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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
2292 Results for "
cell-cycle
" in MedChemExpress (MCE) Product Catalog:
Products (2292)
2292 Results for "cell-cycle" in MCE Product Catalog:
Cat. No.: HY-181727
Research Areas:
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 .
Cat. No.: HY-181906
Target:
Research Areas:
ZnPc-PEG2-VH032 is a VHL-pathway-dependent photodegradation targeting chimera (PDTAC) and cytotoxic agent. ZnPc-PEG2-VH032 (HY-120217) binds to the VHL ligand domain, and then specifically degrades VHL under light irradiation, a process independent of non-specific ROS-mediated protein damage. ZnPc-PEG2-VH032 uses Zinc phthalocyanine (HY-19204) as a photosensitizer, and generates ROS via type I and type II photodynamic pathways under 680 nm LED irradiation. On one hand, it targets and degrades the bound VHL protein through ROS; on the other hand, it exerts direct photodynamic cytotoxicity. Meanwhile, the degradation of VHL downregulates the phosphorylation level of CDK2/4, induces cell cycle arrest in tumor cells, further enhances the sensitivity of tumor cells to oxidative damage caused by ROS, and achieves a synergistic anti-tumor effect. ZnPc-PEG2-VH032 exerts significant in vivo efficacy in an orthotopic mouse model of non-muscle invasive bladder cancer (NMIBC) .
Cat. No.: HY-182759
Research Areas:
MN33-47 is a multi-target anti-tumor compound with broad-spectrum anti-proliferative activity. MN33-47 relieves the inhibition of the mitochondrial apoptosis pathway by downregulating the anti-apoptotic protein Bcl-2, while activating caspase-3 and inhibiting Topoisomerase I activity, thereby promoting its degradation through the ubiquitin-proteasome and autophagy-lysosome pathways. MN33-47 can also induce DNA cross-linking and G2/M cell cycle arrest, inhibit cancer cell migration and activate the mitochondrial apoptosis pathway, thus exerting potent anti-tumor effects. MN33-47 can improve the water solubility of SN-38 (HY-13704), and exhibits dose-dependent tumor growth inhibition effects in CT26 tumor-bearing mouse models without obvious toxic and side effects. MN33-47 can be used in related studies on colorectal adenocarcinoma, cervical adenocarcinoma, hepatocellular carcinoma, alveolar basal epithelial adenocarcinoma, gastric cancer and colon cancer .
Cat. No.: HY-18719H
CAS No.: 1032008-71-1
Research Areas:
Endoxifen Z-isomer methanesulfonate is an orally active selective PKCβ1 inhibitor with an IC50 of 360 nM against human PKCβ1. It also acts as an estrogen receptor modulator and antiestrogen. Endoxifen Z-isomer methanesulfonate binds to and blocks ERα, ERβ and PKCβ1, inhibits estrogen and PI3K/AKT/mTORC1 signaling pathways, suppresses the expression of genes associated with cell cycle, cell proliferation and extracellular matrix remodeling, and induces apoptosis, reactive oxygen species (ROS) production and hypoxic features. Endoxifen Z-isomer methanesulfonate inhibits tumor growth in breast tumor and glioblastoma models, reduces bone turnover and blood lipid levels, and does not require metabolism via CYP2D6. It can be used in research related to ER + breast cancer, invasive breast cancer, glioblastoma multiforme, type I bipolar disorder, desmoid tumor, gynecological malignancies, melanoma and hormone receptor-positive solid tumors .
Cat. No.: HY-N0819R
CAS No.: 89412-79-3
Category:
Cat. No.: HY-N7695
CAS No.: 23133-56-4
Cat. No.: HY-W013724S
Synonyms: IDP-15N4 dilithium; Inosine-5'-diphosphoric acid-15N4 disodium
Cat. No.: HY-109061A
CAS No.: 2411549-88-5
Synonyms: YH25448 mesylate hydrate; GNS-1480 mesylate hydrate
Lazertinib (YH25448; GNS-1480) mesylate hydrate is an orally active, blood-brain barrier permeable third-generation EGFR tyrosine kinase inhibitor, as well as an ABCB1/ABCG2 inhibitor and a TRPA1 activator. Lazertinib mesylate hydrate exhibits IC50 values of 0.4 mM and 0.2 mM against human ABCB1 and ABCG2, respectively. By inhibiting mutant EGFR signaling, EGFR phosphorylation and the downstream ERK/AKT pathway, as well as upregulating surface expression of EGFR/MET, Lazertinib mesylate hydrate induces cell cycle arrest, apoptosis, spontaneous calcium responses, hyperexcitability of dorsal root ganglion (DRG) neurons, and TRPA1-dependent pain-like behaviors. Lazertinib mesylate hydrate competitively binds to the substrate-binding sites of ABCB1/ABCG2, stimulates their ATPase activity without altering their expression or plasma membrane localization, thereby enhancing ADCC activity, acting as a chemosensitizer, and reversing ABCB1-mediated multidrug resistance. It exerts antitumor activity as a single agent or in combination with other drugs. Lazertinib mesylate hydrate is applicable to research related to non-small cell lung cancer, multidrug-resistant cancers, and paresthesia .
