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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
443 Results for "
isoforms
" in MedChemExpress (MCE) Product Catalog:
Products (443)
443 Results for "isoforms" in MCE Product Catalog:
Cat. No.: HY-182245
Research Areas:
Anticancer agent 314 is a multi-target anticancer agent with tubulin polymerization inhibitory activity (IC50 = 6.35 μM) and human carbonic anhydrase IX (Ki = 27.1 nM) and XII (Ki 20.9 = nM) inhibitory activity. Anticancer agent 314 binds to the colchicine-binding pocket of tubulin and inhibits tumor-associated carbonic anhydrase isoforms via zinc coordination within enzyme active sites. Anticancer agent 314 induces G2/M phase cell cycle arrest, apoptosis via p53-dependent signaling, and broad-spectrum antiproliferative activity across multiple cancer cells. Anticancer agent 314 can be used for the research of cancer, such as leukemia, melanoma, ovarian cancer .
Cat. No.: HY-19482
CAS No.: 630100-90-2
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E7107 is a pre-mRNA spliceosome inhibitor and apoptosis (Apoptosis) inducer. E7107 binds to spliceosome-associated protein 130, inhibits spliceosome assembly and pre-mRNA splicing, regulates cellular protein expression, induces G1 and G2/M phase cell cycle arrest, triggers DNA damage, alters R-loop levels, reduces CHEK2 expression, impairs transcriptional elongation, and shifts MCL1 splicing toward pro-apoptotic isoforms. E7107 inhibits tumor growth in xenograft models and reduces leukemia burden. E7107 can be used in the research of advanced solid tumors, acute myeloid leukemia, T-cell acute lymphoblastic leukemia, and triple-negative breast cancer .
Cat. No.: HY-D3441
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LumiPK is an environment-sensitive probe that specifically targets the liver isoform of pyruvate kinase (PKL). LumiPK exhibits high affinity for PKL with a Kd of 37 nM. LumiPK integrates the 4-sulfonamido-7-aminobenzoxadiazole (SBD) fluorophore into a phthalazine scaffold, and its fluorescence intensity changes with the polarity of the chemical environment, thereby directly reflecting protein occupancy. LumiPK binds only to the tetrameric form of PKL, with the binding site being an allosteric pocket formed at the subunit interface, and key water-mediated interactions enhance its potency; in polar environments such as buffer, its fluorescence is significantly quenched, whereas upon binding to the nonpolar allosteric pocket of PKL, its fluorescence is enhanced. In fluorescence detection, its excitation/emission wavelengths are Ex/Em = 450/550 nm .
Cat. No.: HY-10214R
CAS No.: 908112-43-6
Synonyms: PF-04928473 (Standard)
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SNX-2112 (Standard) is the analytical standard of SNX-2112 (HY-10214). This product is intended for research and analytical applications. SNX-2112 (PF 04928473) is an orally active Hsp90 inhibitor, with a Kd of 16 nM for Hsp90 and IC50s of 30 nM, 30 nM for Hsp90 α and Hsp90 β, also induces Her-2 degradation, and inhibits Grp94 and Trap-1, with IC50s of 10 nM, 4.275 μM and 0.862 μM, respectively . SNX-2112 (PF 04928473) binds Hsp90 isoforms Hsp90α, Hsp90β and Hsp90b1/Grp94 with Kds of 4 nM, 6 nM and 484 nM, respectively .
Cat. No.: HY-19471
CAS No.: 1010440-84-2
(rac)-ZK-304709 is an isoform of ZK-304709 and is an orally active multi-targeted tumor growth inhibitor that inhibits multiple cell cycle-dependent kinases (CDKs), vascular endothelial growth factor receptor kinases (VEGF-RTKs), and platelet-derived growth factor receptor kinase β (PDGF-RTKβ). (rac)-ZK-304709 can dose-dependently inhibit the proliferation and colony formation of neuroendocrine tumor (NET) cells. (rac)-ZK-304709 directly acts on NET cells by inducing G2 cell cycle arrest and apoptosis, while reducing the expression of MCL1, survivin, and HIF1α. (rac)-ZK-304709 effectively controls tumor growth by inducing apoptosis and inhibiting tumor-induced angiogenesis, and may become a potential agent for inhibiting NET .
