) hydrochloride is a multi-target inhibitor with anti-tumor and antioxidant activities. Scoulerine mainly targets the PI3K/Akt/mTOR signaling axis and α1D-adrenergic receptor, disrupts microtubule structure, and induces cell cycle arrest and apoptosis. Scoulerine effectively inhibits mitochondrial dehydrogenase activity, targets GABA receptors and BACE1, and suppresses the proliferation, migration, invasion, epithelial-mesenchymal transition and stem cell properties of cancer cells. Scoulerine also exhibits multiple pharmacological activities including anti-Plasmodium falciparum, antibacterial, antiemetic and antitussive effects, and regulates endoplasmic reticulum stress and mitochondrial function (modulates Bax, Bcl-2 and cytochrome c). Scoulerine is applicable to research related to leukemia, ovarian cancer, and colorectal cancer .
|
-
- HY-153916
-
|
T417
|
HOXA
DNA/RNA Synthesis
NEKs
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
TCRS-417 (T417) is a small-molecular inhibitor for PBX1. TCRS-417 can directly block PBX1-binding to DNA (IC50 = 6.58 μM), and affects PBX1 transcription. TCRS-417 is able to hammer out the stemness traits of Carboplatin (HY-17393)-resistant (CR) cells to revert to a differentiated status through tacking PBX1 signaling cascade. TCRS-417 significantly suppresses self-renewal and proliferation of cancer cells expressing high levels of PBX1. TCRS-417 can decrease the mRNA levels of FOXM1, NEK2, and E2F2 in cancer cell lines. TCRS-417 is selectively toxic against chr1q-amp myeloma and solid tumor cells .
|
-
- HY-167854
-
|
|
Aurora Kinase
Apoptosis
IGF-1R
|
Cancer
|
|
KW-2450 Free base is a potent multikinase inhibitor targeting Aurora A and B kinases, demonstrating significant antitumor activity against triple-negative breast cancer (TNBC). KW-2450 Free base effectively reduces cell viability, promotes apoptosis, and inhibits colony formation and mammosphere formation in TNBC cells. KW-2450 Free base significantly suppresses the growth of TNBC xenografts, leading to tetraploid accumulation followed by apoptosis or the survival of octaploid cells. KW-2450 Free base enhances the efficacy of combination therapy with the MEK inhibitor selumetinib, resulting in a synergistic antitumor effect in TNBC models. KW-2450 Free base also acts as an orally bioavailable inhibitor of IGF-1R and IR tyrosine kinases, contributing to its potential antineoplastic activity by inhibiting tumor cell proliferation and inducing apoptosis.
|
-
- HY-149213
-
|
J54; J3-54
|
Histone Demethylase
TLK
Apoptosis
PD-1/PD-L1
|
Cancer
|
|
LSD1/TLK1-IN-1 is an orally active LSD1, TLK1, TLK2, TTK inhibitor with an LSD1 IC50 of 0.247 μM. LSD1/TLK1-IN-1 suppresses phosphorylation of Nek1 at T141 and Rad9 at S328, abrogates the TLK1>Nek1>ATR>Chk1 axis, protects H3K4me1/2 from demethylation, and does not affect LSD2, MAO-A, or MAO-B. LSD1/TLK1-IN-1 induces apoptosis, bypasses cell-cycle arrest, suppresses tumor growth, downregulates PD-L1 expression, enhances T-cell killing response, inhibits gastric cancer cell proliferation. LSD1/TLK1-IN-1 can be used for the research of prostate cancer and gastric cancer .
|
-
- HY-164445
-
|
|
STAT
c-Myc
CDK
|
Cancer
|
|
STAT3-IN-32 is an orally active, selective STAT3 SH2 domain inhibitor with a Kd of 21.3 nM, showing selectivity over STAT1/5. STAT3-IN-32 binds to the STAT3 SH2 domain, blocks Tyr705 and Ser727 phosphorylation, abrogates nuclear transcription and mitochondrial oxidative phosphorylation functions. STAT3-IN-32 suppresses pancreatic cancer cell proliferation. STAT3-IN-32 inhibits tumor growth in mouse pancreatic cancer xenograft models. STAT3-IN-32 can be used for the research of pancreatic cancer .
|
-
- HY-183335
-
|
|
Smo
Hedgehog
Gli
Apoptosis
Caspase
|
Cancer
|
|
Anticancer agent 321 is a Smoothened (SMO) inhibitor with a human IC50 of 0.12 μM, enhanced aqueous solubility, good plasma and metabolic stability, moderate therapeutic index, preliminary safety profile, and moderate oral bioavailability in rats.Anticancer agent 321 binds to SMO’s 7-transmembrane helical channel, forming hydrogen bonds with Asp384 and hydrophobic/π-π interactions with His470, Phe391, Tyr394, stabilizing SMO’s inactive conformation to inhibit Hedgehog/GLI signaling.Anticancer agent 321 inhibits proliferation, suppresses colony formation, induces apoptosis, and downregulates Hedgehog/GLI pathway target genes GLI1, GLI2, Ptch1, HHip in cancer cells.Anticancer agent 321 inhibits tumor growth, downregulates Ki67 and SOX2, and upregulates cleaved-caspase 3 in tumor tissues.Anticancer agent 321 can be used for the research of cutaneous squamous cell carcinoma .
|
-
- HY-164490
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
LS-106 is an orally active and potent inhibitor against epidermal growth factor receptor (EGFR) . LS-106 exhibits antitumor activities both in vitro and in vivo. LS-106 inhibits the kinase activities of EGFR 19del/T790M/C797S and EGFR L858R/T790M/C797S with IC50 values of 2.4 nmol/L and 3.1 nmol/L, respectively, which is more potent than Osimertinib (HY-15772). LS-106 induces Apoptosis, suppresses cell proliferation of tumor cells harboring EGFR 19del/T790M/C797S and leas to significant tumor regression in a C797S-mutant xenograft model .
|
-
- HY-161826
-
|
|
Wnt
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-151137
-
|
|
mTOR
HSP
Apoptosis
Autophagy
|
Cancer
|
|
HSP90/mTOR-IN-1 is a potent and orally active Hsp90 and mTOR inhibitor with IC50 values of 69 nM and 29 nM, respectively. HSP90/mTOR-IN-1 suppresses the proliferation of SW780 cells through the over-activation of the PI3K/AKT/mTOR pathway. HSP90/mTOR-IN-1 induces apoptosis and autophagy via selective Hsp90 and mTOR inhibition. HSP90/mTOR-IN-1 also has considerable in vivo anti-tumor activity. HSP90/mTOR-IN-1 can be used for researching bladder cancer .
|
-
- HY-183784
-
|
|
P2X Receptor
FAK
MMP
|
Cancer
|
|
P2X7R antagonist-1 is an orally active P2X7 receptor antagonist with an IC50 of 3.57 μM. P2X7R antagonist-1 inhibits the proliferation, invasion and metastasis abilities of cancer cells. P2X7R antagonist-1 downregulates the expression of FAK and MMP-9. P2X7R antagonist-1 suppresses tumor growth and metastasis in a mouse breast cancer model. P2X7R antagonist-1 promotes the activation of CD4 and CD8 T cells. P2X7R antagonist-1 can be used in breast cancer-related research .
