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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
19 Results for "
aberrant activation
" in MedChemExpress (MCE) Product Catalog:
Products (19)
19 Results for "aberrant activation" in MCE Product Catalog:
7
7 Publications Verification
Synonyms: TNO155
Target:
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Batoprotafib (TNO155) is a potent selective and orally active allosteric inhibitor of wild-type SHP2 (IC50=0.011 µM). Batoprotafib has the potential for the study of RTK-dependent malignancies, especially advanced solid tumors .
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1 Cited Publications
Synonyms: ZIO 301; D 24851
Research Areas:
Indibulin (ZIO 301), an orally applicable inhibitor of tubulin assembly, shows potent anticancer activity with a minimal neurotoxicity. Indibulin reduces inter-kinetochoric tension, produces aberrant spindles, activates mitotic checkpoint proteins Mad2 and BubR1, and induces mitotic arrest and apoptosis .
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Alicapistat (ABT-957) is an orally active selective inhibitor of human calpains 1 and 2 for the potential application of Alzheimer's disease (AD) . Alicapistat mitigates the metabolic liability of carbonyl reduction and inhibits calpain 1 with an IC50 value of 395 nM .
Cat. No.: HY-113081R
CAS No.: 15763-06-1
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PKM2 activator 5 (compound 8) is a PKM2 activator with an AC50 value of 0.316 µM. PKM2 activator 5 has the potential to alter the aberrant metabolism of cancer cells .
Cat. No.: HY-19916
CAS No.: 1263384-43-5
Synonyms: BAL-101553
Research Areas:
Lisavanbulin (BAL-101553) is the prodrug of the microtubule targeting agent Avanbulin (BAL 27862) (HY-106008). Lisavanbulin is a BBB-penetrant and orally active antitumor agent, especially in tumors that express high levels of end-binding protein 1. Lisavanbulin has ability to target tumor cell proliferation and affects the tumor microenvironment by reducing tumor microvasculature. Lisavanbulin is also a spindle assembly checkpoint activator. Lisavanbulin induces cell cycle arrest and subsequent death or aberrant chromosome segregation. Lisavanbulin can be studied in research for diffuse large B cell lymphoma (DLBCL) and glioblastoma .
Cat. No.: HY-19916A
CAS No.: 1387574-54-0
Synonyms: BAL-101553 dihydrochloride
Research Areas:
Lisavanbulin (BAL-101553) dihydrochloride is the prodrug of the microtubule targeting agent Avanbulin (BAL 27862) (HY-106008). Lisavanbulin dihydrochloride exhibits antitumor activity, especially in tumors that express high levels of end-binding protein 1. Lisavanbulin dihydrochloride has ability to target tumor cell proliferation and affects the tumor microenvironment by reducing tumor microvasculature. Lisavanbulin dihydrochloride is also a spindle assembly checkpoint activator. Lisavanbulin dihydrochloride induces cell cycle arrest and subsequent death or aberrant chromosome segregation. Lisavanbulin dihydrochloride can be studied in research for diffuse large B cell lymphoma (DLBCL) and glioblastoma .
Cat. No.: HY-111033
CAS No.: 947182-25-4
RO5068760 is a potent, orally active and selective non-ATP-competitive MEK1/2 inhibitor with an IC50 of 0.025 μM for MEK1. RO5068760 significantly inhibits MAPK pathway activity, thereby inducing G1 cell cycle arrest and apoptosis to inhibit cancer cell growth. RO5068760 exhibits significant efficacy in a broad spectrum of tumors with aberrant MAPK pathway activation. RO5068760 can be used for melanoma, colorectal cancer, non-small cell lung cancer (NSCLC), and pancreatic cancer research .
Cat. No.: HY-161465
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HDAC8-IN-7 (H7E), a HDAC8 inhibitor, exerts retinoprotective effects against glaucomatous injury via ameliorating aberrant Müller glia activation and oxidative stress. HDAC8-IN-7 alleviates functional and structural defects within the inner retina .
Synonyms: (1S,2R)-ABT-957
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(1S,2R)-Alicapistat ((1S,2R)-ABT-957) is an orally active selective inhibitor of human calpains 1 and 2 for the potential application of Alzheimer's disease (AD) . (1S,2R)-Alicapistat mitigates the metabolic liability of carbonyl reduction and inhibits calpain 1 with an IC50 value of 395 nM .
Cat. No.: HY-13649R
CAS No.: 204205-90-3
Synonyms: ZIO 301 (Standard); D 24851 (Standard)
Research Areas:
Indibulin (Standard) is the analytical standard of Indibulin. This product is intended for research and analytical applications. Indibulin (ZIO 301), an orally applicable inhibitor of tubulin assembly, shows potent anticancer activity with a minimal neurotoxicity. Indibulin reduces inter-kinetochoric tension, produces aberrant spindles, activates mitotic checkpoint proteins Mad2 and BubR1, and induces mitotic arrest and apoptosis .
