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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
796 Results for "
Inactivation
" in MedChemExpress (MCE) Product Catalog:
Products (796)
796 Results for "Inactivation" in MCE Product Catalog:
Research Areas:
2-Hydroxy atorvastatin calcium salt is an orally active OATP1B1 substrate and inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A reductase (3-hydroxy-3-methylglutaryl-coenzyme A reductase). 2-Hydroxy atorvastatin calcium salt enters cells via OATP1B1-mediated cellular uptake and inhibits de novo hepatic cholesterol synthesis. As an active metabolite of Atorvastatin (HY-B0589), 2-Hydroxy atorvastatin calcium salt contributes to the inhibitory activity against plasma HMG-CoA reductase. 2-Hydroxy atorvastatin calcium salt can be biotransformed into an inactive lactone form, which can be hydrolyzed back to its active acid form chemically or enzymatically. 2-Hydroxy atorvastatin (calcium salt) can be used in the research of hypercholesterolemia .
Cat. No.: HY-13551C
CAS No.: 80277-14-1
Synonyms: m-AMSA isethionate; Acridinyl anisidide isethionate
Target:
Topoisomerase DNA/RNA Synthesis DNA Alkylator/Crosslinker ERK Akt GSK-3 Bcl-2 Family Caspase Apoptosis Potassium Channel
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Amsacrine isethionate (m-AMSA isethionate) is a Topoisomerase II inhibitor. Amsacrine isethionate intercalates into DNA. Amsacrine isethionate induces Ca 2+-mediated inactivation of ERK, and also downregulates AKT, promoting MCL1 downregulation mediated by GSK3β via reducing the phosphorylation level of GSK3β. Amsacrine isethionate induces Apoptosis by activating Caspase-9 and Caspase-3. Amsacrine isethionate blocks HERG potassium channels in the open/inactivated state. Amsacrine isethionate induces chromosomal aberrations and sister chromatid exchanges, and inhibits the synthesis of RNA and DNA. Amsacrine isethionate exhibits anti-leukemic activity. Amsacrine isethionate causes cardiac repolarization disorders, QT interval prolongation, ventricular arrhythmias, and increases the risk of sudden cardiac death. Amsacrine isethionate can be used in research related to acute myeloid leukemia, lymphoma and progressive malignancies .
Cat. No.: HY-13551D
CAS No.: 80277-11-8
Synonyms: m-AMSA lactate; Acridinyl anisidide lactate
Target:
Topoisomerase DNA/RNA Synthesis DNA Alkylator/Crosslinker ERK Akt GSK-3 Bcl-2 Family Caspase Apoptosis Potassium Channel
Research Areas:
Amsacrine lactate (m-AMSA lactate) is a Topoisomerase II inhibitor. Amsacrine lactate intercalates into DNA. Amsacrine lactate induces Ca 2+-mediated inactivation of ERK, and also downregulates AKT, promoting MCL1 downregulation mediated by GSK3β via reducing the phosphorylation level of GSK3β. Amsacrine lactate induces Apoptosis by activating Caspase-9 and Caspase-3. Amsacrine lactate blocks HERG potassium channels in the open/inactivated state. Amsacrine lactate induces chromosomal aberrations and sister chromatid exchanges, and inhibits the synthesis of RNA and DNA. Amsacrine lactate exhibits anti-leukemic activity. Amsacrine lactate causes cardiac repolarization disorders, QT interval prolongation, ventricular arrhythmias, and increases the risk of sudden cardiac death. Amsacrine lactate can be used in research related to acute myeloid leukemia, lymphoma and progressive malignancies .
Cat. No.: HY-176785S
Cat. No.: HY-181964
CAS No.: 3023465-19-9
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KRAS G12C-IN-77 is an orally active and selective KRAS G12C covalent dual-state inhibitor that binds with high affinity to both GDP-bound (inactive state) and GTP-bound (active state) KRAS G12C (IC50 = 133 nM). KRAS G12C-IN-77 rapidly inhibits ERK1/2 phosphorylation, induces the formation of covalent adducts with endogenous KRAS G12C, suppresses the expression of MAPK pathway genes, and inhibits the proliferation of KRAS G12C-mutant cells. KRAS G12C-IN-77 is applicable to research related to KRAS G12C-mutant solid tumors, including pancreatic ductal adenocarcinoma and non-small cell lung cancer .
Cat. No.: HY-L024
931 compounds
A histone modification, a covalent post-translational modification (PTM) to histone proteins, includes methylation, phosphorylation, acetylation, ubiquitylation, and sumoylation, etc. In general, histone modifications are catalyzed by specific enzymes that act predominantly at the histone N-terminal tails involving amino acids such as lysine or arginine, as well as serine, threonine, tyrosine, etc. The PTMs made to histones can impact gene expression by altering chromatin structure or recruiting histone modifiers. Histone modifications act in diverse biological processes such as transcriptional activation/inactivation, chromosome packaging, and DNA damage/repair. Deregulation of histone modification contributes to many diseases, including cancer and autoimmune diseases.
