149092-50-2
Chemical Structure
AG-825
Synonym(s): Tyrphostin AG-825
- CAS No.: 149092-50-2
- Formula:C19H15N3O3S2
- Molecular Weight:397.47
IUPAC Name: (E)-3-(3-((benzo[d]thiazol-2-ylthio)methyl)-4-hydroxy-5-methoxyphenyl)-2-cyanoacrylamide
InChIKey: KXDONFLNGBQLTN-WUXMJOGZSA-N
SMILES: O=C(N)/C(C#N)=C/C1=CC(OC)=C(O)C(CSC2=NC3=CC=CC=C3S2)=C1
Biological Activity: AG-825 is a selective, ATP-competitive, tyrosine phosphorylation ErbB2 inhibitor with an IC50 of 0.35 μM. AG825 significantly accelerates Apoptosis of human neutrophils. AG-825 increases β1AR density. AAG-825 has anticancer and anti-inflammatory activities. AAG-825 can be used in cardiovascular disease research[1][2][3][4][5][6][7].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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AG-825 | 98.13% | AG-825 is a selective, ATP-competitive, tyrosine phosphorylation ErbB2 inhibitor with an IC50 of 0.35 μM. AG825 significantly accelerates Apoptosis of human neutrophils. AG-825 increases β1AR density. AAG-825 has anticancer and anti-inflammatory activities. AAG-825 can be used in cardiovascular disease research. | ||||||||||||||||||||
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ST638 | ST638 is a potent tyrosine kinase inhibitor (IC50=370 nM). ST638 also targets the CSF-1 receptor and inhibits PGE2 production. | |||||||||||||||||||||
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TLSC702 | 95.61% | TLSC702 is a human glyoxalase I (hGLO I) inhibitor with an IC50 of 2.0 μM. TLSC702 inhibits the activity of human glyoxalase I, thereby leading to the accumulation of methylglyoxal and its derived advanced glycation end products. TLSC702 inhibits tumor cell proliferation, induces apoptotic morphological changes, internucleosomal DNA fragmentation and PARP cleavage in tumor cells. TLSC702 can be used in research related to leukemia and lung cancer. | ||||||||||||||||||||
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Chst15-IN-1 | 98.01% | Chst15-IN-1 is a potent reversible covalent Chst15 inhibitor. Chst15-IN-1 effectively inhibits chondroitin sulfate-E (CS-E) sulfation levels and other closely related glycosaminoglycans (GAG) sulfotransferases. Chst15-IN-1, as a selective sulfotransferase inhibitor, can diminish the inhibitory effects of chondroitin sulfate proteoglycans (CSPGs), and can be used for the stimulation of neuronal repair. | ||||||||||||||||||||
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I-OMe-Tyrphostin AG 538 | 98.03% | I-OMe-Tyrphostin AG 538 (I-OMe-AG 538) is a specific inhibitor of IGF-1R (insulin-like growth factor-1 receptor tyrosine kinase). I-OMe-Tyrphostin AG 538 inhibits IGF-1R-mediated signaling and is preferentially cytotoxic to nutrient-deprived PANC1 cells.?I-OMe-Tyrphostin AG 538 is an ATP-competitive inhibitor of phosphatidylinositol-5-phosphate 4-kinase α (PI5P4Kα), with an IC50?of 1 μM. | ||||||||||||||||||||
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Anti-hyperglycemic agent-1 | Anti-hyperglycemic agent-1 (compound 10) is a potent α-Glucosidase inhibitor, with an IC50 of 0.53 μM. Anti-hyperglycemic agent-1 can be used for diabetes research. | |||||||||||||||||||||
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PTP1B-IN-22 | 98.12% | PTP1B-IN-22, a ZINC02765569 derivative, is a potent protein tyrosine phosphatase 1B (PTP1B) inhibitor. PTP1B-IN-22 has PTP1B inhibition and glucose uptake in skeletal muscle L6 myotubes. | ||||||||||||||||||||
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HDAC6-IN-43 | HDAC6-IN-43 (compound 26) is a potent HDAC inhibitor. HDAC6-IN-43 effectively inhibits several HDACs, notably HDAC1, HDAC2, and HDAC6 (IC50 < 150 nM), displaying a particularly high sensitivity towards HDAC6 (IC50 = 11 nM). HDAC6-IN-43 can be used for the research of autosomal dominant polycystic kidney disease (ADPKD). | |||||||||||||||||||||
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MU1409 | 98.52% | MU1409 is an inhibitor of MRE11 nuclease with an IC50 of 12.1 μM. Additionally, MU1409 also inhibits FEN1 and EXO1, with IC50 values of 24.2 and 176.4 μM, respectively. MU1409 affects DNA repair in cells, preventing the degradation of stalled replication forks in BRCA2-deficient cells, making it a promising candidate for research on BRCA2 mutation-induced cancers. | ||||||||||||||||||||
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YL-109 | 98.91% | YL-109 is an antitumor agent that can induce carboxyl terminus of Hsp70-interacting protein (CHIP) expression through aryl hydrocarbon receptor (AhR) signaling. YL-109 has ability to inhibit breast cancer cell growth and invasiveness. | ||||||||||||||||||||
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HMBI | HMBI is a fluorescent probe that enables dual-color visualization of both the nucleus and mitochondria and monitors apoptosis. HMBI emits green fluorescence in the nucleus with Ex/Em=405/510-560 nm, and red fluorescence in mitochondria with Ex/Em=543/560-660 nm. The localization and emission properties of HMBI depend on subcellular pH and mitochondrial membrane potential. HMBI can serve as a feed additive for in vitro rumen fermentation; it is partially degraded, absorbed or converted into HMB by microorganisms in the system, so as to support microbial protein synthesis, alter the concentration of rumen metabolites and adjust the composition of bacterial communities. | |||||||||||||||||||||
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References
- [1]. Wolfson E, et al. Nucleolin and ErbB2 inhibition reduces tumorigenicity of ErbB2-positive breast cancer. Cell Death Dis. 2018 Jan 19;9(2):47. [Content Brief]
- [2]. Gazit A, et al. Tyrphostins. 3. Structure-activity relationship studies of alpha-substituted benzylidenemalononitrile 5-S-aryltyrphostins. J Med Chem. 1993 Nov 12;36(23):3556-64. [Content Brief]
- [3]. He H, et al. Signal therapy for RAS-induced cancers in combination of AG 879 and PP1, specific inhibitors for ErbB2 and Src family kinases, that block PAK activation. Cancer J. 2001 May-Jun;7(3):191-202. [Content Brief]
- [4]. Rahman A, et al. Inhibition of ErbB kinase signalling promotes resolution of neutrophilic inflammation. Elife. 2019 Oct 15;8. pii: e50990. [Content Brief]
- [5]. Ling J, et al. Identifying key genes, pathways and screening therapeutic agents for manganese-induced Alzheimer disease using bioinformatics analysis. Medicine (Baltimore). 2018 Jun;97(22):e10775. [Content Brief]
- [6]. Piven YA, et al. Novel O-acylated (E)-3-aryl-6,7-dihydrobenzisoxazol-4(5H)-one oximes targeting HSP90-HER2 axis in breast cancer cells. Bioorg Med Chem. 2022 Jan 1;53:116521. [Content Brief]
- [7]. Gupta MK, et al. Anthracycline Cardiotoxicity Is Associated With Elevated β1-Adrenergic Receptor Density. J Am Heart Assoc. 2022 Feb 15;11(4):e023457. [Content Brief]