SB 218078 CAS: 135897-06-2
MF: C24H15N3O3
MW: 393.4
A potent inhibitor of Type I 5-phosphatase and Chk1.

SB 218078 (CAS 135897-06-2)

SB 218078 | CAS 135897-06-2 is rated 5.0 out of 5 by 1.
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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.
* Refer to Certificate of Analysis for lot specific data (including water content).

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 IP3R (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 (Cdk 1)(IC50 = 250 nM) and PKC (IC50 = 1μM).


References

1. Balla, T., et al. 1991. J. Biol. Chem. 266: 24719-24726. PMID: 1662215
2. Cullen, P.J. 1998. Biochim. Biophys. Acta. 1436: 35-47. PMID: 9838034
3. Hermosura, M.C., et al. 2000. Nature. 408: 735-740. PMID: 11130077

Physical State :
Solid
Solubility :
Soluble in DMSO (100 mM), and water.
Storage :
Store at -20° C
Melting Point :
314.67° C (Predicted)
Boiling Point :
718.51° C (Predicted)
Density :
1.81 g/cm3 (Predicted)
Refractive Index :
n20D 1.97 (Predicted)
IC50 :
CDK2: IC50 = 5.6 nM; CDK4: IC50 = 16 nM; CDK1: IC50 = 23 nM; Cdc2: IC50 = 250 nM; PKC: IC50 = 1 µM; Chk1: IC50 = 15
Ki Data :
Chk1: Ki= 15 nM
pK Values :
pKa: 9.75 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
Available in US only.
PubChem CID :
SMILES :
C1CC2N3C4=CC=CC=C4C5=C6C(=C7C8=CC=CC=C8N(C1O2)C7=C53)C(=O)NC6=O

Download SDS (MSDS)

Certificate of Analysis

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Good morning. Are you sure that SB 218078 is the phosphorylation product of inositol 1,4,5-trisphosphate (Ins (1,4,5)P3)?. Are you sure that the IC50 value for Chk1 inhibition is 15 M?

Asked by: Giul
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Rated 5 out of 5 by from Akasaka T; et al Akasaka T; et al. (PubMed ID:25310623) determined that SB 218078 in combination of 5-FU does not stimulate apoptosis in chemoresistant cancer cells. -SCBT Publication Review
Date published: 2015-03-30
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