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CDK/cyclin inhibitor
Inhibitor of CDK1/cyclin B1 and CDK1/cyclin A. Reversibly arrests human cells at the G2/M border of the cell cycle. Allows for effective cell synchronisation in early mitosis. Downregulates expression of the antiapoptotic proteins Bcl-2 and survivin and blocks p53-mediated induction of p21 and MDM2.
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Product Details
| Alternative Name |
(5Z)-2-((Thiophen-2-yl)methylamino)-5-((quinolin-6-yl)methylene)thiazol-4(5H)-one |
|---|---|
| Appearance |
Brown solid. |
| CAS |
872573-93-8 |
| Couple Target |
CDK, Cyclin |
| Couple Type |
Inhibitor |
| Formula |
C18H13N3OS2 |
| Identity |
Determined by 1H-NMR and MS. |
| MW |
351.4 |
| Purity |
≥95% (HPLC) |
| Solubility |
Soluble in DMSO (50mM). |
Handling & Storage
| Use/Stability |
As indicated on product label or CoA when stored as recommended. Stable for at least 6 months after receipt when stored at -20°C in the dark. |
|---|---|
| Handling |
Protect from light. |
| Long Term Storage |
-20°C |
| Shipping |
Ambient Temperature |
| Regulatory Status |
RUO – Research Use Only |
|---|
- Spatial organization of supercoil dynamics during DNA replication: Kusano, Y., Shinkai, S., et al.; bioRxiv , (2024)
- Cyclin A/B RxL Macrocyclic Inhibitors to Treat Cancers with High E2F Activity: Singh, S., Gleason, C. E., et al.; bioRxiv , (2024)
- Chromosomal rearrangements associated with SMC5/6 deficiency in DNA replication: Kusano, Y., Kinugasa, Y., et al.; Genes. Cells 29, 1251 (2024), Abstract
- ASPP2 Is Phosphorylated by CDK1 during Mitosis and Required for Pancreatic Cancer Cell Proliferation: Y. Xiao, et al.; Cancers 15, 5424 (2023), Abstract
- Chromosome arm length, and a species-specific determinant, define chromosome arm width: Y. Kakui, et al.; Cell Rep. 41, 111753 (2022), Abstract
- The phosphatase CTDSPL2 is phosphorylated in mitosis and a target for restraining tumor growth and motility in pancreatic cancer: Y. Xiao, et al.; Cancer Lett. 526, 53 (2021), Abstract
- Phosphorylation of the androgen receptor at Ser81 is co-sustained by CDK1 and CDK9 and leads to AR-mediated transactivation in prostate cancer: Gao, X., Liang, J., et al.; Mol. Oncol. 15, 1901 (2021), Abstract
- Quantitative differences between cyclin-dependent kinases underlie the unique functions of CDK1 in human cells: H.W. Lau, et al.; Cell Rep. 37, 109808 (2021), Abstract
- The mTORC1/S6K/PDCD4/eIF4A Axis Determines Outcome of Mitotic Arrest: Moustafa-Kamal, M., Kucharski, T. J., et al.; Cell Rep. 33, 108230 (2020), Abstract
- Cell cycle oscillators underlying orderly proteolysis of E2F8: Wasserman, D., Nachum, S., et al.; Mol. Biol. Cell 31, 725 (2020), Abstract
- Local actin nucleation tunes centrosomal microtubule nucleation during passage through mitosis: F. Farina, et al.; EMBO J. 38, e99843 (2019), Abstract — Full Text
- PCNT is critical for the association and conversion of centrioles to centrosomes during mitosis: Kim, J., Kim, J., et al.; J. Cell Sci. 132, (2019), Abstract
- Adducin-1 is essential for spindle pole integrity through its interaction with TPX2: W.H. Hsu, et al.; EMBO Rep. 2018, e45607 (2018), Abstract
- The M-phase specific hyperphosphorylation of Staufen2 involved the cyclin-dependent kinase CDK1: Beaujois, R., Ottoni, E., et al.; BMC Cell Biol. 18, 25 (2017), Abstract
- Phosphorylation of Astrin regulates its Kinetochore Function: H. Chung, et al.; J. Biol. Chem. 291, 17579 (2016), Application(s): Cell culture for kinase inhibition, Abstract — Full Text
- Dominant-Negative Effects of Adult-Onset Huntingtin Mutations Alter the Division of Human Embryonic Stem Cells-Derived Neural Cells: C. Lopes, et al.; PLoS One. 11, e0148680 (2016), Application(s): Cell culture, Abstract — Full Text
- Aurora-A mediated histone H3 phosphorylation of threonine 118 controls condensin I and cohesin occupancy in mitosis: Wike, C. L., Graves, H. K., et al.; Elife 5, e11402 (2016), Abstract
- Benzobisthiazoles Represent a Novel Scaffold for Kinase Inhibitors of CLK Family Members: Prak, K., Kriston-Vizi, J., et al.; Biochemistry 55, 608 (2016), Abstract
- MST2 phosphorylation at serine 385 in mitosis inhibits its tumor suppressing activity: X. Chen, et al.; Cell. Signal. 28, 1826 (2016), Application(s): CDK1 Inhibitor, identification of the corresponding kinase for MST2 phosphorylation, Abstract
- An epigenetic regulator emerges as microtubule minus-end binding and stabilizing factor in mitosis: S. Meunier, et al.; Nat. Commun. 6, 7889 (2015), Application(s): Cell synchronization, Abstract
- Interkinetic nuclear migration is centrosome independent and ensures apical cell division to maintain tissue integrity: Strzyz, P. J., Lee, H. O., et al.; Dev. Cell 32, 203 (2015), Abstract
- JAM-A regulates cortical dynein localization through Cdc42 to control planar spindle orientation during mitosis: H. Tuncay, et al.; Nat. Commun. 6, 8128 (2015), Application(s): Cell culture , Abstract — Full Text
- Oncoprotein YAP Regulates the Spindle Checkpoint Activation in a Mitotic Phosphorylation-dependent Manner through Upregulation of BubR1: S. Yang, et al.; J. Biol. Chem. 290, 6191 (2015), Application(s): Cell Culture, Abstract — Full Text
- The structure and substrate specificity of human Cdk12/Cyclin K: Bösken, C. A., Farnung, L., et al.; Nat. Commun. 5, 3505 (2014), Abstract
- Cyclin-dependent kinase 2 phosphorylates s/t-p sites in the hepadnavirus core protein C-terminal domain and is incorporated into viral capsids: Ludgate, L., Ning, X., et al.; J. Virol. 86, 12237 (2012), Abstract
- Mps1 promotes rapid centromere accumulation of Aurora B: van der Waal, M. S., Saurin, A. T., et al.; EMBO Rep. 13, 847 (2012), Abstract
- Cyclin-dependent kinase 1 inhibitor RO-3306 enhances p53-mediated Bax activation and mitochondrial apoptosis in AML: K. Kojima, et al.; Cancer Sci. 100, 1128 (2009), Abstract
- Cell cycle synchronization at the G2/M phase border by reversible inhibition of CDK1: L.T. Vassilev; Cell Cycle 5, 2555 (2006), Abstract — Full Text
- Selective small-molecule inhibitor reveals critical mitotic functions of human CDK1: L.T. Vassilev, et al.; PNAS 103, 10660 (2006), Abstract — Full Text
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