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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
34 Results for "
Target engagement
" in MedChemExpress (MCE) Product Catalog:
Products (34)
34 Results for "Target engagement" in MCE Product Catalog:
14
6
6 Cited Publications
Target:
研究分野:
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
Target:
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) .
製品番号: HY-178129
CAS 番号: 1312534-69-2
Target:
研究分野:
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 .
製品番号: HY-P99404
CAS 番号: 2084037-83-0
別名: E6011
Target:
Target:
研究分野:
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 .
製品番号: HY-P99431
CAS 番号: 2489390-15-8
別名: Alomfilimab; SAR 445256
Target:
製品番号: HY-148281
CAS 番号: 2418022-85-0
Target:
研究分野:
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 .
製品番号: HY-136557
CAS 番号: 2095109-82-1
別名: PAD2-IN-1
Target:
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) .
製品番号: HY-158821A
Target:
研究分野:
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 .
製品番号: HY-157605
CAS 番号: 2973402-91-2
Target:
研究分野:
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 .
製品番号: HY-157606
CAS 番号: 2973399-28-7
Target:
研究分野:
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 .
製品番号: HY-157607
CAS 番号: 2973398-27-3
Target:
研究分野:
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 .
製品番号: HY-157611
CAS 番号: 2973397-26-9
Target:
研究分野:
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 .
製品番号: HY-157612
CAS 番号: 2973397-48-5
Target:
研究分野:
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 .
製品番号: HY-157602
CAS 番号: 2973746-64-2
Target:
研究分野:
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 .
製品番号: HY-175656
Target:
研究分野:
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 .
製品番号: HY-158821
CAS 番号: 2179222-27-4
Target:
研究分野:
ISTH0036 is a phosphorothioate LNA-modified antisense oligonucleotide gapmer that selectively targets and downregulates TGF-β2 mRNA. ISTH0036 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 exhibits long-lasting, dose-dependent ocular tissue distribution and target engagement in rabbit and non-human primate eyes. ISTH0036 can be used for the study of various ocular disorders, such as glaucoma and neovascular retinal diseases .
製品番号: HY-112081A
CAS 番号: 2223023-19-4
Target:
研究分野:
BAY-707 acetate is a highly potent and selective substrate-competitive inhibitor of MTH1 with superior cellular target engagement and pharmacokinetic properties.
製品番号: HY-157603
CAS 番号: 2973400-87-0
Target:
研究分野:
DHX9-IN-7 (550) is a RNA helicase DHX9 inhibitor, with an EC50 of 0.105 μM in DHX9 cellular target engagement. Used in cancer 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