MCE owns a unique collection of 931 bioactive compounds targeting Epigenetic Reader Domain, HDAC, Histone Acetyltransferase, Histone Demethylase, Histone Methyltransferase, Sirtuin, etc. Histone Modification Research Compound Library is a useful tool for histone modification research and drug screening.
Cat. No.: HY-151886
CAS No.: 2759420-43-2
Research Areas:
NU223612 is a cereblon (CRBN)-recruiting IDO1 PROTAC degrader, with a DC50 value of 0.329-0.5438 μM against human IDO1, and it is capable of penetrating the blood-brain barrier. NU223612 directly binds to IDO1, mediates the degradation of both wild-type and catalytically inactive mutant IDO1 proteins, and does not degrade TDO2. NU223612 inhibits IDO1-mediated enzymatic activity. NU223612 directly binds to CRBN and promotes the formation of a cooperative ternary complex with IDO1. NU223612 induces ubiquitin-dependent proteasomal degradation of the IDO1 protein. NU223612 suppresses IDO1-mediated non-enzymatic phosphorylation of NF-κB p65 and the DNA-binding activity of downstream transcription factors. NU223612 can be used in studies of glioblastoma (malignant glioma) .
Cat. No.: HY-183335
Anticancer agent 321 is a Smoothened (SMO) inhibitor with a human IC50 of 0.12 μM, enhanced aqueous solubility, good plasma and metabolic stability, moderate therapeutic index, preliminary safety profile, and moderate oral bioavailability in rats.Anticancer agent 321 binds to SMO’s 7-transmembrane helical channel, forming hydrogen bonds with Asp384 and hydrophobic/π-π interactions with His470, Phe391, Tyr394, stabilizing SMO’s inactive conformation to inhibit Hedgehog/GLI signaling.Anticancer agent 321 inhibits proliferation, suppresses colony formation, induces apoptosis, and downregulates Hedgehog/GLI pathway target genes GLI1, GLI2, Ptch1, HHip in cancer cells.Anticancer agent 321 inhibits tumor growth, downregulates Ki67 and SOX2, and upregulates cleaved-caspase 3 in tumor tissues.Anticancer agent 321 can be used for the research of cutaneous squamous cell carcinoma .
Cat. No.: HY-P10984
CAS No.: 206536-96-1
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Cat. No.: HY-P2114
CAS No.: 173959-12-1
Target:
Research Areas:
Cat. No.: HY-169798
CAS No.: 23481-50-7
Target:
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1,9-Dimethylmethylene blue is a photosensitizer, virus inactivator and hemoglobin oxidant derived from methylene blue. When activated, 1,9-Dimethylmethylene blue generates reactive oxygen species including singlet oxygen, and acts as a metachromatic dye. When activated in monomeric or dimeric form, 1,9-Dimethylmethylene blue induces photoinactivation of R17 phage and vesicular stomatitis virus and oxidizes hemoglobin via non-singlet oxygen reactive oxygen species or singlet oxygen-mediated pathways, respectively. The monomeric form, with higher nucleic acid affinity, achieves virus inactivation under specific conditions without forming methemoglobin. 1,9-Dimethylmethylene blue binds to substances such as glycosaminoglycans to produce color changes. Although it is susceptible to interference from non-glycosaminoglycan components in urine, it is still applicable to spectrophotometric analysis for glycosaminoglycan quantification. With these unique photochemical and binding properties, 1,9-Dimethylmethylene blue is widely used in studies of viral infections and related biochemical analyses .
Cat. No.: HY-W720629
CAS No.: 21420-37-1
Cat. No.: HY-P991736
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Cat. No.: HY-184501
CAS No.: 486440-74-8
UE01 is an orally active, selective small-molecule modulator targeting both ULK1/ERK1/2. UE01 activates hULK1 with an EC50 of 695.30 nM and a KD of 114.3 nM for ULK1; it inhibits hERK1 with an IC50 of 179.90 nM and a KD of 114 nM for ERK1; it shows weak binding to ERK2 with a KD of 2.8 mM. UE01 induces the conformational transition of ULK1 from an inactive to an active state, enhances the phosphorylation of ULK1 Ser317 and mAtg13 Ser355, and reduces the phosphorylation of ULK1 Ser757. UE01 competitively occupies the ATP-binding pocket of ERK1, inhibits ERK1 kinase activity, and reduces the activity of the ERK1/2 signaling pathway. UE01 induces complete autophagy flux and apoptosis, upregulates Atg5, Atg7, LC3-II/LC3-I, Bax, cytochrome C (Cyt c), Cleaved-Caspase 3, Cleaved-PARP1 and E-cadherin, downregulates p62, Bcl-2, MMP-2 and MMP-9, reduces the phosphorylation of Exo70 Ser250, and promotes the proteasome-dependent degradation of Cav-1, thereby inhibiting EMT-related phenotypes and extracellular matrix degradation. UE01 can be used in studies related to triple-negative breast 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
