Click Chemistry

16-(tert-Butoxy)-16-oxohexadecanoic acid is a linker containing a hydroxyl group with a carboxylic acid. The hydroxyl group enables further derivatization or replacement with other reactive functional groups. The terminal carboxylic acid can react with primary amine groups of activated NHS ester to form a stable amide bond. Reagent grade, for research purpose.

Azide-PEG8-Val-Cit-PABC-SN-38 is a cleavable ADC linker with the SN-38 drug. SN-38 (7-Ethyl-10-hydroxycamptothecin) is a topoisomerase I inhibitor, and it inhibits DNA and RNA synthesis with IC50s of 0.077 and 1.3 μM, respectively. SN-38 is the active component of ADC drugs, IMMU-132. and also is the active metabolite of irinotecan. The Val-Cit will specifically be cleaved by Cathepsin B. As this enzyme is only present in the lysosome, the ADC payload will be released only in the cell. Azido group will react with DBCO, BCN or other Alkyne group through click chemistry, PEG spacer increases aqueous solubility. Reagent grade, for research purpose.

DBCO-PEG-tBoc, MW 3,400 is an azide reactive PEGylation reagent. DBCO reacts with azide (N3) efficiently without the presence of Cu catalyst known to be highly toxic for cells. Under mild acidic conditions, t-Boc group can be removed to yield the free amine. Reagent grade, for research purpose.

Fmoc-Gly-Gly-Phe-Gly-OH is a self-assembly of N- and C-protected tetrapeptide containing an Fmoc-protected amine. The Fmoc group can be deprotected under basic condition to obtain the free amine which can be used for further conjugations. The compound is a protease cleavable linker used for the antibody-drug conjugate (ADC). Reagent grade, for research purpose.

4SC-202, also known as Domatinostat, is an orally bioavailable benzamide and inhibitor of human class I histone deacetylases (HDACs) isoenzymes 1, 2 and 3, with potential antineoplastic activity. 4SC-202 is a low-molecular weight, water soluble molecule that can penetrate the cytosol of cells, where it binds to the retinoic acid receptor and inhibits cell growth. Domatinostat induces apoptosis by inhibiting the phosphorylation of Akt and ERK1/2, which are proteins involved in regulating cell survival and proliferation pathways. Reagent grade, for research purpose.

Abexinostat is a novel hydroxamic acid HDAC inhibitor. Abexinostat also inhibits metallo-β-lactamase domain-containing protein 2 (MBLAC2) hydrolase activity. Reagent grade, for research purpose.

Belinostat is an inhibitor of class I histone deacetylases. Belinostat has also been used in formulation in the treatment of relapsed or refractory peripheral T cell lymphoma. Reagent grade, for research purpose.

CUDC-101 is a small-molecule inhibitor of histone deacetylase (HDAC), EGFR (epidermal growth factor receptor), and HER2 ( human epidermal growth factor receptor 2) inhibitor for the treatment of cancer. Reagent grade, for research purpose.

Dacinostat is a hydroxamate-based inhibitor of histone deacetylases (HDAC1 and HDAC2). Reagent grade, for research purpose.