Bioactivity | Itaconate-alkyne (ITalk) is a specific bioorthogonal probe for quantitative and site-specific chemoproteomic profiling of Itaconation in living cells. Itaconate-alkyne, a functional analogue of Itaconate, exhibits comparable antiinflammatory effect with Itaconate and enables the labeling of bona fide targets of Itaconate[1]. | ||||||||||||
Invitro | Itaconate-alkyne (ITalk; 0.005, 0.01, 0.05, 0.1, 0.5, 1, 5, 10 mM; 0-4 hours) has the concentration- and time-dependent labeling in the lysates of Raw264.7 cells[1]. Itaconate-alkyne (100 μM; for 4 hours) significantly increases the protein level of NRF-2 in LPS (100 ng/mL)-stimulated Raw264.7 cells and significantly inhibits lactate production in LPS-stimulated Raw264.7 cells. Itaconate-alkyne significantly inhibits the secretion of interlukin-1β (IL-1β) in LPS-timulated Raw264.7 cells[1]. Itaconate-alkyne (100 μM; for 12 hours) does not affect the cell viability of Raw264.7 cells[1]. Itaconate-alkyne can capture itaconate targets including DNA damage-binding protein 1 (DDB1), Gelsolin (GSN), ATP-citrate synthase (ACLY) and Adenylate kinase 2 (AK2) in inflammatory macrophages[1]. | ||||||||||||
Name | Itaconate-alkyne | ||||||||||||
CAS | 2454181-83-8 | ||||||||||||
Formula | C13H18O4 | ||||||||||||
Molar Mass | 238.28 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [1]. Wei Qin, et al. Chemoproteomic Profiling of Itaconation by Bioorthogonal Probes in Inflammatory Macrophages. J Am Chem Soc . 2020 Jun 24;142(25):10894-10898. |