2632-29-3
Chemical Structure
Tubulosine
- CAS No.: 2632-29-3
- Formula:C29H37N3O3
- Molecular Weight:475.62
InChIKey: JRVWIILYWSBUMC-PRUVNFMMSA-N
SMILES: 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
Biological Activity: 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].
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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. | |||||||||||||||||||||
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- [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]
Keywords
