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Key Documents

217714

Sigma-Aldrich

5-氨基-3-((4 -(氨基磺酰基)苯基)氨基)-N-(2,6-二氟苯基)-1H-1,2,4-三唑-1-硫代乙酰胺

The Cdk1/2 Inhibitor III, also referenced under CAS 443798-55-8, controls the biological activity of Cdk1/2. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

同義詞:

5-氨基-3-((4 -(氨基磺酰基)苯基)氨基)-N-(2,6-二氟苯基)-1H-1,2,4-三唑-1-硫代乙酰胺, 5-氨基-3-((4-(磺酰胺)苯基)氨基)-N-(2,6-二氟苯基)-1H-1,2,4-三唑-1-硫代酰胺

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About This Item

經驗公式(希爾表示法):
C15H13F2N7O2S2
CAS號碼:
分子量::
425.44
分類程式碼代碼:
12352200
NACRES:
NA.77

品質等級

化驗

≥95% (HPLC)

形狀

solid

製造商/商標名

Calbiochem®

儲存條件

OK to freeze
protect from light

顏色

white

溶解度

DMSO: 10 mg/mL
THF: soluble
acetone: soluble

運輸包裝

ambient

儲存溫度

2-8°C

InChI

1S/C15H13F2N7O2S2/c16-10-2-1-3-11(17)12(10)21-15(27)24-13(18)22-14(23-24)20-8-4-6-9(7-5-8)28(19,25)26/h1-7H,(H,21,27)(H2,19,25,26)(H3,18,20,22,23)

InChI 密鑰

ARIOBGGRZJITQX-UHFFFAOYSA-N

一般說明

一种可渗透细胞的三唑并二胺化合物,在各种人类癌细胞中均具有抗增殖特性(HCT-116,HeLa和A375细胞的IC50分别为20 nM,35 nM和92 nM)。作为Cdk1/细胞周期蛋白B和Cdk2/细胞周期蛋白A(IC50分别为600 pM和500 pM)的高效,可逆,ATP竞争性抑制剂,对VEGF-R2(IC50=32 nM),GSK-3β(IC50=140 nM)和一组其他八种激酶(IC50 ≥ 1 µM)具有选择性。

生化/生理作用

主要靶标
Cdk1/细胞周期蛋白B,Cdk2/细胞周期蛋白A
产物与ATP竞争。
可逆性:是
细胞可渗透性:是
靶标IC50:对于HCT-116,HeLa和A375细胞的抗增殖特性,分别为20 nM,35 nM和92 nM;针对Cdk1/细胞周期蛋白B和Cdk2/细胞周期蛋白A,分别为600 pM和500 pM

包裝

用惰性气体包装

警告

毒性:有害(C)

重構

复溶后,等分并冷冻保存(-20°C)。储备液在-20°C条件下可稳定保存6个月。

其他說明

Lin, R., et al. 2005.J.Med. Chem.48, 4208.

法律資訊

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 1

閃點(°F)

Not applicable

閃點(°C)

Not applicable


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Cell differentiation involves profound changes in global gene expression that often has to occur in coordination with cell cycle exit. Because cyclin-dependent kinase inhibitor p27 reportedly regulates proliferation of neural progenitor cells in the subependymal neurogenic niche of the adult mouse
Sungsoo Kim et al.
Scientific reports, 12(1), 16810-16810 (2022-10-08)
External signaling controls cell-cycle entry until cells irreversibly commit to the cell cycle to ensure faithful DNA replication. This process is tightly regulated by cyclin-dependent kinases (CDKs) and the retinoblastoma protein (Rb). Here, using live-cell sensors for CDK4/6 and CDK2
Yilin Fan et al.
Cell reports, 36(4), 109436-109436 (2021-07-29)
Contact inhibition of cell proliferation regulates tissue size and prevents uncontrolled cell expansion. When cell density increases, contact inhibition can force proliferating cells into quiescence. Here we show that the variable memory of local cell density experienced by a mother
Jenny F Nathans et al.
Science advances, 7(3) (2021-02-02)
The G1-S checkpoint is thought to prevent cells with damaged DNA from entering S phase and replicating their DNA and efficiently arrests cells at the G1-S transition. Here, using time-lapse imaging and single-cell tracking, we instead find that DNA damage

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