SIAIS630121

SIAIS630121 : Degrader (PROTAC) of NAMPT

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(0 ratings)

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Probe SIAIS630121 is in the process of SERP review.

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Information

NAMPT

Degrader (PROTAC)

up to 10 nM

In Vitro Validations

No in Vitro Validations

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): To assess selectivity of 630121, a mass spectrometry-based quantitative proteomics analysis in the HCT116 CRC cell line was performed, in the absence and presence of the NAMPT-targeting PROTAC compound. 630121-treated cells showed 86.2% reduction in NAMPT protein levels and minimal off-target side effects on other proteins.

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SERP ratings and comments

SERP+ Ratings

In Cell Rating

SERP+ Comments:

We would recommend 630121 for studies of NAMPT degradation/inhibition. The probe demonstrates degradation of NAMPT with consequent inhibition of NAMPT NAD+ synthase activity. The probe results in cytotoxicity for NAMPT-dependent cell lines, having a greater effect than ligands targeting NAMPT alone

(last updated: 6 Feb 2026 )