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217714

Sigma-Aldrich

Cdk1/2 Inhibitor III

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.

Sinonimo/i:

Cdk1/2 Inhibitor III, 5-Amino-3-((4-(aminosulfonyl)phenyl)amino)-N-(2,6-difluorophenyl)-1H-1,2,4-triazole-1-carbothioamide

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About This Item

Formula empirica (notazione di Hill):
C15H13F2N7O2S2
Numero CAS:
Peso molecolare:
425.44
Codice UNSPSC:
12352200
NACRES:
NA.77

Livello qualitativo

Saggio

≥95% (HPLC)

Forma fisica

solid

Produttore/marchio commerciale

Calbiochem®

Condizioni di stoccaggio

OK to freeze
protect from light

Colore

white

Solubilità

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

Condizioni di spedizione

ambient

Temperatura di conservazione

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)
ARIOBGGRZJITQX-UHFFFAOYSA-N

Descrizione generale

A cell-permeable triazolo-diamine compound that displays anti-proliferative properties in various human cancer cells (IC50 = 20 nM, 35 nM and 92 nM in HCT-116, HeLa, and A375 cells, respectively). Acts as a highly potent, reversible, ATP-competitive inhibitor of Cdk1/cyclin B and Cdk2/cyclin A (IC50 = 600 pM and 500 pM, respectively) with selectivity over VEGF-R2 (IC50 = 32 nM), GSK-3β (IC50 = 140 nM), and a panel of eight other kinases (IC50 ≥ 1 µM).

Azioni biochim/fisiol

Cell permeable: yes
Primary Target
Cdk1/cyclin B, Cdk2/cyclin A
Product competes with ATP.
Reversible: yes
Target IC50: 20 nM, 35 nM and 92 nM for anti-proliferative properties in HCT-116, HeLa, and A375 cells, respectively; 600 pM and 500 pM, against Cdk1/cyclin B and Cdk2/cyclin A, respectively

Confezionamento

Packaged under inert gas

Attenzione

Toxicity: Harmful (C)

Ricostituzione

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Altre note

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

Note legali

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

Codice della classe di stoccaggio

11 - Combustible Solids

Classe di pericolosità dell'acqua (WGK)

WGK 1

Punto d’infiammabilità (°F)

Not applicable

Punto d’infiammabilità (°C)

Not applicable


Certificati d'analisi (COA)

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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
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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
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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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