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DiSC3(5) is a fluorescent probe commonly used as a tracer dye to evaluate mitochondrial membrane potential. The excitation/emission wavelength of DiSC3(5) is up to 622/670 nm. DiSC3(5) can inhibit the respiratory system associated with mitochondrial NAD, and the IC50 value is 8 μM. DiSC3(5) in the presence of Na +/K +-ATPase inhibitor ouabain 2 can induce membrane hyperpolarization of Ehrlich ascites tumorcells .
MANS peptide is an inhibitor for myristoylated alanine-rich C kinase substrate (MARCKS), which competes with MARCKS in cells for membrane binding, and thus inhibits the stimulation of mucin secretion and tumor metastasis .
Tachyplesin I is a β-hairpin antimicrobial peptide that contains 17 amino acid residues. Tachyplesin I exhibits cytotoxic properties against various human tumorcell lines acting primarily by impairing the integrity of the outer cellmembrane .
CP-46665 dihydrochloride is an anticancer agent that inhibits the incorporation of tritiated thymidine into leukemia cells and human solid tumorcells in vitro. It can lead to the loss of surface characteristics in tumorcells and disrupt cellmembranes, inhibiting cell proliferation .
d-(KLAKLAK)2, as an antibacterial and anti-tumor polypeptide, is a representative of the antimicrobial peptide group, and also has good anticancer properties. d-(KLAKLAK)2 is able to kill bacteria by damaging their cellmembranes, causing cell contents to leak out. d-(KLAKLAK)2 can also inhibit tumorcell proliferation by causing mitochondrial swelling and mitochondrial membrane destruction, triggering apoptosis (programmed cell death) .
Tolnapersine exhibits multidrug resistance (MDR) reversal activity, which reverses the resistance of tumorcells to multiple chemotherapy drugs by affecting P-glycoprotein (Pgp) on the cellmembrane .
MTIC-d3 is deuterium labeled MTIC. MTIC is the active metabolite of Temozolomide (TMZ). MITC has lower bioavailability in the brain compared with TMZ, because the agent’s permeability through biological barriers and tumorcellmembranes affects bioavailability. MITC exhibits low affinity to biological membrane[1].
CHD-1 is a a hypoxia-activated antitumor prodrug. CHD-1 impairs mitochondrial morphology and membrane potential in hypoxic tumorcells, further triggering excessive mitophagy and inducing apoptosis. CHD-1 inhibits the growth of hypoxic tumorcells in vitro and the growth of HeLa xenograft in vivo .
IPH10 is an anti-cancer agent that exhibits a strong anti-tumor effect in vivo without hepatic and renal toxicity. IPH10 can significantly increase the content of ROS, decrease the mitochondrial membrane potential, and induce apoptosis in tumorcells .
Tachyplesin I TFA is a β-hairpin antimicrobial peptide that contains 17 amino acid residues. Tachyplesin I TFA exhibits cytotoxic properties against various human tumorcell lines acting primarily by impairing the integrity of the outer cellmembrane .
BTCy is a near-infrared (NIR) fluorescence probe with polarity-responsive and cell plasma membrane-targeting properties. BTCy can be used for in vivo imaging of tumor tissue (λex = 561 nm, λem = 600-700 nm) .
Biotin-NH-PSMA-617 is a biotin-tagged PSMA-617. PSMA-617 is a small molecule targeting the prostate-specific membrane antigen (PSMA), which is directly expressed by the tumorcells .
CyPep-1 is a novel cationic lytic peptide with antitumor activity. CyPep-1 is highly cytotoxic by interacting with the negatively charged cellmembrane of cancer cells. CyPep-1 has strong cytolytic activity on cancer cells both in vivo and in vitro, and can be used in the study of solid tumors .
RS17 is an anti-tumor peptide designed to bind specifically to the CD47 molecule and block the interaction between CD47 and its ligand, SIRPα, on the surface membrane of macrophages. The main regulatory mechanism of RS17 is to prevent CD47 from transmitting selective phagocytosis signals to SIRPα by binding to CD47, so that macrophages do not recognize tumorcells as their own tissue, but phagocytose them as foreign substances, thereby inhibiting immune escape of tumorcells. RS17 can be used to study the mechanism of anti-tumor response and immune escape .
Cevostamab (BFCR4350A; RG6160; RO7187797) is a humanized IgG1-based BsAb that targets membrane-proximal extracellular domain of FcRH5 on multiple myeloma (MM) cells as well as CD3 on T cells. Moreover, Cevostamab facilitates efficient synapse formation, improves killing activity of T cells against MM tumorcells .
PKMYT1-IN-1 (Compound 1) is an inhibitor for membrane-associated tyrosine and threonine kinase (PKMYT1), with an IC50 of 8.8 nM. PKMYT1-IN-1 inhibits proliferation of tumorcell HCC1569 with IC50 of 42 nM .
Cysmethynil is an Icmt inhibitor(IC50 = 2.4 μM). Cysmethynil inhibites RAS membrane binding and EGF signal transduction. Cysmethynil prevents the cells in the G1 phase and induces autophagy. Cysmethynil inhibits PC3 cells proliferation, has synergistic effect with Paclitaxel (HY-B0015) and Doxorubicin (HY-15142A). Cysmethynil has anti-tumor effects and can be used for solid tumor (such as prostate cancer et al.) research .
