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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
20 Results for "
Ctgf Inhibitors
" in MedChemExpress (MCE) Product Catalog:
Products (20)
20 Results for "Ctgf Inhibitors" in MCE Product Catalog:
1
1 Cited Publications
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(rel)-AR234960 is a selective and competitive agonist of the G protein-coupled receptor MAS. (rel)-AR234960 binds to the MAS receptor to activate the downstream ERK1/2 signaling pathway, inducing the expression of connective tissue growth factor (CTGF) and its downstream collagen subtype genes (such as COL1A1, COL3A1). (rel)-AR234960 promotes collagen synthesis in cardiac fibroblasts through the MAS-ERK1/2-CTGF pathway and aggravates extracellular matrix remodeling. (rel)-AR234960's in vitro effect can be blocked by the MAS inverse agonist AR244555 and MEK1 inhibitor. (rel)-AR234960 regulates the expression of cardiac fibrosis-related genes and can be used in the study of heart failure .
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PRX-08066 is a selective and orally active 5-hydroxytryptamine receptor 2B (5-HT2BR) antagonist with a Ki of 3.4 nM. PRX-08066 inhibits the MAPK pathway, 5-HT release and fibrotic factor (TGFβ1, CTGF and FGF2) expression. PRX-08066 inhibits the proliferation of KRJ-I cells and induces apoptosis (caspase-3 activation). PRX-08066 inhibits pulmonary vascular remodeling. PRX-08066 can be used of pulmonary Arterial Hypertension (PAH) and neuroendocrine tumor (NET) .
Cat. No.: HY-N0136B
CAS No.: 111003-33-9
Synonyms: (-)-Dihydroquercetin
Cat. No.: HY-179505
CAS No.: 2866423-35-8
OPN-9652 is a potent, orally active, and covalent TEAD inhibitor (MSTO-211H TEAD IC50 = 0.005 µM) targeting the central palmitate binding pocket of TEADs. OPN-9652 reduces TEAD-dependent reporter activity and expression of TEAD targets (CTGF and CYR61). OPN-9652 resensitizes drug-tolerant SOX10 KO cells to BRAFi + MAPKi. OPN-9652 delays the onset of tumor resistance to BRAFi + MEKi from minimal residual disease (MRD) in a BRAF mutant A375 xenograft mouse model. OPN-9652 can be used for melanoma research .
Cat. No.: HY-120409
CAS No.: 1463912-49-3
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AB1 is a highly selective S1P2 receptor antagonist (IC50=3.5 nM). AB1 inhibits sphingosine-1-phosphate (S1P) signaling, suppressing tumor cell migration, angiogenesis, and profibrotic mediator CTGF expression while inducing apoptosis. AB1 is promising for research of solid tumors .
Cat. No.: HY-168704
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YAP/TAZ-TEAD-IN-2 (Compound 51) is a YAP/TAZ-TEAD inhibitor that inhibits the interaction between YAP/TAZ and TEAD. YAP/TAZ-TEAD-IN-2 suppresses the transcriptional activity of TEAD, with an IC50 of 1.2 nM. YAP/TAZ-TEAD-IN-2 inhibits YAP/TAZ-TEAD target genes expression (Cyr61, CTGF, AXL and Survivin) and breast cancer cell proliferation .
Cat. No.: HY-179440
EA-C15 is a potent and selective TEAD inhibitor with an IC50 of 0.34 μM. EA-C15 covalently binds to the TEAD palmitoylation site, blocks palmitoylation and transcriptional activity, and inhibits YAP-dependent cancer cell proliferation and YAP-TEAD target gene (CTGF and CYR61) transcription. EA-C15 can be used for cancer research .
Cat. No.: HY-159912
CAS No.: 3027484-09-6
pan-TEAD-IN-1 (Compound 3) is an orally active pan-TEAD inhibitor targeting the palmitoylation site of TEAD, disrupting its interaction with the coactivators YAP/TAZ, thereby suppressing the transcriptional upregulation of oncogenes (e.g., Ctgf and Cyr61) in the Hippo signaling pathway. pan-TEAD-IN-1 exhibits excellent activity with a luciferase IC50 of 0.36 nM and an H226 cell IC50 of 1.52 nM. It also shows favorable pharmacokinetics (AUC0–∞ = 228.7 μg/mL·min, T1/2 = 183.9 min). In TEAD-dependent xenograft mouse models, pan-TEAD-IN-1 significantly inhibited tumor growth, showing promise for research in TEAD-dependent cancers .
