1. Cell Cycle/DNA Damage
  2. Checkpoint Kinase (Chk)
  3. VRX0466617

VRX0466617 is a selective and ATP-competitive Chk2 inhibitor with an IC50 of 120 nM and a Ki of 11 nM. VRX0466617 does not inhibit the related Chk1 activity. VRX0466617 can be used in the study of cancer.

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VRX0466617

VRX0466617 Estructura química

No. CAS : 926906-64-1

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Descripciòn

VRX0466617 is a selective and ATP-competitive Chk2 inhibitor with an IC50 of 120 nM and a Ki of 11 nM. VRX0466617 does not inhibit the related Chk1 activity. VRX0466617 can be used in the study of cancer.

IC50 & Target[1]

Chk1

120 nM (IC50)

Chk1

11 nM (Ki)

In Vitro

VRX0466617 (10-30 μM) inhibits both the autophosphorylation of Chk2 and the phosphorylation of Cdc25C substrate in vitro kinase reactions[1].
VRX0466617 (0.05-10 μM; 30-180 min) inhibits the phosphorylation of Chk2 Ser19 and Ser33-35, but not of Chk2 Thr68 in ionizing radiation (IR)-induced cells[1].
VRX0466617 induces the phosphorylation of Chk2 Thr68 in the absence of DNA damage[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: LCL-N cells treated with ionizing radiation (IR).
Concentration: 0.05 μM, 0.5 μM, 5 μM, 10 μM
Incubation Time: 30 min, 180 min
Result: Markedly inhibited the phosphorylation of Ser33-35 and, to a less extent, of Ser19, but not of Thr68.
Peso molecular

462.36

Fòrmula

C19H20BrN5O2S

No. CAS
Appearance

Solid

Color

White to off-white

SMILES

OCC(C)NC(C(C(NS1)=O)=C1NC2=CC=C(NC3=CC=C(Br)C=C3)C=C2)=N

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Pureza y Documentación
Referencias
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Inquiry Information

Nombre del producto:
VRX0466617
Cat. No.:
HY-106009
Cantidad:
MCE Japan Authorized Agent: