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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.

Synonym(s):

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

Empirical Formula (Hill Notation):
C15H13F2N7O2S2
CAS Number:
443798-55-8
Molecular Weight:
425.44
UNSPSC Code:
12352200
NACRES:
NA.77

Quality Level

100

Assay

≥95% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

white

solubility

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

shipped in

ambient

storage temp.

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 key

ARIOBGGRZJITQX-UHFFFAOYSA-N

General description

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).

Biochem/physiol Actions

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

Packaging

Packaged under inert gas

Warning

Toxicity: Harmful (C)

Reconstitution

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

Other Notes

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

Legal Information

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

Storage Class Code

11 - Combustible Solids

WGK

WGK 1

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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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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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
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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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