|
-
- HY-168669
-
|
|
PROTACs
Ras
Caspase
ERK
|
Cancer
|
|
PROTAC K-Ras Degrader-5 is a cereblon-based K-Ras PROTAC degrader with a DC50 of <100 nM for KRAS G12D. PROTAC K-Ras Degrader-5 recruits KRAS G12D to the cereblon E3 ubiquitin ligase complex for ubiquitination and subsequent proteasomal degradation. PROTAC K-Ras Degrader-5 suppresses pERK levels downstream of KRAS G12D degradation in cancer cells. PROTAC K-Ras Degrader-5 reduces proliferation of cancer cells. PROTAC K-Ras Degrader-5 induces caspase 3/7 activity and cPARP, markers of apoptosis, in pancreatic cancer spheroids and tumors. PROTAC K-Ras Degrader-5 can be used for the research of pancreatic cancer and colorectal cancer .
|
-
- HY-181727
-
|
|
Androgen Receptor
HSP
CDK
|
Cancer
|
|
AR/AR-V7 degrader-1 is an orally active AR and AR-V7 degrader. AR/AR-V7 degrader-1 disrupts the interaction between AR/AR-V7 and HSP90, leading to their ubiquitination and degradation in castration-resistant prostate cancer cells. AR/AR-V7 degrader-1 regulates the expression of cell cycle-related proteins in prostate cancer cells (downregulates CDK4, CDK6, Cyclin D1, Cyclin E1; upregulates P21) and induces G0/G1 phase arrest. AR/AR-V7 degrader-1 inhibits the proliferation and migration of prostate cancer cells. AR/AR-V7 degrader-1 suppresses the growth of castration-resistant prostate cancer tumors in nude mice and induces the degradation of AR and AR-V7 in tumor tissues. AR/AR-V7 degrader-1 is applicable to the research of castration-resistant prostate cancer .
|
-
- HY-182361
-
|
|
AMPK
JAK
Cadherin
|
Cancer
|
|
NUAK1-IN-3 is a potent and selective NUAK1 inhibitor with an IC50 of 0.49 nM. NUAK1-IN-3 also inhibits NUAK2 and JAK3 with IC50 values of 265 and 225 nM. NUAK1-IN-3 engages Glu139 of NUAK1, forms a salt bridge between its bicyclic ring nitrogen and Asp142, and uses a fluorine atom to enhance hydrophobic binding interactions. NUAK1-IN-3 attenuates MYPT1 phosphorylation, suppresses the NUAK1-MYPT1 signaling axis, and inhibits proliferation, migration, and invasion of triple-negative breast cancer cells. NUAK1-IN-3 reverses TGF-β1-induced epithelial-mesenchymal transition (EMT) marker alterations, downregulates Snail and N-cadherin, and upregulates E-cadherin in tumor tissues. NUAK1-IN-3 suppresses tumor growth in triple-negative breast cancer xenograft models. NUAK1-IN-3 can be used for the research of triple-negative breast cancer .
|
-
- HY-159607
-
|
|
PROTACs
SWI/SNF Complex
|
Cancer
|
|
PRT3789 is a selective SMARCA2 PROTAC degrader (DC50 in HeLa cell: 0.72 nM for SMARCA2, 14 nM for SMARCA4). PRT3789 forms a stable ternary complex with Von Hippel-Lindau (VHL) E3 ligase, induces polyubiquitination at SMARCA2-specific lysine residues, and drives proteasome-dependent SMARCA2 degradation. PRT3789 disrupts SWI/SNF chromatin remodeling complex integrity, induces dissociation of specific subunits, suppresses oncogenic gene expression, reduces chromatin accessibility, and upregulates antigen processing/presentation-related gene expression. PRT3789 induces synthetic lethality, inhibits proliferation and colony formation, and drives tumor growth inhibition and regression in SMARCA4-deficient contexts. PRT3789 can be used for the research of SMARCA4-mutated solid tumors, non-small cell lung cancer, endometrial cancer, colorectal cancer, bladder cancer, esophageal cancer, ovarian cancer, and gastric cancer .
|
-
- HY-161176
-
|
|
PROTACs
Ras
ERK
|
Cancer
|
|
PROTAC KRAS G12D degrader 1 is a selective PROTAC KRAS G12D degrader. PROTAC KRAS G12D degrader 1 inhibits proliferation of KRAS G12D-mutant cells and suppresses ERK phosphorylation. PROTAC KRAS G12D degrader 1 inhibits tumor growth in mice bearing AsPC-1 xenografts. PROTAC KRAS G12D degrader 1 can be used for the study of KRAS G12D-driven cancers.(Pink: KRAS ligand (HY-175892), Blue: VHL Ligand (HY-112078), Black: Linker, E3 ligase ligand-linker conjugate (HY-175893)) .
|
-
- HY-181842
-
|
|
PARP
ERK
Apoptosis
|
Cancer
|
|
PARP1/ERK IN-1 is a dual PARP1/ERK inhibitor, with a PARP1 IC50 of 0.9 nM and an ERK2 IC50 of 1.8 nM. PARP1/ERK IN-1 inhibits proliferation and migration of various cancer cell lines, and induces apoptosis and DNA damage. PARP1/ERK IN-1 suppresses tumor growth in mouse models of colorectal cancer, and reduces the expression of Ki‑67, BRCA1 and Rad51. PARP1/ERK IN-1 can be used in the research of colorectal cancer, triple-negative breast cancer and pancreatic cancer .
|
-
- HY-167262
-
|
|
RAR/RXR
|
Metabolic Disease
Cancer
|
|
AGN-191659 is an orally active RAR/RXR agonist with EC50 values of 11 nM, 23 nM, and 37 nM for RXRα, RARβ, and RARγ, respectively. AGN-191659 activates RXRα, RARβ and RARγ to induce gene transcription. AGN-191659 induces tissue transglutaminase activity, inhibits ornithine decarboxylase activity induced by tumor promoters, and suppresses chondrogenesis. AGN-191659 reverses basic fibroblast growth factor-induced endothelial cell proliferation. AGN-191659 induces hypertriglyceridemia in rat models. AGN-191659 inhibits total heparin-releasable lipase activity. AGN-191659 can be used in research related to promyelocytic leukemia and hypertriglyceridemia .
