SML1048

GSK2830371

≥98% (HPLC)

• Synonim(y): (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-(cyclopropylamino)-2-oxoethyl]-2-thiophenecarboxamide
• Wzór empiryczny (zapis Hilla): C₂₃H₂₉ClN₄O₂S
• Numer CAS: 1404456-53-6
• Masa cząsteczkowa: 461.02
• UNSPSC Code: 12352200
• NACRES: NA.77
• Assay: ≥98% (HPLC)
• Form: powder

Właściwości

• Quality Segment: 100
• assay: ≥98% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 20 mg/mL, clear
• storage temp.: 2-8°C
• SMILES string: [s]1c(ccc1C(=O)N[C@@H](CC4CCCC4)C(=O)NC3CC3)CNc2c(ncc(c2)Cl)C
• InChI: 1S/C23H29ClN4O2S/c1-14-19(11-16(24)12-25-14)26-13-18-8-9-21(31-18)23(30)28-20(10-15-4-2-3-5-15)22(29)27-17-6-7-17/h8-9,11-12,15,17,20,26H,2-7,10,13H2,1H3,(H,27,29)(H,28,30)/t20-/m0/s1
• InChI key: IVDUVEGCMXCMSO-FQEVSTJZSA-N

Opis

Biochem/physiol Actions

GSK2830371 is an orally active allosteric inhibitor of wild-type p53-induced phosphatase (Wip1).

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.

GSK2830371 prevents the development of neuroblastoma by stimulating cell death mediated by Chk2 (checkpoint kinase 2)/p53. In neuroblastoma (NB) cell lines, GSK2830371 increased the cytotoxicity stimulated by doxorubicin- (Dox) and etoposide- (VP-16). It also blocks the capability of a subset of NB cells in multiplication and colony formation.

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Informacja o środkach bezpieczeństwa

• Klasa składowania: 11 - Combustible Solids
• Co się dzieje?: WGK 3
• Temperatura zapłonu (°F): Not applicable
• Temperatura zapłonu (°C): Not applicable