For research use only. Not for therapeutic Use.
CCT251921（Cat No.:I005900）is a selective and potent inhibitor of the WNT signaling pathway, primarily targeting the enzyme TNKS2 (Tankyrase 2). This compound disrupts the stabilization of β-catenin, a key protein in the WNT pathway, which is often upregulated in cancers, particularly colorectal cancer. By inhibiting TNKS2, CCT251921 prevents the proliferation of cancer cells dependent on WNT signaling. It is widely used in cancer research to explore targeted therapies aimed at blocking aberrant WNT pathway activation, making it a promising agent in the development of novel anticancer treatments.
| Catalog Number | I005900 |
| CAS Number | 1607837-31-9 |
| Synonyms | CCT251921; CCT-251921; CCT 251921; CAS#1607837-31-9;8-(2-amino-3-chloro-5-(1-methyl-1H-indazol-5-yl)pyridin-4-yl)-2,8-diazaspiro[4.5]decan-1-one |
| Molecular Formula | C21H23ClN6O |
| Purity | ≥95% |
| Target | CDK19 inhibitor |
| Solubility | Soluble in DMSO, not in water |
| Storage | 0 - 4°C for short term ,or -20 °C for long term |
| IC50 | IC50 data: CDK8:=2.3 nM; CDK19 = 2.6 Nm |
| IUPAC Name | 8-[2-amino-3-chloro-5-(1-methylindazol-5-yl)pyridin-4-yl]-2,8-diazaspiro[4.5]decan-1-one |
| InChI | InChI=1S/C21H23ClN6O/c1-27-16-3-2-13(10-14(16)11-26-27)15-12-25-19(23)17(22)18(15)28-8-5-21(6-9-28)4-7-24-20(21)29/h2-3,10-12H,4-9H2,1H3,(H2,23,25)(H,24,29) |
| InChIKey | VPJXPDLMACOGIZ-UHFFFAOYSA-N |
| SMILES | CN1C2=C(C=C(C=C2)C3=CN=C(C(=C3N4CCC5(CCNC5=O)CC4)Cl)N)C=N1 |
| Reference | </br>Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19. Aurélie Mallinger, Kai Schiemann, Christian Rink, Frank Stieber, Michel Calderini, Simon Crumpler, Mark Stubbs, Olajumoke Adeniji-Popoola, Oliver Poeschke, Michael Busch, Paul Czodrowski, Djordje Musil, Daniel Schwarz, Maria-Jesus Ortiz-Ruiz, Richard Schneider, Ching Thai, Melanie Valenti, Alexis de Haven Brandon, Rosemary Burke, Paul Workman, Trevor Dale, Dirk Wienke, Paul A. Clarke, Christina Esdar, Florence I. Raynaud, Suzanne A. Eccles, Felix Rohdich, and Julian Blagg, Publication Date (Web): January 21, 2016 (Article), DOI: 10.1021/acs.jmedchem.5b01685 |
