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Merck

238803

Cdk2 Inhibitor III

The Cdk2 Inhibitor III, also referenced under CAS 199986-75-9, controls the biological activity of Cdk2. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

Synonyme(s) :

Cdk2 Inhibitor III, 2( bis-(Hydroxyethyl)amino)-6-(4-methoxybenzylamino)-9-isopropyl-purine, CVT-313, 2(bis-(Hydroxyethyl)amino)-6-(4-methoxybenzylamino)-9-isopropyl-purine, CVT-313

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A propos de cet article

Formule empirique (notation de Hill) :
C20H28N6O3
Numéro CAS:
199986-75-9
Poids moléculaire :
400.47
MDL number:
MFCD06411412
UNSPSC Code:
12352200
NACRES:
NA.77

Principaux documents

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Nom du produit

Cdk2 Inhibitor III, The Cdk2 Inhibitor III, also referenced under CAS 199986-75-9, controls the biological activity of Cdk2. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

SMILES string

[n]1(c2nc(nc(c2nc1)NCc3ccc(cc3)OC)N(CCO)CCO)C(C)C

InChI

1S/C20H28N6O3/c1-14(2)26-13-22-17-18(21-12-15-4-6-16(29-3)7-5-15)23-20(24-19(17)26)25(8-10-27)9-11-28/h4-7,13-14,27-28H,8-12H2,1-3H3,(H,21,23,24)

InChI key

NQVIIUBWMBHLOZ-UHFFFAOYSA-N

assay

≥98% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

white

solubility

DMSO: 10 mg/mL

shipped in

ambient

storage temp.

2-8°C

Quality Level

100

Catégories apparentées

Biochem/physiol Actions

Cell permeable: yes
Primary Target
Cdk2/A, Cdk2/E
Product competes with ATP.
Reversible: yes
Target IC50: 0.5 µM for Cdk2/A and Cdk2/E; 4.2 µM for Cdk1/B; 215 µM for Cdk4/D1

Disclaimer

Toxicity: Carcinogenic / Teratogenic (D)

General description

A cell-permeable purine analog that acts as a potent, selective, reversible, and ATP-competitive inhibitor of Cdk2 (IC50 = 0.5 µM for Cdk2/A and Cdk2/E; 4.2 µM for Cdk1/B; 215 µM for Cdk4/D1). Inhibits other kinases only at much higher concentrations (IC50 >1.25 mM for MAPK, PKA, and PKC). Shown to induce tumor cells growth arrest (IC50 = ~1.25-20 µM) in vitro and prevent neointima formation in vivo.

Legal Information

Sold under license of U.S. Patents 6,617,331 and 6,803,371.
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Bhattacharjee, R.N., et al. 2001. Mol. Cell. Biol.21, 5417.
Brooks, E.E., et al. 1997. J. Biol. Chem.272, 29207.

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Classe de stockage

11 - Combustible Solids

wgk

WGK 1

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Haitao Liu et al.
Journal of virology, 95(12) (2021-04-02)
Hepatitis B virus (HBV) capsid or core protein (HBc) consists of an N-terminal domain (NTD) and a C-terminal domain (CTD) connected by a short linker peptide. Dynamic phosphorylation and dephosphorylation of HBc regulate its multiple functions in capsid assembly and
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
Tom Kaufman et al.
Nature communications, 13(1), 2725-2725 (2022-05-19)
While multiplexing samples using DNA barcoding revolutionized the pace of biomedical discovery, multiplexing of live imaging-based applications has been limited by the number of fluorescent proteins that can be deconvoluted using common microscopy equipment. To address this limitation, we develop
Arnav Moudgil et al.
Cell, 182(4), 992-1008 (2020-07-28)
Cellular heterogeneity confounds in situ assays of transcription factor (TF) binding. Single-cell RNA sequencing (scRNA-seq) deconvolves cell types from gene expression, but no technology links cell identity to TF binding sites (TFBS) in those cell types. We present self-reporting transposons

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