Porfimer sodium (Photofrin II) is a photosensitizing compound used primarily for photodynamic inhibition. Porfimer sodium is selectively taken up by tumorcells and can generate oxygen free radicals upon activation. Porfimer sodium causes changes in Ca(2+) concentrations within cells, exhibiting acute electrophysiological responses and changes in cell morphology. The application of porfimer sodium can lead to the formation of micropores on the cellmembrane surface, resulting in necrotic cell death .
tert-Butyl-DCL is a small molecule PSMAM inhibitor with anticancer activity that targets prostate-specific membrane antigen (PSMA). tert-Butyl-DCL is also an effective bioimaging agent that has high selectivity and affinity, allowing it to target and highlight specific receptors on the surface of tumorcells .
IALYLQQNW is a specific nonapeptide sequence derived from the tumor-associated antigen latent membrane protein 1 (LMP1) encoded by Epstein-Barr virus (EBV). As a latent T-cell epitope, IALYLQQNW is able to activate EBV-specific cytotoxic T lymphocytes (CTLs), which are able to recognize and kill EBV-infected cells expressing LMP1. IALYLQQNW plays an important role in the immune response against EBV-associated tumors and can be used in the study of Hodgkin's disease and nasopharyngeal carcinoma .
MANS peptide TFA is the TFA salt form of MANS peptide (HY-P10218). MANS peptide TFA is an inhibitor for myristoylated alanine-rich C kinase substrate (MARCKS), which competes with MARCKS in cells for membrane binding, and thus inhibits the stimulation of mucin secretion and tumor metastasis .
Phosphorylethanolamine (Standard) is the analytical standard of Phosphorylethanolamine. This product is intended for research and analytical applications. Phosphorylethanolamine (Monoaminoethyl phosphate) is present in most animal tissues and is also present in various human extracranial tumors. Phosphorylethanolamine is considered as the intermediate product of phospholipid metabolism. Phosphorylethanolamine is essential for the formation and maintenance of the cellmembrane .
EAPB0503 is a quinoline compound with anti-tumor activity, showing strong cytotoxicity against melanoma cells in vitro (IC50=200 nM). EAPB0503 can induce specific cell cycle arrest in mitosis of CML cells and directly activate apoptosis, leading to an increase in the G0 cell population, disruption of mitochondrial membrane potential, PARP cleavage, and DNA fragmentation. EAPB0503 also reduces the levels of BCR-ABL protein .
BMS-214662 is a farnesyl transferase inhibitor. BMS-214662 can effectively block the localization and function of Ras protein in the cellmembrane by inhibiting the pro-group modification of Ras protein, thereby exerting anti-tumor activity. BMS-214662 has an IC50 value of 1.3 nM for H-Ras and 8.4 nM for K-Ras. BMS-214662 can be used to study Ras-related tumor diseases .
BMS-214662 hydrochloride is an inhibitor of farnesyltransferase (Farnesyl Transferase). BMS-214662 hydrochloride can effectively block the localization and function of Ras proteins on the cellmembrane by inhibiting the prenylation modification of Ras proteins, thereby exerting anti-tumor activity. The IC50 value of BMS-214662 hydrochloride for H-Ras is 1.3 nM, and for K-Ras it is 8.4 nM. BMS-214662 hydrochloride can be used in the research of tumor diseases related to Ras .
HYNIC-PSMA is a ligand for molecular imaging of tumors. Hynic-psma consists of two components: HYNIC (6-hydrazinonicotinamide) and PSMA (Prostate-Specific Membrane Antigen). HYNIC is a compound used to attach radioactive isotopes to targeted molecules, such as 188Re-HYNIC-PSMA. PSMA is a membrane antigen that is specifically expressed on the surface of prostate cancer cells. HYNIC-PSMA can be used in prostate cancer research . HYNIC-PSMA can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
Lewis X trisaccharide (Lewis X, Le x) is a potent TH2 regulator, antagonizes LPS-induced IL-12 immune expression. Lewis X trisaccharide is a human histo-blood group antigen, plays an key role in cell-cell adhesion, and servers as a tumor marker. Lewis X trisaccharide is highly expressed in the outer membrane of the parasite, can be used for the immunology research of schistosomiasis .
Anticancer agent 59 (compound 11) has inhibitory activity against kinds of cancer cell lines, especially in A549 with IC50 of 0.2 μM. Anticancer agent 59 induces apoptosis and an increase of Ca 2+ and ROS in cancer cells. Anticancer agent 59 significantly decreases mitochondrial membrane potential. Anticancer agent 59 can suppress tumor growth in A549 mouse xenograft model .
Phosphorylethanolamine (Monoaminoethyl phosphate) is a membrane phospholipid and an important precursor of Phosphatidylcholine (HY-B2233B). It is found in most animal tissues and various human extracranial tumors, playing a critical role in membrane integrity, cell division, mitochondrial respiratory function, and more. Studies have shown that changes in the abundance of Phosphorylethanolamine are associated with Alzheimer's disease and Parkinson's disease. Lowering the ratio of Phosphorylethanolamine to Phosphatidylcholine in the liver can improve insulin signaling. Phosphorylethanolamine holds promise for research in the fields of cancer, neurodegenerative disorders, and metabolic diseases .
IMAB027 (ASP1650) is a specific anti-CLDN6 mAb, while CLDN6 (Claudin 6) is a tight junction membrane protein, aberrantly expressed in various human cancer types, ovarian cancers particularly. IMAB 027 shows anti-tumor activity, and induces apoptosis in CLDN6 + ovarian and testicular cancer cell lines .
