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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
621 Results for "
triple
" in MedChemExpress (MCE) Product Catalog:
Products (621)
621 Results for "triple" in MCE Product Catalog:
88
88 Publications Verification
GW6471 is a selective peroxisome proliferator-activated receptor α (PPARα) antagonist. GW6471 reduces cancer stem cell viability, proliferation, and spheroid formation. GW6471 induces apoptosis and causes metabolic impairment including energy imbalance. GW6471 can be used for the research of paragangliomas and triple-negative breast cancer .
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Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
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78 Cited Publications
Synonyms: BIBF 1120 esylate
Nintedanib esylate (BIBF 1120 esylate) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
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25 Cited Publications
Synonyms: GSK 525762C; I-BET 762 besylate
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Molibresib besylate (GSK 525762C; I-BET 762 besylate) is an orally active pan-BET inhibitor that targets and binds to BRD2, BRD3, BRD4 and BRDT. By competitively occupying acetylated lysine binding sites, Molibresib besylate disrupts the interaction between BET proteins and chromatin, thereby effectively inhibiting MYC expression and target gene transcription. Molibresib besylate exhibits broad antiproliferative activity, which not only inhibits cancer cell growth and induces growth arrest, but also downregulates mitosis-related genes and upregulates the level of p-ERK1/2. When combined with MEK inhibitors, Molibresib besylate shows a significant synergistic effect, reduces tumor burden in mouse models of leukemia, modulates the immune microenvironment and prolongs survival. Molibresib besylate is widely applicable to research related to acute myeloid leukemia, multiple myeloma, triple-negative breast cancer, small-cell lung cancer and various advanced refractory solid tumors .
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21 Cited Publications
SR-4835 is a potent, highly selective and ATP competitive dual inhibitor of CDK12/CDK13 (CDK12: IC50=99 nM, Kd=98 nM; CDK13: Kd=4.9 nM). SR-4835 acts in synergy with DNA-damaging chemotherapy and PARP inhibitors and provokes triple-negative breast cancer (TNBC) cell death .
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20 Cited Publications
RMC-7977 is an orally active triple-complex RAS inhibitor that can simultaneously bind to cyclophilin A (CYPA) (Kd = 195 nM) and KRAS (G12V) (Kd = 292 μM). It exhibits broad-spectrum inhibitory activity against KRAS, NRAS, and HRAS proteins and their various wild-type and mutant variants. RMC-7977 induces apoptosis by inhibiting the phosphorylation of ERK, CRAF, and RSK, as well as increasing PARP cleavage. This leads to tumor regression, reduces resistance in KRAS G12C cancer models, and demonstrates good tolerability across various RAS cancer models .
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Rebastinib (DCC-2036) is an orally active, non-ATP-competitive Bcr-Abl inhibitor, with IC50 values of 0.8 nM and 4 nM against Abl1 WT and Abl1 T315I, respectively. Rebastinib potently inhibits CYP2C8 (IC50 = 0.0533 μM) and CYP2C9 (IC50 = 2.54 μM). Rebastinib allosterically inhibits Tie2 with an IC50 of 0.63 nM. Rebastinib inhibits the transcriptional activity of FoxO1. Rebastinib inhibits SRC family kinases, KDR and FLT3 kinases. Rebastinib induces Apoptosis. Rebastinib exerts anti-tumor activity in breast cancer. Rebastinib exerts anti-angiogenic effects. Rebastinib increases myotube diameter and improves reduced contractility. Rebastinib can be used in research related to triple-negative breast cancer, luminal breast cancer, pancreatic neuroendocrine tumors, muscle atrophy, cancer cachexia, chronic myeloid leukemia, and B-lymphocytic leukemia .
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11 Cited Publications
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AGX51 is a pan-Id (inhibitors of DNA-binding/differentiation proteins) antagonist that disrupts ID-E protein interactions, thereby triggering ubiquitin-mediated proteasomal degradation of ID1, ID2, ID3 and ID4. AGX51 induces ROS production, G0/G1 cell cycle arrest, non-apoptotic cell death, and regulates EMT-related proteins. AGX51 reduces the proliferation, migration and myofibroblast differentiation of lung fibroblasts, alleviates pulmonary fibrosis, inhibits cancer cell viability and tumor growth, impairs neovascularization, and shows no obvious toxicity in mice. AGX51 can be used in research related to idiopathic pulmonary fibrosis, triple-negative breast cancer, breast cancer, pancreatic ductal adenocarcinoma, colorectal tumors, wet age-related macular degeneration and retinopathy of prematurity .
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Sacituzumab is a humanized IgG1 monoclonal antibody targeting Trophoblast cell surface antigen 2 (TROP2). Sacituzumab demonstrates a lack of antitumor effects alone and does not inhibit the function of TROP-2 during tumor metastasis, binding to the linear epitopes of TROP-2 protein. Sacituzumab can be used for the synthesis of antibody-drug conjugates (ADC) drug Sacituzumab govitecan (HY-132254). Sacituzumab govitecan can be used in the field of triple-negative breast cancer .
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9 Cited Publications
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Col003 is a selective and potent inhibitor of Hsp47 and competitively binds to the collagen binding site on Hsp47 (IC50=1.8 μM). Col003 discourages the interaction of Hsp47 with collagen and inhibits collagen secretion by destabilizing the collagen triple helix. Col003 can be used for the investigation of fibrosis
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7 Cited Publications
LYN-1604 dihydrochloride is a potent UNC-51-like kinase 1 (ULK1) activator (EC50=18.94 nM) for the research of triple negative breast cancer (TNBC) .
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Vanzacaftor (VX-121) is an orally active noval corrector of Cystic fibrosis transmembrane conductance regulator (CFTR). Vanzacaftor improves processing and trafficking of CFTR protein as well as increases chloride transport in triple combined with Tezacaftor (HY-15448) and Deutivacaftor. Vanzacaftor-Tezacaftor-Deutivacaftor is safe and well tolerated, improving lung function, respiratory symptoms, and CFTR function with cystic fibrosis, which is promising for research in the field of cystic fibrosis diseases .
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6 Cited Publications
Synonyms: BSI-201; NSC-746045; IND-71677
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Iniparib (BSI-201) is an irreversible inhibitor of PARP1, used in the research of triple negative breast cancer.
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PD146176 (NSC168807), a 15-Lipoxygenase (15-LO) inhibitor, inhibits rabbit reticulocyte 15-LO (Ki=197 nM, IC50=0.54 μM). PD146176 reverses cognitive impairment, brain amyloidosis, and tau pathology by stimulating autophagy in aged triple transgenic mice .
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Category:
Alkaloids Monophenols Phenols Nymphaeaceae Extract Nelumbo nucifera Gaertn. Plants Disease Research Fields Isoquinoline Alkaloids Inflammation/Immunology
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5 Cited Publications
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BMS-986158 is a potent BET inhibitor with IC50s of 6.6 and 5 nM in NCI-H211 small cell lung cancer (SCLC) cells and MDA-MB231 triple negative breast cancer (TNBC) cells, respectively .
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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