|
-
- HY-125209A
-
|
|
Apoptosis
PARP
DNA/RNA Synthesis
|
Cancer
|
|
TH5427 hydrochloride is a NUDT5 inhibitor with a human target IC50 of 29 nM, ~690-fold selectivity over MTH1 in vitro, and selective functional inhibition over other NUDIX hydrolases including NUDT9 .TH5427 hydrochloride binds to the active site of NUDT5, blocking enzymatic activity related to ADP-ribose metabolism and PAR-derived ATP synthesis .TH5427 hydrochloride blocks progestin-dependent nuclear ATP synthesis, impairs progestin-induced chromatin remodeling, inhibits histone H1 displacement, disrupts progestin-dependent gene regulation, and abrogates progestin-dependent proliferation in breast cancer cells .TH5427 hydrochloride functions as a versatile probe to study nuclear ATP dynamics and ADP-ribose-related metabolism in cells .TH5427 hydrochloride engages NUDT5 at physiological temperatures, as demonstrated by Drug Affinity Responsive Target Stability (DARTS) assay .TH5427 hydrochloride stabilizes NUDT5 against thermal denaturation in cell lysates and intact cells, as shown by cellular thermal shift assay (CETSA) .TH5427 hydrochloride functionally inhibits NUDT5 activity, leading to downstream effects on oxidative DNA damage and DNA replication in triple-negative breast cancer (TNBC) cells .TH5427 hydrochloride suppresses proliferation of TNBC cells without inducing cell death or apoptosis, slows DNA replication in TNBC cells, promotes accumulation of oxidative DNA lesions, and triggers DNA damage response in TNBC cells .TH5427 hydrochloride suppresses growth of TNBC cells in vitro, inhibits growth of TNBC xenograft tumors in nude mice in vivo, and shows greater potency against TNBC cell lines compared to ER-positive and normal-like breast cell lines .TH5427 hydrochloride can be used for the research of breast cancer and triple-negative breast cancer .
|
-
- HY-182083
-
|
|
PROTACs
PI3K
|
Cancer
|
|
PROTAC PI3Kα/δ degrader-1 is an orally active PI3Kα/δ PROTAC degrader, with an IC50 of 0.34 nM for PI3Kα and 1.85 nM for PI3Kδ. PROTAC PI3Kα/δ degrader-1 inhibits the proliferation and migration of cancer cells, induces G1-phase cell cycle arrest and PI3Kα degradation. PROTAC PI3Kα/δ degrader-1 suppresses tumor growth in breast cancer xenograft mouse models. PROTAC PI3Kα/δ degrader-1 can be used for the research of breast cancer .
|
-
- HY-181964
-
|
|
|
Cancer
|
|
KRAS G12C-IN-77 is an orally active and selective KRAS G12C covalent dual-state inhibitor that binds with high affinity to both GDP-bound (inactive state) and GTP-bound (active state) KRAS G12C (IC50 = 133 nM). KRAS G12C-IN-77 rapidly inhibits ERK1/2 phosphorylation, induces the formation of covalent adducts with endogenous KRAS G12C, suppresses the expression of MAPK pathway genes, and inhibits the proliferation of KRAS G12C-mutant cells. KRAS G12C-IN-77 is applicable to research related to KRAS G12C-mutant solid tumors, including pancreatic ductal adenocarcinoma and non-small cell lung cancer .
|
-
- 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) .
|
-
- HY-157229
-
STX-721
1 Publications Verification
|
EGFR
ERK
|
Cancer
|
|
STX-721 is an orally active, irreversible, covalent EGFR exon 20 insertion (ex20ins) inhibitor that selectively targets ex20ins-mutant dynamic protein states. STX-721 potently inhibits the kinase activity of EGFR ex20ins mutants (NPG, ASV, SVD). STX-721 inhibits phosphorylation of EGFR (pEGFR Y1068) and downstream ERK (pERK Thr202/Tyr204), and suppresses proliferation of ex20ins-mutant Ba/F3 cells and human NSCLC cell lines (NCI-H2073 ASV KI, CUTO-14 ASV). STX-721 induces tumor regression in EGFR ex20ins-mutant PDX/CDX models. STX-721 can be used for the study of non-small cell lung cancer (NSCLC) harboring EGFR or HER2 ex20ins mutations .
|
-
- HY-175369
-
|
|
PI3K
Akt
PD-1/PD-L1
Interleukin Related
CD3
|
Inflammation/Immunology
Cancer
|
|
PI3Kδ-IN-25 is an orally active selective PI3Kδ inhibitor (IC50 = 2.1 nM). PI3Kδ-IN-25 has IC50s of 272, 285, and 1171 nM for PI3Kα, PI3Kγ, and PI3Kβ, respectively. PI3Kδ-IN-25 inhibits AKT Ser473 phosphorylation, suppresses Treg cell proliferation, and downregulates PD-L1 expression in B16F10 cells. PI3Kδ-IN-25 exhibits anticancer effects in B16F10 melanoma and Lewis lung cancer mouse models by reducing tumor-infiltrating Treg cells and enhancing immune responses. PI3Kδ-IN-25 is potentially useful in the study of melanoma, lung cancer, and other cancers .
|
-
- HY-N2445
-
|
|
Apoptosis
Akt
JNK
PERK
Caspase
PARP
MDM-2/p53
IAP
Reactive Oxygen Species (ROS)
SOD
FABP
Autophagy
AMPK
mTOR
GLUT
EGFR
PI3K
HSP
VEGFR
FAK
|
Cancer
|
|
Flavokawain C is an orally active natural chalcone. Flavokawain C inhibits the proliferation of various cancer cells. Flavokawain C upregulates GADD153 in cancer cells, inhibits the phosphorylation of Akt and JNK, suppresses early ERK phosphorylation, activates late ERK phosphorylation, activates caspase related subtypes, induces PARP-1 cleavage, causes upregulation of p21 and p27, downregulation of mutant p53 and anti-apoptotic IAP proteins, elevates intracellular ROS levels, reduces SOD activity, and induces apoptosis. Flavokawain C downregulates FABP4, induces autophagy in cancer cells, and activates the AMPK/mTOR pathway . Flavokawain C decreases the expression of glycolysis-related proteins GLUT1 and HK2, and inhibits glycolysis in nasopharyngeal carcinoma cells. Flavokawain C inhibits the activation of the EGFR/PI3K/Akt/mTOR signaling pathway and reduces the expression of HSP90B1. Flavokawain C inhibits angiogenesis by decreasing the expression of angiogenic proteins Ang-1 and VEGF in human umbilical vein endothelial cells. Flavokawain C increases γ-H2AX levels in cells, inhibits the phosphorylation of FAK, PI3K and AKT in cells, and induces DNA damage in cells. Flavokawain C exerts anti-tumor activity in multiple tumor xenograft mouse models. Flavokawain C is applicable to research related to colorectal cancer, colon adenocarcinoma, nephroblastoma, nasopharyngeal carcinoma and liver cancer .
|
-
- HY-N1510
-
|
|
Glycosidase
Notch
Toll-like Receptor (TLR)
NF-κB
Mucin
Reactive Oxygen Species (ROS)
Bacterial
TGF-beta/Smad
Anaplastic lymphoma kinase (ALK)
|
Infection
Inflammation/Immunology
Cancer
|
|
Kaempferol 3-O-gentiobioside is an orally active flavonoid, with a Ka value of 57 µM against human NOTCH1 and an IC50 value of 50 μM against α-glucosidase. Kaempferol 3-O-gentiobioside inhibits the NOTCH signaling pathway. It downregulates the expression of TLR4 and NLRP3, and suppresses the activation and nuclear translocation of NF-κB. Kaempferol 3-O-gentiobioside inhibits the expression of MUC5AC, reduces nitrite and ROS levels, and attenuates excessive mucus secretion. It exhibits antibacterial activity, reducing the formation and growth of MRSA biofilms. Kaempferol 3-O-gentiobioside blocks the TGF-β/ALK5/Smad signaling pathway and inhibits epithelial-mesenchymal transition. It suppresses the proliferation, migration, invasion and metastatic growth of tumor cells. Kaempferol 3-O-gentiobioside alleviates airway inflammation and mucus hypersecretion in mice with allergic asthma . It reduces the volume of ovarian cancer xenografts in mice. Kaempferol 3-O-gentiobioside can be used in research related to allergic asthma, diabetes, MRSA infection, breast cancer, gastric cancer and ovarian cancer .
