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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
840 Results for "
Efficient
" in MedChemExpress (MCE) Product Catalog:
Products (840)
840 Results for "Efficient" in MCE Product Catalog:
Cat. No.: HY-178122
Research Areas:
THNAN69 is a PROTAC degrader targeting LIMK2, which efficiently degrades ectopically expressed EGFP-LIMK2 in live HuCCT1 cells with a DC50 of 1 nM. THNAN69 induces isoform-specific ubiquitin-mediated degradation of LIMK2 by recruiting the CRBN E3 ligase, forming a stable ternary complex with LIMK2 and CRBN; this degradation process depends on the activity of cullin-RING ligase. THNAN69 does not reduce phosphorylated cofilin levels, as LIMK1 can compensate for the loss of LIMK2; it also stimulates compensatory activation of the Rho signaling pathway including PAK1/2 and ROCK1/2. THNAN69 serves as a selective chemical probe for dissecting the LIMK2 isoform-dependent biological mechanisms. THNAN69 can be used in the research of cholangiocellular carcinoma and acute lymphoblastic leukemia .
Cat. No.: HY-179424
CAS No.: 3095636-64-6
PROTAC HIF-1α degrader-2 is a highly efficient and selective PROTAC degrader targeting HIF-1α. PROTAC HIF-1α degrader-2 promotes HIF-1α degradation via the ubiquitin-proteasome pathway by facilitating the formation of a HIF-1α/VHL ternary complex. PROTAC HIF-1α degrader-2 inhibits HeLa cell proliferation, migration, and colony formation, and induces apoptosis. PROTAC HIF-1α degrader-2 reduces p-MEK and p-AKT expression in the MAPK and PI3K/AKT pathways. PROTAC HIF-1α degrader-2 can be used for the study of cervical cancer .
Cat. No.: HY-180261
CAS No.: 3107761-81-6
GP262 is a PI3K/mTOR PROTAC degrader targeting PI3Kγ, PI3Kα and mTOR with DC50 values of 42.23 nM, 227.4 nM and 45.4 nM, respectively in MDA-MB-231 cells. GP262 induces degradation of p110α and p110γ with a DC50 of 227.4 and 42.23 nM. GP262 efficient modulates the PI3K/AKT/mTOR pathway, achieving degradation through the ubiquitin-proteasome system (UPS). GP262 also exhibits robust antiproliferative activity and induces apoptosis in vitro. GP262 exhibits tumor growth suppression capability and biosafety profile. GP262 can be used for leukemia and triple-negative breast cancer (TNBC) .
Cat. No.: HY-180467
CAS No.: 2823367-76-4
Target:
Research Areas:
Neu5Ac-2Galβ1-3Glc-oxazoline-(2)Me (Compound G12) is a disaccharide linker. Neu5Ac-2Galβ1-3Glc-oxazoline-(2)Me can be efficiently recognized by the endo-glycosidase Endo-S2 and can be directedly transferred to the conserved N-glycosylation site (Asn297 position) of the antibody's Fc domain through enzymatic catalytic reactions, thereby achieving site-specific modification of the antibody. Neu5Ac-2Galβ1-3Glc-oxazoline-(2)Me can be used for for the synthesis of antibody-conjugated drugs (ADCs) .
Cat. No.: HY-180467A
Target:
Research Areas:
Neu5Ac-2Galβ1-3Glc-oxazoline-(2)Me (Compound G12) sodium is a disaccharide linker. Neu5Ac-2Galβ1-3Glc-oxazoline-(2)Me sodium can be efficiently recognized by the endo-glycosidase Endo-S2 and can be directedly transferred to the conserved N-glycosylation site (Asn297 position) of the antibody's Fc domain through enzymatic catalytic reactions, thereby achieving site-specific modification of the antibody. Neu5Ac-2Galβ1-3Glc-oxazoline-(2)Me sodium can be used for for the synthesis of antibody-conjugated drugs (ADCs) .
