Paprotrain (CAS 57046-73-8)
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Paprotrain is a cell-permeable acrylonitrile compound that inhibits the kinesin-6 family member MKLP-2 (Mitotic kinesin-like protein 2, or KIF20A). Paprotrain has an IC50 against basal and microtubule-/MT-stimulated ATPase activity = 1.35 and 0.83 muM, respectively in a reversible, ATP-uncompetitive (Ki = 3.36 muM), and MT-noncompetitive (Ki = 1.6 muM) manner, with little effect against the ATPase activity of 12 other kinesins (≤20% inhibition at 50 muM), including the close related MKLP-1 and MPP1 (M-phase phosphoprotein 1). Paprotrain may act to inhibit cellular ARK-2 (Aurora B) and survivin anaphase centromere-to-spindle midzone relocation in HeLa cultures (50 muM for 8 h), but not MKLP-1- or Kif4-mediated PRC1 relocation, resulting in misaligned chromosomes (70% of total metaphase cells), multipolar spindles (14% of total metaphase cells), and eventual apoptosis.
Paprotrain (CAS 57046-73-8) References
- Relocation of Aurora B and survivin from centromeres to the central spindle impaired by a kinesin-specific MKLP-2 inhibitor. | Tcherniuk, S., et al. 2010. Angew Chem Int Ed Engl. 49: 8228-31. PMID: 20857469
- MKlp2 inhibitor paprotrain affects polar body extrusion during mouse oocyte maturation. | Liu, J., et al. 2013. Reprod Biol Endocrinol. 11: 117. PMID: 24359300
- KIF20A regulates porcine oocyte maturation and early embryo development. | Zhang, Y., et al. 2014. PLoS One. 9: e102898. PMID: 25036038
- Further investigation of Paprotrain: Towards the conception of selective and multi-targeted CNS kinase inhibitors. | Labrière, C., et al. 2016. Eur J Med Chem. 124: 920-934. PMID: 27676471
- Coupling fission and exit of RAB6 vesicles at Golgi hotspots through kinesin-myosin interactions. | Miserey-Lenkei, S., et al. 2017. Nat Commun. 8: 1254. PMID: 29093437
- KIF20A, highly expressed in immature hematopoietic cells, supports the growth of HL60 cell line. | Morita, H., et al. 2018. Int J Hematol. 108: 607-614. PMID: 30182171
- Role of a Kinesin Motor in Cancer Cell Mechanics. | Mandal, K., et al. 2019. Nano Lett. 19: 7691-7702. PMID: 31565944
- Characterization of KIF20A as a prognostic biomarker and therapeutic target for different subtypes of breast cancer. | Nakamura, M., et al. 2020. Int J Oncol. 57: 277-288. PMID: 32467984
- MKLP2 Is a Motile Kinesin that Transports the Chromosomal Passenger Complex during Anaphase. | Adriaans, IE., et al. 2020. Curr Biol. 30: 2628-2637.e9. PMID: 32502404
- An anaphase surveillance mechanism prevents micronuclei formation from frequent chromosome segregation errors. | Orr, B., et al. 2021. Cell Rep. 37: 109783. PMID: 34758324
- The kinesin KIF20A promotes progression to castration-resistant prostate cancer through autocrine activation of the androgen receptor. | Copello, VA. and Burnstein, KL. 2022. Oncogene. 41: 2824-2832. PMID: 35418689
- KIF20A promotes the development of fibrosarcoma via PI3K-Akt signaling pathway. | Jin, Z., et al. 2022. Exp Cell Res. 420: 113322. PMID: 36037925
- Identification of the KIF and MCM protein families as novel targets for combination therapy with CDK4/6 inhibitors in bladder cancer. | Kositza, J., et al. 2023. Urol Oncol. 41: 253.e11-253.e20. PMID: 36813612
Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
Paprotrain, 5 mg | sc-364124A | 5 mg | $92.00 | |||
Paprotrain, 10 mg | sc-364124 | 10 mg | $132.00 |