GL0388 is a Bax activator that results in Bax insertion into mitochondrial membrane. GL0388 shows antiproliferative activities against various cancer cells, with IC50s of 0.299-1.57 μM. GL0388 activates Bax and induce Bax-mediated apoptosis. GL0388 suppresses breast cancer xenograft tumor growth in vivo .
Antitumor agent-115 (SS-12) is an effective anti-tumor compound with an IC50 value of 0.34 μM-24.14 μM for cell line 4T1. Antitumor agent-115 can block the cell cycle of mouse breast cancer cell line 4T1, reduce the mitochondrial membrane potential, and induce apoptosis, and the IC50 value is 8-25 μmol/L for cell viability. Antitumor agent-115 can be used for breast cancer research .
Apoptosis inducer 30 (Compound 15a) is an anticancer agent. Apoptosis inducer 30 induces MCF-7 cellsapoptosis through mitochondrial pathway. Apoptosis inducer 30 induces intracellular reactive oxygen species levels and decreases mitochondrial membrane potential, and blocks the cell cycle in the G0/G1 phase. Apoptosis inducer 30 inhibits cell growth, with an IC50 value of 0.32 μM against MCF-7 cells, and inhibits tumor growth in a mouse model of breast cancer .
Antitumor agent-190 (Compound 26) is a Hexokinase 2 inhibitor that demonstrates significant anti-tumor activity by targeting microtubules and Hexokinase 2, with an IC50 value of 0.764 μM against MD-MBA-231 cells. Antitumor agent-190 effectively inhibits the activity of Hexokinase 2, leading to the accumulation of Reactive Oxygen Species and dysfunction of the mitochondrial membrane potential (MMP), thereby promoting apoptosis and blocking the cell cycle .
Apoptosis inducer 32 (Compound 7g) is an apoptosis inducer with a KD of 42 μM, showing anti-tumor activity. Apoptosis inducer 32 caused significant cellular morphological changes in MDA-MB-231 cells, including membrane bubbling, nuclear fragmentation, and apoptotic body formation. The IC50 of Apoptosis inducer 32 in MCF-7, MDA-MB-231, and HEK cells is 4.77, 6.56 and 337.8 μM respectively .
Lysosomal P-gp targeted agent 1 (Compound 14) is an anti-tumor agent targeting lysosomal P-glycoprotein (Pgp). Lysosomal P-gp targeted agent 1 is selectively transported into lysosomes by overexpressed Pgp, release nitric oxide (NO) to generate reactive oxygen species (ROS), resulting in lysosomal membrane permeabilization (LMP) and inducing apoptosis. Lysosomal P-gp targeted agent 1 can overcome P-glycoprotein-mediated drug resistance and lead to cell cycle arrest, but relatively low toxicity to normal cells. Lysosomal P-gp targeted agent 1 has antitumor activity, significantly inhibits tumor volume .
DW10075 is a highly selective and orally active VEGFR inhibitor targeting the VEGF/VEGFR pathway. DW10075 selectively inhibits VEGFR-1, VEGFR-2, and VEGFR-3, but has no effect on FGFR and PDGFR. DW10075 inhibits VEGF-induced HUVEC proliferation, migration, and tube formation. And DW10075 inhibits angiogenesis in both the rat aortic ring model and the chick chorionic membrane model. DW10075 also exhibits antiproliferative activity against human cancer cell lines, with IC50s of 2.2 μM and 22.2 μM against U87-MG human glioblastoma cells and A375 melanoma cells, respectively. In the nude mouse U87-MG xenograft tumor model, DW10075 (po) significantly inhibits tumor growth and reduces the expression of CD31 and Ki67 in tumor tissues.
1-Stearoyl-sn-glycerol 3-phosphate sodium is a bioactive phospholipid that plays a crucial role in modulating cellular processes such as motility, proliferation, invasion, survival, and growth factor production, primarily through its interaction with G protein-coupled receptors (GPCRs). Typically found at low concentrations in plasma (~100nM), this compound is synthesized during the formation of membrane phospholipids and is derived from various cell types, including activated platelets, epithelial cells, leukocytes, neuronal cells, and tumorcells. Its unique structure includes stearic acid at the sn-1 position alongside a hydroxyl group at the sn-2 position.
Squalamine (MSI-1256) is an aminosterol compound with broad-spectrum antiviral activity. Squalamine makes cells less conducive to certain viral replication by altering the electrostatic interactions in the inner membrane of host cells. Squalamine also has antibacterial and antitumor activities. Squalamine has broad-spectrum antibacterial activity against Gram-negative and Gram-positive bacteria, fungi and protozoa. Squalamine inhibits tumor-related angiogenesis and the growth of human breast cancer cells. Squalamine restores the function of enteric nervous system in Parkinson ,s disease mouse models .
BQ7876 is a probe targeting prostate-specific membrane antigen (PSMA) that contains a DOTA chelator. BQ7876, after being radiolabeled with radionuclide (177Lu), functions in both radionuclide imaging and tumorcell destruction by specifically binding to PSMA. BQ7876 shows potential for research in the field of metastatic castration-resistant prostate cancer (mCRPC) . BQ7876 can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
API-1 is a potent selective Akt/PKB inhibitor that reduces the level of phosphorylated Akt (IC50 = 0.8 μM). API-1 binds to the PH domain and inhibits Akt membrane translocation. API-1 induces c-FLIP degradation. API-1 reduces cell proliferation and induces apoptosis. API-1 decreases tumor growth in mouse xenograft model .
p38-α MAPK-IN-8 (Compound 13) is a lipophilic cationic derivative. p38-α MAPK-IN-8 is cytotoxic to various tumorcells, and can induce cell cycle arrest, apoptosis, increase reactive oxygen species (ROS) production, and induce mitochondrial membrane potential depolarization. The antitumor activity of p38-α MAPK-IN-8 may be related to p38α MAPK pathway, which can be used in the study of cancer .
