[CAS NO. 1404456-53-6] GSK2830371
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PRODUCTS SPECIFICATIONS [1404456-53-6]
Store
Catalog
SLK-S7573
Brand
Selleck
CAS
1404456-53-6
DESCRIPTION [1404456-53-6]
Overview
| MDL | MFCD28009442 |
|---|---|
| Molecular Weight | 461.02 |
| Molecular Formula | C23H29ClN4O2S |
| SMILES | ClC1=CN=C(C)C(NCC2=CC=C(C(N[C@@H](CC3CCCC3)C(NC4CC4)=O)=O)S2)=C1 |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1691 mL | 10.8455 mL | 21.6910 mL |
| 5 mM | 0.4338 mL | 2.1691 mL | 4.3382 mL |
| 10 mM | 0.2169 mL | 1.0846 mL | 2.1691 mL |
| 50 mM | 0.0434 mL | 0.2169 mL | 0.4338 mL |
Description
GSK2830371 is an orally active, allosteric inhibitor with of 6 nM.
Targets
| Wip1 phosphatase [1] (Cell-free assay) |
| 6 nM |
In vitro
In the PPM1D-amplified MCF7 breast carcinoma cells, GSK2830371 increases the phosphorylation of multiple Wip1 substrates, including p53 (S15), Chk2 (T68), H2AX (S139) and ATM (S1981). GSK2830371 shows selective antiproliferative activity in a subset of lymphoid cell lines, all of which carry a wild-type TP53 allele. Furthermore, co-treatment of doxorubicin and GSK2830371 results in a synergistic antiproliferative effect in DOHH2 and MX-1 tumor cells.
In vivo
In vivo, GSK2830371 increases phosphorylation of Chk2 (T68) and p53 (S15) and decreases Wip1 protein concentrations in DOHH2 tumors. GSK2830371 (150 mg/kg p.o.) also inhibits the growth of DOHH2 tumor xenografts via inhibition of Wip1.
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