|
-
- HY-B0327
-
|
Dicloguamine
|
Phosphodiesterase (PDE)
NF-κB
AP-1
TRP Channel
Interleukin Related
|
Inflammation/Immunology
Cancer
|
|
Irsogladine (Dicloguamine) is an orally active gastric mucosal protective agent. Irsogladine inhibits breast cancer recurrence and lung metastasis in nude mice . Irsogladine inhibits the transcriptional activities of NF-κB and AP-1, suppresses the activities of PDE and PDE4 to elevate intracellular cAMP levels, and activates TRPV1 and KATP channels. Irsogladine enhances iNOS expression, NO production, and the activation of cAMP-responsive elements. Irsogladine inhibits the development and progression of intestinal polyps in Apc-mutant mice. Irsogladine alleviates oxidative stress, increases gastric mucosal blood flow, and stimulates the production of endogenous prostaglandins. Irsogladine promotes insulin secretion in MIN6 cells. Irsogladine inhibits tumor angiogenesis, cancer cell proliferation, and the production of proinflammatory cytokines. Irsogladine exerts protective effects on astrocytes in ethanol/hydrochloric acid-induced gastric ulcers in mice. Irsogladine prevents colitis in IL-10 gene-deficient mice by reducing the production of IL-12 and IL-23. Irsogladine upregulates gap junction intercellular communication in pancreatic cancer cells via the PKA pathway. Irsogladine is applicable to research related to breast cancer, intestinal polyposis, gastric ulcer, spontaneous colitis, glioma, liver cancer, and pancreatic cancer [5][6] .
|
-
- HY-N0660R
-
|
|
Reference Standards
ERK
p38 MAPK
Akt
PI3K
11β-HSD
STING
VEGFR
Ferroptosis
Autophagy
Apoptosis
Keap1-Nrf2
Caspase
PARP
AMPK
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Jujuboside B (Standard) is the analytical standard of Jujuboside B. This product is intended for research and analytical applications. Jujuboside B is a bioactive saponin component isolated from Ziziphi Spinosae Semen (sour jujube seed), with oral efficacy and blood-brain barrier permeability. Jujuboside B induces acute leukemia cell death and drives necroptosis apoptosis by activating the RIPK1/RIPK3/MLKL pathway. Jujuboside B upregulates the expression of NOXA, PARP and caspase-3, activates AMPK, inhibits the proliferation of breast cancer cells, and induces cell apoptosis and autophagy. Jujuboside B inhibits angiogenesis and tumor growth by blocking the VEGFR-2 signaling pathway. Jujuboside B alleviates liver injury in mice by regulating the Nrf2-STING signaling pathway . Jujuboside B alleviates liver injury by regulating anti-inflammatory responses and downregulating the expression of 11β-HSD2. Jujuboside B induces ferroptosis and overcomes radioresistance in non-small cell lung cancer via the PPARγ-ATF3-Gpx4 signaling pathway. Jujuboside B exerts inhibitory effects on platelet aggregation. Jujuboside B inhibits febrile seizures by suppressing the activity of AMPA receptors. Jujuboside B reverses chronic unpredictable mild stress-promoted tumor progression by blocking the PI3K/Akt and MAPK/ERK pathways and dephosphorylating CREB signaling. Jujuboside B is applicable to related studies on acute leukemia, breast cancer, PM2.5-induced lung injury, hepatotoxicity, liver injury, colorectal cancer, non-small cell lung cancer, thromboembolic diseases, cardiovascular diseases associated with high platelet aggregation, febrile seizures, and depressive-like phenotypes.
|
-
- HY-N0660
-
|
|
Apoptosis
PARP
Caspase
AMPK
Autophagy
VEGFR
Keap1-Nrf2
STING
11β-HSD
Ferroptosis
PI3K
Akt
p38 MAPK
ERK
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Jujuboside B is a bioactive saponin component isolated from Ziziphi Spinosae Semen (sour jujube seed), with oral efficacy and blood-brain barrier permeability. Jujuboside B induces acute leukemia cell death and drives necroptosis apoptosis by activating the RIPK1/RIPK3/MLKL pathway. Jujuboside B upregulates the expression of NOXA, PARP and caspase-3, activates AMPK, inhibits the proliferation of breast cancer cells, and induces cell apoptosis and autophagy. Jujuboside B inhibits angiogenesis and tumor growth by blocking the VEGFR-2 signaling pathway. Jujuboside B alleviates liver injury in mice by regulating the Nrf2-STING signaling pathway . Jujuboside B alleviates liver injury by regulating anti-inflammatory responses and downregulating the expression of 11β-HSD2. Jujuboside B induces ferroptosis and overcomes radioresistance in non-small cell lung cancer via the PPARγ-ATF3-Gpx4 signaling pathway. Jujuboside B exerts inhibitory effects on platelet aggregation. Jujuboside B inhibits febrile seizures by suppressing the activity of AMPA receptors. Jujuboside B reverses chronic unpredictable mild stress-promoted tumor progression by blocking the PI3K/Akt and MAPK/ERK pathways and dephosphorylating CREB signaling. Jujuboside B is applicable to related studies on acute leukemia, breast cancer, PM2.5-induced lung injury, hepatotoxicity, liver injury, colorectal cancer, non-small cell lung cancer, thromboembolic diseases, cardiovascular diseases associated with high platelet aggregation, febrile seizures, and depressive-like phenotypes .
|
-
-
-
HY-L083
-
|
|
3,626 compounds
|
|
Mutations in oncogenes and tumor suppressor genes can modify multiple signaling pathways and in turn cell metabolism, which facilitates tumorigenesis. The paramount hallmark of tumor metabolism is “aerobic glycolysis” or the Warburg effect, coined by Otto Warburg in 1926, in which cancer cells produce most of energy from glycolysis pathway regardless of whether in aerobic or anaerobic condition. Usually, cancer cells are highly glycolytic (glucose addiction) and take up more glucose than do normal cells from outside. The increased uptake of glucose is facilitated by the overexpression of several isoforms of membrane glucose transporters (GLUTs). Likewise, the metabolic pathways of glutamine, amino acid and fat metabolism are also altered. Recent trends in anti-cancer drug discovery suggests that targeting the altered metabolic pathways of cancer cells result in energy crisis inside the cancer cells and can selectively inhibit cancer cell proliferation by delaying or suppressing tumor growth.