Cat. No.: HY-181532
Target:
Research Areas:
IAP ligand 8 is an ASX-series, non-peptidic SMAC mimetic and IAP binder with high cell permeability. IAP ligand 8 selectively targets cIAP1-BIR3, XIAP-BIR2 (with a KD of 15.8 nM for both). IAP ligand 8 serves as an IAP ligand moiety to synthesize IAP-recruiting protein degrader (IPD) (HY-181590). This IPD simultaneously forms two ternary complexes, cIAP1-A538-TEAD1 and XIAP-A538-TEAD1, and efficiently degrades TEAD1 via a dual E3 recruitment mechanism, while inducing the autodegradation of cIAP1. IAP ligand 8 and its series of degraders are applicable to targeted research on Hippo pathway-dysregulated cancers such as NF2-mutant mesothelioma .
Cat. No.: HY-181607
TEAD ligand-Linker Conjugate 3 (the blue structure + black structure of A536 in the literature) is a conjugate of a TEAD1-targeting ligand and a linker. TEAD ligand-Linker Conjugate 3 can be coupled with an IAP ligand (HY-181531) to form an IAP-recruiting bifunctional protein degrader (IPD) (HY-181594), also known as a SNIPER degrader. This TEAD SNIPER simultaneously binds to the TEAD1 palmitoylation pocket and the BIR3 domain of cIAP1 to form a ternary complex, efficiently inducing the ubiquitination and degradation of both TEAD1 and cIAP1 (DC50=110 nM, Dmax=51%; IC50=122 nM for cIAP1). TEAD ligand-Linker Conjugate 3 and its synthesized SENIPER molecule can be utilized in research on Hippo pathway dysregulation-related diseases, such as NF2-mutant tumors .
Cat. No.: HY-D2745
CAS No.: 1638544-48-5
Cat. No.: HY-W012572R
CAS No.: 351-50-8
Category:
Cat. No.: HY-145973A
Purity: ≥99.0%
Synonyms: m7(3'OMeG)(5')ppp(5')(2'OMeA)pG ammonium solution (100 mM)
306-N16B is a selective lung-targeted lipid nanoparticle that reversibly targets lung endothelial cells and specific immune cells through selective adsorption of a protein corona mediated by differences in tail structure (such as fibrinogen β/γ chain). 306-N16B binds to specific plasma proteins in the blood to form a protein corona, which guides the particles to be enriched in the lungs, releases mRNA and promotes target cell gene expression, exerts efficient lung cell transfection activity, and can precisely regulate gene delivery of different cell types in the lungs (such as endothelial cells and macrophages). 306-N16B can be used in gene therapy technologies for hereditary lung diseases including pulmonary lymphangioleiomyomatosis (LAM), restoring tumor suppressor function by delivering Tsc2 mRNA, and can also be used for lung-specific mRNA vaccines and gene editing therapies .
Cat. No.: HY-164899
CAS No.: 2765091-45-8
Synonyms: 2-aminopyridine-3-carboxylic acid imidazolide
Target:
Research Areas:
2A3 (2-aminopyridine-3-carboxylic acid imidazolide) is a covalent probe reagent for Selective 2'-Hydroxyl Acylation analyzed by Primer Extension (SHAPE) that targets the RNA ribose 2'-OH group. 2A3 efficiently permeates the biological membranes of Gram-negative bacteria, Gram-positive bacteria, and mammalian cells. 2A3 exhibits no base bias and specifically labels conformationally flexible, unpaired regions within RNA.
2A3 forms covalent adducts by acylating the 2'-OH groups of flexible RNA residues. When combined with SHAPE-MaP (mutational profiling) sequencing technology, these modification sites are converted into detectable mutational signals, thereby accurately reflecting local RNA backbone flexibility and base-pairing status. 2A3 is primarily utilized in molecular biology and transcriptomics research, including the resolution of RNA structuromes in living cells, the study of RNA folding regulatory mechanisms, and the investigation of non-coding RNA functions .
Cat. No.: HY-178984
CAS No.: 3095278-75-1
Research Areas:
PI3Kα-IN-28 (Compound 23) is an efficient dual targeted PI3K/BRD4 inhibitor. PI3Kα-IN-28 can inhibit the proliferation of various cells, such as KYSE180 and KYSE450 cells. PI3Kα-IN-28 can concentration dependently inhibit migration and colony formation, induce G0/G1 phase arrest, significantly inhibit DNA synthesis, and significantly increase the proportion of senescent cells. PI3Kα-IN-28 can inhibit the expression of p-AKT and c-Myc and activate the AMPK-p27 pathway. PI3Kα-IN-28 can be used for research on cancers such as esophageal cancer .
