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GSK 2830371

GSK 2830371 Structure
GSK 2830371
  • CAS No.1404456-53-6
  • Chemical Name:GSK 2830371
  • CBNumber:CB72682001
  • Molecular Formula:C23H29ClN4O2S
  • Formula Weight:461.02
  • MOL File:1404456-53-6.mol
GSK 2830371 Property
  • 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
  • UNSPSC Code 12352200
  • NACRES NA.77
Safety
  • WGK Germany  :3
Hazard and Precautionary Statements (GHS)
  • Symbol(GHS)
  • Signal word
  • Hazard statements
  • Precautionary statements
GSK 2830371 Price More Price(2)
  • Brand: Sigma-Aldrich(India)
  • Product number: SML1048
  • Product name : GSK2830371
  • Purity: ≥98% (HPLC)
  • Packaging: 5MG
  • Price: ₹11528.63
  • Updated: 2022/06/14
  • Buy: Buy
  • Brand: Sigma-Aldrich(India)
  • Product number: SML1048
  • Product name : GSK2830371
  • Purity: ≥98% (HPLC)
  • Packaging: 25MG
  • Price: ₹46515.03
  • Updated: 2022/06/14
  • Buy: Buy

GSK 2830371 Chemical Properties,Usage,Production

  • 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 2830371 Preparation Products And Raw materials
Raw materials
Preparation Products
GSK 2830371 Suppliers
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GSK 2830371 Spectrum
1404456-53-6, GSK 2830371Related Search:
  • Inhibitors
  • 化学试剂
  • 抑制剂
  • 合成有机化合物配体
  • 小分子抑制剂，天然产物
  • C23H29ClN4O2S
  • 化合物GSK2830371,10 MM DMSO 溶液
  • GSK 2830371,WIP1磷酸酶的变构抑制剂
  • (S)-5-(((5-氯-2-甲基吡啶-3-基)氨基)甲基)-N-(3-环戊基-1-(环丙基氨基)-1-氧代丙烷-2-基)噻吩-2-甲酰胺
  • (S)-5-((((5-氯-2-甲基吡啶-3-基)氨基)甲基)-N-(3-环戊基-1-(环丙基氨基)-1-氧丙烷-2-基)噻吩-2 -羧酰胺
  • 1404456-53-6
  • PPM1D Phosphatase Inhibitor II, GSK2830371
  • GSK 2830371, 10 mM in DMSO
  • GSK 2830371 (S)-5-(((5-chloro-2-methylpyridin-3-yl)amino)methyl)-N-(3-cyclopentyl-1-(cyclopropylamino) -1-oxopropan-2-yl)thiophene-2-carboxamide
  • 5-[[(5-Chloro-2-methyl-3-pyridinyl)amino]methyl]-N-[(1S)-1-(cyclopentylmethyl)-2-(cycloprpylamino)-2-oxoethyl]-2-thiophenecarboxamide
  • 2-Thiophenecarboxamide, 5-[[(5-chloro-2-methyl-3-pyridinyl)amino]methyl]-N-[(1S)-1-(cyclopentylmethyl)-2-(cyclopropylamino)-2-oxoethyl]-
  • GSK 2830371 USP/EP/BP
  • (S)-5-((5-chloro-2-methylpyridin-3-ylamino)methyl)-N-(3-cyclopentyl-1-(cyclopropylamino)-1-oxopropan-2-yl)thiophene-2-carboxamide
  • 5-[[(5-Chloro-2-methyl-3-pyridinyl)amino]methyl]-N-[(1S)-1-(cyclopentylmethyl)-2-(cyclopropylamino)-2-oxoethyl]-2-thiophenecarboxamide
  • GSK 2830371

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