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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
18 Results for "
TGFβR inhibitor
" in MedChemExpress (MCE) Product Catalog:
Products (18)
18 Results for "TGFβR inhibitor" in MCE Product Catalog:
24
24 Publications Verification
Synonyms: HTS466284
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LY-364947 (HTS466284) is a potent ATP-competitive inhibitor of TGFβR-I with IC50 of 59 nM, and exhibits 7-fold selectivity over TGFβR-II .
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1 Cited Publications
Cat. No.: HY-18766
CAS No.: 1352609-28-9
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EW-7195 is a potent and selective ALK5 (TGFβR1) inhibitor with an IC50 of 4.83 nM. EW-7195 has >300-fold selectivity for ALK5 over p38α. EW-7195 efficiently inhibits TGF-β1-induced Smad signaling, epithelial-to-mesenchymal transition (EMT) and breast tumour metastasis to the lung .
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1 Cited Publications
Cat. No.: HY-N7694
CAS No.: 97871-44-8
Category:
Triterpenes Terpenoids Melia toosendan Sieb. et Zucc. Plants Disease Research Fields Inflammation/Immunology Meliaceae
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1 Cited Publications
Cat. No.: HY-163121
CAS No.: 1096144-06-7
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PST3.1a is an orally active and brain-penetrant N-acetylglucosamine glycosyltransferase (MGAT5) inhibitor with a human IC50 of 2 µM. PST3.1a inhibits TGFβR and FAK signaling pathway activity. PST3.1a alters β1,6-GlcNAc N-glycans and microtubule/microfilament integrity, increases OLIG2 expression, and inhibits proliferation, migration, invasiveness, and clonogenic capacities of glioblastoma initiating cells. PST3.1a reduces invasive and proliferative capacity of glioblastoma initiating cells in orthotopic graft models, increases overall survival of orthotopic graft model mice. PST3.1a blunts MGAT5 overexpression, decreases renal fibrosis via collagen 1, collagen 4, and galectin 3 downregulation in a rat chronic kidney disease model. PST3.1a can be used for the research of glioblastoma multiforme and chronic kidney disease .
Cat. No.: HY-168990
CAS No.: 2647949-48-0
Synonyms: AGMB-129
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Ontunisertib (AGMB-129) is an orally active and selective gastrointestinal-restricted ALK5 (TGFβR1) inhibitor. Ontunisertib blocks signalling of the pro-fibrotic TGFβ pathway. Ontunisertib can be used for the research of fibrostenotic Crohn’s disease .
Cat. No.: HY-W107024
CAS No.: 2001559-19-7
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BMS-986260, an immuno-oncology agent, is a potent, selective, and orally active TGFβR1 inhibitor (IC50=1.6 nM). BMS-986260 displays exquisite selectivity for TGFβR1 over its isozyme TGFβR2, as well as in a panel of more than 200 kinases examined. BMS-986260 inhibits TGFβ mediated nuclear translocation of pSMAD2/3 in MINK and NHLF cells lines with an IC50 of 350 nM and 190 nM, respectively .
Cat. No.: HY-117887
CAS No.: 2141955-96-4
Synonyms: BLU-782; IPN-60130; ALK2-IN-1
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Fidrisertib (BLU-782) is the orally active inhibitor for activin receptor-like kinase 2 (ALK2) that inhibits ALK2 R206H, ALK2, ALK1, ALK6, ALK3, ALK4, TGFβR2 and ALK5 with IC50s of 0.2, 0.6, 3, 24, 45, 65, 67 and 155 nM, respectively .
Cat. No.: HY-160215
CAS No.: 2169299-67-4
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GFH018 is an orally active, selective and ATP-competitive TGF-βR1 inhibitor with an IC50 of 40 nM. GFH018 reactivates the immune system by blocking the immunosuppression mediated by regulatory T cells and M2 macrophages. GFH018 inhibits tumor angiogenesis. GFH018 suppresses tumor growth in mouse tumor models. GFH018 can be used for the research of solid tumors, hepatocellular carcinoma, colorectal cancer, breast cancer, and relapsed/metastatic nasopharyngeal carcinoma .
Cat. No.: HY-P990009
CAS No.: 2649854-92-0
Synonyms: NIS-793
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CJJ300 is a transforming growth factor-β (TGF-β) inhibitor with an IC50 of 5.3 µM. CJJ300 inhibits TGF-β signaling by disrupting the formation of the TGF-β-TβR-I-TβR-II signaling complex .
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TGFβRI-IN-3 inhibits TGFβR1 at an IC50 of 0.79 nM with 2000-fold selectivity against MAP4K4. TGFβRI-IN-3 represents a highly selective TGFβR1 inhibitor that has potential applications in immuno-oncology .
Cat. No.: HY-P10414A
Synonyms: KP1 (human) hydrochloride
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Cat. No.: HY-P10414
Synonyms: KP1 (human)
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Cat. No.: HY-160215A
CAS No.: 2345717-52-2
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GFH018 is an orally active, selective and ATP-competitive TGF-βR1 inhibitor with an IC50 of 40 nM. GFH018 reactivates the immune system by blocking the immunosuppression mediated by regulatory T cells and M2 macrophages. GFH018 inhibits tumor angiogenesis. GFH018 suppresses tumor growth in mouse tumor models. GFH018 can be used for the research of solid tumors, hepatocellular carcinoma, colorectal cancer, breast cancer, and relapsed/metastatic nasopharyngeal carcinoma .
Cat. No.: HY-139858
CAS No.: 2857845-36-2
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TGFβR-IN-1 is a long-acting tumor-activated proagent of a TGFβR inhibitor.
Cat. No.: HY-151279
CAS No.: 2785430-86-4
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ALK5-IN-30 (EX-07) is a potent ALK inhibitor, inhibits ALK5 and TGFβ-R1 with both IC50s <10 nM .
Cat. No.: HY-187187
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TGF-βR1/VEGFR2-IN-1 is a dual inhibitor targeting TGF-βR1/VEGFR2, with an IC50 of 232.5 nM against human TGF-βR1 and an IC50 of 371.4 nM against human VEGFR2. TGF-βR1/VEGFR2-IN-1 mediates antiproliferative effects by inhibiting the TGF-βR1 and VEGFR2 signaling pathways. TGF-βR1/VEGFR2-IN-1 can be used in research related to colorectal cancer, non-small cell lung cancer, cervical cancer, and hepatocellular carcinoma .
Cat. No.: HY-149196
CAS No.: 2857845-34-0
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TGFβ-IN-3 (Compound 8) is a long-acting tumor-activating prodrug of TGFβR1 inhibitor. TGFβ-IN-3 can achieve selective drug release in tumors, and the tumor/blood ratio is increased by 2.2 times. TGFβ-IN-3 can be used for the study of colon cancer .
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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