Cat. No.: HY-179433
Research Areas:
PROTAC AR Degrader-12 is a highly efficient PROTAC targeting AR coactivator binding site (AR-CBS). PROTAC AR Degrader-12 induces AR degradation in a ubiquitin proteasome system (UPS) pathway-dependent manner. PROTAC AR Degrader-12 inhibits tumor cell growth by affecting DNA replication and cell division PROTAC AR Degrader-12 could not only effectively degrade AR, but also potently inhibit the proliferation of MCF-7 and multiple mutant or resistant BC cells. PROTAC AR Degrader-12 effectively blocked estrogen receptor α (ERα) signaling through a dual mechanism involving ERα protein downregulation and suppression of its transcriptional activity. PROTAC AR Degrader-12 significantly inhibits the mRNA expression of FOXA1, GREB1, SRC, and PELP1. PROTAC AR Degrader-12 can be used for the study of breast cancer .
Cat. No.: HY-E70115A
Feruloyl esterase, Acetivibrio cellulolyticus is a subclass of carboxylesterases that hydrolyzes the ester linkages between hydroxycinnamic acids and arabinoxylan/pectin polysaccharides in plant cell walls. Feruloyl esterase, Acetivibrio cellulolyticus can hydrolyze ethyl ferulate to release ferulic acid, disrupt plant cell wall structure, promote fiber swelling, and facilitate cellulase hydrolysis. Feruloyl esterase, Acetivibrio cellulolyticus synergizes with xylanase by removing ferulic acid side chains, thereby promoting efficient hydrolysis of xylan into monomers. Feruloyl esterase, Acetivibrio cellulolyticus acts as a virulence factor for Verticillium dahliae VdFAE and Magnaporthe oryzae Fae1, facilitating host infection and colonization. Feruloyl esterase, Acetivibrio cellulolyticus promotes the degradation of cotton GhDFR through binding to its NADPH domain, thereby inhibiting flavonoid-mediated innate immunity and inducing cell death in Nicotiana benthamiana. Feruloyl esterase, Acetivibrio cellulolyticus can be used in studies related to verticillium wilt and rice blast .
Cat. No.: HY-P11698
CAS No.: 476667-31-9
Research Areas:
Cat. No.: HY-P4087
CAS No.: 1417221-06-7
Cat. No.: HY-P4087B
Cat. No.: HY-L102
1,900 compounds
Rare diseases are an important public-health issue and a challenge for the medical community. Most rare diseases are genetic disorders, which are often severely disabling, substantially affect life expectancy, and impair physical and mental abilities. Currently, there are about 7,000 identified rare diseases, together affecting 10% of the population. However, fewer than 6% of all rare diseases have an approved treatment option, highlighting their tremendous unmet needs in drug development. The process of repurposing drugs for new indications, compared with the development of novel orphan drugs, is a time-saving and cost-efficient method resulting in higher success rates, which can therefore drastically reduce the risk of drug development for rare diseases.
MCE carefully collects a unique of 1,900 compounds studied in preclinical, clinical trials or approved used in rare diseases treatment. MCE rare diseases drug library is a useful tool for the research of rare diseases. All compounds can provide corresponding indications for rare diseases.
Cat. No.: HY-L945
74 compounds
Sulfonyl fluoride (-SO₂F) overcomes the poor target selectivity of traditional covalent warheads that rely heavily on cysteine. With high stability and tunable electrophilicity under physiological conditions, it targets multiple nucleophilic residues including Lys, Tyr, Ser and His, offering expanded druggable space, lower off-target risks and prolonged efficacy. It is widely used in covalent inhibitors, molecular glues, PROTACs and chemical probes.
MCE has built a highly diverse sulfonyl fluoride fragment library with 1,162 structurally diverse, drug-like fragments. Designed for balanced reactivity, stability and compatibility, these molecules feature tunable electrophilicity, simple scaffolds and high derivatization potential. Combined with SuFEx click chemistry, the library enables efficient modular modification and rapid structure optimization.
Ideal for targeting non-cysteine residues, this library improves covalent screening and probe development efficiency, serving as a precise tool for early-stage covalent drug discovery and chemical biology research.
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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