Cat. No.: HY-172747
CAS No.: 2580941-64-4
TNKS-2-IN-3 (Compound 5) is a selective competitive tankyrase 2 (TNKS2) inhibitor with an IC50 value of 0.3 nM, showing over 20-fold selectivity over TNKS1 and more than 100-fold selectivity over PARP1/2. TNKS-2-IN-3 stabilizes axin and suppresses the Wnt/β-catenin pathway by inhibiting TNKS2-mediated ADP-ribosylation, exhibiting antiproliferative activity in colorectal cancer cells. TNKS-2-IN-3 is proming for rasearch of solid tumors with aberrant Wnt pathway activation, such as colorectal cancer .
Cat. No.: HY-186073
CAS No.: 300399-36-4
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HDAC1 activator-1 is a specific HDAC1 activator with orally activity, exerting no significant effects on other HDAC family members. HDAC1 activator-1 exhibits neuroprotective activity, ameliorates cognitive and motor function deficits by reducing neuronal loss and gliosis. HDAC1 activator-1 specifically activates HDAC1 in SH-SY5Y cells and exerts regulatory effects on aberrant cell cycle and DNA damage. HDAC1 activator-1 can be used for the research of TDP-43 proteinopat1-related neurodegenerative diseases including Amyotrophic Lateral Sclerosis (ALS) and cerebral ischemia-related neurological injury .
Cat. No.: HY-109001R
CAS No.: 1254698-46-8
Synonyms: ABT-957 (Standard)
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Alicapistat (Standard) is the analytical standard of Alicapistat (HY-109001). This product is intended for research and analytical applications. Alicapistat (ABT-957) is an orally active selective inhibitor of human calpains 1 and 2 for the potential application of Alzheimer's disease (AD) . Alicapistat mitigates the metabolic liability of carbonyl reduction and inhibits calpain 1 with an IC50 value of 395 nM .
Cat. No.: HY-E70716
Focal adhesion kinase (FAK), a non-receptor tyrosine kinase in the cytoplasm, couples with integrins and growth factor receptors to regulate cell adhesion, proliferation, migration, invasion, and metastasis. FAK is overexpressed and aberrantly activated in many cancer types, including triple negative breast cancer (TNBC). FAK aa411-686 Recombinant Human Active Protein Kinase is a recombinant FAK aa411-686 protein that can be used to study FAK aa411-686-related functions .
Cat. No.: HY-180291
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Anti-inflammatory agent 109 (Compound 2m) is an anti-inflammatory agent. Anti-inflammatory agent 109 directly interacts with p65, attenuates aberrant activation of the NF-κB pathway. Anti-inflammatory agent 109 significantly suppresses the release of key pro-inflammatory mediators, including IL-1β, COX-2, and iNOS. Anti-inflammatory agent 109 conferres robust protection against LPS-induced acute liver injury in septic mice .
Cat. No.: HY-L020
643 compounds
The developmental proteins Hedgehog, Notch and Wnt are key regulators of cell fate, proliferation, migration and differentiation in several tissues. Their related signaling pathways are frequently activated in tumors, and particularly in the rare subpopulation of cancer stem cells. The Wnt signaling pathway is a conserved pathway in animals. Deregulated Wnt signaling has catastrophic consequences for the developing embryo and it is now well appreciated that defective Wnt signaling is a causative factor for a number of pleiotropic human pathologies, including cancer. Hedgehog signaling pathway is linked to tumorigenesis and is aberrantly activated in a variety of cancers. The Notch signaling pathway is a highly conserved cell signaling system present in most animals. It plays an important role in cell-cell communication, and further regulates embryonic development.
MCE designs a unique collection of 643 Wnt/Hedgehog/Notch signaling pathway-related small molecules. Wnt/Hedgehog/Notch Compound Library serves as a useful tool for stem cell research and anti-cancer drug screening.
Cat. No.: HY-L237
337 compounds
Pattern Recognition Receptors (PRRs) are a crucial class of protein molecules expressed in cells of the innate immune system. The core function of Pattern Recognition Receptors is to recognize Pathogen-Associated Molecular Patterns (PAMPs) and Damage-Associated Molecular Patterns (DAMPs). Upon recognizing and binding to PAMPs or DAMPs, PRRs rapidly initiate intracellular signaling pathways (such as the NF-κB, IRF, and inflammasome pathways). This triggers the production of inflammatory factors, chemokines, and type I interferons, thereby initiating inflammatory responses to eliminate pathogens or repair damage. PRRs represent the body's first line of defense against infection, and the rapidity and broad specificity of their response are crucial for host survival. However, aberrant activation of PRR signaling is also a cause of many chronic inflammatory diseases, autoimmune disorders, and neurodegenerative diseases. Therefore, precisely regulating PRR activity has become a key therapeutic strategy for these conditions.
MCE has cataloged 337 inhibitors targeting key PRRs, such as NLRs, TLRs, C-type Lectin Receptors (CLRs), and cGAS, to support drug discovery efforts for chronic inflammatory diseases.
Cat. No.: HY-P991744
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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