Anticancer agent 58 (compound 16) has inhibitory activity against kinds of cancer cell lines, especially in A549 and T24 with IC50s of 0.6 μM and 0.7 μM, respectively. Anticancer agent 58 induces apoptosis by activating caspase 3/8/9 activity, and induces an increase of Ca 2+ and ROS in cancer cells. Anticancer agent 58 significantly decreases mitochondrial membrane potential. Anticancer agent 58 can suppress tumor growth in T24 mouse xenograft model .
N-Acetyl-L-tyrosine is an orally active endogenous mitochondrial stress response regulator that can permeate the cellmembrane by passive diffusion. N-Acetyl-L-tyrosine induces low-level reactive oxygen species (ROS) generation by transiently perturbing mitochondrial membrane potential, triggering reverse signaling to activate FoxO and Keap1 pathways. As a result, N-Acetyl-L-tyrosine enhances the expression of antioxidant enzyme genes, exerting anti-stress and cytoprotective effects. N-Acetyl-L-tyrosine can improve heat stress tolerance, inhibit tumor growth, and regulate energy metabolism. N-Acetyl-L-tyrosine can be used in the research of aging, metabolic diseases (such as diabetes), and cancer .
MTIC (Standard) is the analytical standard of MTIC. This product is intended for research and analytical applications. MTIC, the active metabolite of Temozolomide (TMZ), is a DNA alkylating agent. MTIC has antitumor activity
[1][2][3][4].
Azacyclonol (γ-pipradol) hydrochloride is a compound with promising anticancer activity, showing effectiveness in inhibiting NOX-derived ROS in A549 human lung cancer cells. Azacyclonol hydrochloride exhibits enhanced proliferation inhibition against androgen-refractory cancer cell lines, specifically DU145 and PC-3. Azacyclonol hydrochloride demonstrates antitumor activity in DU145-xenografted chorioallantoic membranetumor models. Azacyclonol hydrochloride also acts as a ligand for the M3 muscarinic acetylcholine receptor, which is overexpressed in ARPC. Azacyclonol hydrochloride effectively blocks carbachol-induced proliferation and NOX activity in DU145 cells. Azacyclonol hydrochloride can also be utilized for the treatment of chronic schizophrenia.
VEGFR-2-IN-51 (compound 19) is an orally active dual-target inhibitor of VEGFR-2 (IC50=15.33 μM) and tubulin (IC50=0.76 μM) with anti-tumor activity. VEGFR-2-IN-51 induces tumorcellapoptosis by reducing mitochondrial membrane potential and increasing reactive oxygen species (ROS) levels. VEGFR-2-IN-51 exerts anti-angiogenic effects by blocking the VEGFR-2/PI3K/AKT signaling pathway. In addition, VEGFR-2-IN-51 has significant anti-proliferative activity against the gastric cancer cell line MGC-803 (IC50=0.005 μM) .
GR 159897 is a highly potent, selective, competitive, brain-penetrated non-peptide neurokinin 2 (NK2) receptor antagonist. GR 159897 has little or no affinity for NK1 and NK3 receptors. GR 159897 inhibits binding of [ 3H]GR100679 to human NK2 (hNK2)-CHO cells and rat colon membranes with pKis of 9.51 and 10, respectively. Antagonizes bronchoconstriction. Anxiolytic-like and anti-tumor effects .
Collagenase, Type VI (EC 3.4.24.3) is a collagenase that can degrade type VI collagen. Type VI collagen is a component of cellmembranes in various tissues (such as skin, heart, blood vessels, cartilage, and synovial fluid). Excessive collagenase can cause extracellular matrix lesions. Collagenase is also a biomarker for tumor invasion and metastasis. Collagenase, Type VI can specifically act on the peptide bond between proline and glycine. This feature can be used to quickly and sensitively detect its concentration level in experiments using corresponding modified electrodes .
anti-TNBC agent-8 (Compound TP2) is a photodynamic therapeutic agent targeting mitochondrial DNA G4 (mtG4). Under white light irradiation, its IC50 against 4T1 cells is 0.42 μM. anti-TNBC agent-8 binds tightly to mtG4 and generates a large amount of reactive oxygen species (ROS) under white light irradiation, leading to the loss of mitochondrial membrane potential (MMP), a decrease in ATP production, and an increase in the ROS level. This, in turn, induces significant apoptosis in triple-negative breast cancer (TNBC) cells, exerting the activity of inhibiting tumorcell growth. anti-TNBC agent-8 can be used in the research of triple-negative breast cancer.
PI3Kα-IN-14 (compound F8) is a selective PI3Kα inhibitor with an IC50 of 0.14 nM. PI3Kα-IN-14 induces a great decrease in mitochondrial membrane which caused cell cycle arrest at G1 phase and apoptosis in U87-MG cells. PI3Kα-IN-14 shows significant anti-proliferative activities against three tumor-derived cell lines (PC-3: IC50 of 0.28 μM; HCT-116: IC50 of 0.57 μM; and U87-MG: IC50 of 1.37 μM) .