Cat. No.: HY-P99830
CAS No.: 1227158-72-6
Synonyms: KH902
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Cat. No.: HY-W762015
CAS No.: 57117-44-9
Synonyms: 1,2,3,6,7,8-HxCDF
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1,2,3,6,7,8-Hexachlorodibenzofuran (1,2,3,6,7,8-HxCDF) is a dioxin-like polychlorinated dibenzofuran (PCDF). 1,2,3,6,7,8-Hexachlorodibenzofuran induces expression of the genes encoding aryl hydrocarbon hydroxylase (AHH) and ethoxyresorufin-O-deethylase (EROD) in H-4-II-E rat hepatoma cells (EC50s = 1.47 and 1.24 nM, respectively). 1,2,3,6,7,8-Hexachlorodibenzofuran reduces weight, induces thymic atrophy, and induces the expression of genes encoding the cytochrome P450 (CYP) isoform CYP1A1 and 4-chlorobiphenyl hydroxylase in rats (EC50s = 3.2, 0.9, 0.35, and 0.21 µmol/kg, respectively) .
Cat. No.: HY-109056A
CAS No.: 867365-40-0
Synonyms: R-1206 sodium
Elsulfavirine sodium (R-1206) is an orally active human carbonic anhydrase (carbonic anhydrase, CA) inhibitor and an allosteric inhibitor of HIV-1 non-nucleoside reverse transcriptase (NNRT). Elsulfavirine sodium also targets and blocks the interaction between adenylosuccinate lyase (ADSL) and insulin-induced gene proteins INSIG1/2, blocks SREBP-1-mediated de novo lipid synthesis, and inhibits the proliferation of liver cancer cells. The combination of Elsulfavirine sodium and Lenvatinib (HY-10981) produces a synergistic anti-tumor effect. Elsulfavirine sodium is converted into the active metabolite VM1500A in vivo, blocks the DNA polymerase activity of reverse transcriptase, and inhibits HIV-1 replication. Elsulfavirine sodium exhibits a Ki of 1960 nM-52400 nM against human carbonic anhydrase isoforms including I, VII, VI, VA, VB, IX, XIII, XIV. Elsulfavirine sodium is used in studies related to HIV-1 infection and liver cancer .
Cat. No.: HY-179503
Target:
Phosphodiesterase (PDE) TRP Channel NOD-like Receptor (NLR) NF-κB TNF Receptor Interleukin Related
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PDE/TRPA1/CHIT1-IN-1 is a phosphodiesterases (PDEs), TRPA1, and hCHIT1 (KD of 37.7 μM) inhibitor. PDE/TRPA1/CHIT1-IN-1 is a broad-spectrum PDE inhibitor, potently targeting key isoforms including PDE4B, PDE7A, PDE3A, and PDE8A with IC50s of 15.54, 15.15, 8.39 and 16.46 μM. PDE/TRPA1/CHIT1-IN-1 suppresses NLRP3 inflammasome activation and inhibits NF-κB phosphorylation, downregulating the expression of pro-inflammatory genes (TNF-α and IL-6) in vivo. PDE/TRPA1/CHIT1-IN-1 can be used for chronic obstructive pulmonary disease (COPD) and related inflammatory lung disorders research .
Cat. No.: HY-183309
Research Areas:
FXR/HSD17B13-modulator-2 is a dual FXR activator and HSD17B13 inhibitor with human FXR EC50 of 128 nM, human HSD17B13 IC50 of 0.18 μM, high selectivity over related nuclear receptors and HSD17B isoforms, and oral effectiveness.FXR/HSD17B13-modulator-2 alleviates fatty liver, regulates lipid metabolism, reduces inflammation, and attenuates hepatic fibrosis.FXR/HSD17B13-modulator-2 is the first non-carboxylic acid dual FXR/HSD17B13 modulator.FXR/HSD17B13-modulator-2 can be used for the research of metabolic dysfunction-associated steatohepatitis .
