Propargyl-Gly(m-PEG4)-Val-Cit-PAB(m-PEG4)-MMAE

SOLU-KNEX® cleavable linker features a Val-Cit dipeptide. In this product, a Propargyl-Gly(m-PEG4) moiety replaces the conventional maleimidocaproyl (MC) unit to enhance aqueous solubility. The propargyl functional group is widely employed in click chemistry to undergo selective cycloaddition with azides. Additionally, m-PEG4 is attached to the commonly used self-immolative para-aminobenzyl (PAB) moiety to further increase aqueous solubility. The payload is monomethyl auristatin E (MMAE), a highly potent antimitotic agent that inhibits tubulin polymerization, leading to cell-cycle arrest and subsequent apoptosis.

Derived from established ADC linker architectures, SOLU-KNEX® ADC linkers integrate solubilizing moieties—such as PEG, amine-containing groups, or polysarcosine (PSAR), to enhance aqueous solubility. Solubility and physicochemical properties can be finely tuned through selection and combination of these groups, making the linkers highly adaptable for diverse ADC and related applications. SOLU-KNEX® is a registered trademark of Tenova Pharmaceuticals, Inc. For research use only.

References

(1) Lee, H. M., Abdul-Hadi, K., Appleman, V. A., Cardin, D., Dong, L., England, D., Ganno, M. L., Gershman, R., Gigstad, K., Gulavita, N., Hu, Z., Huang, J., Huang, S. C., Lok, D., Ma, L., Malley, J., Mizutani, M., Molchanova, N., Piatkov, K. I., … Abu-Yousif, A. O. (2025). Identification of a Novel Linker Enabling the Bioconjugation of a Cyclic Dinucleotide for the STING Antibody-Drug Conjugate TAK-500. Bioconjugate Chemistry, 36(11), 2423–2435. https://doi.org/10.1021/acs.bioconjchem.5c00424

(2) Yamazoe, S., Poudel, Y., Sega, E., Mukhopadhyay, A., Ramakrishnan, R., Ukairo, O., Liu, S., Akter, R., Sadanala, K., Que, K., Cheng, Q., Kotapati, S., Deshpande, M., Cox, M., Chourey, S., Gupta, A., Kempson, J., Pabbisetty, K., Kaspady, M., … Chekler, E. P. (2025). Discovery and Characterization of a First-in-Class LIV1-TLR7/8 Immunomodulatory Conjugate with Robust Myeloid Activation and Antitumor Activity. Journal of Medicinal Chemistry. https://doi.org/10.1021/acs.jmedchem.5c00324

Documents 

Datasheet          MSDS

Citations

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