Nampt degrader-2 

Nampt degrader-2 is a fluorescent PROTAC, which efficiently degrades NAMPT with an IC₅₀ of 41.9 nM. Nampt degrader-2 binds to NAMPT and VHL to form a ternary complex and subsequently induced NAMPT degradation via ubiquitin-proteasome system (UPS). Nampt degrader-2 leads to significant reduction of NAD⁺ and exerts potent antitumor activities^[1].

Nampt degrader-2 (Compound B4; 30 nM; 24 h) is able to degrade NAMPT with a DC₅₀ value of 8.4 nM. Nampt degrader-2 enables the visualization of degradation in A2780 cells^[1].
Nampt degrader-2 (Compound B4) shows the best antitumor activity in suppression of the proliferation in A2780 cells (IC₅₀ = 12.1 nM)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Nampt degrader-2 (Compound B4; 10-30 mg/kg; i.p; once a day; for 14 consecutive days) shows excellent antitumor effects in a dose-dependent manner. And Nampt degrader-2 significantly decreases the NAMPT levels in the tumors^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

1052.33

C₅₉H₇₃N₉O₇S

O=C(C(C1=CC=C(C=C1)C(NCC2=CN=CC=C2)=O)=NC3=C4C=C(C=C3)NC(CCCCCCCCCCC(N[C@@H](C(C)(C)C)C(N5C[C@H](O)C[C@H]5C(N[C@@H](C)C6=CC=C(C7=C(C)N=CS7)C=C6)=O)=O)=O)=O)N4CCC

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• [1]. Junfei Cheng, et al. Making Protein Degradation Visible: Discovery of Theranostic PROTACs for Detecting and Degrading NAMPT. J Med Chem. 2022 Dec 8;65(23):15725-15737.  [Content Brief]