GFB-12630
GFB-12630 is a selective CDK5 inhibitor with an IC50 of 3.2 nM. GFB-12630 can be used for research on autosomal dominant polycystic kidney disease.
For research use only. We do not sell to patients.
- CAS No.: 2757673-53-1
- Formula: C25H31FN6O2
- Molecular Weight:466.55
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[1]|
Cdk5/p25 3.2 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
1.2 nM
|
CDK5/p35 target engagement in HEK293 cells assessed as NanoBRET IC50 using K-10 tracer incubated 1 hr.
CDK5/p35 target engagement in HEK293 cells assessed as NanoBRET IC50 using K-10 tracer incubated 1 hr.
|
35143203 |
| HEK-293T | IC50 |
10 μM
|
Antiproliferative activity against human HEK293T cells assessed as inhibition of EdU incorporation incubated 48 hrs by Click-iT EdU high-content imaging with IC50 greater than 10 μM.
Antiproliferative activity against human HEK293T cells assessed as inhibition of EdU incorporation incubated 48 hrs by Click-iT EdU high-content imaging with IC50 greater than 10 μM.
|
35143203 |
In Vitro
GFB-12630 (500 nM) inhibits none of the 54 tested kinases by more than 50%[1].
GFB-12630 (1 h) binds to CDK5/p35 in HEK293 cells with a NanoBRET IC50 of 1.2 nM[1].
GFB-12630 (10 μM; 48 h) does not affect HEK293T cell proliferation (IC50 >10 μM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK293T cells
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Concentration:10 μM
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Incubation Time:48 h (cells); 2 h (EdU)
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Result:Showed <50% inhibition of HEK293T proliferation at 10 μM.
Antiproliferation IC50 was >10 μM.
Parmacokinetics
Chemical Information
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CAS No. 2757673-53-1
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Molecular Weight 466.55
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Formula C25H31FN6O2
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SMILES
C[C@@](C1CCN(C)CC1)(C2=NC3=CC(NC4=CC(N5CCOCC5)=NC=C4F)=NC=C3C=C2)O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)