1. Cell Cycle/DNA Damage Neuronal Signaling
  2. Choline Kinase Checkpoint Kinase (Chk)
  3. Chk2-IN-1

Chk2-IN-1 (compound 1) is a potent and selective inhibitor of checkpoint kinase 2 (Chk2), with IC50s of 13.5 nM and 220.4 nM for Chk2 and Chk1, respectively. Chk2-IN-1 can elicit a strong ataxia telangiectasia mutated (ATM)-dependent Chk2-mediated radioprotection effect.

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Chk2-IN-1

Chk2-IN-1 Estructura química

No. CAS : 724708-21-8

Tamaño Precio Stock Cantidad
500 μg Obtener un presupuesto 3 - 4 Weeks 4 - 5 Weeks 5 - 6 Weeks 2 - 3 weeks
1 mg Obtener un presupuesto 3 - 4 Weeks 4 - 5 Weeks 5 - 6 Weeks 2 - 3 weeks
5 mg   Obtener un presupuesto  
10 mg   Obtener un presupuesto  
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Descripciòn

Chk2-IN-1 (compound 1) is a potent and selective inhibitor of checkpoint kinase 2 (Chk2), with IC50s of 13.5 nM and 220.4 nM for Chk2 and Chk1, respectively. Chk2-IN-1 can elicit a strong ataxia telangiectasia mutated (ATM)-dependent Chk2-mediated radioprotection effect[1].

IC50 & Target[1]

Chk2

13.5 nM (IC50)

Chk1

220.4 nM (IC50)

CHKα1

 

Cellular Effect
Cell Line Type Value Description References
CCRF-CEM GI50
1.7 μM
Compound: 4
Growth inhibition of human CCRF-CEM cells up to 48 hrs by trypan blue exclusion assay
Growth inhibition of human CCRF-CEM cells up to 48 hrs by trypan blue exclusion assay
[PMID: 22995819]
Jurkat IC50
3.5 μM
Compound: 4
Inhibition of PMA- and PHA-stimulated IL2 production in human Jurkat T cells incubated for 30 mins prior to PMA- and PHA-stimulation by competitive enzyme immunoassay
Inhibition of PMA- and PHA-stimulated IL2 production in human Jurkat T cells incubated for 30 mins prior to PMA- and PHA-stimulation by competitive enzyme immunoassay
[PMID: 22995819]
Jurkat IC50
3.5 μM
Compound: 64
Antiinflammatory activity in PMA induced human Jurkat cells assessed as inhibition of IL-2 production by EIA assay
Antiinflammatory activity in PMA induced human Jurkat cells assessed as inhibition of IL-2 production by EIA assay
[PMID: 36496202]
Jurkat IC50
3.55 μM
Compound: 2
Inhibition of IL-2 production was determined in Jurkat cells after PMA/PHA activation by Enzyme immunoassay
Inhibition of IL-2 production was determined in Jurkat cells after PMA/PHA activation by Enzyme immunoassay
[PMID: 15214798]
THP-1 IC50
3.5 μM
Compound: 2d
Antiinflammatory activity in human THP-1 cells assessed as inhibition of LPS-stimulated IL2 production
Antiinflammatory activity in human THP-1 cells assessed as inhibition of LPS-stimulated IL2 production
[PMID: 33901899]
THP-1 IC50
8.16 μM
Compound: 2
Inhibition of TNF-alpha production was determined in THP-1cells after LPS activation by Enzyme immunoassay
Inhibition of TNF-alpha production was determined in THP-1cells after LPS activation by Enzyme immunoassay
[PMID: 15214798]
THP-1 IC50
8.2 μM
Compound: 4
Inhibition of LPS-induced TNFalpha production in human THP1 cells incubated for 30 mins prior to LPS-challenge by competitive enzyme immunoassay
Inhibition of LPS-induced TNFalpha production in human THP1 cells incubated for 30 mins prior to LPS-challenge by competitive enzyme immunoassay
[PMID: 22995819]
THP-1 IC50
8.2 μM
Compound: 2d
Antiinflammatory activity in human THP-1 cells assessed as inhibition of LPS-stimulated TNFalpha production
Antiinflammatory activity in human THP-1 cells assessed as inhibition of LPS-stimulated TNFalpha production
[PMID: 33901899]
THP-1 IC50
8.2 μM
Compound: 64
Antiinflammatory activity in LPS induced human THP-1 cells assessed as inhibition of TNF-alpha production by EIA assay
Antiinflammatory activity in LPS induced human THP-1 cells assessed as inhibition of TNF-alpha production by EIA assay
[PMID: 36496202]
Peso molecular

295.30

Fòrmula

C15H13N5O2

No. CAS
SMILES

O=C(C(N1)=C/2C3=C1C=CC=C3)NCCC2=C4N=C(N)NC\4=O

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Please store the product under the recommended conditions in the Certificate of Analysis.

Pureza y Documentación
Referencias
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  • 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:
Chk2-IN-1
Cat. No.:
HY-112477
Cantidad:
MCE Japan Authorized Agent: