Results for Click Chemistry ( 996 )
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Azido-PEG3-Val-Cit-PAB-PNP is a cleavable peptide ADC linker. The Val-Cit will specifically be cleaved by Cathepsin B. PNP groupg is a good leaving group when treating with aminebearing payload. Azido group will react with DBCO, BCN or other Alkyne group through click chemistry, PEG spacer increases aqueous solubility. Reagent grade, for research purpose. Please contact us for GMP-grade inquiries.
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MS436, through a set of water-mediated interactions, exhibits low nanomolar affinity (estimated Ki of 30-50 nM) with preference for the first bromodomain over the second. MS436 effectively blocks BRD4 transcriptional activity in lipopolysaccharide-induced production of both nitric oxide and IL-6 in mouse macrophages (IC50 values are 3.8 and 4.9 μM, respectively). MS436 represents a new class of bromodomain inhibitors and will facilitate further investigation of the biological functions of the two bromodomains of BRD4 in gene expression. Reagent grade, for research purpose. Please contact us for GMP-grade inquiries.
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Apabetalone (RVX-208) is an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain. Apabetalone has C50s are 87+/-10 μM and 0.51+/-0.041 μM for BD1 and BD2, respectively. Apabetalone binds to the acetyl-lysine binding pocket in a peptide-competitive way, which accounts for its pharmacological activity. Reagent grade, for research purpose. Please contact us for GMP-grade inquiries.
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3,4-Dibromo-Mal-PEG4-t-butyl ester is a PEG linker with a dibromomaleimide group and t-butyl protecting group. The dibromomaleimide group allows for two points of attachment because both bromine atoms can be substituted. Dibromo-Maleimide is sensitive to high temperature and light. The t-butyl ester can be removed under acidic conditions. The hydrophilic PEG chain increases the water solubility of the compound in aqueous media. Reagent grade, for research purpose. Please contact us for GMP-grade inquiries.
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BI 2536 is a potent, ATP-competitive, well tolerated and effects Polo-like kinases (Plks) as well as a pan-BET (bromodomain and extra-terminal motif) family inhibitor. BI 2536 has an IC50s of 0.83 and 25 nM with PLK1 and BRD4 inhibitor, respectively. BI 2536 also blocks the activities of Plk2 and Plk3 to a slightly lesser extent with IC50 of 3.5 nM and 9.0 nM, respectively. BI-2536 suppresses IFNB (encoding IFN-beta) gene transcription. It also shows good blood-brain barrier permeability and causes mitotic arrest in glioblastoma-derived neural stem cells but not normal neural stem cells. Reagent grade, for research purpose. Please contact us for GMP-grade inquiries.