NSC 109555 ditosylate - CAS 66748-43-4
Category: Inhibitor
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Molecular Formula:
C19H24N10O.2C7H8O3S
Molecular Weight:
752.86
COA:
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Targets:
Checkpoint Kinase (Chk)
Description:
NSC-109555 Ditosylate is an ATP-competitive Chk2 inhibitor with IC50 value of 0.2 μM. It acts by inhibiting histone H1 phosphorylation and attenuating mitochondrial ATP synthesis. It is an antileukemic agent.
Purity:
≥98% by HPLC
Synonyms:
NSC-109555 Ditosylate; NSC 109555 Ditosylate; NSC109555 Ditosylate; 4,4'-diacetyldiphenylurea bis(guanylhydrazone) ditosylate
MSDS:
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InChIKey:
DIQGNVANOSOABS-UHFFFAOYSA-N
InChI:
InChI=1S/C19H24N10O.2C7H8O3S/c1-11(26-28-17(20)21)13-3-7-15(8-4-13)24-19(30)25-16-9-5-14(6-10-16)12(2)27-29-18(22)23;2*1-6-2-4-7(5-3-6)11(8,9)10/h3-10H,1-2H3,(H4,20,21,28)(H4,22,23,29)(H2,24,25,30);2*2-5H,1H3,(H,8,9,10)
Canonical SMILES:
CC1=CC=C(C=C1)S(=O)(=O)O.CC1=CC=C(C=C1)S(=O)(=O)O.CC(=NN=C(N)N)C1=CC=C(C=C1)NC(=O)NC2=CC=C(C=C2)C(=NN=C(N)N)C
1.Oroxylin A reverses P-glycoprotein-mediated multidrug resistance of MCF7/ADR cells by G2/M arrest.
Zhu L;Zhao L;Wang H;Wang Y;Pan D;Yao J;Li Z;Wu G;Guo Q Toxicol Lett. 2013 May 23;219(2):107-15. doi: 10.1016/j.toxlet.2013.01.019. Epub 2013 Mar 5.
Oroxylin A is a naturally occurring monoflavonoid isolated from the root of Scutellaria baicalensis Georgi, which has been used in traditional Chinese medicine for its anti-tumor, anti-inflammatory and anti-bacterial properties. The purpose of this study is to investigate the reversal effect and the fundamental mechanisms of oroxylin A in MCF7/ADR cells. Data indicated that oroxylin A showed strong reversal potency in MCF7/ADR cells and the reversal fold (RF) reached 4.68. After treatment with oroxylin A, MCF7/ADR cells displayed reduced functional activity and expression of MDR1 at both the protein and mRNA levels. Meanwhile, oroxylin A induced cells G2/M arrest in a concentration-dependent manner by increasing the expression of p-Chk2 (Thr68). Moreover, western blot and EMSA assays were used to reveal the inhibition of NF-κB in nucleus and the suppression of NF-κB binding activity by oroxylin A. NSC 109555 ditosylate-Chk2 inhibitor partly dismissed G2/M arrest induced by oroxylin A, reversed the increased trend of p-Chk2 and p-P53 (Ser20), inhibited the decreasing effect of oroxylin A on the expression of P-gp and decreased the reversal fold of 90 μM oroxylin A from 4.68 fold to 1.
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CAS 66748-43-4 NSC 109555 ditosylate

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