MCE provides a unique collection of 3,626 compounds which cover various tumor metabolism-related signaling pathways. These compounds can be used for anti-cancer metabolism targets identification, validation as well anti-cancer drug discovery.
|
| Cat. No. |
Product Name |
Target |
Research Area |
Image |
-
- HY-P99364
-
|
Anti-VEGFR1/FLT1 Reference Antibody; IMC-18F1
|
VEGFR
Apoptosis
p38 MAPK
Akt
|
Endocrinology
Cancer
|
|
Icrucumab (Anti-VEGFR1/FLT1 Reference Antibody; IMC-18F1) is an IgG1 antibody inhibitor targeting VEGFR-1/FLT1 with anti-tumor activity. By blocking ligand-dependent phosphorylation and downstream signal transduction, Icrucumab reduces the activities of MAPK and Akt in breast cancer xenograft models, inhibits the proliferation and invasion of VEGFR-1-positive tumor cells, and reverses the conversion of M1 macrophages to the pro-tumor M2-like phenotype. Icrucumab also inhibits tumor cell proliferation, promotes apoptosis, and effectively suppresses tumor growth through direct targeting of tumors and host support mechanisms. In addition, Icrucumab exhibits a synergistic effect when combined with chemotherapeutic agents, and it is used in research related to various cancers including advanced solid malignancies, thyroid cancer, melanoma, and lung cancer .
|
-
(5)
-
- HY-P991358
-
|
LFA-102; X213
|
Estrogen Receptor/ERR
STAT
Akt
|
Cancer
|
|
XOMA-213 (LFA-102; X213) is a human monoclonal antibody (mAb) targeting the prolactin receptor (PRLR), with a Kd value of 2 nM against the human target. XOMA-213 blocks PRL-induced cell proliferation and inhibits the activation of multiple PRLR ligands, including PRL and human growth hormone (hGH). XOMA-213 suppresses PRL-induced phosphorylation of Stat5, Akt and ERK1/2 in cells. XOMA-213 induces tumor regression, delays disease progression, and inhibits PRLR signaling as well as tumor growth. XOMA-213 can be used in research related to breast cancer .
|
-
(5)
-
- HY-P991530
-
|
|
Biochemical Assay Reagents
|
Inflammation/Immunology
Cancer
|
|
YH004 is an anti-CD137 agonistic monoclonal antibody, with immunostimulating and antineoplastic activities. YH004 activates CD137 expressed on a variety of leukocyte subsets including activated T lymphocytes and natural killer cells. YH004 enhances CD137-mediated signaling and induces cytotoxic T-lymphocyte (CTL) proliferation, cytokine production and promotes anti-tumor response mediated by CTL. YH004 induces NK-mediated tumor cell killing and suppresses the immunosuppressive activity of regulatory T cells. YH004 can be studied in anticancer research .
|
-
(5)
-
- HY-P991999
-
|
|
FGFR
IFNAR
Interleukin Related
|
Cancer
|
|
OM-RCA-01 is an anti-FGFR1 monoclonal antibody with a Kd of 1.59 nM for human FGFR1. OM-RCA-01 inhibits the phosphorylation of FGFR1, blocks FGF-mediated signaling pathways, and suppresses the proliferation of downstream tumor cells. OM-RCA-01 delays tumor growth in lung cancer and renal cancer xenograft models expressing FGFR1. When combined with Nivolumab, OM-RCA-01 enhances the release of IFN-γ and IL-2. OM-RCA-01 is applicable for the research of lung cancer and renal cell carcinoma .
|
-
(5)
-
- HY-P992401
-
|
|
EGFR
CD3
PI3K
Akt
p38 MAPK
Caspase
Apoptosis
IFNAR
TNF Receptor
Interleukin Related
|
Cancer
|
|
M802 is an anti-HER2/CD3 bispecific antibody, with a Kd of 0.578 nM for human HER2 and a Kd of 71.2 nM for human CD3. M802 inhibits the PI3K/AKT and MAPK signaling pathways, suppresses tumor cell proliferation, activates caspase-3, and promotes tumor cell apoptosis (apoptosis). M802 recruits and activates CD3-positive immune cells, mediates cytotoxicity against HER2-positive tumor cells, and induces immune cells to secrete IFN-γ, TNF-α, IL-2 and IL-6. M802 exhibits anti-tumor efficacy in mice with gastric cancer xenografts. M802 can be used in research related to HER2-positive breast cancer, HER2-positive gastric cancer and other cancers. The recommended isotype control is human IgG1 kappa (HY-P99001) .
|
-
(5)
-
- HY-P992200
-
|
|
Transmembrane Glycoprotein
PI3K
Akt
p38 MAPK
NF-κB
MMP
Apoptosis
Caspase
Bcl-2 Family
|
Cardiovascular Disease
Cancer
|
|
Anti-CD146 Antibody (AA98) is an antibody targeting CD146 and an angiogenesis inhibitor. Anti-CD146 Antibody (AA98) blocks the dimerization of CD146 as well as its downstream PI3K/AKT, p38 MAPK and NF-κB signaling pathways; it inhibits the expression of MMP9 and ICAM1, epithelial-mesenchymal transition (EMT), and the proliferation, migration and tube formation of endothelial cells. Anti-CD146 Antibody (AA98) enhances radiation-induced cancer cell apoptosis and survival inhibition, reduces tumor microvessel density, and suppresses tumor growth, invasion and vasculogenic mimicry. Anti-CD146 Antibody (AA98) can be used in research related to cervical cancer, liver cancer, malignant phyllodes tumor of the breast, uveal melanoma, leiomyosarcoma, pancreatic cancer, other tumors and angiogenesis .
|
-
(5)
-
- HY-P991977
-
|
5G9
|
EGFR
Apoptosis
PARP
Akt
ERK
|
Cancer
|
|
BSI-001 (5G9) is a HER2-targeting antibody. BSI-001 inhibits cell proliferation and migration, induces apoptosis and PARP cleavage, and suppresses HER2-mediated downstream signaling pathways (including the phosphorylation of EGFR, HER3, AKT and ERK) when combined with Trastuzumab (HY-P9907) in HER2-positive cancer cells. BSI-001 exhibits synergistic anti-tumor efficacy in animal models of gastric cancer and breast cancer when combined with Trastuzumab. BSI-001 can be used for the research of HER2-positive breast cancer and HER2-overexpressing gastric cancer .
|
-
(5)
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-16938
-
-
-
- HY-N3005
-
-
-
- HY-N0448
-
-
-
- HY-N6950
-
-
-
- HY-N0743
-
-
-
- HY-N1255
-
|
(-)-Scoulerine; Discretamine
|
Alkaloids
Structural Classification
other families
Classification of Application Fields
Phenols
Polyphenols
Plants
Isoquinoline Alkaloids
Disease Research Fields
Source Classification
Cancer
|
Bcl-2 Family
Apoptosis
mTOR
GABA Receptor
PI3K
Adrenergic Receptor
Beta-secretase
Akt
|
|
Scoulerine ((-)-Scoulerine; Discretamine) hydrochloride is a multi-target inhibitor with anti-tumor and antioxidant activities. Scoulerine mainly targets the PI3K/Akt/mTOR signaling axis and α1D-adrenergic receptor, disrupts microtubule structure, and induces cell cycle arrest and apoptosis. Scoulerine effectively inhibits mitochondrial dehydrogenase activity, targets GABA receptors and BACE1, and suppresses the proliferation, migration, invasion, epithelial-mesenchymal transition and stem cell properties of cancer cells. Scoulerine also exhibits multiple pharmacological activities including anti-Plasmodium falciparum, antibacterial, antiemetic and antitussive effects, and regulates endoplasmic reticulum stress and mitochondrial function (modulates Bax, Bcl-2 and cytochrome c). Scoulerine is applicable to research related to leukemia, ovarian cancer, and colorectal cancer .
