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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
44 Results for "
MES model
" in MedChemExpress (MCE) Product Catalog:
Products (44)
44 Results for "MES model" in MCE Product Catalog:
17
17 Publications Verification
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CPI-455 is a specific, pan-KDM5 inhibitor with an IC50 of 10 nM for KDM5A. CPI-455 mediates KDM5 inhibition, elevates global levels of H3K4me3, and decreases the number of drug-tolerant persister cancer cells in multiple cancer cell line models treated with standard chemotherapy or targeted agents .
17
17 Publications Verification
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EED226 is a polycomb repressive complex 2 (PRC2) inhibitor, which binds to the K27me3-pocket on embryonic ectoderm development (EED) and shows strong antitumor activity in xenograft mice model . EED226 is a potent, selective, and orally bioavailable EED inhibitor . EED226 inhibits PRC2 with an IC50 of 23.4 nM when the H3K27me0 peptide is used as a substrate in the in vitro enzymatic assays .
17
17 Publications Verification
Cat. No.: HY-100421A
CAS No.: 2095432-28-1
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CPI-455 hydrochloride is a specific, pan-KDM5 inhibitor with an IC50 of 10 nM for KDM5A. CPI-455 hydrochloride mediates KDM5 inhibition, elevates global levels of H3K4me3, and decreases the number of drug-tolerant persister cancer cells in multiple cancer cell line models treated with standard chemotherapy or targeted agents .
2
2 Cited Publications
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TAK-418 is an orally active, blood-brain barrier-penetrant LSD1 inhibitor with a human IC50 of 2.9 nM. TAK-418 irreversibly inhibits LSD1 by forming a compact flavin-FAD adduct with the catalytic domain FAD, blocking the demethylation of H3K4me1/2 and H3K9me1/2 without disrupting the LSD1-GFI1B interaction. TAK-418 restores normally dysregulated brain gene expression and DNA methylation, increases H3K4me1/2/3 and H3K9me2 at the Ucp2 locus, and induces Ucp2 mRNA expression. TAK-418 rescues defective H3K4 histone modifications, normalizes adult neurogenesis, and improves recognition memory, social behavior, and cognition in rodent models. TAK-418 can be used in research related to neurodevelopmental disorders, Alzheimer's disease, and autism spectrum disorders .
1
1 Cited Publications
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ZK53 is a selective activator of mitochondrial caseinolytic protease P (HsClpP) (EC50: 1.37?μM for α-casein hydrolysis by HsClpP). ZK53 is is inactive toward bacterial ClpP proteins. ZK53 induces apoptosis in H1703, H520 and SK-MES-1 cells. ZK53 induces dysregulation of mitochondrial functions in lung squamous cell carcinoma (LUSC) cells. ZK53 inhibits tumor growth in H1703 xenograft mouse model .
Cat. No.: HY-172431
CAS No.: 2376397-93-0
Synonyms: BHV-7000
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Opakalim (BHV-7000) is a selective Kv7.2/7.3 potassium channels activator with an EC50 of 0.6 μM. Opakalim shows minimal GABAA receptor activation and exhibits potent anti-seizure efficacy in the maximal electroshock seizure (MES) model. Opakalim can be used for the study of seizures .
Cat. No.: HY-162275
CAS No.: 861224-48-8
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JMJD1C-IN-1 is an orally active and selective inhibitor of JMJD1C (IC50 = 0.59 μM, Kd = 1.96 μM). JMJD1C-IN-1 inhibits the binding of JMJD1C to H3K9me2 peptide substrate in the HTRF assay (IC50 = 1.47 μM). JMJD1C-IN-1 disrupts intratumoral regulatory T (Treg) cell fitness by dual mechanisms: promoting H3K9me2 accumulation to downregulate PD1 expression and reducing STAT3 demethylation to enhance STAT3 activation. JMJD1C-IN-1 demonstrates dose-dependent antitumor efficacy in multiple mouse tumor models (MCA205 fibrosarcoma, B16-F10 melanoma, LLC lung cancer, Hepa1-6 hepatocellular carcinoma, CT26 colorectal cancer). JMJD1C-IN-1 can be used for the study of tumor immunotherapy by selectively targeting intratumoral Treg cells .
Cat. No.: HY-154484
CAS No.: 179479-04-0
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3’-O-Me-G(iBu)-2’-phosphoramidite is a guanosine analog. Some guanosine analogs have immunostimulatory activity. In some animal models, they also induce type I interferons, producing antiviral effects. Studies have shown that the functional activity of guanosine analogs is dependent on the activation of Toll-like receptor 7 (TLR7) .
Cat. No.: HY-177578
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NN3201 is a c-Kit-targeting antibody-drug conjugate (ADC) with high affinity (KD = 0.19 pM). NN3201 is composed of 4-(3-Tosyl-2-(tosylmethyl)propanoyl)benzoic acid-glu(PEG24-Me)-val-cit-NH-benzyloxyformic acid-MMAE (HY-178219) and an anti-c-Kit human monoclonal antibody NN2101 (HY-P991293). NN3201 rapidly internalizes and inhibits stem cell factor (SCF)-driven signaling, thereby delivering its payload to induce cell cycle arrest and apoptosis. NN3201 exhibits no Fc-mediated effector functions antibody-dependent cell-mediated cytotoxicity (ADCC)/complement-dependent cytotoxicity (CDC) due to reduced FcγR binding. NN3201 exhibits significant c-Kit-dependent anti-tumor efficacies in various tumor models. NN3201 can be used in small cell lung cancer (SCLC) and gastrointestinal stromal tumor (GIST) and acute myeloid leukemia (AML) research [1][2].
