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)

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SB 218078 is rated 5.0 out of 5 by 1.
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备用名: 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
应用; SB 218078 is a potent inhibitor of Type I 5-phosphatase and Chk1
CAS号码: 135897-06-2
纯度: ≥98%
分子量: 393.4
分子式: C24H15N3O3
仅供科研使用。不可用于诊断或治疗。
* 参考分析证明 大量特定数据 (包括水 含量).

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).


参考文献

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

物理状态 :
Solid
溶解度 :
Soluble in DMSO (100 mM), and water.
保存 :
Store at -20° C
熔点 :
314.67° C (Predicted)
沸点 :
718.51° C (Predicted)
密度 :
1.81 g/cm3 (Predicted)
折射率 :
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 数据 :
Chk1: Ki= 15 nM
pK值 :
pKa: 9.75 (Predicted)
仅供科研使用。不可用于诊断或治疗。
PubChem CID :
SMILES :
C1CC2N3C4=CC=CC=C4C5=C6C(=C7C8=CC=CC=C8N(C1O2)C7=C53)C(=O)NC6=O

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