|
-
-
- HY-N0660
-
|
|
Cardiovascular Disease
Triterpenes
Structural Classification
other families
Classification of Application Fields
Terpenoids
Plants
Disease Research Fields
Source Classification
|
Apoptosis
PARP
Caspase
AMPK
Autophagy
VEGFR
Keap1-Nrf2
STING
11β-HSD
Ferroptosis
PI3K
Akt
p38 MAPK
ERK
|
|
Jujuboside B is a bioactive saponin component isolated from Ziziphi Spinosae Semen (sour jujube seed), with oral efficacy and blood-brain barrier permeability. Jujuboside B induces acute leukemia cell death and drives necroptosis apoptosis by activating the RIPK1/RIPK3/MLKL pathway. Jujuboside B upregulates the expression of NOXA, PARP and caspase-3, activates AMPK, inhibits the proliferation of breast cancer cells, and induces cell apoptosis and autophagy. Jujuboside B inhibits angiogenesis and tumor growth by blocking the VEGFR-2 signaling pathway. Jujuboside B alleviates liver injury in mice by regulating the Nrf2-STING signaling pathway . Jujuboside B alleviates liver injury by regulating anti-inflammatory responses and downregulating the expression of 11β-HSD2. Jujuboside B induces ferroptosis and overcomes radioresistance in non-small cell lung cancer via the PPARγ-ATF3-Gpx4 signaling pathway. Jujuboside B exerts inhibitory effects on platelet aggregation. Jujuboside B inhibits febrile seizures by suppressing the activity of AMPA receptors. Jujuboside B reverses chronic unpredictable mild stress-promoted tumor progression by blocking the PI3K/Akt and MAPK/ERK pathways and dephosphorylating CREB signaling. Jujuboside B is applicable to related studies on acute leukemia, breast cancer, PM2.5-induced lung injury, hepatotoxicity, liver injury, colorectal cancer, non-small cell lung cancer, thromboembolic diseases, cardiovascular diseases associated with high platelet aggregation, febrile seizures, and depressive-like phenotypes .
|
-
-
- HY-W040055
-
|
D-(+)-Neopterin; D-erythro-Neopterin
|
Natural Products
Classification of Application Fields
Endogenous metabolite
Inflammation/Immunology
Disease Research Fields
Source Classification
|
NF-κB
PPAR
ERK
Raf
Src
|
|
Neopterin is an immune system activator metabolized by GTP and can be produced by activated macrophages. Neopterin has the potential to resist vascular inflammation and atherosclerosis. Neopterin inhibits the phosphorylation of NF-κB and promotes the expression of PPAR-γ, thereby suppressing the inflammatory response of vascular endothelial cells, reducing the formation of macrophage foam cells, and regulating the migration and proliferation of vascular smooth muscle cells. Neopterin can be used in research fields such as cardiovascular diseases (such as atherosclerosis), inflammation-related diseases and tumor immunomonitoring .
|
-
-
- HY-N2445
-
|
|
Structural Classification
Classification of Application Fields
Piperaceae
Plants
Chalcones
Flavonoids
other families
Phenols
Polyphenols
Piper methysticum G.Forst.
Disease Research Fields
Source Classification
Cancer
|
Apoptosis
Akt
JNK
PERK
Caspase
PARP
MDM-2/p53
IAP
Reactive Oxygen Species (ROS)
SOD
FABP
Autophagy
AMPK
mTOR
GLUT
EGFR
PI3K
HSP
VEGFR
FAK
|
|
Flavokawain C is an orally active natural chalcone. Flavokawain C inhibits the proliferation of various cancer cells. Flavokawain C upregulates GADD153 in cancer cells, inhibits the phosphorylation of Akt and JNK, suppresses early ERK phosphorylation, activates late ERK phosphorylation, activates caspase related subtypes, induces PARP-1 cleavage, causes upregulation of p21 and p27, downregulation of mutant p53 and anti-apoptotic IAP proteins, elevates intracellular ROS levels, reduces SOD activity, and induces apoptosis. Flavokawain C downregulates FABP4, induces autophagy in cancer cells, and activates the AMPK/mTOR pathway . Flavokawain C decreases the expression of glycolysis-related proteins GLUT1 and HK2, and inhibits glycolysis in nasopharyngeal carcinoma cells. Flavokawain C inhibits the activation of the EGFR/PI3K/Akt/mTOR signaling pathway and reduces the expression of HSP90B1. Flavokawain C inhibits angiogenesis by decreasing the expression of angiogenic proteins Ang-1 and VEGF in human umbilical vein endothelial cells. Flavokawain C increases γ-H2AX levels in cells, inhibits the phosphorylation of FAK, PI3K and AKT in cells, and induces DNA damage in cells. Flavokawain C exerts anti-tumor activity in multiple tumor xenograft mouse models. Flavokawain C is applicable to research related to colorectal cancer, colon adenocarcinoma, nephroblastoma, nasopharyngeal carcinoma and liver cancer .
|
-
-
- HY-N0475
-
-
-
- HY-N1510
-
|
|
Flavonols
Structural Classification
Flavonoids
Sauropus spatulifolius Beille
Classification of Application Fields
Phenols
Polyphenols
Metabolic Disease
Euphorbiaceae
Plants
Disease Research Fields
Source Classification
|
Glycosidase
Notch
Toll-like Receptor (TLR)
NF-κB
Mucin
Reactive Oxygen Species (ROS)
Bacterial
TGF-beta/Smad
Anaplastic lymphoma kinase (ALK)
|
|
Kaempferol 3-O-gentiobioside is an orally active flavonoid, with a Ka value of 57 µM against human NOTCH1 and an IC50 value of 50 μM against α-glucosidase. Kaempferol 3-O-gentiobioside inhibits the NOTCH signaling pathway. It downregulates the expression of TLR4 and NLRP3, and suppresses the activation and nuclear translocation of NF-κB. Kaempferol 3-O-gentiobioside inhibits the expression of MUC5AC, reduces nitrite and ROS levels, and attenuates excessive mucus secretion. It exhibits antibacterial activity, reducing the formation and growth of MRSA biofilms. Kaempferol 3-O-gentiobioside blocks the TGF-β/ALK5/Smad signaling pathway and inhibits epithelial-mesenchymal transition. It suppresses the proliferation, migration, invasion and metastatic growth of tumor cells. Kaempferol 3-O-gentiobioside alleviates airway inflammation and mucus hypersecretion in mice with allergic asthma . It reduces the volume of ovarian cancer xenografts in mice. Kaempferol 3-O-gentiobioside can be used in research related to allergic asthma, diabetes, MRSA infection, breast cancer, gastric cancer and ovarian cancer .