Synonyms: 15-Deoxy-Δ12,14-PGD2
Research Areas:
15-deoxy-Δ12,14-Prostaglandin D2 (15-Deoxy-Δ12,14-PGD2) is a metabolite of prostaglandin D₂ (PGD₂) (HY-101988), which can undergo further dehydration metabolism to 15-deoxy-Δ12,14-PGJ₂. 15-deoxy-Δ12,14-Prostaglandin D2 is a highly selective agonist for DP2 receptor and PPARγ. 15-deoxy-Δ12,14-Prostaglandin D2 causes morphological changes in eosinophils and migration of type II innate lymphoid cells (ILC2). 15-deoxy-Δ12,14-Prostaglandin D2 has a growth inhibitory effect on prostate cancer cells expressing PPARγ, induces cell cycle arrest and promotes apoptosis. 15-deoxy-Δ12,14-Prostaglandin D2 can be used in related research on asthma and prostate cancer .
Cat. No.: HY-164729
Cat. No.: HY-181163
Research Areas:
Caspase-3/7 activator 4 is a caspase-3 activator and caspase-7 activator. Caspase-3/7 activator 4 inhibits key enzymes in estrogen biosynthesis, including aromatase (IC50 = 38.3 nM) and steroid sulfatase (IC50 = 12.7 µM), and selectively suppresses COX-2 (IC50 = 5.38 µM). Caspase-3/7 activator 4 shows strong antioxidant activity (DPPH: IC50 = 16.26 µM). Caspase-3/7 activator 4 inhibits estrogen synthesis, suppresses estrogen availability, reduces prostaglandin production, increases caspase-3/7 expression, induces G0/G1 cell cycle arrest, induces apoptotic cell death, reduces circulating TNF-α and VEGFR-II levels, restores hepatorenal function markers and histoarchitecture, restores antioxidant defense enzyme activity, reduces lipid peroxidation, exerts antiproliferative activity against breast cancer cells, exerts antitumor activity in the Ehrlich ascites carcinoma models. Caspase-3/7 activator 4 can be used for the research of breast cancer, ehrlich ascites carcinoma .
Cat. No.: HY-184378
CAS No.: 2922221-22-3
Target:
Research Areas:
MDB5 is a Hedgehog pathway and Smoothened inhibitor that binds to the 7-TM domain of Smo . MDB5 reduces hepatic stellate cell activation, extracellular matrix-related gene expression, collagen deposition, hydroxyproline content and epithelial-mesenchymal transition, and prevents sinusoidal endothelial cell capillarization . MDB5 induces G1 and S phase cell cycle arrest, triggers apoptosis by upregulating Bax and downregulating Bcl-2, and also decreases oxygen consumption rate, glucose uptake, transglutaminase activity and fibronectin matrix assembly . MDB5 reduces the levels of liver injury markers, hepatic triglyceride deposition and hepatic steatosis, restores the tissue structure of the kidney and spleen, and inhibits pancreatic tumor growth without causing body weight loss . MDB5 can be loaded into PEG-PCC-g-DC micelles, achieving high drug loading, sustained release, improved water solubility, enhanced cellular uptake and optimized hepatic distribution, with good tolerance in mice . MDB5 is applicable to research related to alcohol-associated liver disease, liver fibrosis and pancreatic cancer .
Cat. No.: HY-N0566
CAS No.: 85999-40-2
Synonyms: Anemosapogenin
Cat. No.: HY-N20674
CAS No.: 76472-89-4
Category:
Research Areas:
U7D-1 is a USP7 PROTAC degrader that induces selective proteasomal degradation of USP7. U7D-1 destabilizes and downregulates the expression of variant PRC1 complex subunits PCGF1, RING1A and PCGF6, and also slightly reduces the protein level of KDM2B. U7D-1 decreases cell viability, arrests neuroblastoma cells at the G0/G1 cell cycle phase, and downregulates the expression of target genes of PAX3::FOXO1 in FP-RMS cells. U7D-1 increases the level of cleaved PARP in FP-RMS cells, induces cell apoptosis, and upregulates the expression of muscle differentiation markers MYH1 and MYF5. U7D-1 inhibits the growth and proliferation of p53 wild-type and mutant cancer cells, and regulates the apoptosis pathway and E2F pathway. U7D-1 is applicable to studies on neuroblastoma, fusion-positive rhabdomyosarcoma, p53-mutant cancers and cancer-related research .
Cat. No.: HY-170576
FLT3-IN-28 (Compound 12y) is an orally active FLT3 inhibitor with antitumor activity. FLT3-IN-28 selectively inhibits cancer cells harboring the FLT3 internal tandem duplication (ITD) mutation, with IC50 values of 85, 290, 130, 65, and 220 nM for BaF3-FLT3-ITD, BaF3-TEL-VEGFR2, MV4-11, MOLM-13, and MOLM-14 cell lines respectively (MV4-11 and MOLM-13/14 are acute myeloid leukemia (AML) cell lines carrying the FLT3-ITD mutation). Additionally, FLT3-IN-28 can downregulate the phosphorylation levels of FLT3 and STAT5 in MOLM-13 cells and induce cell cycle arrest and Apoptosis. FLT3-IN-28 has an oral bioavailability of 19.2% in SD rats and can prolong survival in a dose-dependent manner in NSG mice xenografted with MOLM-13 cells. FLT3-IN-28 holds promise for research in cancer fields related to FLT3-ITD .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