N-Acetyl-L-tyrosine (Standard) is the analytical standard of N-Acetyl-L-tyrosine (HY-W012382). This product is intended for research and analytical applications. N-Acetyl-L-tyrosine is an orally active endogenous mitochondrial stress response regulator that can permeate the cellmembrane by passive diffusion. N-Acetyl-L-tyrosine induces low-level reactive oxygen species (ROS) generation by transiently perturbing mitochondrial membrane potential, triggering reverse signaling to activate FoxO and Keap1 pathways. As a result, N-Acetyl-L-tyrosine enhances the expression of antioxidant enzyme genes, exerting anti-stress and cytoprotective effects. N-Acetyl-L-tyrosine can improve heat stress tolerance, inhibit tumor growth, and regulate energy metabolism. N-Acetyl-L-tyrosine can be used in the research of aging, metabolic diseases (such as diabetes), and cancer .
N-Acetyl-L-tyrosine-d3 is the deuterated form of N-Acetyl-L-tyrosine (HY-W012382). N-Acetyl-L-tyrosine is an orally active endogenous mitochondrial stress response regulator that can permeate the cellmembrane by passive diffusion. N-Acetyl-L-tyrosine induces low-level reactive oxygen species (ROS) generation by transiently perturbing mitochondrial membrane potential, triggering reverse signaling to activate FoxO and Keap1 pathways. As a result, N-Acetyl-L-tyrosine enhances the expression of antioxidant enzyme genes, exerting anti-stress and cytoprotective effects. N-Acetyl-L-tyrosine can improve heat stress tolerance, inhibit tumor growth, and regulate energy metabolism. N-Acetyl-L-tyrosine can be used in the research of aging, metabolic diseases (such as diabetes), and cancer .
ALK/EGFR-IN-1-d5 (Compound (-)-9a) is a deuterated dual-target inhibitor of EGFR and ALK, with an IC50 of 1.08 nM for EGFR and an IC50 of 2.395 nM for ALK. ALK/EGFR-IN-1-d5 inhibits the phosphorylated proteins in the EGFR, ALK, and BRK signaling pathways, blocking the cell cycle, leading to a reduction in mitochondrial membrane potential and cell apoptosis (Apoptosis). ALK/EGFR-IN-1-d5 also significantly inhibits tumor growth in animal models and demonstrates good safety. ALK/EGFR-IN-1-d5 holds promise for research in the field of cancer treatment
Lipid C2 is an ionizable cationic lipid that has been used in the formation of lipid nanoparticles (LNP) for mRNA delivery in vivo. LNPs containing Lipid C2 and encapsulating an mRNA reporter selectively accumulate in the liver and spleen but not the heart, lungs, or kidneys in mice. LNP containing Lipid C2 and encapsulating mRNA encoding the Epstein-Barr virus (EBV) protein latent membrane protein 2 (LMP-2), in combination with an anti-programmed cell death protein 1 (PD-1) antibody, decrease tumor volume and reverse T cell exhaustion, as well as increase the percentage of CD3 +CD8 + central and CD3 +CD8 + effector memory T cells and decrease the percentage of CD3 + T cells expressing Pd-1, in the spleen in a CT26 murine EBV-infected colon cancer model .
PT-129 is an RPOTAC degrader targeting the NTF2 domain (protein-RNA interaction site) of G3BP1/2, which mediates the disassembly of intracellular stress granules. PT-129 can inhibit the formation of stress granules in stressed cells and disassemble existing stress granules, and can disrupt the transmission of ATF4, thereby inhibiting the proliferation of cancer cells. Stress granules (SGs) are membrane-less cytoplasmic compartments formed under stress stimuli. SGs promote the transmission of ATF4 from fibroblasts to tumorcells through a migratory effect, mediating fibroblast-related tumor growth. And G3BP1/2 is a central protein of the SGs network, and the inhibition of G3BP1/2 may reduce the stress resistance of cancer cells in the tumor microenvironment. PT-129 is composed of a target protein ligand (red part) G3BP1/2-Targeting ligand-1 (HY-170873), an E3 ligase ligand (blue part) Thalidomide 4-fluoride (HY-41547), and a PROTAC linker (black part) Amino-PEG3-C2-acid (HY-W040165); among them, the E3 ligase ligand + linker form a complex Thalidomide-NH-PEG3-propionic acid (HY-136166) .
Meso-tetraphenylchlorin (TPCS2a) is a photosensitizer with poor water solubility, which limits its use in the blood circulation. However, TPCS2a@NPs nanoparticles can be prepared based on polylactic-co-polyethylene glycol acid (PLGA) polymer core loaded with TPCS2. Such nanoparticles can be coated with mesenchymal stem cell-derived plasma membranes (mMSCs) to form mMSC-TPCS2a@NPs, which prolongs blood circulation time and improves tumor targeting ability. Compared with uncoated TPCS2a@NPs, mMSC-TPCS2a@NPs can reduce macrophage uptake by 54% to 70% under different conditions. Both nanoparticle forms are effectively accumulated in MCF7 and MDA-MB-231 breast cancer cells, while uptake in normal breast epithelial cells MCF10A is significantly lower .
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 2,620 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.
DiSC3(5) is a fluorescent probe commonly used as a tracer dye to evaluate mitochondrial membrane potential. The excitation/emission wavelength of DiSC3(5) is up to 622/670 nm. DiSC3(5) can inhibit the respiratory system associated with mitochondrial NAD, and the IC50 value is 8 μM. DiSC3(5) in the presence of Na +/K +-ATPase inhibitor ouabain 2 can induce membrane hyperpolarization of Ehrlich ascites tumorcells .
tert-Butyl-DCL is a small molecule PSMAM inhibitor with anticancer activity that targets prostate-specific membrane antigen (PSMA). tert-Butyl-DCL is also an effective bioimaging agent that has high selectivity and affinity, allowing it to target and highlight specific receptors on the surface of tumorcells .