Cat. No.: HY-P86889
Synonyms: Adenylate cyclase stimulating G alpha protein antibody; AHO antibody; Alternative gene product encoded by XL exon antibody; C20orf45 antibody; dJ309F20.1.1 antibody; dJ806M20.3.3 antibody; Extra large alphas protein antibody; GNAS antibody; GNAS complex locus antibody; GNAS1 antibody; Adenylate cyclase stimulating G alpha protein antibody; AHO antibody; Alternative gene product encoded by XL exon antibody; C20orf45 antibody; dJ309F20.1.1 antibody; dJ806M20.3.3 antibody; Extra large alphas protein antibody; GNAS antibody; GNAS complex locus antibody; GNAS1 antibody; GPSA antibody; Gs alpha subunit antibody; GSA antibody; GSP antibody; Guanine nucleotide binding protein (G protein) alpha stimulating activity polypeptide 1 antibody; Guanine nucleotide binding protein alpha stimulating activity polypeptide 1 antibody; Guanine nucleotide binding protein G(s) subunit alpha isoforms short antibody; Guanine nucleotide binding protein G(s) subunit alpha isoforms XLas antibody; Guanine nucleotide regulatory protein antibody; MGC33735 antibody; NESP antibody; NESP55 antibody; Neuroendocrine secretory protein antibody; PHP1A antibody; PHP1B antibody; PHP1C antibody; POH antibody; Protein ALEX antibody; Protein GNAS antibody; Protein NESP55 antibody; SCG6 antibody; Secretogranin VI antibody; XLalphas antibody; XLas antibody;
Synonyms: 5,6-EET; (±)5,6-EpETrE
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5,6-Epoxyeicosatrienoic acid (5,6-EET; (±)5,6-EpETrE) is a fully racemic version of the enantiomeric forms biosynthesized from arachidonic acid by cytochrome P450 enzymes. In solution, 5,6-Epoxyeicosatrienoic acid degrades into 5,6-DiHET and 5,6-δ-lactone, which can be converted to 5,6-DiHET and quantified by GC-MS. In neuroendocrine cells, such as the anterior pituitary and pancreatic islets, 5,6-Epoxyeicosatrienoic acid has been implicated in the mobilization of calcium and hormone secretion. 5,6-Epoxyeicosatrienoic acid is an inhibitor of T-type voltage-gated calcium channels (Cav3) that inhibits isoforms Cav3.1, Cav3.2 (IC50=0.54 μM), and Cav3. and decreases nifedipine-resistant phenylephrine-induced vasoconstriction in isolated mouse mesenteric arteries via Cav3.2 blockade when used at a concentration of 3 μM. In addition, it is a substrate of COX-1 and COX-2.
Cat. No.: HY-109056R
CAS No.: 868046-19-9
Synonyms: R-1206 (Standard)
Elsulfavirine (Standard) is the analytical standard of Elsulfavirine (HY-109056). This product is intended for research and analytical applications. Elsulfavirine (R-1206) is an orally active human carbonic anhydrase (carbonic anhydrase, CA) inhibitor and an allosteric inhibitor of HIV-1 non-nucleoside reverse transcriptase (NNRT). Elsulfavirine also targets and blocks the interaction between adenylosuccinate lyase (ADSL) and insulin-induced gene proteins INSIG1/2, blocks SREBP-1-mediated de novo lipid synthesis, and inhibits the proliferation of liver cancer cells. The combination of Elsulfavirine and Lenvatinib (HY-10981) produces a synergistic anti-tumor effect. Elsulfavirine is converted into the active metabolite VM1500A in vivo, blocks the DNA polymerase activity of reverse transcriptase, and inhibits HIV-1 replication. Elsulfavirine exhibits a Ki of 1960 nM-52400 nM against human carbonic anhydrase isoforms including I, VII, VI, VA, VB, IX, XIII, XIV. Elsulfavirine is used in studies related to HIV-1 infection and liver cancer .
CHMFL-PI3KD-317 is a highly potent, selective and orally active PI3Kδ inhibitor, with an IC50 of 6 nM, and exhibits over 10-1500 fold selectivity over other class I, II and III PIKK family isoforms, such as PI3Kα (IC50, 62.6 nM), PI3Kβ (IC50, 284 nM), PI3Kγ (IC50, 202.7 nM), PIK3C2A (IC50, >10000 nM), PIK3C2B (IC50, 882.3 nM), VPS34 (IC50, 1801.7 nM), PI4KIIIA (IC50, 574.1 nM) and PI4KIIIB (IC50, 300.2 nM). CHMFL-PI3KD-317 inhibits PI3Kδ-mediated Akt T308 phosphorylation in Raji cells, with an EC50 of 4.3 nM. CHMFL-PI3KD-317 has antiproliferative effects on cancer cells .
Cat. No.: HY-120078
CAS No.: 1845753-81-2
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AZD2716 is an orally active secretory phospholipase A2 (sPLA2) inhibitor. AZD2716 inhibits human GIIA sPLA2 (IC50=10 nM), human GV sPLA2 (IC50=40 nM), human GX sPLA2 (IC50=400 nM), snake venom sPLA2 (IC50=2 pM), and snake (Bothrops jararacussu) Lys49-PLA2-like toxin (Kd=110 μM). AZD2716 inhibits sPLA2 isoforms IIa, V, X, snake venom sPLA2s, and snake venom Lys49-PLA2-like toxin myotoxic activity via hydrophobic channel binding. AZD2716 suppresses GIIA sPLA2 production, neutralizes snake venom-induced myotoxicity, and improves survival in envenomed mice. AZD2716 can be used for the research of coronary artery disease, atherosclerosis, and snakebite envenoming .