Cat. No.: HY-130011
CAS No.: 2349373-70-0
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CCG-232964 is an orally active inhibitor of Rho/MRTF/SRF. CCG-232964 inhibits LPA-induced CTGF gene expression .
Cat. No.: HY-168085
CV-4-26 (Compound 22) is a covalent inhibitor of TEAD. CV-4-26 inhibits YAP/TEAD-based transcription, leading to the reduction of CTGF and CYR61 expression. CV-4-26 inhibits Huh7 and HepG2 cell colony formation, induces cell cycle arrest, and apoptosis. CV-4-26 shows antitumor activity against hepatocellular carcinoma (HCC) and hepatoblastoma (HB) .
Cat. No.: HY-15472A
CAS No.: 866206-55-5
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PRX-08066 maleate is a selective and orally active 5-hydroxytryptamine receptor 2B (5-HT2BR) antagonist with a Ki of 3.4 nM. PRX-08066 maleate inhibits the MAPK pathway, 5-HT release and fibrotic factor (TGFβ1, CTGF and FGF2) expression. PRX-08066 maleate inhibits the proliferation of KRJ-I cells and induces apoptosis (caspase-3 activation). PRX-08066 maleate inhibits pulmonary vascular remodeling. PRX-08066 maleate can be used of pulmonary Arterial Hypertension (PAH) and neuroendocrine tumor (NET) .
Cat. No.: HY-179559
CAS No.: 2866423-06-3
OPN-9643 is a covalent inhibitor targeting the central palmitate binding pocket of TEADs with an IC50 of 15 nM, preventing autopalmitoylation and reducing TEAD-driven luciferase activity and canonical TEAD targets, CTGF and CYR61. OPN-9643 can be used for the research of cancer, such as melanoma .
Cat. No.: HY-P991950
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Cat. No.: HY-186148
CAS No.: 3081701-84-7
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YL-602 is an orally active Hippo pathway activator. YL-602 activates the Hippo pathway via MST1/2, with downstream pathway activation. YL-602 inhibits YAP and CTGF expression in cells irrespective of cell density and serum presence. YL-602 induces tumor cell apoptosis and inhibits colony formation. YL-602 suppresses tumor growth in mice. YL-602 can be used for the research of cancer, such as breast cancer .
Cat. No.: HY-181594
PROTAC TEAD/IAP degrader-1 is a TEAD/IAP PROTAC degrader. PROTAC TEAD/IAP degrader-1 is also a specific and Nongenetic inhibitor of apoptosis protein (IAP)-dependent protein eraser (SNIPERs). PROTAC TEAD/IAP degrader-1 recruits cIAP1 to form ternary complexes, induces ubiquitination, proteasomal TEAD1, TEAD4 degradation. PROTAC TEAD/IAP degrader-1 inhibits TEAD transcriptional activity, reduces CTGF expression, and reduces cell proliferation. PROTAC TEAD/IAP degrader-1 can be used for the research of mesothelioma .
Cat. No.: HY-181537
PROTAC TEAD1/IAP degrader-2 is an IAP-harnessing TEAD1 PROTAC degrader, with a DC50 of 170 nM against TEAD1 in NCI-H2052 cells. PROTAC TEAD1/IAP degrader-2 exhibits moderate antiproliferative activity in Hippo pathway-dependent mesothelioma cells. PROTAC TEAD1/IAP degrader-2 inhibits the expression of CTGF, but with a weaker effect than the TEAD inhibitor VT-107 (HY-134957). PROTAC TEAD1/IAP degrader-2 can be used in mesothelioma-related research .
Cat. No.: HY-181590
PROTAC TEAD1/IAP degrader-3 is a TEAD1/IAP PROTAC degrader. PROTAC TEAD1/IAP degrader-3 recruits the cIAP1 and XIAP E3 ligases to form a ternary complex, drives proteasomal degradation of TEAD1, and triggers autoubiquitination and proteasomal degradation of cIAP1. PROTAC TEAD1/IAP degrader-3 inhibits cell proliferation. PROTAC TEAD1/IAP degrader-3 regulates Hippo pathway activity by downregulating CTGF gene expression in a TEAD-dependent manner. PROTAC TEAD1/IAP degrader-3 is applicable to the research of mesothelioma .
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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