MANS peptide is an inhibitor for myristoylated alanine-rich C kinase substrate (MARCKS), which competes with MARCKS in cells for membrane binding, and thus inhibits the stimulation of mucin secretion and tumor metastasis .
Tachyplesin I is a β-hairpin antimicrobial peptide that contains 17 amino acid residues. Tachyplesin I exhibits cytotoxic properties against various human tumorcell lines acting primarily by impairing the integrity of the outer cellmembrane .
RS17 is an anti-tumor peptide designed to bind specifically to the CD47 molecule and block the interaction between CD47 and its ligand, SIRPα, on the surface membrane of macrophages. The main regulatory mechanism of RS17 is to prevent CD47 from transmitting selective phagocytosis signals to SIRPα by binding to CD47, so that macrophages do not recognize tumorcells as their own tissue, but phagocytose them as foreign substances, thereby inhibiting immune escape of tumorcells. RS17 can be used to study the mechanism of anti-tumor response and immune escape .
IALYLQQNW is a specific nonapeptide sequence derived from the tumor-associated antigen latent membrane protein 1 (LMP1) encoded by Epstein-Barr virus (EBV). As a latent T-cell epitope, IALYLQQNW is able to activate EBV-specific cytotoxic T lymphocytes (CTLs), which are able to recognize and kill EBV-infected cells expressing LMP1. IALYLQQNW plays an important role in the immune response against EBV-associated tumors and can be used in the study of Hodgkin's disease and nasopharyngeal carcinoma .
MANS peptide TFA is the TFA salt form of MANS peptide (HY-P10218). MANS peptide TFA is an inhibitor for myristoylated alanine-rich C kinase substrate (MARCKS), which competes with MARCKS in cells for membrane binding, and thus inhibits the stimulation of mucin secretion and tumor metastasis .
d-(KLAKLAK)2, as an antibacterial and anti-tumor polypeptide, is a representative of the antimicrobial peptide group, and also has good anticancer properties. d-(KLAKLAK)2 is able to kill bacteria by damaging their cellmembranes, causing cell contents to leak out. d-(KLAKLAK)2 can also inhibit tumorcell proliferation by causing mitochondrial swelling and mitochondrial membrane destruction, triggering apoptosis (programmed cell death) .
HN-1 is a 12-mer peptide with specific activity to head and neck squamous cell cancer (HNSCC) cells. HN-1, as a tumor-specific peptide, is capable of penetrating tumor tissues. HN-1 is capable of translocating agents across cellmembranes .
Tachyplesin I TFA is a β-hairpin antimicrobial peptide that contains 17 amino acid residues. Tachyplesin I TFA exhibits cytotoxic properties against various human tumorcell lines acting primarily by impairing the integrity of the outer cellmembrane .
CyPep-1 is a novel cationic lytic peptide with antitumor activity. CyPep-1 is highly cytotoxic by interacting with the negatively charged cellmembrane of cancer cells. CyPep-1 has strong cytolytic activity on cancer cells both in vivo and in vitro, and can be used in the study of solid tumors .
Cys-Asp-Pro-Gly-Tyr-Ile-Gly-Ser-Arg-NH2 is a linear peptide from laminin B1 chain that interferes with tumorcell attachment and invasion into basement membrane and has anti-angiogenic effects .
HYNIC-PSMA is a ligand for molecular imaging of tumors. Hynic-psma consists of two components: HYNIC (6-hydrazinonicotinamide) and PSMA (Prostate-Specific Membrane Antigen). HYNIC is a compound used to attach radioactive isotopes to targeted molecules, such as 188Re-HYNIC-PSMA. PSMA is a membrane antigen that is specifically expressed on the surface of prostate cancer cells. HYNIC-PSMA can be used in prostate cancer research . HYNIC-PSMA can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
pH-Low Insertion Peptide (pHLIP) is a short, pH-responsive peptide capable of inserting across a cellmembrane to form a transmembrane helix at acidic pH. pH-Low Insertion Peptide targets the acidic tumor microenvironment for tumors at early and metastatic stages with high specificity, used as a specific ligand. pH-Low Insertion Peptide successfully modify polylysine polymers to have the pH-responsive capability. pH-Low Insertion Peptide-based targeting of cancer presents an opportunity to monitor metabolic changes, and to selectively deliver imaging and therapeutic agents to tumors .
pH-Low Insertion Peptide TFA (pHLIP TFA) is a short, pH-responsive peptide capable of inserting across a cellmembrane to form a transmembrane helix at acidic pH. pH-Low Insertion Peptide TFA targets the acidic tumor microenvironment for tumors at early and metastatic stages with high specificity, used as a specific ligand. pH-Low Insertion Peptide TFA successfully modifys polylysine polymers to have the pH-responsive capability. pH-Low Insertion Peptide TFA -based targeting of cancer presents an opportunity to monitor metabolic changes and to selectively deliver imaging and therapeutic agents to tumors .