Cat. No.: HY-153932
CAS No.: 2550399-06-7
NR-7h is a selective p38α/p38β MAPK PROTAC degrader with multiple activities including anti-leishmanial, anti-malarial, and anti-Mayaro virus properties. NR-7h induces specific degradation of p38α/p38β isoforms and p38-MAPK via the ubiquitin-proteasome system. NR-7h reduces the load of Leishmania donovani, modulates the cytokine profile toward a pro-inflammatory phenotype, and enhances the oxidative burst of macrophages. NR-7h inhibits the growth of Plasmodium falciparum in human red blood cells and merozoite invasion. NR-7h reduces the replication of Mayaro virus and the expression of E1 protein in primary human dermal fibroblasts. NR-7h can be used in studies related to parasitic infections, viral infections, and breast cancer .
Cat. No.: HY-173132
CAS No.: 3114057-78-9
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AKR1Cs-IN-1 (Compound 29) is a potent and broad-spectrum inhibitor targeting members of the Aldo-Keto Reductase 1C family (AKR1C1-1C4). By simultaneously occupying the SP2 and SP3 pockets, it effectively inhibits multiple isoforms and disrupts metabolic pathways associated with drug resistance. In enzymatic activity assays, AKR1Cs-IN-1 exhibited significant inhibitory potency, with IC50 values of 0.09, 0.28, 0.05, and 0.51 µM against AKR1C1, AKR1C2, AKR1C3, and AKR1C4, respectively. In the doxorubicin (DOX)-resistant breast cancer cell line MCF-7/ADR, AKR1Cs-IN-1 showed remarkable resensitization effects and significantly enhanced the cytotoxicity of DOX. AKR1Cs-IN-1 holds promise for research on overcoming drug resistance in breast cancer .
Cat. No.: HY-128633
CAS No.: 2269470-35-9
PI3K-IN-4 is a potent Pan-PI3K inhibitor. PI3K-IN-4 has high activity for three PI3K isoforms with the IC50 values of picomole. PI3K-IN-4 shows superior inhibitory activity against PI3Kα (IC50 = 0.20 nM), PI3Kβ (IC50 = 2.99 nM), PI3Kδ (IC50 = 0.48 nM) and PI3Kγ (IC50 = 0.58 nM) and has no significant activity against EGFR. PI3K-IN-4 inhibits cancer cell growth though PI3K/Akt signaling pathway, leading to the inhibition of colony formation and the induction of apoptosis. PI3K-IN-4 can be used for lung, colon and breast cancer research .
Cat. No.: HY-130133
CAS No.: 2378831-21-9
Target:
PI3K mTOR Akt Apoptosis Paraptosis p38 MAPK Mitochondrial Metabolism P-glycoprotein CDK MMP HIF/HIF Prolyl-Hydroxylase VEGFR
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DHW-221 is a potent orally active dual PI3K/mTOR inhibitor, exhibiting low nanomolar potency against all four Class I PI3K isoforms and mTOR (PI3Kα, IC50 = 0.50 nM; PI3Kβ, IC50 = 1.9 nM; PI3Kγ, IC50 = 1.8 nM; PI3Kδ, IC50 = 0.74 nM; mTOR, IC50 = 3.9 nM). DHW-221 exerts antitumor effects by blocking the PI3K/Akt/mTOR pathway and inducing mitochondrial apoptosis and paraptosis (via Endoplasmic Reticulum (ER) stress and MAPK signaling) and arrests cell cycle, thereby inhibiting cell migration, invasion and angiogenesis. DHW-221 inhibits tumor growth in both the A549/Taxol (HY-B0015) and the HCC827 xenograft mouse models. DHW-221 can be used for non-small cell lung cancer (NSCLC), colon and breast cancer research .
Cat. No.: HY-141439
CAS No.: 936475-62-6
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TBE 31 is an orally active Keap1/Nrf2 pathway activator and NQO1 inducer with a Dm value of 1.1 nM for NQO1. TBE 31 binds to cysteine residues of Keap1, inhibits ubiquitination and degradation of Nrf2, thereby activating the expression of ARE-dependent genes. TBE 31 induces cytoprotective enzymes including NQO1 and GST isoforms, promotes Nrf2 accumulation, and upregulates Nrf2-regulated genes related to antioxidation and lipid metabolism. TBE 31 inhibits pro-inflammatory responses, formation of AFB1-DNA adducts, endoplasmic reticulum stress, cell apoptosis (apoptosis), hepatic fibrosis, oxidative stress, and the expression of ChREBP. TBE 31 reduces the number of tumors in a mouse model of ultraviolet-induced skin carcinogenesis. TBE 31 enhances nerve growth factor-induced neurite outgrowth. TBE 31 attenuates LPS-induced serum TNF-α levels and immobility time in mice. TBE 31 can be used in research related to liver cancer, skin cancer, inflammation-related depression, and non-alcoholic steatohepatitis .
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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
