Molecular structure of SB 218078, CAS Number: 135897-06-2
SB 218078 (CAS 135897-06-2)
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Alternate Names:
9,10,11,12-Tetrahydro- 9,12-epoxy-1H-diindolo[1,2,3-fg:3',2',1'-kl]pyrrolo[3,4-i][1,6]benzodiazocine-1,3(2H)-dione
Application:
SB 218078 is a potent inhibitor of Type I 5-phosphatase and Chk1
CAS Number:
135897-06-2
Purity:
≥98%
Molecular Weight:
393.4
Molecular Formula:
C24H15N3O3
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
Available in US only.
Available in US only.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
SB 218078 is the phosphorylation product of inositol 1,4,5-trisphosphate (Ins (1,4,5)P3). SB 218078 acts as a potent inhibitor of Type I 5-phosphatase (Ins (1,4,5)P3 5-phosphatase) (IC50 ~150 nM). SB 218078 facilitates Ca2+ influx by sensitising Ins (1,4,5)P3-mediated activation of ICRAC. At higher concentrations, SB 218078 acts as an inhibitor of Ins (1,4,5)P3 receptors. SB 218078 is also an inhibitor of checkpoint kinase 1(Chk1) with an IC50 value of 15 M. SB-218078 is a much weaker inhibitor of Cdc2 p34 (Cdk 1)(IC50 = 250 nM) and PKC (IC50 = 1 µM).
SB 218078 (CAS 135897-06-2) References
- InsP4 facilitates store-operated calcium influx by inhibition of InsP3 5-phosphatase. | Hermosura, MC., et al. 2000. Nature. 408: 735-40. PMID: 11130077
- Structural basis for Chk1 inhibition by UCN-01. | Zhao, B., et al. 2002. J Biol Chem. 277: 46609-15. PMID: 12244092
- G2 checkpoint abrogators as anticancer drugs. | Kawabe, T. 2004. Mol Cancer Ther. 3: 513-9. PMID: 15078995
- Agonist-induced calcium signaling is impaired in fibroblasts overproducing inositol 1,3,4,5-tetrakisphosphate. | Balla, T., et al. 1991. J Biol Chem. 266: 24719-26. PMID: 1662215
- Checkpoint kinase 1-mediated phosphorylation of Cdc25C and bad proteins are involved in antitumor effects of loratadine-induced G2/M phase cell-cycle arrest and apoptosis. | Chen, JS., et al. 2006. Mol Carcinog. 45: 461-78. PMID: 16649252
- Synthetic lethal RNAi screening identifies sensitizing targets for gemcitabine therapy in pancreatic cancer. | Azorsa, DO., et al. 2009. J Transl Med. 7: 43. PMID: 19519883
- Genetic instability and mammary tumor formation in mice carrying mammary-specific disruption of Chk1 and p53. | Fishler, T., et al. 2010. Oncogene. 29: 4007-17. PMID: 20473325
- A screen of kinase inhibitors reveals a potential role of Chk1 in regulating Hydra head regeneration and maintenance. | Lee, Y., et al. 2021. Int J Dev Biol. 65: 523-536. PMID: 34549798
- Hydrogen sulfide ameliorates lipopolysaccharide-induced anxiety-like behavior by inhibiting checkpoint kinase 1 activation in the hippocampus of mice. | Shentu, Y., et al. 2024. Exp Neurol. 371: 114586. PMID: 37898396
- Bridging the GAP in inositol 1,3,4,5-tetrakisphosphate signalling. | Cullen, PJ. 1998. Biochim Biophys Acta. 1436: 35-47. PMID: 9838034
Inhibitor of:
4921501E09Rik, CD300LD, Cdc2, Chk1, GRK 6, IP3R, MYT1L, Olfr71, Olfr710, PKC, Rad17, Ser/Thr Protein Kinase, Sval2, Sval3, SVEP1, TopBP1, Troponin I-FS, Twinkle, and Type I 5-phosphatase.Activator of:
BUBR1, CCDC74A, cyclin E, and TIGD1.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
SB 218078, 1 mg | sc-203692 | 1 mg | $133.00 | |||
| US: Only available in the US | ||||||