GSK 2830371
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- CAS号:
- 1404456-53-6
- 英文名:
- GSK 2830371
- 英文别名:
- GSK 2830371;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-(cycloprpylamino)-2-oxoethyl]-2-thiophenecarboxamide;5-[[(5-Chloro-2-methyl-3-pyridinyl)amino]methyl]-N-[(1S)-1-(cyclopentylmethyl)-2-(cyclopropylamino)-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 (S)-5-(((5-chloro-2-methylpyridin-3-yl)amino)methyl)-N-(3-cyclopentyl-1-(cyclopropylamino) -1-oxopropan-2-yl)thiophene-2-carboxamide
- 中文名:
- GSK 2830371
- 中文别名:
- 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
- CBNumber:
- CB72682001
- 分子式:
- C23H29ClN4O2S
- 分子量:
- 461.02
- MOL File:
- 1404456-53-6.mol
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GSK 2830371化学性质
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沸点:
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704.1±60.0 °C(Predicted)
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密度:
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1.30±0.1 g/cm3(Predicted)
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储存条件:
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2-8°C
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溶解度:
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DMSO: soluble20mg/mL, clear
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酸度系数(pKa):
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13.29±0.46(Predicted)
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形态:
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powder
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颜色:
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white to beige
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GSK 2830371性质、用途与生产工艺
GSK2830371是一种口服具有活性的，变构的Wip1 phosphatase抑制剂，IC50为6 nM。
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, 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.
GSK2830371是一种口服具有活性的，变构的Wip1 phosphatase抑制剂，IC50为6 nM。
| Target | Value |
Wip1 phosphatase
(Cell-free assay)
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6 nM
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在PPM1D扩增的MCF7乳腺癌细胞中，GSK2830371增加多重Wip1底物，包括p53 (S15)，Chk2 (T68)，H2AX (S139) 和 ATM (S1981)的磷酸化。GSK2830371在一部分携带野生型TP53等位基因的淋巴样细胞系中表现出选择性抗增殖活性。此外，doxorubicin 和 GSK2830371共处理在DOHH2和MX-1肿瘤细胞中表现出协同的抗增殖作用。
在体内，GSK2830371增加Chk2 (T68) 和 p53 (S15)的磷酸化，并减少DOHH2肿瘤中Wip1蛋白质浓度。GSK2830371 (150 mg/kg p.o.)通过抑制Wip1也会抑制DOHH2肿瘤异种移植物的生长。
GSK 2830371
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/01/25 | HY-15832 | GSK 2830371 | | 1 mg | 295元 |
| 2024/01/25 | HY-15832 | GSK 2830371
GSK 2830371 | 1404456-53-6 | 5mg | 650元 |
1404456-53-6, GSK 2830371 相关搜索:
- Inhibitors
- 合成有机化合物配体
- 小分子抑制剂，天然产物
- C23H29ClN4O2S
- 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
- 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