Tubulosine 

Tubulosine is an alkaloid. Tubulosine can be isolated from Pogonopus tubulosus (DC.) Schumann. Tubulosine is an ATP-competitive, selective JAK3 inhibitor with an IC₅₀ value of 9.9 nM. Tubulosine also inhibits the kinase activities of other JAK family members, the extent of inhibition is less than that of JAK3, with IC₅₀ values of 69.5, 84.9 and 76.3 nM for JAK1, JAK2 and TYK2, respectively. Tubulosine selectively inhibits JAK3 signalling by binding to the ATP-binding site of the kinase of JAK3. Tubulosine induces apoptotic and necrotic/autophagic cell death. Tubulosine inhibits the process of peptide chain elongation by eukaryotic polysomes by, specifically preventing the elongation-factor-2-dependent step of translocation. Tubulosine exhibits anticancer activity in breast cancer cells^[1][2][3][4].

475.62

C₂₉H₃₇N₃O₃

2632-29-3

OC1=CC=C(N2)C(C(CCN3)=C2[C@H]3C[C@H]4C[C@@]5([H])C6=CC(OC)=C(OC)C=C6CCN5C[C@@H]4CC)=C1

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Brauchli P, et al. The structure of tubulosine, a novel alkaloid from Pogonopus tubulosus (DC.) Schumann. Journal of the American Chemical Society, 1964, 86(9): 1895-1896.

  [2]. Carrasco L, et al. Specific inhibition of translocation by tubulosine in eukaryotic polysomes. Eur J Biochem. 1976 Apr 15;64(1):1-5.  [Content Brief]

  [3]. Kim BH , et al. Anticancer Activity of Tubulosine through Suppression of Interleukin-6-Induced Janus Kinase 2/Signal Transducer and Activation of Transcription 3 Signaling. J Breast Cancer. 2019 Sep;22(3):362-374.  [Content Brief]

  [4]. Kim BH, et al. Tubulosine selectively inhibits JAK3 signalling by binding to the ATP-binding site of the kinase of JAK3. J Cell Mol Med. 2020 Jul;24(13):7427-7438.  [Content Brief]