GSK 2830371
GSK 2830371 Basic information
- Product Name:
- GSK 2830371
- Synonyms:
-
- 5-[[(5-Chloro-2-methyl-3-pyridinyl)amino]methyl]-N-[(1S)-1-(cyclopentylmethyl)-2-(cycloprpylamino)-2-oxoethyl]-2-thiophenecarboxamide
- GSK 2830371
- 5-[[(5-Chloro-2-methyl-3-pyridinyl)amino]methyl]-N-[(1S)-1-(cyclopentylmethyl)-2-(cyclopropylamino)-2-oxoethyl]-2-thiophenecarboxamide
- (S)-5-((5-chloro-2-methylpyridin-3-ylamino)methyl)-N-(3-cyclopentyl-1-(cyclopropylamino)-1-oxopropan-2-yl)thiophene-2-carboxamide
- 2-Thiophenecarboxamide, 5-[[(5-chloro-2-methyl-3-pyridinyl)amino]methyl]-N-[(1S)-1-(cyclopentylmethyl)-2-(cyclopropylamino)-2-oxoethyl]-
- GSK 2830371 USP/EP/BP
- GSK 2830371 (S)-5-(((5-chloro-2-methylpyridin-3-yl)amino)methyl)-N-(3-cyclopentyl-1-(cyclopropylamino) -1-oxopropan-2-yl)thiophene-2-carboxamide
- GSK 2830371, 10 mM in DMSO
- CAS:
- 1404456-53-6
- MF:
- C23H29ClN4O2S
- MW:
- 461.02
- Product Categories:
-
- Inhibitors
- Mol File:
- 1404456-53-6.mol
GSK 2830371 Chemical Properties
- Boiling point:
- 704.1±60.0 °C(Predicted)
- Density
- 1.30±0.1 g/cm3(Predicted)
- storage temp.
- 2-8°C
- solubility
- DMSO: soluble20mg/mL, clear
- pka
- 13.29±0.46(Predicted)
- form
- powder
- color
- white to beige
GSK 2830371 Usage And Synthesis
Uses
GSK 2830371 is used in biological studies as allosteric Wip1(wild-type p54-induced phosphatase) inhibition through flap-subdomain interaction.
Biochem/physiol Actions
GSK2830371 is an orally active allosteric inhibitor of wild-type p53-induced phosphatase (Wip1, also known as PPM1D/ PP2Cδ), an oncogenic type 2C serine/threonine phosphatase that negatively regulates key proteins in the DNA damage–response pathway. GSK2830371 is selective for Wip1 with an IC50 of 6 nM against Wip1 compared to >10 μM IC50 for PPM1A & PPM1K, and >30 μM IC50 for 22 other phosphatases tested. GSK2830371 is believed to interact with the flap subdomain located near the Wip1 catalytic site, a feature that distinguishes Wip1 from other members of the protein phosphatase 2C (PP2C) family. GSK2830371 increased phosphorylation of Wip1 substrates and caused growth inhibition in both hematopoietic tumor cell lines and Wip1-amplified breast tumor cells harboring wild-type TP53.
in vivo
In a pharmacodynamic assay, orally administered GSK 2830371 increases phosphorylation of Chk2 (T68) and p53 (S15) and decreased Wip1protein concentrations in DOHH2 tumors. Following 14 d of oral dosing at 150 mg per kg body weight, BID (twice daily) and TID (thrice daily), GSK 2830371 inhibits the growth of DOHH2 tumor xenografts by 41% and 68%, respectively. Comparable tumor growth inhibition is observed in mice treated BID with either 75 or 150 mg per kg body weight. Greater tumor growth inhibition with the TID schedule is consistent with a short half-life of GSK 2830371 in mice and suggests that sustained inhibition of Wip1 may be required for maximal antitumor effect[1].
storage
Store at -20°C
GSK 2830371Supplier
- Tel
- sales@boylechem.com
- Tel
- 021-58950125
- info@chemexpress.com
- Tel
- 021-58955995
- sales@medchemexpress.cn
- Tel
- 025-846993838003-8003 18013301590
- njduly@126.com
- Tel
- 021-021-33632979 15002134094
- marketing@targetmol.com