|
-
-
- HY-N6865
-
-
-
- HY-16938R
-
|
5'-(Methylthio)-5'-deoxyadenosine (Standard); 5'-Deoxy-5'-(methylthio)adenosine (Standard); 5'-S-Methyl-5'-thioadenosine (Standard)
|
Structural Classification
Natural Products
Microorganisms
Endogenous metabolite
Source Classification
|
Reference Standards
Endogenous Metabolite
Apoptosis
Parasite
|
|
5'-Methylthioadenosine (Standard) is the analytical standard of 5'-Methylthioadenosine. This product is intended for research and analytical applications. 5'-Methylthioadenosine (5'-(Methylthio)-5'-deoxyadenosine) is a nucleoside generated from S-adenosylmethionine (SAM) during polyamine synthesis[1]. 5'-Methylthioadenosine suppresses tumors by inhibiting tumor cell proliferation, invasion, and the induction of apoptosis while controlling the inflammatory micro-environments of tumor tissue. 5'-Methylthioadenosine and its associated materials have striking regulatory effects on tumorigenesis[2].
|
-
-
- HY-N6950R
-
-
-
- HY-N0448R
-
|
|
Zingiber officinale Roscoe
Structural Classification
Natural Products
Monophenols
Phenols
Plants
Source Classification
Zingiberaceae
|
Reference Standards
Others
|
|
10-Gingerol (Standard) is the analytical standard of 10-Gingerol (HY-N0448). This product is intended for research and analytical applications. 10-Gingerol is an AMPK agonist, which is found in the ginger oleoresin from fresh rhizome with anti-inflammatory, antioxidant and anti-proliferative activities. 10-Gingerol suppresses neointimal hyperplasia and inhibits vascular smooth muscle cell proliferation. 10-Gingerol exhibits substantial scavenging activities with an IC50 value of 10.47 μM against DPPH radical, an IC50 value of 1.68 μM against superoxide radical and an IC50 value of 1.35 μM against hydroxyl radical. 10-Gingerol inhibits the proliferation of MDA-MB-231 tumor cell line with an IC50 of 12.1 μM. 10-Gingerol suppresses the proliferation, migration, invasion, and induced apoptosis through targeting the PI3K/Akt signaling pathway in MDA-MB-231/IR cells. 10-Gingerol is promising for research of ulcerative colitis .
|
-
-
- HY-N4308
-
|
Hexa-O-methylquercetagetin; Quercetagetin hexamethyl ether; 3,5,6,7,3',4'-Hexamethoxyflavone
|
Flavonols
Structural Classification
Flavonoids
other families
Classification of Application Fields
Plants
Disease Research Fields
Source Classification
Cancer
|
NF-κB
IKK
Bcl-2 Family
|
|
Hexamethylquercetagetin (Hexa-O-methylquercetagetin; Quercetagetin hexamethyl ether; 3,5,6,7,3',4'-Hexamethoxyflavone) is an orally active NF-κB inhibitor. Hexamethylquercetagetin inhibits NF-κB-derived luciferase activity, reduces phosphorylated p65 and IκBα, Cyclin D1, Bcl-2 and blocks TNFα-induced NF-κB activation. Hexamethylquercetagetin inhibits survival and proliferation of cervical carcinoma cells. Hexamethylquercetagetin suppresses tumor volume and weight in BALB/c nude mouse xenograft models of cervical carcinoma. Hexamethylquercetagetin can be used for the research of cancer, such as cervical carcinoma .
|
-
-
- HY-N0475R
-
|
Hypolide (Standard); (+)-Triptophenolide (Standard)
|
Structural Classification
Monophenols
Terpenoids
Celastraceae
Phenols
Diterpenoids
Tripterygium wilfordii Hook. f.
Plants
Source Classification
|
Reference Standards
Androgen Receptor
Pyroptosis
Caspase
Bcl-2 Family
Apoptosis
|
|
Triptophenolide (Standard) (Hypolide) is the analytical standard of Triptophenolide (HY-N0475). This product is intended for research and analytical applications. Triptophenolide is a colorless crystal isolated from the ethyl acetate extract of Tripterygium wilfordii. Triptophenolide is an orally active pan‑antagonist of the androgen receptor (AR) with an IC50 of 467 nM against human wild‑type AR. Triptophenolide reduces AR expression, inhibits AR nuclear translocation, downregulates prostate‑specific antigen mRNA levels, and suppresses the growth of AR‑positive prostate cancer cells. Triptophenolide shows anti-tumor effects against breast cancer by inhibiting cell proliferation and migration, inducing G1-phase arrest and apoptosis, repressing xenograft tumor growth. Triptophenolide inhibits pyroptosis, alleviates tissue inflammation, and ameliorates synovial injury. Triptophenolide can be used for the study of prostate cancer, rheumatoid arthritis and breast cancer .
|
-
-
- HY-N19830
-
-
-
- HY-N1255A
-
|
(-)-Scoulerine hydrochloride; Discretamine hydrochloride
|
Structural Classification
Alkaloids
Phenols
Polyphenols
Umbelliferae
Plants
Isoquinoline Alkaloids
Carphephorus corymbosus (Nutt.) Torr. & A.Gray
Source Classification
|
Apoptosis
PI3K
Akt
mTOR
Adrenergic Receptor
GABA Receptor
Beta-secretase
Bcl-2 Family
|
|
Scoulerine ((-)-Scoulerine; Discretamine) hydrochloride is a multi-target inhibitor with anti-tumor and antioxidant activities. Scoulerine hydrochloride mainly targets the PI3K/Akt/mTOR signaling axis and α1D-adrenergic receptor, disrupts microtubule structure, and induces cell cycle arrest and apoptosis. Scoulerine hydrochloride effectively inhibits mitochondrial dehydrogenase activity, targets GABA receptors and BACE1, and suppresses the proliferation, migration, invasion, epithelial-mesenchymal transition and stem cell properties of cancer cells. Scoulerine hydrochloride also exhibits multiple pharmacological activities including anti-Plasmodium falciparum, antibacterial, antiemetic and antitussive effects, and regulates endoplasmic reticulum stress and mitochondrial function (modulates Bax, Bcl-2 and cytochrome c). Scoulerine hydrochloride is applicable to research related to leukemia, ovarian cancer, and colorectal cancer .
