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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- CAS No.: 724708-21-8
- 화학식: C15H13N5O2
- 분자량:295.30
-
보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
|
Chk2 13.5 nM (IC50) |
Chk1 220.4 nM (IC50) |
CHKα1 |
|
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] |
Chemical Information
-
CAS No. 724708-21-8
-
분자량 295.30
-
화학식 C15H13N5O2
-
SMILES
O=C(C(N1)=C/2C3=C1C=CC=C3)NCCC2=C4N=C(N)NC\4=O
-
Synonyms
Hymenialdisine analogue-1
-
선적
Room temperature in continental US; may vary elsewhere.
-
보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)