Cat. No.: HY-161759
CAS No.: 3107476-89-8
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MS152 is an orally active, blood-brain barrier penetrant inhibitor of EHMT2/G9a and EHMT1/GLP, with IC50s of 76 nM and 126 nM, repsectively. MS152 reduces H3K9me2 levels and reactivates maternally silenced Prader-Willi syndrome (PWS) genes. MS152 significantly improves perinatal lethality and growth retardation in mouse models, and is applicable to research related to Prader-Willi syndrome .
Cat. No.: HY-178825
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LD-110 is a PROTAC degrader targeting LSD1 with a DC50 of 0.44-1.24 μM. LD-110 acts through the CRBN E3 ubiquitin ligase and the ubiquitin-proteasome system, leading to H3K4me2 accumulation. LD-110 induces apoptosis and inhibits the growth and survival of multiple esophageal squamous cell carcinoma (ESCC) cell lines. LD-110 inhibits tumor growth in the KYSE-150 xenograft model. LD-110 can be used in research related to esophageal squamous cell carcinoma .
Cat. No.: HY-W012481
CAS No.: 631-07-2
Synonyms: Ethylphenylhydantoin; Phenylethyihydantoin; Desmethylmephenytoin
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Nirvanol (Ethylphenylhydantoin) is a metabolite of Mephenytoin (HY-B1184) that exerts anticonvulsant effects in the maximal electroshock (M.E.S.) seizure model in mice. Nirvanol shows potential for research in epilepsy-related neurological disorders .
Cat. No.: HY-N16374
CAS No.: 68373-95-5
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Cat. No.: HY-155313
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β-Glucuronide-NB-bis[N(Me)-methyl ester]-MMAE (compound 20) is auristatins-glucuronide conjugate. Antitumor agent-122 shows in vitro antiproliferative activities against β-glucuronidase pretreated and untreated cancer cells with an IC50 value of 5.7 nM - 9.7 nM. Antitumor agent-122 shows potent antitumor efficacy in HCT-116 xenograft mouse model without inducing side effects .
Cat. No.: HY-156292
CAS No.: 3018914-66-1
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IHMT-EZH2-426 is an orally active and selective EZH2 degrader. IHMT-EZH2-426 forms a covalent bond with Cys663 of EZH2, inhibits its catalytic activity, and reduces the protein levels of EZH2 as well as the level of H3K27me3. IHMT-EZH2-426 acts as an antiproliferative agent against B-cell lymphoma and triple-negative breast cancer cells, and also exhibits anti-tumor related activity in Pfeiffer and MDA‑MB‑231 xenograft models. IHMT-EZH2-426 can be used in studies related to B-cell lymphoma and triple-negative breast cancer .
Cat. No.: HY-171509
CAS No.: 2682939-57-5
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Mal-N(Me)-C6-N(Me)-PNU-159682 (Compound 27), an agent-linker conjugate for ADC, consists the ADC linker Mal-N(Me)-C6-N(Me) and a potent ADC cytotoxin PNU-159682. Mal-N(Me)-C6-N(Me)-PNU-159682 (Compound 27) selectively delivers the payload to CD46-expressing cells, where the linker is cleaved by cathepsin B to release PNU-159682, inducing DNA damage and apoptosis. Mal-N(Me)-C6-N(Me)-PNU-159682 shows durable tumor regression in xenograft (PDX) models of non-small cell lung cancer (NSCLC) and colorectal cancer (CRC) .
Cat. No.: HY-106424
CAS No.: 130403-08-6
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Soretolide is an antiepileptic agent. Soretolide is effective in maximal electroshock-induced seizure (MES) test in rodents. Soretolide inhibits metabolism of Phenytoin (HY-B0448). Soretolide exhibits a good pharmacokinetic character in rats model .
Cat. No.: HY-170833
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Anticonvulsant agent 8 (compound D4) is an anticonvulsant agent that inhibits GABAA currents with ED50 values of 2.23 and 24.60 mg/kg in the maximum electroshock (MES) and pentylenetetrazol (PTZ) tests in mouse models, respectively .
Cat. No.: HY-W012481R
CAS No.: 631-07-2
Synonyms: Ethylphenylhydantoin (Standard); Phenylethyihydantoin (Standard); Desmethylmephenytoin (Standard)
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Research Areas:
Nirvanol (Ethylphenylhydantoin) is a metabolite of Mephenytoin (HY-B1184) that exerts anticonvulsant effects in the maximal electroshock (M.E.S.) seizure model in mice. Nirvanol shows potential for research in epilepsy-related neurological disorders .
Cat. No.: HY-114300
CAS No.: 1226855-28-2
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DSP-0565 (compound 17a) is a strong, broad-spectrum anti-epileptic agent (AED) candidate with unique GABAergic function. DSP-0565 shows anti-convulsant activity in various models (scPTZ, MES, 6 Hz and amygdala kindling) with good safety margin .
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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