BQ7876 is a probe targeting prostate-specific membrane antigen (PSMA) that contains a DOTA chelator. BQ7876, after being radiolabeled with radionuclide (177Lu), functions in both radionuclide imaging and tumorcell destruction by specifically binding to PSMA. BQ7876 shows potential for research in the field of metastatic castration-resistant prostate cancer (mCRPC) . BQ7876 can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
IT9302 is a synthetic IL-10 agonist with the activity of inducing tolerogenic dendritic cells. IT9302 is able to mimic multiple effects of IL-10, including downregulating the antigen presentation machinery and increasing the sensitivity of tumorcells to natural killer cell-mediated lysis. IT9302 can also hinder the response of human monocytes to differentiation factors and reduce the antigen presentation and co-stimulatory capacity of dendritic cells. Dendritic cells treated with IT9302 showed a weakened ability to stimulate T cell proliferation and interferon-γ production. IT9302 exerts its effects through mechanisms that are partially different from IL-10, involving STAT3 inactivation and regulation of the NF-κB intracellular pathway. IT9302-treated dendritic cells showed enhanced expression of membrane-bound TGF-β, associated with the effective induction of foxp3+ regulatory T cells .
MCE Basement Membrane Matrix IPSC-qualified is primarily composed of natural basement membrane matrix extracted from mouse tumors. This product is mainly used for stem cells culture.
MCE Basement Membrane Matrix GFR&HC (Growth Factor Reduced, High Concentration) is primarily composed of natural basement membrane matrix extracted from mouse tumors, is suitable for cell cultures that need to reduce growth factor induction and studies related to growth factors, signaling pathways, etc.
Cevostamab (BFCR4350A; RG6160; RO7187797) is a humanized IgG1-based BsAb that targets membrane-proximal extracellular domain of FcRH5 on multiple myeloma (MM) cells as well as CD3 on T cells. Moreover, Cevostamab facilitates efficient synapse formation, improves killing activity of T cells against MM tumorcells .
IMAB027 (ASP1650) is a specific anti-CLDN6 mAb, while CLDN6 (Claudin 6) is a tight junction membrane protein, aberrantly expressed in various human cancer types, ovarian cancers particularly. IMAB 027 shows anti-tumor activity, and induces apoptosis in CLDN6 + ovarian and testicular cancer cell lines .
Phosphorylethanolamine (Standard) is the analytical standard of Phosphorylethanolamine. This product is intended for research and analytical applications. Phosphorylethanolamine (Monoaminoethyl phosphate) is present in most animal tissues and is also present in various human extracranial tumors. Phosphorylethanolamine is considered as the intermediate product of phospholipid metabolism. Phosphorylethanolamine is essential for the formation and maintenance of the cellmembrane .
Lewis X trisaccharide (Lewis X, Le x) is a potent TH2 regulator, antagonizes LPS-induced IL-12 immune expression. Lewis X trisaccharide is a human histo-blood group antigen, plays an key role in cell-cell adhesion, and servers as a tumor marker. Lewis X trisaccharide is highly expressed in the outer membrane of the parasite, can be used for the immunology research of schistosomiasis .
Phosphorylethanolamine (Monoaminoethyl phosphate) is a membrane phospholipid and an important precursor of Phosphatidylcholine (HY-B2233B). It is found in most animal tissues and various human extracranial tumors, playing a critical role in membrane integrity, cell division, mitochondrial respiratory function, and more. Studies have shown that changes in the abundance of Phosphorylethanolamine are associated with Alzheimer's disease and Parkinson's disease. Lowering the ratio of Phosphorylethanolamine to Phosphatidylcholine in the liver can improve insulin signaling. Phosphorylethanolamine holds promise for research in the fields of cancer, neurodegenerative disorders, and metabolic diseases .
Squalamine (MSI-1256) is an aminosterol compound with broad-spectrum antiviral activity. Squalamine makes cells less conducive to certain viral replication by altering the electrostatic interactions in the inner membrane of host cells. Squalamine also has antibacterial and antitumor activities. Squalamine has broad-spectrum antibacterial activity against Gram-negative and Gram-positive bacteria, fungi and protozoa. Squalamine inhibits tumor-related angiogenesis and the growth of human breast cancer cells. Squalamine restores the function of enteric nervous system in Parkinson ,s disease mouse models .
N-Acetyl-L-tyrosine is an orally active endogenous mitochondrial stress response regulator that can permeate the cellmembrane by passive diffusion. N-Acetyl-L-tyrosine induces low-level reactive oxygen species (ROS) generation by transiently perturbing mitochondrial membrane potential, triggering reverse signaling to activate FoxO and Keap1 pathways. As a result, N-Acetyl-L-tyrosine enhances the expression of antioxidant enzyme genes, exerting anti-stress and cytoprotective effects. N-Acetyl-L-tyrosine can improve heat stress tolerance, inhibit tumor growth, and regulate energy metabolism. N-Acetyl-L-tyrosine can be used in the research of aging, metabolic diseases (such as diabetes), and cancer .
N-Acetyl-L-tyrosine (Standard) is the analytical standard of N-Acetyl-L-tyrosine (HY-W012382). This product is intended for research and analytical applications. N-Acetyl-L-tyrosine is an orally active endogenous mitochondrial stress response regulator that can permeate the cellmembrane by passive diffusion. N-Acetyl-L-tyrosine induces low-level reactive oxygen species (ROS) generation by transiently perturbing mitochondrial membrane potential, triggering reverse signaling to activate FoxO and Keap1 pathways. As a result, N-Acetyl-L-tyrosine enhances the expression of antioxidant enzyme genes, exerting anti-stress and cytoprotective effects. N-Acetyl-L-tyrosine can improve heat stress tolerance, inhibit tumor growth, and regulate energy metabolism. N-Acetyl-L-tyrosine can be used in the research of aging, metabolic diseases (such as diabetes), and cancer .
