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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 "
engagement
" in MedChemExpress (MCE) Product Catalog:
Products (44)
44 Results for "engagement" in MCE Product Catalog:
14
6
6 Cited Publications
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SETDB1-TTD-IN-1 is a SETDB1 methyltransferase activator and SETDB1-TTD competitive inhibitor (Kd of 88 nM), and selectivity for SETDB1-TTD over other tudor and bromodomain proteins. SETDB1-TTD-IN-1 stimulates methyltransferase activity via increased catalytic activity, promotes Akt1 Lys64 methylation, Akt1 Thr308 phosphorylation and activation. SETDB1-TTD-IN-1 prevents SETDB1-TTD-histone H3 peptide association, induces global gene expression changes, exhibits cellular target engagement, and acts as a tool compound for SETDB1-TTD function exploration. SETDB1-TTD-IN-1 can be used for the research of breast cancer .
2
2 Cited Publications
Synonyms: PAD2-IN-1 hydrochloride
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AFM32a (PAD2-IN-1) hydrochloride, a benzimidazole-based derivative, is a potent and selective protein arginine deiminase 2 (PAD2) inhibitor. AFM32a hydrochloride shows superior selectivity for PAD2 over PAD4 (95-fold) and PAD3 (79-fold) .
1
1 Cited Publications
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BPK-25, an active acrylamide, promotes degradation of nucleosome remodeling and deacetylation (NuRD) complex proteins by a post-translational mechanism involving covalent protein engagement. BPK-25 inhibits TMEM173 activation by the cyclic dinucleotide ligand cGAMP .
Cat. No.: HY-178129
CAS No.: 1312534-69-2
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MRL-SYKi is a chemical probe for gain-of-function variants of spleen tyrosine kinase (SYK). MRL-SYKi reduces the catalytic activity of SYK S550Y, SYK S550F and SYK P342T, and downregulates the phosphorylation level of SYK S550Y. MRL-SYKi serves as a template for developing NanoBRET tracers targeting SYK, enabling NanoBRET cellular target engagement assays for gain-of-function variants of SYK. MRL-SYKi is applicable to research related to inflammatory and immune diseases .
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KSC-34, a covalent modifier of protein disulfide isomerase A1 (PDIA1), is also a selective and potent a-site inhibitor of PDIA1 with an IC50 of 3.5 μM. KSC-34 displays a 30-fold selectivity for a domain over a′ domain and displays high selectivity for PDIA1 in complex proteomes with minimal engagement of other members of the PDI family . KSC-34 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Cat. No.: HY-P99404
CAS No.: 2084037-83-0
Synonyms: E6011
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Cat. No.: HY-148739
CAS No.: 2170679-42-0
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dBRD 9-A is a selective BRD9 PROTAC degrader. dBRD 9-A induces near complete BRD9 degradation dependent on E3 ubiquitin ligase CRBN and BRD9 bromodomain engagement, and drives loss of BRD9 chromatin binding genome-wide. dBRD 9-A downregulates oncogenic SS18-SSX-driven transcriptional programs, super enhancer-associated gene expression, and SS18-SSX1 super enhancer binding, and depletes GBAF complex members GLTSCR1/1L from SS18-SSX complexes. dBRD 9-A induces cell cycle arrest and increases apoptosis in synovial sarcoma cells. dBRD 9-A can be used for the research of synovial sarcoma .
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DHX9-IN-9 (509) is a RNA helicase DHX9 inhibitor, with an EC50 of 0.0177 μM in DHX9 cellular target engagement. Used in cancer research .
Cat. No.: HY-P99431
CAS No.: 2489390-15-8
Synonyms: Alomfilimab; SAR 445256
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Cat. No.: HY-148281
CAS No.: 2418022-85-0
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TMX-2164 is a potent, irreversible B-cell lymphoma 6 (BCL6) inhibitor with an IC50 value of 152 nM. TMX-2164 displays sustained target engagement and antiproliferative activity in cells .
Cat. No.: HY-136557
CAS No.: 2095109-82-1
Synonyms: PAD2-IN-1
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AFM32a (PAD2-IN-1), a benzimidazole-based derivative, is a potent and selective protein arginine deiminase 2 (PAD2) inhibitor. AFM32a shows superior selectivity for PAD2 over PAD4 (95-fold) and PAD3 (79-fold) .
Cat. No.: HY-158821A
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ISTH0036 sodium is a phosphorothioate LNA-modified antisense oligonucleotide gapmer that selectively targets and downregulates TGF-β2 mRNA. ISTH0036 sodium suppresses TGF-β2 expression, reduces choroidal neovascularization and vascular leakage, inhibits fibrosis, blocks epithelial-to-mesenchymal transition, and inhibits angiogenesis while promoting bleb survival. ISTH0036 sodium exhibits long-lasting, dose-dependent ocular tissue distribution and target engagement in rabbit and non-human primate eyes. ISTH0036 sodium can be used for the study of various ocular disorders, such as glaucoma and neovascular retinal diseases .
Cat. No.: HY-157605
CAS No.: 2973402-91-2
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DHX9-IN-11 (469) is a RNA helicase DHX9 inhibitor, with an EC50 of 0.0838 μM in DHX9 cellular target engagement. Used in cancer research .
Cat. No.: HY-157606
CAS No.: 2973399-28-7
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DHX9-IN-13 (389) is a RNA helicase DHX9 inhibitor, with an EC50 of 3.4 μM in DHX9 cellular target engagement. Used in cancer research .
Cat. No.: HY-157607
CAS No.: 2973398-27-3
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DHX9-IN-15 (287) is a RNA helicase DHX9 inhibitor, with an EC50 of 0.232 μM in DHX9 cellular target engagement. Used in cancer research .
Cat. No.: HY-157611
CAS No.: 2973397-26-9
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DHX9-IN-17 (186) is a RNA helicase DHX9 inhibitor, with an EC50 of 0.161 μM in DHX9 cellular target engagement. Used in cancer research .
Cat. No.: HY-157612
CAS No.: 2973397-48-5
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DHX9-IN-16 (208) is a RNA helicase DHX9 inhibitor, with an EC50 of 0.125 μM in DHX9 cellular target engagement. Used in cancer research .
Cat. No.: HY-157602
CAS No.: 2973746-64-2
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DHX9-IN-8 (Compound 6) is a RNA helicase DHX9 inhibitor, with an EC50 of 3.4 μM in DHX9 cellular target engagement. Used in cancer research .
Cat. No.: HY-175656
CAS No.: 3107269-84-8
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MDI-117740 is a dual LIMK1/2 inhibitor. MDI-117740 shows effective cellular target engagement with LIMK1 (pIC50 = 6.73) and LIMK2 (pIC50 = 7.18) in HEK293 cells. MDI-117740 exerts significant anti-migratory activity in MDA-MB-231 cells. MDI-117740 can be used for the study of cancers and neurodegenerative disorders .
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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
