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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-130652
CAS No.: 2271036-46-3
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Pomalidomide 4'-PEG3-azide is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide-based cereblon ligand and a linker. Pomalidomide 4'-PEG3-azide can be used for the synthesis of iRucaparib-TP3 (Compound 3). iRucaparib-TP3 is a highly efficient PARP1?degrader based on Rucaparib by using the PROTAC approach . Pomalidomide 4'-PEG3-azide is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
Cat. No.: HY-145973B
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3'OMe-m7GpppAmpG (Tris) is a trinucleotide Cap1 analog with the structure m7 (3'OMeG)(5') ppp (5')(2'OMeA) pG, and also functions as a cis-acting ligase ribozyme inhibitor. 3'OMe-m7GpppAmpG (Tris) effectively reduces free 5'-triphosphate groups on RNA transcripts, thereby enabling efficient co-transcriptional capping of in vitro transcribed mRNA. 3'OMe-m7GpppAmpG (Tris) is not only widely used in the preparation of modified mRNA including trivalent influenza vaccine candidates, but also applicable to studies related to SARS-CoV-2 infection and other relevant research .
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GBD-9 is a degrader based on the E3 ubiquitin ligase CRBN that targets BTK and the G1 to S phase transition protein GSPT1. GBD-9 has both PROTAC and molecular glue properties by inducing ubiquitination and proteasomal degradation of target proteins. GBD-9 can efficiently degrade wild-type and mutant BTK (such as C481S mutation) and GSPT1. GBD-9 significantly inhibits tumor cell proliferation by inducing G1 phase arrest in cancer cells, downregulating anti-apoptotic proteins (BCL-2, MCL-1) and activating Caspase-3 to induce apoptosis. GBD-9 is mainly used in the research of hematological tumors such as diffuse large B-cell lymphoma (DLBCL) and acute myeloid leukemia (AML) .
Cat. No.: HY-156096
CAS No.: 3033039-28-7
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HDAC3-IN-2 (compound 4i) is a pyrazinyl hydrazide-based HDAC3 inhibitor (IC50: 14 nM) that efficiently targets triple-negative breast cancer cells. HDAC3-IN-2 is cytotoxic with an IC50 of 0.55 μM against 4T1 and an IC50 of 0.74 μM against MDA-MB-231. HDAC3-IN-2 has anti-tumor efficacy in vivo in tumor-bearing mouse models, selectively increasing the acetylation levels of H3K9, H3K27 and H4K12, increasing the contents of apoptosis-related caspase-3, caspase-7 and cytochrome c, and reducing Proliferation-related Bcl-2, CD44, EGFR, and Ki-67 levels .
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PolQi1 is a selective inhibitor targeting the Polθ domain of DNA polymerase. PolQi1 inhibits the Polθ-mediated microhomology end joining (TMEJ/alt-EJ) pathway, reducing insertion/deletion (Indels) and imprecise editing events during DNA repair. PolQi1 can enhance the efficiency and accuracy of homology-directed repair (HDR) or Prime editing, and reduce off-target effects; and in combination with DNA-PK inhibitor AZD-7648 (HY-111783), exert efficient genome editing capabilities with dual pathway regulation. PolQi1 can be mainly used in gene editing research (such as CRISPR-Cas9 or Prime editing system optimization) to improve the precision editing efficiency of difficult-to-edit cells (such as primary hepatocytes and mouse embryos) .
Cat. No.: HY-179112
CAS No.: 2826215-20-5
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PROTAC IKKβ/NR4A1 degrader-1 is a highly efficient and effective dual-PROTAC degrader targeting IKKβ and NR4A1. PROTAC IKKβ/NR4A1 degrader-1 can increase the levels of caspase 3 and cleaved caspase 3 proteins, while the necroptosis marker RIP kinase remained unchanged, indicating that it can induce apoptosis. PROTAC IKKβ/NR4A1 degrader-1 can be used for the study of Acute myeloid leukemia (AML). Red: IKKβ/NR4A1 ligand (HY-13067); Blue: E3 ligase CRBN ligand (HY-14658); Black: Linker (HY-79577) .
Cat. No.: HY-179388
CAS No.: 3123329-68-7
PROTAC Sirt2 Degrader-2 is a highly efficient and selective PROTAC degrader targeting SIRT2. PROTAC Sirt2 Degrader-2 demonstrates the most potent anti-proliferative activity both in vitro and in vivo. PROTAC Sirt2 Degrader-2 leads to a marked increase in H4K16Ac levels. PROTAC Sirt2 Degrader-2 significantly suppresses clonogenic formation and migration, induces cell cycle arrest, and promotes apoptosis. PROTAC Sirt2 Degrader-2 inhibits the AKT/mTOR signaling pathway by indirectly degrading SIRT2 and blocking downstream protein phosphorylation, thereby disrupting the signaling cascade and suppressing tumor development. PROTAC Sirt2 Degrader-2 can be used for the study of ovarian cancer .
Cat. No.: HY-179588
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PROTAC BET Degrader-14 is a highly efficient PROTAC targeting BET (bromodomain and extra-terminal domain). PROTAC BET Degrader-14 can degrade all BET (BRD2, BRD3, BRD4) family proteins. PROTAC BET Degrader-14 potently degrades BET proteins in U2OS osteosarcoma cell lines (BRD4 DC50 = 130 nM) and KYSE180 esophageal squamous cell carcinoma cell lines (DC50 = 40 nM). PROTAC BET Degrader-14’s dependence on the ubiquitin-proteasome system. PROTAC BET Degrader-14 decreases levels of BET-regulated gene products c-Myc, RUNX2, and KRT14. PROTAC BET Degrader-14 can be used for the study of osteosarcoma .
Cat. No.: HY-182945
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IKZF2-degrader 5 is a highly efficient, highly selective, rapidly acting, and orally active IKZF2 molecular glue degrader. IKZF2-degrader 5 induces IKZF2 degradation via the Cullin-CRBN-dependent pathway. IKZF2-degrader 5 promotes the production of pro-inflammatory IL-2. IKZF2-degrader 5 attenuates the immunosuppressive function of regulatory T cells (Tregs). IKZF2-degrader 5 triggers rapid, significant, and sustained IKZF2 degradation in the spleen and thymus of mice. IKZF2-degrader 5 inhibits tumor growth. IKZF2-degrader 5 can be used for the research of B16F melanoma .
Cat. No.: HY-184389
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PROTAC HDAC6 degrader 10 is a highly efficient, safe and selective HDAC6 PROTAC degrader with a pIC50 of 8.75 and a pDC50 of 9.2 in BEAS-2B cells. PROTAC HDAC6 degrader 10 recruits cereblon to form a ternary complex with HDAC6, thereby achieving the degradation of HDAC6. PROTAC HDAC6 degrader 10 significantly induces hyperacetylation of α-tubulin without affecting the acetylation of H3, and achieves sustained HDAC6 knockdown in mouse lung tissues. PROTAC HDAC6 degrader 10 exhibits high bioavailability after subcutaneous administration in mice. PROTAC HDAC6 degrader 10 enables the study of HDAC6 pharmacology via chemical knockdown of HDAC6 in vitro and in vivo, and can be used for research on pulmonary diseases .
Cat. No.: HY-D2763
CAS No.: 890928-51-5
Cat. No.: HY-E70115
CAS No.: 134712-49-5
Feruloyl esterase is a subclass of carboxylesterases that hydrolyzes the ester linkages between hydroxycinnamic acids and arabinoxylan/pectin polysaccharides in plant cell walls. Feruloyl esterase can hydrolyze ethyl ferulate to release ferulic acid, disrupt plant cell wall structure, promote fiber swelling, and facilitate cellulase hydrolysis. Feruloyl esterase synergizes with xylanase by removing ferulic acid side chains, thereby promoting efficient hydrolysis of xylan into monomers. Feruloyl esterase acts as a virulence factor for Verticillium dahliae VdFAE and Magnaporthe oryzae Fae1, facilitating host infection and colonization. Feruloyl esterase 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 can be used in studies related to verticillium wilt and rice blast .
Cat. No.: HY-P11261
Cat. No.: HY-P11490
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Cat. No.: HY-P11590
Cat. No.: HY-P5377
CAS No.: 221055-89-6
Synonyms: Cathepsin K substrate
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Cat. No.: HY-W012166
CAS No.: 42014-51-7
Synonyms: NHS-Bromoacetate
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N-Succinimidyl bromoacetate (NHS-Bromoacetate) is a heterobifunctional crosslinking reagent, mainly used to modify the ɛ-amino group of lysine side chains. By covalently linking its bromoacetyl moiety to the ɛ-amino group of lysine in peptidomimetics, N-Succinimidyl bromoacetate enables their conjugation with thiol-modified nanoparticles via thioether bonds. N-Succinimidyl bromoacetate also performs bromoacetylation modification on carrier proteins, which then forms stable thioether bonds with the thiol groups of cysteine in peptides, thus efficiently preparing soluble peptide-protein conjugates with high substitution ratios. N-Succinimidyl bromoacetate can be used to prepare activated Sepharose derivatives for affinity chromatography, protein affinity labeling reagents, and peptide-protein immunogen conjugates with non-immunogenic linkages. N-Succinimidyl bromoacetate is applicable to studies related to HIV-1 infection and glioblastoma multiforme .
Cat. No.: HY-145973
CAS No.: 2089461-55-0
Synonyms: m7(3'OMeG)(5')ppp(5')(2'OMeA)pG
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3’OMe-m7GpppAmpG (m7(3'OMeG)(5')ppp(5')(2'OMeA)pG) is a trinucleotide Cap1 analog with the structure m7 (3'OMeG)(5') ppp (5')(2'OMeA) pG, and also functions as a cis-acting ligase ribozyme inhibitor. 3’OMe-m7GpppAmpG effectively reduces free 5'-triphosphate groups on RNA transcripts, thereby enabling efficient co-transcriptional capping of in vitro transcribed mRNA. 3’OMe-m7GpppAmpG is not only widely used in the preparation of modified mRNA including trivalent influenza vaccine candidates, but also applicable to studies related to SARS-CoV-2 infection and other relevant research .
Cat. No.: HY-175849
Research Areas:
ALK degrader 1 is a potent, hydrophobic tag (HyT)-based degrader that induces ubiquitin-proteasome system (UPS)-dependent EML4-ALK degradation (DC50 = 0.13 μM). ALK degrader 1 demonstrates potent ALK degradation and antiproliferative effects in ALK-dependent cell lines, while showing minimal cytotoxicity in ALK fusion-negative cells. ALK degrader 1 triggers cell cycle arrest at the G0/G1 phase and stimulates apoptosis. ALK degrader 1 not only facilitates efficient degradation of the ALK protein but also disrupts key downstream effectors, including the STAT3 signaling axis. ALK degrader 1 mediates robust EML4-ALK degradation in vivo. ALK degrader 1 can be used for ALK-related diseases research .
Cat. No.: HY-176243
CAS No.: 1947405-90-4
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15-Deoxy-Δ12,14-Prostaglandin J2-2-glyceryl ester is a derivate of 15-Deoxy-Δ-12,14-prostaglandin J2 (HY-108568). 15-Deoxy-Δ-12,14-prostaglandin J2 (15d-PGJ2) is a cyclopentenone prostaglandin and a metabolite of PGD2. 15-Deoxy-Δ-12,14-prostaglandin J2 is a selective PPARγ (EC50 of 2 µM) and a covalent PPARδ agonist. 15-Deoxy-Δ-12,14-prostaglandin J2 promotes efficient differentiation of C3H10T1/2 fibroblasts to adipocytes with an EC50 of 7 μM .
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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