Tumor associated calcium signal transducer 2 (TACSTD2) is a carcinoma-associated antigen which is a cell surface receptor that transduces calcium signals and may also function as a growth factor receptor. TACSTD2 is involved in negative regulation of branching involved in ureteric bud morphogenesis; negative regulation of cellular component organization; negative regulation of substrate adhesion-dependent cell spreading; positive regulation of stem cell differentiation; and regulation of epithelial cell proliferation. TROP-2 Protein, Rhesus macaque (HEK293, His) is the recombinant Rhesus Macaque-derived TROP-2 protein, expressed by HEK293 , with C-6*His labeled tag.
The TROP-2 protein emerged as a potential growth factor receptor, implying involvement in cellular processes related to growth and signaling. As a putative receptor, TROP-2 may play a crucial role in transducing signals that regulate cell growth and proliferation. TROP-2 Protein, Human (HEK293, His-Avi) is the recombinant human-derived TROP-2 protein, expressed by HEK293 , with C-Avi, C-6*His labeled tag.
The TROP-2 protein emerged as a potential growth factor receptor, implying involvement in cellular processes related to growth and signaling. As a putative receptor, TROP-2 may play a crucial role in transducing signals that regulate cell growth and proliferation. TROP-2 Protein, Human (248a.a, HEK293, His) is the recombinant human-derived TROP-2 protein, expressed by HEK293 , with C-6*His labeled tag.
The TROP-2 protein emerged as a potential growth factor receptor, implying involvement in cellular processes related to growth and signaling. As a putative receptor, TROP-2 may play a crucial role in transducing signals that regulate cell growth and proliferation. TROP-2 Protein, Human (187a.a, HEK293, His) is the recombinant human-derived TROP-2 protein, expressed by HEK293 , with C-6*His labeled tag.
The TROP-2 protein emerged as a potential growth factor receptor, implying involvement in cellular processes related to growth and signaling. As a putative receptor, TROP-2 may play a crucial role in transducing signals that regulate cell growth and proliferation. TROP-2 Protein, Human (187a.a, HEK293, Fc) is the recombinant human-derived TROP-2 protein, expressed by HEK293 , with C-hFc labeled tag.
The TROP-2 protein emerged as a potential growth factor receptor, implying involvement in cellular processes related to growth and signaling. As a putative receptor, TROP-2 may play a crucial role in transducing signals that regulate cell growth and proliferation. TROP-2 Protein, Human (248a.a, HEK293, hFc) is the recombinant human-derived TROP-2 protein, expressed by HEK293 , with C-hFc labeled tag.
The EpCAM/TROP1 protein serves as an important homogeneous interacting molecule that promotes direct contact between intestinal epithelial cells (IEC) and intraepithelial lymphocytes (IEL) in the mucosal epithelium. This feature helps establish an immune barrier against mucosal infections. EpCAM/TROP1 Protein, Human (His-SUMO) is the recombinant human-derived EpCAM/TROP1 protein, expressed by E. coli , with N-6*His, N-SUMO labeled tag.
N-Acetyl-L-tyrosine-d3 is the deuterated form of N-Acetyl-L-tyrosine (HY-W012382). N-Acetyl-L-tyrosine is an orally active endogenous mitochondrial stress response regulator that can permeate the cellmembrane by passive diffusion. N-Acetyl-L-tyrosine induces low-level reactive oxygen species (ROS) generation by transiently perturbing mitochondrial membrane potential, triggering reverse signaling to activate FoxO and Keap1 pathways. As a result, N-Acetyl-L-tyrosine enhances the expression of antioxidant enzyme genes, exerting anti-stress and cytoprotective effects. N-Acetyl-L-tyrosine can improve heat stress tolerance, inhibit tumor growth, and regulate energy metabolism. N-Acetyl-L-tyrosine can be used in the research of aging, metabolic diseases (such as diabetes), and cancer .
MTIC-d3 is deuterium labeled MTIC. MTIC is the active metabolite of Temozolomide (TMZ). MITC has lower bioavailability in the brain compared with TMZ, because the agent’s permeability through biological barriers and tumorcellmembranes affects bioavailability. MITC exhibits low affinity to biological membrane[1].
ALK/EGFR-IN-1-d5 (Compound (-)-9a) is a deuterated dual-target inhibitor of EGFR and ALK, with an IC50 of 1.08 nM for EGFR and an IC50 of 2.395 nM for ALK. ALK/EGFR-IN-1-d5 inhibits the phosphorylated proteins in the EGFR, ALK, and BRK signaling pathways, blocking the cell cycle, leading to a reduction in mitochondrial membrane potential and cell apoptosis (Apoptosis). ALK/EGFR-IN-1-d5 also significantly inhibits tumor growth in animal models and demonstrates good safety. ALK/EGFR-IN-1-d5 holds promise for research in the field of cancer treatment
TROP2 Antibody (YA2130) is a rabbit-derived non-conjugated IgG antibody (Clone NO.: YA2130), targeting TROP2, with a predicted molecular weight of 36 kDa (observed band size: 45-65 kDa). TROP2 Antibody (YA2130) can be used for WB, IHC-F, IHC-P, ICC/IF experiment in human background.
TROP2 Antibody (YA1496) is a mouse-derived non-conjugated IgG antibody (Clone NO.: YA1496), targeting TROP2. TROP2 Antibody (YA1496) can be used for WB,IHC-P,FC,ELISA experiment in human background.
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