|
-
-
- HY-N0660R
-
|
|
Triterpenes
Structural Classification
other families
Terpenoids
Plants
Source Classification
|
Reference Standards
ERK
p38 MAPK
Akt
PI3K
11β-HSD
STING
VEGFR
Ferroptosis
Autophagy
Apoptosis
Keap1-Nrf2
Caspase
PARP
AMPK
|
|
Jujuboside B (Standard) is the analytical standard of Jujuboside B. This product is intended for research and analytical applications. Jujuboside B is a bioactive saponin component isolated from Ziziphi Spinosae Semen (sour jujube seed), with oral efficacy and blood-brain barrier permeability. Jujuboside B induces acute leukemia cell death and drives necroptosis apoptosis by activating the RIPK1/RIPK3/MLKL pathway. Jujuboside B upregulates the expression of NOXA, PARP and caspase-3, activates AMPK, inhibits the proliferation of breast cancer cells, and induces cell apoptosis and autophagy. Jujuboside B inhibits angiogenesis and tumor growth by blocking the VEGFR-2 signaling pathway. Jujuboside B alleviates liver injury in mice by regulating the Nrf2-STING signaling pathway . Jujuboside B alleviates liver injury by regulating anti-inflammatory responses and downregulating the expression of 11β-HSD2. Jujuboside B induces ferroptosis and overcomes radioresistance in non-small cell lung cancer via the PPARγ-ATF3-Gpx4 signaling pathway. Jujuboside B exerts inhibitory effects on platelet aggregation. Jujuboside B inhibits febrile seizures by suppressing the activity of AMPA receptors. Jujuboside B reverses chronic unpredictable mild stress-promoted tumor progression by blocking the PI3K/Akt and MAPK/ERK pathways and dephosphorylating CREB signaling. Jujuboside B is applicable to related studies on acute leukemia, breast cancer, PM2.5-induced lung injury, hepatotoxicity, liver injury, colorectal cancer, non-small cell lung cancer, thromboembolic diseases, cardiovascular diseases associated with high platelet aggregation, febrile seizures, and depressive-like phenotypes.
|
-
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-16938S1
-
1 Publications Verification
|
|
5'-Methylthioadenosine-d3 is the deuterium labeled 5'-Methylthioadenosine . 5'-Methylthioadenosine (5'-(Methylthio)-5'-deoxyadenosine) is a nucleoside generated from S-adenosylmethionine (SAM) during polyamine synthesis. 5'-Methylthioadenosine suppresses tumors by inhibiting tumor cell proliferation, invasion, and the induction of apoptosis while controlling the inflammatory micro-environments of tumor tissue. 5'-Methylthioadenosine and its associated materials have striking regulatory effects on tumorigenesis .
|
-
-
- HY-W654139
-
|
|
|
5'-Deoxy-5'-(methylthio)adenosine-d3 is deuterium labeled 5'-Methylthioadenosine. 5'-Methylthioadenosine (5'-(Methylthio)-5'-deoxyadenosine) is a nucleoside generated from S-adenosylmethionine (SAM) during polyamine synthesis . 5'-Methylthioadenosine suppresses tumors by inhibiting tumor cell proliferation, invasion, and the induction of apoptosis while controlling the inflammatory micro-environments of tumor tissue. 5'-Methylthioadenosine and its associated materials have striking regulatory effects on tumorigenesis.
|
-
-
- HY-16938S
-
|
|
|
5'-Methylthioadenosine- 13C6 is the 13C-labeled 5'-Methylthioadenosine. 5'-Methylthioadenosine (5'-(Methylthio)-5'-deoxyadenosine) is a nucleoside generated from S-adenosylmethionine (SAM) during polyamine synthesis . 5'-Methylthioadenosine suppresses tumors by inhibiting tumor cell proliferation, invasion, and the induction of apoptosis while controlling the inflammatory micro-environments of tumor tissue. 5'-Methylthioadenosine and its associated materials have striking regulatory effects on tumorigenesis .
|
-
-
- HY-W753201
-
|
|
|
5'-Methylthioadenosine- 13C (5'-(Methylthio)-5'-deoxyadenosine- 13C) is the 13C-labeled 5'-Methylthioadenosine (HY-16938). 5'-Methylthioadenosine (5'-(Methylthio)-5'-deoxyadenosine) is a nucleoside generated from S-adenosylmethionine (SAM) during polyamine synthesis . 5'-Methylthioadenosine suppresses tumors by inhibiting tumor cell proliferation, invasion, and the induction of apoptosis while controlling the inflammatory micro-environments of tumor tissue. 5'-Methylthioadenosine and its associated materials have striking regulatory effects on tumorigenesis .
|
-
-
- HY-16938S2
-
|
|
|
5'-Methylthioadenosine- 13C5 (5'-(Methylthio)-5'-deoxyadenosine- 13C5) is the 13C--labeled 5'-Methylthioadenosine (HY-16938). 5'-Methylthioadenosine (5'-(Methylthio)-5'-deoxyadenosine) is a nucleoside generated from S-adenosylmethionine (SAM) during polyamine synthesis . 5'-Methylthioadenosine suppresses tumors by inhibiting tumor cell proliferation, invasion, and the induction of apoptosis while controlling the inflammatory micro-environments of tumor tissue. 5'-Methylthioadenosine and its associated materials have striking regulatory effects on tumorigenesis .
|
-
-
- HY-180885S
-
|
|
|
KRAS G12D-IN-35 (example 7) is a potent and orally active KRAS G12D inhibitor. KRAS G12D-IN-35 suppresses p-ERK in AGS cells and potently inhibits the proliferation of various KRAS G12D-mutant cancer cell lines. KRAS G12D-IN-35 inhibits tumor growth in HPAC and GP2D mouse models. KRAS G12D-IN-35 can be used for cancer research, such as pancreatic and colorectal cancer .
|
-
-
- HY-W766368
-
|
|
|
C6 Ceramide- 13C2,d2 (C6-Cer- 13C2,d2) is the deuterium labeled and 13C-labeled C6 Ceramide (HY-19542). 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 .
|
-
| Cat. No. |
Product Name |
|
Classification |
-
- HY-159147
-
|
|
|
Azide
|
|
SIAIS039 is an orally active c-ros oncogene 1 (ROS1)-specific PROTAC with DC50s of 154.46 nM, 126.47 nM, 143.69 nM for HCC78 cells, Ba/F3 expressing the CD74-ROS1 fusion and Ba/F3 expressing the SDC4-ROS1 fusion, respectively. SIAIS039 suppresses cell proliferation, induces cell cycle arrest and apoptosis, and inhibits clonogenicity against ROS1-positive cells. SIAIS039 demonstrates anti-tumour effects against ROS1-driven tumor growth vivo. SIAIS039 is composed of the ALK inhibitor Brigatinib (HY-12857), a linker EM-12 (HY-138793), and a VHL ligand E3 ubiquitin ligase 1-Butyne (Red: Brigatinib; Blue: VHL ligand; Black: linker) .
|
-
- HY-180200
-
|
|
|
Alkynes
|
|
RNK08954 is an orally active KRASG12D inhibitor with a Kd of 0.0395 nM. RNK08954 selectively binds the inactive GDP-bound KRASG12D form, suppresses downstream KRAS-mediated signaling pathways p-ERK1/2 experssion. RNK08954 inhibits KRASG12D-mutant cell proliferation, induces G0-G1 cell cycle arrest, and inhibits tumor growth in mouse xenograft models. RNK08954 can be used for the research of non-small cell lung cancer, pancreatic ductal adenocarcinoma .
|
Your information is safe with us. * Required Fields.
Inquiry Information
- Product Name:
- Cat. No.:
- Quantity:
- MCE Japan Authorized Agent: